Human pharmacokinetics of dihydroergotamine administered by nasal spray.

摘要: Objectives A nasal spray of dihydroergotamine was developed for the treatment migraine headaches, and pharmacokinetic studies were scheduled to evaluate bioavailability by this new route administration. Methods Nine performed with administered versus intramuscular route, linearity kinetics, interindividual intraindividual variations, influence different factors. Results Nasally (1 mg) becomes rapidly available systemic circulation, peak plasma levels 1 ng/ml achieved in 0.9 hour. The relative is 38.4%. Dihydroergotamine exhibits linear dose proportionality 4 mg). Intraindividual variations evaluated a 1-year period higher (29%) than those found (20%) but comparable oral route. Interindividual greater (25% 14% route) Caffeine contained solution (1%) had no effect on absorption. Vasomotor phenomena, which could also affect mucosa during headache, do not modify bioavailability. constriction fenoxazoline leads slight decrease (−15%) presence acute viral rhinitis did result any change absorption compared normal state mucosa. From point view, nasally can be given, without risk overdose, patients receiving long-term medication. Conclusion These results show reliability reproducibility administration adapted headaches. Clinical Pharmacology & Therapeutics (1996) 60, 265–275; doi: