Pharmacokinetics and safety of montelukast oral granules in children 1 to 3 months of age with bronchiolitis.
The single-dose pharmacokinetics of montelukast 4-mg oral granules and tolerability of daily administration of 2 different doses of montelukast (4 mg and 8 mg given once daily for 7 days) versus placebo were evaluated in 12 infants 1 to 3 months of age with bronchiolitis or a history of bronchiolitis and asthma-like symptoms. The population area under the concentration-time curve estimate after a single 4-mg dose of montelukast was 13 195.7 +/- 2309.8 (standard error) ng.hr/mL, 3.6 times higher than historical values in infants 3 to 24 months of age. Six patients had 10 total clinical adverse experiences; none was considered serious or drug related. Three patients had transient drug-related increases in aspartate aminotransferase (montelukast 8 mg [n = 2]; placebo [n = 1]). Despite increased systemic exposure after administration of a single dose of montelukast 4-mg oral granules in infants 1 to 3 months of age compared with that in pediatric patients 3 to 24 months of age, administration of montelukast at 4 and 8 mg once daily for 7 days in 1- to 3-month-old infants was generally well tolerated.
Kearns
Gregory L
GL
Division of Pediatric Clinical Pharmacology and Medical Toxicology, Children's Mercy Hospitals and Clinics, 2401 Gillham Road, Kansas City, MO 64108, USA. gkearns@cmh.edu
Lu
Susan
S
Maganti
Lata
L
Li
Xiujiang Susie
XS
Migoya
Elizabeth
E
Ahmed
Tuli
T
Knorr
Barbara
B
Reiss
Theodore F
TF
D000085:Acetates / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics*; D018927:Anti-Asthmatic Agents / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics*; D019540:Area Under Curve; D001249:Asthma / Q000188:drug therapy; D001988:Bronchiolitis / Q000188:drug therapy / Q000378:metabolism*; D002675:Child, Preschool; D003521:Cyclopropanes; D004305:Dose-Response Relationship, Drug; D004311:Double-Blind Method; D005260:Female; D006801:Humans; D007223:Infant; D008297:Male; D017711:Nonlinear Dynamics; D011208:Powders; D011804:Quinolines / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics*; D013440:Sulfides
D000085:Acetates; D018927:Anti-Asthmatic Agents; D003521:Cyclopropanes; D011208:Powders; D011804:Quinolines; D013440:Sulfides; C093875:montelukast