Ziltem/Ziltem IM

Ziltem: Each film-coated tablet contains: Hydroxyzine Hydrochloride USP 25 mg.
Ziltem IM: Each mL contains: Hydroxyzine hydrochloride USP 50 mg, Benzyl alcohol USP (As preservative) 0.9% v/v, Water for injection USP q.s.
Excipients/Inactive Ingredients: Ziltem: q.s. Colour: Titanium Dioxide BP & Quinoline Yellow.

Antihistamine (H₁-Receptor Antagonist).
Pharmacology: Pharmacokinetics: Hydroxyzine is rapidly absorbed from the gastrointestinal tract and is metabolized. Metabolites include cetirizine which has antihistamine activity. An elimination half-life of about 20 hours has been reported.

Used as anxiolytic, as an adjunct to pre-and postoperative medication and in the management of pruritus and urticaria. It has been used as an adjunct to opioid analgesia in the management of cancer pain.

Hydroxyzine may be given orally as the hydrochloride or the embonate; doses are expressed in terms of the hydrochloride. Hydroxyzine embonate 170 mg is equivalent to about 100 mg of hydroxyzine hydrochloride. The usual oral doses in adults are: 50 to 100 mg four times daily for the short-term management of anxiety; for pruritus an initial dose of 25 mg given at night, increased if necessary to 25 mg three or four times daily; and 50 to 100 mg for pre or post operative sedation.
For pruritus in children over 6 years of age the initial dose is 15 to 25 mg daily increased if necessary to 50 mg daily in divided doses.
Hydroxyzine may be given IM; Alternatively, 1 mg/kg may be given in divided doses, to a maximum of 2.5 mg/kg in children aged 1 to 6 years, and to a maximum of 2 mg/kg daily in those aged 6 years and over. The pre- or postoperative sedative dose in children is 600 micrograms/kg. Dosage should be reduced in patients with hepatic or renal impairment.
For adult psychiatric and emotional emergencies including acute alcoholism IM: 50-100 mg stat., and q. 4-6h., p.r.n.
Nausea and vomiting excluding nauseas and vomiting of pregnancy: Adults: 25-200 mg IM.
Children 0.5 mg/lb body weight IM.
Pre and postoperative adjunctive medication: Adults: 25-200 mg IM.
Children: 0.5 mg/lb body weight IM Pre and postpartum adjunctive therapy 25-100 mg IM.

The most common adverse effect of the sedating antihistamine is CNS depression, with effects varying from slight drowsiness to deep sleep, and including lassitude, dizziness, and incoordination (although paradoxical stimulation may occasionally occur, especially at high doses and in children or the elderly). These sedative effects, when they occur, may diminish after a few days of treatment.
Other adverse effects that are more common with the sedating antihistamines include headache, psychomotor impairment and antimuscarinic effects, such as dry mouth, thickened respiratory-tract secretions, blurred vision, urinary difficulty or retention, constipation and increased gastric reflux.
Antihistamines sometimes cause rashes and hypersensitivity reactions (including bronchospasm, angioedema and anaphylaxis) and cross-sensitivity to related drugs may occur. Photosensitivity can be a problem, particularly with the phenothiazine antihistamines. Blood disorders, including agranulocytosis, leucopenia, haemolytic anaemia and thrombocytopenia, although rare, have been reported. Jaundice has also been observed, particularly with the phenothiazine antihistamines.
Other adverse effects that have been reported with the antihistamines include convulsions, sweating, myalgia, paraesthesias, extrapyramidal effects, tremor, sleep disturbances, depression, confusion, tinnitus, hypotension and hair loss.
Despite reports suggesting a possibility of human fetal abnormalities resulting from the use of some antihistamines, especially the piperazine derivatives, a causal relationship has largely been rejected.

Sedating antihistamines may enhance the sedative effects of CNS depressants including alcohol, barbiturates, hypnotics, opioid analgesics, anxiolytic sedatives, and antipsychotic. Sedative interactions apply to a lesser extent with the non-sedating antihistamines; they do not appear to potentiate the effects of alcohol, but it should be avoided in excess.
Sedating antihistamines have an additive antimuscarinic action with other antimuscarinic drugs, such as atropine and some antidepressants (both tricyclic and MAOIs).
Potentially hazardous ventricular arrhythmias have occurred when the non-sedating antihistamines astemizole and terfenadine have been given with drugs liable to interfere with their hepatic metabolism, with other potentially arrhythmogenic drugs including those that prolong the QT interval, or with those likely to cause electrolyte imbalance.
It has been suggested that some sedating antihistamines could mask the warning signs of damage caused by ototoxic drugs such as aminoglycoside antibiotics. Antihistamines may suppress the cutaneous histamine response to allergen extracts and should be stopped several days before skin testing.

Store at temperatures not exceeding 30°C.
Shelf-life: 36 months.
Ziltem IM: Protect from light.

Anxiolytics

N05BB01 - hydroxyzine ; Belongs to the class of diphenylmethane derivatives anxiolytics. Used in the management of anxiety, agitation or tension.

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