MARAVIROC
| MARAVIROC (mar-a-vir'ok) Selzentry Classifications: antiviral; antiretroviral; cellular chemokine co-receptor-5 (ccr-5) antagonist; Therapeutic: antiviral; antiretroviral Pregnancy Category: B |
Availability
150 mg and 300 mg tablets
Action
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.
Therapeutic Effect
Prevents infection of helper T cells by HIV-1 viruses with CCR-5 tropism.
Uses
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 agents.
Contraindications
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.
Cautious Use
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. |
Administration
- 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: Neutropenia. Metabolic: 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.Interactions
Drug: 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.Pharmacokinetics
Absorption: Bioavailability is 23–33%. Peak: 0.5–4 h (dose-dependent). Distribution: 75% protein bound. Metabolism: In liver via CYP3A4. Elimination: Primarily in stool. Half-Life: 14–18 h.Nursing Implications
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.
Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; 
Canadian drug name; 
Prototype drug