Antiviral 1

Question 1

Nucleoside analogues

Answer 1

Acyclovir Famciclovir Valacyclovir Panciclovir Ganciclovir Valganciclovir Cidofovir Trifluridine

Question 2

Nucleoside analogues - MoA

Answer 2

Prodrugs that are converted to monophosphate by virus enzymes, and then to active triphosphate metabolites by host enzymes. Competitive inhibition of viral DNA polymerase.

Question 3

Acyclovir - Clinical use

Answer 3

HSV, VZV Prophylaxis of CMV Chickenpox IV form: most effective treatment for serious herpesvirus infections, including herpetic encephalitis and severe HSV and VZV infections in immunocompromised patients Topical form: herpes genitalis and mild mucocutaneous infections in immunocompromised patients. In cases of herpes genitalis, however, topical form is less effective than oral form

Herpetic encephalitis

Question 4

Acyclovir - Adverse effects

Answer 4

Well tolerated Headache, GI disturbances, rash (General for all the nucleoside analoges) IV: phlebitis + reversible renal dysfunction

Question 5

Famciclovir - Clinical use

Answer 5

HSV VZV

Question 6

Valacyclovir - Clinical use

Answer 6

HSV, VZV Prophylaxis of CMV , such as in bone marrow and organ transplant recipients and in persons with HIV

Question 7

Panciclovir - Clinical use

Answer 7

Herpes labialis

Question 8

Ganciclovir - Clincal use

Answer 8

Prevent CMV diseases, including retinitis, esophagitis, and colitis HSV: keratitis (infection of the corneal epithelium) caused by HSV-1 and HSV-2

Question 9

Ganciclovir - Adverse effects

Answer 9

Leukopeina, thrombocytopenia Retinal detachment, liver and renal dysfunction

Question 10

Ganciclovir - Interactions

Answer 10

Severe myelosupression with zidovudine

Question 11

Valganciclovir - Clinical use

Answer 11

Prevent and treatment of less severe CMV infections, including those occurring in renal and heart transplant patients

Question 12

Cidofovir - Clinical use

Answer 12

Prevent CMV diseases resistant to ganciclovir

Question 13

Cidofovir - Contraindications

Answer 13

Contraindicated in patients taking other nephrotoxic drugs, such as aminoglycosides and amphotericin B.

Question 14

Cidofovir - Adverse effects

Answer 14

Nephrotoxicity, neutropenia, metabolic acidosis.

Question 15

Trifluridine - Clinical use

Answer 15

Ocular herpervirus infections, primarily herpetic epithelial keratitis and keratoconjuctivitis

Question 16

Pyrophosphate derivative (HSV drug)

Answer 16

Foscarnet

Question 17

Foscarnet - MoA

Answer 17

Blocks pyrophosphate-binding sites on viral DNA polymerase and prevents attachment of nucleotide precursor to DNA. Does not need activation by viral/host kinases.

Question 18

Foscarnet - Clinical use

Answer 18

CMV, VZV, HSV CMV retinitis in AIDS patients Acyclovir-resistant HSV infections Shingles Combined with ganciclovir to treat infections resistant to either drug alone because of their synergistic effect on viral DNA polymerase

Question 19

Foscarnet - Adverse effects

Answer 19

Renal impairment and acute renal failure, hematologic deficiencies, cardiac arrhythmias + heart failure, seizures, pancreatitis Renal toxicity can be minimized by administering intravenous fluids to induce diuresis before and during treatment

Question 20

Nucleoside reverse transcriptase inhibitors (NRTIs)

Answer 20

Didanosine Lamivudine Stavudine Emtricitabine Zidovudine (ZDV) Abacivir (ABC) Tenofovir

Question 21

Nucleoside reverse transcriptase inhibitors (NRTIs) - MoA

Answer 21

Triphosphate metabolites of the drug compete with nucleoside triphosphates for incorporation into viral DNA. Cause DNA chain termination. Inhibit host cell DNA polymerase somewhat.

Question 22

Nucleoside reverse transcriptase inhibitors (NRTIs) - Clinical use

Answer 22

HIV Some are active for Epstein-Barr virus and hepatitis B virus

Question 23

Nucleoside reverse transcriptase inhibitors (NRTIs) - Special considerations

Answer 23

Included in almost all HIV treatment regimens. Often more effective with multiple NRTIs (antimetabolites of different bases of DNA). Cross BBB. Careful with renal impairment

Question 24

Nucleoside reverse transcriptase inhibitors (NRTIs) - Adverse effects

Answer 24

Lactic acidosis, hepatic steatosis, lipodystrophy

Question 25

First line HIV drugs

Answer 25

Abacivir (ABC) Tenofovir Emtricitabine Lamivudine

Question 26

Alternative for 1st line drugs for HIV

Answer 26

Stavudine Didanosine

Question 27

ucleoside reverse transcriptase inhibitors (NRTIs) - For treatment of hepatitis B

Answer 27

Lamivudine Tenofovir

Question 28

Which NRTI is used to treat HIV in pregnant women?

Answer 28

Zidovudine (ZDV)

Question 29

Which NRTIs are not used together and why?

Answer 29

Zidovudine and stavudine because they appear to be antagonistic

Question 30

Abacavir - Adverse effects

Answer 30

Hypersensitivity reactions

Question 31

Which NRTIs cause Pancreatitis and Peripheral neuropathy

Answer 31

Didanosine and Stavudine

Question 32

Tenofovir - Adverse effect (the most important)

Answer 32

Renal impairment

Question 33

Zidovudine - Adverse effect (the most important)

Answer 33

Bone marrow suppression

Question 34

Nonnucleoside reverse transcriptase inhibitors (NNRTIs)

Answer 34

Efavirenz Nevirapine Delavirdine

Question 35

Nonnucleoside reverse transcriptase inhibitors (NNRTIs) - MoA

Answer 35

Direct inhibition of reverse transcriptase

Question 36

Nonnucleoside reverse transcriptase inhibitors (NNRTIs) - Clinical use

Answer 36

HIV

Question 37

Nonnucleoside reverse transcriptase inhibitors (NNRTIs) - Special considerations

Answer 37

Cross BBB Act synergistically with NRTIs and PIs against HIV. Never used alone for HIV

Question 38

Nonnucleoside reverse transcriptase inhibitors (NNRTIs) - Contraindications

Answer 38

Contraindicated for hepatic impairment

Question 39

Nonnucleoside reverse transcriptase inhibitors (NNRTIs) - Adverse effects

Answer 39

Moderately well tolerated Rash (can progress to Stevens-Johnson syndrome) Hepatotoxicity Drug interactions

Question 40

Which is the most potent NNRTI?

Answer 40

Efavirenz

Question 41

Efavirenz - Contraindications

Answer 41

Contraindicated during pregnancy

Question 42

Efavirenz - Adverse effects

Answer 42

Teratogenic Neuropsychiatric reactions

Question 43

Nevirapine - Interactions

Answer 43

Induces CYP3A4 + CYP2B6: Increases metabolism of certain drugs Increases metabolism of PIs, contraceptive steroids, other drugs

Question 44

Nevirapine - Adverse effects

Answer 44

Hepatotoxicity, rash (+Stevens-Johnson syndrome)

Question 45

Delavirdine - Special consideration

Answer 45

Usually not recommended for HIV (less potent)

Question 46

Protease inhibitors (PIs) (Most important)

Answer 46

Ritonavir Atazanavir Darunavir

Question 47

Protease inhibitors (PIs) - MoA

Answer 47

Bind HIV protease and inhibits proteolytic activity. Production of immature, noninfectious viral particles.

Question 48

Protease inhibitors (PIs) - Clinical use

Answer 48

HIV

Question 49

Protease inhibitors (PIs) - Adverse effects

Answer 49

Lipodystrophy, hyperlipidemia, insulin resistance and DM, liver dysfunction, hepatitis.

Question 50

Protease inhibitors (PIs) - Interactions

Answer 50

Inhibits metabolism of other drugs: PIs, antiarrhythmic agents, opioids, tricyclic antidepressants Nevirapine: Increase PI metabolism.