Rupatadine


Generic Medicine Info
Indications and Dosage
Oral
Allergic rhinitis, Urticaria
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.
Administration
May be taken with or without food.
Special Precautions
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.
Adverse Reactions
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.
Drug Interactions
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).
Food Interaction
Increased systemic exposure with grapefruit juice; avoid concomitant administration. May increase the CNS depressant effect of alcohol.
Action
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.
Chemical Structure

Chemical Structure Image
Rupatadine

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 133017, Rupatadine. https://pubchem.ncbi.nlm.nih.gov/compound/Rupatadine. Accessed Nov. 24, 2020.

Storage
Store between 15-30°C. Tab: Protect from light.
ATC Classification
R06AX28 - rupatadine ; Belongs to the class of other antihistamines for systemic use.
References
Anon. Rupatadine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 30/10/2020.

Buckingham R (ed). Rupatadine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 30/10/2020.

Joint Formulary Committee. Rupatadine. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 30/10/2020.

Prosp Rupafin Singapur (Hyphens Pharma Pte Ltd). MIMS Singapore. http://www.mims.com/singapore. Accessed 30/10/2020.

Rupafin 10 mg Tablets (Hyphens Pharma Pte Ltd). MIMS Singapore. http://www.mims.com/singapore. Accessed 30/10/2020.

Rupafin 10 mg Tablets (J. Uriach y Compañia., S.A.). MHRA. https://products.mhra.gov.uk/. Accessed 30/10/2020.

Rupatadine 1 mg/mL Oral Solution (J. Uriach y Compañia, S.A.). MHRA. https://products.mhra.gov.uk/. Accessed 30/10/2020.

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