Raltegravir Potassium

Trade Names:
Isentress
- Tablets 400 mg

Pharmacology

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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 and C _max by approximately 2-fold, and delays T _max . Administration with a low-fat meal decreased the AUC and C _max 46% and 52%, respectively.

Distribution

Human plasma protein binding is approximately 83%.

Metabolism

Raltegravir is metabolized to raltegravir-glucuronide by the enzyme UGT1A1.

Elimination

The half-life is approximately 9 h. Approximately 51% and 32% of an administered dose is excreted in feces and urine, respectively.

Special Populations

Because the extent to which raltegravir is dialyzable is unknown, avoid dosing before dialysis.

Effect of severe hepatic function impairment has not been studied.

No dosage adjustments are needed.

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

PO 400 mg twice daily.

PO 800 mg twice daily.

General Advice

• May be given with or without food.

Storage/Stability

Store at 59° to 86°F.

Drug Interactions

Raltegravir plasma levels may be reduced.

Raltegravir plasma levels may be increased; however, dosage adjustments are not needed with coadministration of atazanavir/ritonavir.

Raltegravir plasma concentrations may be reduced. The clinical importance has not been assessed.

Raltegravir plasma concentrations may be increased because of increased solubility at higher pH. Dosage adjustments do not appear to be necessary.

Laboratory Test Interactions

None well documented.

Adverse Reactions

CNS

Headache (3%); asthenia, fatigue (2%); dizziness (less than 2%); depression, suicidal ideation (postmarketing).

Dermatologic

Rash, Stevens-Johnson syndrome (postmarketing).

GI

Nausea (2%); abdominal pain, gastritis (less than 2%).

Genitourinary

Genital herpes, renal failure (less than 2%).

Hepatic

Hepatitis (less than 2%).

Hypersensitivity

Hypersensitivity (less than 2%).

Lab Tests

Decreased hemoglobin, neutrophils, and platelets; increased serum alkaline phosphatase, ALT, AST, bilirubin, creatine kinase, fasting glucose, lipase, and pancreatic amylase.

Miscellaneous

Herpes zoster (less than 2%).

Precautions

Pregnancy

Category C .

Lactation

Undetermined; however, HIV-infected mothers should not breast-feed.

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.

Renal Function

No dosage adjustment is needed.

Hepatic Function

No dosage adjustment is needed in patients with mild to moderate hepatic function impairment.

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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