Pharmacokinetics and safety of montelukast in children aged 3 to 6 months.
The single-dose population estimate of the area under the concentration-time curve (AUC(pop)) from time zero to infinity (AUC(0-infinity)), maximum plasma concentration (C(max)), and time to C(max) (t(max)) of montelukast 4-mg oral granules were investigated in infants aged 3 to 6 months. Montelukast concentrations were quantitated after a single 4-mg dose of montelukast oral granules. Pharmacokinetic parameters were determined using a population-based approach with a nonlinear mixed-effect, 1-compartment model with first-order absorption and elimination. Ninety-five percent confidence intervals for the AUC(pop) ratio (3 to 6 months/6 to 24 months) were determined. Safety and tolerability were assessed. Montelukast 4-mg oral granules in children 3 to 6 months of age yielded systemic exposure (AUC(pop) = 3644.3 +/- 481.5 ng x h/mL) similar to that observed in children aged 6 to 24 months (3226.6 +/- 250.0 ng x h/mL). Systemic exposure after a 4-mg dose of montelukast as oral granules is similar in children aged 3 to 6 months and 6 to 24 months.
Knorr
Barbara
B
Merck Research Laboratories, Respiratory and Allergy Department, RY34B-332, 126 East Lincoln Avenue, Rahway, NJ 07065, USA. Barbara_knorr@merck.com
Maganti
Lata
L
Ramakrishnan
Rohini
R
Tozzi
Carol A
CA
Migoya
Elizabeth
E
Kearns
Gregory
G
D000085:Acetates / Q000009:adverse effects* / Q000493:pharmacokinetics* / Q000627:therapeutic use; D018927:Anti-Asthmatic Agents / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use; D001988:Bronchiolitis / Q000188:drug therapy* / Q000378:metabolism; D003521:Cyclopropanes; D004311:Double-Blind Method; D005260:Female; D006801:Humans; D007223:Infant; D020024:Leukotriene Antagonists / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use; D008297:Male; D011804:Quinolines / Q000009:adverse effects* / Q000493:pharmacokinetics* / Q000627:therapeutic use; D013440:Sulfides
D000085:Acetates; D018927:Anti-Asthmatic Agents; D003521:Cyclopropanes; D020024:Leukotriene Antagonists; D011804:Quinolines; D013440:Sulfides; C093875:montelukast