Hydroxyzine (/haɪˈdrɒksɨziːn/; sold as Vistaril, Atarax) is a first-generation antihistamine of the diphenylmethane and piperazineclass. It was first synthesized by Union Chimique Belge in 1956 and was marketed by Pfizer in the United States later the same year, and is still in widespread use today.
Due to its antagonistic effects on several receptor systems in the brain, hydroxyzine is claimed to have strong anxiolytic and mildantiobsessive as well as antipsychotic properties. Today it is used primarily for the symptomatic relief of anxiety and tension associated with psychoneurosis and as an adjunct in organic disease states in which anxiety is manifested. Because of itsantihistamine effects it can also be used for the treatment of severe cases of itching, hyperalgesia and motion sickness-inducednausea, it has also been used in some cases to relieve the effects of opioid withdrawal. Even though it is an effectivesedative, hypnotic, and anxiolytic, it allegedly shares virtually none of the abuse, dependence, addiction, and toxicity potential of other drugs used for the same range of therapeutic reasons. Hydroxyzine has also been used to potentiate the analgesia of opioids and to alleviate some of their side effects, such as itching, nausea, and vomiting.
Hydroxyzine preparations usually require a doctor's prescription. The drug is available in two formulations, the pamoate and thedihydrochloride or hydrochloride salts. Vistaril, Equipose, Masmoran, and Paxistil are preparations of the pamoate salt, whileAtarax, Alamon, Aterax, Durrax, Tran-Q, Orgatrax, Quiess, and Tranquizine are of the hydrochloride salt.
Other drugs related to hydroxyzine are cyclizine, buclizine, and meclizine, and they share all or most of the benefits, indications, contraindications, cautions, and side effects of hydroxyzine. The second-generation antihistamine cetirizine is in fact one of themetabolites of hydroxyzine produced in the human body. Unlike hydroxyzine, cetirizine is not reported to appreciably cross theblood-brain barrier, but it has been reported to be associated with dystonic reactions as well as sedation. Therefore it has a narrower spectrum of effects, making it an effective antihistamine but removing some or all of the anxiolytic and other psychoactive properties, but it may cause dystonic reactions and drowsiness in some patients.