Estazolam

Source: Wikipedia, the free encyclopedia.
Estazolam
Clinical data
Trade namesProsom, Esilgan, Eurodin, Nuctalon, others
Other namesDesmethylalprazolam
AHFS/Drugs.comMonograph
MedlinePlusa691003
License data
Routes of
administration		By mouth
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability93%
MetabolismLiver
Elimination half-life10–24 hours
ExcretionKidney
Identifiers
  • 8-chloro-6-phenyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine
JSmol)
  • ClC1=CC2=C(C=C1)N3C=NN=C3CN=C2C4=CC=CC=C4
  • InChI=1S/C16H11ClN4/c17-12-6-7-14-13(8-12)16(11-4-2-1-3-5-11)18-9-15-20-19-10-21(14)15/h1-8,10H,9H2 checkY
  • Key:CDCHDCWJMGXXRH-UHFFFAOYSA-N checkY
  (verify)

Estazolam, sold under the brand name Prosom among others, is a

skeletal muscle relaxant properties. Estazolam is an intermediate-acting oral benzodiazepine. It is used for short-term treatment of insomnia
.

It was patented in 1968 and came into medical use in 1975.[5]

Medical uses

Estazolam 1mg pills, sold as Eurodin, from Japan.

Estazolam is prescribed for the short-term treatment of certain sleep disorders. It is an effective hypnotic drug showing efficacy in increasing the time spent asleep as well as reducing awakenings during the night. Combination with non-pharmacological options for sleep management results in long-term improvements in sleep quality after discontinuation of short-term estazolam therapy.[6][7] Estazolam is also sometimes used as a preoperative sleep aid. It was found to be superior to triazolam in side effect profile in preoperative patients in a trial.[8] Estazolam also has anxiolytic properties and due to its long half life can be an effective short-term treatment for insomnia associated with anxiety.[9]

Side effects

A hang-over effect commonly occurs with next day impairments of mental and physical performance.[10] Other side effects of estazolam include somnolence, dizziness, hypokinesia, and abnormal coordination.[11]

In September 2020, the U.S. Food and Drug Administration (FDA) required the boxed warning be updated for all benzodiazepine medicines to describe the risks of abuse, misuse, addiction, physical dependence, and withdrawal reactions consistently across all the medicines in the class.[12]

Tolerance and dependence

The main safety concern of benzodiazepines such as estazolam is a

rebound insomnia and CNS related adverse effects. Estazolam should only be used short term and at the lowest effective dose to avoid complications related to long-term use. Non-pharmacological treatment options however, were found to have sustained improvements in sleep quality.[13][14] The short-term benefits of benzodiazepines on sleep begin to reduce after a few days due to tolerance to the hypnotic effects of benzodiazepines in the elderly.[15]

Contraindications and special caution

Benzodiazepines require special precaution if used in the elderly, during pregnancy, in children, alcohol or drug-dependent individuals and individuals with

psychiatric disorders.[16]

Pharmacology

Estazolam is classed as a "triazolo" benzodiazepine drug.[17] Estazolam exerts its therapeutic effects via its benzodiazepines receptor agonist properties.[18] Estazolam at high doses decreases histamine turnover via its action at the benzodiazepine-GABA receptor complex in mouse brains.[19]

Pharmacokinetics

Peak plasma levels are achieved within 1–6 hours. Estazolam is an intermediate acting

elimination half life of estazolam is an average of 19 hours, with a range of 8–31 hours.[20][21] The major metabolite of estazolam is 4-hydroxyestazolam.[22] Other identified metabolites include 1-oxo-estazolam, 4'-hydroxy-estazolam, and benzophenone.[3]

Interactions

Alcohol enhances the sedative hypnotic properties of estazolam.[23] In package inserts, the manufacturer clearly warns about an interaction with ritonavir, and although clinical interactions of ritonavir with estazolam have not yet been described, the lack of clinical descriptions of the interactions does not negate the seriousness of the interaction.[24]

EEG effects in rabbits

An animal study in rabbits demonstrated that estazolam induces a drowsy pattern of spontaneous

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.[25]

Abuse

See also:
Benzodiazepine drug misuse

A primate study found that estazolam has abuse potential.[26] Two types of drug misuse can occur; recreational misuse, where the drug is taken to achieve a high or when the drug is continued long term against medical advice.[27] Estazolam became notorious in 1998 when a large amount of an 'herbal sleeping mix' called Sleeping Buddha was recalled from the shelves after the FDA discovered that it contained estazolam.[28] In 2007, a Canadian product called Sleepees was recalled after it was found to contain undeclared estazolam.[29][30]

See also

References

  1. FDA
    . Retrieved 22 Oct 2023.
  2. ^ Anvisa (2023-03-31). "RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial" [Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control] (in Brazilian Portuguese). Diário Oficial da União (published 2023-04-04). Archived from the original on 2023-08-03. Retrieved 2023-08-16.
  3. ^ a b "Estazolam tablet". DailyMed. 30 September 2020. Retrieved 25 October 2020.
  4. ^ "Estazolam (Prosom) Use During Pregnancy". Drugs.com. 18 September 2020. Retrieved 25 October 2020.
  5. ISBN 9783527607495
    .
  6. S2CID 9143614
    .
  7. PMID 11040460
    .
  8. PMID 2889169
    .
  9. S2CID 7890993
    .
  10. PMID 6125155
    .
  11. PMID 1968713
    .
  12. ^ "FDA expands Boxed Warning to improve safe use of benzodiazepine drug". U.S. Food and Drug Administration (FDA). 23 September 2020. Retrieved 23 September 2020. Public Domain This article incorporates text from this source, which is in the public domain.
  13. PMID 10533351
    .
  14. S2CID 7936406
    .
  15. PMID 7595266
    .
  16. PMID 19900604
    .
  17. PMID 639854
    .
  18. PMID 12538007
    .
  19. PMID 3089825
    .
  20. S2CID 23882114
    .
  21. PMID 2862746
    .
  22. S2CID 10576075
    .
  23. S2CID 1543185. Archived from the original
    (PDF) on 2007-07-09.
  24. PMID 12036118
    .
  25. PMID 3758874
    .
  26. S2CID 21917850
    .
  27. PMID 16336040
    .
  28. ^ Food and Drug Administration; U.S. Department of Health and Human Services (10 March 1998). "FDA WARNS CONSUMERS AGAINST TAKING DIETARY SUPPLEMENT "SLEEPING BUDDHA"". FDA. Archived from the original on October 6, 2008. Retrieved 21 December 2008.
  29. ^ "Potentially habit-forming herbal sleep aid recalled". CBC News. Feb 23, 2007. Retrieved 2020-07-03.
  30. ^ André P (Aug 14, 2007). "Losing sleep over 'natural' aids". The Globe and Mail. Retrieved 2020-07-03.

External links

  • "Estazolam". Drug Information Portal. U.S. National Library of Medicine.
Retrieved from "https://en.wikipedia.org/w/index.php?title=Estazolam&oldid=1214873999"