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Pharmacology Semester II > Exam III HIV Pharm > Flashcards

Exam III HIV Pharm Flashcards

Identify when not to use, ADRs and DDIs

1
Q

PathoPhys of HIV

A
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2
Q

HIV 1 versus HIV 2

A

HIV = retrovirus = lentivirus

HIV - 1

  • More Prevalent*
  • More Pathogenic*
  • HIV-1 VArients divided into groups: M, N, O, P*
  • Within M (Major) group there are classes A, B, C, D, F, G, H, J, K*
  • Origins Chimpanzee*

HIV - 2

  • Largely limited to Western Africa*
  • Less pathogenic*
  • Treatment differences (HIV-2 resisitant to NNRTI’s)*
  • Origins: Sooty Mangabey*
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3
Q

Cell Surface receptors for HIV

A

1. CD4 Receptors

2. Chemokine Receptors

CCR5

  • Found in majority of sexually transmitted HIV - 1 infection*
  • Generally detectable over the entire course of infection*
  • FDA-approved CCR5 inhibitor available*
  • Rare delta 32 genetic mutation (immunity)*

CXCR4

Generally observed in PTs with advanced AIDS

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4
Q

HIV testing

A

Seroconversion window period

Time of infection to production of antibodies

Average 3-4 weeks but up to 6 months

Acute HIV

HIV tests

Rapid (antibody tests)

  • Blood or oral fluid sample (eg., in-home oral HIV test through OraQuick)*
  • Faster results; require confirmation if reactive*

Combination immunoassy (‘fourth - generation test’)

  • Detects HIV-1 and HIV-2 antibodies and HIV-1 protein 24 (p24) antigen*
  • More sensitive in diagnosing early infection*

PCR test (polymerase chain reaction test)

Viral load tests: detect genetic material of HIV

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5
Q

Antiretroviral (ART) Drug Classes

A

Nucleoside and nucleotide RT inhibitors (NRTI/NtRTI)

Generic names and in INE (eg., emtricitabine)

Non-nucleoside RT inhibitors (NNRTI)

Generic names end in virine (eg., rilpivirine)

Protease inhibitors (PI)

Generic names end in: NAVIR (eg., darunavir)

Integrase inhibitors (INSTI)

Generic names and in TEGRAVIR

Phamacokinetic boosters (for PIs and INSTIs)

Norvir (ritonavir): protease inhibitor

Tybost (cobicistat, COBI)

CCR5 inhibitor

Fusion inhibitor

Monclonal antibody (post-attachment inhibitor)

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6
Q

Nucleoside and nucleotide reverse transcriptase inhibitors (NRTI)

A

Emtricitabine, FTC

Lamivudine, 3TC

Tenofovir Disoproxil Fumarate or TDF

Tenofovir alafenamide, TAF

  • Better tolerated version of Tenofovir*
  • Co-formulated with Emtricitabine in Descovy for HIV and HBV*
  • FDA approved for HBV as Vemlidy*
  • Not FDA approved for HIV as Vemlidy*

Abacavir, ABC

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7
Q

Combination NRTI Products

A
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8
Q

NRTI Characteristics I

A
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9
Q

NRTI Characteristics II

A
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10
Q

NRTI Characteristics III

A
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11
Q

Non-nucleoside reverse transcriptase inhibitors (NNRTI)

A

Doravirine

Rilpivirine, RPV

Efavirenz, EFV

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12
Q

Combination NNRTI Products

A
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13
Q

NNRTI Characteristics

A

MoA

Inhibit RT by directly binding to it (non-competitive inhibition of RT)

Drug class side effects

Rash

  • Often diffuse, slightly raised, itchy*
  • Severe skin reactions reported (rare):*
  • Toxic epidermal necrolysis (TEN)*
  • Steven-Johnson Syndrome (SJS)*

Liver Toxicity

Livertox Database: https://livertox.nih.gov/

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14
Q

NNRTI Drug Specific Side Effects

A

Doravirine:

N/D, abdominal pain, dizziness, HA, fatigue, Abnormal dream

Rilpivirine:

Depression, insomnia, HA, rash

Efavirenz:

CNS effects such as: dizziness, drowsiness, sleepiness, insomnia, vivid dreams

Bedtime dosing

Retrospective case reports of Neural Tube Defects in the first trimester

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15
Q

NNRTI Characteristics

A

Pharmacokinetics:

Absorption/food effects:

Take with food: Rilpivirine

Take on empty stomach: Efavirenz

Metabolism

Liver metabolism via CYP450

Substrates of CYP3A4

Efavirenz is a substrate of CYP2B6 and its levels may accumulate in genetic polymorphism

<em>Lower-dose Efavirenz in Symfi Lo may be better tolerated</em>

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16
Q

NNRTI Drug interactions

A
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17
Q

Protease Inhibitors (PI)

A

Darunavir, DRV

600mg tab - dosed VID with Ritonavir (PK Booster) 100mg BID

800 mg tab - dosed QD with Ritonavir (PK Booster) 100mg QD or Cobicistat 150mg QD

Ritonavir, RTV

Atazanavir, ATV

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18
Q

Combination PI products

A
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19
Q

PI MoA and Class side effects

A

MoA:

Inhibit HIV protease

Prevent cleavage of proteins, resulting in no active proteins

Drug Class Side Effects:

GI

Hyperlipidemia

Possible CV risk

Blood Glucose elevations

Liver toxicity

Possible bleeding risk in hemophiliacs

Body fat re-distribution

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20
Q

PI Drug-specific side effects:

A

Possible skin reaction due to sulfonaminde:

Darunavir

Fosamprenavir

Tipranavir

Potential Cardiovascular risk (recent study data):

Darunavir

Hyperbilirubinemia and nephrolithiasis:

Atazanavir

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21
Q

PI Pharmacokinetics

A

Absorption/food effects:

Acid-suppressive therapy interacts with atazanavir

Metabolism:

Substrates of CYP 450 (hepatic and intestinal) and P-gp

Most PIs are also inhibitors of CYP enzymes

Many drug interactions (eg., statins, fluticasone, salmeterol, rifampin, Hep C antivirals, anticoagulants, certain antifungals, quetiapine, St. John’s Wort)

Ritonavir: strongest metabolic inhibitor in class (CYP3A4 and 2D6)=> boosts levels of other PIs

22
Q

Integrase Inhibitors (INSTI)

A

Raltegravir, RAL

Dolutegravir, DTG

Elvitegravir, EVG

Discontinued as an individual tablet

Evitegravir available in combo product

23
Q

INSTI Combinations

A
24
Q

INSTI MoA, Side Effects

A

MoA:

Inhibit integrase, prevent integration of Viral DNA into Human DNA

Drug Class side effects:

Insomnia, HA, possible weight gain, increase in liver enzymes, and creatine kinase (CK)

Drug-specific side effects:

Dolutegravir

Neuropsychiatric effects

Neural tube defects (avoid in women of childbearing age not on contraception or within 12 weeks post conception)

Boosted INSTI (Genvoya, Stribild)

N/D, renal impairment, decrease bone mineral density (renal/bone side effects: less with Genvoya)

25
Q

INSTI Pharmacokinetics

A

Absorption:

Elvitegravir regimens - Genvoya, Stribild:

Take with food

Metabolism:

All INSTIs are substrates of UGT1A1

Some are substrates of Pg-p (raltegravir)

CYP3A substrates:

Bictegravir , dolutegravir and elvitegravir regimens

Elvitegravir requires PK boosting through CYP34A

26
Q

INSTI Drug Interactions

A
27
Q

INSTI Drug Interactions II

A
28
Q

NNRTI and INSTI Combo

A
29
Q

Pharmacokinetic Boosters

A
30
Q

CCR5 Inhibitor

A
31
Q

Fusion Inhibitor

A

Enfuvirtide, T20:

36-Amino acid synthetic peptide

Inhibits function of transmembrane gp 41

Product has to be constituted

Side effects: Injectuion site reactions >90%

Pharmacokinetics:

Metabolism: peptide; undergoes catabolism

Drug Interactions:

No Effect on CYP enzymes

No significant Drug interactions

32
Q

Post-Attachment inhibitor Ibalizumab

A
33
Q

Initiation of Antiretroviral Therapy (ART)

A
34
Q

HIV Treatment Guidelines: What to start?

A
35
Q

HIV Treatment Guidelines: What to start in certain clinical situations Integrase inhibitor + 2 NRTIs?

A
36
Q

HIV Treatment Guidelines: What to start in certain clinical situations NNRTI + 2 NRTIs?

A
37
Q

HIV Treatment Guidelines: What to start in certain clinical situations Boosted PI + 2 NRTIs?

A
38
Q

HIV Treatment Guidelines: What to start in certain clinical situations, cannot use abacavir, TAF, and TDF?

A
39
Q

Antiretroviral Treatments Not Recommended

A
40
Q

Characteristics of Dual NRTIs in initial ART regimens

A
41
Q

Characteristics of INSTIs in initial ART regimens

A
42
Q

Characteristics of NNRTIs in initial ART regimens

A
43
Q

Characteristics of PIs in initial ART regimens

A
44
Q

Considerations for selecting an initial ART regimen

A
45
Q

Current CDC PrEP recommendations

A
46
Q

CDC Guideline: Clinical Eligibility for PrEP

A
47
Q

CDC Guideline: REquirements before prescribing PrEP

A

Negative HIV test result within 1 week of PrEP start

No signs of symptoms of acute HIV injection

Normal Renal Function (eCrCl 60 mL/min or higher)

No Contraindications to Emtricitabine/TDF

Documented Hep B virus infection and immunization status

Tests for HCV infection and link to care if needed

Screen for STDs

48
Q

PT monitoring while on PrEP

A
49
Q

On-demand PrEP

A
50
Q

HIV PEP (Post-Exposure prophylaxis)

A

Pharmacology Semester II (21 decks)

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