Zolpidem ( Zolpidem , N, N, 6-Trimethyl-2- (4-methylphenyl) imidazolo [1,2-a] pyridin-3-acetamide, in the form of tartrate ) is a hypnotic drug from the imidazopyridine group, which is used in many modern sleeping pills. In terms of effectiveness, the benzodiazepine analogue has a very short half-life (about 2 hours) and is not a source of pharmacologically active metabolites. It is quickly absorbed by the body, the maximum plasma concentration is reached after about two hours. Currently, the most common sleeping pills in the USA and Europe , known abroad under many different commercial names: Adormix, Ambien, Edluar, Damixan, Hypnogen, Ivedal, Lioran, Myslee, Nytamel, Sanval, Stilnoct, Stilnox, Sucedal, Zoldem, Zolnod and Zolpihexal .
| Zolpidem | |
|---|---|
| Zolpidem | |
 | |
 | |
| Chemical compound | |
| IUPAC | N , N , 6-Trimethyl-2- (4-methylphenyl) - imidazo [1,2- a ] pyridine-3-acetamide |
| Gross formula | C 19 H 21 N 3 O |
| Molar mass | 307.395 g / mol |
| Cas | |
| PubChem | |
| Drugbank | |
| Classification | |
| ATX | |
| ICD-10 | |
| Pharmacokinetics | |
| Bioavailable | about 70% |
| Metabolism | liver , CYP3A4 |
| The half-life. | 2 to 2.6 hours |
| Excretion | 56% kidney 34% cal |
| Dosage Forms | |
| pills | |
| Route of administration | |
| Oral | |
| Other names | |
| Hypnogen, Ivadal, Nitrest, Dreamwright, Sanval | |
There are reports of the paradoxical effect of zolpidem on patients in some coma , in which people are conscious, but cannot move and speak. In some of these patients, after the use of zolpidem, a temporary restoration of motor activity was noted up to the possibility of talking, eating and walking [1] [2] [3] .
Content
- 1 History
- 2 Indications
- 3 Pharmacological properties
- 4 Pharmacokinetics
- 5 side effects
- 6 Tolerance and dependence
- 7 notes
- 8 Literature
- 9 References
History
Zolpidem was synthesized for short-term (usually two to six weeks) treatment of insomnia. The medicine was studied for 180 days in 1991 [4] , in 1992 the results of the study [5] were published ; the final report was published in 1993 [6] .
The US Air Force uses zolpidem as one of the approved sedatives known as “ No Go Pills ”. The drug is used to help pilots and special personnel to achieve a full sleep before completing tasks. The use of zolpidem by the military requires special permission, which is issued for the use of drugs in an operational setting [7] .
Indications
Treatment of insomnia [8] , which is situational and transient, including frequent awakenings from sleep and difficulty falling asleep.
Pharmacological properties
The pharmacological activity of the drug is close to benzodiazepines and has muscle relaxant , anxiolytic , sedative , hypnotic, amnestic and anticonvulsant effects.
The action of the drug is based on specific agonism with central omega receptors ( type I and II benzodiazepine receptors ) - macromolecular GABA receptor complexes that cause the opening of neuronal anion channels for chlorine .
Interaction with central benzodiazepine receptors of type I (omega-1) occurs selectively, which makes the sedative effect noticeable at lower doses than necessary to achieve other (muscle relaxant, anxiolytic, amnestic) effects.
Reduces the time of falling asleep and reduces the number of night awakenings, prolongs the duration of sleep and improves its quality. The duration of the II stage of sleep and deep sleep of the III and IV stages increases, there is no effect on the duration of the REM phase .
Pharmacokinetics
At therapeutic doses, the pharmacokinetics remain linear.
After oral administration, bioavailability is about 70%, the maximum plasma concentration of 92% occurs within 0.5-3 hours after ingestion.
The drug does not induce liver enzymes.
Side Effects
The most common side effects of zolpidem are drowsiness (5%), dizziness (5%), headache (3%), gastrointestinal upset (4%). From 15% to 20% of patients taking this drug experience memory problems, complain of nightmares, confusion. Individual cases of sensory disturbances and psychotic symptoms have been reported with zolpidem. In particular, delusions , hallucinations , distortion of sensory perception can develop. Amnesia , including bulimia associated with sleep, is more commonly observed with this drug than with triazolam [9] .
In patients taking zolpidem, the presence of adverse reactions should be monitored, since the use of zolpidem can be a potential provoking factor in cases where unreasonable violence for the patient is observed, which may be accompanied by psychosis, amnesia and confusion [9] .
The following factors increase the risk of side effects when using zolpidem: female gender, advanced age, taking zolpidem at a dose of 10 mg or higher, and the simultaneous use of selective serotonin reuptake inhibitors [9] .
Tolerance and Addiction
It has been established that prolonged use of zolpidem can be addictive and addictive . It is recommended to use the medicine only for short periods of time, using the lowest effective doses. Animal studies have shown that rodents have a lower tolerance to zolpidem than benzodiazepines, but in primates, tolerance to zolpidem is comparable to benzodiazepines. In some people, addiction can develop within a few weeks. Stopping the drug after prolonged use can cause seizures or other consequences, especially if it has been used for a long time and at high doses.
To relieve physical dependence on zolpidem, a gradual dose reduction over a month is usually used in order to minimize withdrawal symptoms , which may resemble withdrawal of benzodiazepines.
Alcohol enhances the effect of the drug, acting in the same way as with benzodiazepines. For this reason, alcoholism leads to an increased risk of physical dependence on zolpidem. In addition, there is the possibility of the development of psychological dependence on zolpidem.
Notes
- ↑ A sleepy drug returned a woman from a two-year-old coma . MEMBRANA.RU (March 14, 2007). Date of treatment February 5, 2010.
- ↑ Christine Brefel-Courbon; Pierre Payoux, Fabierine Ory, Agnes Sommet, Tarik Slaoui, Gaelle Raboyeau, Beatrice Lemesle, Michele Puel, Jean-Louis Montastruc, Jean-Francois Demonet, Dominique Cardebat. Clinical and imaging evidence of zolpidem effect in hypoxic encephalopathy (English) . Annals of Neurology (Mar 13, 2007). Date of treatment February 5, 2010. Archived April 12, 2012.
- ↑ Sleepy powder awakened plant people . MEMBRANA.RU (May 24, 2006). Date of treatment February 5, 2010.
- ↑ Schlich D. , L'Heritier C. , Coquelin JP , Attali P. , Kryrein HJ Long-term treatment of insomnia with zolpidem: a multicentre general practitioner study of 107 patients. (English) // The Journal of international medical research. - 1991. - Vol. 19, no. 3 . - P. 271—279. - DOI : 10.1177 / 030006059101900313 . - PMID 1670039 .
- ↑ Maarek L. , Cramer P. , Attali P. , Coquelin JP , Morselli PL The safety and efficacy of zolpidem in insomniac patients: a long-term open study in general practice. (English) // The Journal of international medical research. - 1992. - Vol. 20, no. 2 . - P. 162-170. - DOI : 10.1177 / 030006059202000208 . - PMID 1521672 .
- ↑ Kummer J. , Guendel L. , Linden J. , Eich FX , Attali P. , Coquelin JP , Kyrein HJ Long-term polysomnographic study of the efficacy and safety of zolpidem in elderly psychiatric in-patients with insomnia. (English) // The Journal of international medical research. - 1993. - Vol. 21, no. 4 . - P. 171-184. - DOI : 10.1177 / 030006059302100402 . - PMID 8112475 .
- ↑ Permission form (inaccessible link)
- ↑ Buzunov, 2009 .
- ↑ 1 2 3 Kotova O. V., Ryabokon I. V. Modern aspects of insomnia therapy // Attending physician. - 2013. - No. 5 .
Literature
- Buzunov R.V. Insomnia in the practice of a therapist . - M. , 2009 .-- 25 p.