Product Code : A-AL-03
PACK : – 20 x 10
Tablets
COMPOSITION:Each film coated tablet contains:
Levocetirizine Dihydrochloride IP 5 mgg
Dosage Form :TABLET
INFORMATION FOR THE USER
Levocetirizine dihydrochloride 5mgTablets
Read all of this information carefully before you start taking this medicine because it contains important information for you.
•Keep this information. You may need to read it again.
•If you have any further questions, ask your doctor, pharmacist or nurse.
•This medicine is prescribed for you only. Do not pass it on to others. It may harm them, even if their signs of illness are the same as yours.
If you get any side effects, talk to your doctor, pharmacist or nurse. This includes any possible side effects not listed in this information.
1.COMPOSITION:
Each film coated tablet contains:
Levocetirizine dihydrochloride – 5mg
For oral use only.
2.DESCRIPTION:
Levocetirizine is a second-generation anti-histamine. They are a class of medications that block the action of histamine at the H1 receptor, helping to relieve allergic reactions.
3.PHARMACOLOGICAL ACTION:
Levocetirizine, the (R) enantiomer of cetirizine, is a potent and selective antagonist of peripheral H1-receptors.
It has a high affinity for human H1-receptors which is 2-fold higher than that of cetirizine. Levocetirizine dissociates from H1-receptors with a half-life of 115 ± 38 min. After single administration, levocetirizine shows a receptor occupancy of 90% at 4 hours.
Pharmacodynamic studies demonstrate that, at half the dose, levocetirizine has comparable activity to cetirizine, both in the skin and in the nose.
In a study comparing the effects of levocetirizine 5mg, desloratadine 5mg, and placebo on histamine-induced wheal and flare, levocetirizine treatment resulted in significantly decreased wheal and flare formation, compared with placebo and desloratadine.
The onset of action of levocetirizine 5 mg in controlling pollen-induced symptoms has been observed at 1 hour post drug.
Levocetirizine inhibits the histamine-mediated early phase of the allergic reaction and also reduces the migration of certain inflammatory cells and the release of certain mediators associated with the late allergic response.
The efficacy and safety of levocetirizine has been demonstrated in several clinical trials performed in adult patients suffering from seasonal allergic rhinitis or perennial allergic rhinitis.
The paediatric safety and efficacy of levocetirizine tablets has been studied and it was found that, levocetirizine significantly improved symptoms and increased health-related quality of life.
Treatment with levocetirizine resulted in significant decrease in pruritus. Levocetirizine also resulted in a larger improvement of health-related quality of life as assessed by the Dermatology Life Quality Index.
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4. CLINICAL PHARMACOKINETICS:
The pharmacokinetics of levocetirizine are linear with dose- and time-independent with low inter-subject variability. No chiral inversion occurs during the process of absorption and elimination.
Levocetirizine is rapidly and extensively absorbed following oral administration. Peak plasma concentrations are achieved 0.9 h after dosing. Steady state is achieved after two days. The extent of absorption is dose-independent and is not altered by food, but the peak concentration is reduced and delayed.
No tissue distribution data are available in humans, neither concerning the passage of levocetirizine through the blood-brain-barrier.
Levocetirizine is 90% bound to plasma proteins. The distribution of levocetirizine is restrictive.
The extent of metabolism of levocetirizine in humans is less than 14% of the dose and therefore differences resulting from genetic polymorphism or concomitant intake of enzyme inhibitors are expected to be negligible.
Due to its low metabolism and absence of metabolic inhibition potential, the interaction of levocetirizine with other substances, or vice-versa, is unlikely.
The plasma half-life in adults is 7.9 ± 1.9 hours. The major route of excretion of levocetirizine and metabolites is via urine. Excretion via feces accounts for only a minor part. Levocetirizine is excreted both by glomerular filtration and active tubular secretion.
Renal impairment:The apparent body clearance of levocetirizine is correlated to the creatinine clearance. It is therefore recommended to adjust the dosing intervals of levocetirizine, based on creatinine clearance in patients with moderate and severe renal impairment.
5. INDICATIONS:
Levocetirizine is indicated for:
– the relief of nasal and ocular symptoms of seasonal and perennial allergic rhinitis
– the relief of symptoms of chronic idiopathic urticaria.
6. CONTRAINDICATIONS:
Hypersensitivity to levocetirizine, to any of the excipients, to hydroxyzine or to any piperazine derivatives.
Patients with severe renal impairment at less than 10 ml/min creatinine clearance.
7. WARNINGS AND PRECAUTIONS:
Do not exceed the stated dose.
The use of levocetirizine dihydrochloride is not recommended in children aged less than 6 years since the currently available film-coated tablets do not yet allow dose adaptation.
At therapeutic doses, no clinically significant interactions have been demonstrated with alcohol. Nevertheless, precaution is recommended if alcohol is taken concomitantly.
Caution in epileptic patients and patients at risk of convulsions is recommended.
8.ADVERSE EFFECTS:
The commonly reported side effects are:
• Sleepiness
• Dizziness andheadache
• Inflammation of the throat
• Swelling and irritation inside the nose (in children)
• Dry mouth
• Feeling sick
• Tiredness
9.DRUG INTERACTIONS:
Due to the pharmacokinetic, pharmacodynamic and tolerance profile of levocetirizine, no interactions are expected with this antihistamine. Actually, neither pharmacodynamic nor significant pharmacokinetic interaction was reported in drug-drug interactions studies performed, notably with pseudoephedrine or theophylline.
10.DOSAGE:
Adults and adolescents 12 years and above: 1 tablet once daily.
Children aged 6 to 12 years: 1 tablet once daily.
Levocetirizine is not recommended for use in children below age 6 due to insufficient data on safety and efficacy.
Elderly:For the time being, there is no data to suggest that the dose needs to be reduced in elderly patients provided that the renal function is normal.
Patients with moderate to severe renal impairment:in cases no alternative treatment can be used, the dosing intervals must be individualized according to renal function.
Patients with hepatic impairment: No dose adjustment is needed in patients with solely hepatic impairment.
11. ADMINISTRATION:
The tablets need to be swallowed with a glass of liquid. Do not crush or break the tablet as it will destroy the film coating.
Dose to be taken on an empty stomach and prior to meals.
12. STORAGE:
Do not store above 25°C. Store in the original package. Keep away from children. Do not expose to direct sunlight.
13. MANUFACTURED BY:
14. MARKETED BY:
Last revised on May 2019.