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Flashcards in Antivirals Deck (29):
1

Prophylaxis against influenza A but not B; Blocks viral uncoating by interfering with influenza A M2 protein; SE: CNS effects

Amantadine

2

Prodrug; competitive inhibitor of influenza neuraminidases; interferes with viral release and viral penetration; Used for the treatment of uncomplicated influenza A and B; Give within 48 hours of symptom onset; SE: nausea/vomiting/diarrhea, bronchitis,

Oseltamivir

3

Inhibitor of nucleic acid synthesis; interferes with DNA synthesis; thymidine analog; Used opthalmic for Herpes simplex types 1 and 2

Trifluridine

4

Inhibits herpes DNA polymerase 10-30x more than host cell DNA polymerase; acts as a competitive inhibitor of dGTP and as a DNA chain terminator; Used IV, Oral and topical; generally well-tolerated, SE: rash, itching, nausea, vomiting, headache, fatigue

Acyclovir

5

Prodrug converted to penciclovir, then phosphorylated which is what inhibits viral DNA polymerase; Used for acute herpes zoster <3 days duration and for genital herpes

Famciclovir

6

Used for recurrent herpes of the lips and face; topical administration

Penciclovir

7

Monophosphorylation catalyzed by CMV protein kinase; Used for CMV retinitis in AIDS patients and for CMS prophylaxis for transplant patients; Toxicity: BM suppression, leukopenia, thrombocytopenia, anemia, may enhance bone marrow suppression when given with AZT

Ganciclovir

8

Inhibits CMV DNA polymerase by binding to its pyrophosphate-binding site; does not require conversion to triphosphate form to be active; Used for CMV retinitis and acyclovir-resistant herpes simplex

Foscarnet

9

Toxicity of Foscarnet

Renal damage, electrolyte imbalances, seizures

10

Nucleoside analog inhibitor of the reverse transcriptase domain of the hepatitis B DNA polymerase; approved for Hep B; SE: nausea, diarrhea

Lamivudine

11

Adenosine monophosphate analog, inhibits reverse transcriptase domain of the hepatitis B DNA polymerase; Approved for Hep B; SE: GI upset

Tenofovir

12

Interferes with viral mRNA synthesis; inhibits inosine-5-P dehydrogenase and thus GTP synthesis; inhibits GTP-dependent capping of viral mRNA; Used aerosol in infants and young children with severe RSV, and for Hep C (oral) in combo with interferon-a

Ribavirin

13

Toxicity of Ribavirin

Aerosol use: may precipitate in and clog respiratory equipment, pulmonary function deterioration, rash
IV or oral use: anemia, bm suppression

14

Used for condyloma acuminata, Hep B and C, used in combo with ribavirin for Hep C; Toxicity: flu-like symptoms, Leukopenia, BM suppression, neurotoxicity, myalgia

Interferon

15

Reversible inhibitor of Hep C NS3 protease, blocking formation of infectious virus particles; Used for Hep C genotype I in combo with PEG-interfereon + ribavirin; SE: anemia and neutropenia, contraindicated with drugs that are CYP3A substrates or inducers

Boceprevir

16

Thymidine nucleoside analog; phosphorylated by cellular kinases; inhibits reverse transcriptase and is a DNA chain terminator; Used for treatment of HIV in adults and children

Zidovudine or AZT

17

Toxicity of Zidovudine (AZT)
What types of drugs should be avoided if someone is on this drug?

Bone marrow suppression, neutropenia, anemia; drugs that inhibit glucuronyl transferase increase hematologic toxicity of AZT and should be avoided, myopathy

18

Nucleoside analog inhibitor of RT, synergistic with AZT; SE: nausea, diarrhea

Lamivudine

19

Nucleotide prodrug that is hydrolyzed to its active form, inhibits RT by competing with dATP for incorporation into DNA resulting in chain termination; used for combination therapy for HIV-infected patients

Tenofovir

20

Fluorinated analog of 3TC inhibits RT by competing for dCTP incorporation into DNA, resulting in chain termination; used as combo therapy for HIV

Emtricitabine

21

Nucleoside analog inhibitor of RT; used as combination therapy for HIV-infected patients; Toxicity: hypersensitivity reactions (assoc with HLA-B*5701 antigen)

Abacavir

22

Two other side effects associated with NRTI's as a group

lactic acidosis, hepatic steatosis

23

non-nucleoside inhibitor of RT; does not require phosphorylation for activity; Used as part of multi-drug therapy for HIV; SE: rash, CNS/psychiatric symptoms, nightmares

Efavirenz

24

Inhibitors of aspartic protease; used in combo with inhibitors of RT, significantly decrease viral blood load; Prevents viral protease from cleaving Gag-pol polypeptide into separate functional proteins

Lopinavir, Ritonavir

25

Toxicities of protease inhibitors

Diabetes, alterations in lipid metabolism, fat redistribution, alters metabolism of many other drugs
Lopinavir -- Diarrhea
Ritonavir -- avoid drugs metabolized by CYP3A

26

Effective against HIV-1 only, detectable viral replication despite ongoing therapy; inhibits fusion of viral (HIV-1) and cellular (CD4+) membranes, binds gp41 subunit of HIV glycoprotein, blocking membrane fusion; Toxicity: local injection site reactions, diarrhea, nausea, fatigue

Enfuvirtide

27

Chemokine co-receptor (CCR5) antagonist, blocks entry of HIV into cells; SE: hepatotoxicity, cardiovascular events

Maraviroc

28

Treatment of HIV-1, works on virus that is resistant to other drugs; inhibits HIV-1 integrate preventing integration of HIV-1 DNA into the genome

Raltegravir

29

How are drugs prescribed for HIV in clinic?

Used 3 (or more) drugs per patient (2 or more drug classes)
Keep replication at zero to prevent resistance