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85 Cards in this Set

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What is HAART?
• Highly Active Antiretroviral Therapy
• a combination of 3 or more ART
What is adherence?
• how closely a patient follows a prescribed treatment regimen
• willingness and ability to start and take medications as prescribed
• can also be affected by cost of medication
What are the different antiretroviral classes?
• Fusion inhibitors
• Nucleos/tide Reverse Transcriptase Inhibitors (NRTIs)
• Non-Nucleos/tide Reverse Transcriptase Inhibitors (NNRTIs)
• Protease Inhibitors (PIs)
What are goals of antiretroviral therapy?
• improvement of quality of life
• maximum and durable suppression of viral load
• reduction of HIV-related morbidity and mortality
• restoration and/or preservation of immunologic function
What are risks of not treating HIV with antiretrovirals?
• increase possibility of progression to AIDS
• increase risk of HIV transmission
• possible damage to immune system
What are benefits of not treating an HIV patient with antiretrovirals?
• avoid drug-related toxicities that impact quality of life
• decrease risk of treatment fatigue
• delay in resistance development
• more time for new drug development
• preserve treatment options
What is the MOA of fusion inhibitors?
prevent GP120 from binding to CD4 cells
Give an example of a fusion inhibitor
Enfuvirtide (Fuzeon); T-20
What is the dose for Enfuvirtide (Fuzeon) T-20?
90 mg SC BID
What are local site reactions caused by Enfuvirtide/T-20 (Fuzeon)?
• bruising
• itching
• nodules or cysts
• pain
• redness
• symptoms of induration
What is the MOA of Nucleos/tide Reverse Transcriptase Inhibitors?
• inhibit reverse transcriptase by competitively incorporating themselves into DNA
• causes chain temination
List examples of NRTIs
• Abacavir/ABC (Ziagen)
• Didanosine/DDI (Videx)
• Emtricitabine/FTC (Emtriva)
• Lamivudine/3TC (Epivir)
• Stavudine/d4T (Zerit)
• Tenofovir/TDF (Viread)
• Zidovudine/AZT (Retrovir)
Which is the only NRTI that does not need to be renally adjusted?
Abacavir/ABC (Ziagen)
What is the dosage of Zidovudine/AZT (Retrovir)?
300 mg BID
Which NRTI also has non-HIV uses and is used to prevent perinatal transmission?
Zidovudine/AZT (Retrovir)
Which drug should Zidovudine/AZT (Retrovir) not be combined with?
Stravudine/d4T (Zerit)
What is the dosing for Didanosine/DDI (Videx)?
• > 60 kg: 400 mg EC QD
• < 60 kg: 250 mg EC QD

* EC = enteric-coated
Why should Didanosine/DDI (Videx) not be taken with food?
it decreases the bioavailability of the drug
Didanosine/DDI (Videx) can be taken with food if combined with this drug?
Tenofovir/TDF (Viread)
What is the dosing of Stavudine/d4T (Zerit)?
• > 60 kg: 40 mg BID
• < 60 kg: 30 mg BID
Stavudine/d4T (Zerit) should not be combined with which drug?
Zidovudine/AZT (Retrovir)
What is the dosing for Lamivudine/3TC (Epivir)?
• 150 mg BID OR
• 300 mg QD
Which drug should you not combine with Lamivudine/3TC (Epivir)?
Emitricitabine/FTV (Emtriva)
Lamivudine/3TC (Epivir) is also FDA-approved to treat what (besides HIV)?
hepatitis B
What is the dosing for Abacavir/ABC (Ziagen)?
• 300 mg BID OR
• 600 mg QD
What is the dosing for Tenofovir/TDF (Viread)?
300 mg QD
Which drug is the only nucleotide reverse transcriptase inhibitor?
Tenofovir/TDF (Viread)
What is the dosing for Emtricitabine/FTC (Emtriva)?
200 mg QD
What drug should not be combined with Emtricitabine/FTC (Emtriva)?
Lamivudine/3TC (Epivir)
List the NRTI combination drugs
• Combivir
• Trizivir
• Epzicom
• Truvada
Combivir is a combination of what drugs? How would you dose it?
• Zidovudine 300 mg + Lamivudine 150 mg
• 1 tablet BID
Trizivir is combination of what drugs? How would you dose it?
• Zidovudine 300 mg + Lamivudine 150 mg + Ziagen 300 mg
• 1 tablet BID
Epzicom is a combination of what drugs? How would you dose it?
• Epivir 300 mg + Ziagen 600 mg
• 1 tablet QD
Truvada is a combination of what drugs? How would you dose it?
• Emtriva 200 mg + Viread 300 mg
• 1 tablet QD
Which drug would be given to a hospital worker who got stuck by a needle?
Combivir (Zidovudine + Lamivudine)
What are side effects of NRTIs?
• Headache
• Lactic acidosis w/ hepatic steatosis: SOB, irregular HR, fatigue, N/V, weight loss (esp. w/ DDI & d4T)
• Lipoatrophy: fat thinning (esp. w/ DDI & d4T)
• Pancreatitis (esp. w/ DDI & d4T; DDI > d4T)
• Peripheral neuropathy (esp. w/ DDI, d4T, hydroxyurea, INH)
• Stomach upset: N/V/D (esp. w/ DDI)
What are side effects of Zidovudine/AZT (Retrovir)?
• anemia
• muscle aches
• neutropenia
• tiredness
What are side effects of Stavudine/d4T (Zerit)?
• increased cholesterol
• increased triglycerides
What statins would you use on a patient with HIV?
• Atorvastatin (Lipitor) 80 mg
• Rosuvastatin (Crestor) 10 mg
What are symptoms of an Abacavir Hypersensitivity Reaction?
symptoms of skin rash + 2 or more of the following:

• body aches
• cough
• fatigue
• fever
• N/V/D/stomach pain
• SOB
What is the MOA of Non-nucleoside Reverse Transcriptase Inhibitors?
inhibit reverse transcriptase by noncompetatively attaching to and inhibiting the enzyme itself
List examples of NNRTIs
• Delavirdine/DLV (Rescriptor)
• Efavirenz/EFV (Sustiva)
• Nevirapine/NVP (Viramune)
What is the dosing for Nevirapine/NVP (Viramune)?
• 200 mg QD x 14 days, then 200 mg BID OR
• 400 mg QD
Why is Nevirapine/NVP (Viramune) often dose titrated?
to decrease the incidence of rash
Is Nevirapine/NVP (Viramune) an inhibitor or inducer of the CYP450 3A system?
inducer
What is the dosing for Efavirenz/EFV (Sustiva)?
600 mg QD (at bedtime)
What is the dosing of Efavirenz/EFV (Sustiva)?
600 mg QD (at bedtime)
True/False: Efavirenz/EFV (Susdtiva) should not be taken with food.
The correct answer is: True
Is Efavirenz/EFV (Sustiva) an inhibitor or inducer?
inhibitor & inducer
What are side effects of NNRTIs?
• Rash: #1 reason for D/C drug (nevirapine > delavirdine > efavirenz)

• Liver toxicity (greatest freqency w/ nevirapine)

• CNS toxicity (w/ Efavirenz): confusion, difficulty concentrating, abnormal thinking, abnormal dreams (colorful vs. dreams), dizziness
What is the MOA of Protease Inhibitors?
prevent HIV from being successfully assembled and release from infected CD4 cells
List examples of protease inhibitors
• Amprenavir/APV (Agenerase)
• Atazanavir/ATV (Reyataz)
• Fosamprenavir/f-APV (Lexiva)
• Indinavir/IDV (Crixivan)
• Lopinavir/ritonavir - LPV/r (Kaletra)
• Nelfinavir/NFV (Viracept)
• Ritonavir/RTV (Norvir)
• Saquinavir/SQV (Invirase)
• Tipranavir (Aptivus)
Which protease inhibitor is often given for its boosting effects on other protease inhibitors?
ritonavir/RTV (Norvir)
What is the dosing of Saquinavir/SQV (Invirase)?
only boosted with Ritonavir/RTV

• 1000/100 mg BID or
• 2000/100 mg QD

* 100 mg doses are Ritonavir/RTV
What is the dosing of Ritonavir/RTV (Norvir)?
• 600 mg BID (as a sole protease inhibitor)
• 100-200 mg QD-BID (as a booster)
Is Ritonavir a CYP450 inhibitor or inducer?
a very powerful inhibitor
What is the dosing for Indinavir?
• 800 mg TID (unboosted)
• 800/100-200 mg QD (w/ RTV)
Can you take Indinavir/IDV (Crixivan) with food?
do not take with food except when taken with RTV
Which drug should not be combined with Indinavir/IDV (Crixivan)?
Atazanavir/ATV (Reyataz)
Indinavir/IDV (Crixivan) should be taken with a lot of water. Why?
to prevent kidney stones
What is the dosing of Lopinavir/ritonavir (Kaletra) LPV/r?
• 2 tablets BID OR
• 4 tablets QD
What is the dosing for Atazanavir/ATV (Reyataz)?
• unboosted: 400 mg QD
• w/ RTV: 300/100 mg QD
Atazanavir/ATV (Reyataz) should be taken with food, but should not be combined with what other medication?
Indinavir/IDV (Crixivan)
What is dosing for Fosamprenavir/f-APV (Lexiva)?
• unboosted: 1400 mg BID
• w/ RTV: 1400/200 mg QD
Fosamprenavir/f-APV (Lexiva) should not be combined with what drug?
• Amprenavir/APV
• f-APV is a prodrug of APV
What is the doing for Tipranavir (Aptivus)?
• only comes boosted: 500/200 mg BID
What are side effects of protease inhibitors?
• diarrhea (esp. w/ Nelfinavir, but also w/ saquinavir, Lopinavir/ritonavir)

• increased cholesterol (esp. w/ ritonavir containing regimens; except Atazanavir)

• increased glucose (esp. w/ indinavir)

• lipodystrophy: increase in abdominal girth, breast size, and buffulo hump (most common side effect)

• stomach upset: N/V/D/stomach pain
Which protease inhibitors contain a sulfonamide moiety and can cause a rash?
• Amprenavir
• fos-amprenavir
• Tipranavir
Which protease inhibitors can increase bilirubin levels?
• Atazanavir
• Indinavir
Which protease inhibitor can cause kidney stones, hematuria, and skin reactions?
Indinavir/IDV (Crixivan)
What are drug interactions with Zidovudine/AZT (Retrovir)?
• antagonism with Stavudine/d4T
• caution with combo products Combivir & Trizivir
Why should you not administer Lamivudine/3TC (Epivir) and Emtricitabine/FTC (Emtriva) together?
they are similar compounds
Which combination products should you not administer with Lamivudine/3TC (Epivir) or Emtricitabine/FTC (Emtriva) because they also contain the same products?
• Combivir, Trizivir, Epzicom (contain Lamivudine)

• Truvada (contains Emtricitabine)
What is the affect of Tenofovir/TDF (Viread) on Didanosine/DDI (Videx) and how do you dose adjust?
• Tenofovir will increases Didanosine levels regardless if taken with or without food or if taken separate or together

• decrease Didanosine dose: 200 mg QD if < 60 kg; 250 mg QD if > 60 kg
What are the affects of either Tenofovir or Efavirenz on Atazanavir?
• both drugs will decrease Atazanavir levels

• recommoended dose adjustment for both: ATV 300 mg + 100 mg RTV
List drugs that will decrease Lopinavir/ritonavir levels. What are recommended dosage adjustments?
• Efavirenz
• Nevirapine
• Fosamprenavir

• recommended dose adjustment for EFV and NFV: increase LPV/r to 600/150 mg BID in protease inhibitor experienced patients

* Fosamprenavir should not be co-administered as doses are not established
What happens to levels of Didanosine/DDI if taken with food?
• it will decrease DDI levels by 55%

• DDI should be taken at least 30 min before or 2 hours after a meal (except when taken with Tenofovir)
What is the affect of food on Efavirenz?
• will increase Cmax by 39-79& with high fat/caloric meals
• should take Efavirenz on an empty stomach to decrease incidence of CNS toxicity
What is the affect of food on Indinavir (unboosted)?
• food with decrease levels by 77%
• should take 1 hour before or 2 hrs after a meal (except when taken with Ritonavir)
What is the affect of food on Atazanavir?
• food increases bioavailability of the drug
• should take Atazanavir with food
• should avoid antacids, PPIs, & H2 blockers (will decrease bioavailabilty)
What is the affect of food on Lopinavir/r (Kaletra)?
• will increase area under the curve (AUC) by 48-80% with a moderate fat meal
• should take Lopinavir/r (Kaletra) with food
What is the affect of food on Nelfinavir?
• food increases the levels 2-3 fold
• should take with a meal or snack
What patients will you always treat with antiretrovirals?
• all patients with AIDS
• patients with severe symptoms regardless of CD4 count
• asymptomatic patients with CD4 < 200
What patients should you offer treatment?
asymptomatic patients with CD4 > 200 but < 350
What patients will you defer treatment?
asymptomatic patient with:
• CD4 > 350 and viral load > 100,000
• CD4 > 350 and viral load < 100,000