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Mechanism of Action
Cetirizine¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ 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.
Pharmacology
Cetirizine¿¡ ´ëÇÑ Pharmacology Á¤º¸ Cetirizine, the active metabolite of the piperazine H1 -receptor antagonist hydroxyzine, is used to treat chronic idiopathic urticaria, perennial allergic rhinitis, seasonal allergic rhinitis, allergic asthma, physical urticaria, and atopic dermatitis.
Metabolism
Cetirizine¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 3A43 (CYP3A43)
Protein Binding
Cetirizine¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ Very high (93%) plasma protein binding
Half-life
Cetirizine¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 8.3 hours
Absorption
Cetirizine¿¡ ´ëÇÑ Absorption Á¤º¸ mean peak plasma concentration (Cmax) of 114 ng/mL at a time (Tmax) of 2.2 hours postdose was observed for cetirizine
Biotransformation
Cetirizine¿¡ ´ëÇÑ Biotransformation Á¤º¸ Not Available
Toxicity
Cetirizine¿¡ ´ëÇÑ Toxicity Á¤º¸ Somnolence (sleepiness or unusual drowsiness), restlessness, irritability
Drug Interactions
Cetirizine¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Not Available
CYP450 Drug Interaction
[CYP450 TableÁ÷Á¢Á¶È¸]
Food Interaction
Cetirizine¿¡ ´ëÇÑ Food Interaction Á¤º¸ Avoid alcohol.Take without regard to meals.
Drug Target
[Drug Target]
Description
Cetirizine¿¡ ´ëÇÑ Description Á¤º¸ 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. [PubChem]
Dosage Form
Cetirizine¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Syrup OralTablet Oral
Drug Category
Cetirizine¿¡ ´ëÇÑ Drug_Category Á¤º¸ Anti-Allergic AgentsAntihistaminesHistamine H1 Antagonists, Non-Sedating
Smiles String Canonical
Cetirizine¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ OC(=O)COCCN1CCN(CC1)C(C1=CC=CC=C1)C1=CC=C(Cl)C=C1
Smiles String Isomeric
Cetirizine¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ OC(=O)COCCN1CCN(CC1)[C@H](C1=CC=CC=C1)C1=CC=C(Cl)C=C1
InChI Identifier
Cetirizine¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/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)/f/h25H
Chemical IUPAC Name
Cetirizine¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 2-[2-[4-[(4-chlorophenyl)-phenylmethyl]piperazin-1-yl]ethoxy]acetic acid
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ÀüÈ: 02-3486-1061 ¤Ó À̸ÞÀÏ: webmaster@druginfo.co.kr
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The database contains the following fields:
The generic name of each chemical
For module A10 (liver enzyme composite module):
Overall activity category for each compound (A for active, M for marginally active, or I for inactive) based on the number of active and marginally active scores for each compound at the five individual endpoints (see research article for full description of method)
Number of endpoints at which each compound is marginally active (M)
Number of endpoints at which each compound is active (A)
For modules A11 to A15 (alkaline phosphatase increased, SGOT increased, SGPT increased, LDH increased, and GGT increased, respectively):
Overall activity category for each compound (A for active, M for marginally active, or I for inactive) based on the RI and ADR values (see the research article for full description of method)
Number of ADR reports for each compound, given as <4 or ¡Ã4
Reporting Index value for each compound, except where no shipping units were available (NSU)
Group 1 comprises of compounds for which ADR data were available for the first five years of marketing, so when no ADR reports were listed during this period the compounds were evaluated as inactive. Group 2 comprises of compounds for which a 'steady state' period of ADR data were available (1992-1996). In cases where no ADR reports were filed during this period, the compounds were scored as 'NA' (data not available) since they may have had one or more ADR reports during their first five years of marketing which should not be negated by a lack of ADR reports during the steady-state period.
CETIRIZINE [GGT Increase] [Composite Activity] (Score) I (Marginal) 0 (Active) 0 [Alkaline Phosphatase Increase] (Activity Score) I (Number of Rpts) <4 (Index value) 0 [SGOT Increase] (Activity Score) I (Number of Rpts) <4 (Index value) 1 [SGPT Increase] (Activity Score) I (Number of Rpts) ¡Ã4 (Index value) 1.3 [LDH Increase] (Activity Score) I (Number of Rpts) <4 (Index value) 1 [GGT Increase] (Activity Score) I (Number of Rpts) <4 (Index value) 0.6
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