Oxazepam

Bezeichnung:Oxazepam

CAS-Nr604-75-1

Englisch Name:OXAZEPAM

CBNumberCB6444321

SummenformelC15H11ClN2O2

Molgewicht286.71

MOL-Datei604-75-1.mol

Synonyma

Oxazepam

Oxazepam physikalisch-chemischer Eigenschaften

Schmelzpunkt	205-206°
Siedepunkt	506.5±50.0 °C(Predicted)
Dichte	1.3052 (rough estimate)
Brechungsindex	1.5200 (estimate)
Flammpunkt	11 °C
storage temp.	−20°C
Löslichkeit	Practically insoluble in water, slightly soluble in ethanol (96 per cent).
pka	pKa 1.6/11.6(5% MeOH in H2O,t =20,I=0.15) (Uncertain)
Wasserlöslichkeit	20mg/L(22 ºC)
CAS Datenbank	604-75-1(CAS DataBase Reference)
IARC	2B (Vol. Sup 7, 66) 1996
EPA chemische Informationen	Oxazepam (604-75-1)

Sicherheit

Kennzeichnung gefährlicher	Xn,T,F
R-Sätze:	40-39/23/24/25-23/24/25-11
S-Sätze:	7-16-36/37-45
RIDADR	UN 1230 3/PG 2
WGK Germany	3
RTECS-Nr.	DF1400000
HazardClass	6.1(b)
PackingGroup	III
HS Code	2933910000
Giftige Stoffe Daten	604-75-1(Hazardous Substances Data)
Toxizität	LD50 in mice, rats (mg/kg): >5010, >5010 orally (Goldenthal)

Gefahreninformationscode (GHS)

OXAZEPAM Chemische Eigenschaften,Einsatz,Produktion Methoden

R-Sätze Betriebsanweisung:
R40:Verdacht auf krebserzeugende Wirkung.
R39/23/24/25:Giftig: ernste Gefahr irreversiblen Schadens durch Einatmen, Berührung mit der Haut und durch Verschlucken.
R23/24/25:Giftig beim Einatmen, Verschlucken und Berührung mit der Haut.
R11:Leichtentzündlich.
S-Sätze Betriebsanweisung:
S7:Behälter dicht geschlossen halten.
S16:Von Zündquellen fernhalten - Nicht rauchen.
S36/37:Bei der Arbeit geeignete Schutzhandschuhe und Schutzkleidung tragen.
S45:Bei Unfall oder Unwohlsein sofort Arzt zuziehen (wenn möglich, dieses Etikett vorzeigen).
Chemische Eigenschaften
Off-White Solid
Originator
Serax,Wyeth,US,1965
Verwenden
Anxiolytic; muscle relaxant (skeletal); anticonvulsant; ligand for the GABAA receptor benzodiazepine modulatory site. Controlled substance (depressant).
Definition
ChEBI: A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a chloro group at position 7, a hydroxy group at position 3 and phenyl group at position 5.
Manufacturing Process
(A) Suspend 10 g of 7-chloro-1,3-dihydro-5-phenyl-2H-1,4-benzodiazepin-2one 4-oxide in 150 ml of acetic anhydride and warm on a steam bath with stirring until all the solid has dissolved. Cool and filter off crystalline, analytically pure 3-acetoxy-7-chloro-1,3-dihydro-5-phenyl-2H-1,4benzodiazepin-2-one, melting point 242°C to 243°C.
(B) Add to a suspension of 3.4 g of 3-acetoxy-7-chloro-1,3-dihydro-5-phenyl2H-1,4-benzodiazepin-2-one in 80 ml of alcohol.6 ml of 4 N sodium hydroxide. Allow to stand after complete solution takes place to precipitate a solid. Redissolve the solid by the addition of 80 ml of water. Acidify the solution with acetic acid to give white crystals. Recrystallize from ethanol to obtain 7chloro-1,3-dihydro-3-hydroxy-5-phenyl-2H-1,4-benzodiazepin-2-one, melting point 203°C to 204°C.
Trademarks
Serax (Alpharma); Zaxopam (Quantum Pharmics).
Therapeutic Function
Tranquilizer
Allgemeine Beschreibung
Odorless creamy-white to pale-yellow powder or white crystalline solid. Bitter taste. pH (2% aqueous suspension) 4.8-7.
Allgemeine Beschreibung
Oxazepam, 7-chloro-1,3-dihydro-3-hydroxy-5-phenyl-2H-1,4-benzodiazpin-2-one (Serax), isan active metabolite of both chlordiazepoxide and diazepamand can be considered a prototype for the 3-hydroxy benzo-diazepines. It is much more polar than diazepam. Oxazepam is rapidlyinactivated to glucuronidated metabolites that are excretedin the urine. Thus, the half-life of oxazepam is about 4 to 8hours, and it is marketed as a short-acting anxiolytic. As aresult, its cumulative effects with chronic therapy are muchless than with long-acting benzodiazepine such as chlordiazepoxideand diazepam.
Air & Water Reaktionen
Insoluble in water.
Reaktivität anzeigen
OXAZEPAM is stable in light and is non hygroscopic. OXAZEPAM is stable in neutral solution. OXAZEPAM is hydrolyzed by acids and bases.
Brandgefahr
Flash point data for OXAZEPAM are not available; however, OXAZEPAM is probably combustible.
Pharmakokinetik
The half-life of oxazepam is approximately 4 to 8 hours, and cumulative effects with chronic therapy are much less than with long-acting benzodiazepines, such as chlordiazepoxide and diazepam. Lorazepam is the 2′-chloro derivative of oxazepam and has a similarly short half-life (2–6 hours) and pharmacological activity.
Clinical Use
Oxazepam
Arzneimittelwechselwirkung
Potentially hazardous interactions with other drugs
Antibacterials: metabolism possibly increased by rifampicin.
Antipsychotics: enhanced sedative effects; risk of serious adverse effects in combination with clozapine.
Antivirals: possibly increased concentration with ritonavir.
Sodium oxybate: enhanced effects of sodium oxybate - avoid.
Ulcer-healing drugs: metabolism inhibited by cimetidine.
Stoffwechsel
Oxazepam is an active metabolite of both chlordiazepoxide and diazepam and is marketed separately, as a shortacting anxiolytic agent. Oxazepam is rapidly inactivated to glucuronidated metabolites that are excreted in the urine.

OXAZEPAM Upstream-Materialien And Downstream Produkte

604-75-1, OXAZEPAM Verwandte Suche:

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