Clonazepam

Gefahreninformationscode (GHS)

• Bildanzeige (GHS)

  

• Alarmwort

  Achtung

• Gefahrenhinweise

  H225：Flüssigkeit und Dampf leicht entzündbar.

  H370：Schädigt die Organe.

• Sicherheit

  P210：Von Hitze, heißen Oberflächen, Funken, offenen Flammen und anderen Zündquellenarten fernhalten. Nicht rauchen.

  P260：Dampf/Aerosol/Nebel nicht einatmen.

  P280：Schutzhandschuhe/Schutzkleidung/Augenschutz tragen.

  P301+P310：BEI VERSCHLUCKEN: Sofort GIFTINFORMATIONSZENTRUM/Arzt/... (geeignete Stelle für medizinische Notfallversorgung vom Hersteller/Lieferanten anzugeben) anrufen.

  P311：GIFTINFORMATIONSZENTRUM/Arzt anrufen.

Clonazepam 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:

  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).
  S24/25:Berührung mit den Augen und der Haut vermeiden.
  S22:Staub nicht einatmen.

• Beschreibung

  Clonazepam (Item No. 14263) is an analytical reference material categorized as a benzodiazepine. Clonazepam is regulated as a Schedule IV compound in the United States. This product is intended for research and forensic applications.

• Chemische Eigenschaften

  Tan Solid

• Originator

  Rivotril,Roche,France,1973

• Verwenden

  Antiepileptic agent with anxiolytic and antimanic properties. Anticonvulsant. This is a controlled substance (depressant)

• Definition

  ChEBI: 1,3-Dihydro-2H-1,4-benzodiazepin-2-one in which the hydrogens at positions 5 and 7 are substituted by 2-chlorophenyl and nitro groups, respectively. It is used in the treatment of all types of epilepsy and seizures, as well as myoclonus nd associated abnormal movements, and panic disorders. However, its use can be limited by the development of tolerance and by sedation.

• Manufacturing Process

  The following description is taken from US Patent 3,116,203. A stirred solution of 75 g of 2-amino-2'-nitrobenzophenone in 700 ml of hot concentrated hydrochloric acid was cooled to 0°C and a solution of 21.5 g of sodium nitrite in 50 ml of water was added in the course of 3 hours. The temperature of the suspension was kept at 2° to 7°C during the addition. The resulting clear solution was poured into a stirred solution of 37 g of cuprous chloride in 350 ml of hydrochloric acid 1:1. The solid which had formed after a few minutes was filtered off, washed with water and recrystallized from ethanol. Crystals of 2-chloro-2'-nitrobenzophenone melting at 76° to 79°C were obtained.
  A solution of 20 g of 2-chloro-2'-nitrobenzophenone in 450 ml of ethanol was hydrogenated at normal pressure and room temperature with Raney nickel. After uptake of about 6 liters of hydrogen the catalyst was filtered off, and the alcohol then removed in vacuo. The residue was distilled in a bulb tube at 0.4 mm and a bath temperature of 150° to 165°C giving a yellow oil. The oil was dissolved in alcohol, and on addition of water, needles of 2-amino-2'- chlorobenzophenone melting at 58° to 60°C were obtained.
  To a solution of 42 g of 2-amino-2'-chlorobenzophenone in 500 ml of benzene, 19 ml of bromoacetyl bromide was added dropwise. After refluxing for 2 hours, the solution was cooled, washed with 2 N sodium hydroxide and evaporated. The residue was recrystallized from methanol giving crystals of 2- bromo-2'-(2-chlorobenzoyl)acetanilide melting at 119° to 121°C.
  To a solution of 14.5 g of 2-bromo-2'-(2-chlorobenzoyl)acetanilide in 100 ml of tetrahydrofuran, an excess of liquid ammonia (ca 150 ml) was added. The ammonia was kept refluxing with a dry-ice condenser for 3 hours after which time the ammonia was allowed to evaporate and the solution was poured into water. Crystals of 2-amino-2'-(2-chlorobenzoyl)acetanilide were collected, which after recrystallization from ethanol melted at 162° to 164°C.
  A solution of 3 g of 2-amino-2'-(2-chlorobenzoyl)acetanilide in 50 ml of pyridine was refluxed for 24 hours after which time the pyridine was removed in vacuo. The residue was recrystallized from methanol and a mixture of dichloromethane and ether giving crystals of 5-(2-chlorophenyl)-3H-1,4- benzodiazepin-2(1H)-one melting at 212° to 213°C.
  To a solution of 13.5 g of 5-(2-chlorophenyl)-3H-1,4-benzodiazepin-2(1H)-one in 60 ml of concentrated sulfuric acid, a solution of 5.5 g of potassium nitrate in 20 ml concentrated sulfuric acid was added dropwise. The solution then was heated in a bath at 45° to 50°C for 2.5 hours, cooled and poured on ice. After neutralizing with ammonia, the formed precipitate was filtered off and boiled with ethanol. A small amount of white insoluble material was then filtered off. The alcoholic solution on concentration yielded crystals of 7-nitro-5-(2- chlorophenyl)-3H-1,4-benzodiazepin-2(1H)-one which, after recrystallization from dichloromethane, melted at 238° to 240°C.

• Trademarks

  Klonopin (Roche). Antelepsin (Arzneimittelwerk Dresden), Clonopin/ Rivotril (Roche).

• Therapeutic Function

  Anticonvulsant

• Allgemeine Beschreibung

  Clonazepam is useful in absence seizures and in myoclonicseizures. Tolerance to the anticonvulsant effect of the clonazepamoften developed rather quickly, and it is a commonproblem with the BZDs. Metabolism involves hydroxylationof the C-3 position, followed by glucuronidation andnitro group reduction, followed by acetylation.

• Hazard

  Moderately toxic.

• Clinical Use

  Benzodiazepine:
  Anticonvulsant
  
  Anxiolytic
  
  Restless leg syndrome

• Arzneimittelwechselwirkung

  Potentially hazardous interactions with other drugs
  Antibacterials: metabolism possibly increased by rifampicin.
  Antipsychotics: increased sedative effects; increased risk of hypotension, bradycardia and respiratory depression with parenteral clonazepam and IM olanzapine; risk of serious adverse effects in combination with clozapine.
  Antivirals: concentration possibly increased by ritonavir.
  Disulfiram: metabolism inhibited, increased sedative effects.
  Sodium oxybate: enhanced effects of sodium oxybate - avoid.

• Stoffwechsel

  Clonazepam is extensively metabolised in the liver, its principal metabolite being 7-aminoclonazepam, which has no antiepileptic activity; minor metabolites are the 7-acetamido- and 3-hydroxy-derivatives. It is excreted mainly in the urine almost entirely as its metabolites in free or conjugated form.

Clonazepam Upstream-Materialien And Downstream Produkte

1622-61-3, Clonazepam Verwandte Suche: