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Cetirizine dihydrochloride

CAS No.
83881-52-1
Chemical Name:
Cetirizine dihydrochloride
Synonyms
CETIRIZINE DIHYDROCHLORIDE;CETIRIZINE HCL;CETIRIZINE HYDROCHLORIDE;Triz;CETIRIZINE 2HCL;ZYRTEC;CETIRIZINE DI HCL;Certirizine;CETIRIZIN DIHYDROCHLORIDE;Cesta
CBNumber:
CB6135030
Molecular Formula:
C21H26Cl2N2O3
Molecular Weight:
425.35
MDL Number:
MFCD00941428
MOL File:
83881-52-1.mol
MSDS File:
SDS
TDS File:
TDS
Last updated:2026-04-24 12:01:10
Product description Number Pack Size Price
Cetirizine for peak identification European Pharmacopoeia (EP) Reference Standard Y0001197 1.01 mg $175
Cetirizine dihydrochloride solution 1.0?mg/mL in acetonitrile: water (9:1) (as free base), ampule of 1?mL, certified reference material, Cerilliant? C-158 1mL $143
Cetirizine dihydrochloride European Pharmacopoeia (EP) Reference Standard C0980650 100 mg $175
Cetirizine hydrochloride British Pharmacopoeia (BP) Reference Standard BP837 100MG $254
Cetirizine impurity standard British Pharmacopoeia (BP) Reference Standard BP1081 50MG $263
More product size

Cetirizine dihydrochloride Properties

Melting point 110-115°C
storage temp. 2-8°C
solubility H2O: soluble5mg/mL, clear
form powder
color white to beige
Water Solubility Soluble in water, DMSO, ethanol, and methanol.
Merck 14,2022
BCS Class 1,3
Stability Hygroscopic
InChI InChI=1S/C21H25ClN2O3.ClH/c22-19-8-6-18(7-9-19)21(17-4-2-1-3-5-17)24-12-10-23(11-13-24)14-15-27-16-20(25)26;/h1-9,21H,10-16H2,(H,25,26);1H
InChIKey PGLIUCLTXOYQMV-UHFFFAOYSA-N
SMILES O=C(COCCN1CCN(C(C2=CC=CC=C2)C2=CC=C(Cl)C=C2)CC1)O.[H]Cl
CAS DataBase Reference 83881-52-1(CAS DataBase Reference)
FDA UNII 64O047KTOA
EPA Substance Registry System Acetic acid, 2-[2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]-, hydrochloride (1:2) (83881-52-1)
UNSPSC Code 41116107
NACRES NA.25

Pharmacokinetic data

Protein binding 93%
Excreted unchanged in urine 50-60%
Volume of distribution 0.45(L/kg)
Biological half-life 8-10 / 20

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS07
Signal word  Warning
Hazard statements  H302
Precautionary statements  P264-P270-P301+P312+P330-P501
PPE dust mask type N95 (US), Eyeshields, Faceshields, Gloves
Hazard Codes  Xn,Xi
Risk Statements  22-36/37/38
Safety Statements  26-36
RIDADR  3249
WGK Germany  3
RTECS  AG0977500
HazardClass  6.1(b)
PackingGroup  III
HS Code  29339900
Storage Class 11 - Combustible Solids
Hazard Classifications Acute Tox. 4 Oral
NFPA 704
0
3 0

Cetirizine dihydrochloride price More Price(61)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich Y0001197 Cetirizine for peak identification European Pharmacopoeia (EP) Reference Standard 83881-52-1 1.01 mg $175 2026-04-30 Buy
Sigma-Aldrich C-158 Cetirizine dihydrochloride solution 1.0?mg/mL in acetonitrile: water (9:1) (as free base), ampule of 1?mL, certified reference material, Cerilliant? 83881-52-1 1mL $143 2026-04-30 Buy
Sigma-Aldrich C0980650 Cetirizine dihydrochloride European Pharmacopoeia (EP) Reference Standard 83881-52-1 100 mg $175 2026-04-30 Buy
Sigma-Aldrich BP837 Cetirizine hydrochloride British Pharmacopoeia (BP) Reference Standard 83881-52-1 100MG $254 2026-04-30 Buy
Sigma-Aldrich BP1081 Cetirizine impurity standard British Pharmacopoeia (BP) Reference Standard 83881-52-1 50MG $263 2026-04-30 Buy
Product number Packaging Price Buy
Y0001197 1.01 mg $175 Buy
C-158 1mL $143 Buy
C0980650 100 mg $175 Buy
BP837 100MG $254 Buy
BP1081 50MG $263 Buy

Cetirizine dihydrochloride Chemical Properties,Uses,Production

Description

Cetirizine hydrochloride(83881-52-1) is an orally-active and selective histamine (H1)-receptor antagonist. It is a second-generation antihistamine and a human metabolite of hydroxyzine. Three important features of cetirizine are: a high specificity fort he H1-receptor; a low need for metabolism, and the existence of non-H1-dependent activities on cells involved in the pathogenesis of allergy.
Cetirizine is used to treat seasonal allergic rhinitis (SAR), perennial allergic rhinitis, useful in treating urticaria and atopic dermatitis. Cetirizine possesses also mild anti-inflammatory effects.

References

[1] E. J. Corey and Christopher J. Helal, Catalytic Enantioselective Synthesis of the Second-Generation Histamine Antagonist Cetirizine Hydrochloride, Tetrahedron Letters, 1996, vol. 37, 4837-4840
[2] Jay M. Portnoy and Chitra Dinakar, Review of cetirizine hydrochloride for the treatment of allergic disorders, Journal of Expert Opinion on Pharmacotherapy, 2004, vol. 5, 125-135

Description

Cetirizine hydrochloride is a once-daily, non-sedating antihistamine useful in the treatment of allergic rhinitis, urticaria and conjunctivitis. It is reported to be more effective than most other agents in this category such as terfenadine and astemizole.

Chemical Properties

Cetirizine Hydrochloride occurs as a white crystalline powder or crystalline solid. It is very soluble in water, and slightly soluble in ethanol (99.5). It dissolves in 0.1 mol/L hydrochloric acid TS. A solution of Cetirizine Hydrochloride (1 in 10) shows no optical rotation.

Originator

UCB (Belgium)

Application

Cetirizine Hydrochloride may be used as a pharmaceutical reference standard for the determination of the analyte in pharmaceutical formulations by various chromatography techniques.

Uses

Cetirizine hydrochloride is a nonsedating type histamine H1-receptor antagonist. A major metabolite of Hydroxyzine. Pharmacological activity resides primarily in the (R)-isomer. It is Cetirizine is an antihistamine medicine 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.

Definition

ChEBI: Cetirizine hydrochloride is a diarylmethane.

Indications

Cetirizine HCl (Zyrtec) is the carboxylic acid metabolite of hydroxyzine. It is a selective, peripheral H1 receptor antagonist. It is a long-lasting antihistamine. It does not appear to have the same adverse cardiac effects as the other nonsedating H1 antihistamines; however, additional data are required. Indicated for allergic rhinitis and chronic urticaria.

Manufacturing Process

Preparation of 2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]- ethoxy]acetic acid (cetirizine).
To a mixture of 50 g 2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]- ethanol and 225 ml of tert-butanol at 45°C under a nitrogen was added 21 g tert-BuOK. The temperature was raised to 75-80°C and the mixture was kept at this temperature. After 45 min was added 11 g sodium chloracetate; after 1.5 hour was added 5.2 g tert-BuOK; after 2 hours was added 5.64 g sodium chloracetate; after 2.5 hours was added 1.9 g tert-BuOK; after 3 hours was added 1.9 g sodium chloracetate; after 3.5 hours was added 0.8 g tert-BuOK; and after 4 hours was added 1.13 g sodium chloracetate. Then about 150 ml tert-butanol was distilled of, 190 ml of water was added and the distillation of tert-butanol was continued until the temperature of the vapour reaches 100°C. To the reaction mixture was added 60 ml of water and 8 ml concentrated hydrochloric acid to pH 8. Unreacted 2-[4-[(4-chlorophenyl) phenylmethyl]-1-piperazinyl]-ethanol was extracted with diethyl ether. The aqueous phase was acidified to pH 5 by addition of hydrochloric acid and extracted with dichloromethane (200 ml x 3). The extract was dried over MgSO4, filtered and concentrated in a rotary evaporator. An obtained oil was allowed to crystallize by addition of 150 ml of 2-butanone, yields of 2-[4-[(4- chlorophenyl)phenylmethyl]-1-piperazinyl]-ethoxy]acetic acid 55.5%, M.P. 146-148°C.
32.7 g 2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]-ethoxy]acetic acid was suspended in a mixture of 125 ml of water and 13.8 ml 37% aqueous hydrochloric acid. The mixture was concentrated in a rotary evaporator. An obtained oil was allowed to crystallize by addition of 245 ml of 2-butanone, yields of 2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]-ethoxy]acetic acid dihydrochloride 88%, M.P. 228.22°C.

brand name

Zyrtec (Pfizer).

Therapeutic Function

Antihistaminic; Antiallergic

General Description

Cetirizine hydrochloride, a second generation antihistaminic drug, is one of the carboxylated metabolites of hydroxyzine that can typically bind to histamine H1 receptor. It is effective against diseases such as urticaria, angioedema, allergies and hay fever.

Biological Activity

Histamine H 1 receptor antagonist that displays selectivity over other receptors at concentrations up to 10 μ M. A non-sedating antihistamine that inhibits histamine release and eosinophil chemotaxis during secondary phase allergic response. Inhibits activation of eosinophils, neutrophils and monocytes in vivo .

Biochem/physiol Actions

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.

Side effects

There are many side effects of Cetirizine hydrochloride which can be classified into five levels including common side effects (10%), more common side effects (1%), rare side effects (0.1%), very rare side effects (0.01%) and other side effects.
Common side effects include: drowsiness, dizziness, headache, pharyngitis, rhinitis (children), diarrhoea (children), nausea, dry mouth, fatigue. More common side effects include: restlessness, paresthesia (tingling or numbness in the hands and feet), diarrhoea, stomach pain, pruritus (itching), rash, asthenia (unusual weakness), weakness.
Rare side effects include: hypersensitivity, aggression, confusion, depression, hallucinations, insomnia, convulsions, tachycardia (fast heartbeat), abnormal liver function, hives, oedema (swelling), weight gain. Very rare side effects: Thrombocytopenia (low platelet count), anaphylaxis, convulsions (uncontrolled body movements), gustatory disturbances (disturbances in taste or loss of taste), dyskinesia (dyskinesia (uncontrolled movements), dystonia (uncontrolled muscle spasms), syncope (fainting), ophthalmoplegia (uncontrolled circular movements of the eyes), angioedema (severe). allergic reaction that causes swelling of the face or throat), dysuria (pain when urinating), incontinence (bedwetting).
Other side effects include: increased appetite, suicidal thoughts, nightmares, amnesia, memory problems, dizziness (spinning sensation), inflammation of the liver, urinary retention (difficulty in urinating), pain in the joints, rash with pus-containing blisters, and severe itching after stopping the drug (pruritus).

Veterinary Drugs and Treatments

Cetirizine is a H1 receptor blocking antihistamine agent that may be useful for the adjunctive treatment of histamine-mediated pruritic conditions in dogs or cats.

Drug interactions

Potentially hazardous interactions with other drugs
Antivirals: concentration possibly increased by ritonavir.

Metabolism

Cetirizine does not undergo extensive first pass metabolism.
About two thirds of the dose is excreted unchanged in urine.

Dosage forms

5 to 10mg daily.

References

[1] Patent: EP1157016, 2003, B1. Location in patent: Page/Page column 5
[2] Patent: US2005/20608, 2005, A1. Location in patent: Page 5-6
[3] Patent: US2004/266787, 2004, A1. Location in patent: Page/Page column 6

83881-51-0
83881-52-1
Synthesis of Cetirizine dihydrochloride from Cetirizine
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View Lastest Price from Cetirizine dihydrochloride manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
Cetirizine hydrochloride pictures 2026-05-09 Cetirizine hydrochloride
83881-52-1
US $0.00-0.00 / kg 1kg 99%min 500kgs WUHAN FORTUNA CHEMICAL CO., LTD
Cetirizine hydrochloride pictures 2026-04-30 Cetirizine hydrochloride
83881-52-1
US $0.00 / kg 1kg 99 500 Xi an Biohorlden Industry Trade Co Ltd
Cetirizine hydrochloride pictures 2026-04-30 Cetirizine hydrochloride
83881-52-1
US $0.00 / kg 1kg 99% 888kgs Xi an Biohorlden Industry Trade Co Ltd

Cetirizine dihydrochloride Spectrum

(2-(4-((4-chlorophenyl)phenylmethyl)-1-piperazinyl)ethoxy)aceticaciddihydro 2-[2-[4-[(4-chlorophenyl)-phenyl-methyl]piperazin-1-yl]ethoxy]acetic acid dihydrochloride Cetirizine Hydrochloride (250 mg) Alercet Alerid Cesta Cetiriz Cetrak Cetrine Cetrizet CistaMine Epirizine Histazine-1 NoseMin Riztec Ryzen Sancotec Selitex Cetrizide 2-[4-(4-Chlorobenzhy (±)-2-[2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]-acetic acid,dihydrochloride Cetirazine dihydrochloride [2-[4-[(4-Chlorophenyl)-phenylmethyl]-1-piperazinyl]ethoxy]acetic Acid, Dihydrochloride CETIRZINE HYDROCHLORIDE 1-piperazinyl]ethoxy]-,dihydrochloride Acetic acid, [2-[4-[(4-chlorophenyl)phenylmethyl]- Virlix Zeran Zirtec Zirtin Zyrzine Cetrizine Hydrochloride EP Acetic acid,2-[2-[4-[(4-chlorophenyl)phenylMethyl]-1-piperazinyl]ethoxy]-, hydrochloride(1:2) Cetirizine for peak identification Cetirizine dihydrochloride solution 2-(2-{4-[(4-chlorophenyl)(phenyl)-methyl]piperazino}ethoxy)acetic acid dihydrochloride AKOS 92015 (2-(4-((4-chlorophenyl)phenylmethyl)-1-piperazinyl)ethoxy)-aceticacidihyd ucb-p071 Cetirizine dihydrochloride, 99%, a selective histamine H1 receptor antagonist Cetirizine mono hydrochloride Cetirizine dihydrochloride CRS Cetirizine Dihydrochloride > Cetirizine Hydrochloride/Cetirizine HCL Cetirizine dihydrochloride Solution Water/Acetonitrile,100μg/mL Cetirizine hydrochloride USP/EP/BP Cetirizine hydrochloride Impurities Cetirizine DiHCl (P071) Cetirizine for peak identification (Y0001197) Cetirizine hydrochlorideQ: What is Cetirizine hydrochloride Q: What is the CAS Number of Cetirizine hydrochloride Q: What is the storage condition of Cetirizine hydrochloride Q: What are the applications of Cetirizine hydrochloride Cetirizine Hydrochloride (1102929) 5-(and-6)-Carboxyfluorescein mixed isomers CETIRIZIN DIHYDROCHLORIDE CETIRIZINE DI HCL CETIRIZINE DIHYDROCHLORIDE Certirizine ZYRTEC CETIRIZINE HYDROCHLORIDE IP