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24 Cards in this Set

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penicillins (chemistry and action)
1. Beta lactam ring fused to thiazolidine ring with side chain
2. bactericidal, T>MIC, irreversibly binds to penicillin-binding proteins (transpeptidases) which inhibits petidoglycan structure. cell lysis through osmotic pressure
natural penicillin
1. penicillin VK (PO), penicillin G (IV)
2. gram + aerobes (strep but not S. aureus)
3. tx: sensitive Streptococcus, group A strep pharyngitis, syphilis
penicillinase-resistant: nafcillin (IV), oxacillin (IV), methicillin, cloxacillin (PO), dicloxacillin (PO)
1. gram + aerobes (broad): MRSA, Strep. spp.
2. no gram - activity
3. different than other penicillins- liver metabolized, excreted in bile, highly bound
4. tx: MRSA (cellulitis, endocarditis)
extended spectrum penicillins (aminopenicillins, carboxypenicillins, ureidopenicillins)
Aminopenicillins: ampicillin (IV), amoxicillin (PO)
1. gram + aerobes (including Enterococcus) and some gram -
2. tx: enterococcal endocarditis, RTI, UTI, endocarditis prophylaxis

carboxypenicillins: Ticarcillin (IV)
1. less potent with gram + aerobes v. ampicillin. inc gram - activity
2. associated with electrolyte disturbances

Ureidopenicllins: Piperacillin (IV)
1. ~ to ampicillin, with inc gram -
tx: nocosomial
penicillin pharmacokinetics
1. absorption: most degraded by gastic acid. must be given IM or IV. (amoxicillin is oral)
2. Vd: distributes to most tissue. 5-20% of serum levels in CNS (must dose accordingly)
3.metabolism: minimal
4. excretion: renaly excreted in active form (helpful for UTI). dose adjustment for renal disease
penicillin adverse effects
1. hypersensitivity: skin rash, anaphylaxis, cross sensitivity between penicillin and cephalosporins
2. GI: nausea, ab pain, diarrhea (oral agents)
3. neuro: sz, coma, myoclonus
4. electrolyte: Na overload, hypo/hyperkalemia (high dose IV)
5. other: interstitial nephritis, eosinophilia, serum sickness, fever, hematologic effects
penicillin resistance
1. bacterial B-lactamase cleaves B-lactam ring and inactivates drug
2. alterations in PBP (MRSA)
3. alterations in outer membrane permeability (gram -)
Beta lactamase inhibitors: Clavulanic acid
1. mechanism: irreversible, non-competitive B-lactamase inhibitor
Carbapenems (imipenem/ cilastatin (IV), meropenem (IV), doripenem (IV), ertapenem (IV))
1. mechanism: similar to penicillin, T>MIC. cilastatin given with imipenem to prevent renal dehydropeptidase metabolism to nephrotoxic product
2. spectrum: very broad (last line). gram +/- activity (Pseudomonas), anaerobic, and extended spectrum beta lactamase (ESBL) organism
3. PK: only IV. similar to penicillin
4. adverse: GI problems, hypersensitivity (cross react with penicillin), higher sz incidence
Vancomycin
1. mechanism: inhibits glycopeptide cell wall synthesis. bactericidal. AUC/ MIC
2. gram + aerobes and anaerobes. (MRSA)
3. tx: MRSA, gram + infection with B lactams anaphylaxis, second line C.diff (PO)
4. PK: moderate Vd (poor CSF), excreted unchanged via renal (watch serum trough and adjust for renal disease)
5. adverse:
-"red man syndrome" with rapid IV infusion
- hematologic: neutropenia
-hypersensitivity: rash, anaphylaxis, vasculitis (desquamating skin rash and renal failure)
- ototoxicity and nephrotoxicity
5. resistance: enterococci (VRE), VISA, VRSA
Protein synthesis inhibitors: Aminoglycosides (gentamicin)
gentamicin (IV), tobramycin (IV), amikacin (IV)
1. mechanism: irreversibly binds to 30s ribosome causing misreading. bactericidal. Cmax/ MIC. PAE
2. spectrum: gram +/-. used with B-lactam ab for Staph, strept, enterococcus. activity against protozoa and mycobacteria
3. resistance: reduced 30s affinity, reduced intercellular transport, plasmid-mediated modifying enzymes
4. PK: requires IM/IV, Vd to extracellular space (highly polar. no CNS), excreted active in urine
5. adverse: nephrotoxicity (long term and with vanco), irreversible ototoxicity
gentamicIn irreversibly binds 30s
Protein synthesis inhibitors: tetracylines (doxycycline)
doxycyline (IV/PO), minocycline (PO), tetracycline (PO), tigecylcine (IV)
1. mechanism: reversibly binds to 30S. prevents tRNA binding. bacteriostatic
2. spectrum: (broad)
- gram+ aerobes (Strept and Staph. some MRSA)
- gram - (H.influenza
- gram - anaerobes
- RIckettsiae, lyme disease, brucellosis, cholera, syphilis, Chlamydia, Mycoplasm, Legionella
3. PK: oral (binds with Ca, Mg, Al, Fe [dairy products] thereby decreasing absorption), distributes to most tissue (concentrated in bile, liver, kidney, spleen, skin, bone)
-undergoes glucuronidation
-metabolites excreted in urine/ bile
4. adverse: photosensitivity (rash), tooth discoloration, GI,
5. contraindicated in pregnancy and children. alters calcification of bones and cartilage stability
tetra prevents tRNA binding
Protein synthesis inhibitors: Macrolides (azithromycin)
erythromycin (PO/IV), clarithromycin (PO), azithromycin (IV/PO), telithromycin (PO)
1. mechanism: reversibly binds 50S ribosome. bactericidal/ static (dose dependent)
2. spectrum
-erythromycin: gram + (Strep, Staph); gram - (H. influenza). less activity against anaerobes
-azithromycin: ~ to erythromycin, with more H. influenza activity and Chlamydia, Mycoplasm, Legionella activity
3. tx: RTI, pts. allergic to penicillin
4. PK: oral absorption; high Vd but no CNS (drug concentrates in neutrophils and macrophages); hepatic metabolism. acts as CYP450 inhibitor (many drug interactions! not as much with azithromycin); excreted in bile/ urine
5. adverse: GI, thrombophlebitis, cholestatic hepatitis, hearing loss, allergy (rare)
Protein synthesis inhibitors: Clindamycin (IV/PO)
1. mechanism: binds to 50S ribosome, inhibits protein synthesis, bacteriostatic
2. spectrum:
- gram + cocci (penicillin alternative)
- gram +/- anaerobes
- pulmonary, abdominal, pelvic infections, anaerobic coverage
3. PK:
-PO or IV. Vd to most tissue except CSF
- undergoes oxidative metabolism. excreted in urine/ bile in inactive state
4. adverse: diarrhea (C. diff overgrowth); allergy; metallic taste; neutropenia; thrombocytopenia
Protein synthesis inhibitors: others
Daptomycin
- binds to cell membrane, causes depolarization, and disrupts DNA/RNA/protein synthesis
- rapidly bactericidal
- gram + aerobes (MRSA, VRE)
- IV only
- highly protein bound
- minimal metabolism/ renal excretion

Quinupristin/ dalfopristin (IV):
-binds to 50S ribosome.
-bacteriostatic/ cidal dependent on organism
- gram + aerobes (MRSA and VRE faecium)
- high Vd, no CSF

Linezolid (IV/PO)
- binds 50S ribosome
- bacteriostatic
- gram + aerobes (MRSA, VRE)
- IV/ PO at same dose
- high Vd
- oxidized. renal and nonrenal elimination
- adverse effects with SSRI's because of MAO inhibition of drug
Nucleic acid/ chromatin structure inhibitors: Quinolones (levofloxacin)
1. mechanism: inhibit topoisomerase II (gyrase) and IV. arrests DNA replication
-bactericidal. Cmax/ MIC
2. spectrum
- 2nd generation (ciproflaxin, levofloxacin): some gram +, high gram - (Pseudomonas)
- 3rd generation (gatifloxacin, moxiflxacin): more gram + (S. pneumoniae)
-4th generation (trovafloxacin): anaerobic activity
3. tx: gram - infection, RTI, anthrax, gastroenteritis, osteomyelitis, prostatitis
4. PK: IV/PO. good absorption (including bone, prostate); renal excretion
5. adverse: GI upset, HA, dizzy, rash, photosensitivity, QT prolongation, hypo/hyperglycemia
6. contraindicated in pregnancy (affects cartilage development)
QT
Nucleic acid/ chromatin structure inhibitors: Nitroimidazoles (Metronidazole)
1. mechanism: damages DNA (reduction of nitro groups produces cytoxic products); bactericidal
2. spectrum: gram -/+ anaerobes, protozoa (amobea, giardia, trichomonas)
3. tx: C. diff, anaerobic infections
4. PK: high oral. IV/PO at same dose. high Vd (high CSF)
- hepatic metabolism to active metabolites. excreted in urine/ feces
-adjust for renal and hepatic disease!
5. adverse: metallic taste, disulfiram rxn (tx for ETOH abuse), peripheral neuropathy
nitro destroy DNA
Cephalosporins (cefazolin, cefuroxime, cefoxitin, ceftriaxone, cefepime)
1. similar action to penicillin
2. no action against Enterococci

1st generation: (Cefazolin (IV), Cephalexin (PO)
- broad gram + aerobes (strep, MSSA)
- narrow gram -
tx: skin infection, UTI, surgical prophylaxis

2nd generation: (Cefuroxime (IV/PO))
- less broad gram + aerobes (Strep, less staph)
- more gram - activity (not Pseudomonas)
- tx: RTI, CAP

3rd generation: (Ceftriaxone (IV))
- less gram + (strep less staph)
- broad gram -
- inc ability to cross CSF
- tx: PNA, gram -, meningitis

4th generation: Cefepime (IV)
- broad gram + aerobes (~to 1st)
- broad gram - aerobes (including Pseudomonas)
-tx: nocosomial

3. PK: ~ to penicillin
4. adverse: ~ to penicillin
Folate synthesis inhibitors: sulfamethoxazole and trimethoprim
1. mechanism
- sulfonamides: analogue of PABA, inhibits dihydropteroate synthestase, which converts PABA to dihyropteroaste, which is converted to folic acid
- Trimethoprim: inhibits DHF reductase, which converts DHF to THF (required for purine/ pyrimidine synthesis
- folate inhibitors are bacteriostatic
2. spectrum: gram + aerobes (MRSA), gram - aerobes, Listeria, Shigella, Pneumocystis jiroveci (fungus)
3. tx: UTI, PCP, Stenotrophomonas
4. adverse: exfoliative dermatitis, Stevens-johnson syndrome (hypersensitivity rxn-severe erythema multiforme), fever, pancytopenia (dec [RBC, WBC, platelets]), photosensitivity
5. contraindicated in near term pregnancy. risk of kernicterus
sulFa
Anti-mycobacterials (isoniazid, rifampin)
Isoniazid
1. mechanism: unstable electophilic inhibts cell wall mycolic acids. bactericidal (selective for mycobacteria)
2. spectrum: mycobacterium (M. tuberculosis-TB, M kansasii, M. xenopi)
3. adverse: hepatic toxicity (inc. with age), peripheral neuropathy

Rifampin
1. mechanism: blocks RNA polymerase. inhibits transcription. prokaryotic specific
2. spectrum: broad. mycobacterium, gram +/-, leprosy
3. PK: oral absorption, enters CSF, hepatic metabolism, eliminated with bile
4. induces cytochrome P-450 (many drug interactions)
isoniazid = ilectrophilic
rifampin= RNA inhibition
Antifungals: Amphotericin B
1. mechanism: binds to ergsterol leading to inc permeability. fungicidal
2. spectrum: yeasts (Candida, Cryptococcus, histoplasmosi, blastomycoses); molds (Aspergillus, mucormycosis)
3. PK: only IV, high Vd, renal excretion
4. adverse: affects cholesterol in mammals, causing cytokine release and nephrotoxicity; infusion related reactions, K and Mg wasting
tear the cell wall
Antifungals: Azoles (fluconazole)
1. mechanism: depletes [ergosterol] by inhibiting fungal P450 (converts lanosterol to ergosterol). cell wall instability. fungistatic

Fluconazole (IV/PO)
- active against Candida, Coccidioides, Cryptococcus (FCCC)
- IV or PO at same dose
- distributes to tissue and CSF
- some liver metabolism. excreted in urine

Itraconazole (PO)
- broad. active against Candida, Cryptococcus, coccidiodes, histoplasma, blastomycoses, aspergillus
- oral capsules need acidic environment. solution does not
- metabolized in liver and GI. excreted in bile and feces
- inhibits CYP3A4 (drug interactions)

Voriconazole (IV/PO)
- very good against Aspergillus
- IV or PO
- metabolized in liver and GI. excreted in bile and feces
Antifungals: Echinocandins
caspofungin (IV), micafungin (IV), anidulafungin (IV)
1. mechanism: inhibits synthesis of glucan (component of fungal cell wall)
2. spectrum: Candida, Aspergillus
3. tx: invasive candidiasis
4. PK:
-only IV
-highly bound
-hydrolysis and N-acetylation in liver (not by P450)
-eliminated in bile, feces, urine
5. adverse: nephrotoxicity, increased liver enzymes
Antifungals: Flucytosine (PO)
1. mechanism: enters fungal cell via cytosine permease (not found in mammals). deanimated and inhibits thymidylate synthetase, blocking DNA synthesis. fungistatic
2. spectrum: chromoblastomycosis. combo drug for candidiasis and cryptococcsis
3. PK: oral, distribution to CSF, excreted in urine
4.adverse: bone marrow toxicity. contraindicated in pts with depressed bone marrow and hepatic dysfunction