Rupatadine Fumarate
- CAS No.
- 182349-12-8
- Chemical Name:
- Rupatadine Fumarate
- Synonyms
- Ralif;Rupax FuMarate;Rupafin FuMarate;Pafinur FuMarate;UR12592 Fumarate;Rinialer FuMarate;UR 12592 Fumarate;UR-12592 Fumarate;Rupatadin Fumarate;RUPATADINE FUMARATE
- CBNumber:
- CB42131159
- Molecular Formula:
- C26H26ClN3.C4H4O4
- Molecular Weight:
- 532.03
- MOL File:
- 182349-12-8.mol
- Modify Date:
- 2024/5/8 14:18:51
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|---|---|
| Signal word | Warning |
| Hazard statements | H302 |
| Precautionary statements | P264-P270-P301+P312-P501 |
Rupatadine Fumarate price More Price(2)
Rupatadine Fumarate Chemical Properties,Uses,Production
Description
Rupatadine fumarate, a novel antiallergic drug with a dual mechanism of action, was introduced in Spain as an oral treatment for perennial and seasonal rhinitis. Rupatadine acts as non-sedating histamine H1 receptor antagonist and plateletactivating factor (PAF) antagonist. Its Kiapp i values against [3H]WEB-2086 binding to rabbit platelet membrane PAF receptors and [3H]pyralimine binding to guinea pig cerebellum membrane H1 histamine receptors are 0.55 and 0.10 μM, respectively. It has a rapid onset of action, with patients experiencing relief of symptoms within 2 h, and its long duration of action (＞24 h) permits once-daily dosing. Rupatidine is prepared in a 6-step convergent synthesis, with the key steps involving the Grignard reaction of a N-alkyl-4-chloropiperdine with a benzocycloheptapyridinone intermediate, followed by dehydration. Rupatadine is rapidly absorbed after oral administration. The time to reach maximum plasma concentration is 0.75–1 h and the mean half-life in healthy volunteers is ～6 h. It is extensively metabolized, mainly by CYP3A4, and the major elimination route for the drug is biliary excretion. In comparative clinical trials, rupatadine 10 mg once daily was as effective as certizine 10 mg in short-term studies (2–4 weeks duration), but provided a better profile of CNS side effects. In comparison with ebastine 10 mg and loratadine 10 mg, rupatadine showed a superior relief of rhinitis symptoms at the same dose. Rupatadine was well tolerated in clinical trials and, at the recommended daily dose of 10 mg, was free of the sedative effects associated with first-generation antihistamines. In addition, there were no significant differences in the overall incidence of adverse events in rupatidine-treated patients and those treated with placebo or standard reference products.
Chemical Properties
Rupatadine fumarate is white or off-white color crystalline powder, odorless, and mildly bitter flavor, slightly draws moistly, in methanol, dissolves, almost insoluble in water, slightly molten in 0.1mol/L hydrochloric acid solution.
Uses
8-Chloro-6,11-dihydro-11-[1-[(5-methyl-3-pyridyl)methyl]-4-piperidylidene]-5H-benzo[5,6]cyclohepta[1,2-b]pyridine fumarate is a dual antagonist of histamine H1 and platelet-activating factor receptors. Rupatadine is used as an antihistaminic.
Rupatadine Fumarate Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | Inquiry |
|---|---|---|---|---|---|
| Cadila Pharmaceuticals Ltd | +91-7069076657 +91-7069076657 | Ahmedabad, India | 54 | 58 | Inquiry |
| Siddhivinayakchemicals | +91-912225190111 +91-9819773074 | Mumbai, India | 42 | 58 | Inquiry |
| Vadivarhe Speciality Chemicals Limited | +91-9028832204 +91-9028832204 | Maharashtra, India | 38 | 58 | Inquiry |
| Hetero Drugs Limited | +91-4023704923 +91-4023704923 | Telangana, India | 296 | 58 | Inquiry |
| Honour Lab Limited | +919845977466 | Telangana, India | 164 | 58 | Inquiry |
| Anlon Healthcare Pvt Ltd | +91-2812562538 +91-7069690081 | Gujarat, India | 54 | 58 | Inquiry |
| Precise Biopharma Pvt Ltd | +91-2267828600 +91-2267828600 | Maharashtra, India | 46 | 58 | Inquiry |
| Dolphin Chem | +91-9377962666 +91-9377962666 | Gujarat, India | 10 | 58 | Inquiry |
| FDC Limited | +912226782653 | Mumbai, India | 30 | 58 | Inquiry |
| Ralington Pharma | +91-7948911722 +91-9687771722 | Gujarat, India | 1350 | 58 | Inquiry |
| Supplier | Advantage |
|---|---|
| Cadila Pharmaceuticals Ltd | 58 |
| Siddhivinayakchemicals | 58 |
| Vadivarhe Speciality Chemicals Limited | 58 |
| Hetero Drugs Limited | 58 |
| Honour Lab Limited | 58 |
| Anlon Healthcare Pvt Ltd | 58 |
| Precise Biopharma Pvt Ltd | 58 |
| Dolphin Chem | 58 |
| FDC Limited | 58 |
| Ralington Pharma | 58 |
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