Adult: In combination with cabotegravir with or without oral lead-in treatment in patients weighing ≥35 kg, with a viral load of ≤50 copies/mL, on a stable antiretroviral regimen, and no history of resistance or treatment failure with either rilpivirine or cabotegravir: Initially, 900 mg as a single dose, given on the last day of oral lead-in therapy or on the last day of current regimen. Maintenance: 600 mg once monthly, to be given 1 month after the initial dose. Alternatively, Initially, 900 mg given on the last day of oral lead-in therapy or on the last day of current regimen, followed by 900 mg after 1 month. Maintenance: 900 mg every 2 months, to be given 2 months after the 2nd initiation inj. If patient plans to miss a scheduled inj by >7 days, use oral bridging therapy dosing in combination with cabotegravir. Dosing recommendations for missed dose may differ between monthly and every 2 months injection dosing (refer to local guidelines). Child: ≥12 years weighing ≥35 kg: Same as adult dose.
Oral HIV-1 infection
Adult: Doses are expressed in terms of rilpivirine base (25 mg rilpivirine base is equivalent to 27.5 mg rilpivirine hydrochloride). In combination with other antiretroviral agents for treatment-naïve patients weighing ≥25 kg and with a viral load of ≤100,000 copies/mL at baseline: As a film-coated tab: 25 mg once daily. As oral lead-in for tolerability assessment prior to initiation of inj dose in combination with cabotegravir in patients weighing ≥35 kg, with a viral load of ≤50 copies/mL, and on a stable antiretroviral regimen with no history of resistance or treatment failure with either rilpivirine or cabotegravir: As a film-coated tab: 25 mg once daily for approx 1 month (at least 28 days). The last oral dose should be administered on the same day as the 1st inj dose. As oral bridging therapy in combination with cabotegravir in patients weighing ≥35 kg who plan to miss a scheduled inj by >7 days: As a film-coated tab: 25 mg once daily for up to 2 months. The 1st oral dose should be administered at approx the same time as the scheduled missed inj dose and continued until the day the inj is restarted. Child: As combination therapy with other antiretroviral agents in patients with a viral load of ≤100,000 copies/mL at baseline: ≥2 years As a dispersible tab: Patients weighing 14-<20 kg: 12.5 mg once daily; 20-<25 kg: 15 mg once daily. As film-coated tab: Patients weighing ≥25 kg: 25 mg once daily. As oral lead-in for tolerability assessment prior to initiation of inj dose in combination with cabotegravir in patients with a viral load of ≤50 copies/mL, and on a stable antiretroviral regimen with no history of resistance or treatment failure with either rilpivirine or cabotegravir: ≥12 years weighing ≥35 kg: As a film-coated tab: 25 mg once daily for approx 1 month (at least 28 days). The last oral dose should be administered on the same day as the 1st inj dose. As oral bridging therapy in combination with cabotegravir in patients who plan to miss a scheduled inj by >7 days: ≥12 years weighing ≥35 kg: As a film-coated tab: 25 mg once daily for up to 2 months. The 1st oral dose should be administered at approx the same time as the scheduled missed inj dose and continued until the day the inj is restarted.
What are the brands available for Rilpivirine in Malaysia?
Edurant
Special Patient Group
Patients taking rifabutin: As a film-coated tab: 50 mg once daily. Decrease dose to 25 mg once daily if rifabutin is discontinued.
Administration
Rilpivirine Should be taken with food.
Contraindications
Hypersensitivity. Concomitant use with anticonvulsants (e.g. carbamazepine, oxcarbazepine, phenobarbital, phenytoin); antimycobacterials (e.g. rifampicin, rifapentine, rifabutin [if used via IM administration]); PPIs (if used via oral administration [e.g. omeprazole, esomeprazole, lansoprazole, pantoprazole, rabeprazole]); systemic glucocorticoid dexamethasone (except when used as a single dose); St. John's wort. Lactation.
Special Precautions
Patient with depressive disorder, hepatitis B or C. Not indicated for use in patients with CD4 count <200 cells/mm3 and viral load >100,000 copies/mL. Oral dispersible tab is not interchangeable with film-coated tab. Severe renal and moderate to severe hepatic impairment. Children and elderly. Pregnancy.
Adverse Reactions
Significant: Depression, QT interval prolongation (in supratherapeutic doses), hepatotoxicity, immune reconstitution syndrome, hypersensitivity and severe skin reactions (e.g. severe rash, drug reaction with eosinophilia and systemic symptoms). Gastrointestinal disorders: Nausea, vomiting, dry mouth, abdominal pain. IM: Flatulence, diarrhoea. General disorders and administration site conditions: Fatigue. IM: Malaise, pyrexia, asthenia, inj site reactions. Investigations: Increased serum ALT and AST, serum bilirubin, serum creatinine, LDL cholesterol (fasted), triglycerides (fasted), pancreatic amylase, lipase, and weight (IM). Metabolism and nutrition disorders: Hypercholesterolaemia, decreased appetite (oral). Musculoskeletal and connective tissue disorders: Myalgia (IM). Nervous system disorders: Headache, dizziness. Psychiatric disorders: Insomnia, somnolence, abnormal dreams, dysphoria, altered mood. Skin and subcutaneous tissue disorders: Rash.
IM/PO: Z (Generally not recommended unless clinically required.)
Patient Counseling Information
This drug may cause dizziness, drowsiness, or somnolence, if affected, do not drive or operate machinery.
Monitoring Parameters
Monitor cholesterol, triglycerides, and LFTs (prior and during therapy). Assess for signs or symptoms of depressive disorder (e.g. mood changes, suicide tendencies, depression); hypersensitivity reactions, infection (e.g. fever, chills, cough, wheezing); severe skin rash.
Management: Symptomatic and supportive treatment. Monitor clinical status, vital signs, and ECG (particularly QT interval).
Drug Interactions
Decreased plasma concentration with CYP3A4 inducers (e.g. carbamazepine, rifampicin, dexamethasone [multiple-dose treatment], St. John’s wort) or with agents that increase gastric pH (e.g. calcium carbonate, famotidine, omeprazole). Increased plasma concentration with CYP3A4 inhibitors (e.g. clarithromycin, erythromycin, ketoconazole, fluconazole).
Food Interaction
Increased absorption with normal- to high-calorie meal. Decreased serum concentration with St. John's wort.
Action
Description: Overview: Rilpivirine, a diarylpyrimidine non-nucleoside reverse transcriptase inhibitor (NNRTI), is an antiviral agent. Mechanism of Action: Rilpivirine exerts activity against HIV-1 by binding to reverse transcriptase, thereby inhibiting both RNA-dependent and DNA-dependent DNA polymerase activities and preventing viral replication. Pharmacodynamics: Rilpivirine has demonstrated activity against certain isolates of HIV-1 resistant to other NNRTIs. However, rilpivirine-resistant strains have been identified in cell culture and have also emerged during clinical use. Rilpivirine can adapt to mutations in HIV-1 reverse transcriptase due to its structural flexibility. Rapid development of viral resistance occurs when rilpivirine is used as monotherapy; therefore, it is used in combination with other antiretroviral agents. Cross-resistance has been observed among commercially available NNRTIs, particularly in patients who have virologic failure while receiving a regimen containing rilpivirine. Suboptimal adherence (e.g. underdosing, incorrect dosing of a given formulation) with the regimen may lead to the development of viral resistance to rilpivirine. Pharmacokinetics: Absorption: Food, particularly normal- to high-calorie meal, increases absorption. Time to peak plasma concentration: 4-5 hours (oral). Distribution: Enter breast milk. Plasma protein binding: 99.7%, mainly to albumin. Metabolism: Metabolised in the liver by CYP3A4 via oxidation. Excretion: Via faeces (85%; approx 25% as unchanged drug); urine (approx 6%; <1% as unchanged drug). Elimination half-life: Approx 50 hours.
Chemical Structure
Rilpivirine Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 6451164, Rilpivirine. https://pubchem.ncbi.nlm.nih.gov/compound/Rilpivirine. Accessed Jan. 29, 2026.
Storage
Oral: Tab/Dispersible tab for oral susp: Store between 15-30℃. Protect from light and moisture.
Intramuscular: Susp for inj: Store between 2-8℃. Do not freeze. Upon removal from refrigerator to room temperature, use within 6 hours.
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