Classifications: antiviral; antiretroviral; cellular chemokine co-receptor-5 (ccr-5) antagonist; Therapeutic: antiviral; antiretroviral
Pregnancy Category: B
150 mg and 300 mg tablets
Selectively binds to human chemokine coreceptor-5 (CCR-5) on cell membranes of helper T cell lymphocytes preventing interaction
with the HIV-1 gp120 envelope protein necessary for the HIV virus to enter helper T cells.
Prevents infection of helper T cells by HIV-1 viruses with CCR-5 tropism.
Treatment of human immunodeficiency virus (HIV-1) infection in combination with other antiretroviral agents in treatment-experienced
patients who express CCR-5 and who have evidence of HIV-1 replication and HIV-1 strains resistant to multiple antiretroviral
Patients with dual/mixed, or chemokine-related receptor (CCR-4)-tropic HIV-1 virus; treatment na?ve adults or children with
HIV-1; lactation; children <16 y.
Hepatic impairment, hepatitis B or C; renal impairment, especially with co-administration of CYP3A inhibitors; Clcr <50 mL/min; co-administration of antihypertensive agents; patients with cardiac disease or increased risk for cardiovascular
events; older adults; pregnancy (category B).
Route & Dosage
|Regimen without CYP3A Inducers or Inhibitors
Adult: PO 300 mg b.i.d.
Regimen with CYP3A Inhibitor with/without CYP3A Inducer
Adult: PO 150 mg b.i.d.
Regimen with CYP3A Inducers without a Strong CYP3A Inhibitor
Adult: PO 600 mg b.i.d.
- Must be given in combination with other antiretroviral drugs.
- Store at 15°30 °C (59°86°F).
Adverse Effects (≥1%)Body as a Whole:
Appetite disorders, herpes infection, pain and discomfort, pyrexia. CNS: Depression
, disturbances in consciousness, sleep disorders, dizziness,
paresthesias and dysesthesias, peripheral neuropathies, sensory abnormalities. CV:
Vascular hypertension disorders. GI: Abdominal pain, constipation
, dyspepsia, stomatitis, ulceration. Hematologic:
Elevated AST levels. Musculoskeletal:
Joint-related signs and symptoms, muscle pains, musculoskeletal symptoms. Respiratory:
Breathing abnormalities, bronchitis
, bronchospasm, cough, influenza
, paranasal sinus disorder, pneumonia
, respiratory tract disorders, sinusitis
, upper respiratory tract infection. Skin:
Apocrine and eccrine gland disorders, benign neoplasms, dermatitis, eczema
, folliculitis, lipodystrophies, pruritis, rash. Urogenital:
Bladder and urethral symptoms, condyloma acuminatum, urinary tract signs and symptoms.
InteractionsDrug: strong cyp3a4 inhibitors
(hiv protease inhibitors
with the exception of tipranavir/ritonavir, delavirdine, ketoconazole, itrazonazole, clarithromycin
) increase maraviroc plasma level. cyp3a4 inducers
(efavirenz, rifampin, carbamazepine, phenobarbital, phenytoin
) decrease maraviroc plasma level. Food:
Coadministration with a high-fat meal decreases the plasma levels of maraviroc. Herbal: St. John's wort
may decrease the plasma levels of maraviroc.
Bioavailability is 2333%. Peak:
0.54 h (dose-dependent). Distribution:
75% protein bound. Metabolism:
In liver via CYP3A4. Elimination:
Primarily in stool. Half-Life:
Assessment & Drug Effects
- Monitor for and report promptly S&S of hepatotoxicity, hepatitis or infection.
- Monitor for and report S&S of immune reconstitution syndrome (inflammatory response to residual opportunistic infections
such as MAC, CMV, PCP, or reactivation of varicella zoster).
- Monitor BP especially in those on antihypertensive drugs and with a history of postural hypotension.
- Monitor CV status especially in those with preexisting conditions that cause myocardial ischemia.
- Lab tests: Baseline and periodic CD4+ cell count and HIV RNA viral load; periodic LFTs, WBC with differential.
Patient & Family Education
- Exercise caution when arising from a lying or sitting positing. Dizziness is a common adverse effect.
- Do not engage in dangerous activities until response to drug is known.
- Report promptly any of the following: itchy rash, yellow skin or eyes, nausea or vomiting, upper abdominal pain, flu-like
symptoms, unexplained fatigue.