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pharm unit 6 mix > Antibiotics mechs > Flashcards

Antibiotics mechs Flashcards

1
Q

Penicillin G; Penicillin V

A

Complex with PBP, _ transpeptidase: _ cross-linking of peptidoglycans: _ cell wall synthesis

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2
Q

Oxacillin; Dicloxacillin; Nafcillin (Cloxacillin, Methicillin)

A

_ transpeptidase _ _ cell wall synthesis; bulky side group to stop _penicillinases

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3
Q

Ampicillin; Amoxicillin

A

Hydrophilic amino group _ encanced ability to pass through porins _ confers greater Gram negative activity. _ cell wall synthesis

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4
Q

Piperacillin; (Ticarcillin; Azlocillin; Carbencillin)

A

Carboxypenicillin: carboxyl R group allows penetration of porins in G(-) outer memb, _transpeptidase, _cell wall synthesis

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5
Q

Zosyn (Piperacillin + Tazobactam); Augmentin (Amoxicillin + Clavulanate)

A

Suicide inhibitor, binds to and inactivates _ _-Lactamase

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6
Q

Cefazolin; Cephalexin

A

Bacteriocidal: bind and for complex with PBP, _ transpeptidase: _ cross-linking of peptidoglycans: _ cell wall synthesis; relatively resistant to most (not all) _-Lactamases; Resistance via Transpeptidase mutations, _-Lactamases (esp in G-), Enterococci inherently resistant to cephaosporins

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7
Q

Cefuroxime (IV); [Cefaclor (PO), Cefuroxime (PO)]

A

Bacteriocidal: bind and for complex with PBP, _ transpeptidase: _ cross-linking of peptidoglycans: _ cell wall synthesis; relatively resistant to most (not all) _-Lactamases; Resistance via Transpeptidase mutations, _-Lactamases (esp in G-), Enterococci inherently resistant to cephaosporins

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8
Q

Ceftazadime (IV); Cefpodoxime (PO); Ceftriaxone (IV)

A

Bacteriocidal: bind and for complex with PBP, _ transpeptidase: _ cross-linking of peptidoglycans: _ cell wall synthesis; relatively resistant to most (not all) _-Lactamases; Resistance via Transpeptidase mutations, _-Lactamases (esp in G-), Enterococci inherently resistant to cephaosporins

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9
Q

Cefepime

A

Bacteriocidal: bind and for complex with PBP, _ transpeptidase: _ cross-linking of peptidoglycans: _ cell wall synthesis; relatively resistant to most (not all) _-Lactamases; Resistance via Transpeptidase mutations, _-Lactamases (esp in G-), Enterococci inherently resistant to cephaosporins

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10
Q

Imipenem (given w/ Cilastin)

A

Complex with PBP, _ transpeptidase: _ cross-linking of peptidoglycans: _ cell wall synthesis; Highly resistant to _-Lactamases; Broadest Spectrum of Activity of all antibacterials

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11
Q

Aztreonam

A

_ transpeptidase: _ cell wall synthesis, unique peptidoglycan targets, resistant to _-Lactamases

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12
Q

Vancomycin

A

Binds rapidly and irreversibly to the D-alanyl-D-alanine muramyl pentapeptide of cell wall precursors _ _ polymerization of peptidoglycans

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13
Q

Daptomycin

A

Penetrates bacterial cell wall, forming a channel for subsequent leakage of intracellular ions

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14
Q

Colistin (Polymyxin E); Polymyxin B

A

Cationic detergents _ Distortion of the membrane lipid structure, _ permeability to polar molecules, via channel

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15
Q

Ciprofloxacin; (Lomefloxaci, Norfloxacin, Oflaxacin)

A

Inhibits _DNA gyrase (Topo II) (supercoiling control), and _Topoisomerase IV (untangling daughter Chr), traps enzyme on DNA

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16
Q

Levofloxacin

A

Inhibits _DNA gyrase (Topo II) (supercoiling control), and _Topoisomerase IV (untangling daughter Chr), traps enzyme on DNA

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17
Q

Metronidazole

A

Reductive bioactivation via ferredoxins (in anaerobic bacteria, some protozoa) cytotoxic free radicals react with & damages DNA, protein, or bacterial membranes

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18
Q

Rifampin

A

Inhibits _ RNA Polymerase _ _ mRNA transcription; resistance: RNA poly (_) mutation

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19
Q

Gentamicin; Tobramycin; (Neomycin, Streptomycin; Amikacin)

A

O2-dependent uptake (anaerobes innately resistant); binds 30S ribosome _ premature termination, mistranslation (bacteriacidal), _ initiation of translation

20
Q

Doxycycline; (Tetracycline, Minocycline, Dmeclocycline, Tigecycline)

A

Reversibly binds 30S Ribosome Subunit: block access of _aminoacyl tRNA to its codon (bacteriostatic); imported via energy-dependent active transport lacking in humans

21
Q

Clindamycin

A

Binds 50S Ribosome at A site _blocking _peptidyl transferase _peptide bond synthesis

22
Q

Azithromycin (Z pack); (Erythromycin, Clarithromycin, Telithromycin)

A

Reversibly binds 50S subunit _ _translocation via interference with tRNA release; unrelated -agonist at Motilin R. _ _ GI Motility; Resistance via methylation of tRNA

23
Q

Linezolid

A

Binds 50S Ribosome and inhibits _ peptidyl transferase

24
Q

Quinupristin-Dalfopristin

A

Binds 50S Ribosome and inhibits _ amino-acyl tRNA interaction with acceptor site

25
Q

Trimethoprim

A

Folic Acid analogue, inhibits DiHydroFolate Reductase _DHFR _(DHF _ THF), _bacterial recycling of folate, _Purines, AA synthesis

26
Q

Sulfamethoxazole

A

PABA analogue, competitively _ dihydropteric synthetase _(PABA _DHF) _DNA synthesis, selective (humans lack de novo folate)

27
Q

Isoniazid (INH)

A

Prodrug, activated by catalase-peroxidase (KatG) _INH binds enol-ocyl reductase (InhA), _ disrupting _mycolic acid synthesis

28
Q

Pyrazinamide

A

Prodrug; activated by PZase_ pyrazinoic acid_ inhibits mycobacterial fatty acid synthetase I _ _C16, C24 FA, required for mycolic acid synthesis

29
Q

Ethambutol

A

Inhibits _ arabinosyl transferases (EmbAB) _ cell wall biosynthesis (arabingalactan)

30
Q

Acyclovir

A

Phosphorylated acycloGMP via viral Thymidine Kinase. acycloGTP _ Chain terminator (no 3’OH) & _viral DNA polymerase inhibitor

31
Q

Ganciclovir

A

Triphosphate form _ Chain terminator & _viral DNA polymerase inhibitor.

32
Q

Foscarnet

A

Inhibits _viral DNA polymerase without need for activation; also _RNA polymerase inhibition

33
Q

Oseltamivir; (Zanamivir)

A

Prevent viral release from host cells

34
Q

Zidovudine (AZT, ZDV, Azidothymidine)

A

Thymidine analog, tri-phosphorylated by viral enzymes, inhibits HIV’s _reverse transcriptase _chain termination; blocks spread of infection; Resitance via mutations in RT

35
Q

Lamivudine; (Emtricitabine)

A

Thymidine analog, tri-phosphorylated by viral enzymes, inhibits HIV’s _reverse transcriptase _chain termination; blocks spread of infection; Resitance via mutations in RT

36
Q

Efavirenz; (Nevirapine, Delaviradine; Etravirine)

A

High affinity, binds (not at catalytic site), _ inhibits HIV’s RT do not require metabolic activation

37
Q

Ritonavir/Lopinavir; Amprenavir

A

reversibly inhibits _ HIV protease (cleaves HIV polyproteins [gag, gag-pol] to functional parts) virions are packaged but don’t mature or infect

38
Q

Boceprevir; Telapravir

A

Prevents_ HCV serine protease cleavage of HCV protein into functional subunits

39
Q

Enfurvitide

A

Binds first Heptad Repeat (HR1) in _ gp41 envelope glycoprotein, prevents conformational changes require for _fusion to cell membrane

40
Q

Maraviroc

A

Binds CCR5 receptor on macs, T-cells, dendritic cells, preventing HIV from using CCR5 as a co-receptor _entry of CCR5-tropic HIV

41
Q

Raltegravir

A

Reversibly inhibits _HIV integrase, preventing viral genome transfer to host cell chromosome

42
Q

Amphotericin B

A

Binds membrane sterols: _memb. permeability (via pores) _ leakage of K+ and Mg+; selectivity via higher affinity for ergosterol (fungal) vs. cholesterol (mammalian)

43
Q

Nystatin

A

Binds membrane sterols: _memb. permeability (via pores) _ leakage of K+ and Mg+; selectivity via higher affinity for ergosterol (fungal) vs. cholesterol (mammalian)

44
Q

Clotrimazole; Fluconazole (Voriconazole, Terconazole, Posaconazole, Itraconazole)

A

inhibits 14--demethylase (a P450 dependent microsomal enzyme): _ lanosterol _ ergosterol. Destabilizes fungal membrane

45
Q

Terbinafine (Lamisil); Tolnaftate

A

Inhibits _ Squalene Epoxidase _ ergosterol synthesis. Destabilizes fungal membrane. Accumulation of squalene is toxic

46
Q

Caspofungin

A

Inhibits _ glucan synthase complex _ synthesis of _(1,3)-D-Glucan

47
Q

Flucytosine

A

Prodrug activated via fungal cytosine deaminase _ 5-fluorouracil, 5-FU + _ _ 5FdUMP _ active inhibitor of _ Thymidylate synthetase

pharm unit 6 mix (4 decks)

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