Antivirals Flashcards

1
Q

Zanamivir, Oseltamivir MECH

A

Inhibit influenza neuramidase, decreasing the release of progeny virus.

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2
Q

Zanamivir, Oseltamivir USE

A

TX & prophy influenza A & B

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3
Q

Ribavarin MECH

A

Inhibits synth of guanine nucleotides by competitively inhibiting IMP dehydrogenase - stops duplication of viral genome.

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4
Q

Ribavarin USE

A

RSV, Chronic Hep C

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5
Q

Ribavarin TOX

A

Hemolytic anemia, teratogen

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6
Q

Acyclovir Mech

A

Monop’lated by HSV/VZV thymidine kinase. Guanosine analog. Triphosphate formed by cellular enzymes. Preferentially inhibits viral DNA pol by chain termination.

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7
Q

Acyclovir USE

A

HSV & VZV. Weak act against EBV. None against CMV. Used for HSV-induced mucocutaneous & genital lesions, encephalitis. Prophy in immunocompromised patients. No effect on latent HSV & VZV. Valacyclovir has better bioavailability. For herpes zoster use a related agent, famcyclovir

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8
Q

Acyclovir TOX

A

few serious

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9
Q

Acyclovir RESIST

A

mutated viral thymidine kinase

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10
Q

Ganciclovir MECH

A

5’-monophosphate formed by a CMV viral kinase. Guanosine analog. Triphosphate formed by cellular kinases. Preferentially inhibits viral DNA pol

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11
Q

Ganciclovir USE

A

CMV, esp immunocompromised. Valganciclovir = prodrug ganciclovir w/better bioavailability.

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12
Q

Ganciclovir TOX

A

leukopenia, neutropenia, thrombocytopenia, renal tox, More toxic to host enz than acyclovir.

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13
Q

Ganciclovir RESIST

A

mutated CMV DNA pol or lack of viral kinase

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14
Q

Foscarnet MECH

A

Viral DNA pol, RNA pol, & reverse transcriptase inhibitor that binds the pyrophosphate binding site of enz. Does not require activation by viral kinase

Foscarnet = pyroFOSphate analog

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15
Q

Foscarnet USE

A

CMV retinitis in immunocompromised patients (AIDS) when ganciclovir fails; acyclovir-resistant HSV

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16
Q

Foscarnet TOX

A

Nephrotox, hypOcalcemia, hypOmagnesemia, seizures

17
Q

Foscarnet RESIST

A

Mutated DNA pol

18
Q

Cidofovir MECH

A

Preferentially inhibits viral DNA pol. Does NOT require p’lation by viral kinase

19
Q

Cidofovir USE

A

CMV retinitis in immunocompromised; acyclovir-resistant HSV. Long half-life

20
Q

Cidofovir TOX

A

Nephrotox (coadminister w/probenecid & IV saline to reduce tox)

21
Q

HIV Therapy initiation

A

Highly active antiretroviral therapy HAART; initiate when patient presents w/AIDS-defining illness, low CD4 count <500, or high viral load.

22
Q

HAART regimen

A

3 drugs to prevent resistance:
[2 nucleoside reverse transcriptase inhibitors (NRTIs)] + [1 non-nucleoside reverse transcriptase inhibitor (NNRTIs OR 1 protease inhibitor]

23
Q

Protease inhibitors

A

-navir

24
Q

Protease inhibitors MECH

A

Assembly of virions depends on HIV-1 protease (pol gene), which cleaves the polypeptide products of HIV mRNA into their functional parts. Thus, protease inhibitors prevent maturation of new viruses.

**ritonavir boosts other drug [ ]s by inhibiting P450

25
Q

Protease Inhibitor TOX

A

hypERglycemia, GI intolerance (nausea, diarrhea), lipodystrophy

26
Q

Indinavir TOX

A

nephropathy, hematuria

27
Q

NRTIs

A

Tenofovir (TDF), Emtricitabine (FTC), Abacavir (ABC), Lamivudine (3TC), Zidovudine (ZDV, formerly AZT), Didanosine (ddI), Stavudine (d4T)

28
Q

NRTI MECH

A

Competitively inhibit nucleotide binding to reverse transcriptase and terminate the DNA chain (lack of 3’ OH group). Tenofovir = nuc.tide analog & does not need to be activated; rest = nuc.side analogs & must be activated by p’lation. ZDV used for prophy & during pregnancy to reduce fetal transmission.

29
Q

NRTI & NNRTI TOX

A

Bone marrow suppression (can be reversed w/G-CSF & EPO), peripheral neuropathy, lactic acidosis (nuc.sides), rash (non-nuc.sides), anemia (ZDV).

30
Q

NNRTIs

A

Nevirapine, efavirenz, delavirdine

31
Q

NNRTI Mech

A

Bind to reverse transcriptase at site different from NRTIs. Do NOT require p’lation to be active

32
Q

Integrase inhibitors

A

Raltegravir

33
Q

Raltegravir (integrase inhibitor) MECH

A

Inhibits HIV genome integration into host cell chromosome by reversibly inhibitingHIV integrase.

34
Q

Raltegravir TOX

A

Hypercholesterolemia.

35
Q

IFN MECH

A

Glycoproteins synthesized by virus-infected cells; block replication of both RNA & DNA virus.

36
Q

IFN- alpha USE

A

chronic Hep B & C, Kaposi sarcoma

37
Q

IFN-Beta USE

A

MS

38
Q

IFN-gamma USE

A

NADPH oxidase deficiency

39
Q

IFN toxicity

A

Neutropenia, myopathy