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IHO Week 6 (EH) > Antiretroviral Drugs > Flashcards

Antiretroviral Drugs Flashcards

1
Q

Nucleoside Reverse Transcriptase Inhibitors (NRTIs)

A

Zidovudine (Azidothymidine or AZT)
Lamivudine
Abacavir
Emtricitabine

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2
Q

Nucleotide Reverse Transcriptase Inhibitor (NRTIs)

A

Tenofovir

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3
Q

Non-nucleoside reverse transcriptase inhibitors (NNRTIs)

A

Etravirine
Efavirenz
Rilpivirine

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4
Q

Protease Inhibitors – 9 or more available

A

Atazanavir +/- ritonavir (ritonavir boosting)

Darunavir + ritonavir (ritonavir boosting)

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5
Q

Integrase inhibitor

A

Raltegravir

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6
Q

Fusion inhibitors

A

Enfuvirtide (T-20)

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7
Q

CCR5 antagonist

A

Maraviroc

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8
Q

Cobicistat

A

pharmacokinetic enhancer that inhibits CYP3A4 as well as certain intestinal transport proteins and can also act as a booster of protease inhibitors. It is not a protease inhibitor itself

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9
Q

Goal of HIV treatment

A

fully undetectable levels of virus

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10
Q

to achieve maximal and durable suppression of viral RNA need

A

drug combinations and patient compliance

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11
Q

what is recommended before starting therapy

A

resistance testing

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12
Q

what is monitored in HIV therapy

A

HIV RNA levels (viral load) and CD4+ T cell count (increased viral load may implicate drug resistance)

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13
Q

general strategy/combinations for drugs

A

One of these (NNRTI, Protease inh, Integrase inh) + Dual NRTI

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14
Q

Zidovudine (Azidothymidine or AZT) – first HIV drug
Lamivudine
Emtricitabine
Abacavir

A

Nucleoside reverse transcriptase inhibitors

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15
Q

mechanism Nucleoside reverse transcriptase inhibitors

A

Competitively inhibit reverse transcriptase and can be incorporated into viral DNA chain and cause termination. The inhibitor binds to the DNA chain and terminates the production of DNA

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16
Q

what do nucleoside RTIs require to be active

A

phosphorylation by cellular enzymes to the triphosphate

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17
Q

NRTIs resistance issue

A

Resistance to one may result in resistance to another within the class

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18
Q

AE NRTIs (nucleoside)

A

Potentially fatal syndrome of lactic acidosis with hepatic steatosis, probably due to mitochondrial toxicity
Associated with fat redistribution and hyperlipidemia

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19
Q

Zidovudine AEs

A

Granulocytopenia and anemia in up to 45% of treated patients (hematological monitoring at 2 week intervals).
CNS disturbances: severe headache, nausea, insomnia, malaise

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20
Q

Lamivudine and Emtricitabine significance

A

Probably best tolerated of the NRTIs

Also active against Hepatitis B

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21
Q

Abacavir AE

A

hypersensitivity reactions can be a problem.

22
Q

Abacavir and what HLA significance

A

Testing for HLA-B*5701 must be obtained because individuals with this allele are at risk for developing a severe hypersensitivity reaction to this drug

23
Q

Tenofovir

A

Nucleotide reverse transcriptase inhibitor

24
Q

nucleotides are

A

phosphorylated nucleosides

25
Q

mechanism NRTIs (nucleotides)

A

Same as Nucleoside reverse transcriptase inhibitors

The inhibitor binds to the DNA chain and terminates the production of DNA

26
Q

AE NRTIs (nucleotides)

A

N/V, diarrhea
RENAL FAILURE
Lactic acidosis, hepatic steatosis d/t mitochondrial toxicity

27
Q

do not give tenofovir to

A

patients with low baseline GFR

28
Q

Etravirine
Efavirenz
Rilpivirine

A

Non nucleoside reverse transcriptase inhibitors (NNRTI)

29
Q

Mechanism NNRTIs

A

bind directly to the reverse transcriptase at a site distinct from that of NRTI - enzyme cannot produce viral DNA

30
Q

cross resistance NNRTIs and NRTIs and PIs?

A

No cross resistance with NNRTIs and NRTIs and protease inhibitors.

31
Q

General AE of NNRTIs

A

GI intolerance and Rash

CYP450 drug interactions (inducers, inhibitors or both)

32
Q

Efavirenz (dosing, AE)

A 
Once daily dosing
CNS effects (vivid dreams, nightmares and hallucinations)
33
Q

Etravirine (AE)

A

Rash, nausea, peripheral neuropathy

34
Q

Rilpivirine, don’t use in

A

patient wth pretreatment viral loads >100,000 copies/ml

35
Q

Atazanavir
Ritonavir
Darunavir

A

Protease Inhibitors

36
Q

Mechanism PIs

A

Prevent protease action required for maturation of fully assembled virus and budding – do not mature and become infectious

37
Q

what is protease required for

A

cleavage of polypeptide precursors for structural proteins (gag pol polyprotein)

38
Q

General AE PIs

A
  • GI disturbances
  • Hepatotoxicity
  • Hyperglycemia and insulin resistance
  • Dyslipidemia
  • Cardiac conduction abnormalities
  • Peripheral lipoatrophy and central fat accumulation
  • Metabolized by and inhibit hepatic CYP3A4
39
Q

_______ boosting

A

ritonavir
high doses are poorly tolerated but at lower levels increase concentration of other PIs and decrease dosage frequency (CYP3A4 inh)

40
Q

Enfuvirtide (T-20)

A

Fusion inhibitor

41
Q

Mechanism Enfuvirtide

A

After HIV binds to the host cell surface, a conformational change occurs in the transmembrane glycoprotein subunit (gp41) of the viral envelope, facilitating fusion of the viral and host cell membranes, and entry of the virus into the cell. Enfuvirtide is a 36 amino-acid synthetic peptide that binds to gp41 and prevents the conformational change.

42
Q

Dosing/route enfuvirtide

A

SQ BID

43
Q

AE Enfuvirtide

A

High incidence of local reactions with pain, erythema, induration, nodules and cysts.
Systemic hypersensitivity rare.
Maybe a higher incidence of bacterial pneumonia.

44
Q

Raltegravir

A

Integrase inhibitors

45
Q

Mechanism raltegravir

A

Integrase is a viral enzyme essential to the replication of both HIV-1 and HIV-2. By binding integrase, it inhibits strand transfer, the final step of provirus integration.

46
Q

Integrase inhibitor AKA

A

Integrase Strand Transfer Inhibitors (INSTI)

47
Q

Drug reactions Integrase Inhibitors

A

Fewer drug interactions than PI or NNRTIs

48
Q

Maraviroc

A

CCR5 Antagonist

49
Q

Mechanism maraviroc

A

Binds specifically and selectively to host CCR5
CCR5 and CXCR4 are two major co-receptors used by HIV-1 to gain entry into the host cell with the R5 strains predominating during early stages of infection and remaining dominant in 50-60% of late stage disease.

50
Q

AE maraviroc

A

Pyrexia, rash, postural dizziness have been reported as well as other issues.
No evidence yet of increased risk of malignancy or infection.

51
Q

HAART

A

HAART = Highly active antiretroviral therapy

A term generally used in reference to therapy with RTIs in combination with PI.

52
Q

Long term use of combination anti-retroviral therapy associated with

A

secondary effects, the most prevalent being HAART associated lipodystrophy (wasting of SQ fat, central adiposity, hyperlipidemia, insulin resistance and DM)

IHO Week 6 (EH) (9 decks)

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