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Heme Pharm > HIV drugs > Flashcards

HIV drugs Flashcards

1
Q

Fusion inhibitor: Enfuvirtide: 36 amino acid peptide which binds to 1) inhibiting 2) of HIV with the target cell

A

1) gp41 2)fusion

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2
Q

active against HBV, patients co-infected with HIV and HBV should be closely monitored if treatment with either of these drugs is interrupted or discontinued, because of the likelihood of hepatitis flare

A

NRTIs (Emtricitabine, Lamivudine, Tenofovir):

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3
Q

36 amino acid peptide which binds to gp41 inhibiting fusion of HIV with the target cell

A

Fusion inhibitor: Enfuvirtide

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4
Q

a/e Metabolic changes including increased lipids, insulin insensitivity, and central fat accumulation

A

Protease inhibitors: Atazanavir, Darunavir, Ritonavir

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5
Q

binds to CD4

A

gp120

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6
Q

Binds specifically and selectively to CCR5

A

Penetration blocker: Maraviroc

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7
Q

Penetration blocker: Maraviroc resistance

A

develop due to mutations in gp120

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8
Q

Adverse effects i. Rash which could progress to Stevens-Johnson syndrome ii. Fetal abnormalities (neural tube defects)

A

Nonnucleoside: Efavirenz

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9
Q

Long-term complications of ART include 1). The statins are used to lower lipids but their metabolism is inhibited by 2). This can increase the blood levels of the statin and increase the risk of 3)

A

1) hyperlipidemia 2) Protease Inhibitorss 3) rhabdomyolysis

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10
Q

used to “boost” the levels of other protease inhibitors when given in combination, thus acting as a pharmacokinetic enhancer rather than an antiretroviral agent

A

Ritonavir boost

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11
Q

nucleoside analog of cytosine

A

Lamivudine

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12
Q

Life cycle of HIV:Reverse transcription HIV is equipped with 1)

A

1) RNA-dependent DNA polymerase (reverse transcriptase);

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13
Q

These drugs do not compete with nucleoside triphosphates nor require phosphorylation to be active

A

Nonnucleoside: Efavirenz

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14
Q

(nucleotide analog of adenosine

A

Tenofovir

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15
Q

All newborns born to HIV-infected mothers should receive 1) for 6 weeks; Infants born to mothers with no antiretroviral therapy should receive 6 weeks of 2) during the first week of life

A

1) zidovudine 2) zidovudine and three doses of nevirapine (an NNRTI)

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16
Q

gp120 and gp41 is made from cleavage of 1); functions of each?

A

gp160 gp120–> binds to CD4 gp41–> membrane fusion

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17
Q

prevent post-translational cleavage of the Gag-Pol polyprotein resulting in the production of immature, noninfectious viral particle

A

Protease inhibitors: Atazanavir, Darunavir, Ritonavir

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18
Q

bind directly to reverse transcriptase resulting in allosteric inhibition of RNA- and DNA-dependent DNA polymerase

A

Nonnucleoside: Efavirenz

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19
Q

integrase strand transfer inhibitor (INSTI)

A

Integrase inhibitor: raltegravir

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20
Q

Life cycle of HIV: Penetration Viral gp120 binding to CD4 is enhanced by further binding to chemokine receptors, 1)

A

1) CCR5 and CXCR4.

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21
Q

Incorporation into the growing viral DNA chain results in premature chain termination due to inhibition of binding with the incoming nucleotide

A

NRTIs (Emtricitabine, Lamivudine, Tenofovir):

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22
Q

Protease Inhibitor therapy in pregnant women a/e

A

Hyperglycemia Premature birth

23
Q

increases drug exposure, thereby prolonging the drug’s half-life and allowing reduction in frequency; in addition, the genetic barrier to resistance is raised

A

Ritonavir boosting

24
Q

what is protease? cleaves the large precursor 1) into functional proteins which produce a complete virus; Without this step, 2)

A

1) polypeptide, known as gag-pol, 2) the virion is immature and unable to infect other cells.

25
Q

1) catalyzes the process that results in viral DNA insertion into the host genome. 2) block the enzyme’s activity, preventing viral DNA from integrating with cellular DNA.

A

1) HIV-1 integrase 2) Integrase strand transfer (InST) inhibitors

26
Q

Prophylaxis of HIV infection: Pre-exposure: oral fixed-dose combination of 1); resistance to 1) if pt infected with HIV so follow-up HIV antibody testing to ensure early diagnosis

A

1) emtricitabine and tenofovir

27
Q

T/F–>The binding site of NNRTIs is distinct from that of NRTIs

A

True

28
Q

NRTIs therapy in pregnant women a/e

A

Mitochondrial dysfunction in uninfected children with perinatal exposure to NRTIs

29
Q

T/F–>there is no cross-resistance between the NRTIs and the NNRTIs

A

TRUE

30
Q

A/E Peripheral neuropathy, pancreatitis, lipoatrophy, myopathy, anemia, increased transaminases

A

NRTIs (Emtricitabine, Lamivudine, Tenofovir):

31
Q

fluorinated analog of lamivudine

A

Emtricitabine

32
Q

HIV treatment during labor: Women who are already in labor and have had no antiretroviral therapy should receive 1) as a continuous infusion to decrease the risk of HIV transmission to the fetus

A

1) IV zidovudine

33
Q

NRTIs (Emtricitabine, Lamivudine, Tenofovir) are prodrugs which require 1) to be active

A

1) phosphoylation to the 5’-triphosphate moiety

34
Q

Hepatotoxicity

A

Penetration blocker: Maraviroc

35
Q

Adverse effects Well-tolerated: diarrhea, nausea, dizziness, and headache

A

Integrase inhibitor: raltegravir

36
Q

membrane fusion

A

gp41

37
Q

a/e local injection site reactions with mild or moderate pain, erythema, induration, nodules and cysts

A

Fusion inhibitor: Enfuvirtide:

38
Q

Life cycle of HIV: Assembly and release a. HIV proteins coalesce under the host cell lipid bilayer b. The nucleocapsid subsequently is formed with 1) and other components packaged inside. c. The virion then 2) d. 3), another enzyme unique to HIV, begins cleaving the large precursor polypeptide, gag-pol, into functional proteins which produce a complete virus. Without this step, the virion is immature and unable to infect other cells

A

1) viral ssRNA 2) buds through the plasma membrane and maturation begins 3) Protease

39
Q

Drug interactions: Protease inhibitors can inhibit metabolism of drugs as well, in particular, the 1)

A

1) statins (e.g., atorvastatin, lovastatin, and others).

40
Q

Life cycle of HIV: Integration The dsDNA migrates into the 1) and is integrated into the host chromosome by 2) another enzyme unique to HIV

A

1) nucleus 2) integrase,

41
Q

Integrase inhibitor: raltegravir resistance

A

Mutation in integrase

42
Q

Reverse transcription: i. A cDNA is first synthesized using 1) as a template ii. The RNA portion of the cDNA-RNA hybrid is removed by 2) iii. 3) then completes the synthesis of doublestranded DNA

A

1) viral RNA 2) ribonuclease H (RNase H) 3) Reverse transcriptase

43
Q

Fusion inhibitor: Enfuvirtide resistance

A

due tospecific mutations in the enfuvirtide-binding domain of gp41

44
Q

Adverse effects i. Cough, pyrexia, upper respiratory tract infection, rash, musculoskeletal symptoms, abdominal pain and postural dizziness

A

Penetration blocker: Maraviroc

45
Q

T/F–.Most clinicians believe that the benefit of a potent antiretroviral regimen taken during pregnancy greatly outweighs the risk.

A

True

46
Q

Ketoconazole drug interaction with Maraviroc

A

Inhibitors of P450 (and P-glycoprotein) (e.g., ketoconazole, macrolide antibiotics) increase the effects of maraviroc; may need to decrease dose

47
Q

Life cycle of HIV: Uncoating After internalization, the viral protein shell surrounding the 1) is uncoated in preparation for replication.

A

1) nucleic acid (capsid)

48
Q

Life cycle of HIV: Penetration CD4 and coreceptor binding (i.e., binding to CCR5 or CXCR4) promotes membrane fusion which is mediated by 1)

A

1) gp41

49
Q

Pregnancy HIV treatment: In treatment-naive women, 1) and lamivudine plus either lopinavir/ritonavir or atazanavir/ritonavir

A

1) zidovudine (an NRTI)

50
Q

NRTIs (Emtricitabine, Lamivudine, Tenofovir): -triphosphate moiety inhibits 1) by competing with endogenous deoxynucleotides for the catalytic site of the enzyme

A

1) reverse transcriptase

51
Q

Hepatotoxicity (more common in patients who are co-infected with HBV or HCV

A

Protease inhibitors: Atazanavir, Darunavir, Ritonavir

52
Q

Life cycle of HIV: Penetration The outer glycoprotein, gp160, on the surface of HIV is composed of two subunits 1). The 2) subunit is responsible for CD4 binding

A

1) gp120 and gp41 2) gp120

53
Q

Life cycle of HIV:Reverse transcription The genetic material of HIV is 1) (5’ to 3’) 2) The virus must transcribe this RNA into DNA

A

1) positive-sense 2) single-stranded RNA

54
Q

Adverse effects i. Mitochondrial toxicity due to inhibition of mitochondrial DNA polymerase-γ

A

NRTIs (Emtricitabine, Lamivudine, Tenofovir):

Heme Pharm (13 decks)

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