Product Information
Registration Status: ActiveRUPAFIN ORAL SOLUTION 1mg/ml is approved to be sold in Singapore with effective from 2015-09-10. It is marketed by HYPHENS PHARMA PTE LTD, with the registration number of SIN14868P.
This product contains Rupatadine 1mg/ml in the form of SOLUTION. It is approved for ORAL use.
This product is manufactured by ITALFARMACO in SPAIN.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Description
Rupatadine is a dual histamine H1 receptor and platelet activating factor receptor antagonist that is used for symptomatic relief in seasonal and perennial rhinitis as well as chronic spontaneous urticaria. It was approved for marketing in Canada under the tradename Rupall and comes in tablet formulation for adult use and liquid formulation for pediatric use.
Indication
For the symptomatic relief of nasal and non-nasal symptoms of seasonal allergic rhinitis and perennial allergic rhinitis in patients 2 years of age and older [FDA Label]. Also used for the symptomatic relief of chronic spontaneous urticaria in patients 2 years of age and older.
Mechanism of Action
Rupatadine is a dual histamine H1 receptor and platelet activating (PAF) receptor antagonist [A19779] [FDA Label]. During allergic response mast cells undergo degranulation, releasing histamine and other substances [A19780]. Histamine acts on H1 receptors to produce symptoms of nasal blockage, rhinorhea, itching, and swelling. PAF is produced from phospholipids cleaved by phospholipase A2. It acts to produce vascular leakage which contributes to rhinorhea and nasal blockage. By blocking both the H1 receptor and PAF receptor, rupatidine prevents these mediators from exerting their effects and so reduces the severity of allergic symptoms.
Pharmacokinetics
- Absorption
- Rupatidine is rapidly absorbed with a Tmax of 1 h [FDA Label]. Administration with a high fat meal increases exposure by 23% and increases Tmax to 2 h.
- Distribution
- The apparent volume of distribution is 9799 L [FDA Label].
- Metabolism
- Rupatadine is metabolized by oxidation mediated primarily by CYP3A4 [FDA Label]. CYP2C9, CYP2C19, and CYP2D6 are also involved to a lesser extent. The metabolites desloratidine and hydroxylated forms of desloratidine retain some activity as H1 receptor antagonists.
- Elimination
Clearance
Systemic clearance is 1556.2 L/h in young adults and 798.2 L/h in geriatric patients [FDA Label].
Active Ingredient/Synonyms
Rupatadine | Rupatadine |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.