Estazolam



Estazolam
Systematic (IUPAC) name
8-Chloro-6-phenyl-
4H-1,2,4-triazolo(4,3-a)-
1,4-benzodiazepine
Identifiers
CAS number 29975-16-4
ATC code N05CD04
PubChem 3261
DrugBank APRD00955
Chemical data
N4 
Mol. mass 294.7
Pharmacokinetic data
Bioavailability 93%
Metabolism Hepatic
Half life 10-24 hours
Excretion Renal
Therapeutic considerations
Pregnancy cat.

? (USA)

Legal status

Schedule IV(US)

Routes Oral

Estazolam (marketed under the brand names ProSom, Eurodin) is a drug which is a skeletal muscle relaxant properties. Estazolam is an intermediate-acting oral benzodiazepine.

It is commonly prescribed for short-term treatment of insomnia.

Pharmacology

Estazolam is classed as a "triazolo" benzodiazepine drug.[1] An animal study demonstrated that estazolam induces a drowsy pattern of spontaneous EEG including high voltage slow waves and spindle bursts increase in the cortex and amygdala, while the hippocampal theta rhythm is desynchronized. Also low voltage fast waves occur particularly in the cortical EEG. The EEG arousal response to auditory stimulation and to electric stimulation of the mesencephalic reticular formation, posterior hypothalamus and centromedian thalamus is significantly suppressed. The photic driving response elicited by a flash light in the visual cortex is significantly suppressed by estazolam.[2] Estazolam at high doses decreases histamine turnover via it's action at the benzodiazepine-GABA receptor complex.[3]

Estazolam and other oxazolam) decrease the inhibitory potency.[4]

Abuse

Estazolam became notorious in 1998 when a large amount of a 'herbal sleeping mix' called Sleeping Buddha was recalled from the shelves after the FDA descovered that it contained estazolam (as well as some heavy metal salts).[citation needed]

See also

References

  1. ^ Braestrup C; Squires RF. (Apr 1978). "Pharmacological characterization of benzodiazepine receptors in the brain.". Eur J Pharmacol 48 (3): 263-70. PMID 639854.
  2. ^ Watanabe S; Ohta H, Sakurai Y, Takao K, Ueki S. (Jul 1986). "[Electroencephalographic effects of 450191-S and its metabolites in rabbits with chronic electrode implants]". Nippon Yakurigaku Zasshi. 88 (1): 19-32. PMID 3758874.
  3. ^ Oishi R; Nishibori M, Itoh Y, Saeki K. (27). "Diazepam-induced decrease in histamine turnover in mouse brain.". Eur J Pharmacol. 124 (3): 337-42. PMID 3089825.
  4. ^ Usami N; Yamamoto T, Shintani S, Ishikura S, Higaki Y, Katagiri Y, Hara A. (Apr 2002). "Substrate specificity of human 3(20)alpha-hydroxysteroid dehydrogenase for neurosteroids and its inhibition by benzodiazepines." (pdf). Biol Pharm Bull. 25 (4): 441-5. PMID 11995921.
 
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