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6 Appendix: ARV Drug Information

Antiretroviral drug dosing, administration, contraindications, toxicites, and key drug interactions

 Generic nameBrand NameUsual dose in first lineContraindicationsDosing/administration issuesMajor side effects and toxicitiesKey drug interactions
Nucleoside/tide Reverse transcriptase inhibitor (NRTI) abacavir Ziagen® 600 mg daily HLA-B*5701 positivity; pVL>100,000 copies/mL   Hypersensitivity reaction  
lamivudine 3TC® 300 mg daily None   None  
tenofovir disoproxil fumarate (DF) Viread® 300 mg daily Renal impairment (eGFR <50 mL/min)*; caution in post-menopausal women or osteoporosis (established or high risk)   Proximal renal tubular dysfunction, decreased bone mineral density, osteoporotic fractures Didanosine; caution with nephrotoxic drugs
NRTI combination products emtricitabine-tenofovir DF (200–300 mg) Truvada® 1 tablet daily Renal impairment (eGFR <50 mL/min)*; caution in menopausal women or osteoporosis (established or high risk)   Proximal renal tubular dysfunction, decreased bone mineral density, osteoporotic fractures; rash and GI intolerance in women Didanosine; caution with nephrotoxic drugs
abacavir-lamivudine (600–300 mg) Kivexa® 1 tablet daily HLA-B*5701 positivity; pVL>100,000 copies/mL   Hypersensitivity reaction  
lamivudine-zidovudine (150–300 mg) Combivir® 1 tablet BID     Headache, nausea, anemia, neutropenia, lipoatrophy  
abacavir-lamivudine-zidovudine (600-300-300) Trizivir® 1 tablet BID HLA-B*5701 positivity   Hypersensitivity reaction, Headache, nausea, anemia, neutropenia, lipoatrophy  
Non-nucleoside reverse transcriptase inhibitor (NNRTI) efavirenz Sustiva® 600 mg daily Pregnancy Take on empty stomach, preferably at bedtime Sleep disturbance, abnormal dreams, mood changes, rash, hepatotoxicity CYP450 metabolized drugs
etravirine Intelence® 200 mg BID   Take with food Rash CYP450 metabolized drugs
nevirapine Viramune® 400mg daily

CD4>400 cells/mm³ in men, CD4>250 cells/mm³ in women  Lead in dose 200mg daily × 14 day Rash (may be severe), hepatotoxicity CYP450 metabolized drugs
rilpivirine Edurant® 25 mg daily pVL>100,000 copies/mL Take with food Rash; early benign increase in serum creatinine CYP450 metabolized drugs; PPIs
Protease inhibitor (PI) atazanavir Reyataz® 400 mg daily   Take with food Benign hyperbilirubinemia; kidney stones CYP450 metabolized drugs; tenofovir DF; PPIs
atazanavir/ritonavir Reyataz®/Norvir® 300mg/100mg daily   Take with food Benign hyperbilirubinemia; kidney stones CYP450 metabolized drugs; PPIs
darunavir/ritonavir Prezista®/Norvir® 800mg/ 100mg daily   Take with food Rash CYP450 metabolized drugs
darunavir-cobicistat (800mg-150mg) Prezcobix® 1 tablet daily   Take with food; avoid taking with tenofovir DF if eGFR<70 mL/min Rash; early benign increase in serum creatinine CYP450 metabolized drugs
lopinavir-ritonavir (200–50 mg) Kaletra® 2 tablets BID or 4 tablets daily Established or high risk of CVD Take with food GI intolerance, dyslipidemia CYP450 metabolized drugs
Integrase Inhibitor raltegravir Isentress® 400 mg BID       Rifampin, aluminum, magnesium
dolutegravir Tivicay™ 50mg daily     Insomnia, headache, early benign increase in serum creatinine Metformin, iron, calcium, magnesium, aluminum
CCR5 Inhibitor maraviroc Celsentri® 300 mg BID Non-CCR5 tropic virus on tropism testing     CYP450 metabolized drugs
Multi-class combination products efavirenz-tenofovir DF-emtricitabine (600–200–300 mg) Atripla® 1 tablet daily Renal impairment (eGFR <50 mL/min)*; pregnancy; caution in menopausal women or osteoporosis (established or high risk) Take on empty stomach, preferably at bedtime Proximal renal tubular dysfunction, decreased bone mineral density, osteoporotic fractures; sleep disturbance, abnormal dreams, mood changes, rash, hepatotoxicity Didanosine; CYP450 metabolized drugs; caution with nephrotoxic drugs
rilpivirine-tenofovir DF- emtricitabine(25–300-200  mg) Complera® 1 tablet daily

Renal impairment (eGFR <50 mL/min)*; pVL>100,000 copies/mL;caution in menopausal women or osteoporosis (established or high risk)

Take with a meal (400 kcal) Proximal renal tubular dysfunction, decreased bone mineral density, osteoporotic fractures; rash Didanosine; PPIs; CYP450 metabolized drugs; caution with nephrotoxic drugs
elvitegravir-cobicistat-tenofovir DF-emtricitabine (150–150–300–200 mg) Stribild® 1 tablet daily Renal impairment (eGFR <70 mL/min)*; caution in menopausal women or osteoporosis (established or high risk) Take with food Proximal renal tubular dysfunction, decreased bone mineral density, osteoporotic fractures; early benign increase in serum creatinine; GI intolerance Didanosine; CYP450 metabolized drugs; caution with nephrotoxic drugs
dolutegravir-abacavir-lamivudine (50-600-300 mg) Triumeq® 1 tablet daily HLA-B*5701 positivity   Insomnia, headache, early benign increase in serum creatinine Metformin, iron, calcium, magnesium, aluminum
*if required in this situation, consult with the St. Paul's Hospital Ambulatory Pharmacy for dosing and monitoring recommendations
† for further information, see Drug Interactions Table or consult St. Paul's Hospital Ambulatory Pharmacy
‡ recommended doses may vary in the presence of reduced kidney function, drug resistance, or drug interations — see St. Paul's Hospital Ambulatory Pharmacy for further information

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