Lukastma

Properties

Lukastma combines the action of the antileukotriene montelukast with desloratadine, which is a long-acting, non-sedating histamine antagonist with potent antagonist activity of peripheral histamine H1 receptors. Desloratadine has demonstrated antiallergic, antihistamine and anti-inflammatory activity. Montelukast is a selective active leukotriene receptor antagonist that specifically inhibits the cysteinyl leukotriene receptor CysLT1.

Cysteinyl leukotrienes (LTC4, LTD4, LTE4) are potent inflammatory eicosanoids released by various cells, including mast cells and eosinophils.
These important proasmatic mediators bind to and cause various actions in cysteinyl leukotrienes (CysLT) receptors found in human airways, including bronchoconstriction, mucous discharge, vascular permeability, and eosinophil recruitment.

CysLT receptors have been linked to the pathophysiology of asthma and allergic rhinitis. In asthma, leukotriene mediated effects include bronchoconstriction, mucous secretion, vascular permeability, and eosinophil recruitment. In allergic rhinitis, cysteinyl leukotriene (CysLT) receptors are released from the nasal mucosa after exposure to the allergen during early and late phase reactions, and are associated with symptoms of allergic rhinitis. The intranasal challenge test with CysLT has been shown to increase resistance of the nasal airways and symptoms of nasal obstruction. For this reason, blocking the action of leukotrienes improves asthma symptoms and helps prevent asthma attacks. In addition, blocking leukotrienes improves the symptoms of allergic rhinitis (seasonal or perennial also known as indoor or outdoor nasal allergy).

Indications

Lukastma is indicated as an adjunctive alternative treatment for allergic rhinitis, when there has been no or insufficient response when using each of the components separately.

Drug interactions

Montelukast and Desloratadine can be administered with other therapies commonly used in the prophylaxis and treatment of allergic rhinitis. In drug interaction studies, the recommended dose of montelukast had no clinically important effect on the pharmacokinetics of the following drugs: theophylline, prednisone, prednisolone, oral contraceptives (estradiol ethinyl / norethindrone 35/1), terfenadine, digoxin, and warfarin. The area under the plasma concentration-time curve (AUC) for montelukast was decreased by approximately 40% in people with co-administration of phenobarbital. No dosage adjustment of montelukast is recommended.

No clinically significant changes in plasma concentrations of desloratadine were observed in multi-dose drug interaction studies conducted with ketoconazole, erythromycin, azithromycin, fluoxetine, and cimetidine.


Contraindications

Hypersensitivity to desloratadine and montelukast or any excipient in the product.

Cautions

Some cases related to sleep disorders and behavior / mood changes have been reported in isolation for the montelukast molecule. Similarly, it should be borne in mind that, like other leukotriene receptor-blocking drugs, montelukast could produce hepatotoxicity (in some cases, possibly due to an idiosyncratic mechanism), which is why you should be alert and establish a medical surveillance program in this regard.

Side effects

The most common side effects are headache, sore throat, and rash. Abdominal pain, fatigue, dizziness, or dyspepsia have also been observed.

It is recommended to evaluate the dose administered in elderly patients (65 to 70 years old), taking into account that some of them may present altered liver and / or kidney function or concomitant diseases. The dose should be adjusted in patients with impaired liver and / or kidney function, since the elimination half-life, AUC, and plasma concentrations may be increased.

Warnings

Sale under prescription. Keep out of reach of children.

Composition

Adult Lukastma

Each coated tablet contains:

Desloratadine     5.0mg

Monosodium montelukast

Eqv. Montelukast     10.0mg

C.S.P. excipients


Administration route

Oral


Posology

Patients older than 12 years and adults: 1 adult lukastma coated tablet every night.


Presentation

Adult Lukastma: Box containing 1 blister with 10 coated tablets.

 


Storage Recommendations

Store below 30 °C. Protect  from moisture.