Isentress Generic Name & Formulations
Raltegravir (as potassium) 25mg, 100mg+; chew tabs; scored (+); orange-banana flavor; contains phenylalanine; 400mg; film-coated tabs.
HIV-1 integrase strand transfer inhibitor (INSTI).
Chew tabs, film-coated tabs—60; Susp (pkts)—1, 60 (w. syringes, mixing cups)
HIV-1 infection, in combination with other antiretrovirals.
Isentress Dosage and Administration
Film-coated tabs: swallow whole.Treatment-naïve or virologically suppressed on Isentress 400mg twice daily: 1200mg (2 x 600mg) once daily or 400mg twice daily. Treatment-experienced: 400mg twice daily. Avoid dosing before dialysis sessions. Concomitant rifampin: 800mg (2 x 400mg) twice daily.
<4 weeks: use oral susp. Film-coated tabs: swallow whole. ≥4 weeks (<25kg): use other forms; (≥25kg): 400mg twice daily; (≥40kg): treatment-naïve or virologically suppressed on Isentress 400mg twice daily: 1200mg (2 x 600mg) once daily or 400mg twice daily. If unable to swallow, can use chew tabs: (3–<6kg): 25mg twice daily; (6–<10kg): 50mg twice daily; (10–<14kg): 75mg twice daily; (14–<20kg): 100mg twice daily; (20–<25kg): 150mg twice daily; (25–<28kg): 150mg twice daily; (28–<40kg): 200mg twice daily; ≥40kg: 300mg twice daily. Chew tabs max dose: 300mg twice daily. The 25mg chew tabs may be crushed for those who have difficulty chewing. See full labeling.
Isentress Boxed Warnings
Chew tabs or oral susp are not interchangeable with the film-coated tabs. Monitor liver aminotransferases, myopathy, and rhabdomyolysis. Discontinue if signs/symptoms of severe skin or hypersensitivity reactions develop. Hepatic impairment: Isentress HD not recommended. Pregnancy. Nursing mothers: not recommended.
May be antagonized by UGT1A1 inducers (eg, rifampin; see Adult dose) and potentiated by UGT1A1 inhibitors. Concomitant aluminum and/or magnesium-containing antacids, other strong enzyme inducers (eg, carbamazepine, phenobarbital, phenytoin): not recommended. Caution with concomitant drugs known to cause myopathy or rhabdomyolysis (eg, statins). Isentress HD: concomitant calcium carbonate antacid, rifampin, tipranavir/ritonavir, etravirine: not recommended.
Isentress Adverse Reactions
Insomnia, headache, dizziness, nausea, fatigue, creatinine kinase elevations, myopathy, rhabdomyolysis; severe skin reactions (eg, Stevens-Johnson syndrome, toxic epidermal necrolysis), hypersensitivity, immune reconstitution syndrome.
Isentress Clinical Trials
Register pregnant patients exposed to raltegravir by calling (800) 258-4263.
Isentress Patient Counseling