CETIRIZINE DIHYDROCHLORIDE

CETIRIZINE DIHYDROCHLORIDE
PRODUCT IDENTIFICATION
CAS NO.	83881-51-0 (Base) 83881-52-1 (Dihydrochloride)
EINECS NO.
FORMULA	C₂₁H₂₃ClN₂O₃·2HCl
MOL WT.	461.82
H.S. CODE	2933.59.2100
TOXICITY	Oral Rat LD50: 365mg/kg
SYNONYMS	(1S.2S)-2-Methylamino-1-phenyl-1-propanol dichloride;
(2-(4-((4-Chlorophenyl)phenylmethyl)-1-piperazinyl)ethoxy)acetic acid dichloride;
SMILES	N1([C@@H](c2ccc(Cl)cc2)c2ccccc2)CCN(CCOCC(O)=O)CC1.Cl.Cl
CLASSIFICATION	Antihistaminic, Anti-allergic agent, Histamine H1 antagonist
EXTRA NOTES	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 is an orally active and selective H1-receptor antagonist. Antihistaminic; Piperazines. Non-sedating type histamine H1-receptor antagonist; major metabolite of hydroxyzine. Pharmacological activity resides primarily in the (R)-isomer.
PHYSICAL AND CHEMICAL PROPERTIES
PHYSICAL STATE	white to off-white crystalline powder
MELTING POINT
BOILING POINT
SPECIFIC GRAVITY
SOLUBILITY IN WATER	Soluble (Insoluble in acetone )
pH	1.2 - 1.8 (5% sol.)
VAPOR DENSITY
AUTOIGNITION
NFPA RATINGS
REFRACTIVE INDEX
FLASH POINT
STABILITY	Stable under ordinary conditions. Hygroscopic.
EXTERNAL LINKS & GENERAL DESCRIPTION
Wikipedia Linking http://www.drugbank.ca/ Mechanism of action: Cetirizine competes with histamine for binding at H₁-receptor sites on the effector cell surface, resulting in suppression of histaminic edema, flare, and pruritus. The low incidence of sedation can be attributed to reduced penetration of cetirizine into the CNS as a result of the less lipophilic carboxyl group on the ethylamine side chain. Google Scholar Search Drug Information Portal (U.S. National Library of Medicine) - Cetirizine http://www.nlm.nih.gov/ Cetirizine is used to temporarily relieve the symptoms of hay fever (allergy to pollen, dust, or other substances in the air) and allergy to other substances (such as dust mites, animal dander, cockroaches, and molds). These symptoms include sneezing; runny nose; itchy, red, watery eyes; and itchy nose or throat. Cetirizine is also used to treat itching and redness caused by hives. However, cetirizine does not prevent hives or other allergic skin reactions. Cetirizine is in a class of medications called antihistamines. It works by blocking the action of histamine, a substance in the body that causes allergic symptoms. Cetirizine is also available in combination with pseudoephedrine (Sudafed, others). This monograph only includes information about the use of cetirizine alone. If you are taking the cetirizine and pseudoephedrine combination product, read the information on the package label or ask your doctor or pharmacist for more information. Local: Cetirizine is a selective H₁-receptor antagonist used to treat allergic rhinitis and chronic idiopathic urticaria, and as a treatment adjunct in asthma. It is a racemic mixture of levo- and dextro-form, but levo-form is active. Chemically it is described as (1S.2S)-2-methylamino-1-phenyl-1-propanol. The hydrochloride salt of cetirizine is a white powder freely soluble in water, practically insoluble in acetone and dichloromethane; administered orally.
SALES SPECIFICATION
BIBLIOGRAPHY	EP2000
APPEARANCE	white to off-white crystalline powder
ASSAY	99.0 - 100.5% (on dry basis)
LOSS ON DRYING	0.5% max
SULFATED ASH	0.2% max
HEAVY METALS	10ppm max
INDIVIDUAL IMPURITY	0.2% max (total impurity: 0.5% max)
TRANSPORTATION
PACKING
HAZARD CLASS	Not regulated
UN NO.
SAFETY INFORMATION
GHS
SIGNAL WORD	Warning
PICTOGRAMS
HAZARD STATEMENTS	H302 Harmful if swallowed
PRECAUTIONARY STATEMENTS
EC DIRECTIVES
HAZARD CODES	Xn Harmful
RISK PHRASES	22 Harmful if swallowed
SAFETY PHRASES
PRICE INFORMATION