Montelukast
Montelukast. Leukotriene CysLT1 receptor antagonist — blocks LTD4 / LTE4 bronchoconstriction. Adjunctive asthma + allergic rhinitis. FDA… Oral half-life 4.9 h.
Leukotriene CysLT1 receptor antagonist — blocks LTD4 / LTE4 bronchoconstriction. Adjunctive asthma + allergic rhinitis. FDA black-box (2020) for neuropsychiatric adverse events including suicidality.
PK: ITS CITATION IS INTERNALLY CONTRADICTORY AND SHOULD NOT HAVE BEEN THE SOURCE WHATEVER WE STORED — it reports concentrations holding inside a narrow band "at 0.5-12 hours" while also reporting a 2.63 h elimination half-life, which over that span would require a nine-fold fall. Its stored half-life of 4 h matches neither figure in it, and V 24 L is 0.34 L/kg times an assumed weight, a computed APPARENT volume paired with an independent bioavailability and two and a half times the measured intravenous one. All four values now come from one study with rising intravenous doses followed by an oral tablet in the same subjects: "CL, Vss ... were 45.5 ml/min, 10.5 l" and "the AUC, Cmax, Tmax, apparent t1/2, MAT, and bioavailability (F) ... averaged 2441 ng.hr/ml, 385 ng/ml, 3.7 hr, 4.9 hr, 3.4 hr, and 66%". THE LOPERAMIDE QUESTION ANSWERS IN THIS RECORD FAVOUR WITH DIRECT PROOF: intravenous and oral montelukast were run head to head in 51 asthmatics, and the intravenous arm moved lung function within fifteen minutes — the target is unambiguously plasma-coupled.
Pharmacokinetics
- Oral — t½ 4.9 h · F 66% · Vd 10.5 L
Sources: PMID:7621356, PMID:8692739, PMID:10722763