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raltegravir

J05AJ01

Forms & Strengths

Oral tablet: 400 mg
Oral tablet (film-coated): 600 mg
Oral chewable tablet: 25 mg, 100 mg
Oral suspension for reconstitution: 100 mg packet

Adult Dosing

400 mg orally twice daily (film-coated tablets)
1200 mg (two 600 mg tablets) orally once daily (treatment-naive or virologically suppressed on 400 mg twice daily)
Co-administered with rifampin: 800 mg orally twice daily

Pediatric Dosing

Neonates (birth to 4 weeks): 1.5 mg/kg/dose orally twice daily (oral suspension)
Infants and children (4 weeks to less than 12 years): Weight-based dosing using chewable tablets or suspension, administered twice daily
Children and adolescents (at least 12 years and at least 40 kg): 400 mg twice daily or 1200 mg once daily

Indications

Treatment of HIV-1 infection in combination with other antiretroviral agents
Post-exposure prophylaxis (PEP) for occupational and non-occupational HIV exposure

Mechanism of Action

HIV-1 integrase strand transfer inhibitor (INSTI)
Inhibits the catalytic activity of HIV-1 integrase, blocking the strand transfer step of viral DNA integration into the host genome, thus preventing HIV replication

Contraindications

Hypersensitivity to raltegravir or any component of the formulation

Adverse Reactions

Insomnia
Headache
Nausea
Fatigue
Diarrhea
Dizziness
Elevated creatine kinase and myopathy
Severe hypersensitivity reactions (including Stevens-Johnson syndrome and toxic epidermal necrolysis)
Immune reconstitution inflammatory syndrome (IRIS)

Drug Interactions

Rifampin: Potent UGT1A1 inducer; decreases raltegravir concentrations, requiring a dose increase to 800 mg twice daily for the 400 mg formulation
Antacids containing aluminum and/or magnesium: Decreased absorption of raltegravir; co-administration with metal-containing antacids is not recommended
Tipranavir/ritonavir: May decrease raltegravir trough concentrations

Curated Content: Needs Vetting Before Put to Clinical Use