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41 Cards in this Set
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Penicillin G
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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. |
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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
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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)
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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) |
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ciprofloxacin
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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
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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 |
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clofazimine
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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 |