Drug/Small Molecule:
hydroxyzine

PharmGKB contains no dosing guidelines for this drug/small molecule. To report known genotype-based dosing guidelines, or if you are interested in developing guidelines, click here.

PharmGKB has no annotated drug labels with pharmacogenomic information for this drug/small molecule. If you know of a drug label with PGx, send us a message.

PharmGKB contains no Clinical Variants that meet the highest level of criteria.

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The annotations do not account for individual variations among patients, and cannot be considered inclusive of all proper methods of care or exclusive of other treatments. It remains the responsibility of the health-care provider to determine the best course of treatment for a patient. Adherence to any guideline is voluntary, with the ultimate determination regarding its application to be made solely by the clinician and the patient. PharmGKB assumes no responsibility for any injury or damage to persons or property arising out of or related to any use of the PharmGKB clinical annotations, or for any errors or omissions.

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This is a non-comprehensive list of genetic tests with pharmacogenetics relevance, typically submitted by the manufacturer and manually curated by PharmGKB. The information listed is provided for educational purposes only and does not constitute an endorsement of any listed test or manufacturer.

A more complete listing of genetic tests is found at the Genetic Testing Registry (GTR).

PGx Test Variants Assayed Gene?
2D structure from PubChem
provided by PubChem

Overview

Generic Names
  • Hidroxizina [INN-Spanish]
  • Hydroksyzyny [Polish]
  • Hydroxine
  • Hydroxizine
  • Hydroxizinum
  • Hydroxycine
  • Hydroxyzin
  • Hydroxyzine Base
  • Hydroxyzine Hcl
  • Hydroxyzine Pamoate
  • Hydroxyzinum [INN-Latin]
  • Hydroxyzyne
  • Idrossizina [Dcit]
Trade Names
  • Alamon
  • Atara
  • Atarax
  • Ataraxoid
  • Atarazoid
  • Atarox
  • Atazina
  • Aterax
  • Deinait
  • Durrax
  • Equipoise
  • Equipose
  • Fenarol
  • Hy-Pam 25
  • Hychotine
  • Masmoran
  • Neo-Calma
  • Neurozina
  • Nevrolaks
  • Orgatrax
  • Pamazone
  • Paxistil
  • Placidol
  • Plaxidol
  • Quiess
  • Tran-Q
  • Tranquizine
  • Traquizine
  • Vesparaz-Wirkstoff
  • Vistaril
  • Vistaril Pamoate
  • Vistazine
Brand Mixture Names

PharmGKB Accession Id:
PA449943

Description

A histamine H1 receptor antagonist that is effective in the treatment of chronic urticaria, dermatitis, and histamine-mediated pruritus. Unlike its major metabolite cetirizine, it does cause drowsiness. It is also effective as an antiemetic, for relief of anxiety and tension, and as a sedative.

Source: Drug Bank

Indication

For symptomatic relief of anxiety and tension associated with psychoneurosis and as an adjunct in organic disease states in which anxiety is manifested. Useful in the management of pruritus due to allergic conditions such as chronic urticaria.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

Hydroxyzine competes with histamine for binding at H 1-receptor sites on the effector cell surface, resulting in suppression of histaminic edema, flare, and pruritus. The sedative properties of hydroxyzine occur at the subcortical level of the CNS. Secondary to its central anticholinergic actions, hydroxyzine may be effective as an antiemetic.

Source: Drug Bank

Pharmacology

Hydroxyzine, a piperazine antihistamine structurally related to buclizine, cyclizine, and meclizine, is used to treat histamine-mediated pruritus or pruritus due to allergy, nausea and vomiting, and, in combination with an opiate agonist, anxiolytic pain. Hydroxyzine is also used as a perioperative sedative and anxiolytic and to manage acute alcohol withdrawal. Hydroxyzine's active metabolite, cetirizine, is also used as an H 1-antagonist.

Source: Drug Bank

Food Interaction

Avoid alcohol.|Take with food.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatic

Source: Drug Bank

Protein Binding

93%

Source: Drug Bank

Absorption

Rapidly absorbed from the gastrointestinal tract

Source: Drug Bank

Half-Life

20 to 25 hours

Source: Drug Bank

Toxicity

Oral, rat LD 50: 950 mg/kg. Symptoms of overexposure include hypersedation.

Source: Drug Bank

Chemical Properties

Chemical Formula

C21H27ClN2O2

Source: Drug Bank

Isomeric SMILES

c1ccc(cc1)C(c2ccc(cc2)Cl)N3CCN(CC3)CCOCCO

Source: OpenEye

Canonical SMILES

OCCOCCN1CCN(CC1)C(C1=CC=CC=C1)C1=CC=C(Cl)C=C1

Source: Drug Bank

Average Molecular Weight

374.904

Source: Drug Bank

Monoisotopic Molecular Weight

374.176105825

Source: Drug Bank

Genes that are associated with this drug in PharmGKB's database based on (1) variant annotations, (2) literature review, (3) pathways or (4) information automatically retrieved from DrugBank, depending on the "evidence" and "source" listed below.

Curated Information ?

EvidenceGene
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
KCNH2

Drug Targets

Gene Description
HRH1 (source: Drug Bank)

Drug Interactions

Drug Description
hydroxyzine Possible antagonism of action (source: Drug Bank)
hydroxyzine Possible antagonism of action (source: Drug Bank)
hydroxyzine Possible antagonism of action (source: Drug Bank)
hydroxyzine Possible antagonism of action (source: Drug Bank)
donepezil Possible antagonism of action (source: Drug Bank)
donepezil Possible antagonism of action (source: Drug Bank)
galantamine Possible antagonism of action (source: Drug Bank)
galantamine Possible antagonism of action (source: Drug Bank)
rivastigmine Possible antagonism of action (source: Drug Bank)
rivastigmine Possible antagonism of action (source: Drug Bank)
hydroxyzine The therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Hydroxyzine, may be reduced due to antagonism. The interaction may be beneficial when the anticholinergic action is a side effect. Monitor for decreased efficacy of both agents. (source: Drug Bank)
hydroxyzine The therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Hydroxyzine, may be reduced due to antagonism. The interaction may be beneficial when the anticholinergic action is a side effect. Monitor for decreased efficacy of both agents. (source: Drug Bank)
hydroxyzine Trimethobenzamide and Hydroxyzine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects. (source: Drug Bank)
hydroxyzine Triprolidine and Hydroxyzine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Additive CNS depressant effects may also occur. Monitor for enhanced anticholinergic and CNS depressant effects. (source: Drug Bank)
hydroxyzine Triprolidine and Hydroxyzine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Additive CNS depressant effects may also occur. Monitor for enhanced anticholinergic and CNS depressant effects. (source: Drug Bank)
hydroxyzine Trospium and Hydroxyzine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects. (source: Drug Bank)

Publications related to hydroxyzine: 4

No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
KCNH2 pharmacogenomics summary. Pharmacogenetics and genomics. 2010. Oshiro Connie, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Coprescription of tamoxifen and medications that inhibit CYP2D6. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2010. Sideras Kostandinos, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Hydroxyzine, a first generation H(1)-receptor antagonist, inhibits human ether-a-go-go-related gene (HERG) current and causes syncope in a patient with the HERG mutation. Journal of pharmacological sciences. 2008. Sakaguchi Tomoko, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Functional pharmacogenetics/genomics of human cytochromes P450 involved in drug biotransformation. Analytical and bioanalytical chemistry. 2008. Zanger Ulrich M, et al. PubMed

LinkOuts

Web Resource:
Wikipedia
National Drug Code Directory:
0049-5460-74
DrugBank:
DB00557
ChEBI:
5818
KEGG Compound:
C07045
PubChem Compound:
3658
PubChem Substance:
46508556
9257
Drugs Product Database (DPD):
739618
BindingDB:
22875
ChemSpider:
3531
Therapeutic Targets Database:
DAP000324
FDA Drug Label at DailyMed:
aed7d120-5f3d-4276-b341-737244d4f8a5

Clinical Trials

These are trials that mention hydroxyzine and are related to either pharmacogenetics or pharmacogenomics.

Common Searches

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Sources for PharmGKB drug information: DrugBank, Open Eye Scientific Software.