raltegravir
(ral-teg-ra-veer)
Isentress

Classification
Therapeutic: antiretrovirals
Pharmacologic: integrase strand transfer inhibitor (INSTI)

Pregnancy Category C


Copyright © 2008 by F.A. Davis Company

Indications
HIV infection (with other antiretrovirals) in patients who are failing other treatments as evidenced by continued viral replication and resistance to other agents.

Action
Inhibits HIV-1 integrase, which is required for viral replication. Therapeutic Effects: Evidence of decreased viral replication and reduced viral load with slowed progression of HIV and its sequelae.

Pharmacokinetics
Absorption: Well absorbed following oral administration.
Distribution: Unknown.
Metabolism and Excretion: Mostly metabolized by the uridine diphosphate glucuronosyltransferase (UGT) A1A enzyme system; 23% excreted in urine as parent drug and metabolite.
Half-life: 9 hr.

TIME/ACTION PROFILE (blood levels)

ROUTEONSETPEAKDURATION
POunknown3 hr12 hr


Contraindications/Precautions
Contraindicated in: OB: Lactation (breast feeding not recommended in HIV-infected patients);
Use Cautiously in: Geri: Choose dose carefully, considering concurrent disease states, drug therapy and age-related decrease in hepatic and renal function; Concurrent use of medications associated with rhabomyolysis/myopathy (may increase risk); OB: Use in pregnancy only if maternal benefit outweighs fetal risk; Pedi: Safe use in children <16 yr not established;

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

CNS: headache, dizziness, fatigue, weakness. CV: myocardial infarction. GI: diarrhea, abdominal pain, gastritis, hepatitis, vomiting. GU: renal failure/impairment. Hemat: anemia, neutropenia. Metab: lipodystrophy. Misc: hypersensitivity reactions, immune reconstitution syndrome, fever.

Interactions
Drug–Drug: Concurrent use with strong inducers of the UGT A1A enzyme system including rifampin may ↓ blood levels and effectiveness. Concurrent use with strong inhibitors of the UGT A1A enzyme system may ↑ blood levels. ↑ risk of rhabomyolysis/myopathy HMG-CoA reductase inhibitors .

Route/Dosage
PO (Adults): 400 mg twice daily.

Availability
Tablets: 400 mg.

NURSING IMPLICATIONS

Assessment Potential Nursing Diagnoses
Risk for infection (Indications).
Noncompliance (Patient/Family Teaching).

Implementation Patient/Family Teaching Evaluation/Desired Outcomes


Copyright © 2008 by F.A. Davis Company