ma-ra-VI-rok

• HIV infection (with other antiretrovirals), specifically in treatment-experienced or treatment-naive patients with CCR5–tropic HIV-1 infection.

• 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.

Absorption: 2–33% absorbed following oral administration.

Distribution: Unknown.

Metabolism/Excretion: Mostly metabolized by the liver (CYP3A enzyme system); 8% renal excretion as unchanged drug.

Half-life: 14–18 hr.

Contraindicated in:

• Dual/mixed or CXCR4–tropic HIV-1
• Patients with severe renal impairment or end-stage renal disease who are taking potent CYP3A inhibitors or inducers
• Pedi: Children with severe renal impairment or end-stage renal disease who are taking potent CYP3A inhibitors
• 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
• Hepatic impairment
• 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 <2 yr (safety and effectiveness not established)
• Geri: Consider age-related ↓ in renal/hepatic function, concurrent drug therapy and concomitant disease.

CNS: dizziness.

CV: myocardial ischemia/infarction, orthostatic hypotension.

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

GI: HEPATOTOXICITY, abdominal pain, appetite disorder.

MS: musculoskeletal pain.

Resp: cough, upper respiratory tract infection.

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

Drug-Drug:

• Levels are ↑ by CYP3A inhibitors including protease inhibitors (excluding tipranavir/ritonavir), elvitegravir/ritonavir ketoconazole, itraconazole, clarithromycin, nefazodone, lopinavir/ritonavir, saquinavir, and atazanavir ; need to ↓ dosage of maraviroc.
• Levels are ↓ by CYP3A inducers including efavirenz, rifampin, etravirine, carbamazepine, phenytoin, and phenobarbital; need to ↑ dose of maraviroc.
• Antihypertensives may ↑ risk of orthostatic hypotension.

Drug-Natural Products:

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

• PO (Adults): Concurrent potent CYP3A inhibitors (with or without potent CYP3A inducers) including protease inhibitors (except tipranavir/ritonavir), delavirdine, 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 2 yr and 40 kg): Concurrent potent CYP3A inhibitors (with or without potent CYP3A inducers) including protease inhibitors (except tipranavir/ritonavir), delavirdine, 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 — Not recommended; 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 2 yr and 30–39 kg): Concurrent potent CYP3A inhibitors (with or without potent CYP3A inducers) including protease inhibitors (except tipranavir/ritonavir), delavirdine, elvitegravir/ritonavir, ketoconazole, itraconazole, clarithromycin, and other potent CYP3A inhibitors — 100 mg twice daily; Concurrent potent CYP3A inducers (without a potent CYP3A inhibitor) including efavirenz, rifampin, etravirine, carbamazepine, phenytoin, and phenobarbital — Not recommended; 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 2 yr and 20–29 kg): Concurrent potent CYP3A inhibitors (with or without potent CYP3A inducers) including protease inhibitors (except tipranavir/ritonavir), delavirdine, elvitegravir/ritonavir, ketoconazole, itraconazole, clarithromycin, and other potent CYP3A inhibitors — 75 mg twice daily; Concurrent potent CYP3A inducers (without a potent CYP3A inhibitor) including efavirenz, rifampin, etravirine, carbamazepine, phenytoin, and phenobarbital — Not recommended; Noninteracting concomitant medications including NRTIs, tipranavir/ritonavir, nevirapine, raltegravir, enfuvirtide, and other medications that not potent CYP3A inhibitors/inducers — Not recommended.
• PO (Children 2 yr and 10–19 kg): Concurrent potent CYP3A inhibitors (with or without potent CYP3A inducers) including protease inhibitors (except tipranavir/ritonavir), delavirdine, elvitegravir/ritonavir, ketoconazole, itraconazole, clarithromycin, and other potent CYP3A inhibitors — 50 mg twice daily; Concurrent potent CYP3A inducers (without a potent CYP3A inhibitor) including efavirenz, rifampin, etravirine, carbamazepine, phenytoin, and phenobarbital — Not recommended; Noninteracting concomitant medications including NRTIs, tipranavir/ritonavir, nevirapine, raltegravir, enfuvirtide, and other medications that not potent CYP3A inhibitors/inducers — Not recommended.

• PO: May be administered without regard to food. Tablets should be swallowed whole; do not break, crush, or chew.
  • Solution is clear and colorless. Store at room temperature. Discard unused solution 60 days after first opening bottle.

Selzentry

Celsentri

Therapeutic Classification: antiretrovirals

Pharmacologic Classification: ccr5 co.receptor antagonists

• Oral solution (strawberry-flavor): 20 mg/mL;
• Tablets: 25 mg; 75 mg; 150 mg; 300 mg;

(blood levels)

• Assess patient for change in severity of HIV symptoms and for symptoms of opportunistic infections throughout therapy.
• Assess for signs or symptoms of hepatitis or allergic reaction (pruritic rash, jaundice, dark urine, vomiting, abdominal pain, fever, eosinophilia, elevated IgE). If symptoms occur, discontinue maraviroc immediately.
• Assess for rash periodically during therapy. May cause Stevens-Johnson syndrome. Discontinue therapy if severe or if accompanied with fever, general malaise, fatigue, muscle or joint aches, blisters, oral lesions, conjunctivitis, hepatitis, and/or eosinophilia.
• Monitor for signs and symptoms of DRESS (fever, rash, lymphadenopathy, and/or facial swelling, associated with involvement of other organ systems (hepatitis, nephritis, hematologic abnormalities, myocarditis, myositis) during therapy. May resemble an acute viral infection. Eosinophilia is often present. Discontinue therapy if signs occur.

• Testing for CCR5–tropic HIV-1 should be obtained prior to initiating therapy.
  • Monitor viral load and CD4 cell count regularly during therapy.
  • Monitor AST, ALT, and serum bilirubin prior to and periodically during therapy. May cause ↑ AST, ALT, total bilirubin, amylase, and lipase.
  • May cause ↓ absolute neutrophil count.

• Risk for infection (Indications).
• Deficient knowledge, Relate med (Patient/Family Teaching).

• Emphasize the importance of taking maraviroc as directed, at the same time each day. Advise patient to read the Patient Information that comes with the medication with each Rx refill. 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.
• Rep: Advise patients 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. Encourage pregnant women exposed to maraviroc to enroll in the Antiviral Pregnancy Registry by calling 1-800-258-4263 to monitor maternal/fetal outcomes.
• Emphasize the importance of regular follow-up exams and blood counts to determine progress and monitor for side effects.

• Delayed progression of AIDS and decreased opportunistic infections in patients with HIV.
• Decrease in viral load and increase in CD4 cell counts.

NDC Code^*

• 49702- ViiV Healthcare Company
  • 49702-223- SELZENTRY
    • 49702-223-18- 60 TABLET, FILM COATED in 1 BOTTLE (49702-223-18)

• 49702- ViiV Healthcare Company
  • 49702-224- SELZENTRY
    • 49702-224-18- 60 TABLET, FILM COATED in 1 BOTTLE (49702-224-18)

• 49702- ViiV Healthcare Company
  • 49702-233- SELZENTRY
    • 49702-233-08- 120 TABLET, FILM COATED in 1 BOTTLE (49702-233-08)

• 49702- ViiV Healthcare Company
  • 49702-235- SELZENTRY
    • 49702-235-08- 120 TABLET, FILM COATED in 1 BOTTLE (49702-235-08)

• 49702- ViiV Healthcare Company
  • 49702-237- SELZENTRY
    • 49702-237-55- 1 BOTTLE in 1 CARTON (49702-237-55) > 230 mL in 1 BOTTLE

• 50090- A-S Medication Solutions
  • 50090-1486- SELZENTRY
    • 50090-1486-0- 60 TABLET, FILM COATED in 1 BOTTLE (50090-1486-0)