DESCRIPTION
Montelukast -Montelukast is a leukotriene receptor antagonist (LTRA) used for the maintenance treatment of asthma and to relieve symptoms of seasonal allergies. It is usually administered orally. Montelukast blocks the action of leukotriene D4 on the cysteinyl leukotriene receptor CysLT1 in the lungs and bronchial tubes by binding to it. This reduces the bronchoconstriction otherwise caused by the leukotriene, and results in less inflammation. Because of its method of operation, it is not useful for the treatment of acute asthma attacks. Again because of its very specific locus of operation, it does not interact with other allergy medications such as theophylline. Montelukast is marketed in United States and many other countries by Merck & Co. with the brand name Singulair®. It is available as oral tablets, chewable tablets, and oral granules. In India and other countries, it is also marketed under the brand name Montair®, produced by Indian company Cipla.Fexofenadine – Fexofenadine hydrochloride (Allegra) is an antihistamine drug used in the treatment of hayfever and similar allergy symptoms. It was developed as a successor of and alternative to terfenadine. Fexofenadine, like other second and third-generation antihistamines, does not readily pass through the blood-brain barrier, and so causes less drowsiness than first-generation histamine-receptor antagonists.
CATEGORIES
Montelukast -Anti-Arrhythmia Agents,Fexofenadine -Anti-Allergic Agents,Histamine H1 Antagonists, Non-Sedating,Histamine Antagonists.
CHEMICAL FORMULA
Montelukast -C35H36ClNO3S,Fexofenadine – C32H39NO4.
COMPOSITION
Montelukast 10mg + Fexofenadine 120mg
INDICATION
Montelukast -For the treatment of asthma,Fexofenadine – For management of Seasonal allergic rhinitis.
PHARMACODYNAMICS
Montelukast -Montelukast, like zafirlukast, is a leukotriene receptor antagonist used as an alternative to anti-inflammatory medications in the management and chronic treatment of asthma and exercise-induced bronchospasm (EIB). Unlike zafirlukast, montelukast does not inhibit CYP2C9 or CYP3A4 and is, therefore, not expected to affect the hepatic clearance of drugs metabolized by these enzymes.Fexofenadine -Fexofenadine is a second-generation, long lasting H1-receptor antagonist (antihistamine) which has a selective and peripheral H1-antagonist action. Histamine is a chemical that causes many of the signs that are part of allergic reactions, such as the swelling of tissues. Histamine is released from histamine-storing cells (mast cells) and attaches to other cells that have receptors for histamine. The attachment of the histamine to the receptors causes the cell to be “activated,” releasing other chemicals which produce the effects that we associate with allergy. Fexofenadine blocks one type of receptor for histamine (the H1 receptor) and thus prevents activation of cells by histamine. Unlike most other antihistamines, Fexofenadine does not enter the brain from the blood and, therefore, does not cause drowsiness. Fexofenadine lacks the cardiotoxic potential of terfenadine, since it does not block the potassium channel involved in repolarization of cardiac cells.
No Information
ABSORPTION
Montelukast -Rapidly absorbed following oral administration (bioavailability is 64%),Fexofenadine – 33%.
VOLUME DISTRIBUTION
Montelukast -8 to 11 L,
METABOLISM
Montelukast -Hepatic,Fexofenadine – Approximately 5% of the total dose is metabolized, by cytochrome P450 3A4 and by intestinal microflora.
ELIMINATION
Montelukast -Coupled with estimates of montelukast oral bioavailability, this indicates that montelukast and its metabolites are excreted almost exclusively via the bile.
HALF LIFE
Montelukast -2.7-5.5 hours,Fexofenadine – 14.4 hours.
TOXICITY
Montelukast -Side effects include headache, abdominal or stomach pain, cough, dental pain, dizziness, fever, heartburn, skin rash, stuffy nose, weakness or unusual tiredness.Fexofenadine – Side effects include dizziness, drowsiness, and dry mouth..
FOOD INTERACTIONS
avoid alcohol
SIDE EFFECTS
Montelukast -Flu-like signs. These include headache, weakness, fever, shakes, aches, pains, and sweating. Mild pain drugs may help. Nervous and excitable. Headache. Belly pain. Upset stomach or throwing up. Many small meals, good mouth care, sucking hard, sugar-free candy, or chewing sugar-free gum may help. Nose stuffiness.Fexofenadine – Feeling lightheaded, sleepy, having blurred eyesight, or a change in thinking clearly. Avoid driving and doing other tasks or actions that call for you to be alert or have clear eyesight until you see how this drug affects you. – Headache.