EDURANT 25MG TABLET

Indications

• HIV-1 infection
• HIV infection in treatment-naive adults
• HIV infection in treatment-experienced patients with certain resistance patterns

Dosage

Children: Refer to the BNF for Children for appropriate dosing guidelines.

Adults: Refer to the most recent clinical guidelines for specific dosing recommendations.

Mechanism of action

Rapivirine binds to a specific site on the reverse transcriptase enzyme, leading to a conformational change that inhibits its activity. This action prevents the conversion of viral RNA into DNA, a crucial step in the HIV replication cycle. By blocking this enzyme, rapivirine effectively reduces the viral load in the body.

Pharmacodynamics

The pharmacodynamics of rapivirine involves its ability to suppress HIV replication by inhibiting the activity of reverse transcriptase. The drug exhibits dose-dependent effects on viral suppression and has demonstrated efficacy in reducing plasma viral loads in clinical studies. The emergence of drug resistance can occur with suboptimal dosing and adherence, leading to decreased effectiveness over time.

Pharmacokinetics

Rapivirine has a relatively long half-life, allowing for once-daily dosing in most cases. It is well absorbed from the gastrointestinal tract, with peak plasma concentrations occurring within several hours post-administration. The drug is metabolized primarily in the liver via cytochrome P450 enzymes, particularly CYP3A4, and is excreted mainly in feces. Drug interactions can occur with other medications that induce or inhibit these enzymes, affecting the plasma levels of rapivirine.

Contra-indications

• Hypersensitivity to rilpivirine or any excipients
• Concomitant use with certain medications that are strong inducers of CYP3A

Adverse effects

• Depressive disorders
• Insomnia
• Headache
• Rash
• Nausea
• Fatigue
• Elevated liver enzymes

Interactions

• Rilpivirine is primarily metabolized by CYP3A4, and co-administration with strong CYP3A4 inducers (e.g., rifampicin, carbamazepine) may reduce its efficacy
• Concomitant use with proton pump inhibitors may decrease rilpivirine plasma concentrations
• Use with other antiretroviral agents may have additive effects

Precautions

• Monitor for signs of depressive symptoms
• Renal impairment may require dose adjustment
• Assess for potential drug interactions before initiation

Pregnancy

Rilpivirine should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Limited data is available regarding use during pregnancy.

Breast-feeding

Breastfeeding is not recommended during rilpivirine treatment due to potential transmission of HIV and the drug through breast milk.

Storage

Store at room temperature, away from moisture and heat. Keep out of reach of children.

Formulations

• Oral tablet (25 mg)