Clotiazepam

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Clotiazepam
Clinical data
Trade namesVeratran, Rize, Clozan
AHFS/Drugs.comInternational Drug Names
Routes of
administration		Oral, sublingual, liquid drops
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability~90%
MetabolismHepatic
Elimination half-life4 hours[2]
ExcretionRenal
Identifiers
  • 5-(2-chlorophenyl)-7-ethyl-1-methyl-3H-thieno[2,3-e][1,4]diazepin-2-one
JSmol)
  • ClC1=C(C2=NCC(N(C)C3=C2C=C(CC)S3)=O)C=CC=C1
  • InChI=1S/C16H15ClN2OS/c1-3-10-8-12-15(11-6-4-5-7-13(11)17)18-9-14(20)19(2)16(12)21-10/h4-8H,3,9H2,1-2H3 checkY
  • Key:CHBRHODLKOZEPZ-UHFFFAOYSA-N checkY
 ☒NcheckY (what is this?)  (verify)
Clotiazepam pills sold in France as Vératran

Clotiazepam

NREM sleep is significantly increased by clotiazepam.[8]

Indications

Clotiazepam has been trialed and found to be effective in the short-term management of

premedicant in minor surgery in France and Japan, where the drug is commercially available under the brand names Veratran and Rize, respectively.[10][11]

Pharmacokinetics

A cross-over study in six healthy volunteers (median age 28 years) was conducted using single-dose pharmacokinetics of 5 mg clotiazepam drops, oral tablets, and sublingual tablets. The formulations had similar systemic availability. Compared with oral tablets, the sublingual route gave a lower peak concentration and a delayed peak time, while drops gave a greater maximum concentration with a similar peak time. The use of drops is suggested for a more marked initial effect and the sublingual route for easier administration, especially in the elderly.[12]

Pharmacology

Similar to other benzodiazepines clotiazepam has

amnesic, anticonvulsant and muscle relaxant pharmacological properties.[7] Clotiazepam binds to the benzodiazepine site of the GABAA receptor where it acts as a full agonist; this action results in an enhanced GABA inhibitory effect at the GABAA receptor which results in the pharmacological effects of clotiazepam.[13]

Clotiazepam has a short

elimination half-life and is less prone to accumulation after repeated dosing compared to longer-acting benzodiazepine agents. It is metabolised via oxidation.[14] Clotiazepam is metabolised to hydroxy-clotiazepam and desmethyl-clotiazepam. After oral ingestion of a single 5 mg dose of clotiazepam by three healthy volunteers the drug was rapidly absorbed.[15] The elimination half-life of the drug and its metabolites range from 6.5 hours to 18 hours. Clotiazepam is 99 percent bound to plasma protein.[15] In elderly men the elimination half-life is longer and in elderly women the volume of distribution is increased.[16] Individuals with liver impairment have a reduced volume of distribution as well as a reduced total clearance of clotiazepam; renal impairment does not affect the kinetics of clotiazepam.[17]

The dose equivalent to 10 mg diazepam is thought to be between 5 and 10 mg clotiazepam.

Side effects

Side effects experienced with this product will resemble those of other benzodiazepines.

asthenia are common side effects.[18] There has been a report of reversible hepatitis caused by clotiazepam.[19]

Abuse

Clotiazepam is a recognised

drug of abuse.[20]

See also

References

  1. ^ 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.
  2. ^ "Clotiazépam" (PDF). HAS - Direction de l'Evaluation Médicale. Economique et de Santé Publique. 20 May 2015.
  3. ^ DE 2107356, Nakanishi M, Kazuhiko A, Tetsuya T, Shiroki M, "Thieno-(2,3-E)(1,4)diazepin-2-ones", issued 3 May 1978, assigned to Yoshitomi Pharmaceutical Industries, Ltd. 
  4. PMID 16141545
    .
  5. PMID 27828
    .
  6. PMID 6632385
    .
  7. ^
    PMID 18855614
    .
  8. S2CID 13365554
    .
  9. PMID 2885366
    .
  10. ^ "RIZE TABLETS 5mg". Official Japanese Drug Information Sheet (Kusuri-no-Shiori). February 2016.
  11. ^ "Clotiazepam (Veratran)". French Guide to Medicines.
  12. S2CID 29397932
    .
  13. PMID 2574062
    .
  14. S2CID 19691487
    .
  15. ^
    PMID 6125154
    .
  16. S2CID 44321356
    .
  17. S2CID 21304989
    .
  18. PMID 1971433
    .
  19. PMID 2572625
    .
  20. PMID 7920567
    .

External links
Retrieved from "https://en.wikipedia.org/w/index.php?title=Clotiazepam&oldid=1170616024"