Stadeltine

Levocetirizine HCl.

Active ingredient: Levocetirizine dihydrochloride (Levocetirizine hydrochloride) 5 mg.
Excipients/Inactive Ingredients: Microcrystalline cellulose, lactose monohydrate, low-substituted hydroxypropyl cellulose, magnesium stearate, colloidal anhydrous silica, hypromellose, macrogol 6000, talc, titanium dioxide.

For the symptomatic treatment of allergic rhinitis (including persistent allergic rhinitis) and urticaria in adults and children aged 6 years and above.

Administration: Oral use. Swallow whole with liquid and may be taken with or without food. It is recommended to take the daily dose in one single intake.
Dosage: Adults and adolescents 12 years and above: The daily recommended dose is 5 mg (one film-coated tablet).
Elderly: Adjustment of the dose is recommended in elderly patients with moderate to severe renal impairment (see Renal impairment as follows).
Renal impairment: The dosing intervals must be individualized according to renal function. Refer to the following table and adjust the dose as indicated. To use this dosing table, an estimate of the patient's creatinine clearance (CLcr) in ml/min is needed. The CLcr (ml/min) may be estimated from serum creatinine (mg/dl) determination using the following formula: See equation.

Click on icon to see table/diagram/image

Dosing adjustments for patients with impaired renal function: 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 of the patient and his body weight. There are no specific data for children with renal impairment.
Hepatic impairment: No dose adjustment is needed in patients with solely hepatic impairment. In patients with hepatic impairment and renal impairment, adjustment of the dose is recommended (see Renal impairment as previously mentioned).
Paediatric population: Children aged 6 to 12 years: The daily recommended dose is 5 mg (one film-coated tablet).
Duration of use: Intermittent allergic rhinitis (symptoms experienced for less than four days a week or for less than four weeks a year) has to be treated according to the disease and its history; it can be stopped once the symptoms have disappeared and can be restarted again when symptoms reappear. In case of persistent allergic rhinitis (symptoms experienced for more than four days a week or for more than four weeks a year), continuous therapy can be proposed to the patient during the period of exposure to allergens.
There is clinical experience with the use of levocetirizine for treatment periods of at least 6 months. In chronic urticaria and chronic allergic rhinitis, there is clinical experience of use of cetirizine (racemate) for up to one year.

Symptoms: Symptoms of overdose may include drowsiness in adults. In children, agitation and restlessness may initially occur, followed by drowsiness.
Management: There is no known specific antidote to levocetirizine.
Should overdose occur, symptomatic or supportive treatment is recommended. Gastric lavage may be considered shortly after ingestion of the drug. Levocetirizine is not effectively removed by haemodialysis.

Hypersensitivity to the active substance, to cetirizine, to hydroxyzine, to any other piperazine derivatives or to any of the other excipients listed in Description.
Severe renal impairment at less than 10 ml/min creatinine clearance.

Precaution is recommended with concurrent intake of alcohol.
Caution should be taken in patients with predisposing factors of urinary retention (e.g. spinal cord lesion, prostatic hyperplasia) as levocetirizine may increase the risk of urinary retention.
Caution should be taken in patients with epilepsy and patients at risk of convulsion as levocetirizine may cause seizure aggravation.
Response to allergy skin tests are inhibited by antihistamines and a wash-out period (of 3 days) is required before performing them.
Patients with rare hereditary problems of galactose intolerance, total-lactase deficiency or glucose-galactose malabsorption should not take this medicine.
Pruritus may occur when levocetirizine is stopped even if those symptoms were not present before treatment initiation. The symptoms may resolve spontaneously. In some cases, the symptoms may be intense and may require treatment to be restarted. The symptoms should resolve when the treatment is restarted.
Effects on ability to drive and use machines: Comparative clinical trials have revealed no evidence that levocetirizine at the recommended dose impairs mental alertness, reactivity or the ability to drive and use machines.
Nevertheless, some patients could experience somnolence, fatigue and asthenia under therapy with levocetirizine. Therefore, patients intending to drive, engage in potentially hazardous activities or operate machinery should take their response to the medicinal product into account.
Use in Children: The use of the film-coated tablet formulation is not recommended in children aged less than 6 years since this formulation does not allow for appropriate dose adaptation.

Pregnancy: There are no or limited amount of data (less than 300 pregnancy outcomes) from the use of levocetirizine in pregnant women. However, for cetirizine, the racemate of levocetirizine, a large amount of data (more than 1000 pregnancy outcomes) on pregnant women indicate no malformative or feto/neonatal toxicity. Animal studies do not indicate direct or indirect harmful effects with respect to pregnancy, embryonal/fetal development, parturition or postnatal development.
The use of levocetirizine may be considered during pregnancy, if necessary.
Lactation: Cetirizine, the racemate of levocetirizine, has been shown to be excreted in human. Therefore, the excretion of levocetirizine in human milk is likely. Adverse reactions associated with levocetirizine may be observed in breastfed infants. Therefore, caution should be exercised when prescribing levocetirizine to lactating women.

The following adverse reactions from post-marketing experience are listed by class and frequency: Very common (≥1/10); common (≥1/100 to <1/10); uncommon (≥1/1,000 to <1/100); rare (≥1/10,000 to <1/1,000); very rare (<1/10,000); not known (cannot be estimated from the available data).
Not known: Immune system disorders: hypersensitivity including anaphylaxis.
Metabolism and nutrition disorders: increased appetite.
Psychiatric disorders: aggression, agitation, hallucination, depression, insomnia, suicidal ideation, nightmare.
Nervous system disorders: convulsion, paraesthesia, dizziness, syncope, tremor, dysgeusia.
Ear and labyrinth disorders: vertigo.
Eye disorders: visual disturbances, blurred vision, oculogyration.
Cardiac disorders: palpitations, tachycardia.
Respiratory, thoracic and mediastinal disorders: dyspnoea.
Gastrointestinal disorders: nausea, vomiting, diarrhoea.
Hepatobiliary disorders: hepatitis.
Renal and urinary disorders: dysuria, urinary retention.
Skin and subcutaneous tissue disorders: angioneurotic oedema, fixed drug eruption, pruritus, rash, urticaria.
Musculoskeletal, connective tissues, and bone disorders: myalgia, arthralgia.
General disorders and administration site conditions: oedema.
Investigations: weight increased, abnormal liver function tests.
Description of suspected adverse reactions: After levocetirizine discontinuation, pruritus has been reported.

No interaction studies have been performed with levocetirizine (including no studies with CYP3A4 inducers); studies with the racemate compound cetirizine demonstrated that there were no clinically relevant adverse interactions (with antipyrine, azithromycin, cimetidine, diazepam, erythromycin, glipizide, ketoconazole and pseudoephedrine). A small decrease in the clearance of cetirizine (16%) was observed in a multiple dose study with theophylline (400 mg once a day); while the disposition of theophylline was not altered by concomitant cetirizine administration.
In a multiple dose study of ritonavir (600 mg twice daily) and cetirizine (10 mg daily), the extent of exposure to cetirizine was increased by about 40% while the disposition of ritonavir was slightly altered (-11%) further to concomitant cetirizine administration.
The extent of absorption of levocetirizine is not reduced with food, although the rate of absorption is decreased.
In sensitive patients, the concurrent administration of cetirizine or levocetirizine and alcohol or other CNS depressants may cause additional reductions in alertness and impairment of performance.

Store in a well-closed container, in a dry place. Do not store above 30°C.

Antihistamines & Antiallergics

R06AE09 - levocetirizine ; Belongs to the class of piperazine derivatives used as systemic antihistamines.

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