Antibiotics

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Penicillin G

Back 1

Class: β-lactam penicillin
Route: iv
Spectrum: some gram+, few gram-neg cocci (not rods), spirochetes, extracellular only.
DOC: 1° syphillis [treponema] (benzathine repository form, im)
Notes: combine with aminoglycoside for bactericidal against enterococcus.
Resistent: most staph, strep. pneumoniae, n. gonorrhoeae.

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dicloxacillin

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Class: β-lactam penicillin
Route: po
Spectrum: staphlococcus spp.
DOC: staph, but not MRSA.
RE: 70% bile, no renal adjustments necessary

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amoxicillin(-clavulanate)

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Class: β-lactam penicillin
Route: po
Spectrum: more active than penicillin G against some gram neg; routine infxns only.
DOC:
Notes: Better GI absorption, less GI distress, fewer rashes. No food interference. Clavulanate is a lactamase inhibitor, protects amoxicillin.

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piperacillin (-tazobactam)

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Class: β-lactam penicillin
Route: iv
Spectrum: only penicillin active against ps. aeruginosa. Serious gram-neg infxns
DOC:
RE: Urine; dosage ↓ if renal impairment.
Notes: Tazobactam is lactamase inhibitor

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cefazolin

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Class: β-lactam 1st gen. cephalosporin
Route: iv
Spectrum: gram+/- cocci, few gram neg rods
DOC: prophylaxis against infxn in surgical procedures
Note: can't enter CNS

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cephalexin

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Class: β-lactam 1st gen. cephalosporin
Route: po
Spectrum: cocci, some gram neg rods.
Notes: less gram-neg activity than cefazolin; substitute for oral penicillins (V).

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Penicillins

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Class: β-lactams
Types: original, anti-staph, amino-penicillins, anti-pseudomonal.
Side Effects: dose-independent hyptersensitivity (1:2000); anaphylactic shock. Oral cause GI distress. pseudomembranous colitis, yeast infxns. High dose impaired renal fxn, CNS lesion, risk of seizures, hyperkalaemia. Oral contraceptive disruption?
Notes: can cross acutely inflammed meninges (meningitis)
Half-life: short (30-60mim), extended by renal failure, probenecid, aspirin.
RE: urine

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β-lactams

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Types: Penicillins, cephalosporins, carbapenems, monobactams.
Mechanism: binds to PBP, (-) cell wall syn., cross-linking of peptidoglycans.
Resistence: lactamase, altered porins/PBPs.
Spectrum: bactericidal against actively growing bacteria, bacteriostatic for Enterococcus spp.. Extracellular only.
RE: kidney (except dicloxacillin, ceftriaxone)

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Cephalosporins

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Class: β-lactams
Types: 4 generations
Side effects: 10% cross-rxn with penicillins. Phlebitis (iv), rare: nephrotoxicity (w. aminoglycoside). 2/3rd gen. may cause C. difficile enterocolitis superinfxn.
Spectrum: generally broader than penicillins, more active against gram neg rods.
Notes: more resistant to lactamases. Oral less potent, narrower spec.
Resistence: MRSA, enterococcus, listeria.

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1st Generation Cephalosporins

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Class: β-lactam
Spectrum: gram+ cocci, few gram neg rods (more than amoxicillin).
Notes: can't enter CNS. Resistent to gram+ lactamases.

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2nd Generation Cephalosporins

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Class: β-lactam
Spectrum: ↑'d gram neg, less activity against gram+.
Notes: resistent to most lactamases, but not inducible, chr. of pseudomonas, enterobacter, & Serratia. The "Lost Generation", not DOC for ag.

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cefuroxime

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Class: β-lactam
Spectrum: 2nd gen. ceph. Some use against meningitis (but 3rd gen. better)
Route: iv, im, po
Notes: only 2nd gen. ceph. that can cross CNS.

Front 13

cefprozil

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Class: β-lactam
Spectrum: 2nd gen. ceph. For sinusitis, oititis media, UTIs, resp. infxns.
Route: po
Notes: more expensive penicillin sub than 1st gen.

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3rd Generation Cephalosporin

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Class: β-lactam
Spectrum: sig. gram neg action, good against Enterobacteriaceae, and certain gram+ with altered PBPs (strep, pneumococcus)
DOC: initial Tx of meningitis in adults, children >3 months (w. vancomycin ± rifampin)
Notes: not resistent to inducible, chr. of pseudomonas, enterobacter, & Serratia.

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ceftriaxone

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Class: β-lactam 3rd gen ceph.
Spectrum: 1st line against serious gram neg infxns.
Tx: typhoid fever, endocarditis, pneumonia (w. macrolide [community] or aminoglycoside [nosocomial])
DOC: meningitis (w. vancomycin ± rifampin), gonorrhea (follow up with anti-chlamydials)
Route:iv, im
Met: only 3rd gen ceph. NOT excreted in urine.
Notes:

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cefixime

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Class: β-lactam 3rd gen ceph.
Spectrum: gram negs
DOC: meningitis (w. vancomycin ± rifampin), gonorrhea (follow up with anti-chlamydials)
Route: po
Notes:

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cefepime

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Class: β-lactam 4th gen. ceph.
Spectrum: aerobes like Ps. aeruginosa, S. aureus, many enterobacter, and strep.
Route: iv
Notes: more resistent to chr. lactamases.

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imipenem-cilastatin

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Class: β-lactam carbapenem
Spectrum: broadest antibiotic, but not MRSA or most enterococcus. :-(
Tx: nosocomil multidrug-resis. infxns; drug is resistant to most lactamases.
Route: iv, im
Excretion: RE
Adverse: nausea,vomitting, hypersensitivity cross with penicillin, seizures (high dose).
Notes: cilastatin (-)'s renal breakdown of imipenem to nephrotoxic metabolite. Can cross CNS.

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aztreonam

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Class: β-lactam monobactam
Spectrum: aerobic gram negs (ps. aeruginosa, serratia, H. influenzae, enterobacteriaceae)
Route: iv, im
Excretion: RE
Adverse: very few; no cross rxn with penicillin! Rarely phlebitis, skin rash, liver fxn.
Notes:

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Vancomycin

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Class: β-lactam
Route: iv
Spectrum: extracellular gram+
Mech: (-)'s cross-linking of peptidoglycans by binding to D-ala-D-ala.
Resistence: enzymes replace D-ala-D-ala with D-ala-D-lac.
DOC: MRSA (w. gentamicin ± rifampin)
Tx: serious gram+ infxns, endocarditis if allergic to other β-lactams; C. difficile if resis. to metronidazole, penicillin-resis. pneumococcal meningitis.
Adverse: hypersensitivity, red-man/neck syndrome (too rapid iv), rare: oto/nephrotoxicity.

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Aminoglycosides

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Class: protein syn. inhibitors
MOA: enters via O2-dep. mech. Irreversible binding to 30S; bactericidal
MOR: enzymes that deactivate the drug.
Spectrum: aerobic gram negs (Ps., enterobacteriaceae), staph, some mycobacteria.
Adverse: ototoxicity, nephrotoxicity, low TI, NM-block (high dose, m. gravis).
Contra.: pregancy/nursing.
Meta.: RE
Notes: no CNS, highly polar; iv/im only.

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gentamicin

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Class: aminoglycoside protein syn. inhibitor
Route: iv, im
Spectrum: active against ps. aeruginosa.
Combos: +cell wall inhibitor for syngergistic effect against gram+

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Tetracyclines

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Class: protein syn. inhibitor
MOA: binds reversibly to 30S; bacteristatic
MOR: drug efflux
Spectrum: intracellular
Uses: spirochetes (Lyme, syphilis), mycoplasma (pneumonia), chlamydia, rickettsia, vibrio, legionella, acne, malaria.
Adverse: Binds to Ca2+ in dev'g bone/teeth. GI distress, intestinal/vaginal superinfections, photosensitivity.
Met.: RE (except doxycycline)
Contra: pregnant, children <8, dairy/Ca2+ products, "serious" GN infxns
Notes: no CNS

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doxycycline

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Class: tetracycline protein syn. inhibitor
Route: po, iv
Spectrum: intracellulars
Met: faeces
Notes: no food interference (except Ca2+ suppl.), long half-life permits single daily dose.

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Macrolides

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Class: protein syn. inhibitor
MOA: binds to 50S. Static/cidal depending on conc.
MOR: ↓'d perm, efflux, enzymes, ribosomal mut.
Spectrum: gram+, few gram negs, treponema, borrelia, chlamydia, mycoplasma, H. pylori, some mycobacteria.
DOC: community pneumonia, Legionella, diphtheria, chlamydia.
Notes: no CNS, food interferes.

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erythromycin

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Class: macrolide protein syn. inhibitor
Route: po, iv
Spec.: see macrolides
Half-life: short (90min)
Met: faeces
Adverse: GI distress (nausea/diarrhoea), motilin agonist; phlebitis (iv), deafness (high dose, reversible), hypersensitivity hepatitis/fever/rash (rare)
Pharmk.: (-)P450; seizures/CNS toxicity w. theophylline, ventricular arrhythmias w. antihistamines.

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azithromycin

Back 27

Class: macrolide protein syn. inhibitor
Route: po, iv
Spec.: see macrolides; ↑'d action against H. pylori, M. avium (MAC), and chlamydia.
DOC: community-acquired pneumonia
Half-life: longer; daily dose
Notes: accumulates in tissues, 10-100x higher than serum, permits daily dosing (slow release). More expensive, better tolerated than erythromycin.

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Lincosamides

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Class: protein syn. inhibitor
MOA: 50S; same as macrolides
MOR: same as macrolides, cross-resistance.
Adverse: diarrhoea, hypersensitivity rash v. common.
Met.: hepatic!
Notes: no CNS, accumulates in phagocytes, penetrates abscesses.

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clindamycin

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Class: lincosamide protein syn. inhibitor
Route: iv, po
Spectrum: strep, staph, pneumococci, bacteroides, anaerobes.
DOC: anaerobic/mixed infxns, prophylaxis for dental endocarditis.

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Chloramphenicol

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Class: protein syn. inhibitor
Route: iv
MOA: 50S
MOR: CAT inactivates drug
DOC: none; drug of last resort due to risks.
Spectrum: very broad, v. well distributed (incl. CNS!)
Adverse: bone marrow suppression (leukopaenia, anaemia), aplastic anaemia (rare), gray baby synd.
Pharmk: (-)P450

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trimethoprim-sulfamethoxazole (TMP/SMX; bactrin)

Back 31

Class: antifolate
MOA: synergistic (-)n of folate biosyn.
MOR (TMP): mutant DHFR
MOR (SMX): exogenous folate use, overproduction of PABA
MOR (both): ↓perm.
Spectrum: aerobes; most enterobacteriaceae, GNC, many gram+.
DOC: adult sinusitis, UTI, chronic bronchitis, prostatitis, acute otitis media, pneumocystis pneumoia.
Adverse: hypersensitivity (slow acetylaters) [SMX]; GI distress; fever, rashes, diarrhoea, leukopaenia (AIDS)
Rare adverse: urine crystal precip. [SMX], hepatotoxicity (G6PDH def) [SMX], blood disorders [TMP]
Met.: >50% in urine
Distr.: CNS, prostate, foetus.
Pharmk: (-) P450

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Fluoroquinolones

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Class: nucleic acid syn. inhitor
MOA: (-) DNA gyrase; bactericidal.
MOR: ↓perm, mut. gyrase.
Distr.: protate, bone, urine, macs, PMNs.
Met: RE
Adverse: GI distress, headaches, dizziness, skin rases, liver fxn, tendon rupture, psychosis.
Pharmk: (-) P450 (mild)
Contra: pregnancy, nursing, Ca2+/Mg2+ suppl., theophylline (seizures)

Front 33

ciprofloxacin

Back 33

Class: fluoroquinone nucleic acid syn. inhibitor
Route: iv, po
Spectrum: very broad; aerobics, GNB, GNC, some GPC, some intracellular, some mycobacteria.

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Metronidazole

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Class: "other"
Route: iv, po
Spectrum: anaerobes (bacteroides, clostridium, some protozoa/parasites (trich, giardia, entamoeba0
DOC: pseudomembranous colitis due to superinfxn with C. difficile.
Uses: BV, PID, gas gangrene, tetanus.
Adverse: nausea, dry mouth, taste alt., peripheral neuropathy (rare)
Contra: 1st trimester pregancy
Pharmk: (-)s P450; actue psychosis (w. disulfiram, ethanol). Prodrug; converted by nitroreductase.

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isoniazide

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Class: antimycobacterial
Route: po
Spectrum: most potent anti-TB.
Adverse: hepatitis (2.5%), allergy, peripheral neuropathy/neuritis (10-20%, ghigh dose, prevent w. pyridoxine). Rare: SLE, CNS toxicity (Tx; pyridoxine)
Pharmk: (-)P450; avoid warfarin, phenytoin.
Met: hepatic/renal aceytlation
Distr: CNS, phagocytes.
Notes: impaired by food, acetylator effect

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rifampin

Back 36

Class: antimycobacterial
Route: po, iv
MOA: binds RNA poly, (-) RNA syn.
MOR: mut. RNA poly
Spectrum: cocci, some enteric, chlamydia, mycobacteria.
DOC: H. influenzae and N. meningitidis prophylaxis, TB, leprosy.
Adverse: harmless orange colour, rash, fever, nausea. Flulike, jaundice (elderly, alcoholcis).
Pharmk: (+) P450! ↑s met. of oral contraceptives.
Distr..: CNS, phagocytes
Met: liver, bile/faeces
Notes: well absorbed.

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ethambutol

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Class: antimycobacterial
MOA: (-)s mycobacterial cell wall component syn. Enhances lipophilic drugs (rifampin).
Met: 50% urine
Distr: enters CNS only if meninges inflammed..
Adverse: visual disturbances; loss of acuity, red/green colourblindness (dose-dependent, reversible). Hyperuricaemia, can result in gout.
Notes: abosrbed from GI tract)

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pyrazinamide (PZA)

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class: antimycobacterial
Spectrum: only TB
Combos: with cipro for prophylaxis, with INH, rifampin, or ethambutol for Tx of TB.
Adverse: hyperuricaemia/gout, hepatotoxicity (1-5%)

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streptomycin

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Class: aminoglycoside antimycobacterial
Spectrum: only extracellular tubercle bacilli
Use: in combo for serious TB (miliary, meningitis, sever organ)
Adverse: ototoxic, nephrotoxic.
Notes: first available antimycobacterial; rarely used today due to resistance.

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dapsone

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Class: antileprosy antifolate
Spectrum: M. leprae
Uses: phrophylaxis/Tx of pneumocystis pneumonia in AIDS. Combo with clofazimine, rifampin for leprosy.
Adverse: GI disturbance, fever, rash. Rare: haemolysis (G6PDH def.), methaemoglobinaemia
Met: bile, urine

Front 41

clofazimine

Back 41

Class: antimycobacterial
MOA: a dye; binds DNA
use: combo with dapson, rifampin for leproxy. Weak against M. avium complex (MAC)
Adverse: skin discolouration.
Distr: accumulates in reticuloendothelial cells, skin.
Notes: anti-inflammatory, prevents erythaema nodosum leprosum