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SBL Exam 2 > HIV Pharmacology > Flashcards

HIV Pharmacology Flashcards

1
Q

binds specifically and selectively to CCR5 to prevent viral ENTRY into the host cell
- co-receptor tropism should be tested prior to initiating treatment

A

maraviroc

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2
Q

approved for use in combination with other antiretroviral agents infected only with CCR5-tropic HIV

A

maraviroc

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3
Q

binds to GP41 preventing the conformational and structural changes needed to allow fusion of the viral envelope with the host cell membrane

A

enfuvirtide

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4
Q

what drug is the ONLY parenteral (subQ) antiviral agent?

A

enfuvirtide

- it is a large, 36 AA peptide

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5
Q

side effects:

  • local injection site reactions
  • insomnia, HA, dizziness, nausea
  • hypersensitivity is rare
A

enfuvirtide

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6
Q

competitive inhibition of HIV reverse transcriptase
- incorporation into the growing viral DNA chain (leads to premature chain termination d/t inhibition of binding with incoming nucleotide

A

NRTI’s

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7
Q

name the 6 nucleoSIDE reverse transcriptase inhibitors

A
  • abacavir
  • didanosine
  • lamivudine
  • emtricitabine
  • stavudine
  • zidovudine
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8
Q

what is the 1 nucleoTIDE reverse transcriptase inhibitor?

A

tenofovir

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9
Q

guanosine analog

  • available in fixed dosage combinations with lamivudine or zidovudine
  • serum levels can be increased with concurrent ethanol ingestion
A

abacavir

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10
Q

what are the adverse effects of abacavir?

A
  • hypersensitivity (8% in the first 6 weeks of therapy)
  • fever, fatigue, nausea, vomiting, diarrhea, abdominal pain
  • respiratory: dyspnea, pharyngitis, cough
  • skin rash (50%)***
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11
Q

synthetic analog of deoxyadenosine

  • causes dose dependent pancreatitis***
  • retinal changes with optic neuritis
  • increased risk of lactic acidosis and hepatic steatosis when combined with stavudine
A

didanosine

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12
Q

cytosine analog

  • active against both HIV and HBV
  • HA, dizziness, insomnia, fatigue, dry mouth, hsrxn rare
A

lamivudine

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13
Q

fluorinated analog of lamivudine

  • active against both HIV and HBV
  • long intracellular half-life allows for once daily dosing
  • causes HA, diarrhea, nausea, rash
  • hyperpigmentation of palms/soles may be observed, especially in African Americans
A

emtricitabine

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14
Q

thymidine analog

  • causes dose dependent peripheral sensory neuropathy
  • causes dyslipidemia
  • increased risk of lactic acidosis and hepatic steatosis when combined with didanosine
A

stavudine

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15
Q

deoxythymidine analog

  • first antiretroviral drug to be approved
  • causes: macrocytic anemia, neutropenia, GI intolerance
A

zidovudine

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16
Q

acyclic analog of adenosine

  • active against both HIV and HBV
  • disoproxil or alafenamide prodrugs enhance oral absorption
  • generally well tolerated, can cause flatulence
A

tenofovir

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17
Q

bind directly to HIV reverse transcriptase in site distant from active site

  • binding induces conformational change in enzyme (reducing activity)
  • acts as noncompetitive inhibitors
A

NNRTI’s

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18
Q

develops rapidly with monotherapy

  • HIV transcriptase point mutations alter binding
  • no cross resistance between these and NRTI’s
A

NNRTI’s

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19
Q

what are the adverse effects of NNRTI’s?

A

GI intolerance, skin rash

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20
Q

what drug class is metabolized by the CYP450 system, leading to many drug-drug interactions?

A

NNRTI’s

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21
Q

what are the first generation NNRTI’s? (3)

A
  • delavirdine
  • efavirenz
  • nevirapine
22
Q

what are the second generation NNRTI’s? (2)

A
  • etravirine

- rilpivirine

23
Q

this drug not used often d/t decreased potency relative to other NNRTI’s

  • causes skin rash (up to 38% of pts)
  • HA, fatigue, nausea, diarrhea, increased aminotransferase
A

delavirdine

- extensively metabolized by CYP3A and CYPD6

24
Q

can be given once daily d/t increased half-life

  • metabolized by CYP3A4 and CYP2B6
  • CNS adverse effects HA, dizziness, drowsiness, INSOMNIA, NIGHTMARES
  • skin rash in up to (28%)
A

efavirenz

25
Q

the first NNRTI to be approved for HIV

  • metabolized for CYP3A
  • used in preventing transmission of HIV from mother to child
  • causes rash (20%), can be dose limiting
  • liver toxicity (4%)
A

nevirapine

26
Q

diarylpyrimidine

  • designed to overcome HIV resistance to first generation NNRTI’s
  • can cause rash, nausea, diarrhea
A

etravirine

- substrate and inducer of CYP3A4 and an inhibitor of CYP2C9 and CYP2C19

27
Q

diarylpryrimidine

  • coformulated with entricitabine and tenofovir
  • metabolized with CYP3A4
  • can cause rash, depression, HA< insomnia, increased serum aminotransferase
  • high doses associated with QT prolongation
A

rilpivirine

28
Q

bind HIV integrase

- inhibits strand transfer and prevents ligation of reverse-transcribed HIV DNA into the xsome of the host cell

A

INSTI’s

29
Q

what are the adverse effects of INSTI’s?

A

generally well tolerated

- HA and GI effects most common

30
Q

what is the suffic for INST’s?

A

** all end in -gravir **

31
Q

what are the INST’s?

A
  • dolutegravir
  • elvitegravir
  • raltegravir
32
Q

preferred agent for treatment of treatment-naive patients when combined with:

  • tonofovir/emtricitabine
  • abacavir/lamivudine
A

dolutegravir

- adverse effects infrequent

33
Q

approved in 2012

  • only available as combination pill (stribild= elvitegravir, cobicistat, emtricitabine, tenofovir)
  • requires boosting to be efficacious -> combine with cobicistat
A

elvitegravir

- few adverse effects

34
Q

preferred treatment option for treatment-naive patients

  • hald life is 9 hrs
  • adverse effects uncommon
A

raltegravir

35
Q

this group blocks the HIV protease and prevents the maturation of the final structural proteins that make up that mature virion core
- specifically and competitively inhibit the action of HIV aspartyl protease

A

protease inhibitors

36
Q

resistance develops quickly with monotherapy
- causes: GI intolerance, lipodystrophy (hyperglycemia/hyperlipidemia, lipoatrophy/fat deposition), redistribution and accumulation of body fat

A

protease inhibitors

- metabolized by CYP3A4

37
Q

which protease inhibitor has the most pronounced inhibitory effect on CYP3A4 metabolism?

A

ritonavir

38
Q

which protease inhibitor has the least inhibitory effect of CYP3A4 metabolism?

A

saquinavir

39
Q

what are the 9 protease inhibitors?

A
  • atazanavir
  • darunavir
  • fosamprenavir
  • indinavir
  • lopinavir
  • nelfinavir
  • ritonavir
  • saquinavir
  • tipranavir
40
Q

frequently prescribed

  • once daily dosing
  • causes diarrhea and nausea, skin rash
A

atazanavir

- inhibits CYP3A4, CYP2C9, UGT1A1

41
Q

must be co-administered with ritonvir or cobististat

  • causes rash, potential hsrxn in pt with sulfa allergy
  • metabolized by CYP3A4
A

darunavir

42
Q

prodrug of amprenavir

  • often administere with low dose ritonavir
  • causes hA, N/D, paresthesias, depression
  • potential hsrxn in pt with sulfa allergy
A

fosamprenavir

43
Q

this protease inhibitor causes unconjugated bilirubinemia and nephrolithiasis

  • drinking 1.5L of water daily helps prevent kidney stones
  • boosting with ritonavir allows for twice daily dosing (increase chance for kidney stones)
A

indinavir

44
Q

this protease inhibitor only available in combination with low dose ritonavir
- generally well tolerated

A

lopinavir

45
Q

this protease inhibitor causes diarrhea and flatulence

A

nelfinavir

46
Q
  • *high rate of GI side effects at standard doses**
  • very potent CYP450 inhibitor, used primarily as booster
  • lower dose used for inhibitorion of CYP3A4
A

ritonavir

47
Q

first approved protease inhibitor

  • reformulated for once daily dosing with ritonavir
  • causes N/D, GI discomfort, dyspepsia (less effects when boosted by ritonavir)
A

saquinavir

48
Q

indicated in pts resistant to other protease inhibitors

  • combined with ritonavir
  • causes NVD, abd pain
  • urticarual or maculopapular rash
  • potential hsrxn in pt with sulfa allergy
A

tipranavir

49
Q

what are the HAART’s?

A

2 NRTI’s plus either:

  • 1 protease inhibitor
  • 1 NNRTI
  • 1 INSTI
50
Q
  • abacavir + lamivudine + dolutegravir
  • (tenofovir + emtricitabine) + dolutegravir
  • (tenofovir + emtricitabine) + darunavir/ritonavir
  • (tenofovir + emtricabine) + elvitegravir/cobicistat
A

examples of HAART’s

SBL Exam 2 (13 decks)

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