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

Drug Interactions

Drug Interactions between CCR5 Antagonist and Other Drugs

(Last updated:5/1/2014; last reviewed:5/1/2014)

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Table 18e. Drug Interactions between CCR5 Antagonist and Other Drugs
Concomitant Drug
Class/Name 
CCR5 Antagonist  Effect on CCR5 Antagonist or Concomitant Drug Concentrations Dosing Recommendations and Clinical Comments 
Anticonvulsants
Carbamazepine

Phenobarbital

Phenytoin
MVC  ↓ MVC possible If used without a strong CYP3A inhibitor, use MVC 600 mg BID or an alternative antiepileptic agent.
Antifungals
Itraconazole MVC  ↑ MVC possible Dose: MVC 150 mg BID
Voriconazole MVC  ↑ MVC possible Consider dose reduction to MVC 150 mg BID
Antimycobacterials
Clarithromycin MVC  ↑ MVC possible Dose: MVC 150 mg BID
Rifabutin MVC  ↓ MVC possible If used without a strong CYP3A inducer or inhibitor, use MVC 300 mg BID.
If used with a strong CYP3A inhibitor, use MVC 150 mg BID.
Rifampin MVC  MVC AUC ↓ 64% Co-administration is not recommended.

If co-administration is necessary, use MVC 600 mg BID.

If co-administered with a strong CYP3A inhibitor, use MVC 300 mg BID.
Rifapentine MVC  ↓ MVC expected Do not co-administer.
Hepatitis C NS3/4A—PIs
Boceprevir
MVC MVC AUC  ↑ 202% Dose: MVC 150 mg BID
Telaprevir MVC MVC AUC ↑ 850% Co-administration is not recommended
Herbal Products
St. John’s Wort MVC MVC possible Co-administration is not recommended.
Hormonal Contraceptives
Hormonal Contraceptives MVC No significant effect on ethinyl estradiol or levonorgestrel Safe to use in combination
Antiretroviral Drugs
INSTIs
EVG/cobi/TDF/FTC
MVC ↑ MVC possible
Do not co-administer.
RAL MVC RAL AUC ↓ 37%

MVC AUC ↓ 21%

Dose: standard
NNRTIs
EFV MVC  MVC AUC ↓ 45%
Dose: MVC 600 mg BID
ETR MVC MVC AUC ↓ 53%
Dose: MVC 600 mg BID in the absence of a potent CYP3A inhibitor
NVP MVC MVC AUC ↔
Without HIV PI: 
MVC 300 mg BID

With HIV PI (except TPV/r): 
MVC 150 mg BID

PIs
ATV
+/-
RTV


MVC With Unboosted ATV: 
MVC AUC ↑ 257%

With (ATV 300 mg and RTV 100 mg) Once Daily: 
MVC AUC ↑ 388%

Dose: MVC 150 mg BID
DRV/r MVC With (DRV 600 mg and RTV 100 mg) BID
MVC AUC ↑ 305%

With (DRV 600 mg and RTV 100 mg) BID and ETR: 
MVC AUC ↑ 210%

Dose: MVC 150 mg BID
FPV
+/-
RTV


MVC With (FPV 700 mg plus RTV 100 mg) BID plus MVC 300 mg BID:
MVC AUC ↑ 149%, Cmin ↑ 374%

With (FPV 1400 mg plus RTV 200 mg) Once Daily and MVC 300 mg Once Daily: 
MVC AUC ↑ 126%, Cmin ↑ 80%

Dose: MVC 150 mg BID
LPV/r
MVC MVC AUC ↑ 295%

With LPV/r and EFV: 
MVC AUC ↑ 153%

Dose: MVC 150 mg BID
RTV MVC
With RTV 100 mg BID: 
MVC AUC ↑ 161%

Dose: MVC 150 mg BID
SQV/r MVC
With SQV 1000 mg and RTV 100 mg BID: 
MVC: AUC ↑ 877%

With SQV 1000 mg and RTV 100 mg BID plus EFV: 
MVC AUC ↑ 400%

Dose: MVC 150 mg BID
TPV/r MVC
With TPV 500 mg and RTV 200 mg) BID: 
MVC AUC ↔; 
No data for TPV

Dose: MVC 300 mg BID
Key to Acronyms: ARV = antiretroviral; ATV = atazanavir; ATV/r = ritonavir-boosted atazanavir; AUC = area under the curve; BID = twice daily; cobi = cobicistat; CYP = cytochrome P; DRV/r = ritonavir-boosted darunavir; EFV = efavirenz; ETR = etravirine; EVG = elvitegravir; FPV = fosamprenavir; FTC = emtricitabine; INSTI = integrase strand transfer inhibitor; LPV/r = ritonavir-boosted lopinavir; MVC = maraviroc; NVP = nevirapine; PI = protease inhibitor; PK = pharmacokinetic; RAL = raltegravir; RTV = ritonavir; SQV/r= ritonavir-boosted saquinavir; TDF = tenofovir disoproxil fumarate


Note: FPV is a pro-drug of APV

 

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