Cetinal 10Mg

Composition Each chewable tablet of Cetinal contains Cetirizine diHCI10 mg. 

Pharmacology: Pharmacodynamics: Based on literature, Cetirizine is one of piperazine derivate and metabolite of hydroxyzine, is a long acting and non-sedating antihistamine with mast-cell stabilizing activities. Usual dosage of Cetirizine may cause very little drowsiness effect and almost does not possess muscarinic activities.  

Pharmacokinetics: Absorption: Based on literature, oral Cetirizine was rapidly absorbed with a time to maximum concentration (Tmax) following oral administration in adults is approximately 1 hour. A mean peak plasma concentration (Cm-ax) of 311 ng/mL was observed after administered multiple doses of Cetirizine (10 mg tablets once daily for 10 days). No accumulation was observed. Food had no effect on the extent of AUC (Area Under Curve) of the Cetirizine chewable tablet. Distribution: based on literature, at therapeutic concentration, the mean plasma protein binding of Cetirizine is 93%. Metabolism: Based on literature, approximately 70% of the administered dose was recovered in the urine and 10% in the feces. Approximately 50% of the administered dose was identified in the urine as unchanged drug. Most of the rapid increase in peak plasma was associated with parent drug, suggesting a low degree of first-pass metabolism. Cetirizine is metabolized to a limited extent by oxidative O-dealkylation to a metabolite with negligible antihistaminic activity. The enzymes responsible for this metabolism have not been identified. Elimination: Based on literature, the mean elimination half-life was 8.3 hours and the total body clearance for Cetirizine was approximately 53 mL/min. 

Indication: Symptomatic relief of allergy such as hay fever, chronic idiopathic urticaria. 

Contraindications: Cetinal is contraindicated for patients with a known hypersensitivity to Cetirizine or to Hydroxyzine or to other components of Cetinal. 

Warning and precautions: The occurrence of somnolence has been reported in some patients taking Cetirizine; due caution should therefore be exercised when driving a car or operating machinery. Concurrent use of Cetirizine with alcohol or other central nervous system depressants should be avoided because additional reductions in alertness and impairment of central nervous system may occur. 

Drug interaction: Alcohol: increase sedative effect when antihistamine given with alcohol. Analgesics: sedative effects possibly increased when sedating antihistamines given with opioid analgesics. Antimuscarinic: increased risk of antimuscarinic side effects when antihistamine given with antimuscarinic. Anxiolytics and hypnotics: increase sedative effect when antihistamine given with anxiolytics and hypnotics. Betahistine: antihistamines theoretically antagonize effect of betahistine. Histamine: antihistamines theoretically antagonize effects of histamine. Theophylline: There is a small decrease in the clearance of Cetirizine caused by a 400 mg dose of Theophylline; it is possible that larger. Theophylline doses could have a greater effect. 

Side-effects: Cetirizine as one of non-sedating antihistamine cause less sedation and psychomotor impairment than the older antihistamines because they penetrate the blood brain barrier only to a slight extent. Although drowsiness is rare in non-sedating antihistamines, nevertheless patients should be advised that it can occur and may affect performance of skilled tasks (e.g., driving). Excess of alcohol should be avoided. Side-effects that are more common with the older antihistamine include headache, psychomotor impairment, and antimuscarinic effects such as urinary retention, dry mouth, blurred vision and gastro-intestinal disturbances. Other rare side-effects of antihistamine include hypotension, palpitation, arrhythmias, extrapyramidal effects, dizziness, confusion, depression, sleep disturbances, tremor, convulsions, hypersensitivity reactions (including bronchospasm, angioedema, anaphylaxis, rashes, and photosensitivity reactions), blood disorders, liver dysfunction and angle-closure glaucoma. 

Overdosage and treatment: Drowsiness can be a symptom of overdosage, occurring from administration of 50 mg Cetirizine as a single dose. Agitation can occur if Cetirizine use in children. In the case of massive overdosage, gastric lavage should be performed together with the usual supportive measure. To date, there is no specific antidote. 

Manufactured by: PT KALBE FARMA Tbk