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Dental Pharmacology > Antivirals > Flashcards

Antivirals Flashcards

1
Q

fusion inhibitors for treatment of retrovirus (HIV)

A

enfuvirtide, maraviroc

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2
Q

nucleoside reverse transcriptase inhibitors for treatment of retrovirus

A

zidovudine, didanosine, lamivudine, stavudine, abacavir

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3
Q

non-nucleoside reverse transcriptase inhibitors for treatment of retrovirus

A

nevirapine, delavirdine, efavirenz

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4
Q

integrase inhibitor for treatment of retrovirus

A

raltegravir

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5
Q

nucleotide inhibitor for treatment of retrovirus

A

tenofovir

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6
Q

protease inhibitors for treatment of retrovirus

A

atazanavir, saquinavir, ritonavir, lopinavir, indinavir, nelfinavir

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7
Q

treatments for herpes simplex and varicella zoster

A

acyclovir, valacyclovir, famciclovir, penciclovir

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8
Q

treatments for cytomegalovirus

A

ganciclovir, valganciclovir, cidofovir, foscarnet

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9
Q

treatments for hep B and C

A

lamivudine, adefovir, interferon alpha, ribavirin, boceprevir, telaprevir, tenofovir

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10
Q

uncoating inhibitors for treatment of influenza

A

amantadine, rimantadine

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11
Q

viral release inhibitors for treatment of influenza

A

zanamivir, oseltamivir

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12
Q

HAART

A

highly active antiretroviral therapy

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13
Q

36 amino acid synthetic peptide, increases effectiveness of HAART in combination chemotherapy, binds to gp41 of viral envelope, prevents conformational change and impedes the fusion of the viral and host cell membranes, no cross resistance with other HIV agents, potential for resistance developing when given at suboptimal doses

A

enfuvirtide

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14
Q

a 2nd line treatment; SC; high protein binding; metabolized by proteolytic hydrolysis; injection site reactions; increased risk of bacterial pneumonia

A

enfuvirtide

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15
Q

chemokine receptor 5 antagonist; binds to CCR5 co-receptor; prevents virus from entering the host cell; oral; substrate for both CYP3A4 and P-glycoprotein; both feces and urine

A

maraviroc

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16
Q

treatment of CCR5-tropic HIV-1; in combination for patients failing other antiretrovirals, coreceptor tropism assay should be performed when a CCR5 antagonist is being considered

A

maraviroc

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17
Q

adverse effects: cough, pyrexia, rash, musculoskeletal symptoms, abdominal pain and postural dizziness, bladder irritation; possible liver and cardiac problems; interacts with CYP3A inducers and inhibitors

A

maraviroc

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18
Q

AZT (zidovudine) and 3TC (lamivudine)

A

combivir

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19
Q

AZT (zidovudine) and 3TC (lamivudine) and abacavir

A

trizivir

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20
Q

mech of action of which retroviral group: competitive inhibition of viral reverse transcriptase

A

NRTIs

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21
Q

NRTIs: analogs of pyrimidine nucleoside (T); phosphorylated to active triphosphate forms; competes w/ deoxythymidine triphosphate for incorporation into DNA

A

zidovudine and stavudine

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22
Q

NRTIs: analogs of pyrimidine nucleoside (C); compete with deoxycytidine triphosphate for incorporation into viral DNA

A

lamivudine and emtricitabine

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23
Q

NRTI: analog of purine nucleoside (A, G); active 2’,3’-dideoxyadenosine 5’-triphosphate (ddATP) competes with cellular deoxyadenosine triphosphate for incorporation into viral DNA

A

didanosine

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24
Q

NRTI: analog of purine nucleosides (G)

A

abacavir

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25
Q

only NRTI shown to reduce perinatal HIV transmission

A

zidovudine

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26
Q

zidozudine is metabolized to …

A

glucoronide

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27
Q

abacavir is metabolized by …

A

alcohol dehydrogenase

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28
Q

which NRTI is acid labile and taken 1/2 hr before or 2 hour after meals?

A

didanosine

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29
Q

common toxicities of which group?: GI distress, lactic acidosis and hepatic steatosis due to mitochondrial toxicity; lipodystrophy

A

NRTIs

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30
Q

which NRTI can cause bone marrow suppression

A

zidovudine

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31
Q

which NRTI causes diarrhea, peripheral neuropathy, pancreatitis

A

didanosine

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32
Q

which NRTI causes peripheral neuropathy and pancreatitis

A

stavudine

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33
Q

which NRTI causes hypersensitivity reaction due to genetic predisposition

A

abacavir

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34
Q

which NRTI: avoid concurrent administration with drugs that are bone marrow suppressive

A

zidovudine

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35
Q

which NRTI: ganciclovir increases plasma conc 2X and methadone decreases plasma levels

A

didanosine

36
Q

which NRTI: competition with zidovudine for activation enzymes

A

stavudine

37
Q

which NRTI: trimethoprim-sulfamethoxazole increases plasma concentration

A

lamivudine

38
Q

which NRTI: ethanol significantly increases plasma levels

A

abacavir

39
Q

Tenofovir DF and emtricitadine

A

truvada

40
Q

what is effective as antiretroviral chemoprophylaxis before exposure

A

truvada

41
Q

mech of action of which group: bind directly to a hydrophobic pocket of the RT protein; induce conformational change in active site and block enzyme activity; do not require intracellular phosphorylation for activity

A

NNRTIs

42
Q

NNRTI: CYP3A4 inhibitor

A

delavirdine

43
Q

NNRTI: CYP3A4 inducers

A

efavirenz and nevirapine

44
Q

which NNRTI: fever, fatigue, headache, somnolence, nausea, hepatotoxicity (elevated liver ezymes); may be severe and life-threatening

A

nevirapine

45
Q

which NNRTI: neuropsychiatric (headache, dizzines, abnormal dreams), teratogenic in nonhuman primates (FDA Pregnancy Category D)

A

efavirenz

46
Q

inhibits HIV-1 integrase which is needed for insertion of viral DNA into host genome; oral; glucuronidation in liver

A

raltegravir

47
Q

not inducer, inhibitor or substrate of CYP3A4; metabolized by UDP glucouronosyltransferase (UGT)

A

raltegravir

48
Q

what induces UGT

A

rifampin

49
Q

what inhibits UGT

A

PI atazanavir

50
Q

treatment of HIV as part of combination therapy and most effective ART available; effective in both acutely and chronic HIV-1 infected cells; effective in monocytes and macrophages; prevent cleavage of polyprotein and block viral maturation

A

protease inhibitors

51
Q

which group: metabolized by cytochrome P-450 system; potent inhibitors of CYP3A4

A

protease inhibitors

52
Q

which PI is used to increase plasma conc of other PIs

A

ritonavir

53
Q

which drug lowers indinavir AUC and potentially other PIs

A

carbamazepine

54
Q

which drug upregulates PIs AUC

A

ketoconazole

55
Q

which drug’s AUC is augmented by PIs

A

sildenafil

56
Q

which PIs reduce methadone AUC

A

ritonavir and lopinavir

57
Q

adverse effects of which drugs: hyperlipidemia, insulin resistance and diabetes, lipodystrophy (buffalo hump and crix-belly), gynecomastia; increased bleeding risk in hemophiliacs; increased liver function tests

A

PIs

58
Q

which PI: hepatotoxicity at high doses

A

ritonavir

59
Q

which PI: alopecia, kidney stones, and renal insufficiency (patients should drink 2 liters/day)

A

indinavir

60
Q

which PI: hyperbilirubinemia due to inhibition of UDP glucuronosyltransferase

A

atazanavir

61
Q

which group: once phosphorylated by cellular kinases have greater affinity for viral reverse transcriptase than for cellular DNA polymerase

A

NRTIs

62
Q

which group: do not undergo phosphorylation and have greater affinity for viral reverse transcriptase than for cellular DNA polymerase

A

NNRTIs

63
Q

which group: greater affinity for HIV aspartyl protease than for human protease

A

PIs

64
Q

block DNA synthesis by inactivation of viral DNA polymerase through direct binding and competition for dNTPs and by inducing viral DNA chain termination

A

nucleoside analogs

65
Q

chain terminating effect following incorporation of a nucleotide analogue

A

acyclovir

66
Q

absence of viral thymidine kinase gives … against nucleoside analogues

A

resistance

67
Q

acyclic purine nucleoside analogues; indication: herpes simplex, following high IV dose: reversible renal dysfunction and neurologic toxicity

A

acyclovir and valacyclovir

68
Q

acyclic purin nucleoside analogues: indications- CMV retinitis (activity 100x greater than acyclovir), oral CMV prophylaxis; adverse effect- myelosuppression

A

ganciclovir and valganciclovir

69
Q

antiherpesvirus agents: oral alternative to acyclovir

A

penciclovir and famciclovir

70
Q

antiherpesvirus agent: inhibits herpesvirus DNA polymerase»human DNA polymerase; potential human carcinogen; nephotoxicity, neutropenia, ocular hypotony

A

cidofovir

71
Q

a non-nucleoside anti-HSV agent; inhibits cleavage of pyrophosphate from dNTP and blocks viral DNA synthesis; effective in CMV retinitis

A

foscarnet

72
Q

myelosuppressant and has teratogenic potential

A

ganciclovir

73
Q

nephrotoxic

A

cidofovir and foscarnet

74
Q

anti-hep agent: nucleoside analog of guanosine; inhibits all 3 activities of HBV polymerase; equally active against lamivudine-resistan HBV; HBV exacerbation upon discontinuation of treatment

A

entecavir

75
Q

anti-hep agent: nucleotide analog prodrug; active against all HCV genotypes; monotherapy not recommended; once daily oral; metabolized in liver and elimination is renal; extreme caution when used in combo with ribavirin (Pregnancy category X)

A

sofobuvir

76
Q

anti HBV; nucleotide analog; inhibits HBV DNA polymerase; exacerbations of hepatitis after discontinuation; lactic acidosis

A

adefovir

77
Q

nucleotide reverse transcriptase inhibitor

A

tenofovir

78
Q

all nucleoside analogs- lactic acidosis and severe hepatomegaly with steatosis is a more common adverse effect in the treatment of …

A

HIV

79
Q

inhibitors of transcription; potent cytokines that possess antiviral, immunomodulating and antiproliferative actions

A

interferons

80
Q

3 main classes of human IFNs

A

alpha, beta and gamma

81
Q

adverse effects: flu-like syndrome, nausea, vomiting, anorexia, CV abnormalities, myelosupression, neurotoxicity, hepatotoxicity, should not be administered during pregnancy

A

interferon alpha-2

82
Q

nucleoside analog of guanosine; interference with synthesis of GTP and inhibits GTP 5’ capping of viral mRNA; dose dependent hemolytic anemia; bone marrow suppression

A

ribavirin

83
Q

NS3/4A proteas inhibitors; block serine protease; potent inhibitors of CYP3A4/5

A

boceprevir and telaprevir

84
Q

antiinfluenza; inhibitors of uncoating of virus; acts on maturation of influenza HA glycoprotein’ oral prophylaxis against influenza A (not B); good alternative to vaccine

A

amantadine, rimantadine

85
Q

antiinfluenza; inhibitors of influenza neuraminidase; effective against influenza A and B

A

zanamivir, oseltamivir

Dental Pharmacology (30 decks)

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