MOA

Question 1

Phenytoin

Answer 1

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

Question 2

5-fluorouracil (5FU)

Answer 2

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

Question 3

Codeine

Answer 3

Partially converted to morphine by CYP2D6

Question 4

Warfarin

Answer 4

Inhibits VKORC1→ ↓ synthesis of clotting factors

CYP2C9 responsible for inactivating warfarin

Question 5

Albendazole

Answer 5

Binds β-tubulin to inhibit
microtubule polymerization

Inhibit energy production

Metabolized by P450 enzymes to active metabolite albendazole sulfoxide

Question 6

Mebendazole

Answer 6

Binds β-tubulin to inhibit
microtubule polymerization

Inhibit energy production

Question 7

Ivermectin

Answer 7

Activates glutamate- gated Cl- channels → causing flaccid paralysis

Question 8

Pyrantel Pamoate

Answer 8

Stim nicotinic receptor

↑ACh release

Inhibit acetylcholinesterase

All → spastic paralysis

Question 9

Diethylcarbamazine

Answer 9

Alters worm surface mem and stimulates platelet aggregatio → immune resp

Stimulate host immune response

Question 10

Praziquantal

Answer 10

↑ membrane permeability to Ca2+ → spastic paralysis

Question 11

Artemisinins

Answer 11

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

Targets liver stages

Question 12

Chloroquine Phosphate

Answer 12

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

Question 13

Quinne Sulfate

Answer 13

Interferes with heme digestion

Question 14

Primaquine

Answer 14

Potentially converted to electrophilic intermediates

that mediate oxidation‐reduction rx → induces oxidative stress

Question 15

Atovaquone

Answer 15

Inhibits parasite mitochondrial electron transport

Question 16

Proguanil

Answer 16

Inhibits dihydrofolate reductase

Hepatic metabolism → polymorphism may affect metabaolsim

Question 17

Isoniazid (INH)

Answer 17

Bactericidal

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

Penetrates macrophages → effective against intra/extracellular organisms

Question 18

Pyrazinamide

Answer 18

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

Bacterialcydal

Question 19

Ethambutol

Answer 19

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

Question 20

Rifampin

Answer 20

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

No effect on eukaryote RNA polymerase

Question 21

Bedaquiline

Answer 21

Inhibits mycobacterial ATP synthase →. Not making energy and dies

Question 22

Polyenes (amp B and Nystatin)

Answer 22

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

Very broad spectrum of action

Fungicidal

Question 23

Azoles (fluconazole, itraconazole, voriconazole)

Answer 23

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

Selective for fungal P450

Question 24

Caspofungin

Answer 24

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

Question 25

Griseofulvin

Answer 25

``` Mitotic inhibitor (fungistatic) → interferes with microtubule assembly → bugs can’t divide ```

Question 26

Terbinafine | Lamisil

Answer 26

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

Question 27

Flucytosine

Answer 27

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

Question 28

Acyclovir

Answer 28

Metabolically activated via 3 phosphorylations Initial phosphorylation occurs via viral thymidine kinase Inhibits DNA synthesis

Question 29

Ganciclovir

Answer 29

Acycloc guanosine analog Requires tri-phosphorylation (similar to acyclovir) First phos catalyze by CMV kinase

Question 30

Valganciclovir

Answer 30

Pro-drug form of ganciclovir

Question 31

Foscarnet

Answer 31

Inhibits viral DNA polymerase, RNA polymerase, HIV RT No activation required

Question 32

Amantidine

Answer 32

Inhibit uncoating of viral RNA (inhibit M2 proton channel) NMDA antagonists (non-first line agents for Parkinson’s)

Question 33

Oseltamivir (Tamiflu)

Answer 33

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

Question 34

Zanamivir (Relenza)

Answer 34

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

Question 35

Anti-Influenza Agents

Answer 35

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

Question 36

Nucleoside Reverse Transcriptase Inhibitors (NRTIs)

Answer 36

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

Question 37

Abacavir

Answer 37

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

Question 38

Lamivudine

Answer 38

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

Question 39

Emtricitibine

Answer 39

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

Question 40

Tenofovir (AF/DF)

Answer 40

Nucleotide analog of adenosine Pro-drug → only requires 2 phosphorylation to become active Completely inhibits HIV RT → chain termination after incorporation into DNA

Question 41

Efavirenz

Answer 41

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

Question 42

HIV protease Inhibitors

Answer 42

Peptidomimetics Inhibit proteolyticcleavageofGagandGag-Polin HIV-1 and HIV-2 Do not require intracellular activation

Question 43

Ritonavir

Answer 43

Inhibitor of CYP3A4

Question 44

Enfuvirtide

Answer 44

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

Question 45

Maraviroc

Answer 45

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

Question 46

Doutegravir

Answer 46

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

Question 47

Ginko

Answer 47

Free radical scavenger Inhibits platelet aggregation ↑ blood flow

Question 48

St. John’s Wort 

Answer 48

Some components bind to GABA and 5-HT receptors

Question 49

Glucosamine 

Answer 49

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