A-Leaze

Levocetirizine dihydrochloride.

Each tablet contains Levocetirizine dihydrochloride 5 mg.

Pharmacology: Pharmacodynamics: Levocetirizine is the R-enantiomer of cetirizine. Levocetirizine is a third generation antihistamine and is selective for peripheral H₁-receptors. Levocetirizine is less sedating.
Levocetirizine (at half dose the dosage of cetirizine) appears to be as potent as cetirizine in inhibiting histamine-inducing sneezing, increased nasal airway resistance, and skin wheal and flare.
Pharmacokinetics: Absorption: Levocetirizine is rapidly and extensively absorbed following oral administration with peak plasma concentration usually attained in 0.9 hour. Antihistaminic effects occur within 1 hour. Antihistaminic effects persist for at least 24 hours. A high-fat meal reduces peak plasma concentration by about 36% and delays time to peak plasma concentration by 1.25 hours, but has no effect on AUC.
Distribution: Volume of distribution is 0.4 L/kg. Levocetirizine is approximately 91-92% bound to plasma protein.
Metabolism: Hepatic metabolism is limited extent, less than 14% by aromatic oxidation, N-dealkylation, O-dealkylation, and taurine conjugation.
Excretion: Levocetirizine and metabolites is excreted via urine (85.4%) (via glomerular filtration and active tubular secretion) and in feces (12.9%). Half-life is approximately 8-9 hours in adults.

Levocetirizine is indicated for the treatment of symptoms associated with allergic conditions such as: Seasonal allergic rhinitis (including ocular symptoms); Perennial allergic rhinitis; Persistent allergic rhinitis; Chronic urticaria.

Recommended dose and mode of administration: Levocetirizine is administered orally once daily in the evening. Tablet must be taken orally, swallowed whole with liquid and may be taken with or without food.
Adults and adolescents 12 years and above: The daily recommended dose is 5 mg.
Children aged 6 to 12 years: The daily recommended dose is 5 mg.
Children aged 2 to 6 years: It is recommended to use an oral solution.
The daily recommended dose is 2.5 mg. (Administer in 2 intakes of 1.25 mg.)
Children aged less than 2 years: The administration of Levocetirizine to infants and toddlers aged less than 2 years is not recommended.
Patients with renal impairment: The dosing intervals must be individualized according to renal function. To use this dosing table, an estimate of the patient's creatinine clearance (CL_cr) in mL/min is needed. (See table.)

Click on icon to see table/diagram/image

Patients with hepatic impairment: No dosage adjustment is required in patients with hepatic impairment.
Route of administration: For oral use.
Duration of use: Intermittent allergic rhinitis (symptoms < 4 days/weeks or during less than 4 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.
Persistent allergic rhinitis (symptoms > 4 days/weeks or for more than 4 weeks a year), continuous therapy can be proposed to the patient during the period of exposure to allergens.

Symptoms of overdose may include drowsiness in adults and initially agitation and restlessness, followed by drowsiness in children.
There is no specific antidote to Levocetirizine.
Overdose occur, symptomatic or supportive treatment is recommended.
Levocetirizine is not effectively removed by hemodialysis.

Patients with a history of hypersensitivity to Levocetirizine, cetirizine, hydroxyzine, any piperazine derivative or any other ingredient of the product.
Patients with severe renal impairment at less than 10 mL/min creatinine clearance and patients undergoing hemodialysis.

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 antidepressants drugs.
This medicine should be used with caution in patients with liver or renal diseases.
This medicine may cause blurred vision, confusion and dysuria.

Avoid concomitant use with alcohol.
Use with caution in patients with predisposing factors of urinary retention (e.g. spinal cord lesion, prostatic hyperplasia), as Levocetirizine may increase the risk of urinary retention.
Effects on ability to drive and use machine: Although drowsiness is rare, nevertheless patients should be advised that it can occur and may affect performance of skilled tasks (e.g. operating machinery or driving a motor vehicle).
Use in Children: The administration of Levocetirizine to infants and toddlers aged less than 2 years is not recommended.

Pregnancy: Pregnancy category B: No reports describing use of Levocetirizine in human pregnancy have been located. The animal reproduction data suggest low risk.
Lactation: Cetirizine is excreted in human milk. Levocetirizine are expected to be excreted in breast milk.
Weigh the potential benefits of treatment against potential risks before prescribing Levocetirizine during breast-feeding.

Nervous system disorders: headache, somnolence.
Gastrointestinal disorder: dry mouth, abdominal pain.
General disorders: fatigue, asthenia.

Concomitant use of Levocetirizine and CNS suppressants or alcohol (Ethyl) may enhance the CNS suppressant effect. Concomitant use should be avoided.
Concomitant use of Levocetirizine and ritonavir may result in increased exposure of Levocetirine.
Concomitant use of Levocetirizine and theophylline may decrease in the clearance of cetirizine.

Store below 30°C.

Antihistamines & Antiallergics

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

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