emtricitabine + tenofovir disoproxil fumarate: clinical use

Prescribing considerations

• For HIV-1 treatment, use only as part of a complete antiretroviral combination.
• For PrEP, confirm HIV-negative status and assess symptoms or recent exposure that might indicate acute HIV infection.
• Assess hepatitis B and C status, renal function, renal risk factors and relevant bone disease before initiation.
• In hepatitis B, planned discontinuation requires clinical and laboratory follow-up because severe exacerbation can occur.
• Avoid in treatment-experienced HIV-1 with the K65R resistance mutation.

Contraindications and cautions

• Hypersensitivity to either active substance or an excipient.
• Use as PrEP when HIV-1 status is positive or unknown.
• The fixed combination is not recommended for PrEP with creatinine clearance below 60 mL/min, or in severe renal impairment or haemodialysis.

Monitoring

• For PrEP: repeat HIV testing, assess adherence and ongoing HIV risk, and screen for other sexually transmitted infections.
• Monitor creatinine clearance and serum phosphate more frequently when renal risk is higher.
• Investigate progressive renal decline, hypophosphataemia, glycosuria, muscle weakness or persistent bone pain.
• Monitor liver status after discontinuation in patients with hepatitis B.

Clinical pharmacology

Both components are intracellularly phosphorylated to active metabolites that competitively inhibit HIV reverse transcriptase and terminate viral DNA chains. Both are mainly eliminated through the kidneys, and food increases tenofovir exposure.

Formulation and product differences

• The selected Milpharm product is a white-to-off-white, capsule-shaped film-coated tablet containing lactose.
• It can be disintegrated in water, orange juice or grape juice and taken immediately.
• The fixed combination prevents independent adjustment of its components; separate preparations are available when component-specific modification is required.

Tablet

Route: Oral

Strengths: 200 mg + 245 mg