Antibiotics

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You’ve most likely taken an antibiotic at least once in your lifetime.

From
treatments for painful strep throat or ear infections as a child, to burning urinary
tract infections or itchy skin infections as an adult, antibiotics are one of the most
highly utilized and important medication classes we have in medicine.

Understanding the vast world of antibiotics and anti-infectives is no easy


task. Anti-infectives are a large class of drugs that cover a broad range of
infections, including fungal, viral, bacterial, and even protozoal infections.
Athletes foot? That’s a common fungal infection. HIV? Antiviral medications are
always needed. Bladder infection? Yes, that may need a common antibiotic. And
head lice? A topical anti-parasitic can alleviate the itching. There is no one type of
antibiotic that cures every infection. Antibioticsspecifically treat infections
caused by bacteria, such as Staph., Strep., or E. coli., and either kill the bacteria
(bactericidal) or keep it from reproducing and growing (bacteriostatic). Antibiotics
do not work against any viral infection.

When To Use Antibiotics


Antibiotics are specific for the type of bacteria being treated and, in general,
cannot be interchanged from one infection to another. When antibiotics are used
correctly, they are usually safe with few side effects.

However, as with most drugs, antibiotics can lead to side effects that may range
from being a nuisance to serious or life-threatening. In infants and the elderly, in
patients with kidney or liver disease, in pregnant or breastfeeding women, and in
many other patient groups antibiotic doses may need to be adjusted based upon
the specific characteristics of the patient, like kidney or liver function, weight, or
age. Drug interactions can also be common with antibiotics. Health care
providers are able to assess each patient individually to determine the correct
antibiotic and dose.

When NOT To Use Antibiotics


Antibiotics are not the correct choice for all infections. For example, most sore
throats, cough and colds, flu or acute sinusitis are viral in origin (not bacterial)
and do not need an antibiotic. These viral infections are “self-limiting”, meaning
that your own immune system will usually kick in and fight the virus off. In fact,
using antibiotics for viral infections can increase the risk for antibiotic resistance,
lower the options for future treatments if an antibiotic is needed, and put a
patient at risk for side effects and extra cost due to unnecessary drug treatment.

Antibiotic resistant bacteria cannot be fully inhibited or killed by an antibiotic,


even though the antibiotic may have worked effectively before the resistance
occurred. Don't share your antibiotic or take medicine that was prescribed for
someone else, and don't save an antibiotic to use the next time you get sick.

To better understand antibiotics, it’s best to break them down into common
infections, common antibiotics, and the top antibiotic classes as searched on
in Drugs.com:

Top 10 List of Common Infections Treated with


Antibiotics:
1. Acne
2. Bronchitis
3. Conjunctivitis (Pink Eye)
4. Otitis Media (Ear Infection)
5. Sexually Transmitted Diseases (STD’s)
6. Skin or Soft Tissue Infection
7. Streptococcal Pharyngitis (Strep Throat)
8. Traveler’s diarrhea
9. Upper Respiratory Tract Infection
10.Urinary Tract Infection (UTI)

Top 10 List of Antibiotic Classes (Types of


Antibiotics):
1. Penicillins
2. Tetracyclines
3. Cephalosporins
4. Quinolones
5. Lincomycins
6. Macrolides
7. Sulfonamides
8. Glycopeptides
9. Aminoglycosides
10.Carbapenems

Most antibiotics fall into their individual antibiotic classes. An antibiotic class is a
grouping of different drugs that have similar chemical and pharmacologic
properties. Their chemical structures may look comparable, and drugs within the
same class may kill the same or related bacteria.

However, it is important not to use an antibiotic for an infection unless your


doctor specifically prescribes it, even if it's in the same class as another drug you
were previously prescribed. Antibiotics are specific for the kind of bacteria they
kill. Plus, you would need a full treatment regimen to effectively cure your
infection, so don't use or give away leftover antibiotics.

1. Penicillins

Another name for this class is the beta-lactam antibiotics, referring to their
structural formula. The penicillin class contains five groups of antibiotics:
aminopenicillins, antipseudomonal penicillins, beta-lactamase inhibitors, natural
penicillins, and the penicillinase resistant penicillins. Common antibiotics in the
penicillin class include:

 penicillin V potassium
 amoxicillin
 amoxicillin/clavulanate (Augmentin)

View penicillin drugs

What are Penicillins?


Penicillins are a type of antibiotic derived from Penicillium fungi. An antibiotic is a
type of medicine that inhibits the growth of, or kills, bacteria.

Penicillin G (also called benzylpenicillin) was discovered by accident in 1928.


Alexander Fleming, a Scottish physician-scientist was growing a type of bacteria
called Staphylococcus Aureus on an uncovered petri dish when it became
contaminated with mold spores. He observed that the areas of bacteria near the
mold were dying. He isolated the substance from the mold that was killing the
bacteria and called it penicillin.

Another naturally occurring penicillin, penicillin V was later isolated from the
same mold. All other penicillins are semi-synthetic (made by modifying the
structure of the original naturally occurring penicillins). Modification extends their
spectrum of activity, allows them to be taken orally, and increases their resistance
against penicillinase, an enzyme produced by some bacteria that inactivates
penicillin.

Penicillins work by preventing the cross linking of amino acid chains in the
bacterial cell wall. This does not affect pre-existing bacteria, but newly produced
bacterial cells have weak cell walls that easily rupture.

What are penicillins used for?


Penicillins may be used to treat a wide range of infections caused by susceptible
bacteria, such as:

 Dental abscess
 Ear infections (eg, otitis media)
 Gonorrhea
 Pneumonia
 Respiratory tract infections
 Rheumatic fever
 Scarlet fever
 Skin infections
 Urinary tract infections.

What are the differences between


penicillins?
The natural penicillins (penicillin G and penicillin V) are only active against
gram-positive bacteria (see below for an explanation). Penicillin V is more acid-
resistant than penicillin G, which means it can be taken orally.
Modern semi-synthetic penicillins include ampicillin, carbenicillin (discontinued),
and oxacillin. These can be taken orally, have some degree of resistance to beta
lactamase, and are effective against some gram-negative bacteria. Most bacteria
can be classified as gram-positive or gram-negative based on differences in their
cell wall structure, which can be distinguished under a microscope using a type of
dye. One of the most important differences between these two types of bacteria
is that gram-positive bacteria are more susceptible to antibiotics while gram-
negative bacteria are more resistant to antibiotics.

Antipseudomonal penicillins, such as piperacillin and ticarcillin (discontinued) are


penicillins that have additional activity against some hard-to-kill types of gram-
negative bacteria such as Pseudomonas, Enterococcus and Klebsiella. They are
useful for urinary tract infections caused by susceptible bacteria because they
concentrate in the urine.

Some penicillins are combined with a beta-lactamase inhibitor. A beta-lactamase


inhibitor blocks the activity of beta-lactamase enzymes but tends to have little
antibiotic activity on its own. Some penicillins (such as oxacillin, dicloxacillin,
and nafcillin) are naturally resistant to certain beta-lactamases and are called
penicillinase-resistant penicillins. Others, such as amoxicillin, ampicillin,
and piperacillin can have their activity extended by combining them with a beta-
lactamase inhibitor. Clavulanate, sulbactam, and tazobactam are all beta-
lactamase inhibitors.

Common penicillins available in the U.S.


Aminopenicillins

Spectrum of activity:

 Most gram-positive bacteria, some gram-negative bacteria (such as E.


coli and H. influenzae).

Generic name Brand name examples

amoxicillin Amoxil, Moxatag


Generic name Brand name examples

ampicillin Principen

Antipseudomonal penicillins

Spectrum of activity:

 Most gram-positive and gram-negative bacteria


 Antipseudomonal and antiprotozoal activity
 Usually given with a beta lactamase.

Generic name Brand name examples

piperacillin Pipracil

Beta-lactamase inhibitors

Spectrum of activity:

 Effective against most gram-positive and gram-negative bacteria including


those that produce beta-lactamases
(eg, bacteroides sp., enterococcus sp., staphylococcus sp.)

Generic name Brand name examples

amoxicillin/clavulanate Augmentin, Amoclan

ampicillin/sulbactam Unasyn
Generic name Brand name examples

piperacillin/tazobactam Zosyn

Natural penicillins

Spectrum of activity:

 Effective against most gram-positive bacteria and a limited number of


gram-negative bacteria.

Generic name Brand name examples

penicillin g benzathine Bicillin L-A

penicillin v Penicillin VK

Penicillinase-resistant penicillins

Spectrum of activity:

 Effective against most gram-positive and gram-negative bacteria


 Naturally resistant to beta-lactamase.

Generic name Brand name examples

dicloxacillin Dycill

nafcillin Unipen

oxacillin Bactocill
Are penicillins safe?
Penicillins are generally safe, with low toxicity and good efficacy against
susceptible bacteria.

Many people believe that they are allergic to penicillin. However, true penicillin
allergy is rare, and only occurs in 0.01-0.05% of people who take penicillin.
Symptoms may include nausea, vomiting, itchy skin, rash, wheezing, swelling
around the throat, and respiratory collapse.

What are the side effects of penicillins?


Penicillins generally cause few side effects. The most common side effects
reported include abdominal pain, headache, rash, diarrhea, and taste perversion.

Penicillins may cause anaphylaxis in those allergic to penicillin, but the overall
incidence of anaphylaxis is rare (0.01-0.05%).

Rarely, some people may develop a super-infection due to overgrowth of a


naturally occurring bacterium called Clostridium difficile, following use of any
antibiotic, including penicillins. Symptoms may include severe diarrhea.

Uncommonly, an overgrowth of the yeast, Candida albicans, may occur following


penicillin use, resulting in the symptoms of thrush.

Read more

Types of Penicillins
Please refer to the drug classes listed below for further information.

 aminopenicillins
 antipseudomonal penicillins
 beta-lactamase inhibitors
 natural penicillins
 penicillinase resistant penicillins
2. Tetracyclines

Tetracyclines are broad-spectrum against many bacteria and treat conditions


such as acne, urinary tract infections (UTIs), intestinal tract infections, eye
infections, sexually transmitted diseases, periodontitis (gum disease), and other
bacterial infections. The tetracycline class contains well-known drugs such as:

 doxycycline
 tetracycline
 minocycline

View Tetracycline drugs

What are Tetracyclines?


Tetracyclines are a class of antibiotics that may be used to treat infections caused
by susceptible microorganisms such as gram positive and gram negative bacteria,
chlamydiae, mycoplasmata, protozoans, or rickettsiae.

They were discovered in the 1940s and the first tetracyclines were obtained or
derived from Streptomyces bacteria.

Tetracyclines inhibit protein synthesis in the microbial RNA (an important


molecule that acts as a messenger for DNA). They are primarily bacteriostatic
which means that they prevent bacteria from multiplying but don't necessarily kill
them.

Although tetracyclines are still widely used in human and veterinary medicine, the
emergence of bacterial resistance has limited their effectiveness and is of major
concern.

What are tetracyclines used for?


Tetracyclines are used widely in both human and veterinary medicine; for
example, tetracyclines have been used:
 For the prevention of malaria
 For the treatment of moderate-to-severe acne or rosacea
 To treat anthrax
 To treat infections of the eye, gastrointestinal tract, genitourinary tract,
gums, respiratory tract, and skin
 To treat infections caused by lice, mites, or ticks (such as Rocky Mountain
spotted fever, typhus fever)
 To treat infections caused by Campylobacter, Chlamydiae, Yersinia
pestis (plague), Vibrio cholerae(cholera) and other atypical organisms
 To treat respiratory tract infections caused by Mycoplasma pneumoniae
 As a growth promoter in animals.

Because many strains of microorganisms are now resistant to some tetracyclines,


culture and susceptibility testing is recommended before beginning treatment.

Doxycycline is a tetracycline that may be considered when penicillin is


contraindicated.

What are the differences between


tetracyclines?
Although tetracyclines all work in the same way, there are differences between
the four tetracyclines (demeclocycline, doxycycline, minocycline,
and tetracycline) that are available in the U.S.

Doxycycline is the most widely prescribed tetracycline because it has the


advantage of once or twice daily dosing, availability as both an oral and an IV
preparation, and it may be taken with food without significant disruption to its
absorption. It is also less likely than other tetracyclines to cause photosensitivity
or to bind to calcium and cause tooth discoloration or bony growth retardation.
Conversely, there has been a resurgence in use of IV minocycline because
resistance appears less to minocycline compared to other tetracyclines.

Generic name Brand name examples

demeclocycline Declomycin
Generic name Brand name examples

doxycycline Adoxa, Doryx, Vibramycin

minocycline Dynacin, Minocin, Solodyn

tetracycline Ala-tet, Tetracap

Are tetracyclines safe?


Tetracyclines are considered safe when used at the recommended dosages for
the recommended duration of time. However, tetracyclines have been associated
with serious side effects, such as:

 Tooth discoloration (yellow-gray-brown) and bony growth retardation


when given during tooth or bone development (last half of pregnancy,
infancy, and during childhood up until the age of 8 years)
 Clostridium difficile associated diarrhea (CDAD). CDAD ranges in severity
from mild diarrhea to fatal colitis and has been associated with nearly all
antibacterial agents, not just tetracyclines
 Intracranial hypertension (increased pressure within the brain) has been
associated with tetracycline use. Symptoms include a headache; double,
blurred, or loss of vision. Women of childbearing age who
are overweight or who have a history of intracranial hypertension are most
at risk. Coadministration of isotretinoin increases the risk and is
contraindicated
 Toxicity to a developing fetus (tetracyclines can slow skeletal
development). Tetracyclines should only be used in pregnancy if the
benefits outweigh the risk
 Drug Rash with Eosinophilia and Systemic Symptoms (DRESS). Symptoms
include widespread rash, fever, and swollen lymph nodes, and is potentially
fatal. Discontinue the tetracycline immediately.

For a complete list of severe side effects, please refer to the individual drug
monographs.
What are the side effects of tetracyclines?
The following are some of the side effects that have been reported with
tetracyclines:

 Gastrointestinal effects such as acid reflux, diarrhea, nausea, vomiting,


stomach cramps, or loss of appetite
 A headache
 An increase in some laboratory values (such as blood urea nitrogen [BUN])
particularly in people with impaired renal function. This does not appear to
happen with doxycycline
 Photosensitivity reactions (such as an exaggerated sunburn reaction).
Rarely occurs with minocycline
 Pigmentation or discoloration of the skin and mucous membranes
(minocycline only)
 Skin rash or itching
 Sore mouth or tongue
 Vaginal itching or discharge.

Demeclocycline has also been associated with increased thirst, increased


frequency of urination and unusual tiredness. Minocycline has been associated
with dizziness, light-headedness, and unsteadiness. Tetracyclines may also cause
darkening or discoloration of the tongue but this is usually temporary.

For a complete list of side effects, please refer to the individual drug
monographs.

Read more

List of Tetracyclines:
Filter by:

Drug Name View by: Brand | Generic Reviews Avg. Ratings

Adoxa TT (More...)
0 reviews 10
generic name: doxycycline
Drug Name View by: Brand | Generic Reviews Avg. Ratings

Oraxyl (More...)
0 reviews 10
generic name: doxycycline

Adoxa (Pro, More...)


4 reviews 9.0
generic name: doxycycline

Declomycin (Pro, More...)


2 reviews 9.0
generic name: demeclocycline

Acticlate (Pro, More...)


5 reviews 8.3
generic name: doxycycline

Oracea (Pro, More...)


40 reviews 8.2
generic name: doxycycline

Dynacin (Pro, More...)


1 review 8.0
generic name: minocycline

Doxy 100 (Pro, More...)


17 reviews 7.9
generic name: doxycycline

Monodox (Pro, More...)


33 reviews 7.9
generic name: doxycycline

Minocin (Pro, More...)


18 reviews 7.7
generic name: minocycline

Doryx (Pro, More...)


64 reviews 7.5
generic name: doxycycline

Vibramycin (Pro, More...)


8 reviews 7.5
generic name: doxycycline

Solodyn (Pro, More...)


96 reviews 7.0
generic name: minocycline

Terramycin (More...)
0
generic name: oxytetracycline
3. Cephalosporins

There are five generations of cephalosporins, with increasing expanded


coverage to include gram-negative infections. Cephalosporins treat many
infections, including strep throat, ear infections, urinary tract infections, skin
infections, and meningitis. The fifth generation cephalosporin ceftaroline (Teflaro)
is active against methicillin-resistant Staphylococcus aureus (MRSA). You’ve
probably heard of common medications in this class, like:

 cefuroxime (Ceftin)
 ceftriaxone (Rocephin)
 Cefdinir (Omnicef)

View cephalosporin drugs

What are Cephalosporins?


Cephalosporins are a large group of antibiotics derived from the
mold Acremonium (previously called Cephalosporium). This mold yielded three
main compounds, historically called Cephalosporin N and C, and P, from which
the first cephalosporins were derived.

Cephalosporins are bactericidal (kill bacteria) and work in a similar way to


penicillins. They bind to and block the activity of enzymes responsible for making
peptidoglycan, an important component of the bacterial cell wall. They are called
broad-spectrum antibiotics because they are effective against a wide range of
bacteria.

Since the first cephalosporin was discovered in 1945, scientists have been
improving the structure of cephalosporins to make them more effective against a
wider range of bacteria. Each time the structure changes, a new "generation" of
cephalosporins are made. So far there are five generations of cephalosporins. All
cephalosporins start with cef, ceph, or kef.

Types of Cephalosporins
Please refer to the drug classes listed below for further information.
 cephalosporins/beta-lactamase inhibitors
 first generation cephalosporins
 fourth generation cephalosporins
 next generation cephalosporins
 second generation cephalosporins
 third generation cephalosporins
 What are Cephalosporins/beta-lactamase
inhibitors?
 Cephalosporins are a group of broad spectrum, semi-synthetic beta-lactam
antibiotics derived from the mould Cephalosporium. The mechanism of
action of cephalosporins is the same as penicillins in that they interfere
with bacterial cell wall synthesis. They are classified according to the
chronological order in which they were produce. Beta-lactamase inhibitors
block the activity of beta-lactamase enzymes. Some species of bacteria
produce beta-lactamase enzymes, which cleave the beta-lactam group in
antibiotics, such as cephalosporins, that have a beta-lactam ring in their
structure. In doing so the beta-lactamase enzyme inactivates the antibiotic
and becomes resistant to that antibiotic. To avoid development of
resistance, beta-lactamase inhibitors are administered with the beta-lactam
antibiotics so the action of beta-lactamase is inhibited. This tends to widen
the spectrum of antibacterial activity.
 List of Cephalosporins/beta-lactamase
inhibitors:
 Filter by:

Drug Name View by: Brand | Generic Reviews Avg. Ratings

Avycaz (Pro, More...)


0 reviews Add rating
generic name: avibactam/ceftazidime

Cephalosporins are a large group of antibiotics derived from the


mold Acremonium (previously called Cephalosporium). This mold yielded three
main compounds, historically called Cephalosporin N and C, and P, from which
the first cephalosporins were derived.
Cephalosporins are bactericidal (kill bacteria) and work in a similar way to
penicillins. They bind to and block the activity of enzymes responsible for making
peptidoglycan, an important component of the bacterial cell wall. They are called
broad-spectrum antibiotics because they are effective against a wide range of
bacteria.

Since the first cephalosporin was discovered in 1945, scientists have been
improving the structure of cephalosporins to make them more effective against a
wider range of bacteria. Each time the structure changes, a new "generation" of
cephalosporins are made. So far there are five generations of cephalosporins. All
cephalosporins start with cef, ceph, or kef. Note that this classification system is
not used consistently from country to country.

First generation cephalosporins refer to the first group of cephalosporins


discovered. Their optimum activity is against gram positive bacteria such
as staphylococci and streptococci. They have little activity against gram-negative
bacteria.

List of First generation cephalosporins:


Filter by:

Drug Name View by: Brand | Generic Reviews Avg. Ratings

Duricef (Pro, More...)


0 reviews 10
generic name: cefadroxil

Velosef (More...)
0 reviews 10
generic name: cephradine

Kefzol (More...)
0 reviews 9.0
generic name: cefazolin

Keflex (Pro, More...)


56 reviews 7.9
generic name: cephalexin

Ancef (Pro, More...)


0 reviews 6.5
generic name: cefazolin
Drug Name View by: Brand | Generic Reviews Avg. Ratings

Biocef (More...)
0 reviews
generic name: cephalexin

What are Fourth generation cephalosporins?


Cephalosporins are a large group of antibiotics derived from the
mold Acremonium (previously called Cephalosporium). This mold yielded three
main compounds, historically called Cephalosporin N and C, and P, from which
the first cephalosporins were derived.

Cephalosporins are bactericidal (kill bacteria) and work in a similar way to


penicillins. They bind to and block the activity of enzymes responsible for making
peptidoglycan, an important component of the bacterial cell wall. They are called
broad-spectrum antibiotics because they are effective against a wide range of
bacteria.

Since the first cephalosporin was discovered in 1945, scientists have been
improving the structure of cephalosporins to make them more effective against a
wider range of bacteria. Each time the structure changes, a new "generation" of
cephalosporins are made. So far there are five generations of cephalosporins. All
cephalosporins start with cef, ceph, or kef. Note that this classification system is
not used consistently from country to country.

Fourth generation cephalosporins refer to the fourth group of cephalosporins


discovered. They are structurally related to third-generation cephalosporins but
possess an extra ammonium group, which allows them to rapidly penetrate
through the outer membrane of Gram-negative bacteria, enhancing their activity.
They are also active against β-lactamase producing Enterobacteriaceae which may
inactivate third-generation cephalosporins.

Some fourth-generation cephalosporins have excellent activity against gram-


positive bacteria such as methicillin-susceptible staphylococci, penicillin-
resistant pneumococci and viridans group streptococci.
Cefepime is the only fourth generation cephalosporin available in the United
States. Cefpirome is available overseas.

List of Fourth generation cephalosporins:


Filter by:

Drug Name View by: Brand | Generic Reviews Avg. Ratings

Maxipime (Pro, More...)


0 reviews
generic name: cefepime

Cephalosporins are a group of broad spectrum, semi-synthetic beta-lactam


antibiotics derived from the mould Cephalosporium. They are divided into three
groups: Cephalosporin N and C are chemically related to penicillins and
Cephalosporin P a steroid antibiotic resembles fusidic acid.

The mechanism of action of cephalosporins is the same as penicillins. They


interfere with bacterial cell wall synthesis.

Semisynthetic broad-spectrum cephalosporins have been produced by the


addition of different side chains, to the Cephalosporin C nucleus.

They are classified according to the chronological order in which they were
produced.

Next generation cephalosporins will be the next lot of cephalosporins made, after
the fourth generation cephalosporins.

List of Next generation cephalosporins:


Filter by:

Drug Name View by: Brand | Generic Reviews Avg. Ratings

Teflaro (Pro, More...)


0 reviews Add rating
generic name: ceftaroline
What are Second generation cephalosporins?
Cephalosporins are a group of broad spectrum, semi-synthetic beta-lactam
antibiotics derived from the mould Cephalosporium. They are divided into three
groups: Cephalosporin N and C are chemically related to penicillins and
Cephalosporin P a steroid antibiotic resembles fusidic acid.

The mechanism of action of cephalosporins is the same as penicillins. They


interfere with bacterial cell wall synthesis.

Semisynthetic broad-spectrum cephalosporins have been produced by the


addition of different side chains, to the Cephalosporin C nucleus.

They are classified according to the chronological order in which they were
produced.

Second generation cephalosporins followed the first generation cephalosporins.

List of Second generation cephalosporins:


Filter by:

Drug Name View by: Brand | Generic Reviews Avg. Ratings

Lorabid (Pro, More...)


1 review 9.0
generic name: loracarbef

Cefotan (Pro, More...)


0 reviews 8.0
generic name: cefotetan

Zinacef (Pro, More...)


0 reviews 8.0
generic name: cefuroxime

Ceftin (Pro, More...)


37 reviews 7.7
generic name: cefuroxime

Cefzil (Pro, More...)


11 reviews 6.3
generic name: cefprozil
Drug Name View by: Brand | Generic Reviews Avg. Ratings

Lorabid Pulvules (More...)


0 reviews Add rating
generic name: loracarbef

Mefoxin (Pro, More...)


0 reviews Add ratin
generic name: cefoxitin

What are Third generation cephalosporins?


Cephalosporins are a large group of antibiotics derived from the mold
Acremonium (previously called Cephalosporium). This mold yielded three main
compounds, historically called Cephalosporin N and C, and P, from which the first
cephalosporins were derived.

Cephalosporins are bactericidal (kill bacteria) and work in a similar way to


penicillins. They bind to and block the activity of enzymes responsible for making
peptidoglycan, an important component of the bacterial cell wall. They are called
broad-spectrum antibiotics because they are effective against a wide range of
bacteria.

Since the first cephalosporin was discovered in 1945, scientists have been
improving the structure of cephalosporins to make them more effective against a
wider range of bacteria. Each time the structure changes, a new "generation" of
cephalosporins are made. So far there are five generations of cephalosporins. All
cephalosporins start with cef, ceph, or kef.

Third generation cephalosporins followed the second generation cephalosporins.


No one third generation cephalosporin treats all infectious disease scenarios.
Cefotaxime and ceftizoxime offer the best gram-positive coverage out of all the
third-generation agents; ceftazidime and cefoperazone are unique in that they
provide antipseudomonal coverage. Ceftriaxone has a long half life which allows
for once daily dosing and all of the third-generation cephalosporins except for
cefoperazone penetrate cerebrospinal fluid.

List of Third generation cephalosporins:


Filter by:

Drug Name View by: Brand | Generic Reviews Avg. Ratings

Cedax (Pro, More...)


3 reviews 9.2
generic name: ceftibuten

Rocephin (Pro, More...)


77 reviews 8.5
generic name: ceftriaxone

Claforan (Pro, More...)


0 reviews 8.0
generic name: cefotaxime

Vantin (Pro, More...)


6 reviews 7.8
generic name: cefpodoxime

Omnicef (Pro, More...)


46 reviews 6.6
generic name: cefdinir

Suprax (Pro, More...)


8 reviews 6.3
generic name: cefixime

Omnicef Omni-Pac (More...)


2 reviews 4.0
generic name: cefdinir

Spectracef (Pro, More...)


3 reviews 3.7
generic name: cefditoren

Cefizox (More...)
0 reviews Add rating
generic name: ceftizoxime

Cefobid (More...)
0 reviews Add rating
generic name: cefoperazone

Ceptaz (More...)
0 reviews Add rating
generic name: ceftazidime

Fortaz (Pro, More...)


0 reviews Add rating
generic name: ceftazidime

Tazicef (Pro, More...)


0 reviews Add rating
generic name: ceftazidime
4. Quinolones

The quinolones, also known as the fluoroquinolones, are a synthetic, bactericidal


antibacterial class with a broad-spectrum of activity. The quinolones can be used
for difficult-to-treat urinary tract infections when other options are aren’t
effective, hospital-acquired pneumonia, bacterial prostatitis, and even anthrax or
plague. The FDA issued a strong warning about this class in 2016. Familiar
names in the fluoroquinolone class include:

 ciprofloxacin (Cipro)
 levofloxacin (Levaquin)
 moxifloxacin (Avelox)

View quinolone drugs

What are Quinolones?


Quinolones are a type of antibiotic. Antibiotics kill or inhibit the growth of
bacteria.

There are five different quinolone classes. In addition, another class of antibiotic,
called fluoroquinolones, were derived from quinolones by modifying their
structure with fluorine. Quinolones and fluoroquinolones have many things in
common, but also a few differences such as what organisms they are effective
against. Some people use the words quinolones and fluoroquinolones
interchangeably.

Quinolones and fluoroquinolones detrimentally affect the function of two


enzymes produced by bacteria, topoisomerase IV and DNA gyrase, so that they
can no longer repair DNA or help in its manufacture.

What are quinolones and fluoroquinolones


used for?
Quinolones and fluoroquinolones are considered broad-spectrum antibiotics.
This means that they are effective against a wide range of bacteria.

However, because of their risk of serious side effects, the FDA has advised that
they should only be used to treat conditions such as sinusitis, bronchitis, and
uncomplicated urinary tract infections when other, less toxic antibiotics are not
appropriate.

Quinolones and fluoroquinolones may also be used to treat unusual infections


such as anthrax or plague. Doctors may also decide to use them for other types
of infection when other alternative treatment options have failed or cannot be
used.

What are the differences between


quinolones and fluoroquinolones?
Quinolones and fluoroquinolones differ in their activity against the two enzymes
produced by bacteria, topoisomerase IV and DNA gyrase. Those that are more
active against topoisomerase IV have more of an effect against gram-positive
bacteria, those that are active against DNA gyrase, are more active against gram-
negative bacteria. Newer fluoroquinolones tend to target these enzymes equally.

Quinolones and fluoroquinolones also differ in the way they are absorbed,
metabolized and excreted in the body.

Table: List of common quinolones and fluoroquinolones

Generic name Brand name examples

cinoxacin Discontinued in the U.S.

ciprofloxacin Cipro, Proquin XR

delafloxacin Baxdela

gemifloxacin Factive
Generic name Brand name examples

levofloxacin Levaquin

moxifloxacin Avelox

nalidixic acid Discontinued in the U.S.

norfloxacin Discontinued in the U.S.

ofloxacin Floxin

sparfloxacin Discontinued in the U.S.

Are quinolones and fluoroquinolones safe?


Quinolones and fluoroquinolones should be avoided in children under the age of
18 years unless they have a serious infection that cannot be treated with any
other antibiotic. This is because they can damage the weight-bearing joints in
children, and children are also more susceptible to other adverse effects of
quinolones and fluoroquinolones, including tendinitis and tendon rupture.

Quinolones and fluoroquinolones are considered safe when taken by adults for
short periods of time and exactly as directed by a doctor. However, they have
been associated with some serious effects, including tendinitis (inflammation of a
tendon) and tendon rupture. In addition, some people have reported peripheral
neuropathy (nerve pain in the fingers and toes) and central nervous system
effects such as psychosis, convulsions, and hallucinations while taking quinolones
or fluoroquinolones.

The risk of tendinitis and tendon rupture is increased in people over the age of
60, in those taking corticosteroids, or with a history of organ transplant.
Previous tendon disorders or strenuous activity may also increase risk.

Occasionally, liver damage and allergic reactions have occurred in people taking
quinolones or fluoroquinolones.
If any of these very severe side effects happen, the quinolone or fluoroquinolone
should be discontinued immediately, and all other quinolones and
fluoroquinolones avoided in the future.

What are the side effects of quinolones


and fluoroquinolones?
The most commonly reported side effects include diarrhea, nausea, abnormal
liver function tests, vomiting, and rash.

Quinolones and fluoroquinolones may also cause anxiety, insomnia, psychotic


reactions, nerve pain or a loss of feeling in the extremities, electrocardiogram
(ECG) abnormalities, increased sensitivity to light and other effects.

In people with myasthenia gravis, they may exacerbate muscle weakness and
may trigger seizures or increase the risk of having a seizure.

In people with diabetes, quinolones and fluoroquinolones may affect blood


glucose levels requiring extra monitoring.

Quinolones and fluoroquinolones increase the sensitivity of the skin to the sun
and may cause photo-sensitivity reactions and severe sunburn on exposed areas
of skin.

Quinolones and fluoroquinolones are not suitable for people with myasthenia
gravis, certain heart rhythm disturbances, or children and adolescents under the
age of 18 (unless the infection cannot be treated by another antibiotic).

Read more

List of Quinolones:
Filter by:
Drug Name View by: Brand | Generic Reviews Avg. Ratings

Maxaquin (More...)
0 reviews 10
generic name: lomefloxacin

Floxin (Pro, More...)


1 review 9.2
generic name: ofloxacin

Noroxin (Pro, More...)


2 reviews 8.5
generic name: norfloxacin

Tequin (More...)
0 reviews 8.0
generic name: gatifloxacin

Cipro I.V. (More...)


0 reviews 7.0
generic name: ciprofloxacin

Avelox (Pro, More...)


154 reviews 6.8
generic name: moxifloxacin

Cipro (Pro, More...)


240 reviews 5.9
generic name: ciprofloxacin

Levaquin (Pro, More...)


336 reviews 5.5
generic name: levofloxacin

Proquin XR (Pro, More...)


1 review 5.0
generic name: ciprofloxacin

Factive (Pro, More...)


8 reviews 4.1
generic name: gemifloxacin

Avelox I.V. (Pro, More...)


0 reviews Add rating
generic name: moxifloxacin

Baxdela (Pro, More...)


0 reviews Add rating
generic name: delafloxacin

Cinobac (More...)
0 reviews Add rating
generic name: cinoxacin

Cipro XR (Pro, More...)


1 review Add rating
generic name: ciprofloxacin
Drug Name View by: Brand | Generic Reviews Avg. Ratings

NegGram (More...)
0 reviews Add rating
generic name: nalidixic acid

Trovan (More...)
0 reviews Add rating
generic name: trovafloxacin

Zagam (More...)
0 reviews Add rating
generic name: sparfloxacin

5. Lincomycins

This class has activity against gram-positive aerobes and anaerobes (bacteria that
can live without oxygen), as well as some gram-negative anaerobes. The
lincomycin derivatives may be used to treat serious infections like pelvic
inflammatory disease, intra-abdominal infections, lower respiratory tract
infections, and bone and joint infections. These drugs include:

 clindamycin (Cleocin)
 lincomycin (Lincocin)

View lincomycin drugs

What are Lincomycin derivatives?


Lincomycin derivatives are a small group of antibiotics that inhibit synthesis of
bacterial proteins, essential for bacteria to survive. Lincomycin derivatives are
reserved for treatment of infections due to susceptible strains of pneumococci,
staphylococci and streptococci. One derivative is also indicated for treatment of
Plasmodium falciparum (malaria).

List of Lincomycin derivatives:


Surgical Prophylaxis
Filter by:
Drug Name View by: Brand | Generic Reviews Avg. Ratings

Lincocin (Pro, More...)


1 review 10
generic name: lincomycin

Cleocin HCl (More...)


3 reviews 8.5
generic name: clindamycin

Cleocin (Pro, More...)


14 reviews 6.1
generic name: clindamycin

Cleocin Pediatric (Pro, More...)


0 reviews Add rating
generic name: clindamycin

Cleocin Phosphate (Pro, More...)


0 reviews Add ratin
generic name: clindamycin

6. Macrolides

The macrolides can be use to treat community-acquired pneumonia, pertussis


(whooping cough), or for uncomplicated skin infections, among other susceptible
infections. Ketolides are a newer generation of antibiotic developed to overcome
macrolide bacterial resistance. Frequently prescribed macrolides are:

 azithromycin (Zithromax)
 clarithromycin (Biaxin)
 erythromycin

View macrolide drugs

What are Macrolide derivatives?


Macrolide derivatives are either macrolide antibiotics or other antibiotics related
to macrolides.

Macrolides are a class of antibiotics found in streptomycetes. They are natural


lactones with a large ring, consisting of 14 to 20 atoms. Macrolides bind to the
50S subunit of the bacterial ribosome and inhibit ribosomal translocation, leading
to inhibition of bacterial protein synthesis. Their action is primarily bacteriostatic
but may be bactericidal at high concentrations, or depending on the type of
microorganism.

Types of Macrolide derivatives


Please refer to the drug classes listed below for further information.

 ketolides
 macrolides

Macrolides
What are Macrolides?
Macrolides are a class of antibiotics derived from Saccharopolyspora
erythraea (originally called Streptomyces erythreus), a type of soil-borne bacteria.

Macrolides inhibit protein synthesis in bacteria by reversibly binding to the P site


of the 50S unit of the ribosome. Macrolides mainly affect gram-positive cocci and
intracellular pathogens such as mycoplasma, chlamydia, and legionella.
Erythromycin was the first macrolide discovered; other macrolides include
azithromycin, clarithromycin, and roxithromycin.

Their action is primarily bacteriostatic but may be bactericidal at high


concentrations, or depending on the type of microorganism.

List of Macrolides:
Filter by:
Drug Name View by: Brand | Generic Reviews Avg. Ratings

E.E.S.-400 (More...)
1 review 10
generic name: erythromycin

Erythrocin (Pro, More...)


2 reviews 8.0
generic name: erythromycin

Zmax (Pro, More...)


0 reviews 8.0
generic name: azithromycin

Zithromax (Pro, More...)


111 reviews 7.5
generic name: azithromycin

Biaxin XL (More...)
8 reviews 7.0
generic name: clarithromycin

Ery-Tab (Pro, More...)


1 review 7.0
generic name: erythromycin

Azithromycin Dose Pack (More...)


51 reviews 6.9
generic name: azithromycin

Dificid (Pro, More...)


5 reviews 6.8
generic name: fidaxomicin

Erythrocin Stearate Filmtab (More...)


1 review 6.7
generic name: erythromycin

Biaxin (Pro, More...)


74 reviews 6.4
generic name: clarithromycin
Drug Name View by: Brand | Generic Reviews Avg. Ratings

E.E.S.-400 Filmtab (More...)


0 reviews 3.0
generic name: erythromycin

E.E.S. Granules (Pro, More...)


0 reviews Add r
generic name: erythromycin

What are Ketolides?


Ketolides are a new generation of macrolide antibiotics designed to overcome
issues with bacterial resistance to macrolides. They are semi-synthetic antibiotics
derived from erythromycin (macrolide antibiotic) and the changes give ketolides
a broader spectrum of activity.

Ketolides bind to the bacterial 50S ribosomal subunit and inhibit RNA-dependent
protein synthesis. They are bacteriostatic at low concentrations and bactericidal
at high concentration, so basically exhibit concentration dependent killing.

Ketolides have good antibacterial activity against Gram-positive bacteria such as


those that cause respiratory tract infections.

List of Ketolides:
Filter by:

Drug Name View by: Brand | Generic Reviews Avg. Ratings

Ketek (Pro, More...)


0 reviews Add rating
generic name: telithromycin

Ketek Pak (More...)


0 reviews
generic name: telithromycin
7. Sulfonamides

Sulfonamides are effective against some gram-positive and many gram-negative


bacteria, but resistance is widespread. Common uses for sulfonamides include
UTIs, treatment or prevention of pneumocystis pneumonia, or ear infections
(otitis media). Familiar names include:

 sulfamethoxazole-trimethoprim (Bactrim, Bactrim DS, Septra)


 sulfasalazine (Azulfidine)
 sulfisoxazole (combined with erythromycin)

View sulfonamides drugs

What are Sulfonamides?


Sulfonamides are a group of man-made (synthetic) medicines that contain the
sulfonamide chemical group. They are also called sulfa drugs (sometimes spelled
as sulpha drugs or sulphonamides). Sulfanilamide was the first sulfonamide
developed in 1906, although it was not used as an antimicrobial until the late
1930s. Several thousand other substances have since been developed from
sulfanilamide.

Sulfonamide antimicrobials work by interfering with the synthesis of folic acid in


bacteria, which is essential for nucleic acid formation and ultimately DNA and
RNA. People obtain folic acid from their diet but bacteria need to synthesize it.
When used alone, sulfonamides antibiotics are bacteriostatic (stop bacteria from
reproducing but don't necessarily kill them); however, in combination with
trimethoprim (co-trimoxazole), which acts at a different enzyme in the pathway of
folic acid synthesis, sulfonamides tend to be bactericidal (kill bacteria). Many
sulphonamides are rapidly excreted and very soluble in urine so they are used to
treat infections of the urinary tract.

Not all sulfonamides have antibacterial activity. Thiazide diuretics, furosemide,


acetazolamide, sulfonylureas and some COX-2 inhibitors are also sulfonamides.

List of Sulfonamides:
Filter by:

Drug Name View by: Brand | Generic Reviews Avg. Ratings

Sulfatrim (Pro, More...)


3 reviews 8.6
generic name: sulfamethoxazole/trimethoprim

Co-trimoxazole (Pro, More...)


1 review 8.0
generic name: sulfamethoxazole/trimethoprim

Septra (Pro, More...)


16 reviews 6.7
generic name: sulfamethoxazole/trimethoprim

Septra DS (More...)
21 reviews 6.4
generic name: sulfamethoxazole/trimethoprim

Bactrim (Pro, More...)


308 reviews 6.1
generic name: sulfamethoxazole/trimethoprim

Bactrim DS (Pro, More...)


207 reviews 5.7
generic name: sulfamethoxazole/trimethoprim

SMZ-TMP DS (More...)
23 reviews 5.2
generic name: sulfamethoxazole/trimethoprim

Sulfatrim Pediatric (More...)


0 reviews 1.0
generic name: sulfamethoxazole/trimethoprim

Cotrim (More...)
0 reviews Add rating
generic name: sulfamethoxazole/trimethoprim

Gantrisin (More...)
0 reviews Add rating
generic name: sulfisoxazole

Gantrisin Pediatric (More...)


0 reviews Add rating
generic name: sulfisoxazole
8. Glycopeptide Antibiotics

Members of this group may be used for treating methicillin-


resistant staphylococcus aureus (MRSA) infections, complicated skin infections, C.
difficile-associated diarrhea, and enterococcal infections such as endocarditis
which are resistant to beta-lactams and other antibiotics. Common drug names
include:

 dalbavancin (Dalvance)
 oritavancin (Orbactiv)
 telavancin (Vibativ)
 vancomycin (Vancocin)

View glycopeptide drugs

What are Glycopeptide antibiotics?


Glycopeptide antibiotics inhibit bacterial cell wall formation by inhibiting
peptidoglycan synthesis. They are used for treating methicillin-resistant
staphylococcus aureus (MRSA) infections and enterococcal infections, which are
resistant to beta-lactams and other antibiotics. They are also used in cases where
there is allergy to beta-lactams.

List of Glycopeptide antibiotics:


Filter by:

Drug Name View by: Brand | Generic Reviews Avg. Ratings

Vancocin HCl (More...)


1 review 10
generic name: vancomycin

Vancocin (Pro, More...)


1 review 8.0
generic name: vancomycin

Orbactiv (Pro, More...)


1 review 1.0
generic name: oritavancin
Drug Name View by: Brand | Generic Reviews Avg. Ratings

Dalvance (Pro, More...)


0 reviews Add rating
generic name: dalbavancin

Firvanq (Pro, More...)


0 reviews Add rating
generic name: vancomycin

Vancocin HCl Pulvules (More...)


0 reviews Add rating
generic name: vancomycin

Vibativ (Pro, More...)


0 reviews Add rating
generic name: telavancin

9. Aminoglycosides

Aminoglycosides inhibit bacterial synthesis by binding to the 30S ribosome and


act rapidly as bactericidal antibiotics (killing the bacteria). These drugs are usually
given intravenously (in a vein through a needle). Common examples in this class
are:

 gentamicin
 tobramycin
 amikacin

View aminoglycoside drugs

What are Aminoglycosides?


Aminoglycosides are a class of antibiotics used mainly in the treatment of aerobic
gram-negative bacilli infections, although they are also effective against other
bacteria including Staphylococci and Mycobacterium tuberculosis. They are
often used in combination with other antibiotics.

Aminoglycosides are thought to work by inhibiting protein synthesis inside


bacteria. Kill rates of bacteria are increased when higher concentrations of
aminoglycosides are present; however, the margin between a safe and a toxic
dose is narrow and monitoring is often needed, although once daily dosing
increases the safety window. Impairment of kidney function and hearing loss are
the most common side effects of aminoglycosides. Aminoglycosides tend to be
used when other less toxic antibiotics are contraindicated or ineffective.

Aminoglycosides are not well absorbed when given by mouth, so need to be


given by injection by healthcare personnel.

List of Aminoglycosides:
Filter by:

Drug Name View by: Brand | Generic Reviews Avg. Ratings

Paromycin (More...)
0 reviews 10
generic name: paromomycin

Tobi (Pro, More...)


0 reviews 9.0
generic name: tobramycin

Garamycin (More...)
0 reviews 8.0
generic name: gentamicin

Humatin (Pro, More...)


1 review 4.0
generic name: paromomycin

Amikin (Pro, More...)


1 review 2.5
generic name: amikacin

Amikin Pediatric (More...)


0 reviews Add rating
generic name: amikacin

Bethkis (Pro, More...)


0 reviews Add rating
generic name: tobramycin

Kantrex (Pro, More...)


0 reviews Add rating
generic name: kanamycin

Kitabis Pak (Pro, More...)


0 reviews Add rating
generic name: tobramycin
Drug Name View by: Brand | Generic Reviews Avg. Ratings

Nebcin (More...)
0 reviews Add rating
generic name: tobramycin

Neo-Fradin (Pro, More...)


0 reviews Add rating
generic name: neomycin

10. Carbapenems

These injectable beta-lactam antibiotics have a wide spectrum of bacteria-killing


power and may be used for moderate to life-threatening bacterial infections like
stomach infections, pneumonias, kidney infections, multidrug-resistant hospital-
acquired infections and many other types of serious bacterial illnesses. Members
of this class include:

 imipenem/cilastatin (Primaxin)
 meropenem (Merrem)
 doripenem (Doribax)
 ertapenem (Inanz)

View carbapenems drugs

What are Carbapenems?


Carbapenems are a class of beta-lactam antibiotic that are active against many
aerobic and anaerobic gram-positive and gram-negative organisms. Thienamycin
was the first carbapenem to be discovered in 1976. Carbapenems are notable for
their ability to inhibit beta-lactamase enzymes (also called penicillinase) - a type
of enzyme that greatly reduces the activity of antibiotics such as penicillins and
cephamycins. Of all the beta-lactam antibiotics, carbapenems possess the
broadest spectrum of activity and the greatest potency against bacteria. Because
of this, they are often reserved for more severe infections or used as "last-line"
agents.
Carbapenems inhibit bacterial cell wall synthesis by binding to the penicillin-
binding proteins and interfering with cell wall formation.

List of Carbapenems:
Filter by:

Drug Name View by: Brand | Generic Reviews Avg. Ratings

Doribax (Pro, More...)


1 review 10
generic name: doripenem

Merrem (Pro, More...)


0 reviews 6.0
generic name: meropenem

Invanz (Pro, More...)


1 review 1.0
generic name: ertapenem

Primaxin IM (Pro, More...)


0 reviews
generic name: cilastatin/imipenem

Are There Any Over-the-Counter Antibiotics?


Over-the-counter (OTC) oral antibiotics are not approved in the U.S. A bacterial
infection is best treated with a prescription antibiotic that is specific for the type
of bacteria causing the infection. This will increase the chances that the infection
is cured and help to prevent antibiotic resistance. In addition, a lab culture may
need to be performed to pinpoint the bacteria and to help select the best
antibiotic. Taking the wrong antibiotic -- or not enough -- may worsen the
infection and prevent the antibiotic from working the next time.

There are a few OTC topical antibiotics that can be used on the skin. Some
products treat or prevent minor cuts, scrapes or burn on the skin that may get
infected with bacteria. These are available in creams, ointments, and even sprays.
Common OTC topical antibiotics:

 Neosporin, Medi-Quik (bacitracin/neomycin/polymyxin B)


 Polysporin (bacitracin/polymyxin)
 Triple antibiotic, generic (bacitracin/neomycin/polymyxin B)
 Neosporin Plus (neomycin/polymyxin/pramoxine)

There are some OTC antibacterials for acne sufferers, too. They contain the
antibacterial benzoyl peroxide, which also has mild drying effect for acne. Many
products are found on the pharmacy shelves as gels, lotions, solutions, foams,
cleaning pads, and even facial scrubs.

Common OTC antibacterials for acne:

 Clearskin
 Oxy-10
 Proactiv

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Home › Reference › Antibiotics › Antibiotics - Common Side Effects, Allergies and Reactions

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Common Side Effects from


Antibiotics, and Allergies and
Reactions
Medically reviewed on Mar 5, 2017 by L. Anderson, PharmD.

What Are the Common Side Effects of


Antibiotics?
All medications have side effects. When used appropriately, antibiotics are
relatively safe with typically few side effects. However, some antibiotics are
notorious for producing side effects that can be especially intolerable.
An antibiotic side effect is defined as an unwanted reaction that occurs in
addition to the desirable therapeutic action of the antibiotic. Like any drug,
antibiotic side effects can occur and may interfere with the patient’s ability to
tolerate and finish the course of medication.
Common side effects with antibiotics include:

 Rash
 Soft stools, diarrhea
 Upset stomach
 Fungal (yeast) infections like thrush

Contact your health care provider if you have any of these side effects while
taking an antibiotic:

 Severe allergic reaction that results in difficulty breathing, facial swelling


(lips, tongue, throat, face)
 Severe watery or bloody diarrhea or stomach cramps
 Vaginal yeast infection with white discharge and severe itching
 Mouth sores or white patches in your mouth or on your tongue

Side effects of antibiotics can range from mild allergic reactions to severe and
debilitating adverse events. These side effects are extremely variable from patient
to patient and from antibiotic to antibiotic. However, there are some common
side effects that may occur within antibiotic drug classes, as described in Table 1.
Long term side effects of antibiotics can occur, but are infrequent.

Should I Stop My Antibiotic If I'm Having a


Side Effect?
If you are experiencing a bothersome or serious antibiotic side effect, you should
contact your health care provider to discuss your symptoms. The outcomes may
include:

 Staying on the same antibiotic and managing the side effect


 Adjusting the dose
 Switching to a different antibiotic

Usually, antibiotic treatment should not be stopped without a health care


provider’s approval; all medication should be finished. Stopping antibiotics early
due to side effects may allow the infection to worsen and may lead to antibiotic
resistance, making an antibiotic less effective. Even if the infection appears to
have cleared up before all of the medication is gone, the full course of antibiotic
treatment should always be completed unless you are told otherwise by your
doctor.

Antibiotic Allergies
Antibiotic allergies or hypersensitivity reactions are some of the most common
side effects of antibiotics leading to emergency room admission. 1 Always tell your
doctor of any previous allergic reaction to any medication, including antibiotics.
Mild allergic reactions may only result in a skin rash. A more severe allergic
reaction called anaphylaxis is a medical emergency that requires immediate
medical attention.

Anaphylactic reactions due to antibiotics may include:

 Shortness of breath
 Wheezing
 Nausea/vomiting
 Lightheadedness, dizziness
 Fast heart rate
 Swelling of the face, lips or tongue
 Shock

Immediately call for medical help if any of these symptoms should appear after
taking an antibiotic.

Are Antibiotics Effective for a Cold or Flu?


Antibiotics are used to kill bacterial infections; they are not effective against
viral infections, such as a cold or the flu, or against fungal infections, like
ringworm or vaginal yeast infections.

You should avoid demanding an antibiotic from your healthcare provider when
you have a viral infection as it will not cure your infection; it might actually make
it worse. In addition, this adds to the problem of antibiotic resistance, and it costs
you money you do not need to spend. Your doctor can offer symptomatic
treatment to ease your viral infection, or prescribe specific anti-viral medications
if appropriate.

Table 1: List of Antibiotics and Their Side


Effects
What are the side effects of antibiotics? The most common antibiotic classes and
drug members are listed in Table 1, along with the most commonly reported
antibiotic side effects. This is a comprehensive overview, but not a complete list,
of common antibiotics or side effects that may occur.

Antibiotic Class Antibiotic Class Members Most Common Side Effects Additional Clinical Comm

List of Penicillins Penicillin, amoxicillin, Rash, diarrhea, abdominal pain, If bloody stools, anaphyl
amoxicillin-clavulanate, nausea/vomiting, drug severe skin reaction, feve
ampicillin, piperacillin- fever, hypersensitivity (allergic) contact health care prov
tazobactam, nafcillin, reactions immediately; ampicillin m
oxacillin cause pseudomembrano
colitis

List of Cephalosporins Cephalexin, cefaclor, Rash, diarrhea, Cross-hypersensitivity m


cefuroxime, ceftibuten, nausea/vomiting (rare), occur in patients with
cefdinir, cefixime, hypersensitivity (allergic) documented penicillin al
ceftriaxone reactions, serum sickness,
vaginal candidiasis

List of Aminoglycosides Gentamicin, tobramycin, Renal (kidney) toxicity, Long term antibiotic or m
amikacin ototoxicity (hearing loss), treatment periods may l
dizziness, nausea/vomiting, greater risk for ototoxicit
nystagmus (kidney) toxicity

List of Carbapenems Meropenem, ertapenem, Diarrhea, nausea/vomiting, Hypersensitivity reaction


doripenem, imipenem- headache, rash, liver toxicity, reported with meropene
cilastatin eosinophilia (elevated white imipenem in patients wit
blood cells) penicillin allergy
Antibiotic Class Antibiotic Class Members Most Common Side Effects Additional Clinical Comm

List of Antituberculosis Rifampin, rifabutin, Diarrhea, nausea/vomiting, Sides effects vary among
Agents isoniazid, pyrazinamide, anorexia, hemolytic anemia, agents, check individuall
ethambutol, dapsone liver toxicity, headache, vitamin B6 (pyridoxine) m
peripheral neuropathy, taken to help prevent
dizziness, reddish-orange body peripheral neuropathy w
fluids (rifampin, rifabutin only) isoniazid

List of Glycopeptides Vancomycin, telavancin Vancomycin: red man IV infusion of vancomyci


syndrome (flushing, 60 minutes may prevent
hypotension, itching); phlebitis; man syndrome
telavancin: taste alteration,
nausea/vomiting, headache,
dizziness

List of Macrolides(i.e., side Erythromycin, Abdominal pain, diarrhea, High rate of gastrointesti
effects of Z Pak antibiotic) azithromycin (Z Pak), anorexia, nausea/vomiting, (stomach) side effects; d
clarithromycin taste alterations crush, chew, break, open
(clarithromycin) enteric-coated or delaye
release pill

List of Sulfonamides Trimethoprin- Nausea/vomiting, diarrhea, Avoid prolonged sunligh


sulfamethoxazole, anorexia, abdominal pain, rash, exposure; use sunscreen
erythromycin- photosensitivity, headache, protective clothing; antib
sulfisoxazole, sulfadiazine dizziness cause of Stevens Johnson
Syndrome, Toxic Epiderm
Necrolysis

List of Tetracyclines Tetracycline, doxycycline, Nausea/vomiting, diarrhea, Avoid prolonged sunligh


minocycline anorexia, abdominal pain, tooth exposure; use sunscreen
discoloration in children < 8 protective clothing
years, liver toxicity

Quinolones (i.e., Cipro antibiotic Ciprofloxacin (Cipro), Nausea/vomiting, diarrhea, Avoid prolonged sunligh
side effects) levofloxacin (Levaquin), abdominal pain, headache, exposure; use sunscreen
moxifloxacin (Avelox), lethargy, insomnia, protective clothing;
ofloxacin (Floxin) photosensitivity (can be severe) moxifloxacin associated
Antibiotic Class Antibiotic Class Members Most Common Side Effects Additional Clinical Comm

higher rates of side effec


tendon rupture (rare) mo
common in age > 60, wit
corticosteroid use, in kid
heart, lung translant reci

List of Lincomycin derivatives Clindamycin, lincomycin Pseudomembranous If severe diarrhea during


colitis (may be severe), treatment or for up to 8
diarrhea, nausea/vomiting, after treatment consult h
rash, hypersensitivity, jaundice care provider immediate
(clindamycin) be pseudomembranous
(C. dificile); consider use
toxic agents

Miscellaneous Metronidazole Nausea/vomiting, dizziness, Avoid alcohol use during


headache, vaginal candidiasis, treatment and for up to
metallic taste after, combined use may
cramps, nausea/vomiting
flushing, headache; may
discolor urine red-brown

There are several side effects that are common to most antibiotics, regardless of
class or drug. These side effects may include:

 Antibiotic-associated diarrhea
 Yeast infections (vaginal, oral)
 Anaphylaxis
 Serious allergic skin reactions
 Complications from intravenous (IV) use of antibiotics (phlebitis)

In one study, antibiotic side effects led to greater than 140,000 emergency
department admissions per year in the United States. Roughly 50 percent of
emergency visits were due to reactions to antibiotics in the penicillin class of
drugs, and the other 50 percent were due to a wide variety of antibiotics used to
treat many different types of infections. In this study, children less than one year
of age were found to have the highest rate of antibiotic side effects.

 Allergic Reactions, Anaphylaxis: Allergic reactions account for the most


common type of side effect with antibiotics. In one study, it was estimated
that over 142,000 emergency department visits per year were due to
antibiotic adverse events, and approximately four-fifths of these events
were due to allergic reactions. Allergic reactions can typically only be
prevented by avoiding the drug, although desensitization may be possible
in certain circumstances for patients who have no other antibiotic
options.1 Anaphylaxis is the most serious type of allergic reaction and can
be life-threatening.

 Antibiotic-associated diarrhea: Antibiotic-associated diarrhea occurs in


patients receiving antibiotics due to no explainable reason. Five to twenty-
five percent of patients may develop antibiotic-associated diarrhea. The
diarrhea occurs due to eradication of the normal gut flora by the antibiotic
and results in an overgrowth of infectious bacteria, such as Clostridium
dificile. If the diarrhea is severe, bloody, or is accompanied by stomach
cramps of vomiting, a physician should be contacted. The most common
antibiotics implicated in antibiotic-associated diarrhea are amoxicillin-
clavulanate, ampicillin, and cefixime; however, other antibiotics may lead to
this side effect, including cephalosporins, fluoroquinolones (e.g., side
effects of Cipro antibiotic), azithromycin (e.g., Z Pak), clarithromycin
(Biaxin), erythromycin, and tetracycline. 2 Probiotics such as Saccharomyces
boulardii (Florastor) have been shown to be effective in helping to prevent
antibiotic associated diarrhea in children and adults. 4

 Vaginal yeast infections or oral thrush (candida species): Antibiotics


may also change the normal flora balance in the vagina, often leading to
an overgrowth of fungal species. Candida albicans is a common fungus
normally present in small amounts in the vagina, mouth, gastrointestinal
tract, and on the skin and does not normally cause disease or symptoms.
However, the fungus may take over when there is limited competition from
bacteria due to antibiotic treatment.
 Stevens Johnson Syndrome (SJS), Toxic Epidermal
Necrolysis (TEN): Stevens-Johnson syndrome (SJS) and toxic epidermal
necrolysis (TEN) are rare but serious allergic reactions to substances, often
drugs, that result in serious skin and mucous membrane disorders.
Antibiotics such as sulfonamides, penicillins, cephalosporins, and
fluoroquinolones may result in SJS and TEN. SJS and TEN can both cause
rash, skin peeling, and sores on the mucous membranes and may be life-
threatening.3

 Injection site reactions or phlebitis: A reaction to an antibiotic can occur


if the antibiotic is given intravenously in a vein. Injections site reactions and
phlebitis (vein inflammation) can occur. The vein and area with the IV
needle may be red, swollen and hot. An infection may or may not be
present. Typically, the needle must be removed and reinserted elsewhere
to help clear the injection site reaction.

Antibiotics are among the most commonly prescribed medications in the US.
However, many side effects may not be reported. Always consult your doctor or
healthcare specialist for medical advice. You may also report side effects to the
FDA at http://www.fda.gov/medwatch/ or 1-800-FDA-1088 (1-800-332-1088).

See Also
 Acute Bronchitis in Adults
 Alcohol and Antibiotics
 Antibiotic Resistance
 Antibiotic Shortages: A Serious Safety Concern
 Antibiotics and Birth Control Pill Interactions
 Antibiotics for UTI Treatment
 Top 10 FAQs for Middle Ear Infections in Children
 Why Don’t Antibiotics Kill Viruses?

Sources

1. Shehab N, Patel P, Srinivasan A, et al. Emergency department visits for antibiotic-associated


adverse events. Clinical Infectious Diseases 2008;47:735-43.

2. Bartlett JG. Clinical practice. Antibiotic-associated diarrhea. N Engl J Med 2002:346:334-9.


3. The Merck Manual for Health Care Professionals. Stevens-Johnson Syndrome (SJS) and Toxic
Epidermal Necrolysis (TEN).

4. Szajewska H, Kołodziej M. Systematic review with meta-analysis: Saccharomyces boulardii in the


prevention of antibiotic-associated diarrhoea. Aliment Pharmacol Ther. 2015 Oct;42(7):793-801. doi:
10.1111/apt.13344. Accessed online 3/6/2017
at https://www.ncbi.nlm.nih.gov/pubmed/26216624.

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Informed Health Online [Internet].

Using medication: Using antibiotics correctly and avoiding


resistance

Last Update: December 18, 2013; Next update: 2017.

The development of antibiotics was one of the great discoveries in modern medicine.
They fight bacteria and can cure life-threatening infectious diseases such as pneumonia,
for which there was previously no effective treatment. But the improper use of antibiotics
means that more and more bacteria are becoming resistant to this kind of medication. So
it is especially important to use them correctly.
Antibiotics can save lives, but they also relieve symptoms of bacterial infections and help us
recover faster. But treatment with antibiotics also has side effects. Nausea or diarrhea are
common, for example.
Antibiotics are also used far too often, and improper use is widespread. This has caused many
different types of bacteria to become resistant (unresponsive) to antibiotics. Because resistance
has become more common, many diseases cannot be treated as well as they could in the past.
When using antibiotics, it's important to know the following things to prevent resistance and side
effects:
 Antibiotics only work against bacteria. Many infections are caused by viruses and can't
be treated using antibiotics – examples include respiratory illnesses such as a cough,
stuffy nose, bronchitis or the flu.
 Excessive and improper use of antibiotics causes side effects, and in the long term
reduces their effectiveness.

What is antibiotic resistance?


In medicine, bacteria and other germs are said to be resistant if they are especially able to
withstand exposure to external influences. For example, most germs that enter the stomach with
food will be killed by stomach (gastric) acid. But some bacteria are covered with
a mucous coating that protects them from the acid. They are resistant to gastric acid.
Resistance to antibiotics works on a similar principle: The bacteria have acquired a new
property that protects them from the antibiotic. Some types of bacteria can produce a substance
that makes certain antibiotics ineffective, for example. Bacteria that can protect themselves from
several different antibiotics are referred to as "multiresistant."

What causes resistance?


Many of the bacteria that are now resistant used to be sensitive to antibiotics. There are a few
developments that played a role in this. To put it briefly, one kind of antibiotic could originally
neutralize a certain type of bacteria and then effectively stop the infection. But the genetic
material of bacteria can change by chance, sometimes creating new properties. If they protect
the bacteria from an antibiotic, then the bacteria have become resistant. These kinds of
properties can also transfer from one type of bacteria to another.
If antibiotics are used very often, resistant bacteria are better able to reproduce because the
other non-resistant strains of bacteria are stopped. Antibiotics then no longer help against
infections caused by resistant bacteria.

Which bacteria are resistant to antibiotics and why are they dangerous?
Strains of Streptococcus and Staphylococcus bacteria are often resistant to antibiotics. One
example is called “methicillin-resistant Staphylococcus aureus” (MRSA). Staphylococci can be
found on skin and mucous membranes and may cause infection – for example if they get into
open wounds.
Resistant strains have now developed in other types of bacteria, such as Escherichia coli,
Klebsiella and pseudomonads.

What is being done about antibiotic resistance?


In Germany, antibiotics are prescription-only. This means that doctors are first and foremost
responsible for careful and appropriate use. They are to first see whether someone actually has
a bacterial infection. If they do, then it's important that the antibiotic is prescribed at the right
dose and for long enough, and that the right antibiotic is selected that will most effectively fight
the bacteria.
There are also hygiene regulations to keep resistant bacteria from spreading further and
preventable infections from occurring. These measures are especially important inside of a
hospital. Antibiotics are used there relatively frequently, so resistant germs can develop quite
quickly. If you come into contact with someone who has an infection of resistant bacteria, it can
help to wear disposable gloves, a mask and coat, and to use a hand disinfectant to stop the
spread of the germs.
Antibiotics are also used in veterinary medicine and in agriculture. Veterinarians also have to
comply with the rules for handling antibiotics properly.

What can I do to prevent antibiotic resistance?


Being cautious when taking antibiotics can help prevent both antibiotic resistance and side
effects.
The most important thing is to not overestimate what antibiotics can do: Patients often
expect antibiotics to be prescribed to treat medical conditions for which they are not suitable.
Antibiotics are needed to treat serious bacterial infections like lung infections
or meningitis (inflammation of the membranes lining the brain and spinal cord). This is not the
case when, for example, people who are otherwise healthy have respiratory infections caused
by viruses, such as a cold or influenza (“the flu”). Antibiotics will usually be of no help because
they only fight bacteria. Antibiotics also have side effects including allergic
reactions, stomach and bowel problems, nausea and fungal infections. Because of these
associated risks, it's important to carefully consider the advantages and disadvantages of
taking antibiotics.

What's important to consider when taking antibiotics?


Antibiotics should be taken for as long as the doctor has prescribed them. Just because the
symptoms of the illness subside, it doesn't mean that all of the germs have been killed.
Remaining bacteria may cause the illness to start up again.
If there are some tablets left over, they should not be kept for later use or given to other people.
Leftover medication can be disposed of in the normal garbage or dropped off at some
pharmacies. Pharmacies are not obligated to accept opened medicine though. It is important not
to dispose of the medication by pouring it down the drain or flushing it down the toilet. That is
bad for the environment and also contributes to bacterial resistance.
Medications can only work properly if they are used correctly. It's important to know the
following things when taking antibiotics:
 Can the tablets be broken into smaller pieces to make them easier to
swallow? Doing this can stop some medications from working properly.
 What food can you take antibiotics with? Antibiotics are usually taken with water
because taking them together with fruit juices, dairy products or alcohol can affect how
the body absorbs some drugs. Dairy products include milk as well as butter, yogurt, and
cheese. After taking an antibiotic you may need to wait for up to three hours before
eating or drinking any dairy products. Grapefruit juice and dietary supplements
containing minerals like calcium may also work dampen the effect of antibiotics.
 When should you take antibiotics? Some antibiotics are always meant to be taken at
the same time of day, others are meant to be taken before, with or after a meal. If you
are supposed to take the medicine three times a day, for example, it usually needs to be
taken at set times so that the effect is spread out evenly over the course of the day. You
could remember the regular times of 6 a.m., 2 p.m. and 10 p.m. for an antibiotic that
needs to be taken every 8 hours, for example.
 Can you take antibiotics together with other medications? Because antibiotics can
interact with other medications, it's important to tell your doctor if you take other
medications too. Antibiotics might interact with some blood thinners and antacids, for
example. Some antibiotics can make birth control pills less effective.

Facts about Antibiotic Resistance


 Antibiotic resistance is one of the most urgent threats to the public’s
health.
 Every time a person takes antibiotics, sensitive bacteria are killed, but
resistant ones may be left to grow and multiply.
 Overuse of antibiotics is a major cause of increases in drug-resistant
bacteria.
 Overuse and misuse of antibiotics threatens the usefulness of these
important drugs. Decreasing inappropriate antibiotic use is a key
strategy to control antibiotic resistance.
 Antibiotic resistance in children and older adults is of particular
concern because these age groups have the highest rates of antibiotic
use.
 Antibiotic resistance can cause significant suffering for people who
have common infections that once were easily treatable with
antibiotics.
 When antibiotics do not work, infections often last longer, cause more
severe illness, require more doctor visits or longer hospital stays, and
involve more expensive and toxic medications. Some resistant
infections can even cause death.

Read Antibiotic Resistance Threats in the United States, 2013

Antibiotic Prescribing: Attitudes, Behaviors,


Trends and Cost
 At least 30% of antibiotic courses prescribed in the outpatient setting
are unnecessary, meaning no antibiotic was needed at all. Most of this
unnecessary use is for acute respiratory conditions, such as colds,
bronchitis, sore throats caused by viruses, and even some sinus and
ear infections 1.
 Total inappropriate antibiotic use (which includes unnecessary
antibiotic use plus inappropriate antibiotic selection, dosing, and
duration) may approach 50% of all outpatient antibiotic use .
2, 3, 4

 The number of antibiotic prescriptions written for children has


decreased in recent years ., but almost 30% of antibiotics
2, 5, 6

prescribed to children are still unnecessary 1.


 Antibiotics cause 1 out of 5 emergency department visits for adverse
drug events (ADEs) 7,
. Antibiotics are the most frequent cause of
8

ADEs leading to emergency department visits in children, and 7 of the


top 10 drugs involved in ADEs leading to emergency room visits are
antibiotics .
9

 We spent $10.7 billion on antibiotics in the United States in 2009,


including $6.5 billion among patients who visit physician offices and
$3.5 billion among hospitalized patients 10
.
 The NMC states that administration of medicines
is ‘not solely a mechanistic task to be performed
in strict compliance with the written prescription
of a medical practitioner. It requires thought and
exercise of professional judgement’ (NMC, 2002).
 To practise accountably and in accordance with
NMC requirements it is essential that nurses are
competent in the preparation and reconstitution of
a wide variety of drugs pertinent to their clinical
area. This requires an extensive knowledge of
pharmacological agents and their application.
 Although it can be difficult to keep up to date with
best practice and new research, nurses must
ensure their knowledge and practice are informed
and that they are aware of mechanisms to ensure
that procedures are in line with current best
practice, organisational policy and specific
manufacturers’ recommendations in their own
area of practice.

 Risk management
 In preparing to administer any drug nurses must
be aware of the relevant health and safety issues,
notably the safe use and disposal of sharps and
good infection control practice.
 The drug solution and its preparation may be
hazardous to the health of the nurse preparing it
or to those within the environment and the
necessary precautions must be taken to minimise
risk.
 Drug errors can occur for many reasons but it has
been suggested that many are caused by some
nurses having poor mathematical skills (Trim,
2004).
 Prior to any drug preparation it is essential that
the dose/volume is calculated correctly and that
all but the simplest calculations are checked by a
second practitioner. Most organisations require
that two nurses check drugs for IV administration,
although in some working environments this may
not be practical.
 The procedure
 Intravenous drugs come in a variety of
presentations, the most common being single-
dose glass ampoules or rubber-capped vials. The
procedure varies slightly for each presentation.

 Rubber-capped vials

 - Wash the hands and don a clean apron (Fig 1);


 - Check that both drug and diluent packaging are
intact and are to be used prior to their expiry date
(Fig 2);
 - Check the drug and diluent against the
prescription;
 - Break the seal on the container of the diluent;
 - Using a syringe and needle (or a withdrawing
needle) aspirate the required volume;
 - Remove the plastic covering cap from the drug
vial;
 - If required, clean the rubber cap with an alcohol
wipe. The effectiveness of this procedure is
debatable but if it is carried out it is essential that
the alcohol has evaporated before any needles are
inserted;
 - Insert a venting needle into the rubber cap;
 - Insert the diluent syringe into the vial, via the
rubber cap (Fig 3) - at a 45 degs angle, with needle
bevel uppermost. Changing the angle to 90 degs
as the needle pushes through is considered to
minimise coring, in which rubber is forced into the
lumen of the needle with the resultant risk that it
may then be injected into the patient (Dougherty
and Lister, 2004);
 - Inject the diluent, ensuring that it does not rise
above the tip of the venting needle;
 - Remove the diluent syringe and needle. The
venting needle can be covered with an alcohol
wipe;
 - Agitate the vial to reconstitute the drug, taking
care to avoid any spillage from the venting needle;
 - Inspect the drug to ensure it has taken on the
characteristics outlined in the manufacturer’s
instructions. Also ensure that there is no
particulate contamination (Fig 4);
 - Insert the syringe and withdraw the required
amount of the drug, tilting the vial to one side if
necessary (Fig 5);
 - Expel any air from the syringe either into the vial
(by inverting the vial) or into a sheathed needle
(Fig 6).

 Glass ampoules

 The procedure for glass ampoules is similar to


that for rubber-capped vials with the following
considerations:
 - Tap the top of the ampoule to allow any trapped
drug to drain into the bottom;
 - Cover the top of the ampoule with gauze;
 - Snap the top using a dot marker as a guide if
appropriate. Some ampoules may require the
application of a file to snap the neck, although the
dot marker has minimised this;
 - Carefully inspect the drug in order to check for
glass and particulate contamination.

 Professional
responsibilities
 All nurses who prepare drugs for IV administration
must have received approved training and
demonstrated competence under supervision. The
onus is also on the individual to ensure knowledge
and skills are maintained both from a theoretical
and practical perspective. Nurses should also
undertake this role in accordance with their
organisation’s protocols, policies and guidelines.

 COMMENT

 POLYMYXIN B FOR INJECTION


500,000 Units
 To reduce the development of drug-resistant bacteria and maintain the effectiveness of
polymyxin B (polymyxin b sulfate) and other antibacterial drugs, polymyxin B
(polymyxin b sulfate) should be used only to treat or prevent infections that are proven or
strongly suspected to be caused by bacteria.
 WARNING

 CAUTION: WHEN THIS DRUG IS GIVEN INTRAMUSCULARLY AND/OR


INTRATHECALLY, IT SHOULD BE GIVEN ONLY TO HOSPITALIZED
PATIENTS, SO AS TO PROVIDE CONSTANT SUPERVISION BY A PHYSICIAN.
 RENAL FUNCTION SHOULD BE CAREFULLY DETERMINED AND PATIENTS
WITH RENAL DAMAGE AND NITROGEN RETENTION SHOULD HAVE
REDUCED DOSAGE. PATIENTS WITH NEPHROTOXICITY DUE TO
POLYMYXIN B (polymyxin b sulfate) SULFATE USUALLY SHOW
ALBUMINURIA, CELLULAR CASTS, AND AZOTEMIA. DIMINISHING URINE
OUTPUT AND A RISING BUN ARE INDICATIONS FOR DISCONTINUING
THERAPY WITH THIS DRUG.

 NEUROTOXIC REACTIONS MAY BE MANIFESTED BY IRRITABILITY,


WEAKNESS, DROWSINESS, ATAXIA, PERIORAL PARESTHESIA, NUMBNESS
OF THE EXTREMITIES, AND BLURRING OF VISION. THESE ARE USUALLY
ASSOCIATED WITH HIGH SERUM LEVELS FOUND IN PATIENTS WITH
IMPAIRED RENAL FUNCTION AND/OR NEPHROTOXICITY.

 THE CONCURRENT OR SEQUENTIAL USE OF OTHER NEUROTOXIC AND/OR


NEPHROTOX-IC DRUGS WITH POLYMYXIN B (polymyxin b sulfate) SULFATE,
PARTICULARLY BACITRACIN, STREPTOMYCIN, NEOMYCIN, KANAMYCIN,
GENTAM-ICIN, TOBRAMYCIN, AMIKACIN, CEPHALORI-DINE,
PAROMOMYCIN, VIOMYCIN, AND COLISTIN SHOULD BE AVOIDED.

 THE NEUROTOXICITY OF POLYMYXIN B (polymyxin b sulfate) SULFATE CAN


RESULT IN RESPIRATORY PARALYSIS FROM NEUROMUSCULAR
BLOCKADE, ESPECIALLY WHEN THE DRUG IS GIVEN SOON AFTER
ANESTHESIA AND/OR MUSCLE RELAXANTS.

 USAGE IN PREGNANCY: THE SAFETY OF THIS DRUG IN HUMAN


PREGNANCY HAS NOT BEEN ESTABLISHED.

 DESCRIPTION

 Polymyxin B for Injection (polymyxin b (polymyxin b sulfate) sulfate) is one of a group


of basic polypeptide antibiotics derived from B polymyxa (B aerosporous). Polymyxin B
(polymyxin b sulfate) sulfate is the sulfate salt of Polymyxins B1 and B2, which are
produced by the growth of Bacillus polymyxa(Prazmowski) Migula (Fam. Bacillacea).It
has a potency of not less than 6000 polymyxin B (polymyxin b sulfate) units per mg,
calculated on the anhydrous basis.The structural formulae are:
 Each vial contains 500,000 polymyxin B (polymyxin b sulfate) units for parenteral or
ophthalmic administration.
 Polymyxin B (polymyxin b sulfate) forInjection is in powder form suitable for
preparation of sterile solutions for intramuscular, intravenous drip, intrathecal, or
ophthalmic use.
 In the medical literature, dosages have frequently been given in terms of equivalent
weights of pure polymyxin B (polymyxin b sulfate) base.Each milligram of pure
polymyxin B (polymyxin b sulfate) base is equivalent to 10,000 units of polymyxin B
(polymyxin b sulfate) and each microgram of pure polymyxin B (polymyxin b sulfate)
base is equivalent to 10 units of polymyxin B.
 Aqueous solutions of polymyxin B (polymyxin b sulfate) sulfate may be stored up to 12
months without significant loss of potency if kept under refrigeration.In the interest of
safety, solutions for parenteral use should be stored under refrigeration and any unused
portion should be discarded after 72 hours. Polymyxin B (polymyxin b sulfate) sulfate
should not be stored in alkaline solutions since they are less stable.
 Indications & Dosage

 INDICATIONS

 Acute Infections Caused by Susceptible Strains of Pseudomonas aeruginosa.


 Polymyxin B (polymyxin b sulfate) sulfate is a drug of choice in the treatment of
infections of the urinary tract, meninges, and bloodstream caused by susceptible strains
of Ps. aeruginosa. It may also be used topically and subconjunctivally in the treatment of
infections of the eye caused by susceptible strains of Ps. aeruginosa.
 It may be indicated in serious infections caused by susceptible strains of the following
organisms, when less potentially toxic drugs are ineffective or contraindicated: H
influenzae, specifically meningeal infections. Escherichia coli, specifically urinary tract
infections. Aerobacter aerogenes, specifically bacteremia. Klebsiella
pneumoniae, specifically bacteremia.
 NOTE: IN MENINGEAL INFECTIONS, POLYMYX-IN B SULFATE SHOULD BE
ADMINISTERED ONLY BY THE INTRATHECAL ROUTE.
 To reduce the development of drug-resistant bacteria and maintain the effectiveness of
polymyxin B (polymyxin b sulfate) and other antibacterial drugs, polymyxin B
(polymyxin b sulfate) should be used only to treat or prevent infections that are proven or
strongly suspected to be caused by susceptible bacteria.When culture and susceptibility
information are available, they should be considered in selecting or modifying
antibacterial therapy.In the absence of such data, local epidemiology and susceptibility
patterns may contribute to the empiric selection of therapy.
 DOSAGE AND ADMINISTRATION

 Parenteral:
 Intravenous: Dissolve 500,000 polymyxin B (polymyxin b sulfate) units in 300 to 500
mL solutions for parenteral dextrose injection 5% for continuous drip.
 Adults and children: 15,000 to 25,000 units/kg body weight/day in individuals with
normal kidney function.This amount should be reduced from 15,000 units/kg downward
for individuals with kidney impairment. Infusions may be given every 12 hours; however,
the total daily dose must not exceed 25,000 units/kg/day.
 Infants: Infants with normal kidney function may receive up to 40,000 units/kg/day
without adverse effects.
 Intramuscular: Not recommended routinely because of severe pain at injection sites,
particularly in infants and children. Dissolve 500,000 polymyxin B units in 2 mL sterile
water for injection or sodium chloride injection or procaine hydrochloride injection 1%.
 Adults and children: 25,000 to 30,000 units/kg/day.This should be reduced in the
presence of renal impairment.The dosage may be divided and given at either 4 or 6 hour
intervals.
 Infants: Infants with normal kidney function may receive up to 40,000 units/kg/day
without adverse effects.
 Note: Doses as high as 45,000 units/kg/day have been used in limited clinical studies in
treating prematures and newborn infants for sepsis caused by Ps aeruginosa.
 Intrathecal: A treatment of choice for Ps aeruginosameningitis. Dissolve 500,000
polymyxin B (polymyxin b sulfate) units in 10 mL sodium chloride injection USP for
50,000 units per mL dosage unit.
 Adults and children over 2 years of age: Dosage is 50,000 units once daily intrathecally
for 3 to 4 days, then 50,000 units once every other day for at least 2 weeks after cultures
of the cerebrospinal fluid are negative and sugar content has returned to normal.
 Children under 2 years of age: 20,000 units once daily, intrathecally for 3 to 4 days or
25,000 units once every other day. Continue with a dose of 25,000 units once every other
day for at least 2 weeks after cultures of the cerebrospinal fluid are negative and sugar
content has returned to normal.
 IN THE INTEREST OF SAFETY, SOLUTIONS OF PARENTERAL USE SHOULD
BE STORED UNDER REFRIGERATION, AND ANY UNUSED PORTIONS
SHOULD BE DISCARDED AFTER 72 HOURS.
 Topical:

 Ophthalmic: Dissolve 500,000 polymyxin B (polymyxin b sulfate) units in 20 to 50 mL


sterile water for injection or sodium chloride injection USP for a 10,000 to 25,000 units
per mL concentration.
 For the treatment of Ps aeruginosa infections of the eye, a concentration of 0.1 percent to
0.25 percent (10,000 units to 25,000 units per mL) is administered 1 to 3 drops every
hour, increasing the intervals as response indicates.
 Subconjunctival injection of up to 100,000 units/day may be used for the treatment of Ps
aeruginosainfections of the cornea and conjunctiva.
 Note: Avoid total systemic and ophthalmic instillation over 25,000 units/kg/day.
 HOW SUPPLIED

 Polymyxin B for Injection (polymyxin b (polymyxin b sulfate) sulfate) , 500,000


polymyxin B (polymyxin b sulfate) units per vial is supplied in rubber-stoppered glass
vial with flip off cap, carton of 10, NDC 55390-139-10.
 Storage recommendations

 Before reconstitution: Store at controlled room temperature 15° to 30°C (59° to 86°F).
 Protect from light. Retain in carton until time of use.
 After reconstitution: Product must be stored under refrigeration, between 2° to 8°C (36°
to 46°F) and any unused portion should be discarded after 72 hours.

 Manufactured for: Bedford Laboratories™, Bedford, OH 44146. Manufactured by: Ben


Venue Laboratories, Inc., Bedford, OH 44146. February 2004. FDA Rev date: 5/15/2002
 Side Effects & Drug Interactions

 SIDE EFFECTS

 See WARNING box.


 Nephrotoxic reactions: Albuminuria, cylin-duria, azotemia, and rising blood levels
without any increase in dosage.
 Neurotoxic reactions: Facial flushing, dizziness progressing to ataxia, drowsiness,
peripheral paresthesias (circumoral and stocking glove), apnea due to concurrent use of
curariform muscle relaxants, other neurotoxic drugs or inadvertent overdosage, and signs
of meningeal irritation with intrathecal administration, e.g., fever, headache, stiff neck
and increased cell count and protein cerebrospinal fluid.
 Other reactions occasionally reported: Drug fever, urticarial rash, pain (severe) at
intramuscular injection sites, and thrombophlebitis at intravenous injection sites.
 DRUG INTERACTIONS

 No information provided.
 Warnings & Precautions

 WARNINGS

 No information provided.
 PRECAUTIONS

 General. Prescribing polymyxin B (polymyxin b sulfate) in the absence of a proven or


strongly suspected bacterial infection or a prophylactic indication is unlikely to provide
benefit to the patient and increases the risk of the development of drug-resistant bacteria.
 See WARNING box.
 Baseline renal function should be done prior to therapy, with frequent monitoring of renal
function and blood levels of the drug during parenteral therapy.
 Avoid concurrent use of a curariform muscle relaxant and other neurotoxic drugs (ether,
tubocurarine, succinylcholine, gallamine, decamethonium and sodium citrate) which may
precipitate respiratory depression. If signs of
respiratory paralysis appear, respiration should be assisted as required, and the drug
discontinued.
 As with other antibiotics, use of this drug may result in overgrowth of nonsusceptible
organisms, including fungi.
 If superinfection occurs, appropriate therapy should be instituted.
 Overdosage & Contraindications

 OVERDOSE

 No information provided.
 CONTRAINDICATIONS

 This drug is contraindicated in persons with a prior history of hypersensitivity reactions


to polymyxins.
 Clinical Pharmacology

 CLINICAL PHARMACOLOGY

 Polymyxin B (polymyxin b sulfate) sulfate has a bactericidal action against almost


all gram-negative bacilli except the Proteus group. Polymyxins increase the permeability
of bacterial cell wall membranes. All gram-positive bacteria, fungi, and the gram-
negative cocci, N gonorrhoeae and N meningitidis, are resistant.
 Susceptibility plate testing: If the Kirby-Bauer method of disc susceptibility testing is
used, a 300-unit polymyxin B (polymyxin b sulfate) disc should give a zone of over 11
mm when tested against a polymyxin B susceptible bacterial strain.
 Polymyxin B (polymyxin b sulfate) sulfate is not absorbed from the
normal alimentary tract.Since the drug loses 50 percent of its activity in the presence of
serum, active blood levels are low. Repeated injections may give a cumulative effect.
Levels tend to be higher in infants and children.The drug is excreted slowly by the
kidneys.Tissue diffusion is poor and the drug does not pass the blood brain barrier into
thecerebrospinal fluid. In therapeutic dosage, polymyxin B (polymyxin b sulfate) sulfate
causes some nephrotoxicity with tubule damage to a slight degree.
Polymyxin B (polymyxin b sulfate) is an antibiotic used to treat bacterial
infections such as urinary tractinfections, meningitis, blood infections, and eye
infections. Polymyxin B is available in generic form. Common side effects of
Polymyxin B include:

 pain,
 redness, and
 swelling at the injection site, or
 temporary eye stinging/burning/redness/itchiness or
 temporary blurred vision if used as eye drops.

Contact your doctor if you experience serious side effects of Polymyxin B


including:

 flushing,
 dizziness,
 loss of coordination,
 drowsiness,
 fever,
 headache,
 numbness or tingling in the hands or feet,
 back pain,
 stiff neck,
 unsteadiness,
 hives, and
 rash.

Polymyxin B dose is determined by a doctor, based on the condition being


treated. It may be injected into a vein, muscle, or the spinal fluid or into the
area around the eye (subconjunctival sac). It can also be prepared as eye
drops. Polymyxin B may interact with other drugs that can harm the kidneys or
nerves (e.g., cisplatin, colistin, high-dose aspirin, aminoglycosides such as
amikacin, gentamicin, tobramycin, nonsteroidal anti-inflammatory drugs-
NSAIDs such as ibuprofen or naproxen). Tell your doctor all medications you
are taking. During pregnancy, Polymyxin B should be used only when
prescribed. It is unknown if this medication passes into breast milk when used
in the eye. It is unlikely to harm a nursing infant. Consult your doctor before
breastfeeding.

Colistin, also known as polymyxin E, is an antibiotic produced by certain strains of the


bacteria Paenibacillus polymyxa. Colistin is a mixture of the cyclic polypeptides colistin A
and B and belongs to the class of polypeptide antibiotics known as polymyxins. Colistin is
effective against most Gram-negative bacilli.
Colistin is a decades-old drug that fell out of favor in human medicine due to its kidney
toxicity. It remains one of the last-resort antibiotics for multidrug-resistant Pseudomonas
aeruginosa, Klebsiella pneumoniae, and Acinetobacter.[1] NDM-1 metallo-β-lactamase
multidrug-resistant Enterobacteriaceae have also shown susceptibility to colistin.[2]
Resistance to colistin in human pathogens is rare. The first colistin-resistance gene in
a plasmid which can be transferred between bacterial strains was found in 2011 in China
and became publicly known in November 2015. The presence of this plasmid-borne mcr

History[edit]
Colistin was first isolated in Japan in 1949 from a flask of
fermenting Bacillus polymyxa var. colistinus by the Japanese scientist Koyama[3] and
became available for clinical use in 1959.[4]
Colistimethate sodium, a less toxic prodrug, became available for injection in 1959. In the
1980s, polymyxin use was widely discontinued because of nephro- and neurotoxicity. As
multi-drug resistant bacteria became more prevalent in the 1990s, colistin started to get a
second look as an emergency solution, in spite of toxic effects.[5]

Administration and dosage[edit]


Forms[edit]
Two forms of colistin are available commercially: colistin sulfate and colistimethate
sodium (colistin methanesulfonate sodium, colistin sulfomethate sodium). Colistin sulfate
is cationic; colistimethate sodium is anionic. Colistin sulfate is stable, but colistimethate
sodium is readily hydrolysed to a variety of methanesulfonated derivatives. Colistin sulfate
and colistimethate sodium are eliminated from the body by different routes. With respect
to Pseudomonas aeruginosa, colistimethate is the inactive prodrug of colistin. The two
drugs are not interchangeable .

 Colistimethate sodium may be used to treat Pseudomonas aeruginosa infections


in cystic fibrosis patients, and it has come into recent use for treating multidrug-
resistant Acinetobacter infection, although resistant forms have been reported.[6]
[7]
Colistimethate sodium has also been given intrathecally and intraventricularly
in Acinetobacter baumannii and Pseudomonas aeruginosa meningitis/ventriculitis[8][9][10]
[11]
Some studies have indicated that colistin may be useful for treating infections caused
by carbapenem-resistant isolates of Acinetobacter baumannii.[7]
 Colistin sulfate may be used to treat intestinal infections, or to suppress colonic flora.
Colistin sulfate is also used as topical creams, powders, and otic solutions.
 Colistin A (polymyxin E1) and colistin B (polymyxin E2) can be purified individually to
research and study their effects and potencies as separate compounds.
Dosage[edit]
Colistin sulfate and colistimethate sodium may both be given intravenously, but the dosing
is complicated. The very different labeling of the parenteral products of colistin
methanesulfonate in different parts of the world was first revealed by Li et al.
[12]
Colistimethate sodium manufactured by Xellia (Colomycin injection) is prescribed in
international units, but colistimethate sodium manufactured by Parkdale
Pharmaceuticals (Coly-Mycin M Parenteral) is prescribed in milligrams of colistin base:

 Colomycin 1,000,000 units is 80 mg colistimethate;[13]


 Coly-mycin M 150 mg "colistin base" is 360 mg colistimethate or 4,500,000 units.[14]
Because colistin was introduced into clinical practice over 50 years ago, it was never
subject to the regulations that modern drugs are subject to, and therefore there is no
standardised dosing of colistin and no detailed trials on pharmacology or pharmacokinetics:
The optimal dosing of colistin for most infections is therefore unknown. Colomycin has a
recommended intravenous dose of 1 to 2 million units three times daily for patients weighing
60 kg or more with normal renal function. Coly-Mycin has a recommended dose of 2.5 to
5 mg/kg colistin base a day, which is equivalent to 6 to 12 mg/kg colistimethate sodium per
day. For a 60 kg man, therefore, the recommended dose for Colomycin is 240 to 480 mg of
colistimethate sodium, yet the recommended dose for Coly-Mycin is 360 to 720 mg of
colistimethate sodium. Likewise, the recommended "maximum" dose for each preparation is
different (480 mg for Colomycin and 720 mg for Coly-Mycin). Each country has different
generic preparations of colistin, and the recommended dose depends on the manufacturer.
This complete absence of any regulation or standardisation of dose makes intravenous
colistin dosing difficult for any physician.[citation needed]
Colistin has been used in combination with rifampicin, and evidence of in-vitro synergy
exists,[15][16] and the combination has been used successfully in patients.[17] There is also in-
vitro evidence of synergy for colistimethate sodium used in combination with other
antipseudomonal antibiotics.[18]
Colistimethate sodium aerosol (Promixin; Colomycin Injection) is used to treat pulmonary
infections, especially in cystic fibrosis. In the UK, the recommended adult dose is 1–2
million units (80–160 mg) nebulised colistimethate twice daily.[19][13] Nebulized colistin has
also been used to decrease severe exacerbations in patients with chronic obstructive
pulmonary disease and infection with Pseudomonas aeruginosa.[20]

Mechanism of action[edit]
Colistin is a polycationic peptide and has both hydrophilic and lipophilic moieties.[citation
needed]
These cationic regions interact with the bacterial outer membrane, by displacing
magnesium and calcium bacterial counter ions in the lipopolysaccharide.[citation
needed]
Hydrophobic/hydrophilic regions interact with the cytoplasmic membrane just like a
detergent, solubilizing the membrane in an aqueous environment.[citation needed] This effect is
bactericidal even in an isosmolar environment.[citation needed]

Antibacterial spectrum[edit]
Colistin has been effective in treating infections caused by Pseudomonas, Escherichia,
and Klebsiella species. The following represents MIC susceptibility data for a few medically
significant microorganisms:[21][22]

 Escherichia coli: 0.12–128 μg/ml


 Klebsiella pneumoniae: 0.25–128 μg/ml
 Pseudomonas aeruginosa: ≤0.06–16 μg/ml
For example, colistin in combination with other drugs are used to attack P.
aeruginosa biofilm infection in lungs of CF patients.[23] Biofilms have a low oxygen
environment below the surface where bacteria are metabolically inactive and colistin is
highly effective in this environment. However, P. aeruginosa reside in the top layers of the
biofilm, where they remain metabolically active.[24] This is because surviving tolerant cells
migrate to the top of the biofilm via pili motility and form new aggregates via quorum
sensing.[25]

Resistance[edit]
Resistance to colistin is rare, but has been described. As of 2017, no agreement exists
about how to look for colistin resistance. The Société Française de Microbiologie (fr) uses a
cut-off of 2 mg/l, whereas the British Society for Antimicrobial Chemotherapy sets a cutoff of
4 mg/l or less as sensitive, and 8 mg/ml or more as resistant. No standards for measuring
colistin sensitivity are given in the US.
The plasmid-borne mcr-1 gene has been found to confer resistance to colistin.[26] The first
colistin-resistance gene in a plasmid which can be transferred between bacterial strains was
found in 2011 and became publicly known in November 2015.[26][27] This plasmid-borne mcr-
1 gene has since been isolated in China,[26] Europe[28] and the United States.[29]
India reported the first detailed colistin-resistance study which mapped 13 colistin-resistant
cases recorded over 18 months. It concluded that pan-drug resistant infections, particularly
those in the blood stream, have a higher mortality. Multiple other cases were reported from
other Indian hospitals.[30][31] Although resistance to polymyxins is generally[where?] less than
10%,[specify] it is more frequent in the Mediterranean and South-East Asia (Korea and
Singapore), where colistin resistance rates are continually increasing.[32] Colistin-resistant E.
coli was identified in the United States in May 2016.[33]
Use of colistin to treat Acinetobacter baumannii infections has led to the development of
resistant bacterial strains. which have also developed resistance to antimicrobial
compounds LL-37 and lysozyme, produced by the human immune system.[34]
Inherently resistant[edit]

 Brucella
 Burkholderia cepacia
 Chryseobacterium indologenes
 Edwardsiella
 Elizabethkingia meningoseptica
 Francisella tularensis spp.
 Gram-negative cocci
 Helicobacter pylori
 Moraxella catarrhalis
 Morganella spp.
 Neisseria gonorrheae and Neisseria meningitidis
 Proteus
 Providencia
 Serratia

 Some strains of Stenotrophomonas maltophilia[35]


Variable resistance[edit]

 Aeromonas
 Vibrio
 Prevotella
 Fusobacterium
 Escherichia coli

Pharmacokinetics[edit]
No clinically useful absorption of colistin occurs in the gastrointestinal tract. For systemic
infection, colistin must, therefore, be given by injection. Colistimethate is eliminated by the
kidneys, but colistin is supposed to be eliminated by non-renal mechanism(s) that are as of
yet not characterised.[36][37]

Adverse reactions[edit]
The main toxicities described with intravenous treatment are nephrotoxicity (damage to the
kidneys) and neurotoxicity (damage to the nerves),[38][39][40][41] but this may reflect the very high
doses given, which are much higher than the doses currently recommended by any
manufacturer and for which no adjustment was made for renal disease. Neuro- and
nephrotoxic effects appear to be transient and subside on discontinuation of therapy or
reduction in dose.[42]
At a dose of 160 mg colistimethate IV every eight hours, very little nephrotoxicity is seen.[43]
[44]
Indeed, colistin appears to have less toxicity than the aminoglycosides that subsequently
replaced it, and it has been used for extended periods up to six months with no ill effects.[45]
The main toxicity described with aerosolised treatment is bronchospasm,[46] which can be
treated or prevented with the use of beta2-agonists such as salbutamol[47] or following a
desensitisation protocol.[48]

Biosynthesis[edit]
The biosynthesis of colistin requires the use of three amino acids threonine, leucine, and
2,4-diaminobutryic acid. It is important to synthesis the linear form of colistin before
cycliziation. Elongation of non ribosomal peptide biosynthesis begins by a loading module
and then the addition of each subsequent amino acid. The subsequent amino acids are
added with the help of an adenylation domain (A), a peptidyl carrier protein domain (PCP),
an epimerization domain (E), and a condensation domain (C). Cyclization is accomplished
by utilizing a thioesterase.[49] The first step is to have a loading domain, 6-methyl-heptanoic
acid, associate with the A and PCP domains. Now with a C, A, and PCP domain that is
associated with 2,4-diaminobutryic acid. This continues with each amino acid until the linear
peptide chain is completed. The last module will have a thioesterase to complete the
cyclization and form the product colistin.

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