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Pharmacologic class: Human immunodeficiency virus (HIV) integrasestrand transfer inhibitor
Therapeutic class: Antiretroviral
Pregnancy risk category C
Rapidly blocks HIV integrase (enzyme needed for HIV replication), leading to viral load reduction and increased CD4+ count
Tablets (chewable): 25 mg, 100 mg
Tablets (film-coated): 400 mg
Indications and dosages
➣ HIV-1 infection in adults used in combination with other antiretrovirals
Adults and adolescents ages 12 and older: 400 mg film-coated tablet P.O. b.i.d.
Children age 6 to younger than age 12 weighing at least 25 kg (55 lb): One 400-mg film-coated tablet P.O. b.i.d. or chewable tablets, weight based to maximum of 300 mg P.O. b.i.d.
Children age 6 to younger than age 12 weighing less than 25 kg (55 lb): Chewable tablets, weight based to maximum of 300 mg P.O. b.i.d.
Children age 2 to younger than age 6 weighing at least 10 kg (22 lb): Chewable tablets, weight based to maximum of 300 mg P.O. b.i.d.
Use cautiously in:
• treatment-naive adults (safety and efficacy not established)
• increased risk of myopathy or rhabdomyolysis (such as with concomitant use of drugs known to cause these conditions)
• elderly patients
• pregnant patients
• breastfeeding patients (use not recommended)
• children younger than age 2 (safety and efficacy not established).
• Administer with or without food.
• Be aware that film-coated tablets can't be substituted with chewable tablets.
CNS: headache, fatigue, asthenia, dizziness, insomnia
CV: myocardial infarction
GI: nausea, vomiting, diarrhea, abdominal pain, gastritis
GU: toxic nephropathy, renal failure, renal tubular necrosis
Hematologic: anemia, neutropenia
Musculoskeletal: myopathy, rhabdomyolysis
Skin: lipodystrophy, Stevens-Johnson syndrome, toxic epidermal necrolysis
Other: fever, herpes simplex, immune reconstitution syndrome, hypersensitivity reaction
Drug-drug. Strong UGT1A1 inducers (such as rifampin): reduced raltegravir blood level
UGT1A1 inhibitors (such as atazanavir): increased raltegravir blood level
Drug-diagnostic tests. Absolute neutrophil count, hemoglobin, platelets: decreased levels
ALP, ALT, AST, blood glucose, creatine kinase, lipase, pancreatic enzymes, total bilirubin: increased levels
• Monitor renal function tests.
• Be aware that immune reconstitution syndrome has occurred in patients receiving drug with combination antiretroviral therapy. During initial phase of therapy, patient whose immune system responds may develop inflammatory response to indolent or residual opportunistic infections (such as Mycobacterium avium complex, cytomegalovirus, Pneumocystis jiroveci pneumonia, or tuberculosis), which may necessitate further evaluation and treatment.
• Be aware that severe, potentially life-threatening and fatal skin reactions have been reported, including Stevens-Johnson syndrome, hypersensitivity reaction, and toxic epidermal necrolysis. Immediately discontinue drug if severe hypersensitivity, severe rash, or rash with systemic symptoms or liver aminotransferase elevations develops. Closely monitor clinical status, including liver aminotransferases.
• Tell patient drug may be taken with or without food.
• Inform patient with phenylketonuria that chewable tablets contain phenylalanine.
• Inform patient that drug doesn't cure HIV infection or reduce risk of passing it to others through sexual contact, needle sharing, or blood exposure.
☞ Advise patient to immediately report muscle weakness, urinary problems, new infections, rash, fever, general malaise, swelling of face or throat, or chest pain.
• Instruct female patient to notify prescriber if she is pregnant or intends to become pregnant.
• Caution breastfeeding patient to discontinue breastfeeding while taking drug, because of potential HIV transmission and adverse reactions in infants.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs and tests mentioned above.
Pharmacologic: integrase strand transfer inhibitors instis
Time/action profile (blood levels)
|PO||unknown||3 hr||12 hr|
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.
- 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.