Nurses Compass
Drug Guide
Dolutegravir
Classification
Therapeutic: Antiretroviral Agent
Pharmacological: Integrase Strand Transfer Inhibitor (INSTI)
FDA Approved Indications
- Treatment of HIV-1 infection in adults and children aged 4 weeks and older
Mechanism of Action
Dolutegravir inhibits the HIV integrase enzyme, preventing the integration of viral DNA into the host cell genome, thereby inhibiting viral replication.
Dosage and Administration
Adult: 50 mg once daily, with or without food.
Pediatric: For children 4 weeks and older, dosage is based on weight and age, typically starting at 10 mg once daily. Specific dosing should be determined by a healthcare provider.
Geriatric: No specific dosage adjustment needed, but elderly patients should be monitored for drug interactions and renal function.
Renal Impairment: No dosage adjustment for mild to moderate impairment. For severe impairment, use with caution and consider monitoring.
Hepatic Impairment: No dosage adjustment necessary.
Pharmacokinetics
Absorption: Rapidly absorbed, bioavailability >80%.
Distribution: Widely distributed, substantial plasma protein binding (~99%).
Metabolism: Primarily through UGT1A1 with minor CYP3A4 involvement.
Excretion: Excreted mainly in feces (~85% as unchanged drug and metabolites), minimal renal clearance.
Half Life: Approximate half-life of 14 hours.
Contraindications
- Hypersensitivity to dolutegravir or any component of the formulation.
Precautions
- Use with caution in patients with pre-existing depression or hypersensitivity reactions. Consider potential drug interactions, especially with polyvalent cations. Monitor for signs of hypersensitivity and neuropsychiatric symptoms.
Adverse Reactions - Common
- Insomnia (>10%)
- Headache (>10%)
- Fatigue (>10%)
Adverse Reactions - Serious
- Allergic reactions, including hypersensitivity and anaphylaxis (Rare)
- Liver toxicity, including elevated liver enzymes (Less common)
- Neuropsychiatric effects, such as depression, suicidality (Rare)
Drug-Drug Interactions
- Rifampin (decreases dolutegravir levels)
- Cation-containing antacids, supplements, or multivitamins (reduce absorption)
Drug-Food Interactions
N/ADrug-Herb Interactions
N/ANursing Implications
Assessment: Monitor for signs of hypersensitivity, neuropsychiatric symptoms, and hepatic function. Assess for potential drug interactions.
Diagnoses:
- Risk for drug toxicity
- Risk for injury related to neuropsychiatric effects
Implementation: Administer once daily, with or without food. Educate patient on medication adherence and potential side effects.
Evaluation: Evaluate viral load and CD4 count regularly to assess efficacy.
Patient/Family Teaching
- Take medication exactly as prescribed, without missing doses.
- Report any signs of allergic reactions, mood changes, or liver problems.
- Be aware of potential drug interactions, especially with antacids and supplements.
Special Considerations
Black Box Warnings:
- Potential risk of hypersensitivity reactions that may be life-threatening. Patients should be monitored closely, and medication discontinued if hypersensitivity is suspected.
Genetic Factors: Testing for HLA-B*5701 is not required with dolutegravir, unlike with abacavir.
Lab Test Interference: May cause falsely elevated serum creatinine without affecting actual renal function.
Overdose Management
Signs/Symptoms: Nausea, vomiting, dizziness, or somnolence after overdose.
Treatment: Supportive care; no specific antidote. Consider gastric decontamination if ingestion was recent. Dialysis is unlikely to be effective due to high protein binding.
Storage and Handling
Storage: Store at room temperature 20°C to 25°C (68°F to 77°F).
Stability: Stable for at least 24 months when stored properly.