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Pharmacology > Antiviral drugs > Flashcards

Antiviral drugs Flashcards

1
Q

Foscarnet - what is indicated for?

A

Used for CMV retinitis in immunocompromised who have failed ganciclovir therapy

Also used for acyclovir-resistant HSV

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2
Q

Foscarnet- what is the mechanism?

A

Pyrophosphate analog, inhibits viral DNA polymerase, does NOT require activation by viral kinase

Resistance via mutated DNA polymerase

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3
Q

Foscarnet - what is the toxicity?

A

Nephrotoxicity (reversible w hydration and decreased dosage)

Electrolyte abnormalities -> mental status changes, paresthesias, seizures

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4
Q

NRTIs (Nucleoside Reverse Transcriptase Inhibitors) - what are examples and what are they indicated for?

A

Examples: Abacavir (ABC), didanosine (ddl), emtrictabine (FTC), lamivudine (3TC), stavudine (d4T), tenofovir (TDF), zidovudine (ZDV, formerly AZT)

Use: antiretroviral drugs to treat HIV

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5
Q

NRTIs (Nucleoside Reverse Transcriptase Inhibitors) - what is the mechanism of action?

A

Competitively inhibit nucleotide binding to reverse transcriptase and terminate elongating DNA chain

*must be activated in the cell and requires phosphorylation

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6
Q

What NRTI is used for HIV prophylaxis and pregnant women who are HIV positive?

A

Zidovudine (ZDV)

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7
Q

NRTI toxicity

A

Bone marrow suppression-> anemia, rash, neuropathy, pancreatitis (especially w EtOH), lactic acidosis

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8
Q

What can be given to reverse bone marrow suppression toxicity?

A

EPO and G-CSF (granulocyte colony-stimulating factor)

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9
Q

NNRTIs (Non-nucleoside reverse transcriptase inhibitor) - what are examples and what are they indicated for?

A

Ex: Delavirdine, efavirenz, nevirapine

Use:HIV and AIDS

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10
Q

NNRTIs (Non-nucleoside reverse transcriptase inhibitor) - what is their mechanism?

A

Inhibits reverse transcriptase at different site from NRTIs

*do NOT require intracellular activation or phosphorylation

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11
Q

NNRTIs (Non-nucleoside reverse transcriptase inhibitor) - what is their toxicity and contraindication?

A

Side effects: Rash, Hepatotoxicity, CNS symptoms and vivid dreams

Contraindicated: pregnancy, especially delavirdine and efavirenz are teratogenic

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12
Q

Protease inhibitors - what are examples and what are they indicated for?

A

“-navir” Ritonavir, indinavir

Indicated for HIV/AIDS and Hepatitis C

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13
Q

Protease inhibitors - what are their mechanism of action?

A

Inhibits viral protease -> virus cant cleave polyproteins into functional proteins -> inhibits maturation of new viruses

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14
Q

What are the side effects of protease inhibitors?

A

GI distress,
nephropathy (indinavir)
lipodystrophy (usually in face, and can cause buffalo hump),
hyperglycemia (can progress to DM type II)

P450 inhibition

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15
Q

Enfuvirtide - what is it used for? what is the mechanism? what are the side effects?

A

Used for HIV

Mechanism: fusion inhibitor, prevents penetration; binds to gp41 (HIV protein that penetrates host cell membrane) and interferes with ability to fuse with CD4+ cells -> inhibits viral entry

Side effect: skin rxn at injection site

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16
Q

Maraviroc - what is it used for? what is the mechanism?

A

Oral medication, Used for HIV

Mechanism: fusion inhibitor, prevents attachment; binds to CCR5 (chemokine receptor) on CD4+ T-cells and prevents interaction with gp120 -> inhibits HIV entry into host cell

17
Q

What are Integrase inhibitors used for and what are their mechanism of action and side effects?

A

“-gravir” raltegravir

Used for HIV

Mechanism: blocks insertion of viral genome, inhibit actions of integrase (enzyme used by virus to integrate viral genome)

side effects: hypercholesterolemia, insomnia

18
Q

When is HAART (highly-active antiretroviral therapy) indicated?

A

Used for patients with:

AIDS defining illness OR CD4+

19
Q

What drugs are included in HAART (highly-active antiretroviral therapy)

A

3 drugs:
2 NRTIs
+ 1 NNRTI or protease inhibitor or integrase inhibitor

20
Q

What is Cidofovir indicated for? What is its mechanism of action and side effects?

A

indicated for CMV retinitis in immunocompromised and acyclovir-resistant HSV

Mechanism: inhibits viral DNA polymerase, does not require phosphorylation by viral kinase, long half life

Side effect: dose-dependent nephrotoxicity (decreased when co-administered with probenecid and IV saline)

21
Q

Ribavirin - what is it indicated for? what is the mechanism and side effects?

A

Indicated for Hep C, viral hemorrhagic fevers and severe RSV (respiratory syncitial virus) (off-label)

Mechanism: inhibits inosine monophosphate dehydrogenase -> depletes GTP

Side effects: hemolytic anemia, teratogen

22
Q

Oseltamivir, zanamivir - what is their mechanism of action and clinical use?

A

Tamiflu!
Mechanism: inhibits influenza neuraminidase -> cant release progeny

Use: treatment and prevention of influenza A and B

23
Q

Acyclovir, famciclovir, valacyclovir- what is there mechanism of action and clinical use? what are their side effects?

A

Mechanism: guanosine analogs. Monophosphorylated by HSV/VZV thymidine kinase -> inhibits viral DNA polymerase by chain termination

Use: HSV and VZV mucocutaneous and genital lesions as well as encephalitis. Prophylaxis in immunocompromized. Famciclovir for herpes zoster

Toxicity: obstructive crystalline nephropathy and acute renal failure if not hydrated

24
Q

Ganciclovir - what is it used for? what is the mechanism and toxicity?

A

Mechanism: guanosine analog, monophosphorylated by CMV viral kinase -> inhibits viral DNA polymerase by chain termination

Use: CMV, especially in immunocompromised

Toxicity: leukopenia, neutropenia, thrombocytopenia and renal toxicity. More toxic than acyclovir

25
Q

Antihelminthic therapy

A

mebendazole, pyrantel pamoate, ivermectin, diethylcarbamazine, praziquantel

26
Q

INFalpha, beta and gamma - what is the mechanism, clinical use, and toxicity?

A

Mechanism: antiviral and antihumoral properties

INFalpha - Chronic Hep B and C, Kaposi sarcoma, hairy cell leukemia, condyloma acuminatum, renal cell carcinoma, malignant melanoma

INFbeta - MS

INFgamma- chronic granulomatous disease

Toxicity: neutropenia, myopathy

27
Q

Which drugs are used in Hepatitis C therapy?

A

Ribavirin, inhibits guanine nucleotide synthesis (toxicity- hemolytic anemia, teratogen)

Simeprevir, HCV protease inhibitor prevents viral replication, used in combo w/ ribavirin and pegINFalpha (toxicity- photosensitivity and rash) (do NOT use as monotherapy)

Sofosbuvir, inhibits RNA-dependent RNA polymerase -> chain termination, used in combo with ribavirin +/- IFNalpha (toxicity: fatigue, HA, nausea) (do NOT use as monotherapy)

28
Q

RSV treatment

A

Ribavirin in adults, palivizumab in children

Pharmacology (19 decks)

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