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 Infection12 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
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
Interactions
Dolasetron , vandetanib , Dofetilide , Efavirenz , Etravirine , Halofantrine , Grepafloxacin , Doravirine , Dexlansoprazole , Apalutamide , Esomeprazole , Oxecarbazepin , Pantoprazole , Dexamethasone , Rabeprazole , Rifampin , nevirapine , Delavirdine , Phenobarbital , Phenytoin , Lansoprazole , orlistat , Carbamazepine , Rifapentine , bedaquiline , RemdesivirCoadministration 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
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