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Therapeutics 3 > HIV > Flashcards

HIV Flashcards

1
Q

3 primary modes of HIV transmission

A

Sexual
Parenteral (needles)
Perinatal (mother/baby)

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2
Q

Ways to limit risk of transmission

A 
Condoms/safe sex
no needle sharing
screen blood for contamination
HIV treatment during pregnancy
do not breastfeed after delivery if safe alternatives are available
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3
Q

Treatment goals of antiretroviral therapy

A 
Maximally and durably suppress viral replication
Avoid development of drug resistance
Restore and preserve immune function
Prevent opportunistic infections
Minimize drug adverse effects
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4
Q

HIV RNA

A

quantifies viremia, helps to monitor disease progression and treatment effectiveness.
Monitor at baseline, after therapy changes, and every 3-4 months

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5
Q

CD4 lymphocyte count

A

Measures how far the HIV infection has progressed
Measures CD4%, because absolute can vary
Helps decide when to initiate treatment
Should be monitored at diagnosis and every 3-6 months

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6
Q

Indications to start antiretroviral therapy

A

Any AIDS-defining illness
CD4 count 500, initiation is encouraged
Pregnancy
Treating Hep B Co-infections

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7
Q

Antiretroviral therapy guidelines

A

Therapy should contain at least 3 drugs in a combination of an NNRTI or a retonavir-boosted PI with two NRTIs or NtRTIs.

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8
Q

3 combo therapy recommendations for treatment-naive patients

A

NNRTI (efavirenz) + 2 NRTIs (tenofovir + emtricitabine)
Ritonavir-boosted PI (atazanavir+ritonavir or darunavir+ritonavir) + 2 NRTIs (Tenofovir+emtricitabine
Integrase inhibitor (raltegravir) + 2 NRTIs (tenofovir+emtricitabine)

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9
Q

What should be done prior to selecting a new antiretroviral regimen once the patient has failed the original treatment?

A

Comprehensive review of patient’s severity of disease
Antiretroviral treatment history
Adherence to therapy
intolerance or toxicity
concomitant drug therapies
comorbidities
results of current and past HIV resistance testing

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10
Q

Nucleoside Reverse Transcriptase Inhibitors (NRTI) MOA

A

Prevents conversion of RNA to DNA by inhibiting reverse transcriptase

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11
Q

NRTI drugs

A 
Ziagen - abacavir (ABC)
Emtriva - emtricitabine (FTC)
Epivir - lamivudine (3TC)
Viread - tenofovir (TDF)
Retrovir - zidovudine (AZT, ZDV)
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12
Q

NRTI class ADRs

A

Lactic acidosis/hepatic steatosis
pancreatitis - discontinue HAART and treat
Lipodistrophy (only seen with tesamorelin/Egrifta)

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13
Q

Ziagen/abacavir-specific BBW

A

Serious, sometimes fatal hypersensitivity reaction!! - test patients for HLA-B*5701 allele. If positive, pt has 70% likelihood of having a reaction

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14
Q

NRTI Class general BBWs

A

Lactic acidosis

Acute, severe exacerbations of HBV following discontinuation of HAART, do not use in pts with concomitant HBV

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15
Q

Retrovir/zidofudine-specific BBWs

A 
hematologic toxicity (neutropenia and severe anemia)
mypoathy with prolonged use
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16
Q

Which NRTI’s should be used with caution in patients with hepatic impairment?

A

Ziagen/abacavir
Viread/tenofovir
Retrovir/zidovudine

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17
Q

Which NRTIs should be used with caution in patients with renal impairment

A

Emtriva/emtricitabine
Epivir/lamivudine
Viread/tenofovir
Retrovir/zidovudine

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18
Q

Non-Nucleoside Reverse Transcriptase Inhibitor (NNRTI) MOA

A

binds to reverse transcriptase, blocking DNA polymerase activities including replication

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19
Q

NNRTI Class ADRs

A 
Rash including SJS
Drug interactions (3A4 is major!! also 2C19 and 2C9)
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20
Q

NNRTI drugs

A

Sustiva - efavirenz (EFV)
Intelence - etravirine (ETR)
Edurant - rilpivirine (RPV)

21
Q

Sustiva/efavirenz contraindications

A 
significant hypersensitivity (including SJS)
concurrent use of bepridil, cisapride, midazolam, pimozide, triazolam, St. John's Wort, or ergot alkaloids
22
Q

Sustiva/efavirenz side effects

A

CNS effects
fat redistribution
hypercholesterolemia
immune reconstitution syndrome
rash
use with caution in patients with seizure disorder
not recommended for patients with hepatic impairment

23
Q

Intelence/etravirine ADRs

A

fat redistribution
immune reconstitution syndrome
skin reactions/hypersensitivity (SJS)

24
Q

Edurant/rilpivirine contraindications

A

concurrent use of carbamazepine, dexamethasone (more than 1 dose), oxcarbazepine, phenobarb, phenytoin, PPIs, rifabutin, rifampin, rifapentine, or St. John’s Wort

25
Q

Edurant/rilpivirine ADRs

A 
Depressive disorders
Fat Redistribution
Hepatotoxicity
Immune reconstitution syndrome
QT prolongation
26
Q

what drugs make up Truvada

A

tenofovir and emtricitabine (2NRTIs)

27
Q

What drugs make up Atripla

A

tenofovir, entricitabine, and efavirenz (NNRTI + 2NRTIs)

28
Q

What drugs make up Complera

A

tenofovir, rilpivirine, and emtricitabine (NNRTI + 2 NRTIs)

29
Q

Integrase inhibitors MOA

A

Inhibit catalytic activity of integrase, preventing integration of proviral gene into human DNA

30
Q

Integrase inhibitors Class ADRs

A

Rifampin and etravirine decrease raltegravir

Omeprazole increases raltegravir

31
Q

Integrase inhibitor drugs

A

Issentress - raltegravir (RAL)

Stribild - elvitegravir (EVG) (co-formulated with cobicistat, tenofovir, and emtricitabine)

32
Q

Stribild/elvitegravir BBWs

A

CI in concurrent use of afluzosin, cisapride, ergot derivatives, lovastatin, midazolam, pimoxide, rifampin, sildenifil, simvastatin, triazolam, and SJW
Lactic acidosis
exacerbations of HBV with discontinuation

33
Q

Protease Inhibitor (PI) MOA

A

inhibits cleavage of viral polyprotein precursors into individual functional proteins required for infectious HIV

34
Q

PI Class ADRs

A

bleeding - avoid in hemophiliacs or with anticoagulants

hyperlipidemia, insulin resistance/diabetes, increased LFTs, lipodystrophy, decreased bone mineral density

35
Q

PI Drugs

A

Reyataz - atazanavir (ATV)
Prezista - darunavir (DRV)
Kaletra - lopinavir + ritonavir (LPV/r)

36
Q

Reyataz contraindications

A

hypersensitivity

3A4 inducers

37
Q

Prezista contraindications

A

coadministration with other 3A4 substrates

38
Q

Kaletra contraindications

A

hypersensitivity

3A4 substrates

39
Q

how is ritonavir (Norvir) used in therapy?

A

it is a “booster” for PIs

40
Q

how does ritonavir affect the CYP system?

A

potent 3A4 inhibitor and substrate
2D6 substrate
has mixed dose-dependent induction and inhibition of other phase 1 and 2 enzymes

41
Q

Fuzeon (enfuviritide) MOA

A

binds to the first heptad-repeated in the gp41 subunit of viral envelop glycoprotein. inhibits fusion of HIV virus with CD4 cells by blocking the conformational change in gp41 required for membrane fusion and entry into cell

42
Q

Fuzeon drug interactions

A

NONE

43
Q

Fuzeon BBW/ADRs

A 
Hypersensitivity
immune reconstitution syndrome
injection site reactions
pneumonia
use caution in patients with coagulation disorders or receiving anticoagulants - increased risk of bleeding at injection site
do not use in ART-naive patients
44
Q

CCR5 antagonist MOA

A

selectively and reversibly binds to chemokine coreceptors located on human CD4 cells. prevents interaction between human CCR5 coreceptor and the gp120 conformation change required for HIV fusion with CD4 cell and subsequent cell entry

45
Q

CCR5 drugs

A

Selzentry - maraviroc (MVC)

46
Q

Selzentry drug interactions

A

3A4 inducers and inhibitors

47
Q

Selzentry BBW

A

possible drug-induced hepatotoxicity with allergic type features has been reported

48
Q

Selzentry ADRs

A 
immune reconstitution syndrome
infections
postural hypotension
skin and hypersensitivity reactions
use with caution in CV disease
use with caution in hepatic impairment
renal impairment increases drug concentrations

Therapeutics 3 (8 decks)

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