maraviroc
(ma-ra-vi-rok)
Selzentry

Classification
Therapeutic: antiretrovirals
Pharmacologic: CCR5 co-receptor antagonists

Pregnancy Category B


Copyright © 2007 by F.A. Davis Company

Indications
HIV infection (with other antiretrovirals), specifically in patients with only CCR5–tropic HIV-1 detectable, with evidence of viral replication and HIV-1 strains displaying multiple resistance to other antiretrovirals. Use should be determined by treatment history and tropism testing.

Action
Blocks a specific receptor on CD-4 and T-cell surfaces which prevents CCR5–tropic HIV-1 from entering. Therapeutic Effects: Decreased invasion of CD-4 and T-cells by CCR5–tropic HIV-1 virus resulting in viral replication.

Pharmacokinetics
Absorption: 2–33% absorbed following oral administration.
Distribution: Unknown.
Metabolism and Excretion: Mostly metabolized by the liver (CYP3A enzyme system); 8% renal excretion as unchanged drug.
Half-life: 14–18 hr.

TIME/ACTION PROFILE (blood levels)

ROUTEONSETPEAKDURATION
POunknown0.5–4 hr1–2 hr


Contraindications/Precautions
Contraindicated in: Dual/mixed or CXCR4–tropic HIV-1; OB: Lactation (breast-feeding not recommended for HIV-infected patients).
Use Cautiously in: Pre-existing liver disease including Hepatitis B or C (may ↑ risk of hepatotoxicity; Cardiovascular disease or risk factors (increased risk of cardiovascular events; Hepatic impairment; Renal impairment (if CCr <50 ml/min and using a CYP3A inhibitor use only if necessary); Treatment-naive adults (safety/efficacy not established); Geri: Consider age-related decrease in renal/hepatic function, concurrent drug therapy and concomittant disease; OB: Use only if clearly needed; Pedi: Safe use in children <16 yr not established.

Adverse Reactions/Side Effects*
*CAPITALS indicate life threatening; underlines indicate most frequent.

CNS: dizziness. Resp: cough, upper respiratory tract infection. GI: abdominal pain, appetite disorder, HEPATOTOXICITY. Derm: RASH. MS: musculoskeletal pain. Misc: ALLERGIC REACTIONS, fever, immune reconstitution syndrome, ↑ risk of infection.

Interactions
Drug–Drug: Levels are ↑ by CYP3A inhibitors including protease inhibitors (excluding tipranavir/ritonavir), delavirdine, ketoconazole, lopinavir/ritonavir, saquinavir, and atazanavir. Levels are ↓ by CYP3A inducers including efavirenz and rifampin.

Route/Dosage
PO (Adults): Concurrent CYP3A inhibitors (except tipranavir/ritonavir) or delavirdine— 150 mg twice daily; Concurrent NRTIs , tipranavir/ritonavir, nevirapine and other drugs that are not strong inhibitors/inducers of CYP3A— 300 mg twice daily; Concurrent CYP3A inducers including efavirenz— 600 mg twice daily.

Availability
Tablets: 150mg, 300 mg.

NURSING IMPLICATIONS

Assessment Potential Nursing Diagnoses
Risk for infection (Indications).
Deficient knowledge, related to medication regimen (Patient/Family Teaching).

Implementation Patient/Family Teaching Evaluation/Desired Outcomes


Copyright © 2007 by F.A. Davis Company