Montelukast Sodium, the active ingredient in TAIR, is a selective and orally active leukotriene receptor antagonist that inhibits the cysteinyl leukotriene CysLT receptor. Montelukast Sodium is described chemically as [R-(E)]-1-[[[1-[3-[2-(7-chloro-2quinolinyl) ethenyl] phenyl]-3-[2-(1-hydroxy-1-methyl ethyl) phenyl] propyl] thio]methyl]cyclopropaneaceti acid, x 62.74 mm diam salt. The empirical formula is C, HCINNAOS and its molecular weight is 608.18. Monteluk. .8716 mm um is a hygroscopic, optically active, white to off-white powder. Montelukast Sodium is freely soluble in ethanol, methanol and water and practically insoluble in acetonitrile.
MECHANISM OF ACTION:
Montelukast is an orally active compound that binds with high affinity and selectivity to the CyLT1 receptor (n preference to other pharmacologically Important airway receptors, such as the prostanoid, cholinergic, or Badrenergic receptor). Montelukast inhibits physiologic actions of LTD4 at the CysLT1 receptor without any agonist activity.
PHARMACOKINETIC:
Absorption: Montelukast (TAIR) is rapidly absorbed following oral administration, Aher administration of the 10mg chewable tablet to fasted adults, the mean peak Montelukast plasma concentration (Cmax) is achieved in 3 to 4 hours (Tmad. The mean oral bioavailability is 64%. The oral bioavailability and Cmax are not influenced by a standard meal in the morning. For the Montelukast (TAIRO Sing chewable tablet, the mean Cmax is achieved in 2 to 2.5 hours after administration to adults in the fasted state. The mean oral bioavailability is 73% in the fasted state versus 63% when administered with a standard meal in the morning For the Montelukast (TAIR) 4mg chewable tablet, the mean Cmax is achieved 2 hours after administration in pediatric patients 2 to 5 years of age in the fasted state
Distribution: Montelukast is more than 99% bound to plasma proteins. The steady-state volume of distribution of Montelukast averages 8 to 11 ters Studies in rats with radiolabeled Montelukast indicate minimal distribution across the blood-brain barrier. In addition, concentrations of radiolabeled material at 24 hours postdose were minimal in all other tissues.
Metabolism: Montelukast is extensively metabolized. In studies with therapeutic doses, plasma concentrations of metabolites undetectable at steady state in adults and pediatric patients Montelukast are in vitro studies using human liver microsomes indicate that CYP3A4, 208 and 209 are involved in the metabolism of Montelukast. At clinically relevant concentrations, 208 appears to play a major role in the metabolism of Montelukast.
Elimination: The plasma clearance of Montelukast averages 45 ml/min in healthy adults. Following an oral dose of radiolabeled Montelukast, 56% of the radioactivity was recovered in 5-day fecal collections and 0.2% was recovered in urine Coupled with estimates of Montelukast oral bioavailability, this indicates that Montelukast and its metabolites are excreted almost exclusively via the bile.
Special Populations
Hepatic insufficiency: Patients with mild to moderate hepatic insufficiency and clinical evidence of cinhosis had evidence of decreased metabolism of Montelukast resulting in 41% higher mean Montelukast AUC following a single 10mg dose. The elimination of Montelukast was slightly prolonged compared with that in healthy subjects (mean half-life, 74 hours). No dosage adjustment is required in patients with mild to moderate hepatic insufficien cy. The pharmacokinetics of Montelukast (TAIKO in patients with more severe hepatic impairment or hepatitis have not been evaluated.
Renal Insufficiency: Since Montelukast and Its metabolites are not excreted in the urine, the pharmacokinetics of Montelukast were not evaluated in patients with renal insufficiency. No dosage adjustment is recommended in these patients.
Gender: The pharmacokinetics of Montelukast is similar in males and females
DRUG-DRUG INTERACTIONS:
No dose adjustment is needed when Montelukast (TAIFO is coadministered with Theophyine Prednisolone, Oral contraceptives Terfenadine, Digoxin Warfarin, Gemferozil, leraconazole, Thyroid hormones, Sedalivehypnodos, Nonsteroidal antiinflammatory agents, Benzodiazepines, decongestants and Cytochrome P450 (CYP) enzyme Inducer.
STORAGE:
Store in a cool & dry place below 25°C.
Protect from light, heat and moisture.
Keep out of reach of children.
DISCLAIMER
Super Health’s intention is to make sure that its consumers get information that is accurate, reviewed by an expert, and error-free. However, the information mentioned here should not be used as a replacement for the advice of a qualified physician. The information given here is for informational purposes only, and may not cover all possible precautions, side effects, contraindications, or drug interactions. Consult your doctor and discuss your queries related to any medicine or disease.
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