Drug information of rilpivirine

rilpivirine


It is used to treat HIV infection

Mechanism of effect

Rilpivirine is a non-competitive NNRTI(non-nucleoside reverse transcriptase inhibitor ) that binds to reverse transcriptase. Its binding results in the blockage of RNA and DNA- dependent DNA polymerase activities, like HIV-1 replication. It does not present activity against human DNA polymerases α, β and γ.

Pharmacodynamic

Rilpivirine treatment produces a significant and effective reduction in the viral load based on the study of HIV-1 RNA copies per ml or immunologic changes by the determination of counts of CD4+ and CD8+ cells

Pharmacokinetics

Absorption

Increased 40% with a meal (normal-to-high calorie)

Metabolism

Hepatic, primarily by CYP3A4

Excretion

Feces (85%, ~25% as unchanged drug); urine (~6%; <1% as unchanged drug)

Time to Peak

Plasma: 4 to 5 hours

Half-Life Elimination

~50 hours

Protein Binding

99.7% (primarily albumin)

Drug indications

HIV-1 infection: Treatment of HIV-1 infections in antiretroviral treatment-naive patients ≥12 years of age and weighing ≥35 kg, with HIV-1 RNA ≤100,000 copies/mL at the start of therapy in combination with other antiretroviral agents

Dosage

Usual Adult Dose for HIV Infection

25 mg orally once a day

Usual Pediatric Dose for HIV Infection

12 years or older, weighing at least 35 kg: 25 mg orally once a day

Drug contraindications

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

  • depression
  • liver impairment
renal impairment

Side effects

  • Changes in behavior
  • cloudy or bloody urine
  • discouragement
  • feeling sad or empty
  • gaseous abdominal or stomach pain
  • indigestion
  • irritability
  • lack of appetite
  • loss of interest or pleasure
  • recurrent fever
  • severe nausea or vomiting
  • stomach fullness
  • swelling of the face, feet, or lower legs
  • thoughts of killing oneself
  • tiredness
  • trouble concentrating
  • trouble sleeping
yellow eyes or skin

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

 orlistat, other HIV NNRTIs (such as efavirenz, nevirapine, delavirdine)

Alerts

Rilpivirine can cause serious, life-threatening side effects. These include severe skin rash, depression, mood changes, and liver problems.

Contact your health care provider right away if you get a rash

Points of recommendation

Before using this medication, tell your doctor or pharmacist your medical history, especially of: kidney disease, liver disease (such as hepatitis B, hepatitis C), mental/mood disorders (such as depression).

Pregnancy level

US FDA pregnancy category: Not assigned

Drug forms

edurant

Ask a Pharmacist


User's questions
    No comments yet.