Rilpivirine

Oral
HIV-1 infection

Patient taking rifabutin: 50 mg once daily. Return to usual adult dose upon discontinuation of rifabutin.

Should be taken with food. Take w/ meals for optimal absorption.

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.

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.

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.

This drug may cause dizziness and somnolence, if affected, do not drive or operate machinery.

Monitor LFT at baseline and during therapy; cholesterol, triglycerides. Monitor for signs and symptoms of rash, fever, hypersensitivity reactions, inflammation, and infection.

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.

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.

Increased absorption with food. Decreased plasma concentration with St. John’s wort. Increased exposure with grapefruit products.

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.

Source: National Center for Biotechnology Information. PubChem Database. Rilpivirine, CID=6451164, https://pubchem.ncbi.nlm.nih.gov/compound/Rilpivirine (accessed on Jan. 23, 2020)

Store at 25°C. Protect from light.

Antivirals

J05AG05 - rilpivirine ; Belongs to the class of non-nucleoside reverse transcriptase inhibitors. Used in the systemic treatment of viral infections.

Anon. Rilpivirine (Briggs Drugs in Pregnancy and Lactation). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 03/01/2018.

Anon. Rilpivirine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 03/01/2018.

Buckingham R (ed). Rilpivirine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 03/01/2018.

Edurant Tablet, Film Coated (Janssen Products, LP). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 03/01/2018.

Joint Formulary Committee. Rilpivirine. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 03/01/2018.

McEvoy GK, Snow EK, Miller J et al (eds). Rilpivirine Hydrochloride. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 03/01/2018.