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Blood, Lymph, Immune, Bone > HIV > Flashcards

HIV Flashcards

1
Q

Drugs in the NRTI class

MOA

Names

A

inhibit HIV reverse transcriptase and inhibit DNA polymerase

abacavir, didanosine, emtricitabine, lamivudine, stravudine, tenofovir, zidovudine

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2
Q

What class of HIV antivirals must be phosphorylated to be active?

A

NRTIs

NRTIs incorporate into viral DNA chain to cause chain termination

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3
Q

NRTIs

Side effects (general)

A

NRTIs

Mitochondrial toxicity (inhibition of mitochondrial DNA polymerase)

Lactic acidosis with hepatic steatosis

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4
Q

abacavir

side effects

A

Hypersensitivity reactions and increased risk of myocardial infarction

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5
Q

didanosine

side effects

A

Pancreatitis

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6
Q

zidovudine

side effects

A

bone marrow suppression resulting in anemia or neutropenia

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7
Q

zidovudine and stavudine

side effects

A

dislipidemia and insulin resistance

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8
Q

NNRTIs

MOA

Names

A

NNRTIs

bind to HIT RT and inhibit DNA polymerase (noncompetative inhibitors that cause a conformational change in the enzyme structure)

Delavirdine, efavirenz, etravirine, nevirapine, rilpivirine

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9
Q

NNRTIs

Clinical Use

Drug Drug interactions

A

NNRTIs

Use for HIV-1 only

mutation occurs rapidly

metabolized by CYP450: delaviridine is a cyp450 inhibitor, efavirenz, etravirine, nevirapine are inducers

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10
Q

dizziness, drowsiness, insomnia, nightmares, and headache are all side effects of what drug?

A

efavirenz

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11
Q

rilpivirine

side effects

A

depression, insomnia, increased serum cholesterol, fat redistribution syndrome

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12
Q

which NNRTI is teratogenic?

A

efavirenz

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13
Q

Protease inhibitors (PI)

MOA

Names

A

PI

inhibit HIV protease by competitivily binding to the protease active site and thereby preventing the production of functional proteins.

atazanavir, darunavir, fosamprenavir, indinavir, lopinavir, nelfinavir, ritonavir, squinavir, tipanavir

“-navir”

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14
Q

Protease Inhibitors

Side Effects

A

PI

GI intolerance

Metabolic complications- lipodystrophy (cushing-like syndrome, fat accumulation, central obesity, fat around neck, between shoulders), dyslipidemia, hyperglycemia and insulin resistance

Resistance to PI also develops rapidly

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15
Q

which PI is an inhibitor to CYP3A4 and why do we care?

A

ritonavir is an inhibitor of CYP3A4 and can be used to “boost” the effects of other drugs by inhibiting their metabolism

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16
Q

Maraviroc

MOA

A

Maraviroc inhibits entry into the host cell as a CCR5 receptor antagonist. This prevents gp120 binding, fusion and entry

17
Q

Maraviroc

Clinical Use

A

Maravirocis approved for use in combination with other antiretroviral agents in treatment experienced adult patients infected with only CCR5-tropic HIV-1

18
Q

Maraviroc

Side Effects

A

Maraviroc

cough, hepatotoxicity

drug interactions: decrease the dose if being taken in combination with a CYP3A inhibitor

19
Q

What drug is a fusion inhibitor?

MOA

A

enfurvirtide

binds to gp41 and prevents the fusion of viral and cellular membranes

20
Q

enfuvirtide

clinical use

side effects

A

enfuvirtide

HIV1 treatment in patients where other treatments have failed

injection site reactions, (must be given sub q), insomnia, headache, dizziness, nausea, hypersensitivity. Very expensive

metabolism does not involve CYP450- fewer drug interactions

21
Q

Integrase strand transfer inhibitors (INSTIs)

MOA

Names

A

INSTIs

bind to integrase with is essential for viral replication

dolutegravir, elvitegravir, raltegravir

“-gravir”

22
Q

INSTIs

MOA

A

prevent the formation of covalent bonds between host and viral DNA

Active against both HIV 1 and HIV 2

23
Q

INSTIs

Side Effects

A

INSTIs

headache and GI effects

less frequently you see insomnia and dizziness

24
Q

Elvitegravir

administration

A

Elvitegravir requires boosting with additional drugs like ritonavir or cobicistat

Blood, Lymph, Immune, Bone (13 decks)

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