Names and pronunciation
(mah-rav′er-rock) Celsentri , Selzentry
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Drug reference
(mah-rav′er-rock) Celsentri , Selzentry
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Func. class.: Antiretroviral
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Chem. class.: Fusion inhibitor, CCR5-receptor antagonist
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ACTION: Interferes with entry into HIV-1 by inhibiting the fusion of the virus and the cell membrane
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USES: CCR5-tropic HIV in combina- tion with other antiretroviral agents for treating experienced patients
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CONTRAINDICATIONS: Hyper- sensitivity, dialysis, renal impairment Precautions: Pregnancy, Asian patients, breastfeeding, renal/hepatic/car- diac disease, electrolyte imbalance, dehy- dration, immune reconstitution syndrome, infection, MI, orthostatic hypotension, chil- dren, geriatric patients, Graves’ disease, Guillain-Barré syndrome, polymyositis, fever, serious rash
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Black Box Warning: Hepatotoxicity Black Box Warning: Hepatotoxicity: dark urine, vomiting, abdominal pain; yellowing of skin, eyes; hepatomegaly; discontinue product, monitor LFTs • Serious skin rash (Stevens- Johnson syndrome, toxic epidermal necrolysis, DRESS): assess for serious rash; if symptoms develop, discontinue product immediately, provide supportive treatment • Pregnancy/breastfeeding: provide during pregnancy in those who are HIV positive; avoid breastfeeding to reduce risk of HIV transmission; register preg- nant patient with Antiretroviral Pregnancy Registry, 1-800-258-4263
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SIDE EFFECTS CV: MI, cardiac ischemia, orthostatic hypotension CNS: Dizziness, depression, viral menin- gitis, disturbances in consciousness, peripheral neuropathy, paresthesia, dys- esthesia, fever EENT: Gingival hyperplasia, visual changes GI: Diarrhea, constipation, dyspepsia, M CDAD, hepatotoxicity INTEG: Rash, urticaria, pruritus, folliculitis MS: Joint pain, leg pain, muscle cramps RESP: Cough, upper respiratory tract infection, sinusitis, bronchitis, pneu monia, obstruction, bronchospasm, dyspnea SYST: Herpes virus, lipodystrophy, malignancy
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INTERACTIONS Increase: maraviroc levels—CYP3A inhibitors (amiodarone, aprepitant, chlor- amphenicol, clarithromycin, conivaptan, cycloSPORINE, dalfopristin, danazol, dilti- aZEM, erythromycin, estradiol, flucon- azole, fluvoxaMINE, imatinib, isoniazid, itraconazole, ketoconazole, miconazole, nefazodone, niCARdipine, propoxyphene, RU-486, tamoxifen, telithromycin, trolean- domycin, verapamil, voriconazole, zafirlu- kast); reduce dose Decrease: maraviroc levels—CYP3A4 inducers (efavirenz, aminoglutethi- mide, barbiturates, bexarotene, bosen- tan, carBAMazepine, dexamethasone, griseofulvin, modafinil, nafcillin, OX- carbazepine, phenytoin, fosphenytoin, rifabutin, rifAMPin, rifapentine, topira- mate, tipranavir); increase dose Drug/Herb • Decreased maraviroc effect: St. John’s wort Drug/Food • High-fat meal decreases absorption 33% Drug/Lab Test Increase: AST, ALT, bilirubin, amylase, lipase, CK Decrease: ANC
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DOSAGE AND ROUTES Those not taking CYP3A inhibitors/ inducers: Adult/adolescent: PO 300 mg bid Those taking CYP3A4 inhibitors with/without a CYP3A inducer • Adult/adolescent ≥16 yr: PO 150 mg bid Those taking CYP3A4 inducers without a strong CYP3A inhibitor • Adult/adolescent ≥16 yr: PO 600 mg bid
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Available forms: Tabs 25, 75, 150, 300 mg; oral solution 20 mg/mL
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Administer: • May give without regard to meals, with 8 oz water; swallow whole; do not crush, chew, break • Do not double missed dose, take next dose as soon as remembered • Store at room temperature
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Assess: • HIV: CD4, T-cell count, plasma HIV RNA, CCR5-tropic HIV-1; assess for changes in symptoms, other infections during treatment • Severe renal disease (ESRD CCr <30 mL/min): for those taking CYP3A inhibi- tors/inducers and with severe renal dis- ease, drug is contraindicated • Bowel pattern before, during treatment • Allergies: skin eruptions, rash, urti- caria, itching; discontinue product
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Evaluate: • Therapeutic response: improvement in CD4, viral load, T-cell count
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • To take as prescribed; if dose is missed, to take as soon as remembered up to 1 hr before next dose; not to double dose; that product does not cure condition, should not be shared with others • Not to stop product without approval of prescriber • That product does not cure infection, just controls symptoms and does not prevent infecting others • To report sore throat, fever, fatigue (may indicate superinfection); yellow skin/eyes, abdominal pain, vomiting, dark urine, nausea (hepatitis); itching, SOB (allergic reaction) • That product must be taken in equal intervals around the clock to maintain blood levels for duration of therapy • To avoid all OTC products unless ap- proved by prescriber • To avoid driving, other hazardous ac- tivities until reaction is known; that dizzi- ness may occur • To make position changes slowly to prevent postural hypotension • To notify prescriber if pregnancy is planned or suspected; not to breastfeed
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PHARMACOKINETICS Metabolized by P450 system; CYP3A metabolism; excreted 20% urine, 76% feces; protein binding 76%; terminal half-life 14-18 hr
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• Adult/adolescent ≥16 yr: PO 150 mg bid Those taking CYP3A4 inducers without a strong CYP3A inhibitor
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• Adult/adolescent ≥16 yr: PO 600 mg bid
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