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antiBacterial Pharma
antiBacterial Pharma
47
Medical
Graduate
05/24/2011

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Term
Penicillin V
Definition
β-lactam ('cidal); PO
Mech:
1) bind PBPs,
2) block transpeptidase x-linking,
3) activ. autolytic Es
Use: all but G(-) rods
Tox:  hypersens; hemolytic anemia
Term
Methicillin
Definition
Lactamase-resistant β-lactam ('cidal)
Mech:
1) bind PBPs,2) block transpeptidase x-linking,
3) activ. autolytic Es
Use: S. aureus (not MRSA)
Tox:  hypersens; interstitial nephritis
Note "meth = iv drug use = risk staph"
Term
Nafcillin
Definition
Lactamase-resistant β-lactam ('cidal)
Mech: 1) bind PBPs, 2) block transpeptidase x-linking,
3) activ. autolytic Es
Use: S. aureus (not MRSA)
Tox:  hypersens
note "naf for staph"
Term
Dicloxacillin
Definition
Lactamase-resistant β-lactam ('cidal)
Mech: 1) bind PBPs, 2) block transpeptidase x-linking,
3) activ. autolytic Es
Use: S. aureus (not MRSA)
Tox:  hypersens
Term
Ampicillin
Definition
Wide spectrum β-lactam ('cidal)
Mech: 1) bind PBPs, 2) block transpeptidase x-linking, 3) activ. autolytic Es
Use: G(+), G(-) rods
"HELPS kill Enterococci"
Tox:  hypersens, rash, pseudomembrane colitis
Note: combine w/ clavulanic acid to enhance spectrum
"AMPed up penicillin"
Term
Amoxicillin
Definition
Wide spectrum β-lactam ('cidal)
Mech: 1) bind PBPs, 2) block transpeptidase x-linking,
3) activ. autolytic Es
Use: G(+), G(-) rods
"HELPS kill Enterococcus"
Tox:  hypersens, pseudomembrane colitis
Note: greater PO bioavail than amp; combine w/ clavulanic acid to enhance spectrum
Term
Ticarcillin
Definition
Antipseudomanal β-lactam ('cidal)
Mech: 1) bind PBPs, 2) block transpeptidase x-linking,
3) activ. autolytic Es
Use: Pseudomonas, G(-) rods
Tox:  hypersensNote: combine w/ clavulanic acid to enhance spectrum
Term
Carbenicillin
Definition
Antipseudomanal β-lactam ('cidal)
Mech: 1) bind PBPs, 2) block transpeptidase x-linking,
3) activ. autolytic Es
Use: Pseudomonas, G(-) rods
Tox:  hypersens
Note: combine w/ clavulanic acid to enhance spectrum
Term
Piperacillin
Definition
Antipseudomanal β-lactam ('cidal)
Mech: 1) bind PBPs, 2) block transpeptidase x-linking,
3) activ. autolytic Es
Use: Pseudomonas, G(-) rods
Tox:  hypersens
Note: combine w/ clavulanic acid to enhance spectrum
Term
Cephalexin
Definition
1st gen cephalosporin ('cidal) - others: cefazolin
Mech: inhib cell wall synth
Use: G(+) cocci + PEcK
Tox:  hypersens (x-react w/ Pen); incr. nephrotox of aminoglycosides; disulfiram-like
Term
Cefoxitin
Definition
2nd gen cephalosporin ('cidal) -
others: cefaclor, cefuroxime
Mech: inhib cell wall synth
Use: G(+) cocci + HEN PEcKS
Tox:  hypersens (x-react w/ Pen); incr. nephrotox of aminoglycosides; disulfiram-like
Term
Ceftriaxone
Definition
3rd gen cephalosporin ('cidal) -
others: cefotaxime, ceftazidime
Mech: inhib cell wall synth
Use: serious/resistant G(-); meningitis (penetrate BBB)
Tox:  hypersens (x-react w/ Pen); incr. nephrotox of aminoglycosides; disulfiram-like
Term
Cefipime
Definition
4th gen cephalosporin ('cidal)
Mech: inhib cell wall synth
Use: G(+); Pseudomonas; serious/resistant G(-); meningitis (penetrate BBB)
Tox:  hypersens (x-react w/ Pen); incr. nephrotox of aminoglycosides; disulfiram-like
Term
Aztreonam
Definition
Monobactam; lactamase-resistant
Mech: binds PBP3 → inhibs cell wall synth
Use: G(-)
(pen-allergic pts whose renal insuff can't support aminoglycosides)
Tox:  nontoxic; GI upset; no x-sens w/ pen or cephs
Term
Imipenem
Definition
Carbapenem; lact-R; broad-spectrum
Mech: binds PBP → inhibs cell wall synth
Use: kills everything; drug of choice for enterobacter
Tox:  GI, rash, seizures (limits use)
Note:  must admin w/ cilastatin (inhibs renal dihydropeptidase I)
Term
Meropenem
Definition
Carbapenem; lact-R; broad-spectrum
Mech: binds PBP → inhibs cell wall synth
Use: kills everything; drug of choice for enterobacter
Tox:  GI, rash, (less seizures than imipenem)
Note:  stable to renal dihydropeptidase I
Term
Vancomycin
Definition
Antibiotic ('cidal)
Mech: binds D-ala D-ala on wall precursors → inhibs cell wall synth
Use: serious/resistant G(+) - S. aureus, C. diff, MRSA
Tox:  well-tol; nephrotox, ototox, thrombophlebitis, "red man synd" (prevent w/ anti-His pre-tx & slow infusion)
Resist: D-ala D-lac
Term
Gentamycin
Definition
Aminoglycoside (30S, 'cidal)
Mech: inhib formation of initiation complex & misreading of mRNA
Use: severe (G-) aerobic rods
Tox: nephrotox (esp w/ cephs), ototox (esp w/ loops; contra: preg), teratogen
Notes: synergy w/ β-lactams; req 02 for uptake (therefore no anaerobes)
Term
Neomycin
Definition
Aminoglycoside (30S, 'cidal)
Mech: inhib formation of initiation complex & misreading of mRNA
Use: severe (G-) aerobic rods; bowel surg
Tox: nephrotox (esp w/ cephs), ototox (esp w/ loops; contra: preg), teratogen
Notes: synergy w/ β-lactams; req 02 for uptake
Term
Amikacin
Definition
Aminoglycoside (30S, 'cidal)
Mech: inhib formation of initiation complex & misreading of mRNA
Use: severe (G-) aerobic rods
Tox: nephrotox (esp w/ cephs), ototox (esp w/ loops; contra: preg), teratogen
Notes: synergy w/ β-lactams; req 02 for uptake
(no anaerobes)
Term
Tobramycin
Definition
Aminoglycoside (30S, 'cidal)
Mech: inhib formation of initiation complex & misreading of mRNAUse: severe (G-) aerobic rods
Tox: nephrotox (esp w/ cephs), ototox (esp w/ loops; contra: preg), teratogen
Notes: synergy w/ β-lactams; req 02 for uptake
Term
Streptomycin
Definition
Aminoglycoside (30S, 'cidal)
Mech: inhib formation of initiation complex & misreading of mRNA
Use: severe (G-) aerobic rods
Tox: nephrotox (esp w/ cephs), ototox (esp w/ loops; contra: preg), teratogen
Notes: synergy w/ β-lactams; req 02 for uptake
Term
Tetracycline
Definition
Tetracycline (30S)
Mech: prevent attach. of aminoacyl-tRNA
Use: tick-carried bact, acne; some CNS penetration
Tox: GI, discolor teeth, inhib child bone growth (contra: preg), photosens
Notes: must not take with milk, antacids, or Fe-containing preparations (cations inhib abs)
Term
Doxycycline
Definition
Tetracycline (30S)
Mech: prevent attach. of aminoacyl-tRNA
Use: tick-carried bact, acne; some CNS penetration; <em>fecally elim</em> - used in renal failure pts
Tox: GI, discolor teeth, inhib child bone growth (contra: preg), photosens
Notes: must not take with milk, antacids, or Fe-containing preparations (cations inhib abs)
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Term
Demeclocycline
Definition
Tetracycline (30S)
Mech: prevent attach. of aminoacyl-tRNA; ADH antag
Use: tick-carried bact, acne; some CNS penetration; <strong>diuretic in SIADH</strong>
Tox: GI, discolor teeth, inhib child bone growth (contra: preg), photosens
Notes: must not take with milk, antacids, or Fe-containing preparations (cations inhib abs)
Term
Minocycline
Definition
Tetracycline (30S)
Mech: prevent attach. of aminoacyl-tRNA
Use: tick-carried bact, acne; some CNS penetration
Tox: GI, discolor teeth, inhib child bone growth (contra: preg), photosens
Notes: must not take with milk, antacids, or Fe-containing preparations (2+ cations inhib abs)
Term
Erythromycin
Definition
Macrolide (50S)
Mech: binds 23S rRNA &rarr; blocks transloc
Use: URI, pneum, G(+) cocci STDs
Tox: GI (most com cause of noncompliance), acute cholestatic hep, eosinophilia, rashes
Interact: incr. theophylline &amp; oral anticoag conc.
Note: "MJ #23 throw up 50 atyp. &amp; has stds"
Term
Azithromycin
Definition
Macrolide (50S)
Mech: binds 23S rRNA &rarr; blocks transloc
Use: URI, pneum, G(+) cocci STDs; M. avium prophyl
Tox: GI (most com cause of noncompliance), acute cholestatic hep, eosinophilia, rashes
Interact: incr. theophylline &amp; oral anticoag conc.
Note: "MJ #23 throw up 50 atyp. &amp; has stds"
Term
Clarithromycin
Definition
Macrolide (50S)
Mech: binds 23S rRNA &rarr; blocks transloc
Use: URI, pneum, G(+) cocci STDs; M. avium prophyl
Tox: GI (most com cause of noncompliance), acute cholestatic hep, eosinophilia, rashes
Interact: incr. theophylline &amp; oral anticoag conc.
Note: "MJ #23 throw up 50 atyp. &amp; has stds"
Term
Chloramphenicol
Definition
Antibiotic (50S)
Mech: blocks peptidyltransferase activity
Use: meningitis (esp SHiN) (kills ~everything)
Tox: limits use; anemia (dose dep), aplastic anemia (dose indep), gray baby synd (premies lack UDP-glucuronyl transferase; contra: preg)
Contra: preg
Term
Clindamycin
Definition
Antibiotic (50S)
Mech: blocks peptide bond formation
Use: anaerobes (above diaphr) in asperation pneumonia.
= Bacteroides and C. Perfringens
Tox: pseudomembr colitis (dt C. Diff)
Term
Sulfamethoxazole
Definition
Sulfonamide
Mech: PABA antimetabolite &rarr; block dihydropteroate synthetase
Use: G(+)/(-), simple UTI
Tox: hypersens, hemolysis if G6PD defic, nephrotox, photosens, kernicterus (contra: preg)
Interact: displace drugs from albumin (warfarin)
Term
Sulfisoxazole
Definition
Sulfonamide
Mech: PABA antimetabolite &rarr; block dihydropteroate synthetase
Use: G(+)/(-), simple UTI (triple-sulf)
Tox: hypersens, hemolysis if G6PD defic, nephrotox, photosens, kernicterus (infant brain dmg)(contra: preg)
Interact: displace drugs from albumin (warfarin)
Term
Sulfadiazine
Definition
Sulfonamide
Mech: PABA antimetabolite &rarr; block dihydropteroate synthetase
Use: G(+)/(-), simple UTI (triple-sulf)
Tox: hypersens, hemolysis if G6PD defic, nephrotox, photosens, kernicterus (contra: preg)
Interact: displace drugs from albumin (warfarin)
Term
Trimethoprim
Definition
Mech: inhibs (bacterial) DHF reductase
Use: combo w/ sulfonamides for recurrent UTI, Shigella, Salmonella, PCP pneum
Tox: megaloblastic anemia, leukopenia, granulocytopenia (alleviate w/ suppl folinic acid - Leucovorin rescue)
Note: "TMP Treats Marrow Poorly"
Term
Sulfa allergy drug list
Definition
sulfonamides, sulfasalazine, sulfonylureas, thiazides, acetazolamide, furosemide, celecoxib, probenecid
Term
Ciprofloxacin
Definition
Fluoroquinolone ('cidal) - others: -flaxacin
Mech: inhib DNA gyrase (topo II)
Use: G(-) rods of GI &amp; urinary tract (inc pseudomona)
Tox: GI, rash, cartilage dmg (contra: preg), tendonitis/rupture in adults, leg cramps/myalgias in kids
Note: must not take w/ antacids
FlouroquinoLONEs hurt attachment to BONES
Term
Metronidazole
Definition
AB/antiprotozoal ('cidal)
Mech; forms toxic metabolites in bact. cell &rarr; DNA dmg
Use: protozoa (giardia...), anaerobes below diaphr,
triple therapy" vs H.pylori (+bismuth &amp; amox/tet)
Tox: disulfiram-like w/ alcohol
Term
Polymyxins
Definition
Mech: bind cell membr &amp; disrupt osmotic properties
Use: resistant G(-)
Tox: neurotox, acute tubular necrosis
PolyMYXins Mix up Membranes
Term
Pyrazinamide
Definition
Anti-TB
Mech; inhib membrane E's
effective in acidic pH of phagolysosomes (where TB engulfed by Macrophages is)
Tox: hepatotox
Term
Ethambutol
Definition
Anti-TB
Mech: inhibs arabinosoyl transferase &rarr; block cell wall arabinogalactan synth
(dec carbohydrate polymerization of myco wall)
Tox: optic neuropathy (red-green colorblind), hepatotox
Term
Isoniazid
Definition
Anti-TBMech: inhibs enoyl acyl carrier prot. reductase &rarr; blocks synthesis of mycolic acids (myco cell wall)
Use: TB prophylaxis (monotherapy) or tx
Tox: inactivates B6 (&amp; B3) &rarr; pellagra/neurotox (prevent w/ suppl pyridoxine); hepatotox
Note: diff t1/2 in fast vs. slow acetylators
Term
Rifampin
Definition
Anti-TBMech: inhibs RNApol &beta; S.U.
Use: TB, delays dapsone-resist in leprosy;
GC prophyl,H. influ b prophyl
Tox: hepatotox; red/orange body fluids (red urine)
Interact: &uarr; P-450&nbsp;
Term
Streptogramins
Definition
(50S); examples - quinopristin, dalfopristin
Use: VRE (can also use linezolid, 50S)
Term
Clavulanic acid
Definition
&beta;-lactamase inhibitor
Use: extend the spectrum of penicillin-family ABs
Term
Sulbactam
Definition
&beta;-lactamase inhibitor
Term
Tazobactam
Definition
&beta;-lactamase inhibitor
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