dolutegravir sodium: clinical use

Prescribing considerations

• Use under an HIV-experienced prescriber as part of appropriate combination treatment.
• Review integrase-resistance history and concomitant enzyme inducers.
• Coordinate pregnancy and infant-feeding decisions with specialist HIV services.
• Review psychiatric history and counsel about mood deterioration or suicidal thoughts.

Contraindications and cautions

• Hypersensitivity to dolutegravir or a formulation excipient.
• Concomitant fampridine or another narrow-therapeutic-index OCT2 substrate covered by the product contraindication.
• Use caution in severe hepatic impairment because clinical data are unavailable.

Monitoring

• HIV viral load, adherence and treatment response; investigate virological failure and resistance where appropriate.
• Liver biochemistry, particularly with hepatitis B or C coinfection or symptoms of hypersensitivity or hepatic injury.
• Renal function and glycaemic control with metformin.
• Weight and clinically appropriate metabolic parameters.
• OCT2/MATE1 inhibition may cause a small creatinine rise without reducing glomerular filtration.

Clinical pharmacology

Dolutegravir inhibits HIV integrase-mediated strand transfer. It is mainly metabolised by UGT1A1, with a minor CYP3A contribution, and inhibits renal OCT2 and MATE1 transporters.

Formulation and product differences

• Dispersible tablets are suitable for younger or lower-weight children and people for whom film-coated tablets are inappropriate.
• Dispersible tablets can be dispersed in water or swallowed whole but must not be chewed, cut or crushed.
• Dispersible and film-coated tablets have different bioavailability and are not interchangeable milligram for milligram.

Dispersible tablet

Route: Oral

Strengths: 5 mg

Tablet

Route: Oral

Strengths: 50 mg