Clobazam

Bezeichnung:Clobazam

CAS-Nr22316-47-8

Englisch Name:CLOBAZAM

CBNumberCB9205925

SummenformelC16H13ClN2O2

Molgewicht300.74

MOL-Datei22316-47-8.mol

Synonyma

Clobazam

Clobazam physikalisch-chemischer Eigenschaften

Schmelzpunkt	162-164°C
Siedepunkt	211°C (rough estimate)
Dichte	1.2682 (rough estimate)
Brechungsindex	1.5200 (estimate)
Flammpunkt	11 °C
storage temp.	2-8°C
Löslichkeit	Slightly soluble in water, freely soluble in methylene chloride, sparingly soluble in alcohol.
Aggregatzustand	Solid
pka	8.59±0.20(Predicted)
Farbe	White to Off-White
CAS Datenbank	22316-47-8(CAS DataBase Reference)
EPA chemische Informationen	1H-1,5-Benzodiazepine-2,4(3H,5H)-dione, 7-chloro-1-methyl-5-phenyl- (22316-47-8)

Sicherheit

Kennzeichnung gefährlicher	F,T
R-Sätze:	11-23/24/25-39/23/24/25
S-Sätze:	16-36/37-45-24/25-22-7
RIDADR	3249
WGK Germany	3
RTECS-Nr.	DE9600000
HazardClass	6.1(b)
PackingGroup	III
Giftige Stoffe Daten	22316-47-8(Hazardous Substances Data)

Gefahreninformationscode (GHS)

CLOBAZAM Chemische Eigenschaften,Einsatz,Produktion Methoden

R-Sätze Betriebsanweisung:
R11:Leichtentzündlich.
R23/24/25:Giftig beim Einatmen, Verschlucken und Berührung mit der Haut.
R39/23/24/25:Giftig: ernste Gefahr irreversiblen Schadens durch Einatmen, Berührung mit der Haut und durch Verschlucken.
S-Sätze Betriebsanweisung:
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).
S24/25:Berührung mit den Augen und der Haut vermeiden.
S22:Staub nicht einatmen.
Chemische Eigenschaften
N/AWhite Solid
Originator
Urbanyl,Diamant,France,1975
Verwenden
Benzodiazepine psychotherapeutic agent. Clobazam (CLB) has proven efficacy against multiple seizure types. Controlled substance (depressant).
Definition
ChEBI: 7-Chloro-1H-1,5-benzodiazepine-2,4(3H,5H)-dione in which the hydrogen attached to the nitrogen at position 1 is substituted by a methyl group, whilst that attached to the other nitrogen is substitute by a phenyl group. It is used for the short-term management of acute anxiety and as an adjunct in the treatment of epilepsy in association with other antiepileptics.
Manufacturing Process
1.65 g of N-phenyl-N-(2-amino-5-chlorophenyl)-malonic acid ethyl ester amide of MP 108° to 109°C are added to a sodium ethoxide solution, prepared from 20 ml of absolute alcohol and 150 mg of sodium. The solution is allowed to rest for 5 hours at room temperature. Then 1 ml of methyl iodide is added and the reaction mixture is refluxed for 7 hours. After evaporation of the solution in vacuo it is mixed with water and the solution is shaken with
methylene chloride. The methylene chloride phase is dried and evaporated. By treatment of the residue with ethyl acetate/charcoal are isolated 500 mg of 7- chloro-1-methyl-5-phenyl-1H-1,5-benzodiazepine-2,4-(3H,5H)-dione of MP 180° to 182°C. The yield amounts to 34% of theory
Trademarks
Urbanyl (Hoechst- Roussel).
Therapeutic Function
Tranquilizer
Clinical Use
Benzodiazepine:
Anticonvulsant

Anxiolytic
Sicherheitsprofil
Poison by ingestion and intraperitoneal routes. Moderately toxic by subcutaneous route. Human systemic effects by ingestion: wakefulness, withdrawal, nausea and vomiting. An experimental teratogen. Other experimental reproductive effects. A tranquhzer. When heated to decomposition it emits very toxic fumes of NOx and Cl-. See also DIAZEPAM.
Arzneimittelwechselwirkung
Potentially hazardous interactions with other drugs
Antibacterials: metabolism possibly increased by rifampicin.
Antipsychotics: increased sedative effects; serious adverse events reported with clozapine and benzodiazepines.
Antivirals: concentration possibly increased by ritonavir.
Disulfiram: metabolism of clobazam inhibited; increased sedative effects.
Sodium oxybate: enhanced effects of sodium oxybate - avoid.
Stoffwechsel
Clobazam is metabolised in the liver by demethylation and hydroxylation; the cytochrome P450 isoenzyme CYP2C19 plays a role in its metabolism. Unlike the 1,4-benzodiazepines such as diazepam, clobazam, a 1,5-benzodiazepine, is hydroxylated at the 4-position rather than the 3-position.
Clobazam is excreted unchanged and as its main active metabolite, N-desmethylclobazam, mainly in the urine.

CLOBAZAM Upstream-Materialien And Downstream Produkte

22316-47-8, CLOBAZAM Verwandte Suche:

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