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INFORMATION FOR THE USER

Levocetirizine dihydrochloride 5mg + Montelukast 10mgTablets

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
Montelukast sodium – 10mg

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.

Montelukast is a leukotriene receptor antagonist. It blocks the actions of cysteinyl leukotrienes at the CysLT1 receptor on target cells such as bronchial smooth muscle via receptor antagonism and improves asthma symptoms, reduces asthma exacerbations and limits markers of inflammation.

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.
Montelukast is an orally active compound which binds with high affinity and selectivity to the CysLT1 receptor. It inhibits bronchoconstriction at doses as low as 5 mg. Bronchodilation was observed within 2 hours of oral administration. Treatment with montelukast inhibited both early- and late phase bronchoconstriction due to antigen challenge. Montelukast, compared with placebo, decreased peripheral blood eosinophils in adult and paediatric patients. In a separate study, treatment with montelukast significantly decreased eosinophils in the airways (as measured in sputum) and in peripheral blood while improving clinical asthma control.
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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 body clearance of levocetirizine is correlated to the creatinine clearance. It is therefore recommended to adjust the dosing intervals, based on creatinine clearance in patients with moderate and severe renal impairment.
Montelukast is rapidly absorbed following oral administration. The mean peak plasma concentration (Cmax) is achieved 3 hours (Tmax) after administration in adults. The mean oral bioavailability is 64%. The oral bioavailability and Cmax are not influenced by a standard meal. Safety and efficacy were demonstrated in clinical trials.
Montelukast is more than 99% bound to plasma proteins. Studies indicate minimal distribution across the blood-brain barrier.
Montelukast is extensively metabolised. In studies with therapeutic doses, plasma concentrations of metabolites of montelukast are undetectable at steady state in adults and children.
The plasma clearance of montelukast averages 45 ml/min in healthy adults. Montelukast and its metabolites are excreted almost exclusively via the bile.

5.INDICATIONS:
Levocetirizine and Montelukast tabletsare indicated forthe relief of nasal and ocular symptoms of seasonal and perennial allergic rhinitis including sneezing, coughing, itchy watery eyes etc.
6. CONTRAINDICATIONS:
Hypersensitivity to levocetirizine,montelukastor 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.
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.
Physicians should be alert to eosinophilia, vasculitic rash, worsening pulmonary symptoms, cardiac complications, and/or neuropathy presenting in their patients. Patients who develop these symptoms should be reassessed and their treatment regimens evaluated.
Does not alter the need for patients with aspirin-sensitive asthma to avoid taking aspirin and other non-steroidal anti-inflammatory drugs.

8. ADVERSE EFFECTS:
Nervous system disorders:Headache, drowsiness, dizziness
Gastrointestinal disorders:Nausea, dyspepsia, abdominal pain, diarrhoea
General disorders and administration site conditions:Fatigue
Immune system disorders: Hypersensitivity reactions
Psychiatric disorders: Insomnia, nervousness, sleep disorders or nightmares/excessive dreaming
Cardiac disorders:Tachycardia, palpitations
Skin and subcutaneous tissue disorders:Rash, urticaria, pruritus

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.
Not recommended for use in children below age 6 due to insufficient data on safety and efficacy.
Elderly:dosenot needed to be reduced in elderly patients provided 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.
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.