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Pharmacology > Antiretroviral Agents > Flashcards

Antiretroviral Agents Flashcards

1
Q

Classes of Antiretroviral drugs

A 
NRTIs
NNRTIs
Fusion inhibitors
PIs
Co-receptor antagonists
Integrase Inhibitors
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2
Q

NRTIs general characteristic, MOA

A

Target is reverse transcriptase
Mimic nucleotides, inhibit binding to catalytic site
Require cellular kinases to convert to triphosphate form

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3
Q

NRTI general adverse

A

Lactic acidosis, fatty liver disease, and lipodystrophy

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4
Q

Abacavir MOA

A

Guanosine analogue NRTI, given orally

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5
Q

Abacavir Adverse

A

Allergic reaction w/ HLA B5707=> rash, fever, nauea, vomiting, etc.
Increased risk for CV events
May lower effectiveness of methadone

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6
Q

Abacavir Resistance and indications

A

Multiple mutations needed for resistance

Tx for naive and experienced HIV infections

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7
Q

Lamivudine MOA

A

Cytosine analogue NRTI, given orally but low serum half life

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8
Q

Lamivudine adverse

A

Very safe, but higher than recommended doses yield GI and CNS effects

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9
Q

Lamivudine Resistance and indications

A

Single base change=>high resistance
Tx for naive and experienced HIV pts,
Safe for pregnant mothers and neonates

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10
Q

Emtricitabine MOA

A

Fluorinated analogue of lamivudine=> oral, longer half life

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11
Q

Emtricitabine adverse

A

Headache, nausea, diarrhea, hyperpigmentation of palms and soles

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12
Q

Emtricitabine resistance and indications

A

single mutation in reverse transcriptase

Tx for naive and experienced HIV

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13
Q

Emtricitabine Contraindications

A

Young children, pregnant women, pts w/ renal or hepatic failure

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14
Q

Tenofovir MOA

A

Adenosine analogue NRTI, oral, usually given as prodrug

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15
Q

Tenofovir Adverse

A

Normal GI issues
Renal and bone toxicity
Can cross placenta=>decreased bone density and fetal growth

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16
Q

Tenofovir resistance and Indications

A

Single codon change=>resistance
Naive and experienced HIV pts, can reduce transmission
Tx of chronic hep B w/ interferon

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17
Q

Zidovudine (AZT) MOA

A

Deoxythymidine analogue NRTI, oral, well absorbed

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18
Q

Zidovudine Adverse

A

Myelosuppresion, nail hyper-pigmentation, normal GI effects

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19
Q

Zidovudine Resistance and Indications

A

Multiple mutations needed for resistance

Naive and experienced HIV, reduction in vertical transmission

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20
Q

NNRTIs MOA

A

Target is reverse transcriptase, bind to site distinct from active site
do not require phosphorylation for activation
Not active against HIV 2

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21
Q

NNRTI adverse effects

A

Rash, Steven Johnson syndrome, hepatotoxicity

Drug-drug ineractions common b/c of effects on cytochrome P450 enzymes

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22
Q

Efavirenz pharmkinetics

A

Once daily oral, on empty stomach

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23
Q

Efavirenz adverse

A

CNS, rash, headache/nausea

Induces CYP3A4

24
Q

Efavirenz resistance and indications

A

Single base change can confer resitance. Cross resitance w/ Nevirapine common
Naive and experienced HIV

25
Q

Efavirenz contraindications

A

Pregnancy

26
Q

Nevirapine pharmkinetcs

A

NNRTI, oral, lipophilic

27
Q

Nevirapine adverse

A

rash, hepatitis, nausea, headache

28
Q

Nevirapine resistance and indications

A

Single base change=>resistance

Prevents vertical transmission

29
Q

Protease Inhibitors

A

Target=HIV protease, blocks maturation of virion particles after budding
Multiple mutations needed for resistance

30
Q

Protease Inhibitor adverse

A

**Drug interactions due to alteration of cytochrome P450 enzymes
Hyperlipidemia, lypodystrophy, hepatotoxicity, GI problems, increased bleeding

31
Q

Atazanavir Pharmkinetics

A

Once daily oral, requires acid for absorption, do not use with PPIs

32
Q

Atazanavir adverse

A

peripheral neuropathy, indirect hyperbilirubinemia

Inhibitor of CYP3A4 and CYP2C9

33
Q

Atazanavir resistance and adverse

A

Multiple codon changes needed for resistance

naive and experienced HIV, approved for use in children over 6 y.o.

34
Q

Ritonavir pharmkinetics

A

PI, oral, 75% bioavailable

35
Q

Ritonavir adverse

A

Potent inhibitor of CYP3A4

Nausea/diarrhea, paresthesia, hepatitis

36
Q

Ritonavir resistance/indications

A

multiple mutations needed for resistance

Often used in low doses as a booster to increase the half life of co-administered ARV drug due to CYP3A4 effect

37
Q

Duranavir pharmkinetics

A

PI, oral, coadministed with pharmacokinetic enhancer

38
Q

Darunavir adverse

A

increased liver enzymes,increased serum amylase, other general adverse

39
Q

Darunavir resistance and indications

A

Very little resistance

Used for naive and experienced HIV pts

40
Q

Maraviroc-Class and pharmkinetics

A

Co-receptor antagonist, oral administration, substrate of CY34A

41
Q

Maraviroc Adverse

A

URT infections, postural hypotension, sleep disturbance, allergic rxn

42
Q

Maraviroc resistance and indications

A

Occurs through tropism of the virus, or mutations in gp120

Screen for tropism before use

43
Q

Enfuvirtide MOA

A

Fusion inhibitor-inhibits fusion of virion w/ the plasma membrane
**Only parenteral antiretroviral agent

44
Q

Enfuvirtide adverse

A

Painful, erythematous nodule @injection site

insomnia, headache, nausea, etc.

45
Q

Enfuvirtide resistance/indications

A

Multiple mutations needed for resistance

Treatment for experienced pts w/evidence of HIV replication even with ARV treatment

46
Q

Integrase Inhibitors MOA

A

prevents integration of viral DNA into chromosome DNA

47
Q

Raltegravir pharmkinetics

A

integrase inhibitor, oral admin

48
Q

Raltegravir adverse

A

creatine kinase elevation

myopathy, rhabdomyolysis

49
Q

Raltegravir resistance/indications

A

Single mutaiton in gene confers resistance

Naive and experienced HIV pts

50
Q

Elvitegravir pharmkinetics

A

Integrase inhibitor, oral administered, co-administered w/ cobicistat or ritonavir

51
Q

Elvitegravir adverse

A

normal systemic: nausea, diarrhea, headache, fatigue

52
Q

Elvitegravir resistance/indications

A

Single mutation confers resistance

Experienced and naive HIV pts

53
Q

Dolutegravir

A

Integrase inhibitor, oral admin

54
Q

Dolutegravir adverse

A

insomnia/headache, hypersensitivity, fat redistribution syndrome

55
Q

Dolutegravir resistance/indications

A

retains activity against some viruses that are resistant to other integrase inhibitors
HIV infection pts at least 12 y.o. and weighing at least 40 kg

56
Q

General features of ARV therapy

A

Combination of at least three ARV drugs, from at least two different classes

57
Q

Preferred combo ARV therapies for initial therapy

A

1 PI (ritonavir) + 2 NRTIs

1 Integrase inhibitor + 2 NRTIs

Pharmacology (11 decks)

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