Hydroxyzine

Tranquilizer, Sedative/Hypnotic · Anxiolytic

Indications

Pruginous affections, respiratory allergies, digestive, skin and mucous membrane allergies such as urticaria, angioneurotic oedema. Nervous stress, anxiety and neurovegetative disorders observed in internal medicine practice.

Dosage

Adults: ORAL: Antihistamine: 25 mg 3-4 times daily. Anxiety: 50-100 mg four times daily. Adults: INJECTION: Adjust dose based on patients response. Pre-operative Sedation/Antiemetic: IM: 25-100 mg. Children: ORAL: Antihistamine: > 6 yr: 50-100 mg/day in divided doses. <6 yr: 50 mg/day in divided doses. Pruritus: 6 mth-6 yr, initially 5-15 mg at night, increased if necessary to 50 mg daily in 3-4 divided doses; 6-12 yr, initially 15-25 mg at night, increased if necessary to 50-100 mg daily in 3-4 divided doses; 12-18 yr, initially 25 mg at night, increased if necessary to 100 mg in 3-4 divided doses. Anxiety: Below 6 yr, 50 mg/day in divided doses; above 6 yr, 50-100 mg/day in divided doses. Children: INJECTION: Adjust dose based on patients response, Pre-operative Sedation/Antiemetic: IM: 1.1 mg/kg/dose.

Administration

Administered undiluted by IM injection only, preferably into the upper outer quadrant of the buttock or the mid-lateral muscles of the thigh in adults. In children, the mid-lateral muscles of the thigh are preferred. Stability: Stored at controlled room temperature and protect from light and freezing and excessive temperatures.

Adverse Effects

Somnolence, headache, dry mouth, fatigue. Reports of torsade de pointes.

Risk Factor (Pregnancy/Lactation)

Pregnancy: Risk cannot be ruled out. Lactation: Contraindicated or not recommended. Contraindications: Porphyria. Severe hepatic impairment. Active or risk factors for QT prolongation. Asthma patients with previous serious antihistamine-induced adverse bronchopulmonary effect. Precautions: Renal impairment. Warn patients of impaired judgement and dexterity. Mild to moderate hepatic impairment. Bladder outflow obstruction, urinary retention, glaucoma, pyloroduodenal obstruction, decreased GI motility, myasthenia gravis, dementia, hyperthyroidism, cardiovascular disease, hypertension, BPH, seizure disorders, respiratory disorders, stenosing peptic ulcer. Advise patients to report cardiac symptoms. Monitor for signs of arrhythmia. Use lowest effective dose for shortest duration. Elderly.

Interactions

Alcohol, CNS disturbances, anticholinergics, MAOIs, betahistine, anticholinesterases, adrenaline, cimetidine, CYP2D6 substrates, potent inhibitors of CYP3A4/5 or alcohol dehydrogenase, agents that prolong QT interval, agents that cause bradycardia or hypokalaemia.

Advice to Patient

Take oral form with or without meals. Avoid taking alcohol and CNS depressants during therapy. Empty bladder before taking medication. Take sufficient amount of fluids (2-3 litres per day) to maintain hydration, unless restricted by the prescriber.

Pharmacokinetics

Onset of action: Oral: 15-30 mins; IM: Rapid. Duration: Decreased histamine-induced wheal and flare areas: 2 to =36 hrs; Suppression of pruritus: 1-12 hrs. Absorption: Oral: Rapid. Metabolism: Hepatic to multiple metabolites, including cetirizine (active). Half-life elimination: Children and Adolescents 1-14 yrs (mean age: 6.1 ± 4.6 yrs): 7.1 ± 2.3 hrs. Adults: Approx. 20 hrs; Elderly: Approx. 29 hrs; Hepatic dysfunction: Approx. 37 hrs. Time to peak: Oral administration: Serum: Approx. 2 hrs; Peak suppression of antihistamine-induced wheal and flare: 4-12 hrs. Excretion: Urine; active metabolite (cetirizine) is renally eliminated.

Brands with this active ingredient

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