Rilpivirine

Registered South African indications: 

• HIV-1 infection

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients
• Coadministration with other non-nucleoside reverse transcriptase inhibitors (NNRTIs), such as delavirdine, efavirenz, etravirine, or nevirapine
• Combination with carbamazepine, oxcarbazepine, phenobarbital, phenytoin, or dexamethasone (except as a single-dose treatment) due to significant decreases in rilpivirine plasma concentrations caused by the induction of CYP3A enzymes, potentially leading to loss of therapeutic effect
• Combination with rifabutin, rifampicin, or rifapentine as these are potent inducers of CYP3A enzymes, which may cause significant decreases in rilpivirine plasma concentrations and result in loss of therapeutic effect
• Concomitant use of rilpivirine with products containing St. John’s Wort (Hypericum perforatum) is contraindicated because it may cause significant decreases in rilpivirine plasma concentrations, resulting in loss of therapeutic effect
• Proton-pump inhibitors (PPIs) such as lanzoprazole, omeprazole, rabeprazole, pantoprazole, and esomeprazole should not be administered with rilpivirine, as this may result in significant decreases in rilpivirine plasma concentration due to gastric pH increase, leading to a loss of therapeutic effect

Cautions

• Breastfeeding
• Severe renal impairment
• Moderate to severe hepatic impairment
• Elderly
• QTc prolongation
• Autoimmune disorders (Graves' disease and autoimmune hepatitis)
• Co-administered with medications with a known risk of Torsade de Pointes
• Galactose intolerance
• Lapp lactase deficiency 
• Glucose-galactose malabsorption

Forms avail. in SA and covered in this monograph: fct

HIV infection (additional agent required)
- In antiretroviral treatment-naïve adult patients with a viral load ≤ 100 000 HIV-1 RNA copies/ml

• Oral (fct): 25mg, dly with food

See additional prescribing points

Not established for use in children below 18 years

Consult HIV/infectious disease specialists prior to any decisions related to ARV regimen termination/switch

Pregnancy

• Safe: The use of rilpivirine may be considered during pregnancy (only if the potential benefit justifies the potential risk)
• A moderate amount of data on pregnant women (between 300-1000 pregnancy outcomes) indicate no malformative or feto/neonatal toxicity of rilpivirine
• Lower exposures of rilpivirine were observed during pregnancy, therefore viral load should be monitored closely
• Animal studies do not indicate reproductive toxicity
   

Breastfeeding

• Caution; not recommended
• It is not known whether rilpivirine is excreted in human milk. Rilpivirine is excreted in the milk of rats
• Because of both the potential for HIV transmission and the potential for adverse reactions in breastfed infants, mothers should be instructed not to breast-feed if they are receiving rilpivirine

Renal Impairment

• Severe: Caution; no dose adjustment recommended

Hepatic Impairment

• Moderate: Caution; no dose adjustment recommended 
• Severe: Caution; no information available

Elderly

• Caution; no dose adjustment recommended

Porphyria Information

• Probably not porphyrinogenic (PNP)

Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders

• Insomnia
• Abnormal dreams
• Depression
• Sleep disorders
• Headache
• Dizziness
• Somnolence
• Fatigue

Gastrointestinal Disorders

• Nausea and vomiting
• Increased pancreatic amylase
• Abdominal pain
• Increased lipase
• Abdominal discomfort
• Dry mouth

Hepatobiliary Disorders

• Increased transaminases
• Increased bilirubin

Endocrine and Metabolic Disorders

• Increased total cholesterol (fasted)
• Increased low density lipid cholesterol (fasted)
• Decreased appetite
• Increased triglycerides (fasted)

Skin and Subcutaneous Tissue Disorders

• Rash

Immune, Blood and Lymphatic System Disorders

• Decreased white blood cell count
• Decreased haemoglobin
• Decreased platelet count
• Immune reactivation syndrome

• CYP3A inducers
• CYP3A inhibitors
• Agents that increase gastric pH 
• Didanosine
• Other non-nucleoside reverse transcriptase inhibitor
• Delavirdine
• Efavirenz
• Etravirine
• Nevirapine
• Darunavir/ ritonavir
• Lopinavir/ ritonavir
• Carbamazepine
• Oxcarbazepine
• Phenobarbital
• Phenytoin
• Rifabutin
• Rifampicin
• Rifapentine
• Clarithromycin
• Erythromycin
• Dexamethasone (except as a single-dose treatment)
• Proton-pump inhibitors (PPIs)
• Omeprazole
• Lansoprazole
• Rabeprazole
• Pantoprazole
• Esomeprazole
• Famotidine
• Cimetidine
• Nizatidine
• Ranitidine
• Antacids 
• Methadone
• Dabigatran etexilate
• St John's wort 
• QT prolonging agents

• Viral load 
• Cholesterol
• Triglycerides
• Hepatic function

Missed dose

• Within 12 hours of scheduled dose: Take as soon as possible and take next dose at regular scheduled time
• More than 12 hours after regular scheduled time: Omit the missed dose and resume usual dosing schedule

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Therapy should be initiated by a physician experienced in the management of HIV infection

Rilpivirine is a diarylpyrimidine non-nucleoside reverse transcriptase inhibitor of HIV. Rilpivirine activity is mediated by non-competitive inhibition of HIV-1 reverse transcriptase. Rilpivirine does not inhibit the human cellular DNA polymerases α, β and γ.

Film-coated tablet 25mg

• Edurant (Janssen Pharmaceutica) originator