HIV Drugs

The FDA has approved more than 25 antiretroviral drugs to treat HIV infection. They can help in these
ways:

Lower your viral load

Fight infections
Improve your quality of life
Even when these HIV medications are effective, however, you can still transmit HIV to others. They
are not a cure for HIV.
The HIV drug Truvada, however, has been approved for use in those at high risk as a way to prevent
HIV infection. It's to be
used in conjunction with safe sex practices.
A group of HIV specialists has developed guidelines for the use of these HIV medications. The
current goals are to:

Control the growth of the virus

Improve overall immune system function and status
Suppress symptoms
Produce as few side effects as possible
To do this, doctors recommend that you take a combination of HIV drugs from at least two of the main
classes. This combination is called highly active antiretroviral therapy (HAART). It helps combat new
resistant strains of the virus that emerge as HIV makes copies of itself. HAART also decreases the
rate of opportunistic infections.
If you are HIV-positive, you should begin HAART:

If you have symptoms of HIV

If your CD4 cell count falls below 350-500 or if you are newly infected, whether or not you have
symptoms. CD4 cells -- also called T cells -- are a type of immune system cell.
These are five classes of HIV drugs.
1. Reverse transcriptase (RT) inhibitors help block an important step in the HIV life cycle. There
are two types of RT inhibitors.
Nucleoside/nucleotide reverse transcriptase inhibitors (NRTIs) stall reproduction of HIV. They
force the virus to use faulty versions of building blocks.
The FDA has approved these NRTIs:
Brand Name
Combivir
Emtriva

Generic Name
zidovudine + lamivudine
emtricitabine

Abbreviation
AZT + 3TC
FTC

Epivir
Epzicom
Hivid
Retrovir
Stribild

Viread

lamivudine
Abacavir + lamivudine
zalcitabine
zidovudine
tenofovir + emtricitabine +
elvitegravir
abacavir + zidovudine + lamivudine
tenofovir DF + emtricitabine
didanosine: buffered versions
didanosine: delayed-release
capsules
tenofovir disoproxil fumarate (DF)

Zerit
Ziagen

stavudine
abacavir

Trizivir
Truvada
Videx
Videx EC

WebMD Home

Sexual Health Center

3TC
ABC + 3TC
ddC
AZT or ZDV
TDF + FTC + EVG
ABC + AZT + 3TC
TDF + FTC
ddl
ddl
TDF or Bis (POC)
PMPA
d4T
ABC

HIV & AIDS Health Center

HIV & AIDS Guide

Email a Friend
Print Article

HIV & AIDS Health Center

Tools & Resources

Top Myths About HIV & AIDS

HIV and Your Sex Life

HIV: Is a Cure in Reach?

HIV Diagnosis and Treatment

Advances in HIV Treatment

HIV and Pregnancy

Share this:
Listen

Expanding HIV and AIDS Drug Options

(continued)

In this article

HIV Drugs

How to Take HIV Drugs

AIDS and HIV Drugs for Opportunistic Infections and Other HIV-Related Problems

Other AIDS and HIV Drugs in Development

HIV Drugs continued...

Non-nucleoside RT inhibitors (NNRTIs) bind to the RT protein. This disables it, keeping HIV from
making copies of itself.
The FDA has approved these NNRTIs:
Efavirenz (Sustiva)
Nevirapine (Viramune)
Delavirdine (Rescriptor)
Etravirine (Intelence)
Edurant (rilpivirine)
The FDA also approved two one-pill, once-a-day products to treat HIV.Atripla combines three different
RT inhibitors (efavirenz + tenovir DF + emtricitabine). And Complera is a combination
of Truvada (which combines the nucleoside reverse transcriptase inhibitors Emtriva andViread) and
the non-nucleoside reverse transcriptase inhibitor Edurant.
2. Protease inhibitors (PI) interfere with an enzyme that HIV uses to create infectious viral particles.
The FDA has approved these protease inhibitors:
Brand Name

Generic Name

Abbreviation

Agenerase

amprenavir

APV

Aptivus

tipranavir

TPV

Crixivan

indinavir

IDV

Invirase

saquinavir

SQV

Kaletra

lopinavir + ritonavir

LPV

Lexiva

fosamprenavir

FPV

Norvir

ritonavir

RTV

Prezista

darunavir

DRV

Reyataz

atazanavir

ATZ

Viracept

nelfinavir

NFV

Taking Invirase with Norvir has been linked to a potentially seriousdrug interaction causing an
abnormal heart rhythm. Your doctor may recommend heart monitoring. Also, the FDA says that taking
thehepatitis C drug Victrelis (boceprevir) and ritonavir (when also taking atazanavir, lopinavir, or

darunavir) can potentially reduce the effectiveness of these drugs. Tybost (cobicistat) is a drug that
helps protease inhibitors work better.
3. Fusion inhibitors help block HIV's entry into healthy cells. At this time, Fuzeon (enfuvirtide), ENF,
is the only one the FDA has approved.
4. Entry Inhibitors also help block HIV's entry into healthy cells. Currently, maraviroc (Selzentry) is
the only FDA-approved drug, but others are in late stage clinical trials.
5. Integrase inhibitors block insertion of viral DNA into the host cell DNA.
Currently, Isentress (raltegravir), Vitekta (elvitegravir), and Tivicay (dolutegravir) are the only FDAapproved drugs, but others are in clinical trials. Dolutegravir is part of a combination pill called
Triumeg, which also includes abacavir and lamivudine.

How to Take HIV Drugs

There are many types of HIV drugs. Your doctor will provide you with specific directions for the
medications you take. However, remember these important points:

Take all your HIV medication exactly as directed. Never even miss one dose. If you don't take them as
directed, you may develop resistant strains of HIV, and your medication may stop working.

Check with your pharmacist or doctor about whether or not you should take your medications on an
empty stomach. Taking them the right way can reduce side effects.

Tell your pharmacist or doctor about any dietary supplements or other medications you take. Some can
interact with your HIV medications.

WebMD Home

Sexual Health Center

HIV & AIDS Health Center

HIV & AIDS Guide

Email a Friend

Expanding HIV and AIDS Drug Options

(continued)

In this article

HIV Drugs

How to Take HIV Drugs

AIDS and HIV Drugs for Opportunistic Infections and Other HIV-Related Problems

Other AIDS and HIV Drugs in Development

HIV Drugs continued...

Non-nucleoside RT inhibitors (NNRTIs) bind to the RT protein. This disables it, keeping HIV from
making copies of itself.
The FDA has approved these NNRTIs:
Efavirenz (Sustiva)
Nevirapine (Viramune)
Delavirdine (Rescriptor)
Etravirine (Intelence)
Edurant (rilpivirine)
The FDA also approved two one-pill, once-a-day products to treat HIV.Atripla combines three different
RT inhibitors (efavirenz + tenovir DF + emtricitabine). And Complera is a combination
of Truvada (which combines the nucleoside reverse transcriptase inhibitors Emtriva andViread) and
the non-nucleoside reverse transcriptase inhibitor Edurant.
2. Protease inhibitors (PI) interfere with an enzyme that HIV uses to create infectious viral particles.
The FDA has approved these protease inhibitors:
Brand Name

Generic Name

Abbreviation

Agenerase

amprenavir

APV

Aptivus

tipranavir

TPV

Crixivan

indinavir

IDV

Invirase

saquinavir

SQV

Kaletra

lopinavir + ritonavir

LPV

Lexiva

fosamprenavir

FPV

Norvir

ritonavir

RTV

Prezista

darunavir

DRV

Reyataz

atazanavir

ATZ

Viracept

nelfinavir

NFV

Taking Invirase with Norvir has been linked to a potentially seriousdrug interaction causing an
abnormal heart rhythm. Your doctor may recommend heart monitoring. Also, the FDA says that taking
thehepatitis C drug Victrelis (boceprevir) and ritonavir (when also taking atazanavir, lopinavir, or
darunavir) can potentially reduce the effectiveness of these drugs. Tybost (cobicistat) is a drug that
helps protease inhibitors work better.

3. Fusion inhibitors help block HIV's entry into healthy cells. At this time, Fuzeon (enfuvirtide), ENF,
is the only one the FDA has approved.
4. Entry Inhibitors also help block HIV's entry into healthy cells. Currently, maraviroc (Selzentry) is
the only FDA-approved drug, but others are in late stage clinical trials.
5. Integrase inhibitors block insertion of viral DNA into the host cell DNA.
Currently, Isentress (raltegravir), Vitekta (elvitegravir), and Tivicay (dolutegravir) are the only FDAapproved drugs, but others are in clinical trials. Dolutegravir is part of a combination pill called
Triumeg, which also includes abacavir and lamivudine.

How to Take HIV Drugs

There are many types of HIV drugs. Your doctor will provide you with specific directions for the
medications you take. However, remember these important points:

Take all your HIV medication exactly as directed. Never even miss one dose. If you don't take them as
directed, you may develop resistant strains of HIV, and your medication may stop working.

Check with your pharmacist or doctor about whether or not you should take your medications on an
empty stomach. Taking them the right way can reduce side effects.

Tell your pharmacist or doctor about any dietary supplements or other medications you take. Some can
interact with your HIV medications.

Multi-class Combination Products

Approval
Date

Time to
Approval

Brand

Generic Name

Atripla

efavirenz, emtricitabine and tenofovir disoproxil

fumarate

12-July-06

Comple
ra

emtricitabine, rilpivirine, and tenofovir disoproxil

fumarate

10-August11

6 months

elvitegravir, cobicistat, emtricitabine, tenofovir

disoproxil fumarate

27-August12

6 months

Stribild

2.5 months

Nonnucleoside Reverse Transcriptase Inhibitors (NNRTIs);

Brand
Name

Generic Name

Approval
Date

Time to
Approval

Combivir

lamivudine and zidovudine

27-Sep-97

3.9 months

Emtriva

emtricitabine, FTC

02-Jul-03

10 months

Epivir

lamivudine, 3TC

17-Nov-95

4.4 months

Epzicom

abacavir and lamivudine

02-Aug-04

10 months

19-Jun-92

7.6 months

Hivid

zalcitabine, dideoxycytidine, ddC (no longer

marketed)

Retrovir

zidovudine, azidothymidine, AZT, ZDV

19-Mar-87

3.5 months

Trizivir

abacavir, zidovudine, and lamivudine

14-Nov-00

10.9 months

Truvada

tenofovir disoproxil fumarate and emtricitabine

02-Aug-04

5 months

Videx EC

enteric coated didanosine, ddI EC

31-Oct-00

9 months

Videx

didanosine, dideoxyinosine, ddI

9-Oct-91

6 months

Viread

tenofovir disoproxil fumarate, TDF

26-Oct-01

5.9 months

Zerit

stavudine, d4T

24-Jun-94

5.9 months

Ziagen

abacavir sulfate, ABC

17-Dec-98

5.8 months

Brand Name

Generic Name

Approval Date

Time to Approval

Edurant

rilpivirine

20-May-11

10 months

Intelence

etravirine

18-Jan-08

6 months

Rescriptor

delavirdine, DLV

4-Apr-97

8.7 months

Sustiva

efavirenz, EFV

17-Sep-98

3.2 months

Viramune(Immediate Release)

nevirapine, NVP

21-Jun-96

3.9 months

Viramune XR

nevirapine, NVP

25-Mar-11

9.9 months

(Extended Release)

Protease Inhibitors (PIs)

Brand Name

Generic Name

Agenerase

amprenavir, APV (no longer marketed)

Aptivus

tipranavir, TPV

Approval Date

Time to Approval

15-Apr-99

6 months

22-Jun-05

6 months

Crixivan

indinavir, IDV,

13-Mar-96

1.4 months

Fortovase

saquinavir (no longer marketed)

7-Nov-97

5.9 months

Invirase

saquinavir mesylate, SQV

6-Dec-95

3.2 months

15-Sep-00

3.5 months

Kaletra

lopinavir and ritonavir, LPV/RTV

Lexiva

Fosamprenavir Calcium, FOS-APV

20-Oct-03

10 months

Norvir

ritonavir, RTV

1-Mar-96

2.3 months

Prezista

darunavir

23-Jun-06

6 months

Reyataz

atazanavir sulfate, ATV

20-Jun-03

6 months

Viracept

nelfinavir mesylate, NFV

14-Mar-97

2.6 months

Fusion Inhibitors
Brand Name

Fuzeon

Generic Name

enfuvirtide, T-20

Approval Date

Time to Approval

13-Mar-03

6 months

Entry Inhibitors - CCR5 co-receptor antagonist

Brand Name

Selzentry

Generic Name

maraviroc

Approval Date

06-August-07

Time to Approval

8 months

HIV integrase strand transfer inhibitors

Brand Name

Generic Name

Approval Date

Time to Approval

Isentress

raltegravir

12--Oct-07

6 months

Tivicay

dolutegravir

13-August-13

6 months

Antiviral drugs are a class of medication used specifically for treating viral infections.[1] Like antibiotics for bacteria,
specific antivirals are used for specific viruses. Unlike most antibiotics, antiviral drugs do not destroy their
target pathogen; instead they inhibit their development.
Antiviral drugs are one class of antimicrobials, a larger group which also includes antibiotic (also termed
antibacterial), antifungal and antiparasitic drugs,[2] or antiviral drugs based on monoclonal antibodies.[3] Most
antivirals are considered relatively harmless to the host, and therefore can be used to treat infections. They should
be distinguished fromviricides, which are not medication but deactivate or destroy virus particles, either inside or
outside the body. Antivirals also can be found in essential oils of some herbs, such aseucalyptus oil and its
constituents.[4]

Immunosuppressant drugs are a class of drugs that suppress or reduce the

strength of the bodys immune system. They are also called anti-rejection drugs.
One of the primary uses of immunosuppressant drugs is to lower the bodys
ability to reject a transplanted organ, such as a liver, heart or kidney.

(http://www.hopkinslupus.org/lupus-treatment/lupusmedications/immunosuppressive-medications/)

What Do the Drugs

Treat?
Almost everyone who receives an organ transplant has to take
immunosuppressant drugs. The body recognizes a transplanted organ
as a foreign mass. This triggers a response by the bodys immune
system to attack it.
By weakening the immune system, immunosuppressant drugs
decrease the bodys reaction to the foreign organ. The drugs allow the
transplanted organ to remain healthy and free from damage.
Immunosuppressant drugs also are used to treat autoimmune diseases
such as lupus. An autoimmune disorder is a disease process in which
the body attacks its own tissue. Lupus results from just such a
misdirected activity of the bodys own immune system. By suppressing
this reaction, immunosuppressant drugs can help control the impact of
the disease on the body.
Other diseases treated with immunosuppressant drugs include:

psoriasis
rheumatoid arthritis
Crohns disease, a chronic inflammation of the digestive tract
multiple sclerosis
alopecia areata (patchy hair loss)

Part 3 of 6: Categories

What Drugs Are Used?

Immunosuppressant drugs can be classified into four categories:

azathioprine (Imuran)
cyclosporine (Neoral, Sandimmune, SangCya)
monoclonal antibodies, which include: basiliximab (Simulect),
daclizumab (Zenapax), and muromonab (Orthoclone OKT 3)

corticosteroids such as prednisone (Deltasone, Orasone)

Most patients are prescribed drugs from more than one category.

Part 4 of 6: Procedure

How Are the Drugs

Administered?
All immunosuppressant drugs are only available with a prescription
from a physician. They can be administered as tablets, capsules,
liquids, and injections. A physician determines the best course of
treatment using a combination of drugs. The goal of
immunosuppressant therapy is to find the course that will prevent
rejection and have the least harmful side effects.
A person taking immunosuppressant drugs must take them exactly as
prescribed every day. Even the slightest change from the medication
regimen can trigger an organ rejection. After missing a dose, its
important to contact a physician immediately.
The immunosuppressant drugs in a patients regimen are adjusted and
may eventually be reduced. As the risk of organ rejection lessens over
time, the need for these medications may decrease. However, most

people who have had a transplant will have to take at least one
immunosuppressant drug for their lifetime.
Regular blood tests are used to monitor the effectiveness of the drugs
and the need for adjustments.

Part 5 of 6: Risk Factors

What Are the Risks?

When immunosuppressant drugs weaken the immune system, the
body becomes less resistant to infection. Any infections that develop
will be more difficult to treat because of this. These drugs also increase
the likelihood of uncontrolled bleeding due to injury or infection.
People taking immunosuppressant drugs should be careful to avoid
catching an infection. Precautions include:

frequent hand washing

avoiding sports in which injuries occur
extra care when using sharp objects such as knives or razors
avoiding close contact with people who have infections or colds
A physician should be notified immediately when the following
symptoms occur:

fever or chills
pain in the lower back, on the sides
pain or difficulty urinating
unusual bruising or bleeding
blood in your urine
stools that are bloody or black

Immunosuppressant drugs can cause adverse reactions and birth

defects. Physicians should be made aware of the following conditions
before immunosuppressant drugs are prescribed:

allergies
pregnancy
lactation
shingles or chickenpox
kidney or liver disease
intestinal problems

Part 6 of 6: Side Effects

What Are the Side

Effects?
The most significant side effect of immunosuppressant drugs is an
increased risk of infection. The drugs can also put you at a higher risk
for cancer because the immune system also protects you from this
disease.
Other, less serious side effects can include loss of appetite, nausea,
vomiting, increased hair growth, and hand trembling. These effects
typically subside as the body adjusts to the immunosuppressant drugs.
The following side effects indicate the need for immediate attention:

a feeling of being unusually tired or weak

fever or chills
frequent urination
Immunosuppressant drugs can interact with many other medications.
This can cause dangerous effects in which the immunosuppressants

may lose or even increase their effect. The primary caregiver should be
made aware of any prescription or over-the-counter medications their
patients are taking while on immunosuppressant therapy.

Calcineurin inhibitors
Calcineurin catalyses some of the intracellular processes associated with the activation of T-lymphocytes. When
calcineurin inhibitors bind to intracellular proteins called immunophilins, they block the effect of calcineurin. This results in
reduced production of interleukin-2 and reduced proliferation of T-cells.
The nephrotoxicity of calcineurin inhibitors has emerged as an increasing cause of late renal allograft loss. The
pathogenesis appears to be multifactorial and includes calcineurin-induced vasoconstriction, calcineurin-induced release
of endothelin-1 (a potent vasoconstrictor), decreased production of the vasodilator nitric oxide, and increased expression
of transforming growth factor beta1 (a key cytokine associated with interstitial fibrosis).3Reducing the dose of calcineurin
inhibitor, or using protocols including mycophenolate and sirolimus, may minimise the risk of nephrotoxicity and improve
allograft and patient survival.

Gengraf
generic name: cyclosporine

Hecoria

generic name: tacrolimus

Neoral

generic name: cyclosporine

Prograf

generic name: tacrolimus

Astagraf XL

generic name: tacrolimus

Sandimmune
generic name: cyclosporine

What are cytotoxic drugs?

Cytotoxic drugs inhibit or prevent the function of cells. Cytotoxic drugs are primarily used to treat cancer, frequently
as part of a chemotherapy regime. Recently, their uses have expanded to treat certain skin conditions (e.g., psoriasis),
rheumatoid and juvenile rheumatoid arthritis, and steroid-resistant muscle conditions. The most common forms of
cytotoxic drugs are known as antineoplastic. The terms antineoplastic and cytotoxic are often
used interchangeably.
Cytotoxic drugs can prevent the rapid growth and division of cancer cells. They can also affect the growth of other
quick dividing cells in the body, like hair follicles and the lining of the digestive system. As a result of the treatment,
many normal cells are damaged along with the cancer cells.

There are no exposure limits set for cytotoxic drugs. CUPEs position is that even low-level exposure to cytotoxic
drugs should be avoided. The only safe occupational exposure to cytotoxic drugs is no exposure.

Types of Cytotoxic Drugs

Cytotoxic drugs are powerful chemotherapy medications used to kill cancerous cells. Different types of cytotoxic drugs interfere with
varying cellular activities to induce cell death, with most disrupting some aspect of cell replication. If cancer cells cannot multiply, the
disease can potentially be controlled. Although cancer cells are the target of cytotoxic chemotherapy, these medicines also interact
with healthy cells that are actively dividing.

Nucleoside Antagonists
Cancerous tumors grow by continuously replicating--the process of one cell dividing into two new cells. As a cell prepares to divide, it
makes a copy of its genetic material. Chemicals called nucleosides are the building blocks of the cell's genetic material, or genome.
Emory University Winship Cancer Institute explains that nucleoside antagonists are cytotoxic drugs that disrupt the genome copying
process, thereby preventing cell replication and lethally damaging the original cell. Examples of nucleoside antagonists include 5fluorouracil, 6-mercaptopurine, arabinosylcytosine, capecitabine, clofarabine, cytarabine, dacarbazine, fludarabine, gemcitabine and
nelarabine. These medications are frequently used to treat many types of cancer, including melanoma, lymphoma and leukemia and
cancers of the adrenal gland, bladder, breast, cervix, colon, esophagus, endometrium, liver, lungs, ovaries, pancreas, prostate, rectum
and stomach.

Intercalating Agents
Intercalating agents are cytotoxic drugs that bind to a cell's genetic material, arresting the copying process and distorting its chemical
structure, notes chemist Charles Ophardt, Ph.D., of Elmhurst College. Oxaliplatin, cisplatin and carboplatin are platinum-containing
intercalating agents, which are frequently used in combination with other cytotoxic chemotherapy drugs. Combination therapy with
these agents may be used to treat cancers of the adrenal gland, bladder, bone, brain, head and neck, breast, cervix, colon, rectum,
endometrium, esophagus, liver, lung, ovary and testicle.

Spindle Inhibitors
Cell replication, or mitosis, requires formation of a structure called a spindle, which provides the framework for dividing the copied
genetic material between the intended new cells. Spindle inhibitors disrupt the formation of this essential structure, explains Emory
University Winship Cancer Institute. Spindle inhibitors include the taxane drugs docetaxel and paclitaxel, ixabepilone and the vinca
alkaloids vindesine, vincristine, vinorelbine and vinblastine. These drugs may be used alone or in combination therapy regimens for
cancers of the breast, colon, rectum, head and neck, stomach, ovary, lungs, prostate and testicle. Spindle inhibitors are also used to
treat leukemias, lymphomas, rhabdomyosarcomas and neuroblastomas.

Folate Inhibitors
Folate inhibitors interfere with the production of the nucleosides required for copying genetic material for cell replication, notes
Emory University Winship Cancer Institute. Methotrexate and pemetrexed are folate inhibitors often used for the treatment of
lymphoma, leukemia, choriocarcinoma, mesothelioma and cancers of the bone, bladder, head, neck, breast and lungs.

Antibiotics
Class

Generic/Brand

Lipopeptides

Daptomycin (Cubicin), 2003

Fluoroquinolone

Gemifloxacin (Factive), 2003

Lipoglycopeptides

Telavancin (Vibativ), 2009

Cephalosporin
(5th generation)

Ceftaroline (Teflaro), 2010

Macrocyclics

Fidaxomicin (Dificid), 2011

-Lactam Antibiotics
Beta-lactam antibiotics include penicillins, cephalosporins, monobactams, and carbapenems.

Penicillins
Generic

Brand Name

Amoxicillin

Amoxil, Polymox, Trimox, Wymox

Ampicillin

Omnipen, Polycillin, Polycillin-N, Principen,

Totacillin

Bacampicillin

Spectrobid

Carbenicillin

Geocillin, Geopen

Cloxacillin

Cloxapen

Dicloxacillin

Dynapen, Dycill, Pathocil

Flucloxacillin

Flopen, Floxapen, Staphcillin

Mezlocillin

Mezlin

Nafcillin

Nafcil, Nallpen, Unipen

Oxacillin

Bactocill, Prostaphlin

Penicillin G

Bicillin L-A,
Crysticillin 300 A.S., Pentids, Permapen,
Pfizerpen, Pfizerpen-AS, Wycillin

Penicillin V

Beepen-VK, Betapen-VK, Ledercillin VK, V-Cillin

K

Piperacillin

Pipracil

Pivampicillin
Pivmecillinam
Ticarcillin

Ticar

Cephalosporins
Generic

Brand Name

First Generation
Cefacetrile (cephacetrile)

Celospor, Celtol, Cristacef

Cefadroxil (cefadroxyl)

Duricef, Ultracef

Cefalexin (cephalexin)

Keflex, Keftab

Cefaloglycin (cephaloglycin)

Kefglycin

Cefalonium (cephalonium)

Cefaloridine (cephaloradine)
Cefalotin (cephalothin)

Keflin

Cefapirin (cephapirin)

Cefadyl

Cefatrizine
Cefazaflur
Cefazedone
Cefazolin (cephazolin)

Ancef, Kefzol

Cefradine (cephradine)

Velosef

Cefroxadine
Ceftezole
Second Generation
Cefaclor

Ceclor, Ceclor CD, Distaclor, Keflor, Ranicor

Cefamandole

Mandol

Cefmetazole
Cefonicid

Monocid

Cefotetan

Cefotan

Cefoxitin

Mefoxin

Cefprozil (cefproxil)

Cefzil

Cefuroxime

Ceftin, Kefurox, Zinacef, Zinnat

Cefuzonam
Third Generation
Cefcapene
Cefdaloxime
Cefdinir

Omnicef, Cefdiel

Cefditoren

Spectracef

Cefetamet
Cefixime

Suprax

Cefmenoxime

Cefmax

Cefodizime
Cefotaxime

Claforan

Cefpimizole
Cefpodoxime

Vantin

Cefteram
Ceftibuten

Cedax

Ceftiofur

Excede

Ceftiolene
Ceftizoxime

Cefizox

Ceftriaxone

Rocephin

Cefoperazone

Cefobid

Ceftazidime

Ceptaz, Fortum, Fortaz, Tazicef, Tazidime

Fourth Generation
Cefclidine
Cefepime

Maxipime

Cefluprenam
Cefoselis
Cefozopran
Cefpirome

Cefrom

Cefquinome
Fifth Generation
Ceftobiprole

Zeftera

Ceftaroline

Teflaro

Not Classified
Cefaclomezine
Cefaloram
Cefaparole
Cefcanel
Cefedrolor
Cefempidone
Cefetrizole
Cefivitril
Cefmatilen
Cefmepidium
Cefovecin
Cefoxazole
Cefrotil
Cefsumide
Cefuracetime
Ceftioxide
Combinations
Ceftazidime/Avibactam

Avycaz

Monobactams
Generic
Aztreonam

Brand Name
Azactam, Cayston

Carbapenems
Generic

Brand Name

Imipenem,
Imipenem/cilastatin

Primaxin

Doripenem

Doribax

Meropenem

Merrem

Ertapenem

Invanz

Macrolide Antibiotics
Generic
Azithromycin

Brand Name
Zithromax

Erythromycin
Clarithromycin

Biaxin

Dirithromycin

Dynabac

Roxithromycin

Rulid, Surlid

Ketolides
Telithromycin

Ketek

Lincosamides
Generic

Brand Name

Clindamycin

Cleocin

Lincomycin

Lincocin

Streptogramins
Generic

Brand Name

Pristinamycin

Pyostacine

Quinupristin/dalfopristin

Synercid

Aminoglycoside Antibiotics
Generic

Brand Name

Amikacin

Amikin

Gentamicin

Garamycin, G-Mycin, Jenamicin

Kanamycin

Kantrex

Neomycin

Mycifradin, Myciguent

Netilmicin

Netromycin

Paromomycin
Streptomycin
Tobramycin

Nebcin

Quinolone Antibiotics
Generic

Brand Name

First Generation
Flumequine

Flubactin

Nalidixic acid

NegGam, Wintomylon

Oxolinic acid

Uroxin

Piromidic acid

Panacid

Pipemidic acid

Dolcol

Rosoxacin

Eradacil

Second Generation
Ciprofloxacin

Cipro, Cipro XR, Ciprobay, Ciproxin

Enoxacin

Enroxil, Penetrex

Lomefloxacin

Maxaquin

Nadifloxacin

Acuatim, Nadoxin, Nadixa

Norfloxacin

Lexinor, Noroxin, Quinabic, Janacin

Ofloxacin

Floxin, Oxaldin, Tarivid

Pefloxacin

Peflacine

Rufloxacin

Uroflox

Third Generation
Balofloxacin

Baloxin

Gatifloxacin

Tequin, Zymar

Grepafloxacin

Raxar

Levofloxacin

Cravit, Levaquin

Moxifloxacin

Avelox, Vigamox

Pazufloxacin

Pasil, Pazucross

Sparfloxacin

Zagam

Temafloxacin

Omniflox

Tosufloxacin

Ozex, Tosacin

Fourth Generation
Besifloxacin

Besivance

Clinafloxacin
Gemifloxacin

Factive

Sitafloxacin

Gracevit

Trovafloxacin

Trovan

Prulifloxacin

Quisnon

Sulfonamides
Generic

Brand Name

Sulfamethizole

Thiosulfil Forte

Sulfamethoxazole

Gantanol, Urobak

Sulfisoxazole

Gantrisin

Trimethoprim-Sulfamethoxazole

Bactrim, Bactrim DS, Cotrim, Cotrim DS,

Septra, Septra DS, Sulfatrim, Sulfatrim-DS

Tetracycline Antibiotics
Generic

Brand Name

Demeclocycline

Declomycin

Doxycycline

Doryx, Vibramycin

Minocycline

Dynacin, Minocin, Monodox

Oxytetracycline

Terramycin

Tetracycline

Achromycin

Glycylcyclines
Tigecycline

Tygacil

Other Antibiotics
Generic

Brand Name

Chloramphenicol

Chloromycetin

Metronidazole

Flagyl, Helidac, Metizol, Metric 21, Neo-Metric,

Noritate, Novonidazol

Tinidazole

Tindamax

Nitrofurantoin

Furadantin, Macrobid, Macrodantin

Glycopeptides
Vancomycin

Vancocin

Teicoplanin

Targocid

Lipoglycopeptides
Telavancin

Vibativ

Oxazolidinones
Linezolid
Cycloserine

Zyvox
2

Seromycin

Rifamycins
Rifampin

Rifadin

Rifabutin

Mycobutin

Rifapentine

Priftin

Rifalazil
Polypeptides
Bacitracin

Baciguent

Polymyxin B
Tuberactinomycins
Viomycin
Capreomycin

What are Antibiotics?

The word "antibiotics" comes from the Greek anti ("against") and bios ("life"). The noun antibiotic was suggested in 1942 by Dr.
Selman A. Waksman, soil microbiologist 4.
An antibiotic is a drug that kills or slows the growth of bacteria. Antibiotics are one class of antimicrobials, a larger group which
also includes anti-viral, anti-fungal, and anti-parasitic drugs. Antibiotics are chemicals produced by or derived from
microorganisms (i.e. bugs or germs such as bacteria and fungi). The first antibiotic was discovered by Alexander Fleming in
1928 in a significant breakthrough for medical science. Antibiotics are among the most frequently prescribed medications in
modern medicine.
Antibiotics are used to treat many different bacterial infections. Antibiotics cure disease by killing or injuring bacteria. Bacteria
are simple one-celled organisms that can be found, by the billions, all around us: on furniture and counter-tops, in the soil, and
on plants and animals. They are a natural and needed part of life. Bacteria cause disease and infection when they are able to
gain access to more vulnerable parts of our bodies and multiply rapidly. Bacteria can infect many parts of the body: eyes, ears,
throat, sinuses, lungs, airways, skin, stomach, colon, bones, genitals.

Bactericidal and Bacteriostatic Antibiotics

Some antibiotics are bactericidal, meaning that they work by killing bacteria. Other antibiotics arebacteriostatic, meaning
that they work by stopping bacteria multiplying.
Each different type of antibiotic affects different bacteria in different ways. For example, an antibiotic might inhibit a bacterium's
ability to turn glucose into energy, or its ability to construct its cell wall. When this happens, the bacterium dies instead of
reproducing.

Broad-spectrum and Narrow-spectrum Antibiotics

Some antibiotics can be used to treat a wide range of infections and are known as broad-spectrum antibiotics. Others are
only effective against a few types of bacteria and are callednarrow-spectrum antibiotics.

Antibiotic resistance

Antibiotics are extremely important in medicine, but unfortunately bacteria are capable of developing resistance to them.
Antibiotic-resistant bacteria are germs that are not killed by commonly used antibiotics. When bacteria are exposed to the same
antibiotics over and over, the bacteria can change and are no longer affected by the drug.
Bacteria have number of ways how they become antibiotic-resistant. For example, they possess an internal mechanism of
changing their structure so the antibiotic no longer works, they develop ways to inactivate or neutralize the antibiotic. Also
bacteria can transfer the genes coding for antibiotic resistance between them, making it possible for bacteria never exposed to
an antibiotic to acquire resistance from those which have. The problem of antibiotic resistance is worsened when antibiotics are
used to treat disorders in which they have no efficacy (e.g. antibiotics are not effective against infections caused by viruses), and
when they are used widely as prophylaxis rather than treatment.
Resistance to antibiotics poses a serious and growing problem, because some infectious diseases are becoming more difficult
to treat. Resistant bacteria do not respond to the antibiotics and continue to cause infection. Some of these resistant bacteria
can be treated with more powerful medicines, but there some infections that are difficult to cure even with new or experimental
drugs.

Antibiotics Classification
Although there are several classification schemes for antibiotics, based on bacterial spectrum (broad versus narrow) or type of
activity (bactericidal vs. bacteriostatic), the most useful is based on chemical structure. Antibiotics within a structural class will
generally have similar patterns of effectiveness, toxicity, and allergic potential.
The main classes of antibiotics are:

o
o

Beta-Lactams
Penicillins
Cephalosporins
Macrolides
Fluoroquinolones
Tetracyclines
Aminoglycosides
Most commonly used types of antibiotics are: Aminoglycosides, Penicillins, Fluoroquinolones, Cephalosporins, Macrolides, and
Tetracyclines. While each class is composed of multiple drugs, each drug is unique in some way.

Penicillins
The penicillins are the oldest class of antibiotics. Penicillins have a common chemical structure which they share with the
cephalosporins.
Penicillins are generally bactericidal, inhibiting formation of the cell wall. Penicillins are used to treat skin infections, dental
infections, ear infections, respiratory tract infections, urinary tract infections, gonorrhea.
There are four types of penicillins:

The natural penicillins are based on the original penicillin-G structure. Penicillin-G types are effective
against gram-positive strains of streptococci, staphylococci, and some gram-negative bacteria such as
meningococcus.
Penicillinase-resistant penicillins, notably methicillin and oxacillin, are active even in the presence of
the bacterial enzyme that inactivates most natural penicillins.
Aminopenicillins such as ampicillin and amoxicillin have an extended spectrum of action compared
with the natural penicillins. Extended spectrum penicillins are effective against a wider range of bacteria.

Penicillins side effects

Penicillins are among the least toxic drugs known. The most common side effect of penicillin is diarrhea. Nausea, vomiting, and
upset stomach are also common. In rare cases penicillins can cause immediate and delayed allergic reactions - specifically, skin
rashes, fever, and anaphylactic shock. Penicillins are classed as category B during pregnancy.

Cephalosporins
Cephalosporins have a mechanism of action identical to that of the penicillins. However, the basic chemical structure of the
penicillins and cephalosporins differs in other respects, resulting in some difference in the spectrum of antibacterial activity. Like
the penicillins, cephalosporins have a beta-lactam ring structure that interferes with synthesis of the bacterial cell wall and so are
bactericidal. Cephalosporins are derived from cephalosporin C which is produced from Cephalosporium acremonium.
Cephalosporins are used to treat pneumonia, strep throat, staph infections, tonsillitis, bronchitis, otitis media, various types of
skin infections, gonorrhea, urinary tract infections Cephalosporin antibiotics are also commonly used for surgical prophylaxis.
Cephalexin can also be used to treat bone infections.
Cephalosporins are among the most diverse classes of antibiotics, they are grouped into "generations" by their antimicrobial
properties. Each newer generation has a broader spectrum of activity than the one before.

o
o
o
o
o
o

o
o
o
o
o

o
o
o
o
o
o
o
o
o
o
o
o
o

o
o
o
o
o
o

The first generation cephalosporins include: Their spectrums of activity are quite similar. They possess
generally excellent coverage against most gram-positive pathogens and variable to poor coverage against most
gram negative pathogens. The first generation includes:
cephalothin
cefazolin
cephapirin
cephradine
cephalexin
cefadroxil
The second generation cephalosporins. In addition to the gram positive spectrum of the first
generation cephalosporins, these agents have expanded gram negative spectrum. Cefoxitin and cefotetan also
have good activity against Bacteroides fragilis. Enough variation exists between the second generation
cephalosporins in regard to their spectrums of activity against most species of gram negative bacteria, that
susceptibility testing is generally required to determine sensitivity. The second generation includes:
cefaclor
cefamandole
cefonicid
ceforanide
cefuroxime
The third generation cephalosporins have much expanded gram negative activity. However, some
members of this group have decreased activity against gram-positive organisms. They have the advantage of
convenient administration, but they are expensive. The third generation includes:
cefcapene
cefdaloxime
cefditoren
cefetamet
cefixime
cefmenoxime
cefodizime
cefoperazone
cefotaxime
cefpimizole
cefpodoxime
ceftibuten
ceftriaxone
The fourth generation cephalosporins are extended-spectrum agents with similar activity against
gram-positive organisms as first-generation cephalosporins. They also have a greater resistance to betalactamases than the third generation cephalosporins. Many fourth generation cephalosporins can cross blood
brain barrier and are effective in meningitis. The fourth generation includes:
cefclidine
cefepime
cefluprenam
cefozopran
cefpirome
cefquinome

Cephalosporins side effects

Cephalosporins generally cause few side effects. Common side effects associated these drugs include: diarrhoea, nausea, mild
stomach cramps or upset. Approximately 510% of patients with allergic hypersensitivity to penicillins will also have crossreactivity with cephalosporins. Thus, cephalosporin antibiotics are contraindicated in people with a history of allergic reactions
(urticaria, anaphylaxis, interstitial nephritis, etc) to penicillins or cephalosporins. Cephalosporin antibiotics are classed as
pregnancy category B.

Fluoroquinoloness
Fluoroquinolones (fluoridated quinolones) are the newest class of antibiotics. Their generic name often contains the root
"floxacin". They are synthetic antibiotics, and not derived from bacteria. Fluoroquinolones belong to the family of antibiotics
called quinolones. The older quinolones are not well absorbed and are used to treat mostly urinary tract infections. The newer
fluoroquinolones are broad-spectrum bacteriocidal drugs that are chemically unrelated to the penicillins or the cephalosporins.
Because of their excellent absorption fluoroquinolones can be administered not only by intravenous but orally as well.
Fluoroquinolones are used to treat most common urinary tract infections, skin infections, and respiratory infections (such as
sinusitis, pneumonia, bronchitis).
Fluoroquinolones inhibit bacteria by interfering with their ability to make DNA. This activity makes it difficult for bacteria to
multiply. This effect is bacteriocidal.
Fluoroquinolone grope includes:

ciprofloxacin
levofloxacin
lomefloxacin
norfloxacin
sparfloxacin
clinafloxacin
gatifloxacin
ofloxacin
trovafloxacin

Fluoroquinolones side effects

Fluoroquinolones are well tolerated and relatively safe. The most common side effects include nausea, vomiting, diarrhea,
abdominal pain. Other more serious but less common side effects are central nervous system effects (headache, confusion and
dizziness), phototoxicity (more common with lomefloxacin and sparfloxacin). All drugs in this class have been associated with
convulsions. Fluoroquinolones are classed as pregnancy category C.

Tetracyclines
Tetracyclines got their name because they share a chemical structure that has four rings. They are derived from a species of
Streptomyces bacteria.
Tetracycline antibiotics are broad-spectrum bacteriostatic agents and work by inhibiting the bacterial protein synthesis.
Tetracyclines may be effective against a wide variety of microorganisms, including rickettsia and amebic parasites.
Tetracyclines are used in the treatment of infections of the respiratory tract, sinuses, middle ear, urinary tract, skin, intestines.
Tetracyclines also are used to treat Gonorrhoea, Rocky Mountain spotted fever, Lyme Disease, typhus. Their most common
current use is in the treatment of moderately severe acne and rosacea.
Tetracycline antibiotics are:

tetracycline
doxycycline
minocycline
oxytetracycline

Tetracyclines side effects

Drugs in the tetracycline class become toxic over time. Expired drugs can cause a dangerous syndrome resulting in damage to
the kidneys.
Common side effects associated with tetracyclines include cramps or burning of the stomach, diarrhea, sore mouth or tongue.
Tetracyclines can cause skin photosensitivity, which increases the risk of sunburn under exposure to UV light. This may be of
particular importance for those intending to take on holidays long-term doxycycline as a malaria prophylaxis. Rarely,
tetracyclines may cause allergic reactions. Very rarely severe headache and vision problems may be signs of dangerous
secondary intracranial hypertension.
Tetracycline antibiotics should not be used in children under the age of 8, and specifically during periods of tooth development.
Tetracyclines are classed as pregnancy category D. Use during pregnancy may cause alterations in bone development.

Macrolides
The macrolide antibiotics are derived from Streptomyces bacteria, and got their name because they all have a macrocyclic
lactone chemical structure.
The macrolides are bacteriostatic, binding with bacterial ribosomes to inhibit protein synthesis. Erythromycin, the prototype of
this class, has a spectrum and use similar to penicillin. Newer members of the group, azithromycin and clarithyromycin, are
particularly useful for their high level of lung penetration. Macrolide antibiotics are used to treat respiratory tract infections (such
as pharyngitis, sinusitis, and bronchitis), genital, gastrointestinal tract, and skin infections.
Macrolide antibiotics are:

erythromycin
clarithromycin
azithromycin
dirithromycin
roxithromycin
troleandomycin

Macrolides side effects

Side effects associated with macrolides include nausea, vomiting, and diarrhea; infrequently, there may be temporary auditory
impairment. Azithromycin has been rarely associated with allergic reactions, including angioedema, anaphylaxis, and
dermatologic reactions. Oral erythromycin may be highly irritating to the stomach and when given by injection may cause severe
phlebitis. Macrolide antibiotics should be used with caution in patients with liver dysfunction. Pregnancy category B:
Azithromycin, erythromycin. Pregnancy category C: Clarithromycin, dirithromycin, troleandomycin.

Aminoglycosides
Aminoglycosides are derived from various species of Streptomyces.
In 1943, Selman Waksman, together with his co-workers, discovered that a fungus Streptomyces griseus produced an
antibiotic substance which they named "streptomycin." Selman Waksman was awarded the Nobel Prize in Physiology or
Medicine in 1952 for his discovery of streptomycin.
The aminoglycosides are bactericidal and work by stopping bacteria from making proteins.
Aminoglycoside antibiotics are used to treat infections caused by gram-negative bacteria. Aminoglycosides may be used along
with penicillins or cephalosporins to give a two-pronged attack on the bacteria. Aminoglycosides work quite well, but bacteria can
become resistant to them. Since aminoglycosides are broken down easily in the stomach, they can't be given by mouth and
must be injected. Generally, aminoglycosides are given for short time periods.
Aminoglycoside grope includes:

amikacin
gentamicin

kanamycin
neomycin
streptomycin
tobramycin

Monobactams
Print

Aztreonam

Monobactams belong to a group of monocyclic -lactams. Monobactams are obtained from the
bacteria Chromobacterium violaceum. Among monobactams only aztreonam is currently used in
clinical practice. It possesses a narrow spectrum of antibacterial activity and is used to treat
infections caused by gram-negative aerobic flora.
Spectrum

of

activity

Action mechanism is associated with suppressing the formation of bacterial cell wall. Aztreonam is
resistant

to

many

-lactamases

produced

by

gram-negative

flora.

It

is

effective

against

Enterobacteriaceae and P.aeruginosa resistant to nosocomial strains resistant to cephalosporins,

aminoglycosides. It does not act on acynetobacter, S.maltophilia, B.cepacia, gram-positive cocci and
anaerobs.
Indications
Monobactams are indicated for the treatment of lower respiratory tract infections, intra-abdominal
infections, pelvic organ infections, urogenital infections, skin and soft tissue infections, sepsis.
Monobactams are actively used in combination with other preparations for the treatment of mixed
infections.
Contraindications:
Monobactams are contraindicated for patients with known reactions of hypersensitivity to
monobactams or beta-lactam antibiotics. They should be used with caution in patients with liver and
kidney diseases.
Cautions:

Pregnancy. The most of monobactams pass through placenta and enter systemic circulation of
the fetus. The safety of monobactams in pregnant women has not been established, and the
use of monobactams during pregnancy is not recommended

Breastfeeding. Monobactams pass though breast milk and therefore the use of the medication
is contraindicated

Monobactams should be used with caution in pediatric and geriatric patients; in patient with
hepatic or renal failure

Side

effects

The most common side effects typical for monobactams include:

Digestive system: stomach pain, nausea, diarrhea

Liver: jaundice, hepatitis

CNS: headache, drowsiness, confusion, insomnia

Allergic reactions: skin rash, hives, anaphylactic shock

Local reactions: phlebitis, pain in the injection site (in parenteral form of administration)

Drug

interactions:

It is not recommended to combine the medication with carbapenems

Anti-infectives
Anti-infectives are drugs that can either kill an infectious agent or inhibit it from spreading. Antiinfectives include antibiotics and antibacterials, antifungals, antivirals and antiprotozoals.
Please refer to the drug classes listed below for further information.

amebicides

aminoglycosides

anthelmintics

antifungals

azole antifungals

echinocandins

miscellaneous antifungals

polyenes
antimalarial agents

antimalarial combinations

antimalarial quinolines

miscellaneous antimalarials
antituberculosis agents

aminosalicylates

antituberculosis combinations

diarylquinolines

hydrazide derivatives

miscellaneous antituberculosis agents

nicotinic acid derivatives

rifamycin derivatives

streptomyces derivatives
antiviral agents

adamantane antivirals

antiviral boosters

antiviral combinations

antiviral interferons

chemokine receptor antagonist

integrase strand transfer inhibitor

miscellaneous antivirals

neuraminidase inhibitors

NNRTIs

NS5A inhibitors

nucleoside reverse transcriptase inhibitors (NRTIs)

protease inhibitors

purine nucleosides

carbapenems

cephalosporins
o

first generation cephalosporins

fourth generation cephalosporins

next generation cephalosporins

second generation cephalosporins

third generation cephalosporins

glycopeptide antibiotics

glycylcyclines

leprostatics

lincomycin derivatives

macrolide derivatives
o

ketolides

macrolides

miscellaneous antibiotics

oxazolidinone antibiotics

penicillins
o

aminopenicillins

antipseudomonal penicillins

beta-lactamase inhibitors

natural penicillins

penicillinase resistant penicillins

quinolones

sulfonamides

tetracyclines

urinary anti-infectives