Norflurazepam

Norflurazepam
Chemische structuur
	structuurformule
Farmaceutische gegevens
Beschikbaarheid (F)	Oraal ~36% ; I.M. 90%+
Metabolisatie	Hepatisch
Halveringstijd (t1/2)	47 - 100 uur
Uitscheiding	Renaal
Gebruik
Geneesmiddelengroep	Sedativa, anesthetica
Indicaties	Sedatie, premedicatie, anesthesie
Voorschrift/recept	Nee
Toediening	oraal, nasaal, injectie (intramusculair), intraveneus of rectaal
Databanken
ATC-code	N05CD08
PubChem	4540
Chemische gegevens
Molecuulformule	C15H10ClFN2O
IUPAC-naam	7-Chloro-5-(2-fluorophenyl)-1,3-dihydro-1,4-benzodiazepin-2-one
Molmassa	288.71 g/mol
Portaal	Geneeskunde

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N-Desalkylflurazepam (ook bekend als norflurazepam) is een benzodiazepine-analoog en een actieve metaboliet van verschillende andere benzodiazepinegeneesmiddelen, waaronder flurazepam,^[1] flutoprazepam,^[2] fludiazepam,^[3] midazolam,^[4] flutazolam,^[5] quazepam^[6] en ethylloflazepate.^[7]^[8] Het werkt lang, is vatbaar voor accumulatie in het lichaam en bindt zich niet-selectief aan de verschillende subtypen van de benzodiazepinereceptor.^[7] De stof bezit anxiolytische, anticonvulsieve, kalmerende en skelet-spier relaxerende eigenschappen.

↑ (en) Riva, Roberto, de Anna, Marco, Albani, Fiorenzo, Baruzzi, Agostino (1981-03). Rapid quantitation of flurazepam and its major metabolite, N-desalkylflurazepam, in human plasma by gas—liquid chromatography with electron-capture detection. Journal of Chromatography B: Biomedical Sciences and Applications 222 (3): 491–495. DOI:10.1016/S0378-4347(00)84153-5.
↑ (en) Barzaghi, N., Leone, L., Monteleone, M., Tomasini, G., Perucca, E. (1989-10). Pharmacokinetics of flutoprazepam, a novel benzodiazepine drug, in normal subjects. European Journal of Drug Metabolism and Pharmacokinetics 14 (4): 293–298. ISSN:0378-7966. DOI:10.1007/BF03190114.
↑ Descotes J, ed. (December 1996). Human Toxicology (1st ed.). Elsevier Science. p. 43.
↑ (en) Vogt, Susanne, Kempf, Jürgen, Buttler, Jürgen, Auwärter, Volker, Weinmann, Wolfgang (2013-09). Desalkylflurazepam found in patients’ samples after high-dose midazolam treatment: Desalkylflurazepam found in patients’ samples after high dose midazolam treatment. Drug Testing and Analysis 5 (9-10): 745–747. DOI:10.1002/dta.1484.
↑ (en) Miyaguchi, Hajime, Kuwayama, Kenji, Tsujikawa, Kenji, Kanamori, Tatsuyuki, Iwata, Yuko T. (2006-02). A method for screening for various sedative-hypnotics in serum by liquid chromatography/single quadrupole mass spectrometry. Forensic Science International 157 (1): 57–70. DOI:10.1016/j.forsciint.2005.03.011.
↑ (en) Nikaido, A. M., Ellinwood, E. H. (1987-08). Comparison of the effects of quazepam and triazolam on cognitive-neuromotor performance. Psychopharmacology 92 (4): 459–464. ISSN:0033-3158. DOI:10.1007/BF00176478.
↑ ^a ^b (en) Ba, B. B., Iliadis, A., Cano, J. P. (1989-11). Pharmacokinetic modeling of ethyl loflazepate (VictanR) and its main active metabolites. Annals of Biomedical Engineering 17 (6): 633–646. ISSN:0090-6964. DOI:10.1007/BF02367467.
↑ (en) Davi, H., Guyonnet, J., Necciari, J., Cautreels, W. (1985-01). Determination of circulating ethyl loflazepate metabolites in the baboon by radio-high-performance liquid chromatography with injection of crude plasma samples: Comparison with solvent extraction and thin-layer chromatography. Journal of Chromatography B: Biomedical Sciences and Applications 342: 159–165. DOI:10.1016/S0378-4347(00)84498-9.

[1] (en) Riva, Roberto, de Anna, Marco, Albani, Fiorenzo, Baruzzi, Agostino (1981-03). Rapid quantitation of flurazepam and its major metabolite, N-desalkylflurazepam, in human plasma by gas—liquid chromatography with electron-capture detection. Journal of Chromatography B: Biomedical Sciences and Applications 222 (3): 491–495. DOI:10.1016/S0378-4347(00)84153-5.

[2] (en) Barzaghi, N., Leone, L., Monteleone, M., Tomasini, G., Perucca, E. (1989-10). Pharmacokinetics of flutoprazepam, a novel benzodiazepine drug, in normal subjects. European Journal of Drug Metabolism and Pharmacokinetics 14 (4): 293–298. ISSN:0378-7966. DOI:10.1007/BF03190114.

[3] Descotes J, ed. (December 1996). Human Toxicology (1st ed.). Elsevier Science. p. 43.

[4] (en) Vogt, Susanne, Kempf, Jürgen, Buttler, Jürgen, Auwärter, Volker, Weinmann, Wolfgang (2013-09). Desalkylflurazepam found in patients’ samples after high-dose midazolam treatment: Desalkylflurazepam found in patients’ samples after high dose midazolam treatment. Drug Testing and Analysis 5 (9-10): 745–747. DOI:10.1002/dta.1484.

[5] (en) Miyaguchi, Hajime, Kuwayama, Kenji, Tsujikawa, Kenji, Kanamori, Tatsuyuki, Iwata, Yuko T. (2006-02). A method for screening for various sedative-hypnotics in serum by liquid chromatography/single quadrupole mass spectrometry. Forensic Science International 157 (1): 57–70. DOI:10.1016/j.forsciint.2005.03.011.

[6] (en) Nikaido, A. M., Ellinwood, E. H. (1987-08). Comparison of the effects of quazepam and triazolam on cognitive-neuromotor performance. Psychopharmacology 92 (4): 459–464. ISSN:0033-3158. DOI:10.1007/BF00176478.

[:0-7] (en) Ba, B. B., Iliadis, A., Cano, J. P. (1989-11). Pharmacokinetic modeling of ethyl loflazepate (VictanR) and its main active metabolites. Annals of Biomedical Engineering 17 (6): 633–646. ISSN:0090-6964. DOI:10.1007/BF02367467.

[8] (en) Davi, H., Guyonnet, J., Necciari, J., Cautreels, W. (1985-01). Determination of circulating ethyl loflazepate metabolites in the baboon by radio-high-performance liquid chromatography with injection of crude plasma samples: Comparison with solvent extraction and thin-layer chromatography. Journal of Chromatography B: Biomedical Sciences and Applications 342: 159–165. DOI:10.1016/S0378-4347(00)84498-9.

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