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Acrivastine

Zhishang Bio Acrivastine CAS 87848-99-5

CAS:87848-99-5 | C22H24N2O2 |MW:348.44 | EINECS NO:*

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Port: Shanghai Port, Qingdao Port

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Acrivastine
Acrivastine
Acrivastine

Describe

Acrivastine, a second generation antihistamine drug, has a molecular formula of C 2 2H 2 4N 2 O 2, and a weight molecular of 348.45g/mol.

Acrivastine is a member of the class of acrylic acids derivatives. It has a stronger H1 receptor selectivity, lower central nervous inhibition and does not cause drowsiness.

Acrivastine comes as a white powder or off-white powder. It is slightly soluble (but not easily) in water, and is easily soluble (but not very readily) in organic solvents like methanol and alcohol. The synthesis of acrivastine usually begins with p-methylbenzaldehyde, followed by pyrrolidine and multiple reactions, such as condensation and cyclization.

Acrivastine must meet international standards for pharmacopoeia, control all relevant substances, residual solvents and microbial levels to ensure safety and efficacy of the formulation.

Acrivastine, in clinical practice is used primarily to relieve allergic symptoms like allergic rhinitis or urticaria. Acrivastine’s fast onset and short-term duration of action make it ideal for patients with symptoms that need relief quickly and without sedative effects.

Acrivastine is relatively safe for liver function due to its low metabolism dependence. However, patients with severe kidney insufficiency may need to adjust their dosage.

Acrivastine Basic information
Product Name:Acrivastine
Synonyms:(e)-3-[6-[(e)-1-(4-methylphenyl)-3-pyrrolidin-1-ylprop-1-enyl]pyridin-2-yl]prop-2-enoic acid;ACRIVASTINE;Acrivastin;
CAS:87848-99-5
MF:C22H24N2O2
MW:348.44
EINECS: 
Product Categories:API
Mol File:87848-99-5.mol
Acrivastine Chemical Properties
Melting point 222° (dec)
Boiling point 555.1±50.0 °C(Predicted)
density 1.170±0.06 g/cm3(Predicted)
storage temp. 2-8°C
solubility DMSO: >2mg/mL (warmed)
form powder
pka1.99±0.10(Predicted)
color white to beige
Stability:Light Sensitive

Application

Acrivastine belongs to the second-generation of antihistamines and is a selective antagonist H1 receptor.

Acrivastine is a chemical with a high affinity to H1 receptors. Its high polarity makes it difficult to cross the blood-brain barriers. Acrivastine is less likely to cause side effects in the central nervous system compared to first-generation antihistamines.

Acrivastine works primarily by blocking histamine binding to H1 receptors. This inhibits allergic reactions caused by histamine, such as capillary dilation or increased vascular permeability.

Acrivastine, from a pharmacokinetic point of view, is rapidly absorbed following oral administration. It takes effect within 30 minutes, and reaches peak blood concentration in 1-1.5 hours.

Acrivastine’s plasma protein binding is approximately 50%, and its elimination half-life is about 1.5-2 hours. The liver is only responsible for a small portion of the metabolized drug. It is excreted primarily in its original form. It is a metabolic characteristic that requires a dose adjustment for patients with renal failure, but it has comparatively little impact on the liver’s function.

Acrivastine has a duration of 8-12 hours. Therefore, the usual clinical dosage is once every 8 hour.

Acrivastine has a wide range of clinical applications. It is used to treat allergic diseases such as allergic rhinitis and urticaria.

Acrivastine is effective in relieving the symptoms of seasonal allergy rhinitis. This includes nasal itching, runny nose, and sneezing. Acrivastine is difficult to cross the blood-brain barriers, so it does not cause central inhibitory symptoms like drowsiness, even at recommended doses. This makes it ideal for patients who must maintain alertness.

Acrivastine is less likely to interact with other drugs, so it does not require any special adjustments in dosage when combined with erythromycin or ketoconazole.

Acrivastine is relatively safe and has a low incidence of side effects. Mild dry mouth, headaches, and gastrointestinal discomfort are common adverse reactions, but severe reactions are rare. Contraindications include those who are allergic to this drug or have severe renal failure.

Acrivastine is a relatively mild central nervous system drug, but individual reactions can still occur. It is important to monitor the patient during the initial stages of treatment.

Acrivastine is a safe and fast-acting antihistamine that has a significant role in treating allergic symptoms.

Related References

Manufacturer of Acrivastine

Company Info

Zhishang Bio company in China that exports chemicals, Cosmetic raw materials, and Intermediates for over 70 countries now.
 
And a range of 50,000 products with the best quality and competitive price to meet your different purchasing needs.
 
The company integrates research and development, production, and trade, with a modern production base, advanced testing equipment, and an experienced technical team to ensure that products reach industry-leading levels in purity, stability, and environmental friendliness.

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