PHARMACOKINETICS AND PHARMACODYNAMICS:
Zolpidem 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 relaxant 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. Zolpidem is preferentially fixed under the omega 1 subtype. In humans, zolpidem shortens sleep time, reduces the number of nocturnal awakenings, increases sleep duration and improves its quality. These effects are associated with a characteristic electro-encephalographic profile, which differs from that of benzodiazepines. Overnight sleep monitoring studies have shown that zolpidem prolongs phase II, as well as phases III and IV (deep sleep). At the recommended dose, zolpidem does not influence the total duration of paradoxical sleep (REM or Rapid Eye Movements).
Absorption: After oral administration, zolpidem has a bioavailability of approximately 70% with a maximum plasma concentration between 0.5 and 3 hours.
Both the absorption and the onset of the hypnotic effect of zolpidem are rapid. At therapeutic doses, it shows linear kinetics. The therapeutic plasma level is between 80 and 200 ng/mL. With zolpidem sublingual tablet maximum plasma concentrations are achieved between 0.25 and 3.5 hours after administration. The mean time to Cmax was similar compared to a conventional tablet. However, early plasma concentrations at 5-15 minutes were higher with zolpidem Sublingual Tablet.
Distribution: At therapeutic doses, its pharmacokinetics is linear. Plasma protein binding is approximately 92%. The volume of distribution in adults is 0.54 ± 0.02 L/Kg and decreases to 0.34 L/kg in elderly people.
First-pass metabolism in the liver corresponds to approximately 35%. It has been shown that repeated administration does not modify protein binding, indicating the absence of competition between zolpidem and its metabolites for binding sites.
Elimination: The elimination half-life is short. Zolpidem is eliminated as inactive metabolites (hepatic metabolism), mainly in urine (about 60%) and feces (about 40%). It does not have an inducing effect on liver enzymes.
The mean value of the elimination half-life of zolpidem after administration was 2.85 hours (5 mg) and 2.65 hours (10 mg). The duration of action of zolpidem is up to 6 hours.
The plasma elimination half-life is on average 2.4 hours (0.7-3.5 hours).
All metabolites are pharmacologically inactive and are excreted in urine (56%) and feces (37%).
In trials, zolpidem has been shown not to be dialyzable.
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. No dose adjustment is necessary in patients with compromised renal function.
The other kinetic parameters are not modified. Zolpidem is not dialyzable.
In patients with severe hepatic impairment, the bioavailability of zolpidem is increased. Its clearance is significantly reduced and the elimination half-life is prolonged (approximately 10 hours).
Pharmacodynamics:
Pharmacotherapeutic group: Hypnotics and Sedatives, Drugs related to benzodiazepines.
ATC code: N05CF02.
Zolpidem, an imidazopyridine, is a hypnotic agent analogous to benzodiazepines. In experimental studies, it has been shown to have sedative effects at doses lower than those necessary to exert anticonvulsant, muscle-relaxing or anxiolytic effects. These effects are related to a specific agonist action on central receptors belonging to the “macromolecular GABAA-ω receptor complex (BZ1 and BZ2)”, which modulates the opening of the chloride ion channel. Zolpidem acts mainly on the ω1 (BZ1) receptor subtypes.
Zolpidem has been shown to be effective in the short-term treatment of insomnia, which is characterized by difficulties initiating sleep.
In general, zolpidem sublingual tablets at a dose of 5 mg reduce the latency period to persistent sleep by approximately ten minutes compared to conventional tablets containing 10 mg.
Zolpidem also stimulates sleep maintenance. No differences have been observed in sleep maintenance efficacy parameters (wakefulness after sleep onset and total sleep duration) between sublingual tablets and conventional oral tablets.
Zolpidem is indicated for the short-term treatment of transient insomnia. A study showed usefulness in the treatment of chronic insomnia, NOCTE® allows rapid falling asleep, reduces the number of nocturnal awakenings, increases the duration of sleep and improves its quality.
What shipping methods do you offer?
Currently there is only one shipping method available: regular airmail delivery (10-12 business days) via Mexican postal service, USPS, CANADA POST, and PARCEL FORCE.
Regular airmail is an inexpensive and reliable option.
Tracking information:
Please note that while regular airmail can also be tracked in most cases, the tracking information is available only on delivery (or attempted delivery) of the order. This allows us to see if your order was delivered successfully, but does not provide real-time delivery details.
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At the moment we offer 1 shipping option:
Regular Airmail Delivery (10-12 business days)
Once your order has been shipped, we will send you an email to notify you that your product has left our facilities. From this point on, your product is only 15-24 business days.
Please note that orders are shipped on business days only (Monday through Friday, excluding holidays).
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Do you ship internationally?
yes
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The currency used will be the US dollar.
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Your order will be properly packaged for your protection in transit to destination.
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We ship from our office in Acapulco, Gro. Mexico
Where are the drugs you have to sell made?
Most of the drugs we offer are manufactured in Mexico, some are manufactured in countries such as Germany, England, France and others, all manufactured by large multinational laboratories legally established in Mexico.
What is the expiration date of the medications I receive?
We offer the guarantee that your product will have at least 10 months of use at the time of sale, however most of the drugs we sell have an expiration date greater than 1 to 2 years
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Read the refund and cancellation policy
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