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Trade Names:Isentress- Tablets 400 mg
Raltegravir is an HIV-1 antiviral agent that blocks the enzyme HIV-1 integrase that is needed for viral replication.
T max is approximately 3 h postdose. AUC and C max increase dose proportionally. Steady state is reached in approximately 2 days. Administration with a high-fat meal increases the AUC and C max by approximately 2-fold. Administration with a low-fat meal decreased the AUC and C max 46% and 52%, respectively.
Human plasma protein binding is approximately 83%.
Raltegravir is metabolized to raltegravir-glucuronide by the enzyme UGT1A1.
The half-life is approximately 9 h. Approximately 51% and 32% of an administered dose is excreted in feces and urine, respectively.
No clinically important pharmacokinetic differences were observed between subjects with severe renal impairment and healthy subjects. Because the extent to which raltegravir is dialyzable is unknown, avoid dosing before dialysis.
Hepatic Function ImpairmentNo clinically important pharmacokinetic differences were observed between subjects with moderate hepatic impairment and healthy subjects. Effect of severe hepatic impairment has not been studied.
Age, gender, raceNo dosage adjustments are needed.
Treatment of HIV-1 infection in combination with other antiretroviral agents.
None well documented.
PO 400 mg twice daily.
Coadministration of RifampinAdultsPO 800 mg twice daily.
Store at 59° to 86°F.
Raltegravir plasma levels may be reduced. The recommended dosage of raltegravir is 800 mg twice daily during coadministration with rifampin. Coadminister with caution.
Drugs that inhibit UGT1A1 (eg, atazanavir, atazanavir/ritonavir)Raltegravir plasma levels may be increased; however, dosage adjustments are not needed with coadministration of atazanavir/ritonavir. Monitor the response of the patient.
Efavirenz, etravirineRaltegravir plasma concentrations may be reduced. The clinical importance has not been assessed. Monitor the response of the patient.
OmeprazoleRaltegravir plasma concentrations may be increased because of increased solubility at higher pH. Dosage adjustments do not appear to be necessary. Monitor the response of the patient.
Tipranavir/RitonavirRaltegravir plasma concentrations may be reduced. No dosage adjustment is recommended. Monitor the response of the patient.
None well documented.
Insomnia (4%); abnormal dreams, dizziness (less than 2%); asthenia; fatigue; headache; anxiety, depression, paranoia, suicidal ideation and behavior (postmarketing).
Rash, Stevens-Johnson syndrome (postmarketing).
Abdominal pain, gastritis (less than 2%); nausea.
Genital herpes, renal failure (less than 2%).
Hepatitis (less than 2%).
Hypersensitivity (less than 2%).
Decreased hemoglobin, neutrophils, triglycerides, and platelets; increased serum alkaline phosphatase, ALT, AST, bilirubin, creatine kinase, fasting glucose, HDL cholesterol , lipase, LDL cholesterol, total cholesterol, and pancreatic amylase.
Herpes zoster (less than 2%).
MonitorMonitor CD4+ cell count and HIV-1 RNA load. |
Category C .
Undetermined; however, HIV-infected mothers should not breast-feed.
Safety and effectiveness not established.
Select dose with caution because of the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant diseases or other drug therapy.
Effect of severe hepatic impairment has not been studied.
During initial phase of treatment, patients may develop an inflammatory response to indolent or residual opportunistic infections (eg, Mycobacterium avium complex), which may require further evaluation and treatment.
No information is available.
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