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2 Which Regimen to Start

Overview

  • Goal is sustained suppression of pVL to <40 copies/mL
  • Treatment is life-long
  • Individualize based on baseline resistance testing, pVL, HLA*B5701 testing, results of tropism testing if applicable, convenience, tolerability, toxicities, drug interactions, co-morbidities

ARV regimen options for first-line therapy

3rd Agent
 Generic name, abbreviationBrand NameUsual dose in first lineContraindications related to toxicity or lack of efficacyFood effectMajor side effects and toxicitiesMajor 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 Viread 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 (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 HLA-B*5701 positivity; pVL>100,000 copies/mL   Hypersensitivity reaction  
lamivudine-zidovudine (150–300 mg) Combivir 1 tablet BID None   Headache, nausea, anemia, neutropenia, lipoatrophy  
Non-nucleoside reverse transcriptase inhibitor (NNRTI) efavirenz Sustiva 600 mg daily Pregnancy + Take on empty stomach Sleep disturbance, abnormal dreams, mood changes, rash, hepatotoxicity CYP450 metabolized drugs
etravirine Intelence 200 mg BID None + Take with food Rash
nevirapine Viramune 400mg daily
Lead in dose (200mg daily) × 14 days
CD4>400 cells/mm³ in men, CD4>250 cells/mm³ in women   Rash (may be severe), hepatotoxicity
rilpivirine Edurant 25 mg daily pVL>100,000 copies/mL; concomitant PPIs + Take with a meal (400 kcal) Rash; early benign increase in serum creatinine CYP450 metabolized drugs; PPIs
Boosted Protease inhibitor (PI) atazanavir Reyataz 300 mg daily with ritonavir Concomitant PPIs* + Take with food (340 kcal) Benign hyperbilirubinemia
darunavir Prezista 800 mg daily with ritonavir None + Take with food Rash CYP450 metabolized drugs
lopinavir-ritonavir (200–50 mg) Kaletra 2 tablets BID or 4 tablets daily Established or high risk of CVD − (but food may improve tolerability) GI intolerance, dyslipidemia
ritonavir Norvir 100 mg daily with PI   + Take with food GI intolerance
Integrase Inhibitor raltegravir Isentress 400 mg BID None   None Rifampin
CCR5 Inhibitor maraviroc Celsentri 300 mg BID Non-CCR5 tropic virus on tropism testing   None CYP450 metabolized drugs
Multi-class combination products efavirenz-emtricitabine-tenofovir (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 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;
emtricitabine-rilpivirine-tenofovir (200–25–300 mg) Complera Renal impairment (eGFR <50 mL/min)*; pVL>100,000 copies/mL; concomitant PPIs; 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-emtricitabine-tenofovir (150–150–200–300 mg) Stribild 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
* 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

See also: 6 Appendix: ARV Drug Information for the full table

ARVs and special conditions

← § 1 When to Start ARV Therapy § 3 Monitoring →