Rilpivirine


Concise Prescribing Info
Indications/Uses
HIV-1 Infection.
Dosage/Direction for Use
Adult : PO In combination with other antiretrovirals in treatment-naive patient with viral load ≤100,000 copies/mL at baseline: 25 mg once daily.
Dosage Details
Oral
HIV-1 infection
Adult: In combination with other antiretrovirals in treatment-naive patient with viral load ≤100,000 copies/mL at baseline: 25 mg once daily.
Child: ≥12 years Same as adult dose.
Special Patient Group
Patient taking rifabutin: 50 mg once daily. Return to usual adult dose upon discontinuation of rifabutin.
Administration
Should be taken with food. Take w/ meals for optimal absorption.
Contraindications
Hypersensitivity. Lactation. Concomitant use with anticonvulsants (e.g. carbamazepine, oxcarbazepine, phenobarbital phenytoin); antimycobacterials (e.g. rifampicin, rifapentine); proton pump inhibitors (e.g. omeprazole, esomeprazole, lansoprazole, pantoprazole, rabeprazole); systemic glucocorticoid (e.g. dexamethasone); St. John’s wort.
Special Precautions
Patient with elevated transaminases, hepatitis B or C, severe immune deficiency. Not intended for use in patient with viral load >100,000 copies/mL. Severe renal and hepatic impairment. Children. Pregnancy.
Adverse Reactions
Significant: Depression, depressed mood, dysphoria, mood changes, negative thoughts, suicide attempts or suicidal ideation; fat redistribution (e.g. central obesity, buffalo hump); hepatotoxicity; hypersensitivity reactions (e.g. severe rash, angioedema, fever, DRESS); immune reconstitution syndrome, autoimmune disorders (e.g. Grave’s disease).
Gastrointestinal disorders: Nausea, abdominal pain and discomfort, dry mouth, vomiting.
General disorders and administration site conditions: Fatigue.
Investigations: Increased lipase, ALT/AST, bilirubin, total cholesterol, LDL cholesterol, and triglycerides; decreased plasma cortisol, Hb, WBC, and platelet count.
Metabolism and nutrition disorders: Decreased appetite.
Nervous system disorders: Headache, dizziness.
Psychiatric disorders: Drowsiness, insomnia.
Patient Counseling Information
This drug may cause dizziness and somnolence, if affected, do not drive or operate machinery.
MonitoringParameters
Monitor LFT at baseline and during therapy; cholesterol, triglycerides. Monitor for signs and symptoms of rash, fever, hypersensitivity reactions, inflammation, and infection.
Overdosage
Symptoms: Headache, nausea, dizziness, abnormal dreams. Management: Supportive treatment. Monitor vital signs and ECG. Administer activated charcoal to aid in the removal of unabsorbed active substance.
Drug Interactions
H2 antagonists (e.g. cimetidine, ranitidine) may decrease the absorption of rilpivirine. Increased plasma concentration with CYP3A inhibitors (e.g. erythromycin).
Potentially Fatal: Significantly decreased plasma concentration with carbamazepine, oxcarbazepine, phenobarbital, phenytoin, dexamethasone, rifampicin, rifapentine. Reduced absorption due to increase in gastric pH with omeprazole, esomeprazole, lansoprazole, pantoprazole, rabeprazole.
Food Interaction
Increased absorption with food. Decreased plasma concentration with St. John’s wort. Increased exposure with grapefruit products.
Action
Description: Rilpivirine is a 2nd generation diarylpyearsimidine non-nucleoside reverse transcriptase inhibitor (NNRTI), which inhibits HIV-1 from binding to reverse transcriptase, leading to reduced viral DNA synthesis.
Pharmacokinetics:
Absorption: Increased absorption by approx 40% with normal to high-caloric meal. Time to peak plasma concentration: 4-5 hours.
Distribution: Plasma protein binding: 99.7%, primarily to albumin.
Metabolism: Metabolised in the liver via oxidation by CYP3A4 isoenzyme pathway.
Excretion: Mainly via faeces (85%, approx 25% as unchanged drug); urine (approx 6%, <1% as unchanged drug). Terminal elimination half-life: Approx 50 hours.
Chemical Structure

Click on icon to see table/diagram/image
Storage
Store at 25°C. Protect from light.
MIMS Class
ATC Classification
J05AG05 - rilpivirine ; Belongs to the class of non-nucleoside reverse transcriptase inhibitors. Used in the systemic treatment of viral infections.
Disclaimer: This information is independently developed by MIMS based on Rilpivirine from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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