These have also been confirmed in both recent and past studies to have no adverse effects on the liver, blood, nervous system, or urinary tract.Use of hydroxyzine for premedication as a sedative has no effects on tropane alkaloids, such as atropine, but may, following general anesthesia, potentiate meperidine and barbiturates, and use in pre-anesthetic adjunctive therapy should be modified depending upon the state of the individual.Hydroxyzine is used as a non-barbiturate tranquilizer and for the treatment of neurological disorders, such as psychoneurosis and other forms of anxiety or tension states.Doses of hydroxyzine hydrochloride used for sleep range from 25 to 100 mg. As with other antihistamine sleep aids, hydroxyzine is usually only prescribed for short term or "as-needed" use since tolerance to the CNS effects of hydroxyzine can develop in as little as a few days. Contraindications
The administration of hydroxyzine in large amounts by ingestion or intramuscular administration during the onset of pregnancy can cause fetal abnormalities. When administered to pregnant rats, mice and rabbits, hydroxyzine caused abnormalities such as hypogonadism with doses significantly above that of the human therapeutic range.In humans, a significant dose has not yet been established in studies and, by default, the Food and Drug Administration (FDA) has introduced contraindication guidelines in regard to hydroxyzine. Use by those at risk for or showing previous signs of hypersensitivity is also contraindicated. Hydroxyzine is contraindicated for intravenous (IV) injection, as it has shown to cause hemolysis.
The effect of hydroxyzine is notable in 30 minutes.Hydroxyzine is rapidly absorbed and distributed with oral and intramuscular administration, and is metabolized in the liver; the main metabolite (45%), cetirizine, is formed through oxidation of the alcohol moiety to a carboxylic acid by alcohol dehydrogenase, and overall effects are observed within one hour of administration. Higher concentrations are found in the skin than in the plasma. Cetirizine, although less sedating, is non-dialyzable and possesses similar antihistamine properties. The other metabolites identified include a N-dealkylated metabolite, and an O-dealkylated 1/16 metabolite with a plasma half-life of 59 hours. These pathways are mediated principally by CYP3A4 and CYP3A5. "In animals, hydroxyzine and its metabolites are excreted in feces via biliary elimination. "The Tmax of hydroxyzine is about 2.0 hours in both adults and children and its elimination half-life is around 20.0 hours in adults (mean age 29.3 years) and 7.1 hours in children. Its elimination half-life is shorter in children compared to adults. In another study, the elimination half-life of hydroxyzine in elderly adults was 29.3 hours. One study found that the elimination half-life of hydroxyzine in adults was as short as 3 hours, but this may have just been due to methodological limitations.