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Pharm II Exam 4 > MOA > Flashcards

MOA Flashcards

1
Q

Phenytoin

A

Binds to and inhibits voltage-gated sodium channels (VGSC) in brain

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2
Q

5-fluorouracil (5FU)

A

Pyrimidine analog converted to 5FdUMP → inhibits TS activity in tumor cells

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3
Q

Codeine

A

Partially converted to morphine by CYP2D6

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4
Q

Warfarin

A

Inhibits VKORC1→ ↓ synthesis of clotting factors

CYP2C9 responsible for inactivating warfarin

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5
Q

Albendazole

A

Binds β-tubulin to inhibit
microtubule polymerization

Inhibit energy production

Metabolized by P450 enzymes to active metabolite albendazole sulfoxide

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6
Q

Mebendazole

A

Binds β-tubulin to inhibit
microtubule polymerization

Inhibit energy production

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7
Q

Ivermectin

A

Activates glutamate- gated Cl- channels → causing flaccid paralysis

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8
Q

Pyrantel Pamoate

A

Stim nicotinic receptor

↑ACh release

Inhibit acetylcholinesterase

All → spastic paralysis

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9
Q

Diethylcarbamazine

A

Alters worm surface mem and stimulates platelet aggregatio → immune resp

Stimulate host immune response

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10
Q

Praziquantal

A

↑ membrane permeability to Ca2+ → spastic paralysis

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11
Q

Artemisinins

A

Endoperoxide moiety is reduced by heme → free radical production → toxic environment → kills plasmodium

Targets liver stages

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12
Q

Chloroquine Phosphate

A

Plasmodium polymerizes heme to hemozoin which is non toxic but Chloroquine prevents this digestion → toxic to plasmodium

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13
Q

Quinne Sulfate

A

Interferes with heme digestion

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14
Q

Primaquine

A

Potentially converted to electrophilic intermediates

that mediate oxidation‐reduction rx → induces oxidative stress

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15
Q

Atovaquone

A

Inhibits parasite mitochondrial electron transport

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16
Q

Proguanil

A

Inhibits dihydrofolate reductase

Hepatic metabolism → polymorphism may affect metabaolsim

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17
Q

Isoniazid (INH)

A

Bactericidal

Converted by KatG in bacteria → activated drug →
Inhibits InhA and dihydrofolate reductase → inhibits mycolic acid synthesis

Penetrates macrophages → effective against intra/extracellular organisms

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18
Q

Pyrazinamide

A

Penetrates macrophages → converted into POA by mycobacterial enzyme (PcnA)→ blocks mycolic acid synthesis

Bacterialcydal

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19
Q

Ethambutol

A

Inhibits mycobacterial arabinosyl transferases (embAB operon) → enhances permeability of cell wall → bacteriostatic

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20
Q

Rifampin

A

Inhibits RNA synthesis → binds β subunit of bacterial DNA dependent RNA polymerase (rpoB)

No effect on eukaryote RNA polymerase

21
Q

Bedaquiline

A

Inhibits mycobacterial ATP synthase →. Not making energy and dies

22
Q

Polyenes (amp B and Nystatin)

A

Binds to ergosterol →
forms artificial membrane pores and leakage of intracellular ions and macromolecules out of fungal cell

Very broad spectrum of action

Fungicidal

23
Q

Azoles (fluconazole, itraconazole, voriconazole)

A

Block ergosterol synthesis by inhibiting fungal CYP450 enzyme (14-α-sterol demethylase)

Selective for fungal P450

24
Q

Caspofungin

A

Inhibits synthesis of β (1-3) glucan (cell wall synthesis inhibitor) →
disrupts fungal cell wall →
cells die

25
Q

Griseofulvin

A 
Mitotic inhibitor (fungistatic) →
interferes with microtubule assembly →
bugs can’t divide
26
Q

Terbinafine

Lamisil

A

Direct Fungicidal properties

Inhibits fungal enzyme (squalene epoxidase) →
↑ levels of squalene → which is toxic

27
Q

Flucytosine

A

Taken up by cytosine permeate in fungal cells →
converted to 5-FU by cytosine delaminates →
blocks DNA and RNA synthesis

28
Q

Acyclovir

A

Metabolically activated via 3 phosphorylations

Initial phosphorylation occurs via viral thymidine kinase

Inhibits DNA synthesis

29
Q

Ganciclovir

A

Acycloc guanosine analog

Requires tri-phosphorylation (similar to acyclovir)

First phos catalyze by CMV kinase

30
Q

Valganciclovir

A

Pro-drug form of ganciclovir

31
Q

Foscarnet

A

Inhibits viral DNA polymerase, RNA polymerase, HIV RT

No activation required

32
Q

Amantidine

A

Inhibit uncoating of viral RNA (inhibit M2 proton channel)

NMDA antagonists (non-first line agents for Parkinson’s)

33
Q

Oseltamivir (Tamiflu)

A

Neuraminidase inhibitors

Analogs of sialic acid = inhibit release of
progeny influenza by competing for enzyme

34
Q

Zanamivir (Relenza)

A

Neuraminidase inhibitors

Analogs of sialic acid = inhibit release of
progeny influenza by competing for enzyme

35
Q

Anti-Influenza Agents

A

Neuraminidase inhibitors

Analogs of dialect acid → inhibit release of progeny influenza by competing for enzyme

36
Q

Nucleoside Reverse Transcriptase Inhibitors (NRTIs)

A

Competitive inhibition of RT

incorporated into DNA → activated by cellular phosphorylation to triphosphate → prevents transcription

37
Q

Abacavir

A

Guanosine analog

Competitive inhibition of RT
incorporated into DNA → activated by cellular phosphorylation to triphosphate → prevents transcription

38
Q

Lamivudine

A

Cytosine anaolg → inhibits RT

Competitive inhibition of RT
incorporated into DNA → activated by cellular phosphorylation to triphosphate → prevents transcription

39
Q

Emtricitibine

A

Fluoridated analog of lamivudine

Competitive inhibition of RT
incorporated into DNA → activated by cellular phosphorylation to triphosphate → prevents transcription

40
Q

Tenofovir (AF/DF)

A

Nucleotide analog of adenosine

Pro-drug
→
only requires 2 phosphorylation to become active

Completely inhibits HIV RT → chain termination after incorporation into DNA

41
Q

Efavirenz

A

Binds directly to HIV-1 RT → inhibits RNA and DNA polymerase activity

Binding site is distinct site from NRTI (do not compete w/ NRTIs) → allosteric inhibition

42
Q

HIV protease Inhibitors

A

Peptidomimetics

Inhibit proteolyticcleavageofGagandGag-Polin HIV-1 and HIV-2

Do not require intracellular activation

43
Q

Ritonavir

A

Inhibitor of CYP3A4

44
Q

Enfuvirtide

A

Bids to gp41 subunit of viral envelope glycoproteins → prevents conformational changes req for fusion of viral cell mem → no entry pore formed

45
Q

Maraviroc

A

Bnds seelctively to CCR5 receptor (necessary for entrance of HIV into CD4+ cells) → HIV cannot enter

46
Q

Doutegravir

A

Inhibits viral DNA strand integration in host genome by binding to integrase and inhibiting it

47
Q

Ginko

A

Free radical scavenger

Inhibits platelet aggregation

↑ blood flow

48
Q

St. John’s Wort

A

Some components bind to GABA and 5-HT receptors

49
Q

Glucosamine

A

Possibly effective → principle component of GAGs that form CT matrix

Has anti- inflammatory properties

Need 2-4 weeks or longer to see effect, relief described as similar to ibuprofen

Pharm II Exam 4 (7 decks)

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