Adult: In patients with exclusively CCR5-tropic HIV-1 infection in combination with other antiretrovirals: Patients taking potent CYP3A inhibitors with or without potent CYP3A inducers: 150 mg bid. Patients taking neither potent CYP3A inhibitors nor inducers: 300 mg bid. Patients taking potent CYP3A inducers without a potent CYP3A inhibitor: 600 mg bid. Child: In patients with exclusively CCR5-tropic HIV-1 infection in combination with other antiretrovirals: Patients taking potent CYP3A inhibitors with or without potent CYP3A inducers: ≥2 years weighing 10-<20 kg: 50 mg bid; 20-<30 kg: 75-80 mg bid; 30-<40 kg: 100 mg bid; ≥40 kg: 150 mg bid. Patients taking neither potent CYP3A inhibitors nor inducers: ≥2 years weighing 10-<30 kg: Not recommended; 30-≥40 kg: 300 mg bid. Dosage and treatment recommendations may vary among individual products and between countries (refer to specific product or local guidelines).
Renal Impairment
ESRD on haemodialysis: Patients with symptoms of postural hypotension who are taking neither potent CYP3A inhibitors nor inducers: Reduce dose to 150 mg bid. Patients taking potent CYP3A inhibitors or inducers: Contraindicated.
CrCl (mL/min)
Dosage
<30
Patients with symptoms of postural hypotension who are taking neither potent CYP3A inhibitors nor inducers: Reduce dose to 150 mg bid. Patients taking potent CYP3A inhibitors or inducers: Contraindicated.
Dosage may vary among individual products and between countries (refer to specific product or local guidelines).
Administration
May be taken with or without food.
Contraindications
Hypersensitivity. Severe renal impairment (CrCl <30 mL/min), ESRD on regular haemodialysis who are concurrently taking potent CYP3A inhibitors or inducers. Lactation.
Special Precautions
Patient with CV disease, history or current cardiac predisposition for postural hypotension; pre-existing liver dysfunction (including chronic active hepatitis) or HBV and/or HCV coinfection. Not recommended for use in treatment-naive patients. Not indicated for treatment of patients with dual/mixed or CXCR4-tropic HIV-1. Renal and hepatic impairment. Elderly. Pregnancy.
Adverse Reactions
Significant: CNS effect (e.g. dizziness); symptomatic postural hypotension; immune reconstitution syndrome (e.g. activation of Grave's disease, polymyositis, Guillain-Barre syndrome); infections (e.g. URTI, herpes virus infection), increased risk of malignancy; osteonecrosis. Blood and lymphatic system disorders: Anaemia. Gastrointestinal disorders: Nausea, abdominal pain, flatulence. General disorders and administration site conditions: Asthenia. Investigations: Increased ALT, AST. Metabolism and nutrition disorders: Anorexia. Psychiatric disorders: Insomnia, depression. Respiratory, thoracic and mediastinal disorders: Cough, bronchitis. Potentially Fatal: Hepatotoxicity, severe skin and hypersensitivity reactions including Stevens-Johnson syndrome, toxic epidermal necrolysis, drug rash with eosinophilia with systemic symptoms (DRESS), organ dysfunction.
Patient Counseling Information
This drug may cause dizziness, if affected, do not drive or operate machinery.
Monitoring Parameters
Perform tropism assay with validation and sensitivity, resistance testing prior to initiation of treatment. Monitor viral load, CD4 count, transaminases (ALT, AST) and bilirubin (before initiating therapy and periodically during treatment); signs and symptoms of infection, rash, severe skin reactions, hepatitis and/or allergic reaction; postural hypotension.
Drug Interactions
Reduced serum concentration and therapeutic effect with CYP3A inducers (e.g. efavirenz, etravirine, rifampicin, carbamazepine, phenobarbital, phenytoin). Increased serum concentration with CYP3A inhibitors (e.g. clarithromycin, itraconazole, ketoconazole, nefazodone). Increased risk of postural hypotension when used concomitantly with blood pressure-lowering agents.
Food Interaction
Decreased serum concentration with St. John's wort.
Action
Description: Mechanism of Action: Maraviroc, a synthetic antiretroviral agent, selectively and reversibly binds to CCR5 chemokine receptor, thereby preventing interaction of HIV-1 glycoprotein 120 and CCR5 necessary for CCR5-tropic HIV-1 to enter cells. Pharmacokinetics: Absorption: Absorbed from the gastrointestinal tract. Bioavailability: 23-33%. Time to peak plasma concentration: 0.5-4 hours. Distribution: Crosses the placenta. Volume of distribution: Approx 194 L. Plasma protein binding: Approx 76%. Metabolism: Metabolised in the liver by CYP3A and CYP3A5 to inactive metabolites. Excretion: Via urine (approx 20%, 8% as unchanged drug); faeces (76%, 25% as unchanged drug). Elimination half-life: 14-18 hours.
Chemical Structure
Maraviroc Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 3002977, Maraviroc. https://pubchem.ncbi.nlm.nih.gov/compound/Maraviroc. Accessed Nov. 23, 2023.
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