Antivirals Flashcards Preview

Pharmacology Block 3 > Antivirals > Flashcards

Flashcards in Antivirals Deck (23):
1

Amantadine:

MOA: Blocks viral uncoating by interfering with influenza A M2 protein.

Uses: -Prophylaxis against influenza A (NOT influenza B).
-Therapeutic against influenza A if given within the first 2 days of illness.

2

Tamiflu:

MOA: Prodrug, competitive inhibitor of influenza NA; interferes with viral release and viral penetration.

Uses: -Treatment of uncomplicated influenza A and B; must be given within 48 hrs of symptom onset.
-Influenza prophylaxis.

3

Trifluridine:

MOA: Interferes with DNA synthesis; thymidine analog.

Uses: -Treatment of ophthalmic Herpes simplex types 1 and 2.

4

Acyclovir:

MOA: Inhibits herpes DNA polymerase (almost exclusively); phosphorylated form is produced much more rapidly in infected cells via herpes thymidine kinase. Acts as a competitive inhibitor of dGTP and as a DNA chain terminator.

Uses:
-IV: Systemic herpes infection and severe initial genital herpes.
-Oral: Primary genital herpes, primary herpetic gingivostomatosis.
-Topical: Some effect when applied early to primary genital herpes.

5

Famciclovir:

MOA: Similar to acyclovir, but is a prodrug that is converted to penciclovir, which is then phosphorylated intracellulary by herpes thymidine kinase, which then inhibits viral DNA polymerase.

Uses: -Shingles infections.
-Recurrent genital herpes.

6

Penciclovir:

Similar to acyclovir, but only used topically against herpes of the lips and face.

7

Ganciclovir:

MOA: Similar to acyclovir, but phosphorylation is carried out via CMV protein kinase.

Uses: -CMV retinitis.
-CMV prophylaxis for transplant recipients.

SEs: Bone marrow suppression.

8

Foscarnet:

MOA: Inhibits CMV DNA polymerase by binding to its pyrophosphate-binding site. Does not require conversation to triphosphate form to be active.

Uses: -CMV retinitis.
-Acyclovir-resistant herpes simplex (thymidine kinase mutations).

SEs: Renal damage.

9

3TC:

MOA: Nucleoside analog inhibitor of the RT domain of the hep B DNA polymerase.

Uses: -Hep B
-Synergistic with AZT in the treatment of HIV.

10

Tenofovir:

MOA: Nucleotide inhibitor of the RT domain of the hep B DNA polymerase.
For HIV: inhibits RT by competing with dATP for incorporation into DNA, resulting in chain termination.

Uses: -Hep B.
-Given in combination therapy for HIV-infected patients.

11

IFN-alpha:

Uses: -Condyloma cuminata
-Hep B and C
-Pegylation decreases clearance (higher and prolonged plasma concentrations).

SEs: Flu-like symptoms, bone marrow suppression.

12

Ribavirin:

MOA: Inteferes with viral mRNA synthesis; inhibits GTP synthesis, and thus inhibits GTP-dependent capping of viral mRNA.

Uses: -Aerosol use in infants and young children with documented severe RSV infections.
-Given in combination with PEG-IFNa for Hep C.

SEs: Aerosol use: drug may precipitate in respiratory equipment.
-Pulmonary function deterioration.
IV use: bone marrow suppression.

13

Simeprevir:

MOA: Reversibly inhibits hep C NS3/NS4A protease, thus blocking cleavage of the polyprotein and formation of infectious virus.

Uses: -hep C genotype 1
-Always in combination with other drugs.

SEs: -Rash (photosensitivity)
-GI effects
-Avoid using with inducers or inhibitors of CYP3A.

14

Sofosbuvir:

MOA: Prodrug; triphosphate form inhibits HCV NS5B RNAP causing chain termination.

Uses: -hep C genotypes 1,2,3,4.
-Combination with other drugs.

SEs: Avoid with inducers of Pgp.

15

AZT:

MOA: NRTI; phosphorylated by cellular kinases. Inhibits RT, and also acts as a DNA chain terminator.

Uses: Combination therapy for HIV therapy.

SEs: -Bone marrow suppression.
-Drugs which inhibit glucoronyl-transferase increase hematologic toxicity.

16

FTC:

MOA: Fluorinated analog of 3TC that inhibits RT by competing for dCTP incorporation into DNA, resulting in chain termination.

Uses: Combination therapy for HIV.

17

ABC:

MOA: Inhibits viral RT.

Uses: Combination therapy for HIV.

SEs: Hypersensitivity reactions associated with HLA-B*5701 antigen.

18

Efavirenz:

MOA: Non-nucleoside inhibitor of RT; does not require phosphorylation for activity.

Uses: Combination therapy for HIV.

SEs: CNS effects, nightmares.

19

Lopinavir:

MOA: Protease inhibitor; prevents cleavage of Gag-pol polypeptide into separate functional proteins; results in non-infectious viral particles.

Uses: Use in combination with a RT inhibitor for treatment of HIV.

SEs: Redistribution of fat, diabetes.

20

Ritonavir:

MOA: Inhibits CYP3A and enhances the efficacy of other protease inhibitors.

Uses: Use as a protease inhibitor booster.

21

Enfuvirtide:

MOA: Inhibits the fusion of viral and cellular membranes by binding to gp41 subunit of HIV glycoprotein.

Uses: -Effective against HIV-1 only.
-Treatment of strains resistant to other drugs.

22

Maraviroc:

MOA: CCR5 antagonist. Blocks entry of HIV into cells.

Uses: -Treatment of CCR5-tropic HIV-1.
-CCR5-tropic strains tend to predominate early in infection.

SEs: Hepatic and cardiac effects.

23

Raltegravir:

MOA: -Inhibits HIV-1 integrase, preventing integration of HIV-1 DNA into the genome.

Uses: -Treatment of HIV-1, works on virus strains resistant to other drugs.