Cinolazepam

Structural formula
General
Non-proprietary name	Cinolazepam
other names	7-chloro-5- (2-fluorophenyl) -3-hydroxy-2-oxo-2,3-dihydro-1H-1,4-benzodiazepine-1-propionitrile ( IUPAC ); 3- [7-Chloro-5- (2-fluorophenyl) -3-hydroxy-2-oxo-2,3-dihydro-1H-1,4-benzodiazepin-1-yl] propanenitrile; Cinolazepamum; OX-373;
Molecular formula	C 18 H 13 ClFN 3 O 2
External identifiers / databases
PubChem	3033621
ChemSpider	2298251
DrugBank	DB01594
Wikidata	Q667184
Drug information
ATC code	N05 CD13
Drug class	Benzodiazepine; Hypnotic;
properties
Molar mass	357.8 g · mol -1
Melting point	190-193 ° C
safety instructions
	Please note the exemption from the labeling requirement for drugs, medical devices, cosmetics, food and animal feed
GHS hazard labeling ; no classification available
Toxicological data	3500 mg kg −1 ( LD 50 , mouse , oral ) ; 3500 mg 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 .

Cinolazepam is a drug from the benzodiazepine group and has amnestic , anxiolytic , anticonvulsant , hypnotic , sedative and muscle-relaxing potential. The anxiolytic, anticonvulsant and muscle-relaxing properties are only very weak, the hypnotic properties are relatively strong. This is the reason why it is used as a hypnotic in medicine.

It was developed by Gerot Pharmazeutika in 1978 and launched on the European market in 1992 under the finished drug name Gerodorm . The substance is not available in Germany.

Mechanism of action

The effect of cinolazepam is based on a strengthening of GABAergic nerve cells, especially the limbic system . Cinolazepam leads to a shortening of the time to fall asleep, to a reduction in the awakening phases due to noise pollution and to falling asleep again more quickly after awakening at night. The mean sleep duration is extended. The typical pharmaco- EEG shows an increase in mean rapid beta activity and a decrease in alpha activity. REM sleep periods are subject to minimal changes.

Pharmacokinetics

Cinolazepam is rapidly and completely absorbed after ingestion. The maximum plasma concentrations are reached within 2 hours. The half-life is 4-6 hours and the dose equivalent to 10 mg diazepam is 40 mg.

Side effects

Common side effects, especially at the beginning of treatment, are: drowsiness during the day, drowsiness, dizziness, headache, muscle weakness and confusion. In rare cases, a paradoxical (opposing) effect with excitement (fear, aggressiveness, agitated state of confusion) can occur, which must never be answered by increasing the dose. Like all drugs from the benzodiazepine class, cinolazepam has a high potential for dependence and abuse.

Trade names

Monopreparations

Gerodorm (AT, no longer available), Gerodorm (BG, CZ, HU, SK, RO)

Individual evidence

↑ Cinolazepam Product Description. In: chemicalbook.com. ChemicalBook, accessed September 5, 2019 .
↑ This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.
↑ ^a ^b J.R. Prous: Lethal dose cinolazepam . In: Drugs of the Future . 7, No. 5, 1982, pp. 1975-76.
↑ AT Patent 903178A
↑ János Fischer, C. Robin Ganellin (Ed.): Analogue-based Drug Discovery . Hypnotics and Sedatives / Benzodiazepine Derivatives. John Wiley & Sons, 2006, ISBN 978-3-527-31257-3 ( limited preview in Google Book Search).
↑ Saletu; Kindshofer; Another; Grünberger: Short-term sleep laboratory studies with cinolazepam in situational insomnia induced by traffic noise . In: International Journal of Clinical Pharmacology Research . 7, No. 5, 1987, pp. 407-418. PMID 2889679 .
↑ P. Riederer; G. Laux; W. Pöldinger: Neuro-Psychopharmaka A therapy manual . 1st edition. 2 tranquilizers and hypnotics. Springer, 1995, ISBN 978-3-7091-7357-2 , pp. 384 , doi : 10.1007 / 978-3-7091-6593-5 .

[ChemicalBook-1] Cinolazepam Product Description. In: chemicalbook.com. ChemicalBook, accessed September 5, 2019 .

[NV-2] This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.

[LD50-3] J.R. Prous: Lethal dose cinolazepam . In: Drugs of the Future . 7, No. 5, 1982, pp. 1975-76.

[4] AT Patent 903178A

[5] János Fischer, C. Robin Ganellin (Ed.): Analogue-based Drug Discovery . Hypnotics and Sedatives / Benzodiazepine Derivatives. John Wiley & Sons, 2006, ISBN 978-3-527-31257-3 ( limited preview in Google Book Search).

[6] Saletu; Kindshofer; Another; Grünberger: Short-term sleep laboratory studies with cinolazepam in situational insomnia induced by traffic noise . In: International Journal of Clinical Pharmacology Research . 7, No. 5, 1987, pp. 407-418. PMID 2889679 .

[Neuropsychopharma-7] P. Riederer; G. Laux; W. Pöldinger: Neuro-Psychopharmaka A therapy manual . 1st edition. 2 tranquilizers and hypnotics. Springer, 1995, ISBN 978-3-7091-7357-2 , pp. 384 , doi : 10.1007 / 978-3-7091-6593-5 .