• HIV-1 infection (in combination with other antiretrovirals).

Contraindicated in:

• Lactation: Breastfeeding not recommended in women with HIV.

Use Cautiously in:

• Phenylketonuria (chewable tablets contain phenylalanine)
• OB: Considered a preferred integrase strand transfer inhibitor for pregnant patients living with HIV who are antiretroviral-naive, who have had antiretroviral therapy in the past but are restarting, or who require a new antiretroviral therapy regimen
• Pedi: Preterm neonates (safety and effectiveness not established)
• Geri: Choose dose carefully in older adults, considering concurrent disease states, drug therapy, and age-related ↓ in hepatic and renal function.

CV: MI.

Derm: rash, STEVENS-JOHNSON SYNDROME (SJS), TOXIC EPIDERMAL NECROLYSIS.

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

GU: renal failure/impairment.

Hemat: anemia, neutropenia.

Metab: lipodystrophy.

MS: ↑creatine kinase, myopathy, RHABDOMYOLYSIS.

Neuro: headache, depression, dizziness, fatigue, insomnia, SUICIDAL THOUGHTS, weakness.
Misc: fever, immune reconstitution syndrome.

Drug-Drug:

• Concurrent use with strong inducers of the UGT A1A enzyme system, including rifampin, may ↓ levels and effectiveness.
• Concurrent use with strong inhibitors of the UGT A1A enzyme system, including atazanavir, may ↑ levels and the risk of toxicity.
• ↑risk of rhabomyolysis/myopathy with HMG-CoA reductase inhibitors.
• Proton pump inhibitors may ↑ levels and the risk of toxicity.
• Efavirenz, etravirine, and tipranavir/ritonavir may ↓ levels and effectiveness.
• Administration with antacids, containing magnesium or aluminum↓ absorption of raltegravir; separate administration of raltegravir and magnesium- or aluminum-containing antacids by 6 hr.

• Tablets: 400 mg; 600 mg;
• Chewable tablets (orange-banana): 25 mg; 100 mg;
• Packet for oral suspension (banana flavor): 100 mg/pkt;

Do not substitute the chewable tablets or oral suspension for the film-coated tablets.

• PO (Adults): Treatment-naive patients or patients who are virologically suppressed on an initial regimen of raltegravir 400 mg twice daily: Two 600-mg tablets (1200 mg) once daily or 400 mg twice daily; Treatment-experienced patients: 400 mg twice daily; Concurrent use of rifampin (either treatment-naive or treatment-experienced patients): 800 mg twice daily.
• PO (Children 40 kg and either treatment-naive or virologically suppressed on an initial regimen of raltegravir 400 mg twice daily): Tablet: Two 600-mg tablets (1200 mg) once daily or 400 mg twice daily; Chewable tablets: 300 mg twice daily.
• PO (Children 28–39 kg): Tablet: 400 mg twice daily; Chewable tablets (if unable to swallow tablet): 200 mg twice daily.
• PO (Children 25–27 kg): Tablet: 400 mg twice daily; Chewable tablets (if unable to swallow tablet): 150 mg twice daily.
• PO (Children 4 wk and 20–<25 kg): Chewable tablets: 150 mg twice daily.
• PO (Children 4 wk and 14–19 kg): Oral suspension: 100 mg twice daily; Chewable tablets: 100 mg twice daily.
• PO (Children 4 wk and 10–13 kg): Oral suspension: 80 mg twice daily; Chewable tablets: 75 mg twice daily.
• PO (Children 4 wk and 8–9 kg): Oral suspension: 60 mg twice daily; Chewable tablets: 50 mg twice daily.
• PO (Children 4 wk and 6–7 kg): Oral suspension: 40 mg twice daily; Chewable tablets: 50 mg twice daily.
• PO (Children 4 wk and 4–5 kg): Oral suspension: 30 mg twice daily; Chewable tablets: 25 mg twice daily.
• PO (Children 4 wk and 3–<4 kg): Oral suspension: 25 mg twice daily; Chewable tablets: 25 mg twice daily.
• PO (Neonates 1–4 wk and 4–<5 kg): Oral suspension: 15 mg twice daily.
• PO (Neonates 1–4 wk and 3–<4 kg): Oral suspension: 10 mg twice daily.
• PO (Neonates 1–4 wk and 2–<3 kg): Oral suspension: 8 mg twice daily.
• PO (Neonates 0–1 wk and 4–<5 kg): Oral suspension: 7 mg once daily.
• PO (Neonates 0–1 wk and 3–<4 kg): Oral suspension: 5 mg once daily.
• PO (Neonates 0–1 wk and 2–<3 kg): Oral suspension: 4 mg once daily.

Isentress, Isentress HD

• Inhibits HIV-1 integrase, which is required for viral replication.

• Evidence of decreased viral replication and reduced viral load with slowed progression of HIV and its sequelae.

Therapeutic Classification: antiretrovirals

Pharmacologic Classification:

Absorption: Well absorbed following oral administration.

Distribution: Unknown.

Metabolism/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.

(plasma concentrations)

• 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. Take missed doses 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 Rx renewal in case of changes.
• Instruct patient that raltegravir should not be shared with others.
• Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications.
• 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, if any known symptom persists or worsen, or if signs and symptoms of rhabdomyolysis (unexplained muscle pain, tenderness, weakness), rash, or depression or suicidal thoughts occur.
• Immune reconstitution syndrome may trigger opportunistic infections or autoimmune disorders. Notify health care professional if symptoms occur.
• Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected. Inform pregnant women about the pregnancy exposure registry to monitor pregnancy outcomes. Enroll patient in the Antiretroviral Pregnancy Registry by calling 1-800-258-4263. Advise female patient to avoid breastfeeding during therapy.
• Emphasize the importance of regular follow-up exams and blood counts to determine progress and monitor for side effects.

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