MARAVIROC

Maraviroc, a synthetic HIV-1 entry inhibitor, selectively and reversibly antagonises CC chemokine receptor-5 (CCR5) coreceptors found on human CD4+ cells. This prevents interaction of HIV-1 glycoprotein 120 (gp120) and CCR5 necessary for CCR5-tropic HIV-1 to enter cells.

Uses

Maraviroc is used in the treatment of HIV-1 infection.

Warnings

Avoid Maraviroc use in patients with the following conditions:

Hypersensitivity
Lactation
Concomitant use with potent CYP3A enzyme inhibitors and inducers in patients with severe (CrCl <30 mL/min) kidney impairment

Side Effects

Maraviroc may bring about the following side effects:

Significant: Postural hypotension, immune reconstitution syndrome, increased risk of infection and malignancy, osteonecrosis, MI, myocardial ischaemia.
Nervous: Asthenia, dizziness, headache, somnolence, insomnia, depression, malaise, paraesthesia, dysaesthesia, seizures.
GI: Abdominal pain and distention, constipation, diarrhoea, dyspepsia, nausea, vomiting, anorexia, flatulence.
Resp: Cough, upper resp tract infection.
Hepatic: Cirrhosis.
Genitourinary: Renal failure, proteinuria, bladder problems.
Haematologic: Neutropenia, bone marrow depression.
Musculoskeletal: Muscle spasm, back pain, myositis, rhabdomyolysis, increased creatine kinase.
Dermatologic: Pruritus.
Potentially Fatal: Hepatotoxicity and hepatic failure with hypersensitivity reactions [e.g. severe rash, fever, increased IgE, eosinophilia, Stevens-Johnson syndrome, toxic epidermal necrolysis, drug rash with eosinophilia and systemic symptoms (DRESS)].

Precautions

Precautions

Take precautions in people with the following conditions:

Patient with severe heart disease
History of postural hypotension
Liver (e.g. chronic active hepatitis B or C) and kidney impairment
Pregnancy
Patients taking potent CYP3A enzyme inhibitors (with or without potent inducers) or potent CYP3A enzyme inducers (without potent inhibitors)

This drug is not indicated for use in patients with CXCR4- or dual/mixed tropic HIV-1 infection

Interactions

Maraviroc may interact with the following medicines:

CYP3A enzyme inhibitors (e.g. protease inhibitors except ritonavir-boosted tipranavir, delavirdine, ketoconazole, itraconazole, voriconazole, clarithromycin, telithromycin, nefazodone, boceprevir)
CYP3A enzyme inducers (e.g. efavirenz, etravirine, rifampicin, carbamazepine, phenobarbital, phenytoin)
Medications that lower blood pressure

Overdose & Brands

Overdose may lead to postural hypotension. In this case, supportive treatment should be done including keeping the patient in supine position. Assess vital signs, BP, and ECG. Employ gastric lavage/activated charcoal, or induce emesis to remove unabsorbed drug.

Available Brand:

Selzentry