Setin

Film-coated tablet: White oblong biconvex film-coated tablet with "
Click on icon to see table/diagram/image
" logo on one side and engraved with the letter "S" and "T" and score on the other.
Each tablet contains Cetirizine dihydrochloride 10 mg.
Syrup: Clear colorless solution with strawberry flavor (alcohol-free product).
Each mL contains Cetirizine dihydrochloride 1 mg.
Oral solution: Clear colorless solution with strawberry odor (alcohol-free and sugar-free product).
Each mL contains Cetirizine hydrochloride* 1 mg.
*Remark: Cetirizine hydrochloride drug substance is also known as Cetirizine dihydrochloride, which has the same chemical formula (C₂₁H₂₇Cl₃N₂O₃).

Pharmacology: Pharmacodynamics: Cetirizine hydrochloride is a piperazine derivative secondary generation and long-acting non-sedative antihistamine. Cetirizine is the carboxylic acid metabolite of hydroxyzine. Cetirizine is a potent and selective antagonist of peripheral H₁ receptor. The increased polarity of Cetirizine may decrease distribution of the drug into the CNS, resulting in reduced potential for adverse CNS effect compared with some first generation antihistamine.
Pharmacokinetics: Absorption: Cetirizine is rapidly absorbed from the gastrointestinal tract after oral doses and peak plasma concentrations occur within about an hour. Food delays the time to peak plasma concentration but does not decrease the amount of drug absorbed.
Distribution: Cetirizine appears to be extensively distributed into many body tissues, fluids, and milk in humans. Cetirizine is approximately 93% bound to plasma proteins.
Metabolism: Cetirizine undergoes a low degree of first pass metabolism in the liver.
Elimination: About two-thirds of the dose of Cetirizine is excreted unchanged in urine. The terminal half-life is approximately 10 hours.

Adults and children of 2 years or above: Symptomatic treatment of seasonal allergic rhinitis with or without allergic conjunctivitis, perennial allergic rhinitis as well as pruritus and other symptoms of urticaria of allergic origin including insect bites.

Tablets: Children aged from 6 to 12 years: Half of the tablet (5 mg) twice daily.
Adults and children above 12 years of age: 1 tablet (10 mg) once daily.
A half of the tablet starting dose (5 mg) may be proposed in adults if this leads to satisfactory control of the symptoms.
Solution: Children aged from 2 to 6 years: 2.5 mL of oral solution (2.5 mg) twice daily.
Children aged from 6 to 12 years: 5 mL of oral solution (5 mg) twice daily.
Adults and children over 12 years of age: 10 mL of oral solution (10 mg) once daily.
A 5 mL starting dose (5 mg) may be proposed in adults if this leads to satisfactory control of the symptoms.
Elderly: Data does not suggest that the dose needs to be reduced in elderly subjects provided that the renal function is normal.
Renal impairment: Since Cetirizine is mainly excreted via renal route, in cases no alternative treatment can be used, the dosing intervals must be individualized according to renal function. Refer to table. (See table.)

Click on icon to see table/diagram/image

In paediatric patients suffering from renal impairment, the dose will have to be adjusted on an individual basis taking into account the renal clearance, age and body weight of the patient.
Hepatic impairment: No dose adjustment is needed in patients with solely hepatic impairment.
Patients with hepatic impairment and renal impairment: Dose adjustment is recommended following "Renal impairment" as previously mentioned.

Symptoms and signs: Symptoms observed after an overdose of Cetirizine are mainly associated with CNS effects or with effects that could suggest an anticholinergic effect. Adverse events reported after an intake of at least 5 times the recommended daily dose are confusion, diarrhea, dizziness, fatigue, headache, malaise, mydriasis, pruritus, restlessness, sedation, somnolence, stupor, tachycardia, tremor, and urinary retention.
Treatment: There is no known specific antidote to Cetirizine. If overdose occur, symptomatic or supportive treatment is recommended. Cetirizine is not effectively removed by haemodialysis.

Cetirizine is contraindicated in: Hypersensitivity to any of the constituents of this formulation, to hydroxyzine or to any piperazine derivatives.
Patients with severe renal impairment at less than 10 mL/min creatinine clearance.

(Based on the Ministry of Public Health's Announcement): This medicine may cause drowsiness therefore should not drive or operate machinery or perform activities which may be at risk of falling from the height.
While using this medicine, should not drink alcohol or anything that is mixed with alcohol.
This medicine should not be used in the first trimester pregnancy, breast-feeding and children below 2 years.
Use with caution in combination with CNS suppressants e.g., benzodiazepines and antidepressant drugs.
This medicine should be used with caution in patients with liver or renal diseases.
This medicine may cause blurred vision, confusion and dysuria.

Precaution is recommended when Cetirizine concomitant use with alcohol.
Patients should be warned that additive CNS depressants may occur when Cetirizine is administered concomitantly with other CNS depressants (e.g., alcohol, sedatives, tranquilizers) and should be advised to avoid such concomitant use.
Use with caution in patients with predisposing factors of urinary retention (e.g., spinal cord lesion, prostatic hyperplasia), as Cetirizine may increase the risk of urinary retention.
Caution in epileptic patients and patients at risk of convulsion is recommended.
Pruritus and/or urticaria may occur when Cetirizine is stopped, even if those symptoms were not present before treatment initiation. In some cases, the symptoms may be intense and may require treatment to be restarted. The symptoms should resolve when the treatment is restarted.
Use antihistamines with caution in patients with narrow-angle glaucoma, renal impairment, hepatic impairment, stenosing peptic ulcer, pyloroduodenal obstruction, symptomatic prostatic hypertrophy, bronchial asthma, increased intraocular pressure, thyroid dysfunction, cardiovascular disease, and hypertension.
Effect on ability to drive and use machine: Objective measurement of driving ability, sleep latency and assembly line performance have not demonstrated any clinically relevant effects at the recommended dose 10 mg.
However, patients who experience somnolence should refrain from driving, engaging in potentially hazardous activities or operating machinery.
Patients intending to drive, engaging in potentially hazardous activities or operating machinery should not exceed the recommended dose and should take their response to the medicinal product into account.

Pregnancy: Because there are no adequate and controlled studies using Cetirizine in pregnant women. Cetirizine should be used during pregnancy only when clearly needed.
Lactation: Cetirizine is present in breast milk. Weigh the potential benefits of drug treatment against potential risk before prescribing this drug during breastfeeding.

Cardiovascular disorders: Tachycardia.
Immune system disorders: Hypersensitivity, anaphylactic shock.
Nervous system disorders: Paraesthesia, convulsions, dysgeusia, dyskinesia, dystonia, syncope, tremor, amnesia, memory impairment.
Hepatobiliary disorders: Hepatic function abnormal, transaminases increased, blood bilirubin increased, blood alkaline phosphate increased, gamma-glutamyl transferase increased, hepatitis.
Musculoskeletal and connective tissue disorders: Arthralgia.
Renal and urinary disorders: Dysuria, enuresis, urinary retention.
Blood and lymphatic disorders: Thrombocytopenia.
Psychiatric disorders: Agitation, aggression, confusion, depression, hallucination, insomnia, tics, suicidal ideation, nightmare.
Eye disorders: Accommodation disorder, blurred vision, oculogyration.
Gastro-intestinal disorders: Diarrhea.
Skin and subcutaneous tissue disorders: Pruritus, rash, urticaria, angioedema, fixed drug eruption, acute generalized exanthematous pustulosis (AGEP).
Metabolism and nutrition disorders: Increased appetite.
Ear and labyrinth disorders: Vertigo.
Investigations: Weight increased.
General disorders and administration site conditions: Asthenia, malaise, oedema.
Skin reactions occurring after discontinuation of Cetirizine: After discontinuation of Cetirizine, pruritus (intense itching) and/or urticaria have been reported.

No interactions were observed in pharmacokinetic interaction studies when Cetirizine was used concomitantly with pseudoephedrine or antipyrine.
No clinically important interactions have been reported in patients receiving Cetirizine concomitantly with azithromycin, erythromycin, or ketoconazole.
Small decrease in the clearance of Cetirizine was observed in a multiple-dose study when theophylline was administered with Cetirizine; disposition of theophylline was not altered by the concomitant administration with Cetirizine.
In particular, concomitant administration of Cetirizine with macrolides or ketoconazole has never resulted in clinically relevant ECG changes. Concomitantly administration of Cetirizine with drugs known to inhibit cytochrome P450 microsomal enzymes (e.g., azithromycin, erythromycin, ketoconazole) has not been associated with clinically important changes in ECG parameters (e.g., QT_c intervals).
In a multiple dose study of ritonavir and Cetirizine, the extent of exposure to Cetirizine was increased by about 40% while disposition of ritonavir was slightly altered further to concomitant Cetirizine administration.
Concomitant use of Cetirizine with CNS depressants (e.g., alcohol, sedatives, tranquilizers) may result in additive CNS depression.

Store below 30°C.

Antihistamines & Antiallergics

R06AE07 - cetirizine ; Belongs to the class of piperazine derivatives used as systemic antihistamines.

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