 Home > Encyclopedia > Cetirizine hydrochloride

Cetirizine hydrochloride

Cetirizine hydrochloride structure

CAS No:
83881-52-1
Formula:
C21H25ClN2O3.2ClH
Chemical Name:
Cetirizine hydrochloride
Synonyms:
Acetic acid,2-[2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]-,hydrochloride (1:2);Acetic acid,[2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]-,dihydrochloride;Cetirizine hydrochloride;UCB-P 071;Cetirizine dihydrochloride;Alercet;Cetrine;Cetrizet;Cistamine;Histazine;Nosemin;Alerid;Cesta;Ryzen;Sancotec;Selitex;Triz;Virlix;Zeran;Zirtin;Zyrtec;Zyrzine;Alerlisin;Formistin;Zirtek;Zyrlex;Reactine;Riztec;P 071;Zirtec;Cetrak;Cetiriz;Tomazine;Epirizine;Histazine-1;2-(2-[4-[(4-Chlorophenyl)(phenyl)methyl]piperazin-1-yl]ethoxy)acetic acid dihydrochloride;130018-82-5
Categories:
Active Pharmaceutical Ingredients > Antiallergic Drugs

Description

Cetirizine 2Hcl, a second-generation antihistamine, is a major metabolite of hydroxyzine, and a racemic selective H1 receptor inverse agonist used in the treatment of allergies, hay fever, angioedema, and urticaria. IC50 value:Target: Histamine H1 receptorCetirizine crosses the blood-brain barrier only slightly, reducing the sedative side-effect common with older antihistamines. It has also been shown to inhibit eosinophil chemotaxis and LTB4 release. At a dosage of 20 mg, Boone et al. f

Cetirizine hydrochloride is a diarylmethane.|A potent second-generation histamine H1 antagonist that is effective in the treatment of allergic rhinitis, chronic urticaria, and pollen-induced asthma. Unlike many traditional antihistamines, it does not cause drowsiness or anticholinergic side effects.

Cetirizine hydrochloride Basic Attributes

Molecular Weight：

425.35

Exact Mass：

460.109

EC Number：

222-225-5

DSSTox ID：

DTXSID2044268

HScode：

2933599090

Characteristics

PSA：

XLogP3：

3.82600

Appearance：

white to beige

Density：

1.237 g/cm3

Melting Point：

225 °C

Boiling Point：

542.1ºC at 760 mmHg

Flash Point：

281.6ºC

Water Solubility：

soluble in water, DMSO, ethanol, and methanol.H2O: soluble 5 mg/mL, clear

Storage Conditions：

Desiccate at RT

Vapor Pressure：

2.98X10-11 mm Hg at 25 deg C (est)

Collision Cross Section：

198.3 Å² [M+H]+ [CCS Type: TW, Method: calibrated with polyalanine and drug standards]

Safety Information

Packing level：

III

Hazard category：

6.1(b)

Transport codes：

3249

wgk germany：

hazard class code：

22-36/37/38

safety instructions：

26-36

RTECS Number：

AG0977500

Marks：

Xn,Xi

Precautionary statement(s)：

P301 + P312 + P330

Hazard Statements：

H302

GHS Classification：

|Warning|H302 (99.37%): Harmful if swallowed [Warning Acute toxicity, oral]|P264, P270, P301+P312, P330, and P501|Aggregated GHS information provided by 158 companies from 13 notifications to the ECHA C&L Inventory.

Drug Information

MeSH：

A class of non-sedating drugs that bind to but do not activate histamine receptors (DRUG INVERSE AGONISM), thereby blocking the actions of histamine or histamine agonists. These antihistamines represent a heterogenous group of compounds with differing chemical structures, adverse effects, distribution, and metabolism. Compared to the early (first generation) antihistamines, these non-sedating antihistamines have greater receptor specificity, lower penetration of BLOOD-BRAIN BARRIER, and are less likely to cause drowsiness or psychomotor impairment. (See all compounds classified as Histamine H1 Antagonists, Non-Sedating.)|Agents that are used to treat allergic reactions. Most of these drugs act by preventing the release of inflammatory mediators or inhibiting the actions of released mediators on their target cells. (From AMA Drug Evaluations Annual, 1994, p475) (See all compounds classified as Anti-Allergic Agents.)

MeSH Entry Terms：

(2-(4-((4-Chlorophenyl)phenylmethyl)-1-piperazinyl)ethoxy)acetic Acid

Cetirizine hydrochloride Use and Manufacturing

Methods of Manufacturing

2-{2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]-ethoxy}acetic acid was suspended in acetone (150 ml), heated to 50 °C and concentrated hydrochloric acid (6.2 ml, 0.078 mol) was added with vigorous stirring. The resulting almost clear solution was stirred at room temperature for 2 hours after which a fine white precipitate of 2-{2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy}acetic acid dihydrochloride had formed. The solution was filtered, washed with acetone (50 ml) and dried in vacuo leaving 13.8 g (87.9 percent) of 2-{2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy}acetic acid dihydrochloride. M. P. 224-226 °C.By taking the above-described embodiments of the aldehyde intermediate obtained crude product 4.1 g, was dissolved in 50 ml of methylene chloride and 5 ml of DMSO was added potassium dihydrogen phosphate buffer at PH 4.0 phosphate and dubbed between 5 ~ 20 ml, the reaction temperature was controlled at between 5 to 10 degrees, slowly added 30percent hydrogen peroxide 2.1 g; after completion of the reaction at 25 degrees 8 hours; HPLC monitoring after completion of the reaction, 30 ml of methylene chloride, standing layered organic layer was washed with deionized water, 100 g of saturated brine and 100 g, respectively, and then dried over anhydrous sodium sulfate, filtered, and the solvent was evaporated viscous liquid non hydrochloride cetirizine. HPLC purity of 94.8percent.The non-hydrochloride cetirizine was dissolved in 20 ml Butanone And heated to 60 degrees, Continuous access to dry hydrogen chloride gas, The solid was recrystallized by known method to obtain 3.7 g of cetirizine hydrochloride. Yield: 81percent and HPLC purity greater than 99percent.

Uses

Antihistaminic Mainly used for allergic diseases of the respiratory system, skin and eyes

Use Classification：

Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients

Computed Properties

Molecular Weight:461.8
Hydrogen Bond Donor Count:3
Hydrogen Bond Acceptor Count:5
Rotatable Bond Count:8
Exact Mass:460.108726
Monoisotopic Mass:460.108726
Topological Polar Surface Area:53
Heavy Atom Count:29
Complexity:443
Undefined Atom Stereocenter Count:1
Covalently-Bonded Unit Count:3
Compound Is Canonicalized:Yes

Drug Function and Efficacy

Antihistamines

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Cetirizine Hydrochloride Drops
Specifications	10ml:100mg

Cetirizine Hydrochloride Drops
Ingredients	The main ingredient of this product is cetirizine hydrochloride. Chemical name: (±)-2-[2-[4-(4-chlorophenyl)benzyl]-1-piperazinyl]ethoxy]acetic acid dihydrochloride Molecular weight: C21H27Cl3N2O3·2HCl
Indication	No interactions with other drugs have been reported, but caution should be exercised when taking sedatives at the same time.
Specifications	10mg/ml

Cetirizine Hydrochloride Orally Disintegrating Tablets
Ingredients	Cetirizine hydrochloride.
Indication	No interactions with other drugs have been reported, but caution should be exercised when taking sedatives at the same time.
Specifications	10mg
Manufacturer	Shandong FANGMING Pharmaceutical Group Co., Ltd.

See More Related Drugs

Registered Holders

THINQ PHARMA-CRO LTD

United States
Active
GLOCHEM INDUSTRIES PRIVATE LTD

United States
Active
ORBION PHARMACEUTICALS PRIVATE LTD

United States
Active

See More Registered Holders

Recommended Suppliers of Cetirizine hydrochloride

Shandong zhishang chemical Co.,Ltd Contact Supplier

CN
5 YRS

Business licensed Certified factory

Manufactory Supplier of Dichloromethane,Linocaine hydrochloride

Cetirizine dihydrochloride 99.9% prower aly-83881-52-1 lk

CAS No.: 83881-52-1

Grade: Pharmaceutical Grade

Content: 99.9%

Inquiry
SHANDONG LOOK CHEMICAL CO.,LTD Contact Supplier

CN
5 YRS

Business licensed Certified factory

Manufactory Supplier of Agrochemicals,Daily Chemicals,Catalysts & Chemical Auxiliary Agents,Extract,Inorganic Chemicals,Organic Intermediate,Pigment & Dyestuff,Polymer,Flavour & Fragrance,Basic Organic Chemicals,Pharmaceutical

Factory price and High quantity Cetirizine hydrochloride 99% power

CAS No.: 83881-52-1

Grade: Pharmaceutical Grade

Content: 99%

Inquiry
Kindchem Co., Ltd Contact Supplier

CN
4 YRS

Business licensed

Trader Supplier of API OLED Organic intermediate

Cetirizine dihydrochloride Kindchem

CAS No.: 83881-52-1

Inquiry
Shandong Airuike Chemical Co., Ltd. Contact Supplier

CN
3 YRS

Business licensed

Trader Supplier of api,Intermediates,Organic Chemistry,Inorganic Chemistry,Daily Chemicals,Cosmetic Raw Materals,CATALYST AND AUXILIARY,FLAVORS AND FRAGRANCES,Chemical Pesticides,ADDITIVE

Factory price and Higher quantity Cetirizine hydrochloride 99% power

CAS No.: 83881-52-1

Grade: Pharmaceutical Grade

Content: 0%

Inquiry
Blue Sky Biotech Contact Supplier

CN
1 YR

Business licensed

Trader Supplier of Ivermectin,PP405,Aniracetam,toltrazuril,Reta,Enclomiphene citrate,Dihexa peptide,GHK-Cu,NNMTCL

China factory supply directly Cetirizine hcl powder 99% CAS 83881-52-1 Pharma grade

Unit Price: $40-50 /KG FOB

CAS No.: 83881-52-1

Grade: Pharmaceutical Grade

Content: 99%

Inquiry