NOTIX ZOLPIDEM 10MG 30 TABLETS

Description

PHARMACOKINETICS AND PHARMACODYNAMICS:

Pharmacokinetics:

Absorption: After oral administration, NOTIX has a bioavailability of approximately 70% with a maximum plasma concentration between 0.5 and 3 hours.

Distribution: Its pharmacokinetics is linear. Plasma protein binding is approximately 92%. The volume of distribution in adults is 0.54 ± 0.02 L/kg.

Metabolism: Hepatic metabolism of NOTIX produces inactive metabolites that are mainly excreted in the urine. NOTIX is a substrate for the hepatic oxidative microsomal isoenzymes CYP1A2 and CYP2D6.

Elimination: It is eliminated in the form of inactive metabolites (hepatic metabolism), mainly in urine (approximately 60%) and feces (approximately 40%). The plasma elimination half-life is on average 2.4 hours (0.7-3.5 hours).

Special populations: In the elderly subject, a decrease in hepatic clearance is observed. The peak concentration is increased by approximately 50% without significant prolongation of the half-life (3 hours on average). The volume of distribution decreases to 0.34 ± 0.05 L/kg.

In patients with renal failure, whether dialyzed or not, a moderate decrease in renal clearance is observed.

In patients with severe hepatic impairment, the bioavailability of NOTIX is increased. Its clearance is significantly reduced and the elimination half-life is prolonged (approximately 10 hours).

Pharmacodynamics: NOTIX is a hypnotic belonging to the imidazopyridine family. Experimental studies have shown a sedative effect at doses lower than those necessary to obtain anticonvulsant, muscle-relaxing or anxiolytic effects. These effects can be explained by a selective agonist action of the macromolecular GABA-omega receptor complex, modulating the opening of the chloride channel.

NOTIX is preferentially fixed under the omega 1 subtype. NOTIX shortens sleep time, reduces the number of nocturnal awakenings, increases sleep duration and improves its quality. These effects are associated with a characteristic electroencephalographic profile, which differs from that of benzodiazepines. Overnight sleep monitoring studies have shown that NOTIX prolongs phase II, as well as phases III and IV (deep sleep).

At the recommended dose, it does not influence the total duration of paradoxical sleep (REM or rapid eye movements).