elbien is an imidazopyridine derivative that acts by binding to the benzodiazepine (BZD) receptors of the GABA receptor complex resulting in neuronal hyperpolarisation,
action potential inhibition, increased in chloride conductance and decreased in neuronal excitability.
It has strong sedative action but only minimal anxiolytic, myorelaxant and anticonvulsant properties due to its selectivity for the BZ1-receptor over the BZ2-receptor.
Belbien has a rapid onset but short duration of hypnotic action.
Effects on the central nervous system (CNS)
This drug has CNS depressant effects, which may include somnolence, decreased alertness, sedation, drowsiness, dizziness, and other changes in psychomotor function .
Due to the above effects, the FDA has recommended an initial dose of zolpidem (immediate-acting) is a single dose of 5 mg for women and a single dose of 5 or 10 mg for men,
immediately before bedtime with at least 7-8 hours remaining before the planned time of awakening.
Uses
Belbien is used for the short-term treatment of insomnia characterized by difficulties with sleep initiation.
Belbien has been shown to decrease sleep latency for up to 35 days in controlled clinical studies ,
The clinical trials performed in support of efficacy were 4-5 weeks in duration with the final formal assessments of sleep latency performed at the end of treatment.
Belbien is also used to associated treatment for these conditions: Insomnia
How Belbien works
Belbien, the active moiety of zolpidem tartrate, is a hypnotic substance with a chemical structure that is not related to the structure benzodiazepines, barbiturates,
pyrrolopyrazines, pyrazolopyrimidines or other drugs exerting hypnotic effects.
It interacts with a GABA-BZ receptor complex and shares various pharmacological properties with the benzodiazepine class of drugs .
Subunit binding of the GABAA receptor chloride channel macromolecular complex is thought to lead to the sedative, anticonvulsant, anxiolytic, and myorelaxant drug effects of zolpidem.
The main regulatory site of the GABAA receptor complex can be found on its alpha (α) subunit and is called the benzodiazepine (BZ) or omega (ω) receptor.
At least three different subtypes of the (ω) receptor have been identified to this date .
In contrast to benzodiazepine drugs, which are found to modulate all benzodiazepine receptor subtypes in a non-selective fashion,
zolpidem binds the (BZ1) receptor specifically with a potent affinity for the alpha 1/alpha 5 subunits (in vitro) .
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