Class: Antihistamine, Leukotriene receptor antagonists (LTRAs)

Manufacturer: Sterling Lab 57, SIPCOT Industrial Complex, Hosur-635 126 (T.N.), India.

Dosage Form: Tablet

Similar Brands:

Uses:

Montelukast plus Levocetirizine is indicated for the relief of symptoms associated with seasonal and perennial allergic rhinitis.

Dosage:

Adults

One tablet containing Montelukast 10mg plus Levocetirizine 5mg once daily or as prescribed by the physician

Elderly

Dosages in the elderly should be adjusted in accordance with their renal function.

Patients with renal impairment

In adults and children 12 years of age and older with:

• Mild renal impairment (ClCr 50-80ml/min): one tablet containing Montelukast 10mg plus Levocetrizine 2.5mg once daily.
• Moderate renal impairment (ClCr 30-50ml/min): one tablet containing Montelukast 10mg plus Levocetrizine 2.5mg once daily, every other day.

Patients with Hepatic disease

No dosage adjustment is needed in patients solely with mild to moderate hepatic impairment. Usage is not recommended in patients with severe hepatic impairment.

Children and Adolescent

Children aged 15+: one tablet containing 10mg Montelukast and Levocetirizine 5mg once daily, or as prescribed by the physician.

Side Effects:

Montelukast

Body as whole: asthenia/fatigue, fever, abdominal pain, trauma, digestive system disorders, dyspepsia, infectious gastroenteritis, dental pain.

Nervous system/psychiatric: dizziness, headache.

Respiratory system disorder: congestion, nasal cough, influenza.

Skin/skin appendages disorder; rash

Laboratory adverse experiences; ALT increased, AST increased.

Levocetirizine

The following adverse drug reactions were reported at rates of 1% or greater during treatment with levocetirizine 5mg; headache, somnolence; dry mouth, fatigue.

Further uncommon incidences of adverse reaction like asthenia or abdominal pain were observed. In addition to the adverse reactions reported. In addition to the adverse reactions reported during clinical studies and listed above, very rare cases of the following adverse reactions have been reported in post-marketing experience;

• Immune system disorders; hypersensitivity including anaphylaxix
• Psychiatric disorders; aggregation, agitation.
• Nervous system disorders
• Eye disorders; visual disturbances.
• Cardiac disorders
• Respiratory, thoracic and mediastinal disorders
• Gastrointestinal disorders
• Hepatobiliary disorders;
• Skin and subcutaneous disorders, angioneurotic edema, fixed drug eruption, pruritus, rash, urticarial
• Musculoskeletal connective tissues and bone disorders.
• Instigations: weight gain, abnormal liver function tests.

Warnings & Precautions:

Caution

Foods, Drugs, Devices, and Cosmetics Act prohibits dispensing without prescription.

Levocetirizine

The administration of Levocetirizine to infants and toddlers aged less than 2 years is not recommended. In sensitive patients the simultaneous administration of cetirizine or levocetirizine and alcohol or other CNS depressants may have effects on the central nervous system, although it has been shown that the racemate cetirizine does not potentiate the effect of alcohol.

Renal impairment

Montelukast

No dosage adjustment is recommended for Montelukast in patients with renal impairment.

Levocetirizine

Levocetirizine is known to be substantially excreted by the kidneys and the risk of adverse reactions to this drug may be greeter in patients with impaired renal function.

Hepatic impairment

Montelukast

No dosage adjustment is required in patients with mid-to-moderate hepatic insufficiency. The pharmacokinetics of Montelukast in patients with more severe hepatic impairment or with hepatitis have not been adjusted.

Levocetirizine

As levocetirizine is mainly excreted unchanged by the kidneys, it is unlikely that the clearance of levocetirizine is significantly decreased in patients with solely hepatic impairment.

Pediatric use

Montelukast safety and efficiency of montelukast have been established in adequate and well-controlled studies in pediatric patients with asthma 5 to 14 years of age. Safety and efficiency profiles in this age group are similar to those seen in adults.

The safety and effectiveness of levocetirizine in pediatric patients under 2 years of age have not been established.

Geriatric use

Montelukast

The plasma half-life of Montelukast is slightly longer in the elderly. No dosage adjustment in the elderly is required.

Levocetirizine

In general, dose selection for an elderly patient should be cautious usually starting at the low end of the dosing range reflecting the greater frequency of decreased hepatic, renal or cardiac function and of concomitant disease or other drug therapy.

Effects on ability to drive and use machines

Montelukast

Montelukast is not expected to affect a patient’s ability to drive a car or operate machinery. However, in very rare cases, individuals have reported drowsiness or dizziness.

Pregnancy & Lactation:

Pregnancy

There are no adequate and well controlled studies of either Montelukast or levocetirizine in pregnant women women. Animal studies do not indicate harmful effects with respect to effects on pregnancy or embryonal/foetal development.

Montelukast

Limited data from available pregnancy databases do not suggest a causal relationship relationship between Montelukast and malformations (i.e. limb defects) that have been rarely reported in worldwide post marketing experience.

Levocetirizine

In rats and rabbits, levocetirizine was not teratogenic at oral doses approximately 320 and 390, respectively, times the maximum recommended daily oral dose in adults on a mg/m2 basis. Because animal reproduction studies are not always predictive of human response, this combination should be used during pregnancy only if it is considered to be clearly essential.

Lactation

Montelukast studies in rats have shown have shown that Montelukast is excreted in milk. It is not known if Montelukast is excreted in milk. No peri and postnatal animal studies have been conducted with levocetirizine. Cetirizine has been reported to be excreted to be excreted in human breast milk. Because levocetirizine is also expected to be excreted in human milk this combination is not recommended during lactation.

Drug Interactions:

Montelukast

In drug interactions studies, the recommended clinical dose of Montelukast did not have clinically important effects on the pharmacokinetics of the following drugs: theophylline, prednisone, prednisolone, oral contraceptives (ethinyl estradiol/norethindrone 35/1), terfenadine, digoxin and warfarin.

Levocetirizine

In vitro data indicate that levocetirizine is unlikely to produce pharmacokinetic interactions through inhibition or induction of live drug-metabolizing enzymes. In pharmacokinetic interaction studies performed with racemic cetirizine, cetirizine did not interact with antipyrine, pseudoephedrine, erythromycin, azithromycin, ketoconazole or cimetidine.

Contraindications:

It is contraindicated in patients with known hypersensitivity to Montelukast, levocetirizine or cetirizine, or to any of the excipients.

Price: Ksh 450

Notes:

Pack Size: 10s

Pharmacology

Montelukast

Montelukast is an orally active compound which binds with high affinity and selectively to the cysteinyl leukotriene type 1 receptor thereby preventing cysteinyl leukotriene from exerting their effects.

Levocetirizine

Levocetirizine is the active enantiomer of cetirizine, is an antihistamine. Its principal effects are mediated via selective inhibition of H1 receptors. The antihistamine activity of levocetirizine has been documented in a variety of animal and human models.

Over dosage

There is no data reported on the over dosage of this combination. However, over dosage has been reported with individual molecules.

Montelukast

No specific information is available on the treatment of over dosage with Montelukast.

Levocetirizine

Symptoms of overdose may include drowsiness in adults, and in children, initially agitation and restlessness occur, followed by drowsiness.

Marketed by: MICRO LABS LIMITED #31 Race Course Road, Bangalore 560 001, India.

Ref: PL-1790