abacavir sulfate + dolutegravir sodium + lamivudine: clinical use

Prescribing considerations

• Document a negative HLA-B*5701 result before initiation; this does not completely exclude hypersensitivity.
• Review previous abacavir or dolutegravir hypersensitivity and resistance history.
• Assess renal and hepatic function, hepatitis B status, cardiovascular risk and interactions.
• Use individual components if an active ingredient must be adjusted or discontinued.
• Ensure appropriate hepatitis B-active therapy if co-infected.
• Consider an alternative in patients with high cardiovascular risk.

Contraindications and cautions

• HLA-B*5701 positivity.
• Previous suspected abacavir hypersensitivity; do not rechallenge.
• Hypersensitivity to an active ingredient or excipient.
• Concomitant fampridine or another narrow-therapeutic-index OCT2 substrate where increased exposure presents serious risk.
• Not generally recommended in moderate or severe hepatic impairment, or when renal impairment prevents safe fixed-dose lamivudine use.

Monitoring

• HIV viral load, response and adherence.
• Renal function and lamivudine-related haematological toxicity where renal clearance is reduced.
• Liver chemistry, especially with existing disease, viral hepatitis or suspected hypersensitivity.
• Weight, blood glucose and lipids.
• Hypersensitivity, severe skin reactions, psychiatric effects and immune reconstitution.
• Hepatitis B markers and liver function if treatment stops in a co-infected patient.

Clinical pharmacology

Dolutegravir inhibits integrase strand transfer. Intracellular carbovir triphosphate and lamivudine triphosphate inhibit HIV reverse transcriptase and terminate viral DNA chains. Dolutegravir can raise serum creatinine by inhibiting tubular secretion without necessarily reducing glomerular filtration.

Formulation and product differences

• Film-coated tablets are for people weighing at least 25 kg and are swallowed with liquid.
• Dispersible tablets are for younger children within the licensed age and weight range and must be dispersed in drinking water using the supplied cup.
• The formulations are not directly interchangeable because dolutegravir bioavailability is higher from dispersible tablets.
• Keep either formulation protected from moisture in its original tightly closed container with the desiccant.

Dispersible tablet

Route: Oral

Strengths: 5 mg + 60 mg + 30 mg

Tablet

Route: Oral

Strengths: 50 mg + 600 mg + 300 mg