RALTEGRAVIR
| 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