General

Pronunciation
ral-TEG-ra-veer

Trade Name(s)

• Isentress

Pregnancy Category
Category C

Ther. class.
antiretrovirals

Pharm. class.
integrase strand transfer inhibitor (INSTI)

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 Effect(s):
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)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	3 hr	12 hr

Contraindication/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

CNS: headache, dizziness, fatigue, weakness.

CV: myocardial infarction.

GI: diarrhea, abdominal pain, gastritis, hepatitis, vomiting.

GU: renal failure/impairment.

Hemat: anemia, neutropenia.

Metabolic: lipodystrophy.

Misc: hypersensitivity reactions, immune reconstitution syndrome, fever.

*CAPITALS indicates life-threatening.
*italic indicates most frequent.

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

Assessment

• Assess patient for change in severity of HIV symptoms and for symptoms of opportunistic infections during therapy

Lab Test Considerations

• Monitor viral load and CD4 counts regularly during therapy

» May casue ANC, hemoglobin, and platelet counts

» May cause serum glucose, AST, ALT, GGT, total bilirubin, alkaline phosphatase, pancreatic amylase, serum lipase, and creatinine kinase concentrations

Potential Nursing Diagnoses

• Risk for infection (Indications)

• Noncompliance (Patient/Family Teaching)

Implementation

PO: Must be administered without regard to meals

Patient/Family Teaching

• Emphasize the importance of taking raltegravir as directed, at evenly spaced times throughout day. Do not take more than prescribed amount and do not stop taking without consulting health care professional. If a dose is missed, take as soon as remembered unless almost time for next dose. Do not double doses. Advise patient to read Patient Information sheet before starting therapy and with each prescription renewal in chase changes have been made

• Instruct patient that raltegravir should not be shared with others

• Advise patient to avoid taking other Rx, OTC, or herbal products without consulting health care professional

• Inform patient that raltegravir does not cure AIDS or prevent associated or opportunistic infections. Raltegravir does not reduce the risk of transmission of HIV to others through sexual contact or blood contamination. Caution patient to use a condom during sexual contact and to avoid sharing needles or donating blood to prevent spreading the AIDS virus to others. Advise patient that the long-term effects of raltegravir are unknown at this time

• Advise patient to notify health care professional if they develop any unusual symptoms or if any known symptom persists or worsens

• Advise patients to notify health care professional if pregnancy is planned or suspected. Breastfeeding should be avoided during therapy

• Emphasize the importance of regular follow-up exams and blood counts to determine progress and monitor for side effects

Evaluation/Desired Outcomes

• Delayed progression of AIDS and decreased opportunistic infections in patients with HIV

• Decrease in viral load and improvement in CD4 cell counts

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