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Latin name for the substance Hydroxysine
Hydroxyzinum (born Hydroxyzini)
2-[2-[4-[(4-Chlorophenyl)phenylmethyl]-1-piperazinyl]ethanol]ethanol (as dihydrochloride or embonate).
Gross Formula .
Pharmacological group of substance Hydroxysine
Nosological Classification (ICD-10)
Characteristics of the substance Hydroxysine https://reference.medscape.com/drug/atarax-vistaril-hydroxyzine-343395
Hydroxysine hydrochloride - white powder, odorless, very well soluble in water, molecular weight 447.83.
Suction. After ingestion the absorption is high, the Tmax value is 2 hours. After taking an average dose of 50 mg Cmax in adults - 70 ng / ml.
After ingestion of a single dose of 50 mg Cmax is 65 ng/ml.
Distribution. Hydroxysine is more concentrated in tissues than in plasma. The Vd value is 7-
16 l/kg in adults.
penetrates the GHB and placenta, concentrating more in the
fetal than in the maternal tissues.
Hydroxysin penetrates well into the skin, with concentrations of hydroxysin in the skin much higher than those in serum, both after single and repeated use. Plasma concentrations of hydroxysin do not necessarily reflect its binding to tissues or its distribution in the skin.
Metabolism. Hydroxysine is metabolized in the liver. Cetyrizine - the main metabolite (45%) - is a blocker of H1-histamine receptors. Metabolites are found in breast milk. excretion. T1/2 in adults - 14 h (range - 7-20 h). The total clearance of hydroxysine is 13 ml/min/kg. About 0.8% of hydroxysin is excreted unchanged through the kidneys. Cethrysine is excreted mainly in the urine, also in its unchanged form (25% of the hydroxysine dose taken orally or 16% of the hydroxysine dose)
Special groups of patients
Older people. In elderly patients, T1/2 was 29 h, Vd - 22.5 l / kg. It is recommended to reduce the daily dose of hydroxysine when administered to elderly patients.
Children under 1 year old. In children, the total clearance is 2.5 times higher than in adults. Dose should be adjusted. T1/2 is 4 hours.https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/011459s050,011795s027lbl.pdf
Children from 1 to 14 years old. T1/2 is 11 hours.
Liver failure. In patients with secondary liver dysfunction due to primary biliary cirrhosis, total clearance was approximately 66% of the value recorded in healthy volunteers. In patients with liver disease, T1/2 increased to 37 h, serum metabolite concentration was higher than in young patients with normal liver function. Patients with hepatic insufficiency were recommended to reduce the daily dose or frequency of intake. Kidney failure. Pharmacokinetics of hydroxysine was studied in 8 patients with severe renal insufficiency (Cl creatinine (24±7) ml/min). The duration of hydroxysine exposure was not significantly changed, while the duration of cethirisine exposure was increased. To avoid any significant accumulation of cetyrizine after repeated use of hydroxysine in patients with impaired renal function, the daily dose of should be reduced.
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