Telamon Lc


 

COMPOSITION:

Montelukast sodium     10 mg

Levocetirizine                  5 mg

Introduction

Telamon –LC is the combination of montelukast sodium and levocetirizine. Levocetrizine is third generation non-sedative antihistamine. It is derived from second generation cetirizine. It is levo form of cetirizine which belongs to second generation. It causes blocking of histamine receptors and prevents the binding of its receptors. In other words it prevents the release of allergic chemicals and decreased the supply of blood to that area.

Montelukast is a leukotriene receptor antagonist (LTRA). It is mainly used for the treatment of seasonal asthma and symptoms associated with seasonal allergies. It can be taken with or without food. It is also used in many conditions like exercise induced bronchospasm, allergic rhinitis or urticaria.

 

Indication

  • Shortness of breathing caused by asthma
  • Prevention of wheezing
  • Breathing problems occurring during exercise
  • Reduces the use of inhaler
  • Helps in reliving the symptoms associated with hay fever and allergic rhinitis
  • Sneezing, runny, stuffy, itchy nose
  • Seasonal allergic rhinitis
  • Perennial rhinitis
  • Chronic idiopathic urticaria
  • Exercise-induced bronchoconstriction
  • Asthma treatment for pediatric and adults

 

 

Mechanism of action

Montelukast is a leukotriene receptor antagonist (LTRA). It causes antagonism action on leukotriene D4 (LTD4) which is present on cysteinyl leukotriene receptor and Cys LT 1 in human airway. It blocks the action produced by LTD4 which protects airway edema, secretion of thick mucus and smooth muscle contraction.

It can also provide alternative therapy to anti-inflammatory medications for chronic asthma management and exercise induced bronchospasm.

Levocetirizine competes with histamine for binding at H1 receptor on the effectors cell surface which causes the suppression histaminic edema and pruritus. The low incidence of sedation is because the reduced penetration of cetirizine into CNS.

 

Pharmacology

Montelukast

Absorption

It gets rapidly absorbed by the body. The mean plasma concentration is achieved in 3 to 4hrs. The oral bioavailability is about 64%. The bioavailability of the drug is not influenced by meals.

Distribution

About 99% of the drug is bound to plasma proteins. The volume of distribution is about 8-11 liters. The metabolism of the drug is liver by CYP3A4, 2C8 and 2C9.

Excretion

The plasma clearance of montelukast is 45ml/min. Most of the drug is excreted through bile. The plasma half life is 2.7-5.5 hrs.

Levocetirizine

Absorption

It is well absorbed in the body with mean peak plasma concentration (Cmax) of 114 ng/mL at a time (Tmax) of 2.2 hours

Distribution

It is well distributed in the body with 93% plasma protein binding. Vd is 0.41kg

Excretion

 The plasma half life is 7.9 ± 1.9 hours; total body clearance is 0.63 ml/min/kg

 

 

Contraindications

  • Hypersensitivity to any of the product
  • Patients with hypersensitivity to such drugs
  • Renal disease
  • Pediatric patients with renal impairment

 

Precautions

  • Long treatment can cause  somnolence, fatigue, and asthenia
  • Patient should not involved in those task which require complete concentration
  • Patients with predisposing factors of urinary retention
  • Use in pregnant patients when clearly needed
  • Reversal of bronchospasm in acute asthma attacks
  • Exacerbations of asthma after exercise