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Flashcards by lola_smily, updated more than 1 year ago
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Created by lola_smily
over 9 years ago
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| Question | Answer |
| Clarithromycin macrolide semi-synthetic Rapid absorption from GI 50% bioavailability No effect of food on absorption Extensive distribution longer t ½ 3-7hrs MOA: bind to 50S (reversibly): inhibit protein synthesis Metabolism (in the liver) → 14-hydroxy metabolite (active) of t1/2=5-9 hrs Excretion: renal (mainly) DDI: CYP3A4 inhibitor | |
| Azithromycin macrolide Azalide semi-synthetic ring-expanded analogue of erythromycin (N-methyl inserted between C9 and C10 → 15-membered lactone ring) Orally active 37% bioavailability Food decreases absorption by 40% t1/2: 68h --> very long MOA: bind to 50S (reversibly): inhibit protein synthesis Undergoes extensive distribution and metabolism Metabolism: hepatic to inactive metabolite Excretion: 90% biliary | |
| Dirithromycin prodrug semi-synthetic t1/2= 30-40h --> long MOA: bind to 50S (reversibly): inhibit protein synthesis metabolism: hydrolysis of 9N-11O-oxazine --> erythromycylamine (active metabolite ) before absorption | |
| telithromycin ketolide 14 membered ring (like erythromycin) Ketone at position 3 11-12 cyclic carbamate Orally active T1/2=6-10h MOA: bind to 50S (reversibly): inhibit protein synthesis Post antibiotic effect (against respiratory tract pathogens) Metabolism: extensively (in liver) to inactive mtb by CYP3A4 (50%), non CYP3A4 (50%) Excretion: fecal (75%), urinary (unchanged) SE: GI discomfort (diarrhea, nausea) DDI: CYP3A4, CYP2D6 competitive inhibitor | |
| chloramphenicol bacterial protein synthesis inhibitor nitrobenzene derivative natural (from streptomyces venezuella) active against gram+ and gram- MOA: inhibit 50S subunit --> inhibit mitochondrial protein synthesis in mammalian cells orally active very well and rapidly absorbed from GI bitter taste found as palmitate ester and succinate ester high lipid soluble cross: CSF, placenta t1/2= 4h metabolism: extensive glucuronidation not given for elderly, infants excretion: renal SE: hematological (leukopenia, thrombocytopenia, pancytopenia), hemolysis (in G6PD deficient patient), gray baby syndrome, hypersensitivity | |
| linezolid bacterial protein synthesis inhibitor oxazolidine derivative active against gram+, aerobic and anaerobic (less against gram-) active against some MRSA MOA: bind to 50S (unique binding site)--> synergistic effect orally active (100% bioavailable) poor ppb widely distributed t1/2= 4-6h metabolism: to inactive excretion: renal SE: well tolerated, GI disturbance, headache, dizziness, weak MAOI | |
| lincomycin bacterial protein synthesis inhibitor lincosamide 8C sugar, thiomethyl amino-octoside weekly basic (pyrrolidine) form acid salts for serious infections (cause colitis --> fatal) metabolism: to clindamycin | |
| clindamycin bacterial protein synthesis inhibitor lincosamide 7-chloro-7-deoxylincomycin weekly basic (pyrrolidine) form acid salts MOA: bind to 50S--> inhibit protein synthesis cross resistance with erythromycin orally highly absorbed (90%) found in ester form: palmitate (pediatric), phosphate --> IV/IM widely distributed (bones) no CSF entry 90% ppb t1/2= 2-4h metabolism: in liver--> sulfoxide (inactive), N-demethyl mtb (active) excretion: renal SE: GI disturbance, skin rash, pseudomembranous colitis | |
| nalidixic acid first generation old quinolone bacterial nucleic acid synthesis inhibitor | |
| cinoxacin first generation old quinolone bacterial nucleic acid synthesis inhibitor | |
| ciprofloxacin fluoroquinolone bacterial nucleic acid synthesis inhibitor have piperazinyl moiety: most significant antimicrobial improvement piperazinyl at C7 increases binding to GABA: CNS stimulation FDA warning: cause retinal detachment (permanent blindness) orally/IV chelate polyvalent metal ions concentration: high in urine, kidney, lung, prostate tissue, stool, bile, macrophage metabolism: minimally in liver (15-20%) mainly renal excretion SE: GI disturbance, CNS effect (insomnia, seizure), nephrotoxicity (due to crystalluria), allergic reaction, phototoxicity | |
| moxifloxacine fluoroquinolone bacterial nucleic acid synthesis inhibitor have pyrrolidinyl moiety: most significant antimicrobial improvement is predominantly metabolized in the liver orally chelate polyvalent metal ions concentration: high in urine, kidney, lung, prostate tissue, stool, bile, macrophage metabolism: minimally in liver (15-20%) mainly renal excretion SE: GI disturbance, CNS effect (insomnia, seizure), nephrotoxicity (due to crystalluria), allergic reaction, phototoxicity | |
| lomefloxacin fluoroquinolones bacterial nucleic acid synthesis inhibitor alkyl substitution on the piperizine decreases binfing to GABA highest potential for photosensitivity orally chelate polyvalent metal ions concentration: high in urine, kidney, lung, prostate tissue, stool, bile, macrophage metabolism: minimally in liver (15-20%) mainly renal excretion SE: GI disturbance, CNS effect (insomnia, seizure), nephrotoxicity (due to crystalluria), allergic reaction, phototoxicity | |
| ofloxacin fluoroquinolones bacterial nucleic acid synthesis inhibitor alkyl substitution on the piperizine decreases binding to GABA orally/IV chelate polyvalent metal ions concentration: high in urine, kidney, lung, prostate tissue, stool, bile, macrophage metabolism: minimally in liver (15-20%) mainly renal excretion SE: GI disturbance, CNS effect (insomnia, seizure), nephrotoxicity (due to crystalluria), allergic reaction, phototoxicity | |
| sparfloxacin fluoroquinolone bacterial nucleic acid synthesis inhibitor C8 fluoro increases activity but increases photosensitivity heterocyclic at C7 improves the spectrum of activity mainly gram -ve bulky group at N1, substitution on piperazinyl ring on C7 decrease binding to GABA cyclopropyl substitution at N1 broaden spectrum of activity orally chelate polyvalent metal ions concentration: high in urine, kidney, lung, prostate tissue, stool, bile, macrophage metabolism: minimally in liver (15-20%) mainly renal excretion SE: GI disturbance, CNS effect (insomnia, seizure), nephrotoxicity (due to crystalluria), allergic reaction, phototoxicity | |
| levofloxacin S(-) isomer is twice as active as ofloxacin and less toxic than R(+) resulting from increased binding to the DNA gyrase(topoisomerase 2): gram-ve | |
| gatifloxacin fluoroquinolone bacterial nucleic acid synthesis inhibitor substitution at C8 reduce the photosensitivity orally chelate polyvalent metal ions concentration: high in urine, kidney, lung, prostate tissue, stool, bile, macrophage metabolism: minimally in liver (15-20%) mainly renal excretion SE: GI disturbance, CNS effect (insomnia, seizure), nephrotoxicity (due to crystalluria), allergic reaction, phototoxicity | |
| nitrofurantoin bacterial nucleic acid synthesis inhibitor nitrofuran derivative bacteriostatic against gram-ve and gram+ve including E.coli and urinary tract pathogens for UTI cause DNA damage (by strand breaking) more active in acidic urine may develop resistance (due to loss of nitroreductase) orally active concentrated in urine t1/2= 0.5-1.2h short excretion: kidney (urine discoloration: brown) SE: anemia G6PD deficiency,acute pneumonitis and pulmonary fibrosis neurological problems and neuropathy, GI effect, hypersensitivity | |
| methenamine bacterial nucleic acid synthesis inhibitor hexamethylenetetramine prodrug at ph5 20% is converted to formaldehyde (active) while at Ph7 only 6% is converted formulated with mandalic acid and hipuric acid |
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