Rupatadine

532.03

415.96

1312995-182-4

2AE8M83G3E

DTXSID00166534

R06AX28|R - Respiratory system

2933990090

29

0.8

off-white powder

1.233±0.06 g/cm3(Predicted)

136-137 °C @ Solvent: Toluene

586.4±50.0 °C(Predicted)

308.4±30.1 °C

1.646

9.83E-14mmHg at 25°C

|Warning|H315 (100%): Causes skin irritation [Warning Skin corrosion/irritation]|P261, P264, P271, P280, P302+P352, P304+P340, P305+P351+P338, P312, P321, P332+P313, P337+P313, P362, P403+P233, P405, and P501|The GHS information provided by 1 company from 1 notification to the ECHA C&L Inventory.

Rupatidine is 98.5-99.0% bound to human plasma proteins.

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. Also used for the symptomatic relief of chronic spontaneous urticaria in patients 2 years of age and older.|FDA Label

Rupatadine is an anti allergenic and acts to reduce allergic symptoms like urticaria, rhinorrhea, sneezing and itching.

Rupatidine is rapidly absorbed with a Tmax of 1 h. Administration with a high fat meal increases exposure by 23% and increases Tmax to 2 h.|The apparent volume of distribution is 9799 L.|Systemic clearance is 1556.2 L/h in young adults and 798.2 L/h in geriatric patients.

Rupatadine is metabolized by oxidation mediated primarily by CYP3A4. 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.|Rupatadine has known human metabolites that include Desloratadine.

The half life of elimination is 15.9 h in children 2-5 years old, 12.3 h in children 6-11 years old, 5.9 h in adults, and 8.7 h in geriatric patients.

Rupatadine is a dual histamine H1 receptor and platelet activating (PAF) receptor antagonist. During allergic response mast cells undergo degranulation, releasing histamine and other substances. 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.

8-chloro-6,11-dihydro-11-(1-((5-methyl-3-pyridinyl)methyl)-4-piperidinylidene)-5H-benzo(5,6)cyclohepta(1,2-b)pyridine