TITLE:
More Rapid Sleep Onset with Lingual-Spray vs Oral-Tablet Delivery Zolpidem
AUTHORS:
Robert B. Raffa, Gerwin Westfield
KEYWORDS:
Zolpidem, Lingual Spray, Pharmacokinetics, Efficacy, Safety/Tolerability, AMBIEN
JOURNAL NAME:
Pharmacology & Pharmacy,
Vol.10 No.7,
July
31,
2019
ABSTRACT: Insomnia and related sleep disorders (somnipathies) affect
a large segment of the population, and result in a significant negative impact
on quality of life and reduced or lost productivity. The speed of sleep onset
is a critical characteristic of successful pharmacotherapeutic intervention for
insomnia. Zolpidem, a non-benzodiazepine
benzodiazepine receptor agonist (nBzRA) is widely used to treat
insomnia. Although not itself a benzodiazepine (BZD), zolpidem has high binding affinity for the benzodiazepine
receptor, which acts as a positive allosteric modulator of the GABAA receptor
complex. It therefore increases the neuronal transmembrane influx of Cl- ions, thereby decreasing neuronal excitability and promoting sleep. In this
four-way crossover, dose-ranging, multiple-treatment study, a lingual spray formulation
of zolpidem was safe and well-tolerated and yielded
more rapid pharmacokinetics (mean plasma concentration) and efficacy (visual
analog scale and digit symbol substitution test) compared to oral tablets.