Rilpivirine

Mechanism :

As a NNRTI, rilpivirine has activity against HIV-1 by binding to reverse transcriptase.

Indication :

Treatment of HIV-1 infections in antiretroviral treatment-naive patients ≥12 years of age and weighing ≥35 kg

Contraindications :

Co-administration with anticonvulsants (carbamazepine, oxcarbazepine, phenobarbital, phenytoin), antimycobacterial (rifampin, rifapentine), proton pump inhibitors (esomeprazole, lansoprazole, omeprazole, pantoprazole, rabeprazole), systemic dexamethasone (more than a single dose).

Dosing :

≥12 years and ≥35 kg:

25 mg PO once daily.

Adverse Effect :

Depression, headache, drowsiness, hypocortisolism, increased serum cholesterol & triglycerides, nausea, increased AST and ALT, insomnia, skin rash, abdominal pain, increased serum bilirubin and creatinine.

Interaction :

Antacids: May decrease the serum concentration of Rilpivirine.
Antihepaciviral Combination Products: May increase the serum concentration of Rilpivirine.
CYP3A4 Inducers: May increase the metabolism of CYP3A4 Substrates.
CYP3A4 Inhibitors: May increase the serum concentration of Rilpivirine.
Dexamethasone: May decrease the serum concentration of Rilpivirine.
Didanosine: Rilpivirine may decrease the absorption of Didanosine.
Macrolide Antibiotics: May increase the serum concentration of Rilpivirine.
Reverse Transcriptase Inhibitors (Non-Nucleoside): May increase the serum concentration of Rilpivirine.
Rifabutin, Rifamycin: May decrease the serum concentration of Rilpivirine.

Hepatic Dose :

Mild to moderate hepatic impairment: No dosage adjustments are recommended.
Severe hepatic impairment: Guidelines are not available as it has not been studied.
Patients suffering from hepatitis B or C or raised hepatic transaminase levels may be at risk for hepatotoxicity, so use with caution and monitor carefully.