• CCR5–tropic HIV-1 infection (in combination with other antiretrovirals).

Contraindicated in:

• Dual/mixed or CXCR4–tropic HIV-1
• Severe renal impairment or end-stage renal disease in patients who are taking potent CYP3A inhibitors or inducers
• Lactation: Breastfeeding not recommended for mothers infected with HIV.

Use Cautiously in:

• Pre-existing liver disease including hepatitis B or C (may ↑ risk of hepatotoxicity)
• Cardiovascular disease or risk factors (↑ risk of cardiovascular events)
• Orthostatic hypotension
• Patients with severe renal impairment or end-stage renal disease who are not taking potent CYP3A inhibitors or inducers (↓ dose if symptoms of orthostatic hypotension occur)
• OB: Use during pregnancy only if potential maternal benefit justifies potential fetal risk; not recommended for pregnant females with HIV who are antiretroviral nave
• Pedi: Children weighing <2 kg (safety and effectiveness not established)
• Geri: Consider age-related ↓ in renal/hepatic function, concurrent drug therapy and concomitant disease in older adults.

CV: myocardial ischemia/infarction, orthostatic hypotension.

Derm: DRUG RASH WITH EOSINOPHILIA AND SYSTEMIC SYMPTOMS (DRESS), STEVENS-JOHNSON SYNDROME (SJS), TOXIC EPIDERMAL NECROLYSIS.

GI: abdominal pain, appetite disorder, HEPATOTOXICITY.

MS: musculoskeletal pain.

Neuro: dizziness.

Resp: cough, upper respiratory tract infection.
Misc: fever, hypersensitivity reactions (including lip swelling and facial edema), immune reconstitution syndrome, ↑ risk of infection.

Drug-Drug:

• CYP3A inhibitors including protease inhibitors (excluding tipranavir/ritonavir), elvitegravir/ritonavir ketoconazole, itraconazole, clarithromycin, nefazodone, lopinavir/ritonavir, and atazanavir may ↑ levels and the risk of toxicity; ↓ maraviroc dose.
• CYP3A inducers including efavirenz, rifampin, etravirine, carbamazepine, phenytoin, and phenobarbital may ↓ levels and effectiveness; ↑ maraviroc dose.
• Antihypertensives may ↑ risk of orthostatic hypotension.

Drug-Natural Products:

• St. John's wort may ↓ levels; concurrent use not recommended.

(Generic available)

• Tablets: 150 mg; 300 mg;
• Oral solution (strawberry-flavor): 20 mg/mL;

• PO (Adults): Concurrent potent CYP3A inhibitors (with or without potent CYP3A inducers) including protease inhibitors (except tipranavir/ritonavir), elvitegravir/ritonavir, ketoconazole, itraconazole, clarithromycin, and other potent CYP3A inhibitors — 150 mg twice daily; Concurrent potent CYP3A inducers (without a potent CYP3A inhibitor) including efavirenz, rifampin, etravirine, carbamazepine, phenytoin, and phenobarbital — 600 mg twice daily; Noninteracting concomitant medications including NRTIs, tipranavir/ritonavir, nevirapine, raltegravir, enfuvirtide, and other medications that not potent CYP3A inhibitors/inducers — 300 mg twice daily.
• PO (Children 40 kg): Concurrent potent CYP3A inhibitors (with or without a CYP3A inducer), including clarithromycin, cobicistat, elvitegravir/ritonavir, itraconazole, ketoconazole, nefazodone, and protease inhibitors (except tipranavir/ritonavir), — 150 mg twice daily (as tablets [if 2 yr] or oral solution); Concurrent potent and moderate CYP3A inducers (without a potent CYP3A inhibitor), including carbamazepine, efavirenz, etravirine, phenobarbital, phenytoin, and rifampin — Not recommended; Noninteracting concomitant medications that are not potent CYP3A inhibitors/inducers, including dolutegravir, enfuvirtide, nevirapine, all NRTIs, raltegravir, and tipranavir/ritonavir — 300 mg twice daily (as tablets [if 2 yr] or oral solution).
• PO (Children 30–<40 kg): Concurrent potent CYP3A inhibitors (with or without a CYP3A inducer), including clarithromycin, cobicistat, elvitegravir/ritonavir, itraconazole, ketoconazole, nefazodone, and protease inhibitors (except tipranavir/ritonavir) — 100 mg twice daily (as tablets [if 2 yr] or oral solution); Concurrent potent and moderate CYP3A inducers (without a potent CYP3A inhibitor), including carbamazepine, efavirenz, etravirine, phenobarbital, phenytoin, and rifampin — Not recommended; Noninteracting concomitant medications that are not potent CYP3A inhibitors/inducers, including dolutegravir, enfuvirtide, nevirapine, all NRTIs, raltegravir, and tipranavir/ritonavir — 300 mg twice daily (as tablets [if 2 yr] or oral solution).
• PO (Children 20–<30 kg): Concurrent potent CYP3A inhibitors (with or without a CYP3A inducer), including clarithromycin, cobicistat, elvitegravir/ritonavir, itraconazole, ketoconazole, nefazodone, and protease inhibitors (except tipranavir/ritonavir) — 75 mg twice daily (as tablets [if 2 yr] or oral solution); Concurrent potent and moderate CYP3A inducers (without a potent CYP3A inhibitor), including carbamazepine, efavirenz, etravirine, phenobarbital, phenytoin, and rifampin — Not recommended; Noninteracting concomitant medications that are not potent CYP3A inhibitors/inducers, including dolutegravir, enfuvirtide, nevirapine, all NRTIs, raltegravir, and tipranavir/ritonavir — 200 mg twice daily (as tablets [if 2 yr] or oral solution).
• PO (Children 14–<20 kg): Concurrent potent CYP3A inhibitors (with or without a CYP3A inducer), including clarithromycin, cobicistat, elvitegravir/ritonavir, itraconazole, ketoconazole, nefazodone, and protease inhibitors (except tipranavir/ritonavir) — 50 mg twice daily (as tablets [if 2 yr] or oral solution); Concurrent potent and moderate CYP3A inducers (without a potent CYP3A inhibitor), including carbamazepine, efavirenz, etravirine, phenobarbital, phenytoin, and rifampin — Not recommended; Noninteracting concomitant medications that are not potent CYP3A inhibitors/inducers, including dolutegravir, enfuvirtide, nevirapine, all NRTIs, raltegravir, and tipranavir/ritonavir — 200 mg twice daily (as tablets [if 2 yr] or oral solution).
• PO (Children 10–<14 kg): Concurrent potent CYP3A inhibitors (with or without a CYP3A inducer), including clarithromycin, cobicistat, elvitegravir/ritonavir, itraconazole, ketoconazole, nefazodone, and protease inhibitors (except tipranavir/ritonavir) — 50 mg twice daily (as tablets [if 2 yr] or oral solution); Concurrent potent and moderate CYP3A inducers (without a potent CYP3A inhibitor), including carbamazepine, efavirenz, etravirine, phenobarbital, phenytoin, and rifampin — Not recommended; Noninteracting concomitant medications that are not potent CYP3A inhibitors/inducers, including dolutegravir, enfuvirtide, nevirapine, all NRTIs, raltegravir, and tipranavir/ritonavir — 150 mg twice daily (as tablets [if 2 yr] or oral solution).
• PO (Children 6–<10 kg): Concurrent potent CYP3A inhibitors (with or without a CYP3A inducer), including clarithromycin, cobicistat, elvitegravir/ritonavir, itraconazole, ketoconazole, nefazodone, and protease inhibitors (except tipranavir/ritonavir) — Not recommended; Concurrent potent and moderate CYP3A inducers (without a potent CYP3A inhibitor), including carbamazepine, efavirenz, etravirine, phenobarbital, phenytoin, and rifampin — Not recommended; Noninteracting concomitant medications that are not potent CYP3A inhibitors/inducers, including dolutegravir, enfuvirtide, nevirapine, all NRTIs, raltegravir, and tipranavir/ritonavir — 100 mg twice daily (as oral solution).
• PO (Children 4–<6 kg): Concurrent potent CYP3A inhibitors (with or without a CYP3A inducer), including clarithromycin, cobicistat, elvitegravir/ritonavir, itraconazole, ketoconazole, nefazodone, and protease inhibitors (except tipranavir/ritonavir) — Not recommended; Concurrent potent and moderate CYP3A inducers (without a potent CYP3A inhibitor), including carbamazepine, efavirenz, etravirine, phenobarbital, phenytoin, and rifampin — Not recommended; Noninteracting concomitant medications that are not potent CYP3A inhibitors/inducers, including dolutegravir, enfuvirtide, nevirapine, all NRTIs, raltegravir, and tipranavir/ritonavir — 40 mg twice daily (as oral solution).
• PO (Children 2–<4 kg): Concurrent potent CYP3A inhibitors (with or without a CYP3A inducer), including clarithromycin, cobicistat, elvitegravir/ritonavir, itraconazole, ketoconazole, nefazodone, and protease inhibitors (except tipranavir/ritonavir) — Not recommended; Concurrent potent and moderate CYP3A inducers (without a potent CYP3A inhibitor), including carbamazepine, efavirenz, etravirine, phenobarbital, phenytoin, and rifampin — Not recommended; Noninteracting concomitant medications that are not potent CYP3A inhibitors/inducers, including dolutegravir, enfuvirtide, nevirapine, all NRTIs, raltegravir, and tipranavir/ritonavir — 30 mg twice daily (as oral solution).

Selzentry

• Blocks a specific receptor on CD-4 and T-cell surfaces which prevents CCR5–tropic HIV-1 from entering.

• Decreased invasion of CD-4 and T-cells by CCR5–tropic HIV-1 virus resulting in viral replication.

Therapeutic Classification: antiretrovirals

Pharmacologic Classification: ccr5 co.receptor antagonists

Absorption: 2–33% absorbed following oral administration.

Distribution: Unknown.

Metabolism/Excretion: Mostly metabolized by the liver by the CYP3A isoenzyme; 8% renal excretion as unchanged drug.

Half-life: 14–18 hr.

Celsentri

(plasma concentrations)

• Emphasize the importance of taking maraviroc as directed, at the same time each day. Advise patient to read the Patient Informationbefore starting therapy and with each Rx refill in case of changes. Maraviroc must always be used in combination with other antiretroviral drugs. Do not take more than prescribed amount and do not stop taking without consulting health care professional. Take missed doses as soon as remembered, then return to regular dose schedule. If it is within 6 hr of next dose, omit dose and take next dose at regular time. Do not double doses.
• Instruct patient that maraviroc should not be shared with others.
• Inform patient that maraviroc does not cure AIDS or prevent associated or opportunistic infections. Maraviroc may reduce the risk of transmission of HIV to others through sexual contact or blood contamination. Caution patient to use a condom and to avoid sharing needles or donating blood to prevent spreading the AIDS virus to others. The long-term effects of maraviroc are unknown at this time. If new symptoms of infection develop after starting maraviroc, notify health care professional.
• Advise patient to discontinue maraviroc and notify health care professional if chest pain, signs of hepatotoxicity (itchy rash, yellow-colored skin or eyes, dark urine, vomiting, abdominal pain) or signs of immune reconstitution syndrome (signs and symptoms of an infection — Mycobacterium aviumcomplex infection, cytomegalovirus, Pneumocystis jirovecii pneumonia, tuberculosis, reactivation of herpes simplex and herpes zoster) occur.
• May cause dizziness. Caution patient to avoid driving and other activities requiring alertness until response to medication is known.
• Advise patient to make position changes slowly to minimize postural hypotension.
• Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications, especially St. John's Wort; may decrease effectiveness of maraviroc.
• May cause fetal harm. Advise females of reproductive potential taking oral contraceptives to use a nonhormonal method of birth control during maraviroc therapy. Instruct patient to notify health care professional if pregnancy is planned or suspected and to avoid breastfeeding. Inform pregnant women of the pregnancy exposure registry that monitors pregnancy outcomes in women exposed to maraviroc during pregnancy. To enroll in the Antiviral Pregnancy Registry call 1-800-258-4263.
• Emphasize the importance of regular follow-up exams and blood counts to determine progress and monitor for side effects.

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