Triazolam

Structural formula
General
Non-proprietary name	Triazolam
other names	8-Chloro-6- (2-chlorophenyl) -1-methyl-4 H - [1,2,4] triazolo [4,3- a ] [1,4] benzodiazepine
Molecular formula	C 17 H 12 Cl 2 N 4
External identifiers / databases
EC number	249-307-3
ECHA InfoCard	100,044,811
PubChem	5556
DrugBank	DB00897
Wikidata	Q412143
Drug information
ATC code	N05 CD05
Drug class	Benzodiazepine , hypnotic , sedative
properties
Molar mass	343.22 g · mol -1
Physical state	firmly
Melting point	233-235 ° C
safety instructions
	Please note the exemption from the labeling requirement for drugs, medical devices, cosmetics, food and animal feed
GHS labeling of hazardous substances	no GHS pictograms
	no GHS pictograms
H and P phrases	H: no H-phrases
	P: no P-phrases
Toxicological data	1080 mg kg −1 ( LD 50 , mouse , oral ) ; > 7.5 g kg −1 ( LD 50 , rat , oral ) ;
	As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

Triazolam ( trade name Halcion A, D, CH) is an orally active benzodiazepine derivative with a short half-life of 2 to 5 hours. It is used for short-term severe sleep disorders , especially sleep disorders . Psychological and physical dependence can develop after only a short period of use .

Chemically, triazolam belongs to the subgroup of triazole benzodiazepines.

Legal status in Germany

In the Federal Republic of Germany, triazolam is a marketable and prescription narcotic drug due to its listing in Appendix III (to Section 1, Paragraph 1) of the Narcotics Act. Handling without permission or prescription is generally punishable.

This does not include preparations that do not contain any other narcotic drugs and that contain up to 0.25 mg of triazolam per divided form.

Pharmacokinetics

Triazolam is more than 85% absorbed after oral administration. The inundation occurs quickly, but is subject to strong inter-individual fluctuations. The increased bioavailability after sublingual administration compared to oral administration indicates a first-pass effect . Triazolam is rapidly and extensively biotransformed in the intestinal mucosa and in the liver .

The substance is metabolized in the liver via the enzyme CYP 3A4 and is eliminated renally.

Pharmacodynamics

A dose of 0.5 mg triazolam corresponds to the strength of 10 mg diazepam .

Side effects

Like other rapidly absorbable benzodiazepines, triazolam can cause short-term amnesia and can cause memory impairment lasting up to a week after it has been discontinued, which has been described in travelers under the influence of triazolam as Traveller's Amnesia .

In 1991, the then competent BGA in Germany considered suspending approval in order to suspect that central nervous side effects such as excitement, anxiety, aggressiveness, depression and amnesia occurred more frequently and more seriously than before with triazolam, even in lower doses and compared to other benzodiazepines assumed to follow up.

Use during pregnancy and breastfeeding

Triazolam must not be used during pregnancy or while breastfeeding.

Individual evidence

↑ ^a ^b entry on triazolam. In: Römpp Online . Georg Thieme Verlag, accessed on December 28, 2014.
↑ Data triazolam at Sigma-Aldrich , accessed on 29 May 2011 ( PDF ).
↑ Kleemann , Engel, Kutscher, Reichert: Pharmaceutical Substances , 4th edition, Thieme-Verlag Stuttgart 2000, page 2102, ISBN 978-1-58890-031-9 .
↑ ^a ^b ^c Specialist information Halcion (Pfizer Pharma PFE GmbH, Berlin), as of June 2016.
↑ PD Kroboth et al .: Triazolam pharmacokinetics after intravenous, oral, and sublingual administration. J Clin Psychopharmacol. 1995 Aug; 15 (4): 259-62. PMID 7593708 .
↑ JM Scavone et al .: Enhanced bioavailability of triazolam following sublingual versus oral administration. J Clin Pharmacol. 1986 Mar; 26 (3): 208-10. PMID 3958225 .
^ ^A ^b Richard Lawrence Miller: The Encyclopedia of Addictive Drugs. Greenwood Publishing Group, 2002, ISBN 978-0-313-31807-8 , p. 427.
↑ Frank J. Ayd: Lexicon of Psychiatry, Neurology, and the Neurosciences. Lippincott Williams & Wilkins, 2000, ISBN 978-0-781-72468-5 , p. 99.
↑ KK Jain: Drug-Induced Neurological Disorders. Hogrefe Publishing, 2011, ISBN 978-1-616-76425-8 , p. 88.
↑ On the market withdrawal of the sleeping pill triazolam (Halcion) in Great Britain and Finland , arznei-telegram 10/1991.

[RÖMPP_Online-1] try on triazolam. In: Römpp Online . Georg Thieme Verlag, accessed on December 28, 2014.

[Sigma-2] Data triazolam at Sigma-Aldrich , accessed on 29 May 2011 ( PDF ).

[Kleemann-3] Kleemann , Engel, Kutscher, Reichert: Pharmaceutical Substances , 4th edition, Thieme-Verlag Stuttgart 2000, page 2102, ISBN 978-1-58890-031-9 .

[FI-4] Specialist information Halcion (Pfizer Pharma PFE GmbH, Berlin), as of June 2016.

[5] PD Kroboth et al .: Triazolam pharmacokinetics after intravenous, oral, and sublingual administration. J Clin Psychopharmacol. 1995 Aug; 15 (4): 259-62. PMID 7593708 .

[6] JM Scavone et al .: Enhanced bioavailability of triazolam following sublingual versus oral administration. J Clin Pharmacol. 1986 Mar; 26 (3): 208-10. PMID 3958225 .

[Miller-7] A ^b Richard Lawrence Miller: The Encyclopedia of Addictive Drugs. Greenwood Publishing Group, 2002, ISBN 978-0-313-31807-8 , p. 427.

[Ayd-8] Frank J. Ayd: Lexicon of Psychiatry, Neurology, and the Neurosciences. Lippincott Williams & Wilkins, 2000, ISBN 978-0-781-72468-5 , p. 99.

[Jain-9] KK Jain: Drug-Induced Neurological Disorders. Hogrefe Publishing, 2011, ISBN 978-1-616-76425-8 , p. 88.

[10] On the market withdrawal of the sleeping pill triazolam (Halcion) in Great Britain and Finland , arznei-telegram 10/1991.