Adult: 10 mg once daily. Child: 2-11 years ≥10-<25 kg: 2.5 mg once daily; ≥25 kg: 5 mg once daily. ≥12 years Same as adult dose.
May be taken with or without food.
Patient with known QTc interval prolongation, predisposition to arrhythmias (e.g. uncorrected hypokalaemia, bradycardia, acute myocardial ischaemia). Hepatic and renal impairment. Children and elderly. Pregnancy and lactation. Avoid concomitant use with strong CYP3A4 inhibitors.
Significant: Rarely, QTc interval prolongation, torsade de pointes, hypersensitivity reactions (e.g. anaphylaxis, angioedema). Blood and lymphatic system disorders: Eosinophilia, neutropenia (children). Gastrointestinal disorders: Vomiting, dry mouth, oropharyngeal pain, dry throat, abdominal pain, diarrhoea, dyspepsia, nausea, constipation. General disorders and administration site conditions: Fatigue, asthenia, irritability, thirst; night sweats (children). Investigations: Increased ALT, AST, blood creatine phosphokinase, weight; abnormal LFT. Metabolism and nutrition disorders: Increased appetite. Musculoskeletal, connective tissues, and bone disorders: Arthralgia, myalgia, back pain. Nervous system disorders: Somnolence, headache, dizziness, disturbance in attention. Respiratory, thoracic and mediastinal disorders: Cough, rhinitis, pharyngitis, nasal dryness, epistaxis, tonsillitis.
May increase the plasma concentrations of CYP3A4 substrates (e.g. simvastatin, lovastatin, midazolam) and CYP3A4 substrates with narrow therapeutic index (e.g. ciclosporin, tacrolimus, sirolimus, everolimus, cisapride). Increased plasma concentrations with CYP3A4 strong inhibitors (e.g. itraconazole, ketoconazole, voriconazole, posaconazole, HIV protease inhibitors, clarithromycin, nefazodone) and moderate inhibitors (e.g. erythromycin, fluconazole, diltiazem).
Increased systemic exposure with grapefruit juice; avoid concomitant administration. May increase the CNS depressant effect of alcohol.
Description: Rupatadine is a long-acting, 2nd generation antihistamine that possesses selective peripheral H1 receptor and platelet activating factor (PAF) antagonistic activities. At high concentrations, it was noted to prevent the degranulation of mast cells and release of cytokines, specifically TNFα in human mast cells and monocytes. Onset: 1-2 hours. Duration: Antihistaminic activity: 24 hours. Pharmacokinetics: Absorption: Rapidly absorbed from the gastrointestinal tract. Time to peak plasma concentration: 0.75-1 hour. Distribution: Volume of distribution: 9,799 L. Plasma protein binding: 98.5-99%. Metabolism: Almost completely metabolised in the liver via oxidation, N-dealkylation, and hydroxylation mainly by CYP3A4 isoenzyme, and to a lesser extent by CYP2C9, CYP2C19, and CYP2D6, into active metabolites, desloratadine and its hydroxylated derivatives. Excretion: Via faeces (60.9%); urine (34.6%). Elimination half-life: 4.04-6.07 hours.