Home Drug Guide Dolutegravir Sodium

Drug Guide

Generic Name

Dolutegravir Sodium

Brand Names Tivicay, Tivicay PD

Classification

Therapeutic: Antiretroviral agent, integrase strand transfer inhibitor

Pharmacological: Integrase inhibitor

FDA Approved Indications

Treatment of HIV-1 infection in adults and pediatric patients (4 weeks and older)

Mechanism of Action

Dolutegravir inhibits HIV integrase, an enzyme critical for viral DNA integration into the host cell genome, thereby blocking viral replication.

Dosage and Administration

Adult: Typically 50 mg once daily, with or without food. Dose adjustments may be needed for renal or hepatic impairment.

Pediatric: Dosing varies based on weight and age; consult current guidelines.

Geriatric: No specific dosage adjustment, but caution in patients with comorbidities.

Renal Impairment: No dose adjustment for mild to moderate impairment; caution in severe impairment.

Hepatic Impairment: Use with caution; no specific dose adjustment recommended.

Pharmacokinetics

Absorption: Rapidly absorbed, peak plasma concentrations in approximately 2-3 hours.

Distribution: Widely distributed; protein binding about 99%.

Metabolism: Primarily metabolized via UGT1A1 with some hepatic CYP3A involvement.

Excretion: Excreted mainly in feces (approximately 66%) and urine (about 13%).

Half Life: Approximately 14 hours.

Contraindications

Known hypersensitivity to dolutegravir or any component of the formulation.

Precautions

Risk of immune reconstitution inflammatory syndrome (IRIS), hepatic impairment, hypersensitivity reactions. Use caution in patients with a history of psychiatric disorders.

Adverse Reactions - Common

Insomnia (Common)
Headache (Common)
Nausea (Common)

Adverse Reactions - Serious

Allergic reactions including rash and hypersensitivity (Rare)
Liver enzyme elevations (Uncommon)
Suicidal ideation (Rare)

Drug-Drug Interactions

Metformin (may increase levels), certain antacids (carbonate, chewable, or buffered), drugs inducing or inhibiting UGT or CYP3A enzymes.

Drug-Food Interactions

N/A

Drug-Herb Interactions

N/A

Nursing Implications

Assessment: Monitor for signs of hypersensitivity, hepatotoxicity, and neuropsychiatric effects.

Diagnoses:

Risk for infection related to HIV progression
Impaired liver function

Implementation: Administer as prescribed, counsel patient on adherence, monitor liver function tests, and observe for adverse effects.

Evaluation: Assess effectiveness through viral load suppression, monitor for side effects, and assess adherence.

Patient/Family Teaching

Take medication exactly as prescribed.
Report any allergic reactions or unusual side effects.
Use caution with alcohol and other medications.

Special Considerations

Black Box Warnings:

Risk of neuropsychiatric effects including depression and suicidal ideation

Genetic Factors: None specified.

Lab Test Interference: May cause falsely elevated serum creatinine without affecting actual glomerular filtration rate.

Overdose Management

Signs/Symptoms: Nausea, vomiting, dizziness.

Treatment: Supportive care; no specific antidote; consider gastrointestinal decontamination if ingestion is recent.

Storage and Handling

Storage: Store at room temperature (20-25°C).

Stability: Stable under recommended storage conditions for the shelf life indicated by the manufacturer.