Hydroxycin

CAS number68-88-2
PUB number3658
Drugbank IDDB00557
Empirical formulaC21H27CIN2O2
Molar mass (g·mol−1)374,904
Physical statesolid
Melting point (°C)200
Boiling point (°C)220
PKS value2,47

Basics

Hydroxycin is an antihistamine which, in addition to treating allergic conditions (chronic itching and hives), is also used to relieve anxiety and tension, as well as sleep and insomnia. Hydroxycin is commercially available in tablet or syrup form.

Pharmacology

Pharmacodynamics

The antihistamine and antiallergic effects are based on hydroxycin blocking the H1 histamine receptor and actively attenuating its activity. By affecting neurotransmitter systems in the brain, the drug also has sedative, tranquilizing, and antispasmodic effects. The effects of hydroxycin occur within 15 to 60 minutes and last up to 6 hours.

Pharmacokinetics

After oral administration, hydroxycin is rapidly absorbed from the gastrointestinal tract and reaches maximum plasma concentration after approximately 2 hours. The drug is metabolized in the liver by the CYP3A4 and CYP3A5 enzymes. 70% of the active intermediate hydroxyzine is excreted in the urine. The half-life in children, adults, and the elderly is approximately 7, 20, and 29 hours, respectively.

Contraindications

Hydroxycin should not be taken in case of:

  • Hypersensitivity
  • severe liver or kidney failure
  • Prostate enlargement
  • Narrow-angle glaucoma
  • Porphyrias
  • pregnancy and breastfeeding

Drug interactions

Interactions with alcohol, central depressant drugs, MAO inhibitors, parasympathomimetics, and antihypertensives are possible with concomitant use, as well as with betahistine, epinephrine, phenytoin, and cimetidine.

Toxicity

Side effects

Drowsiness, dullness, headache, and dry mouth are common with the use of hydroxycin.

Toxicological data

Severe sedation is most common with overdose, but convulsions, drowsiness, nausea, or vomiting often occur LD50 (rat, oral): 840 mg/kg LD50 (mouse, oral): 400 mg/kg

Markus Falkenstätter, BSc

Markus Falkenstätter, BSc

Mag. pharm. Stefanie Lehenauer

Mag. pharm. Stefanie Lehenauer



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