Guidelines for the Use of Antiretroviral Agents in Adults and Adolescents Living with HIV

The information in the brief version is excerpted directly from the full-text guidelines. The brief version is a compilation of the tables and boxed recommendations.

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Appendix B: Drug Characteristics Tables

Characteristics of the CCR5 Antagonist

Last Updated: October 17, 2017; Last Reviewed: October 17, 2017

Appendix B, Table 6. Characteristics of the CCR5 Antagonist
Generic Name
Trade Name
Formulations Dosing Recommendationsa
Serum Half-Life Elimination/
Metabolic Pathway
Adverse Eventsb
  • 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
a For dosage adjustment in hepatic insufficiency, see Appendix B, Table 7.
b Also see Table 14.

Key to Acronyms: 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

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