Antiretroviral, Antiparasitic, and Antiviral Drugs

Question 1

Converted to active triphosphates by host cell kinases, inhibit HIV RT and retroviral DNA chain termination, low affinity for host DNA polymerase, but can inhibit mitochondrial polymerase

Answer 1

Tenofovir-emtricitabine

Abacavir-lamivudine

Question 2

Bone marrow suppression and mitochondrial toxicity, (Tenofovir: decreased bone density, Abacavir: boxed warning for potentially fatal hypersensitivity reaction)

Answer 2

Tenofovir-emtricitabine

Abacavir-lamivudine

Question 3

Neurologic and psychiatric effects (Include dizziness, headache, insomnia, drowsiness, vivid dreams, depression, suicidality), rash, hyperlipidemia, and prolonged QT interval

Answer 3

Efavirenz

Question 4

Non-competitive inhibition of HIV-1 reverse transcriptase, does not require phosphorylation, does not inhibit host DNA polymerase, given in combination therapy

Answer 4

Efavirenz

Question 5

Comp. Inhibition of HIV protease, prevents cleavage of gag and pol polyproteins; virus fails to mature, human proteases not inhibited

Answer 5

Darunavir

Question 6

GI intolerance, hyperlipidemia, hyperglycemia

Answer 6

Darunavir

Question 7

Injection site reactions (common and persistent pain, erythema and cysts), elevated risk of bacterial pneumonia

Answer 7

Enfuvirtide

Question 8

Synthetic peptide mimic of HIV gp41 protein, binds to gp41 and prevents envelope from fusing with the CD4 T cell membrane (added to existing regimens if HIV replicates despite therapy)

Answer 8

Enfuvirtide

Question 9

Blocks the CCR5 co-receptor; prevents binding of gp120, only antiretroviral that targets a host protein

Answer 9

Maraviroc

Question 10

Boxed warning for hepatotoxicity

Answer 10

Maraviroc

Question 11

Weak base that becomes trapped in acidic parasite food vacuole (site of hemoglobin digestion), inhibits the parasitic biocrystallization of toxic hematin to non-toxic hemozoin (resistance due to mutated pfCRT efflux transporter)

Answer 11

Chloroquine

Question 12

Higher doses result in pruritis (itching), headaches, GI effects, and CV toxicity

Answer 12

Chloroquine

Question 13

First line oral treatment for MDR falciparum

Answer 13

Artemether

Question 14

Safe reputation, neurotoxicity and embryotoxicity demonstrated in animals

Answer 14

Artemether

Question 15

aken orally with chloroquine to achieve clinical and radical cure of vivax/ovale malaria; terminal prophylaxis after travel or primary prophylaxis before travel

Answer 15

Primaquine

Question 16

hemolytic anemia in G6PD deficient patients, pregnant women should avoid because fetal G6PD status is unknown

Answer 16

Primaquine

Question 17

Given in combination with a luminal amebicide to eradicate luminal survivors (GI levels are low due to complete oral absorption)

Answer 17

Metronidazole

Question 18

Aminoglycoside given alone for asymptomatic amebiasis of in combination for amebic colitis/dysentery, alternative to metronidazole in pregnancy (causes GI distress)

Answer 18

Paromomycin

Question 19

Inhibits polymerization of parasite β-tubulin, inhibiting formation of cytosolic microtubules (300x higher affinity than human tubulin)

Answer 19

Albendazole

Question 20

Generally well tolerated, teratogenic effects in animals (avoid use while pregnant), bone marrow suppression

Answer 20

Albendazole

Question 21

Mazzotti reaction (Immune reaction to dying worms that includes pruritis, rash, fever and lymphedema), teratogenic potential demonstrated in animals

Answer 21

Ivermectin

Question 22

Immobilization by tonic muscle paralysis, activates-gated Cl- channels found only in invertebrate neurons, causes hyperpolarization of the neuronal membrane, P-gp efflux transporter of blood brain barrier keeps drugs out of host CNS

Answer 22

Ivermectin

Question 23

CNS: tremors, nervousness, confusion, dizziness, ataxia,

Teratogenic in animals

Answer 23

Amantadine

Question 24

Blocks Influenza A M2 ion channel protein and blocks proton influx needed for viral uncoating (Does not bind Influenza B M2)

Answer 24

Amantadine

Question 25

Generally well tolerated, some nausea/vomiting, headaches

Answer 25

Oseltamivir (Tamiflu)

Question 26

drug (metabolized in liver to active carboxylate form) Analog of neuramic acid, comp. inhibitor of neuraminidase; prevents release of progeny virions for infected cell surface

Answer 26

Oseltamivir (Tamiflu)

Question 27

Used when Oseltamivir-resistant H1N1 influenza is suspected, low oral bioavailability, administered via inhalation as a dry powder

Answer 27

Zanamivir

Question 28

Bronchospasm and deterioration of lung function in patients with COPD

Answer 28

Zanamivir

Question 29

Prodrug converted by UGT1A3 to active form, inhibits cap-dependent endonuclease (viral protein important in RNA synthesis)

Answer 29

Baloxavir-Marboxil

Question 30

Mostly well tolerated, mild diarrhea

Answer 30

Baloxavir-Marboxil

Question 31

Prodrug converted to acyclo-GMP by viral thymidine kinase in cytosol, then converted to acyclo-GTP which is inserted not viral DNA by Viral DNA poly. Where it terminates chain elongation, also comp. inhibitor for viral DNA poly.

Answer 31

Acyclovir

Question 32

Reversible renal dysfunction from crystalline nephropathy, neurotoxicity

Answer 32

Acyclovir

Question 33

Similar to acyclovir (prodrug); converted to ganciclovir-MP by CMV UL97 kinase, converted to di/triphosphates by host kinases, triphosphate form inhibits viral DNA poly.

Answer 33

Ganciclovir

Question 34

Boxed warning for myelosuppression (neutropenia, thrombocytopenia) =major dose limiting toxicity, CNS effects (fever, chills, neuropathy, boxed warning for teratogenic/carcinogenic

Answer 34

Ganciclovir

Question 35

Prodrug, not dependent on viral TK phosphorylation, converted to active form by host kinases, diphosphate form comp. inhibits viral DNA poly.

Answer 35

Cidofovir

Question 36

Boxed warning for nephrotoxicity (proximal tube warning) and Neutropenia, possible carcinogen and teratogen

Answer 36

Cidofovir

Question 37

Inhibits herpesvirus DNA poly. (100x higher inhibition than mammalian DNA poly.)

Answer 37

Foscarnet

Question 38

Boxed warning for nephrotoxicity and seizures (related to electrolyte imbalance), symptomatic hypocalcemia

Answer 38

Foscarnet