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    Antibiotics: Presented By: Bruan, Maria Aida Lumico, Moira Panti, John Christopher Libid, Teryl David, Rafael

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    Louie Bruan
    The document discusses antibiotics, including: 1) Antibiotics are drugs that kill or slow the growth of bacteria and were first discovered by Alexander Fleming in 1928. 2) There are several classes of antibiotics discussed, including sulfonamides, quinolones, and beta-lactams like penicillins. 3) Each antibiotic class has different mechanisms of action, spectrums of coverage, therapeutic uses, and toxicity profiles.

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    Antibiotics: Presented By: Bruan, Maria Aida Lumico, Moira Panti, John Christopher Libid, Teryl David, Rafael

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    Louie Bruan
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    The document discusses antibiotics, including: 1) Antibiotics are drugs that kill or slow the growth of bacteria and were first discovered by Alexander Fleming in 1928. 2) There are several classes of antibiotics discussed, including sulfonamides, quinolones, and beta-lactams like penicillins. 3) Each antibiotic class has different mechanisms of action, spectrums of coverage, therapeutic uses, and toxicity profiles.

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    The document discusses antibiotics, including: 1) Antibiotics are drugs that kill or slow the growth of bacteria and were first discovered by Alexander Fleming in 1928. 2) There are several classes of antibiotics discussed, including sulfonamides, quinolones, and beta-lactams like penicillins. 3) Each antibiotic class has different mechanisms of action, spectrums of coverage, therapeutic uses, and toxicity profiles.

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    40 views44 pages

    Antibiotics: Presented By: Bruan, Maria Aida Lumico, Moira Panti, John Christopher Libid, Teryl David, Rafael

    Uploaded by

    Louie Bruan
    The document discusses antibiotics, including: 1) Antibiotics are drugs that kill or slow the growth of bacteria and were first discovered by Alexander Fleming in 1928. 2) There are several classes of antibiotics discussed, including sulfonamides, quinolones, and beta-lactams like penicillins. 3) Each antibiotic class has different mechanisms of action, spectrums of coverage, therapeutic uses, and toxicity profiles.

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    of 44

    ANTIBIOTICS

    Presented by :

    Bruan, Maria Aida


    Lumico, Moira
    Panti, John Christopher
    Libid, Teryl
    David, Rafael
    Antibiotics
    The word "antibiotics" comes from the Greek anti
    ("against") and bios ("life").

    > 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. Antibiotics are among the most
    frequently prescribed medications in modern medicine.
    •Some antibiotics are bactericidal, meaning that they work
    by killing bacteria. Other antibiotics are bacteriostatic,
    meaning that they work by stopping bacteria multiplying.

    •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 called narrow-spectrum antibiotics.
    Sulfonamides
    • Analogues of PABA
    • Broad spectrum
    • Competitive inhibitors of
    dihydropteroate synthase –
    needed for folic acid synthesis
    • Cidal in urine
    • Mechanisms of resistance
    • Altered affinity of enzyme for drug
    • Decreased permeability or active
    efflux
    • New pathway of folic acid synthesis

    Gerhard Domagk gets a


    Nobel for Medicine, 1939.
    Sulfonamides
    • Mostly absorbed from GI tract
    • Binds variably to serum albumin
    • Wide tissue distribution,
    including transplacentally
    • Variably inactivated in liver by
    acetylation and then excreted in
    urine
    • Some agents can precipitate in
    acid urine
    Rapidly Absorbed and Eliminated
    Sulfonamides
    • Sulfisoxazole,
    sulfamethoxazole,
    sulfadiazine
    • Bind extensively to plasma
    proteins
    • Highly concentrated in
    urine (cidal)
    • Sulfamethoxazole combined
    with trimethoprim (Bactrim) is
    widely used to treat a variety of
    infections (esp. UTI)
    Poorly Absorbed Sulfonamides
    • Sulfasalazine
    • Poorly absorbed in GI tract
    • Used to treat ulcerative
    colitis and irritable bowel
    syndrome
    • Gut flora metabolize drug
    into 2 compounds, 1 toxic,
    1 therapeutic (5-
    aminosalicylate)

    Ulcerative Colitis
    Sulfonamides for Topical Use
    • Sulfacetamide
    • Good penetration in eye
    • Non-irritating
    • Silver sulfadiazine
    • Prevention and
    treatment of burn
    wound infections

    Bacterial corneal infection


    Long Acting Sulfonamide

    • Sulfadoxine
    • Serum half-life is
    measured in days
    rather than minutes or
    hours
    • Combined with
    pyirethamine to treat
    malaria
    Plasmodium vivax
    Therapeutic Uses
    of Sulfonamides
    • Urinary tract infections
    • Nocardiosis
    • Toxoplasmosis (avoid using in
    pregnant women)

    Nocardia asteroides
    Toxicity/Contraindications
    of Sulfonamides - UT
    • Crystallization in acid
    urine
    • Common to uncommon
    depending on drug
    • Alkalize urine or
    increase hydration
    Toxicity/Contraindications
    of Sulfonamides - blood
    • Acute hemolytic anemia
    • Rare to extremely rare
    • Associated with glucose-6-phosphate dehydrogenase activity in RBC
    • Agranulocytosis (extremely rare)
    • Aplastic anemia (extremely rare)
    Toxicity/Contraindications
    of Sulfonamides - immune
    • Hypersensitivity reactions (common to uncommon)
    • Skin and mucous membrane manifestations (rashes)
    • Serum sickness
    • Focal or diffuse necrosis of the liver (rare)
    Toxic Epidermal Necrolysis (TEN)
    Toxicity/Contraindications
    of Sulfonamides - miscellaneous
    • Nausea, anorexia, vomiting
    (common)
    • Kernicterus
    • Displacement of bilirubin from
    plasma albumin to brain
    resulting in encephalopathy
    • Never give sulfa drugs to a
    pregnant or lactating woman
    • Potentiation of oral coagulants,
    sulfonylurea hypoglycemic
    drugs, and hydrantoin
    anticonvulsants
    Bilirubin deposits in
    neonatal brain
    The Quinolones
    • Naladixic acid was a byproduct
    of chloroquine synthesis
    • Current drugs are fluoridated 4-
    quinolones
    • Broad coverage (some broader
    than others)
    • Targets DNA gyrase (G-) and
    topoisomerase IV (G+)
    • Resistance due to efflux and
    mutations in targets
    Quinolones
    • Favorable pharmacological
    attributes
    • Orally administered, quickly absorbed, even
    with a full stomach
    • Excellent bioavailability in a wide range of
    tissues and body fluids (including inside cells)
    • Mostly cleared by the kidneys
    • Exceptions are pefloxacin and moxifloxacin
    which are metabolized by liver
    • Ciprofloxacin, ofloxacin, and
    pefloxacin are excreted in breast
    milk

    “Got Cipro?”
    Therapeutic Uses
    of Quinolones
    • Urinary tract infections
    • Prostatitis
    • STD’s
    • Chlamydia
    • Chancroid
    • Not syphilis or
    gonorrhea (due to
    increased resistance)
    Therapeutic Uses
    of Quinolones
    • GI and abdominal
    • Travelers diarrhea
    • Shigellosis
    • Typhoid fever
    • Respiratory tract
    • All work well against
    atypicals
    • New agents for strep.
    pneumonia
    Therapeutic Uses
    of Quinolones
    • Bone, joint, soft tissue
    • Ideal for chronic
    osteomylitis
    • Resistance developing in S.
    aureus, P. aeruginosa, and S.
    marcesens
    • Good against polymicrobial
    infections like diabetic foot
    ulcers
    Therapeutic Uses
    of Quinolones
    • Ciprofloxacin for
    anthrax and tuleremia
    • Combined with other
    drugs, useful for
    atypical
    Mycobacterium sp. or
    for prophylaxis in
    neutropenic patients

    Pulmonary Anthrax
    Toxicity/Contraindications
    of Quinolones
    • Nausea, vomiting, abdominal discomfort (common)
    • Diarrhea and antibiotic-associated colitis (uncommon to
    rare)
    • CNS side effects
    • Mild headache and dizziness (common to rare)
    • Hallucinations, delirium, and seizures (rare)
    • Arthropy in immature animals (common)
    • Quinolones not given to children unless benefits outweigh the risks
    • Leukopenia, eosinophila, heart arythmias (rare)
    The Beta-Lactams
    Penicillins
    • Penicillium notatum produces
    the only naturally occuring
    agent – penicillin G or
    benzylpenicillin
    • Dosage and potency based on
    IU (1 IU = 0.6 micrograms pure
    penicillin G)
    • P. chrysogenum produces 6-
    aminopenicillanic acid, raw
    material for semi-synthetics
    • Dosage and potency based on
    weight
    Penicillins

    • Spectrum of activity based on R groups added to 6-


    aminopenicillanic acid core
    • All are bactericidal and inhibit transpeptidases
    • Mechanisms of resistance
    • Alter affinity of transpeptidase
    • Enzymatically cleave the beta-lactam ring
    • Efflux pumps
    • Poor penetration into cell
    Penicillins

    • Administered orally, intramuscularly, or


    intravenously depending on agent
    • After oral dose, widely distributed in tissues and
    secretions (except CNS, prostatic fluid, and the
    eye)
    • Do not kill intracellular pathogens
    • Food interferes with adsorption
    • Rapid elimination through kidney, secreted in
    breast milk
    Penicillins G and V

    • Effective against aerobic G+ organisms except Staphylococcus, Pen G


    active against Neisseria and anaerobes
    • 2/3 of oral Pen G destroyed by stomach acid, Pen V is more resistant so
    more is delivered to serum
    • Rapid elimination through kidney so probenecid, procaine, of
    benzathine added to slow excretion
    • Most drug is bound to serum albumin but significant amounts show up
    in liver, bile, kidney, semen, joint fluid, lymph, etc.
    • Cautious use in neonates and infants because renal function is not fully
    established
    • Patients with renal failure clear the drugs through liver although at a
    slow pace
    Penicillins G and V
    Therapeutic Uses
    • Streptococcus pneumoniae
    infections
    • S. pyogenes infections
    • Viridans strep endocarditis (also
    given prophylactically)
    • Anaerobes except Bacteroides
    fragilis group
    • Meningococcal infections
    • Syphilis and other diseases
    caused by spirochetes
    Isoxazolyl Penicillins

    • Oxacillin, cloxacillin, dicloxacillin, nafcillin


    • Designed to resist staphylococcal beta-lactamases
    • Like Pen V, stable in stomach acid but usually given
    parentally for serious staph infections
    • MRSA not covered
    • Absorption and fate of drugs after absorption,
    excretion similar to Pen G and Pen V
    Aminopenicillins

    • Ampicillin and amoxicillin


    • Broad spectrum
    • Not effective against beta-lactamase producers
    • Beta-lactamase inhibitors extend spectrum
    • Both are acid resistant but amoxicillin is better
    absorbed, even with food
    • Don’t bind plasma proteins as much as
    predecessors
    • Secreted through the kidney
    Aminopenicillins
    Therapeutic Uses
    • Upper respiratory tract
    infections
    • Otitis media
    • Uncomplicated UTI
    • Acute bacterial
    meningitis in kids
    • Typhoid fever
    A Carboxypenicillin and
    a Ureidopenicillin
    • Ticarcillin and piperacillin
    • Ticarcillin is anti-
    Pseudomonas drug
    • Piperacillin + tazobactam
    has the broadest spectrum
    • Give parentally
    • Used for serious infections
    Toxicity/Contraindications
    of Penicillins
    • Hypersensitivity reactions (uncommon)
    • Rash, fever, bronchospasm, vasculitis, serum sickness,
    exfoliative dermatitis, SJS, anaphylaxis
    • Drugs act as haptens when bound to serum proteins
    • Rashes will disappear when drug is withdrawn or can
    treat with antihistamines
    • For patients with allergies, switch to a different class of
    antibiotics or try to desensitize
    Toxicity/Contraindications
    of Penicillins
    • Pain and sterile inflammatory
    reaction at injection site (dose-
    related)
    • Large doses given to patients
    with renal failure can cause
    lethargy, confusion twitching
    and seizures
    • Sudden release of procaine can
    cause dizziness, tinnitus,
    headache and hallucinations
    • Pseudomembranous colitis
    Cephalosporins
    • Base molecule is 7-
    aminocephalosporanic acid
    produced by a Sardinian sewer
    mold
    • R groups determine spectrum of
    activity and pharmacological
    properties
    • Mechanism of action/resistance
    and class pharmacology
    essentially the same as penicillins
    First Generation
    Cephalosporins
    • Cefazolin, cephalexin,
    cephadroxil
    • Excellent against susceptible
    staph and strep
    • Modest activity against G-
    • Cefazolin given parentally,
    others orally
    • More than half of the drug is
    bound to plasma proteins
    • Excreted by kidneys
    unmetabolized
    • Good for staph and strep skin
    and soft tissue infections
    Second Generation
    Cephalosporins
    • Cefaclor, cefuroxime, cefprozil
    • Modest activity against G+, increased activity
    against G-, works against anaerobes
    • Cefaclor and cefprozil given orally
    • Absorption and excretion same as first gen.
    • Good for treating respiratory tract infections,
    intra-abdominal infections, pelvic inflammatory
    disease, diabetic foot ulcers
    Third Generation
    Cephalosporins
    • Ceftaxime, ceftriaxzone,
    cefoperazone, cefpodoxime
    • Broad spectrum killers
    • Drugs of choice for serious infections
    • No effect against Listeria and beta-
    lactamase producing pneumococci
    • Cefpodoxime given orally, others
    parentally
    • Most excreted by kidney
    • Therapeutic uses
    • Bacterial meningitis (2 exceptions)
    • Lyme disease
    • Life-threatening G- sepsis
    Fourth Generation
    Cephalosporin
    •Cefepime
    •Same antimicrobial spectrum as third
    generation but resists more beta-
    lactamases
    •Given parentally, excellent penetration
    into CSF
    •Good for nosocomial infections
    Toxicity/Contraindications
    of Cephalosporins
    • Hypersensitivity reactions (uncommon)
    essentially same as for penicillins
    • Cross-reaction between 2 classes
    Carbapenems

    •Beta-lactam ring is fused to a 5


    member ring system
    •Effect on microbes and
    pharmacology of carbapenems
    similar to penicillins
    Select Carbapenems

    • Imipenem
    • Broad spectrum including anaerobes and Pseudomonas
    aeruginosa
    • Parentally administered
    • Must be combined with cilastatin to be absorbed
    • Excreted by kidneys
    • Meropenem, ertapenem, and doripenem are
    similar to imipenem but don’t need co-
    administration with cilastatin
    Aztrenam – a monobactam

    • Works only on G-, including Pseudomonas aeruginosa


    • Useful for treating G- infections that require a beta-lactam because
    it does not elicit hypersensitivity reactions
    Toxicity/Contraindications
    of Carbapenems
    • Nausea and vomiting (common)
    • Hypersensitivity reactions (uncommon)
    • Essentially the same as for penicillins, exception is the monobactam
    • Cross-reactivity is possible, exception is the monobactam

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