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Clorazepate dipotassium

Clorazepate dipotassium structure

CAS No:
57109-90-7
Formula:
C16H11ClN2O3.HKO.K
Chemical Name:
Clorazepate dipotassium
Synonyms:
1H-1,4-Benzodiazepine-3-carboxylic acid,7-chloro-2,3-dihydro-2-oxo-5-phenyl-,potassium salt,compd. with potassium hydroxide (K(OH)) (1:1:1);1H-1,4-Benzodiazepine-3-carboxylic acid,7-chloro-2,3-dihydro-2-oxo-5-phenyl-,monopotassium salt,compd. with potassium hydroxide (1:1);1H-1,4-Benzodiazepine-3-carboxylic acid,7-chloro-2,3-dihydro-2-oxo-5-phenyl-,monopotassium salt,compd. with potassium hydroxide (K(OH)) (1:1);Potassium hydroxide (K(OH)),compd. with 7-chloro-2,3-dihydro-2-oxo-5-phenyl-1H-1,4-benzodiazepine-3-carboxylic acid monopotassium salt (1:1);Potassium hydroxide,compd. with 7-chloro-2,3-dihydro-2-oxo-5-phenyl-1H-1,4-benzodiazepine-3-carboxylic acid monopotassium salt (1:1);CB 4306;[2-Phenyl-2-(2-amino-5-chlorophenyl)-1-azavinyl]malonic acid;Tranxilene;Tranxene;Tranxilen;AB 35616;Chlorazepate dipotassium;Transene;Nevracten;Tencilan;TR 19119;Bipotassium chlorazepate;Clorazepate dipotassium;Dipotassium chlorazepate;Abbott 35616;Dipotassium clorazepate;Tranxilium;Chlorazepate;CM 4306;Mendon;Chlorazepate dipotassic;Novo-Clopate;Gen-Xene;Nu-Clopate;4306CB;Belseren;Dikalium chlorazepate;27665-58-3
Categories:
Analytical Chemistry > Standard

Description

Pale Yellow Solid

Dipotassium clorazepate is the compound of monopotassium clorazepate with potassium hydroxide. It is used for the management of anxiety disorders, for the short-term relief of anxiety, as adjunctive therapy in the management of epilepsy, and for the symptomatic relief of acute alcohol withdrawal. It has a role as a prodrug, an anticonvulsant, an anxiolytic drug and a GABA modulator. It contains a clorazepate monopotassium.|Clobazam is a benzodiazepine that is used as an anticonvulsant in the therapy of severe childhood epilepsy. Therapy with clobazam has not been associated with serum aminotransferase elevations, and clinically apparent liver injury from clobazam has yet to be reported and must be rare, if it occurs at all.|Clorazepate is a benzodiazepine used as an anticonvulsant as adjunctive therapy in management of epilepsy and as an anxiolytic for therapy of anxiety and alcohol withdrawal. Therapy with clorazepate is not associated with serum aminotransferase elevations, and cases of clinically apparent liver injury from clorazepate have been reported but are very rare.|A water-soluble benzodiazepine derivative effective in the treatment of anxiety. It has also muscle relaxant and anticonvulsant actions.

Clorazepate dipotassium Basic Attributes

Molecular Weight：

408.92

Exact Mass：

407.96800

EC Number：

260-565-6

ATC Code：

N - Nervous system

HScode：

2933910000

Characteristics

PSA：

97.14000

XLogP3：

0.57690

Melting Point：

228-235°C

Boiling Point：

563.9ºC at 760mmHg

Flash Point：

11 °C

Water Solubility：

Freely soluble to very soluble in water, very slightly soluble in alcohol, practically insoluble in methylene chloride. Solutions in water and in alcohol are unstable and are to be used immediately.

Storage Conditions：

2-8°C

Toxicity：

Oral-rat LD50: 880 mg/kg; Oral-Mouse LD50: 700 mg/kg

Flammability characteristics：

Thermal decomposition emits toxic nitrogen oxides, chlorides, potassium oxide fumes

Safety Information

Packing level：

III

Hazard category：

6.1(b)

Transport codes：

3249

wgk germany：

hazard class code：

22-63-39/23/24/25-23/24/25-11

safety instructions：

22-36/37/39-45-36/37-16-7

RTECS Number：

DE8750000

Marks：

Xn,T,F

Storage features：

The warehouse is low-temperature, ventilated and dry

Precautionary statement(s)：

P280-P301 + P312 + P330

Hazard Statements：

H302-H361

GHS Classification：

|Warning|H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]|P201, P202, P264, P270, P281, P301+P312, P308+P313, P330, P405, and P501|Aggregated GHS information provided by 42 companies from 4 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Toxicity

Toxicity class：

moderately toxic

Hepatotoxicity：

Limited data are available on the hepatotoxicity of clobazam. In clinical trials, clobazam was not associated with an increased frequency of serum aminotransferase elevations as compared to placebo treatment, and there were no instances of clinically apparent liver injury. No individual case reports of clobazam hepatotoxicity have been published since its wide spread clinical availability. Liver injury from benzodiazepines is quite rare, but isolated instances of hepatotoxicity have been reported for clorazepate and clonazepam, two other benzodiazepines used predominantly in the therapy of epilepsy. Thus, clinically apparent liver injury due to clobazam must be rare, if it occurs at all.|Clorazepate, as with other benzodiazepines, is rarely associated with serum ALT elevations, and clinically apparent liver injury from clorazepate is extremely rare. A few only partially convincing case reports of acute hepatocellular injury from clorazepate have been reported. Rare instances of drug induced liver injury have been reported with other benzodiazepines, such as chlordiazepoxide, diazepam, flurazepam, triazolam and alprazolam. In benzodiazepine related cases of acute liver injury, the latency has ranged from a few weeks to 6 months; the typical pattern of liver enzyme elevations has been cholestatic or mixed, but instances of hepatocellular patterns have also been reported. The injury is usually mild to moderate in severity and self-limited. Fever and rash have not been described nor has autoantibody formation.

Drug Information

LiverTox Summary：

Clobazam is a benzodiazepine that is used as an anticonvulsant in the therapy of severe childhood epilepsy. Therapy with clobazam has not been associated with serum aminotransferase elevations, and clinically apparent liver injury from clobazam has yet to be reported and must be rare, if it occurs at all.|Clorazepate is a benzodiazepine used as an anticonvulsant as adjunctive therapy in management of epilepsy and as an anxiolytic for therapy of anxiety and alcohol withdrawal. Therapy with clorazepate is not associated with serum aminotransferase elevations, and cases of clinically apparent liver injury from clorazepate have been reported but are very rare.

Drug Classes：

Anticonvulsants

MeSH：

Substances that do not act as agonists or antagonists but do affect the GAMMA-AMINOBUTYRIC ACID receptor-ionophore complex. GABA-A receptors (RECEPTORS, GABA-A) appear to have at least three allosteric sites at which modulators act: a site at which BENZODIAZEPINES act by increasing the opening frequency of GAMMA-AMINOBUTYRIC ACID-activated chloride channels; a site at which BARBITURATES act to prolong the duration of channel opening; and a site at which some steroids may act. GENERAL ANESTHETICS probably act at least partly by potentiating GABAergic responses, but they are not included here. (See all compounds classified as GABA Modulators.)|Agents that alleviate ANXIETY, tension, and ANXIETY DISORDERS, promote sedation, and have a calming effect without affecting clarity of consciousness or neurologic conditions. ADRENERGIC BETA-ANTAGONISTS are commonly used in the symptomatic treatment of anxiety but are not included here. (See all compounds classified as Anti-Anxiety Agents.)|Drugs used to prevent SEIZURES or reduce their severity. (See all compounds classified as Anticonvulsants.)

MeSH Entry Terms：

4306-CB

Clorazepate dipotassium Use and Manufacturing

Uses

Anxiolytic. Controlled substance (depressant).

Use Classification：

Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients

Computed Properties

Molecular Weight:408.92
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:5
Rotatable Bond Count:1
Exact Mass:407.9681475
Monoisotopic Mass:407.9681475
Topological Polar Surface Area:82.6
Heavy Atom Count:25
Complexity:482
Undefined Atom Stereocenter Count:1
Covalently-Bonded Unit Count:4
Compound Is Canonicalized:Yes