Raltegravir
Pronouncation: (ral-TEE-gra-veer)Class: Antiretroviral, Integrase Inhibitor
Trade Names:
Isentress
- Tablets 400 mg
Pharmacology
Raltegravir is an HIV-1 antiviral agent that blocks the enzyme HIV‐1 integrase that is needed for viral replication.
Pharmacokinetics
Absorption
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 by 19%, decreases C max by approximately 34%, and delays T max .
Distribution
Human plasma protein binding is approximately 83%.
Metabolism
Raltegravir is metabolized to raltegravir-glucuronide by the enzyme UDP-glucuronosyltransferase (UGT) 1A1.
Elimination
The t ½ is approximately 9 h. Approximately 51% and 32% of an administered dose is excreted in feces and urine, respectively.
Special Populations
Hepatic Function ImpairmentEffect of severe hepatic function impairment has not been studied.
Renal function impairmentBecause the extent to which raltegravir is dialyzable is unknown, avoid dosing before dialysis.
Indications and Usage
Treatment of HIV-1 infection in combination with other antiretroviral agents in treatment-experienced adult patients who have evidence of viral replication and HIV-1 strains resistant to multiple antiretroviral agents.
Contraindications
None.
Dosage and Administration
AdultsPO 400 mg twice daily.
Storage/Stability
Store at 59° to 86°F.
Drug Interactions
Drugs that are strong inducers of UGT1A1 (eg, rifampin, ritonavir, tipranavir)Raltegravir plasma levels may be reduced.
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.
Laboratory Test Interactions
None well documented.
Adverse Reactions
Cardiovascular
MI.
CNS
Headache (10%); pyrexia (5%); asthenia, dizziness, fatigue (less than 2%).
Dermatologic
Acquired lipodystrophy (less than 2%).
GI
Diarrhea (17%); nausea (10%); abdominal pain, vomiting (less than 2%); gastritis.
Genitourinary
Chronic renal failure; renal failure; renal tubular necrosis; toxic nephropathy.
Hematologic-Lymphatic
Anemia; neutropenia.
Hepatic
Hepatitis.
Hypersensitivity
Hypersensitivity.
Lab Tests
Decreased hemoglobin, neutrophils, and platelets; elevated alkaline phosphatase, ALT, AST, blood glucose, serum creatine kinase, serum lipase test, serum pancreatic amylase test, and total serum bilirubin.
Musculoskeletal
Myopathy; rhabdomyolysis.
Miscellaneous
Cancer (eg, anal cancer, hepatocellular carcinoma, Kaposi sarcoma, lymphoma, squamous cell carcinoma); herpes simplex.
Precautions
MonitorMonitor CD4+ cell count and HIV‐1 RNA load. |
Pregnancy
Category C .
Lactation
Undetermined; however, HIV-infected mothers should not breast-feed their infants.
Children
Safety and effectiveness not established in children younger than 16 yr of age.
Elderly
Select dose with caution because of the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant diseases or other drug therapy.
Immune reconstitution syndrome
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.
Overdosage
Symptoms
No information is available.
Patient Information
- Advise patient to read the patient information leaflet before using product the first time and with each refill.
- Inform patient that this medication is not a cure for HIV infection or AIDS.
- Emphasize to patient, family, and significant others that this medication does not reduce the risk of transmitting HIV to others through sexual contact or blood contamination.
- Instruct patients that if they miss a dose, they should take it as soon as they remember. If they do not remember until it is time to take the next dose, they should skip the missed dose and go back to their regular schedule. They should not double the next dose.
- Advise patients to take this medication exactly as prescribed, with or without food.
- Warn patients not to alter dose or discontinue medication without consulting health care provider.
- Explain that the long-term effects of this medication are not known.
- Inform patients to report any persistent bothersome adverse reactions.
- Inform patients to report symptoms of unexplained muscle pain, tenderness, or weakness to health care provider.
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