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Guidelines for the Use of Antiretroviral Agents in HIV-1-Infected Adults and Adolescents

Appendix B: Drug Characteristics Tables

Characteristics of CCR5 Antagonist

(Last updated:3/27/2012; last reviewed:2/12/2013)

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Appendix B, Table 6. Characteristics of CCR5 Antagonist
Generic Name (Abbreviation)/ Trade Name Formulation Dosing Recommendations
(For dosage adjustment in hepatic insufficiency, see Appendix B, Table 7.)
Serum Half-Life Elimination Adverse Events
(Also see
Table 13)
150 and 300 mg tablets 150 mg BID when given with drugs that are strong CYP3A inhibitors (with or without CYP3A inducers) including PIs (except TPV/r) 300 mg BID when given with NRTIs, T20, TPV/r, NVP, RAL, and other drugs that are not strong CYP3A inhibitors or inducers 600 mg BID when given with drugs that are CYP3A inducers, including EFV, ETR, etc. (without a CYP3A inhibitor) Take without regard to meals 14-18 hours CYP3A4 substrate
  • Abdominal pain
  • Cough
  • Dizziness
  • Musculoskeletal symptoms
  • Pyrexia
  • Rash
  • Upper respiratory tract infections
  • Hepatotoxicity, which may be preceded by severe rash or other signs of systemic allergic reactions
  • Orthostatic hypotension, especially in patients with severe renal insufficiency

Key to Abbreviations: BID = twice daily, CYP = cytochrome P, EFV = efavirenz, ETR = etravirine, MVC = maraviroc, NRTI = nucleoside reverse transcriptase inhibitor, NVP = nevirapine, PI = protease inhibitor, RAL = raltegravir, T20 = enfuvirtide, TPV/r = tipranavir + ritonavir