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QuickView for Hydroxyzine (compound)

Summary
General Info

PubChem

PubChem Compound 1548976

PubChem Compound 1548976

Name:	Hydroxyzine
PubChem Compound ID:	1548976
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.
Molecular formula:	C₂₁H₂₇ClN₂O₂
Molecular weight:	374.904 g/mol
Synonyms:	NCGC00016608-01; CAS-2192-20-3

DrugBank

Identification

Name:	Hydroxyzine
Name (isomeric):	DB00557
Drug Type:	small molecule
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.
Synonyms:	Hydroxine; Hydroxyzyne; Hydroxizine; Hydroxizinum; Hydroksyzyny [Polish]; Hydroxyzinum [INN-Latin]; Hydroxyzine Base; Hydroxycine; Hydroxyzin; Hydroxyzine Pamoate. show more » Hydroxine; Hydroxyzyne; Hydroxizine; Hydroxizinum; Hydroksyzyny [Polish]; Hydroxyzinum [INN-Latin]; Hydroxyzine Base; Hydroxycine; Hydroxyzin; Hydroxyzine Pamoate; Idrossizina [Dcit]; Hydroxyzine Hcl; Hidroxizina [INN-Spanish] show less «
Brand:	Hy-Pam 25, Equipoise, Tranquizine, Traquizine, Atarazoid, Aterax, Vesparaz-Wirkstoff, Deinait, Vistaril, Atazina, Ataraxoid, Fenarol, Neo-Calma, Atarox, Masmoran, Vistaril Pamoate, Orgatrax, Pamazone, Neurozina, Equipose, Plaxidol, Placidol, Alamon, Vistazine, Quiess, Atarax, Atara, Tran-Q, Hychotine, Durrax, Nevrolaks, Paxistil
Category:	Histamine H1 Antagonists, Antipruritics, Anxiolytics sedatives and hypnotics
CAS number:	68-88-2

Pharmacology

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.
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 alcoho... show more » 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 H₁-antagonist. show less «
Mechanism of Action:	Hydroxyzine competes with histamine for binding at H₁-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 antiem... show more » Hydroxyzine competes with histamine for binding at H₁-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. show less «
Absorption:	Rapidly absorbed from the gastrointestinal tract
Protein binding:	93%
Biotransformation:	Hepatic
Half Life:	20 to 25 hours
Toxicity:	Oral, rat LD₅₀: 950 mg/kg. Symptoms of overexposure include hypersedation.
Affected organisms:	Humans and other mammals

Interactions

Food interaction:

Avoid alcohol.

Take with food.

Drug interaction:

Butabarbital	Hydroxyzine may enhance the CNS depressant effect of barbiturates like butabarbital. Consider a decrease in the barbiturate dose, as appropriate, when used together with hydroxyzine. With concurrent use, monitor patients closely for excessive response to the combination.
Tacrine	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.
Donepezil	Possible antagonism of action
Rivastigmine	Possible antagonism of action
Trospium	Trospium and Hydroxyzine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.

Targets

Histamine H1 receptor

Enzymes

Cytochrome P450 2D6