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25 May 2020

Pharmacologic Effect

Ambien is a hypnotic drug belonging to the imidazopyridine group, and is a selective agonist of the subclass of omega1-benzodiazepine receptors. It has a sedative effect, while when used in usual doses, it does not have an anxiolytic, central muscle relaxant and anticonvulsant effect.


Buy Ambien fast shipping usa as it excites benzodiazepine receptors (omega) in the alpha subunit of GABA receptor complexes localized in the region of the IV plate of the sensory-motor zones of the cortex, reticular sections of the substantia nigra, visual tubercles of the ventral thalamic complex, bridge, pale ball, etc. Interaction with omega receptors leads to the discovery of neuronal isoform channels for chlorine ions.


It Shortens the time of falling asleep, reduces the number of night awakenings, increases the total duration of sleep and improves its quality. Extends the II stage of sleep and the stage of deep sleep (III and IV). It does not cause drowsiness during the day.



The time to reach C max in blood plasma after oral administration is 0.5-3 hours. Bioavailability is 70%, binding to plasma proteins is 92%. There is a linear relationship between the dose of a drug and its plasma concentrations. It is metabolized in the liver with the formation of three inactive metabolites, which are excreted by the kidneys (56%) and through the intestines (37%). The average T 1/2 is 2.4 hours. V d is 0.5 ± 0.02 l / kg. Does not induce liver enzymes. In elderly people, clearance in blood plasma can decrease without a significant increase in T 1/2 (average 3 hours), while C max increases by 50%. In patients with severe renal impairment, clearance increases slightly. In patients with impaired liver function, bioavailability increases, T 1/2 increases to 10 hours. It is excreted in small quantities with breast milk.


Special instructions

Persistence of insomnia for 7-14 days of treatment indicates the presence of primary mental disorders and / or disorders of the nervous system. Therefore, to identify these disorders, it is necessary to regularly reassess the patient's condition, buy ambien for sale online.


To reduce the risk of developing anterograde amnesia, patients should have conditions for continuous 7-8 hours of sleep.


When Ambien is used, mental and behavioral (including paradoxical) reactions can occur (the risk of development is higher in elderly patients). If such reactions occur, the intake of Ambien should be discontinued. After a course of treatment for several weeks, a slight decrease in the sedative and hypnotic effects of Ambien is possible.


The use of Ambien (especially prolonged) can lead to the formation of physical and / or mental dependence, the risk of which increases with increasing dose and duration of treatment, as well as in patients with a history of abuse of alcohol or other drugs and non-drug substances. Such patients should be closely monitored during the treatment period. However, addiction (extremely rare) can occur with the use of therapeutic doses and / or in patients without individual risk factors.


The combination of Ambien with benzodiazepines increases the risk of drug dependence.


In elderly patients or with impaired liver function, a significant increase in T 1/2 of Ambien is possible, which can lead to a cumulation of the drug when it is taken again. Based on the characteristics of the pharmacokinetics of Ambien, with chronic renal failure, the accumulation of the drug is not expected.


When using Ambien in the elderly, care must be taken, due to the risk of developing pronounced sedative and / or muscle relaxant effects.


Influence on the ability to drive vehicles and control mechanisms


During the treatment period, one should refrain from engaging in potentially hazardous activities that require an increased concentration of attention (driving a car, working with mechanisms) and the speed of psychomotor reactions.



Symptoms: impaired consciousness (from confusion and lethargy to coma), ataxia, decreased blood pressure, respiratory depression.


Treatment: induction of vomiting within 1 hour after an overdose, activated charcoal, if more than 1 hour has passed after an overdose (with preserved consciousness, inside, with an unconscious through a probe), gastric lavage, symptomatic therapy. Flumazenil (an antagonist of benzodiazepine receptors) is recommended as an antidote, however, it should be remembered that antagonism with benzodiazepine receptors can lead to the development of seizures, especially in patients with epilepsy. Dialysis is ineffective.


Drug interaction

Not recommended combinations: ethanol enhances the sedative effect of Ambien.


Combinations requiring caution in use:

Drugs that depress the central nervous system (antipsychotics, barbiturates, other sleeping pills, anxiolytics/sedatives, antidepressants with sedative effects, narcotic analgesics, central antitussive drugs), antiepileptic drugs, drugs for general anesthesia, antihistamines with a sedative effect, hypotensive central effects; baclofen; thalidomide; pizotifen - increased inhibitory effect on the central nervous system and the risk of respiratory depression;

buprenorphine - the risk of respiratory depression;

ketoconazole (a potent CYP3A4 inhibitor) at a dose of 200 mg 2 times/day increases T 1/2, AUC and reduces the clearance of Ambien (possibly an increase in the sedative effect of Ambien);

Itraconazole (an inhibitor of CYP3A4) is a minor, clinically insignificant change in the pharmacokinetics and pharmacodynamics of Ambien.


Interactions to consider:

Rifampicin (inducer of CYP3A4) - accelerates metabolism, reduces the concentration and, as a result, the effectiveness of Ambien. buy ambien online in USA


Terms and conditions of storage

Store the drug in a dry, dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children. The shelf life of this drug is 3 years.


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