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MS2 Unit 6 Pharm > Antivirals > Flashcards

Antivirals Flashcards

1
Q

4 targets for antivirals in HIV drugs

A

entry, reverse transcriptase, integrase, protease

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2
Q

mechanism of action for NRTI’s

A

viral DNA chain termination via inhibition of reverse transcriptase enzyme. pose as pieces of DNA and get picked up and stop the enzyme!

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3
Q

NRTI class side effects

A

lactic acidosis (much less common with newer agents). GI side effects.

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4
Q

NRTI agents

A

zidovudine, stavudine, didanosine, tenofovir, abacavir, zalcitabine, lamivudine, emtricitabine

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5
Q

NNRTI mechanism of action

A

bind directly to reverse transcriptase and inhibit its actions

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6
Q

NNRTI agents

A

efavirenz, nevirapine, etravirine, rilpivirine

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7
Q

NNRTI side effects

A

cause a rash. may cause CNS effects like vivid dreams, drowsiness.

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8
Q

protease inhibitor agents

A

norvir, lexiva, kaletra, reyataz, prezista

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9
Q

protease inhibitor mechanism of action

A

bind within active pocket of protease, inhibiting binding of the virus. without protease cleavage, virus cannot cause infection!

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10
Q

what is curious about ritonavir?

A

ritonavir at low doses enhances blood levels of other protease inhibitors! give together to increase clinical effectiveness and require less doses of other drugs!

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11
Q

protease inhibitor class toxicities

A

GI: N/V, diarrhea
Metabolic: dyslipidemia, hyperglycemia, lipodystrophy

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12
Q

enfuvirtide mechanism of action

A

messes with GP41, which makes the connection for CD4 binding. messes with HIV attachment and fusing

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13
Q

enfuvirtide adverse effects

A

local injection sight reaction. increased rate of bacterial pneumonia. hypersensitivity.

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14
Q

CCR5 antagonists

A

HIV often uses CCR5 as a co-receptor necessary to enter T cells. Maraviroc is only agent. Only drug that acts on the host cell, all others act on HIV molecules.

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15
Q

CCR5 adverse effects

A

hepatotoxicity. cough, fever, URI, rash, musculoskeletal, ab pain, dizziness

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16
Q

integrase inhibitor agents

A

raltegravir, elvitegravir, dolutegravir.

17
Q

integrase inhibitor mechanism of action

A

inhibit viral enzyme integrase. necessary for insertion of viral DNA into human genomic DNA

18
Q

integrase inhibitor adverse effects

A

generally few adverse effects. commonly seen: Nausea, headache, diarrhea, pyrexia. myopathy seen sometimes

19
Q

basics of HAART

A

use at least 3 active agents representative of 2 classes of agents

20
Q

goals of HAART

A

suppress viral load, restore immune function, improve quality of life, reduce HIV related morbidity and mortality, minimize risk for antiretroviral resistance

21
Q

NS5B polymerase inhibitors agents

A

sofosbuvir, paritaprevir

22
Q

NS5B polymerase inhibitors mechanism of action

A

inhibitor of Hep C NS5B RNA dependent RNA polymerase. competes with natural viral nucleotides to cause chain termination

23
Q

NS5A inhibitor agents

A

ledipasvir, daclatasvir, ombitasvir

24
Q

NS5A inhibitor mechanism of action

A

inhibits hep C NS5A, a viral phosphoprotein required for viral replication.

25
Q

NS3/4A protease inhibitor agents

A

simeprevir, boceprevir, telaprevir

26
Q

NS3/4A protease inhibitor mechanism of action

A

prevent viral maturation through the inhibition of protein synthesis

27
Q

acyclovir mechanism of action

A

after phosphorylation by cellular enzymes, acyclovir triphosphate competes with DNA analogues to cause viral DNA chain termination. needs viral thymidine kinase to become active

28
Q

other drugs like acyclovir

A

valacyclovir, peniciclovir, famciclovir

29
Q

acyclovir toxicity concerns

A

CNS: malaise, headache, confusion.

N/V, diarrhea. renal dysfunction seen in high doses of IV therapy due to drug crystallizing in kidneys

30
Q

ganciclovir

A

active mainly against Cytomegalovirus. (CMV). Use the prodrug when you need to give orally, as the actual drug has bad bioavailability. biggest side effect is myelosuppression

31
Q

foscarnet

A

inhibitory effect on herpesvirus and HIV. directly inhibits herpesvirus DNA polymerase or HIV reverse transcriptase.

32
Q

foscarnet tox issues

A

nephrotox, electrolyte/metabolic abnormalities, CNS side effects, myelosuppression. only used when people have resistance to other herpes drugs

33
Q

neuraminidase inhibitors

A

oseltamivir, zanamivir, peramivir. inhibit enzyme critical in penetration of respiratory tract mucus and in the release of virus from infected cells. active against flu A and B

34
Q

neuraminidase inhibitor adverse effects

A

N/V, diarrhea. neuropsychiatric events reported. zanamavir can cause bronchospasm. peramivir is used only in critically ill

MS2 Unit 6 Pharm (9 decks)

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