Acrivastine

Acrivastine

Cat Number
API0232173
CAS Number
87848-99-5

For research use only. We do not supply to patients.

For pharmaceutical-grade products or other inquiries, please contact our experts.

CAS Number
87848-99-5
EINECS
618-080-6
Storage
Store at room temperature
Synonyms
Semprex; Acrivastina; BW-825C; Acrivastinum; DTXSID6022555
Molecular Formula
C22H24N2O2
Molecular Weight
348.4
Smiles
CC1=CC=C(C=C1)/C(=C\\CN2CCCC2)/C3=CC=CC(=N3)/C=C/C(=O)O
Appearance
White to pale cream crystalline powder
Melting Point
222°C (dec.)
Boiling Point
555.1±50.0°C (Predicted)
Relative Density
1.170±0.06 (Predicted)
General Description
Acrivastine is a second-generation, short-acting histamine H1 receptor antagonist belonging to the propylamine class, structurally related to triprolidine. Its structure features a pyridine ring, a propenyl group, and a carboxylic acid moiety, which confers zwitterionic properties.
Mechanism of Action
Acrivastine acts as a selective, competitive antagonist at peripheral H1 receptors, blocking histamine-induced vasodilation, increased vascular permeability, and sensory nerve stimulation. Its carboxylic acid group limits penetration across the blood-brain barrier, significantly reducing central nervous system effects. The drug has a rapid onset but a relatively short duration of action, requiring more frequent dosing compared to other second-generation antihistamines.
Application
Acrivastine is indicated for the symptomatic relief of seasonal allergic rhinitis and chronic idiopathic urticaria, effectively reducing sneezing, rhinorrhea, and pruritus. Its fast onset makes it suitable for on-demand use. The drug is approved in combination with pseudoephedrine and is generally well-tolerated, with drowsiness occurring at a slightly higher rate than with cetirizine or loratadine.

Does Acrivastine require protection from light during long-term storage?

Yes, it is photosensitive. UV exposure can cause photodegradation of the acrylic acid side chain. Store in light-resistant containers, preferably amber glass.

What is the recommended storage temperature for Acrivastine?

Store at controlled room temperature (15-25°C). Avoid excessive heat above 30°C, which can accelerate oxidation and degradation.

Is Acrivastine hygroscopic, and how is this managed?

It is slightly hygroscopic. Under high humidity (>70% RH), it may absorb moisture and clump. Storage in tightly sealed containers with desiccant is recommended.

How is the impurity acrivastine E-isomer (geometric isomer) monitored?

This geometric isomer is specifically quantified using a stability-indicating HPLC method, ensuring it remains within pharmacopoeial limits.
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