.

RALTEGRAVIR

Medical Diagnosis and Drugs, Medications
RALTEGRAVIR
(ral-te-gra'vir)
Isentress
Classifications: antiviral; antiretroviral agent; integrase inhibitor;
Therapeutic: antiviral; antiretroviral agent
Pregnancy Category: C

Availability

400 mg tablets

Action

Inhibits HIV-1 integrase, an enzyme required for integration of proviral DNA into the helper T-cell genome, thus preventing formation of the HIV-1 provirus.

Therapeutic Effect

Inhibiting integration inhibits replication and proliferation of the HIV-1 virus.

Uses

In combination with other antiretroviral agents for the treatment of HIV-1 infection in treatment-experienced adult patients who have evidence of viral replication and HIV-1 strains resistant to multiple antiretroviral agents.

Contraindications

Treatment of na?ve HIV-1 patients; pregnancy (category C); lactation; children <16 y. Safety and efficacy in patients with severe hepatic impairment are unknown.

Cautious Use

Mild to moderate hepatic impairment.

Route & Dosage

HIV-1 Infection
Adult: PO 400 mg b.i.d.

Administration

  • May be given without regard to food.
  • Give before dialysis.
  • Store at 15–30° C (59–86° F).

Adverse Effects (≥1%)

Body as a Whole: Asthenia, fatigue, pyrexia. CNS: Dizziness, headache. GI: Abdominal pain, diarrhea, nausea, vomiting. Skin: Lipodystrophy.

Interactions

Drug: Atazanavir may increase plasma levels of raltegravir; rifampin and tipranavir/ritonavir may decrease plasma levels of raltegravir.

Pharmacokinetics

Peak: 3 h. Distribution: 83% protein bound. Metabolism: In the liver. Elimination: Stool and urine. Half-Life: 9 h.

Nursing Implications

Assessment & Drug Effects

  • Monitor for and report S&S of immune reconstitution syndrome (inflammatory response to residual opportunistic infections such as MAC, CMV, PCP, or reactivation of varicella zoster).
  • Lab tests: Baseline and periodic CD4+ cell count and HIV RNA viral load; periodic CBC with differential, LFTs.
  • Monitor diabetics for loss of glycemic control.

Patient & Family Education

  • Inform physician immediately if you plan to become or become pregnant during therapy.
  • Report promptly unexplained leg pain or muscle cramping.

Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug

(22)