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Pregnancy Category: C
Pharmacologic: integrase strand transfer inhibitors instis
Pharmacologic: integrase strand transfer inhibitors instis
HIV-1 infection (with other antiretrovirals) in treatment-experienced or treatment-naïve patients.
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.
Absorption: Well absorbed following oral administration.
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)
|PO||unknown||3 hr||12 hr|
Contraindicated in: Lactation: Breast feeding not recommended in HIV-infected patients.
Use Cautiously in: Concurrent use of medications associated with rhabdomyolysis/myopathy (may ↑ risk);Phenylketonuria (chewable tablets contain phenylalanine) Geriatric: Choose dose carefully, considering concurrent disease states, drug therapy, and age-related ↓ in hepatic and renal function; Obstetric: Use in pregnancy only if maternal benefit outweighs fetal risk; Pediatric: Children <4 wk (safety and effectiveness not established).
Adverse Reactions/Side Effects
Central nervous system
- suicidal thoughts (life-threatening)
- headache (most frequent)
- myocardial infarction
- diarrhea (most frequent)
- abdominal pain
- renal failure/impairment
- stevens johnson syndrome (life-threatening)
- toxic epidermal necrolysis (life-threatening)
- rhabdomyolysis (life-threatening)
- ↑ creatine kinase
- hypersensitivity reactions
- immune reconstitution syndrome
- fever (most frequent)
Drug-Drug interactionConcurrent 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 including atazanavir may ↑ blood levels.↑ risk of rhabomyolysis/myopathy HMG-CoA reductase inhibitors.Proton pump inhibitors may ↑ levels.Efavirenz, etravirine, and tipranavir/ritonavir may ↓ levels.Administration with antacids, containing magnesium, aluminum, or calcium ↓ absorption of tipranavir; separate administration of tipranavir and magnesium- or aluminum-containing antacids by ≥2 hr.
Oral (Adults) 400 mg twice daily; ↑ dose to 800 mg twice daily when used with rifampin.
Oral (Children ≥4 wk and ≥25 kg) Tablet—400 mg twice daily; Chewable tablets (if unable to swallow tablet)—25–28 kg: 150 mg twice daily; 28–39.9 kg: 200 mg twice daily; ≥40 kg: 300 mg twice daily
Oral (Children ≥4 wk and 20–<25 kg) Chewable tablets—150 mg twice daily
Oral (Children ≥4 wk and 14–<20 kg) Oral suspension—100 mg twice daily; Chewable tablets—100 mg twice daily
Oral (Children ≥4 wk and 11–<14 kg) Oral suspension—80 mg twice daily; Chewable tablets—75 mg twice daily
Oral (Children ≥4 wk and 8–<11 kg) Oral suspension—60 mg twice daily
Oral (Children ≥4 wk and 6–<8 kg) Oral suspension—40 mg twice daily
Oral (Children ≥4 wk and 4–<6 kg) Oral suspension—30 mg twice daily
Oral (Children ≥4 wk and 3–<4 kg) Oral suspension—20 mg twice daily
Tablets: 400 mg
Chewable tabletsorange-banana: 25 mg, 100 mg
Packet for oral suspension: 100 mg
- Assess patient for change in severity of HIV symptoms and for symptoms of opportunistic infections during therapy.
- Monitor for anxiety, depression (especially in patients with a history of psychiatric illness), suicidal ideation, and paranoia during therapy.
- Assess for rash periodically during therapy. May cause Stevens-Johnson syndrome. Discontinue therapy if severe or if accompanied with fever, general malaise, fatigue, muscle or joint aches, blisters, oral lesions, conjunctivitis, hepatitis, and/or eosinophilia.
- 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 DiagnosesRisk for infection (Indications)
Noncompliance (Patient/Family Teaching)
- Tablets are not interchangeable with chewable tablets or packets for oral suspension.
- Oral: May be administered without regard to meals.
- Swallow tablets whole; do not break, crush, or chew.
- Chewable tablets may be chewed or swallowed.
- Pour packet for oral solution into 5 mL of water and mix. Once mixed, administer with syringe orally within 30 min of mixing. Discard unused solution.
- 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 prescription renewal in case changes have been made.
- 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 patients to notify health care professional if pregnancy is planned or suspected. Breast feeding should be avoided during therapy.
- Emphasize the importance of regular follow-up exams and blood counts to determine progress and monitor for side effects.
- Delayed progression of AIDS and decreased opportunistic infections in patients with HIV.
- Decrease in viral load and improvement in CD4 cell counts.
a trademark for raltegravir.