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Chemistry

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Also known as: 83881-51-0, Cetirizina, Cetirizin, Virlix, Cetirizinum, Zirtek
Molecular Formula
C21H25ClN2O3
Molecular Weight
388.9  g/mol
InChI Key
ZKLPARSLTMPFCP-UHFFFAOYSA-N
FDA UNII
YO7261ME24

Cetirizine
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 is a Histamine-1 Receptor Antagonist. The mechanism of action of cetirizine is as a Histamine H1 Receptor Antagonist.
1 2D Structure

Cetirizine

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
2-[2-[4-[(4-chlorophenyl)-phenylmethyl]piperazin-1-yl]ethoxy]acetic acid
2.1.2 InChI
InChI=1S/C21H25ClN2O3/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)
2.1.3 InChI Key
ZKLPARSLTMPFCP-UHFFFAOYSA-N
2.1.4 Canonical SMILES
C1CN(CCN1CCOCC(=O)O)C(C2=CC=CC=C2)C3=CC=C(C=C3)Cl
2.2 Other Identifiers
2.2.1 UNII
YO7261ME24
2.3 Synonyms
2.3.1 MeSH Synonyms

1. (2-(4-((4-chlorophenyl)phenylmethyl)-1-piperazinyl)ethoxy)acetic Acid

2. Alerlisin

3. Aller-tec

4. Cetalerg

5. Ceterifug

6. Ceti Tad

7. Ceti-puren

8. Cetiderm

9. Cetidura

10. Cetil Von Ct

11. Cetilich

12. Cetirigamma

13. Cetirizin Al

14. Cetirizin Azu

15. Cetirizin Basics

16. Cetirizine Dihydrochloride

17. Cetirlan

18. Dihydrochloride, Cetirizine

19. P 071

20. P-071

21. P071

22. Reactine

23. Virlix

24. Voltric

25. Zetir

26. Zirtek

27. Zyrtec

2.3.2 Depositor-Supplied Synonyms

1. 83881-51-0

2. Cetirizina

3. Cetirizin

4. Virlix

5. Cetirizinum

6. Zirtek

7. Cetiderm

8. 2-(2-{4-[(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl}ethoxy)acetic Acid

9. Cetirizine Hydrochloride

10. Ac-170

11. Cetirizine (inn)

12. 2-[2-[4-[(4-chlorophenyl)-phenylmethyl]piperazin-1-yl]ethoxy]acetic Acid

13. Cetryn

14. Setir

15. Ziptek

16. Chembl1000

17. Chebi:3561

18. 1133210-23-7

19. Cetirizinum [latin]

20. (r)-cetirizine (dihydrochloride)

21. Hitrizin Film Tablet

22. Cetirizina [spanish]

23. Yo7261me24

24. (2-(4-((4-chlorophenyl)phenylmethyl)-1-piperazinyl)ethoxy)acetic Acid

25. (2-{4-[(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl}ethoxy)acetic Acid

26. 2-[2-[4-[(4-chlorophenyl)-phenyl-methyl]piperazin-1-yl]ethoxy]acetic Acid Dihydrichloride

27. P071

28. Zyrlex

29. Cetirizine [inn]

30. 2-(2-(4-((4-chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)acetic Acid

31. Acetic Acid, [2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]-

32. Cetirizine [inn:ban]

33. Xarlin

34. Acetic Acid, (2-(4-((4-chlorophenyl)phenylmethyl)-1-piperazinyl)ethoxy)-

35. Cetiderm (tn)

36. Levocetirizine (dihydrochloride)

37. Irizine

38. Benaday

39. Humex

40. Unii-yo7261me24

41. Cetrizine Dihcl

42. [2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]acetic Acid

43. Hsdb 7739

44. 2-[2-[4-[(r)-(4-chlorophenyl)-phenylmethyl]piperazin-1-yl]ethoxy]acetic Acid

45. Cetirizine [mi]

46. Prestwick0_000503

47. Prestwick1_000503

48. Prestwick2_000503

49. Prestwick3_000503

50. Cetirizine [hsdb]

51. Cetirizine [vandf]

52. Schembl4176

53. Timtec1_002075

54. Cetirizine [who-dd]

55. Bspbio_000425

56. Bspbio_002302

57. Spbio_002346

58. Bpbio1_000469

59. Gtpl1222

60. Dtxsid4022787

61. Bdbm22890

62. Hms1539o07

63. Hms3259d06

64. Hms3370i19

65. Hms3393n10

66. Amy22576

67. Bcp08787

68. Bcp28477

69. Bbl009968

70. Cet83881-51-0

71. Stk711108

72. (r)-cetirizine-[d4] Dihydrochloride

73. [(2-{4-[(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl}ethyl)oxy]acetic Acid

74. 2-[2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]acetic Acid

75. Acetic Acid, 2-[2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]-

76. Akos003589059

77. Akos021729457

78. Ac-5545

79. Cs-0886

80. Db00341

81. Nc00696

82. Sdccgsbi-0206838.p002

83. Ncgc00167781-01

84. Ncgc00167781-02

85. Ncgc00167781-03

86. Ncgc00167781-04

87. Ncgc00167781-07

88. Ncgc00167781-12

89. Ncgc00167781-18

90. As-77105

91. Hy-17042

92. Sbi-0206838.p001

93. Db-049948

94. Ft-0603001

95. Ft-0664488

96. En300-52521

97. 81c510

98. C07778

99. D07662

100. E75781

101. L000655

102. Q423075

103. J-005737

104. Brd-a42571354-300-05-4

105. Brd-a42571354-300-07-0

106. Z1182332250

107. [2-[4-[(4-chlorophenyl)-phenyl Methyl]-1-piperazinyl] Ethoxy] Acetic Acid

108. [2-[4-[(4-chlorophenyl)phenylmethyl] 1-piperazinyl]-ethoxy] Acetic Acid

109. [2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]-ethoxy]acetic Acid

110. 2-(2-(4-((4-chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)aceticacid

111. 2-(2-{4-[(4-chlorophenyl)(phenyl)methyl]piperazino}ethoxy)acetic Acid

112. (+/-)-(2-(4-(p-chloro-a-phenylbenzyl)-1-piperazinyl)ethoxy)acetic Acid

113. Acetic Acid, (2-(4-((4-chlorophenyl)phenylmethyl)-1-piperazinyl)ethoxy)-, (+/-)-

2.4 Create Date
2005-03-25
3 Chemical and Physical Properties
Molecular Weight 388.9 g/mol
Molecular Formula C21H25ClN2O3
XLogP31.7
Hydrogen Bond Donor Count1
Hydrogen Bond Acceptor Count5
Rotatable Bond Count8
Exact Mass388.1553704 g/mol
Monoisotopic Mass388.1553704 g/mol
Topological Polar Surface Area53 Ų
Heavy Atom Count27
Formal Charge0
Complexity443
Isotope Atom Count0
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count1
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently Bonded Unit Count1
4 Drug and Medication Information
4.1 Drug Information
1 of 2  
Drug NameZyrtec
PubMed HealthKetotifen
Drug ClassesMast Cell Stabilizer, Ophthalmologic Agent, Piperidine
Active IngredientCetirizine hydrochloride
Dosage FormSyrup
RouteOral
Strength5mg/5ml
Market StatusPrescription
CompanyMcneil Consumer

2 of 2  
Drug NameZyrtec
PubMed HealthKetotifen
Drug ClassesMast Cell Stabilizer, Ophthalmologic Agent, Piperidine
Active IngredientCetirizine hydrochloride
Dosage FormSyrup
RouteOral
Strength5mg/5ml
Market StatusPrescription
CompanyMcneil Consumer

4.2 Therapeutic Uses

Cetirizine alone or in fixed combination with pseudoephedrine hydrochloride is used for self-medication to provide symptomatic relief of seasonal allergic rhinitis (e.g., hay fever) or other upper respiratory allergies. Cetirizine alone or in fixed combination with pseudoephedrine hydrochloride also is used for the symptomatic treatment of perennial allergic rhinitis. It is recommended that the fixed combination generally be used only when both the antihistamine and nasal decongestant activity of the combination preparation are needed concurrently. /Included in US product label/

American Society of Health System Pharmacists; AHFS Drug Information 2009. Bethesda, MD. (2009), p. 26


Cetirizine is used for self-medication to provide symptomatic relief of pruritus associated with chronic idiopathic urticaria (e.g., hives). /Included in US product label/

American Society of Health System Pharmacists; AHFS Drug Information 2009. Bethesda, MD. (2009), p. 26


MEDICATION (VET): The efficacy of antihistamines for the treatment of pruritus is highly variable. The most commonly used antihistamines include ... cetirizine hydrochloride ... . /Cetirizine hydrochloride/

Kahn, C.M. (Ed.); The Merck Veterinary Manual 9th ed. Merck & Co. Whitehouse Station, NJ. 2005, p. 677


4.3 Drug Warning

In a controlled study of 1 week's duration in patients 6-11 months of age, those receiving cetirizine exhibited greater irritability/fussiness than those receiving placebo. In a controlled study in patients 12 months of age and older, insomnia occurred more frequently with cetirizine than with placebo (9 vs 5.3%, respectively). In those who received 5 mg or more daily, fatigue occurred in 3.6 or 1.3% and malaise in 3.5 or 1.8% of those receiving cetirizine or placebo, respectively.

American Society of Health System Pharmacists; AHFS Drug Information 2009. Bethesda, MD. (2009), p. 27-8


Fatigue or dizziness occurred in 5.9 or 2%, respectively, of patients 12 years of age and older receiving cetirizine, whereas these effects occurred in 2.6 or 1.2%, respectively, of patients receiving placebo. Headache was reported in more than 2% of patients 12 years of age and older receiving the drug; however, headache occurred more frequently in patients receiving placebo. In clinical trials in patients 6-11 years of age, headache occurred in 11, 14, or 12.3% of patients receiving 5-mg doses, 10-mg doses, or placebo, respectively. Abnormal coordination, ataxia, confusion, abnormal thinking, agitation, amnesia, anxiety, depersonalization, depression, emotional lability, euphoria, impaired concentration, insomnia, sleep disorders, nervousness, paroniria, dysphonia, asthenia, malaise, pain, hyperesthesia, hypoesthesia, hyperkinesia, hypertonia, migraine headache, myelitis, paralysis, paresthesia, ptosis, syncope, tremor, twitching, and vertigo have been reported in less than 2% of patients 12 years of age and older and children 6-11 years of age receiving cetirizine hydrochloride; however, a causal relationship to the drug has not been established. Aggressive reaction, seizures, hallucinations, suicidal ideation, and suicide have been reported rarely during postmarketing surveillance.

American Society of Health System Pharmacists; AHFS Drug Information 2009. Bethesda, MD. (2009), p. 27


The most frequent adverse effect in patients 12 years of age and older reported during cetirizine therapy is somnolence, occurring in 11, 14, or 6% of patients receiving 5-mg doses, 10-mg doses, or placebo, respectively. Overall, somnolence has been reported in 13.7 or 6.3% of patients receiving cetirizine or placebo, respectively. In addition, in clinical trials in patients 6-11 years of age, somnolence occurred in 1.9, 4.2, or 1.3% of patients receiving 5-mg doses, 10-mg doses, or placebo, respectively. Discontinuance of therapy because of somnolence has been reported in 1 or 0.6% of patients receiving cetirizine or placebo, respectively.1 3 In patients 6-24 months of age, somnolence occurred with essentially the same frequency in those who received cetirizine versus placebo.

American Society of Health System Pharmacists; AHFS Drug Information 2009. Bethesda, MD. (2009), p. 27


Adverse effects reported in 1% or more of patients 12 years of age and older with seasonal allergic rhinitis who received extended-release tablets of cetirizine hydrochloride in fixed combination with pseudoephedrine hydrochloride (Zyrtec-D) included insomnia, dry mouth, fatigue, somnolence, pharyngitis, epistaxis, accidental injury, dizziness, and sinusitis.

American Society of Health System Pharmacists; AHFS Drug Information 2009. Bethesda, MD. (2009), p. 27


For more Drug Warnings (Complete) data for Cetirizine (31 total), please visit the HSDB record page.


4.4 Drug Indication

**Seasonal Allergic Rhinitis**: Indicated for the relief of symptoms associated with seasonal allergic rhinitis caused by allergens such as ragweed, grass and tree pollens in adults and children 2 years of age and above. Symptoms treated effectively include sneezing, rhinorrhea, nasal pruritus, ocular pruritus, tearing, and redness of the eyes. **Perennial allergic rhinitis**: This drug is indicated for the relief of symptoms associated with perennial allergic rhinitis due to allergens including dust mites, animal dander, and molds in adults and children 6 months of age and older. Symptoms treated effectively include sneezing, rhinorrhea, postnasal discharge, nasal pruritus, ocular pruritus, and tearing. **Chronic urticaria**: Cetirizine is indicated for the treatment of the uncomplicated skin manifestations of chronic idiopathic urticaria in adults and children 6 months of age and older. It markedly reduces the occurrence, severity, and duration of hives and significantly reduces pruritus.


FDA Label


5 Pharmacology and Biochemistry
5.1 Pharmacology

**General effects and respiratory effects** Cetirizine, the active metabolite of the piperazine H1-receptor antagonist hydroxyzine, minimizes or eliminates the symptoms of chronic idiopathic urticaria, perennial allergic rhinitis, seasonal allergic rhinitis, allergic asthma, physical urticaria, and atopic dermatitis. The clinical efficacy of cetirizine for allergic respiratory diseases has been well established in numerous trials. **Effects on urticaria/anti-inflammatory effects** It has anti-inflammatory properties that may play a role in asthma management. There is evidence that cetirizine improves symptoms of urticaria. Marked clinical inhibition of a wheal and flare response occurs in infants, children as well as adults within 20 minutes of one oral dose and lasts for 24 h. Concomitant use of cetirizine reduces the duration and dose of topical anti-inflammatory formulas used for the treatment of atopic dermatitis.


5.2 MeSH Pharmacological Classification

Anti-Allergic Agents

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.)


Histamine H1 Antagonists, Non-Sedating

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.)


5.3 FDA Pharmacological Classification
5.3.1 Active Moiety
CETIRIZINE
5.3.2 FDA UNII
YO7261ME24
5.3.3 Pharmacological Classes
Histamine-1 Receptor Antagonist [EPC]; Histamine H1 Receptor Antagonists [MoA]
5.4 ATC Code

R06AE07

S76 | LUXPHARMA | Pharmaceuticals Marketed in Luxembourg | Pharmaceuticals marketed in Luxembourg, as published by d'Gesondheetskeess (CNS, la caisse nationale de sante, www.cns.lu), mapped by name to structures using CompTox by R. Singh et al. (in prep.). List downloaded from https://cns.public.lu/en/legislations/textes-coordonnes/liste-med-comm.html. Dataset DOI:10.5281/zenodo.4587355


R - Respiratory system

R06 - Antihistamines for systemic use

R06A - Antihistamines for systemic use

R06AE - Piperazine derivatives

R06AE07 - Cetirizine


S - Sensory organs

S01 - Ophthalmologicals

S01G - Decongestants and antiallergics

S01GX - Other antiallergics

S01GX12 - Cetirizine


5.5 Absorption, Distribution and Excretion

Absorption

Cetirizine was rapidly absorbed with a time to maximum concentration (Tmax) of about 1 hour after oral administration of tablets or syrup formulation in adult volunteers. Bioavailability was found to be similar between the tablet and syrup dosage forms. When healthy study volunteers were given several doses of cetirizine (10 mg tablets once daily for 10 days), a mean peak plasma concentration (Cmax) of 311 ng/mL was measured. **Effect of food on absorption** Food had no effect on cetirizine exposure (AUC), however, Tmax was delayed by 1.7 hours and Cmax was decreased by 23% in the fed state.


Route of Elimination

Mainly eliminated in the urine,. Between 70 85% of an orally administered dose can be found in the urine and 10 13% in the feces.


Volume of Distribution

Apparent volume of distribution: 0.44 +/- 0.19 L/kg.


Clearance

Apparent total body clearance: approximately 53 mL/min. Cetirizine is mainly eliminated by the kidneys,. Dose adjustment is required for patients with moderate to severe renal impairment and in patients on hemodialysis.


A mass balance study in 6 healthy male volunteers indicated that 70% of the administered radioactivity was recovered in the urine and 10% in the feces. Approximately 50% of the radioactivity was identified in the urine as unchanged drug. Most of the rapid increase in peak plasma radioactivity was associated with parent drug, suggesting a low degree of first-pass metabolism. Cetirizine is metabolized to a limited extent by oxidative O-dealkylation to a metabolite with negligible antihistaminic activity. The enzyme or enzymes responsible for this metabolism have not been identified.

US Natl Inst Health; DailyMed. Current Medication Information for Zyrtec - cetirizine hydrochloride (May 2006). Available from, as of July 2, 2009 https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?id=2115


The mean plasma protein binding of cetirizine is 93%, independent of concentration in the range of 25-1000 ng/mL, which includes the therapeutic plasma levels observed.

US Natl Inst Health; DailyMed. Current Medication Information for Zyrtec - cetirizine hydrochloride (May 2006). Available from, as of July 2, 2009 https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?id=2115


Cetirizine was rapidly absorbed with a time to maximum concentration (Tmax) of approximately 1 hour following oral administration of tablets, chewable tablets or syrup in adults. Comparable bioavailability was found between the tablet and syrup dosage forms. Comparable bioavailability was also found between the Zyrtec tablet and the Zyrtec chewable tablet taken with or without water. When healthy volunteers were administered multiple doses of cetirizine (10 mg tablets once daily for 10 days), a mean peak plasma concentration (Cmax) of 311 ng/mL was observed. No accumulation was observed. Cetirizine pharmacokinetics were linear for oral doses ranging from 5 to 60 mg. Food had no effect on the extent of exposure (AUC) of the cetirizine tablet or chewable tablet, but Tmax was delayed by 1.7 hours and 2.8 hours respectively, and Cmax was decreased by 23% and 37%, respectively in the presence of food.

US Natl Inst Health; DailyMed. Current Medication Information for Zyrtec - cetirizine hydrochloride (May 2006). Available from, as of July 2, 2009 https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?id=2115


When pediatric patients aged 7 to 12 years received a single, 5-mg oral cetirizine capsule, the mean Cmax was 275 ng/mL. Based on cross-study comparisons, the weight-normalized, apparent total body clearance was 33% greater and the elimination half-life was 33% shorter in this pediatric population than in adults. In pediatric patients aged 2 to 5 years who received 5 mg of cetirizine, the mean Cmax was 660 ng/mL. Based on cross-study comparisons, the weight-normalized apparent total body clearance was 81 to 111% greater and the elimination half-life was 33 to 41% shorter in this pediatric population than in adults. In pediatric patients aged 6 to 23 months who received a single dose of 0.25 mg/kg cetirizine oral solution (mean dose 2.3 mg), the mean Cmax was 390 ng/mL. Based on cross-study comparisons, the weight-normalized, apparent total body clearance was 304% greater and the elimination half-life was 63% shorter in this pediatric population compared to adults. The average AUC(0-t) in children 6 months to <2 years of age receiving the maximum dose of cetirizine solution (2.5 mg twice a day) is expected to be two-fold higher than that observed in adults receiving a dose of 10 mg cetirizine tablets once a day.

US Natl Inst Health; DailyMed. Current Medication Information for Zyrtec - cetirizine hydrochloride (May 2006). Available from, as of July 2, 2009 https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?id=2115


For more Absorption, Distribution and Excretion (Complete) data for Cetirizine (7 total), please visit the HSDB record page.


5.6 Metabolism/Metabolites

A mass balance clinical trial comprised of 6 healthy male study volunteers showed that 70% of the administered radioactivity was measured in the urine and 10% in the feces after cetirizine administration. About 50% of the radioactivity was measured in the urine as unchanged cetirizine. Most of the rapid increase in peak plasma radioactivity was related to the parent drug, implying a low level of first pass metabolism. This prevents potential interactions of cetirizine with drugs interacting with hepatic cytochrome enzymes. Cetirizine is metabolized partially by oxidative O-dealkylation to a metabolite with insignificant antihistaminic activity. The enzyme or enzymes responsible for this step in cetirizine metabolism have not yet been identified.


A mass balance study in 6 healthy male volunteers indicated that 70% of the administered radioactivity was recovered in the urine and 10% in the feces. Approximately 50% of the radioactivity was identified in the urine as unchanged drug. Most of the rapid increase in peak plasma radioactivity was associated with parent drug, suggesting a low degree of first-pass metabolism. Cetirizine is metabolized to a limited extent by oxidative O-dealkylation to a metabolite with negligible antihistaminic activity. The enzyme or enzymes responsible for this metabolism have not been identified.

US Natl Inst Health; DailyMed. Current Medication Information for Zyrtec - cetirizine hydrochloride (May 2006). Available from, as of July 2, 2009 https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?id=2115


Pharmacokinetic parameters of hydroxyzine and its active metabolite cetirizine were determined after oral and intravenous administration of 2 mg kg(-1) of hydroxyzine to six healthy dogs. Plasma drug levels were determined with high-pressure liquid chromatography. Pharmacodynamic studies evaluated the suppressive effect on histamine and anticanine IgE-mediated cutaneous wheal formation. Pharmacokinetic and pharmacodynamic correlations were determined with computer modelling. The mean systemic availability of oral hydroxyzine was 72%. Hydroxyzine was rapidly converted to cetirizine regardless of the route of administration. The mean area-under-the-curve was eight and ten times higher for cetirizine than hydroxyzine after intravenous and oral dosing, respectively. After oral administration of hydroxyzine, the mean peak concentration of cetirizine was approximately 2.2 microg mL(-1) and that of hydroxyzine 0.16 ug mL(-1). The terminal half-life for cetirizine varied between 10 and 11 hr after intravenous and oral administration of hydroxyzine. A sigmoidal relationship was fit to the data comparing cetirizine plasma concentration to wheal suppression. Maximum inhibition (82% and 69% for histamine and anticanine IgE-mediated skin reactions, respectively) was observed during the first 8 hr, which correlated with a plasma concentration of cetirizine greater than 1.5 ug mL(-1). Pharmacological modelling suggested that increasing either hydroxyzine dosages or frequencies of administration would not result in histamine inhibition superior to that obtained with twice daily hydroxyzine at 2 mg kg(-1). In conclusion, there was rapid conversion of hydroxyzine to cetirizine. The reduction of wheal formation appeared almost entirely due to cetirizine. Pharmacodynamic modelling predicted that maximal antihistamine effect would occur with twice daily oral administration of hydroxyzine at 2 mg kg(-1).

PMID:18980631 Bizikova P et al; Vet Dermatol 19 (6): 348-57 (2008).


5.7 Biological Half-Life

Plasma elimination half-life is 8.3 hours.


The mean elimination half-life in 146 healthy volunteers across multiple pharmacokinetic studies was 8.3 hours ... .

US Natl Inst Health; DailyMed. Current Medication Information for Zyrtec - cetirizine hydrochloride (May 2006). Available from, as of July 2, 2009 https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?id=2115


The pharmacokinetics of the second generation H1-receptor antagonist cetirizine were studied in 15 infants and toddlers (mean +/- SD age, 12.3 +/- 5.4 months) who were treated with a single 0.25 mg/kg dose of cetirizine solution. ... The elimination half-life was 3.1 +/- 1.8 hours ...

PMID:9084458 Spicak V et al; Clin Pharmacol Ther 61 (3): 325-30 (1997).


5.8 Mechanism of Action

Cetirizine, a metabolite of _hydroxyzine_, is an antihistamine drug. Its main effects are achieved through selective inhibition of peripheral H1 receptors. The antihistamine activity of cetirizine has been shown in a variety of animal and human models. _In vivo_ and _ex vivo_ animal models have shown insignificant anticholinergic and antiserotonergic effects. In clinical studies, however, dry mouth was found to be more frequent with cetirizine than with a placebo. In vitro receptor binding studies have demonstrated no detectable affinity of cetirizine for histamine receptors other than the H1 receptors. Studies with radiolabeled cetirizine administration in the rat have demonstrated insignificant penetration into the brain. _Ex vivo_ studies in the mouse have shown that systemically administered cetirizine does not occupy cerebral H1 receptors significantly.


Cetirizine, a human metabolite of hydroxyzine, is an antihistamine; its principal effects are mediated via selective inhibition of peripheral H1 receptors. The antihistaminic activity of cetirizine has been clearly documented in a variety of animal and human models. In vivo and ex vivo animal models have shown negligible anticholinergic and antiserotonergic activity. In clinical studies, however, dry mouth was more common with cetirizine than with placebo. In vitro receptor binding studies have shown no measurable affinity for other than H1 receptors. Autoradiographic studies with radiolabeled cetirizine in the rat have shown negligible penetration into the brain. Ex vivo experiments in the mouse have shown that systemically administered cetirizine does not significantly occupy cerebral H1 receptors.

US Natl Inst Health; DailyMed. Current Medication Information for Zyrtec - cetirizine hydrochloride (May 2006). Available from, as of July 2, 2009 https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?id=2115


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31-Jul-2025
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ABOUT THIS PAGE

Looking for 83881-51-0 / Cetirizine API manufacturers, exporters & distributors?

Cetirizine manufacturers, exporters & distributors 1

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PharmaCompass offers a list of Cetirizine API manufacturers, exporters & distributors, which can be sorted by GMP, USDMF, JDMF, KDMF, CEP (COS), WC, Price,and more, enabling you to easily find the right Cetirizine manufacturer or Cetirizine supplier for your needs.

Send us enquiries for free, and we will assist you in establishing a direct connection with your preferred Cetirizine manufacturer or Cetirizine supplier.

PharmaCompass also assists you with knowing the Cetirizine API Price utilized in the formulation of products. Cetirizine API Price is not always fixed or binding as the Cetirizine Price is obtained through a variety of data sources. The Cetirizine Price can also vary due to multiple factors, including market conditions, regulatory modifications, or negotiated pricing deals.

API | Excipient name

Cetirizine

Synonyms

83881-51-0, Cetirizina, Cetirizin, Virlix, Cetirizinum, Zirtek

Cas Number

83881-51-0

Unique Ingredient Identifier (UNII)

YO7261ME24

About Cetirizine

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 Manufacturers

A Cetirizine manufacturer is defined as any person or entity involved in the manufacture, preparation, processing, compounding or propagation of Cetirizine, including repackagers and relabelers. The FDA regulates Cetirizine manufacturers to ensure that their products comply with relevant laws and regulations and are safe and effective to use. Cetirizine API Manufacturers are required to adhere to Good Manufacturing Practices (GMP) to ensure that their products are consistently manufactured to meet established quality criteria.

click here to find a list of Cetirizine manufacturers with USDMF, JDMF, KDMF, CEP, GMP, COA and API Price related information on PhamaCompass.

Cetirizine Suppliers

A Cetirizine supplier is an individual or a company that provides Cetirizine active pharmaceutical ingredient (API) or Cetirizine finished formulations upon request. The Cetirizine suppliers may include Cetirizine API manufacturers, exporters, distributors and traders.

click here to find a list of Cetirizine suppliers with USDMF, JDMF, KDMF, CEP, GMP, COA and API Price related information on PharmaCompass.

Cetirizine WC

A Cetirizine written confirmation (Cetirizine WC) is an official document issued by a regulatory agency to a Cetirizine manufacturer, verifying that the manufacturing facility of a Cetirizine active pharmaceutical ingredient (API) adheres to the Good Manufacturing Practices (GMP) regulations of the importing country. When exporting Cetirizine APIs or Cetirizine finished pharmaceutical products to another nation, regulatory agencies frequently require a Cetirizine WC (written confirmation) as part of the regulatory process.

click here to find a list of Cetirizine suppliers with Written Confirmation (WC) on PharmaCompass.

Cetirizine NDC

National Drug Code is a comprehensive database maintained by the FDA that contains information on all drugs marketed in the US. This directory includes information about finished drug products, unfinished drug products, and compounded drug products, including those containing Cetirizine as an active pharmaceutical ingredient (API).

Finished drug products

The FDA updates the NDC directory daily. The NDC numbers for Cetirizine API and other APIs are published in this directory by the FDA.

Unfinished drugs

The NDC unfinished drugs database includes product listing information submitted for all unfinished drugs, such as active pharmaceutical ingredients (APIs), drugs intended for further processing and bulk drug substances for compounding.

Pharmaceutical companies that manufacture Cetirizine as an active pharmaceutical ingredient (API) must furnish the FDA with an updated record of all drugs that they produce, prepare, propagate, compound, or process for commercial distribution in the US at their facilities.

Compounded drug products

The NDC directory also contains data on finished compounded human drug products that contain Cetirizine and are produced by outsourcing facilities. While these outsourcing facilities are not mandated to assign a Cetirizine NDC to their finished compounded human drug products, they may choose to do so.

click here to find a list of Cetirizine suppliers with NDC on PharmaCompass.

Cetirizine GMP

Cetirizine Active pharmaceutical ingredient (API) is produced in GMP-certified manufacturing facility.

GMP stands for Good Manufacturing Practices, which is a system used in the pharmaceutical industry to make sure that goods are regularly produced and monitored in accordance with quality standards. The FDA’s current Good Manufacturing Practices requirements are referred to as cGMP or current GMP which indicates that the company follows the most recent GMP specifications. The World Health Organization (WHO) has its own set of GMP guidelines, called the WHO GMP. Different countries can also set their own guidelines for GMP like China (Chinese GMP) or the EU (EU GMP).

PharmaCompass offers a list of Cetirizine GMP manufacturers, exporters & distributors, which can be sorted by USDMF, JDMF, KDMF, CEP (COS), WC, API price, and more, enabling you to easily find the right Cetirizine GMP manufacturer or Cetirizine GMP API supplier for your needs.

Cetirizine CoA

A Cetirizine CoA (Certificate of Analysis) is a formal document that attests to Cetirizine's compliance with Cetirizine specifications and serves as a tool for batch-level quality control.

Cetirizine CoA mostly includes findings from lab analyses of a specific batch. For each Cetirizine CoA document that a company creates, the USFDA specifies specific requirements, such as supplier information, material identification, transportation data, evidence of conformity and signature data.

Cetirizine may be tested according to a variety of international standards, such as European Pharmacopoeia (Cetirizine EP), Cetirizine JP (Japanese Pharmacopeia) and the US Pharmacopoeia (Cetirizine USP).

Inform the supplier about your product requirements, specifying if you need a product with particular monograph like EP (Ph. Eur.), USP, JP, BP, or any other quality. In addition, clarify whether you need hydrochloride (HCl), anhydricum, base, micronisatum or a specific level of purity. To find reputable suppliers, utilize the filters and select those certified by GMP, FDA, or any other certification as per your requirement.
For your convenience, we have listed synonyms and CAS numbers to help you find the best supplier. The use of synonyms and CAS numbers can be helpful in identifying potential suppliers, but it is crucial to note that they might not always indicate the exact same product. It is important to confirm the product details with the supplier before making a purchase to ensure that it meets your requirements.
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