Levocetirizine & Montelukast Syrup

(PRESENTATION: Levocetirizine HCl 2.5 mg + Montelukast 4 mg
syrup per 5 ml in a Amber Bottle )

Montelukast: Leukotriene receptor antagonists. (is used for maintenance treatment of asthma and to relive symptoms of seasonal allergies) It is a selective and orally active leukotrien antagonist that inhibits the cysteinyl leukotrien CysLT1 receptor.
Levocetirizine: Third – generation non – sedative antihistamine. (is prevents the release of other allergy chemicals and increased blood supply to the area, and provides relief from the typical symptoms of hay fever). Levocetirizine, the R – entaiomer of Cetirizine, is a potent and selective antagonist of peripheral H1 – receptors.
It has been demonstrated by recent studies concomitant administration of an antileukotrien (montelukast) and an antihistamine (levocetirizine), shows significantly better symptoms relief compared with the modest improvement of rhinitis symptomatology with each of the treatments alone.

Perennial allergic rhinitis
Chronic idiopathic urticarial
Asthma
Exercise-Induced Bronchospasm

Levocetirizine selectively inhibits the H1 receptor and prevents the release of histamine which causes smooth muscle contraction, increase vascular permeability, stimulation of cough. All this acitivities is blocked by levocetirizine.
Montelukast is a leukotriene receptor antagonist that demonstrates a marked affinity and selectivity to the cysteinyl leukotriene receptor type-1 in preference to many other crucial airway receptors like the prostanoid, cholinergic, or beta-adrenergic receptors. Leukotrienes are eicosanoids released by a variety of cells like mast cells and eosinophils. They bind to corresponding CysLT receptors located on respiratory airway smooth muscle cells, airway macrophages, and on various pro-inflammatory cells like eosinophils and some specific myeloid stem cells activities that facilitate the pathophysiology of asthma and allergic rhinitis are stimulated.

Levocetirizine is well orally absorbed and is highly bound to plasma proteins. It is poorly metabolized, but undergoes O-dealkylation and glucuronide conjugation. The half-life of levocetrizine is 8-9 hours.
Montelukast is quickly absorbed from GIT with the bioavailability of 64%. The average volume of distribution of montelukast is 8-11 L with protein binding exceeding 99%. It is majorly metabolised by CYP enzyme family and is excreted into bile and feces with a half-life of 2.7-5.5 hours.

Headache
Upset stomach
Nausea
Diarrhea
Dizziness
Skin Rash

Hypersensitivity, pregnant patients, patients with blood and lymphatic system disorder and psychiatric disorder.

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