Tetrazepam

Source: Wikipedia, the free encyclopedia.
Tetrazepam
Clinical data
AHFS/Drugs.comInternational Drug Names
Routes of
administration		Oral
ATC code
Legal status
Legal status
Pharmacokinetic data
Elimination half-life3–26 hours
Identifiers
  • 7-chloro-5-(cyclohexen-1-yl)-1-methyl-3H-1,4-benzodiazepin-2-one
JSmol)
  • CN1C(=O)CN=C(C2=C1C=CC(=C2)Cl)C3=CCCCC3
  • InChI=1S/C16H17ClN2O/c1-19-14-8-7-12(17)9-13(14)16(18-10-15(19)20)11-5-3-2-4-6-11/h5,7-9H,2-4,6,10H2,1H3 checkY
  • Key:IQWYAQCHYZHJOS-UHFFFAOYSA-N checkY
  (verify)

Tetrazepam

depression, premenstrual syndrome or agoraphobia. Tetrazepam has relatively little sedative effect at low doses while still producing useful muscle relaxation and anxiety relief. The Co-ordination Group for Mutual Recognition and Decentralised Procedures-Human (CMD(h)) endorsed the Pharmacovigilance Risk Assessment Committee (PRAC) recommendation to suspend the marketing authorisations of tetrazepam-containing medicines across the European Union (EU) in April 2013.[3] The European Commission has confirmed the suspension of the marketing authorisations for Tetrazepam in Europe because of cutaneous toxicity, effective from the 1 August 2013.[4]

Delayed type 4 allergic hypersensitivity reactions including

eczema and Stevens–Johnson syndrome can occasionally occur as a result of tetrazepam exposure. These hypersensitivity reactions to tetrazepam share no cross-reactivity with other benzodiazepines.[5]

Indications

Tetrazepam is used therapeutically as a muscle relaxant.[6][7]

Availability

The indicated adult dose for muscle spasm is 25 mg to 150 mg per day, increased if necessary to a maximum of 300 mg per day, in divided doses. Tetrazepam is not generally recommended for use in children, except on the advice of a specialist.

Tetrazepam is only available in one strength and formulation, 50 mg

benzodiazepine equivalent of tetrazepam is approximately 100 mg of tetrazepam = 10 mg of diazepam.[8]

Adverse effects

Allergic reactions to tetrazepam occasionally occur involving the skin.[5]

Allergic reactions can develop to tetrazepam[9][10] and it is considered to be a potential allergen.[11][12] Drug rash and drug-induced eosinophilia with systemic symptoms is a known complication of tetrazepam exposure.[13][14] These hypersensitive allergic reactions can be of the delayed type.[15][16][17]

contact allergy can also develop from regularly handling tetrazepam.[30][31] Airborne contact dermatitis can also occur as an allergy which can develop from occupational exposure.[32]

Patch test

Patch testing has been used successfully to demonstrate tetrazepam allergy.[33][34] Oral testing can also be used. Skin prick tests are not always accurate and may produce false negatives.[35]

Drowsiness is a common side effect of tetrazepam.[36] A reduction in muscle force can occur.[37] Myasthenia gravis, a condition characterised by severe muscle weakness is another potential adverse effect from tetrazepam.[38] Cardiovascular and respiratory adverse effects can occur with tetrazepam similar to other benzodiazepines.[27]

Tolerance, dependence and withdrawal

See also: Benzodiazepine withdrawal syndrome

Prolonged use, as with all

benzodiazepines, should be avoided, as tolerance occurs and there is a risk of benzodiazepine dependence and a benzodiazepine withdrawal syndrome after stopping or reducing dosage.[27]

Overdose

See also: Benzodiazepine overdose

Tetrazepam, like other benzodiazepines is a drug which is very frequently present in cases of overdose. These overdoses are often mixed overdoses, i.e. a mixture of other benzodiazepines or other drug classes with tetrazepam.[39][40]

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.[41]

Pharmacology

Tetrazepam is an unusual benzodiazepine in its molecular structure as it has cyclohexenyl group which has substituted the typical 5-phenyl moiety seen in other benzodiazepines.[42] Tetrazepam, is rapidly absorbed after oral administration, within 45 mins and reaches peak plasma levels in less than 2 hours. It is classed as an intermediate acting benzodiazepine with an elimination half-life of approximately 15 hours. It is primarily metabolised to the inactive metabolites 3-hydroxy-tetrazepam and

active metabolites of diazepam are produced from metabolism of tetrazepam.[47][48] The metabolism of tetrazepam has led to false accusations of prisoners prescribed tetrazepam of taking illicit diazepam; this can lead to increased prison sentences for prisoners.[42]

Abuse

See also:
Benzodiazepine misuse

Tetrazepam as with other benzodiazepines is sometimes abused. It is sometimes abused to incapacitate a victim in order to carry out a drug-facilitated crime.[49] or abused in order to achieve a state of intoxication.[50] Tetrazepam's abuse for to carry out drug facilitated crimes may be less however, than other benzodiazepines due to its reduced hypnotic properties.[51]

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. ^ NL Patent 6600095
  3. ^ Recommendation to suspend tetrazepam-containing medicines endorsed by CMDh, European Medicines Agency, published 29 April 2013
  4. ^ Ruhen der Zuhlassung aller Tetrazepam-haltiger Arzneimittel, Sanofi-Avensis Deutschland GmbH (German), published June 2013
  5. ^
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