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Clozapine

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Name

Clozapine

EINECS 227-313-7
CAS No. 5786-21-0 Density 1.319 g/cm3
Solubility ethanol: 1 mg/mL Melting Point 182-185 °C
Formula C18H19ClN4 Boiling Point 489.159 °C at 760 mmHg
Molecular Weight 326.86 Flash Point 249.635 °C
Transport Information UN 2811 6.1/PG 3 Appearance Yellow Crystalline Solid
Safety 26 Risk Codes 22-36/37/38
Molecular Structure Molecular Structure of 5786-21-0 (Clozapine) Hazard Symbols HarmfulXn, IrritantXi
Synonyms

Clorazil;Fazaclo;Iprox;Clozapina [INN-Spanish];8-Chloro-11-(4-methyl-1-piperazinyl)-5H-dibenzo(b,e)(1,4)diazepine;5H-Dibenzo(b,e)(1,4)diazepine, 8-chloro-11-(4-methyl-1-piperazinyl)-;Leponex;Asaleptin;Clozaril (TN);Clozapine [USAN:BAN:INN];8-chloro-11(4-methy-1-piperaziong)-5-H-dibenzo[b,e][1.4]diazepine;

 

Clozapine Chemical Properties

Empirical Formula: C18H19ClN4
Molecular Weight: 326.8233 g/mol
EINECS: 227-313-7 
Index of Refraction: 1.681
Density: 1.31 g/cm3
Flash Point: 249.6 °C
Melting point: 182-185 °C
Solubility: Ethanol: 1 mg/mL
Appearance: Yellow crystalline solid
Enthalpy of Vaporization: 75.54 kJ/mol
Boiling Point: 489.2 °C at 760 mmHg
Vapour Pressure: 1.02E-09 mmHg at 25 °C
Structure of Clozapine (CAS NO.5786-21-0):
                     
IUPAC Name: 3-Chloro-6-(4-methylpiperazin-1-yl)-5H-benzo[c][1,5]benzodiazepine
Product Category: Active Pharmaceutical Ingredients;Intermediates & Fine Chemicals;Dopamine receptor

Clozapine History

 Clozapine (CAS NO.5786-21-0) by Sandoz in 1961, and introduced in Europe in 10 years. In 1975, the report of agranulocytosis leading to death in some patients treated with clozapine, clozapine manufacturers to voluntarily withdraw. Clozapine fell out of favor for more than a decade. However, studies have shown that clozapine is more effective for refractory schizophrenia than other antipsychotics, the U.S. Food and Drug Administration and health authorities in most other countries approved its use only for refractory schizophrenia Patients require regular blood tests to monitor the neutrophil, and then agranuloctytosis development. December 2002, clozapine was also approved to reduce the risk of suicide in patients with schizophrenia or schizoaffective is considered in the risk of suicide.

Clozapine Uses

 Clozapine (CAS NO.5786-21-0) can be used as an antipsychotic.

Clozapine Production

 Clozapine (CAS NO.5786-21-0) can be obtained from the reaction of 2 - Amino -4 - chloro-aniline 2 -2 '- carboxylic acid (4''-methyl) piperazine with Phosphorus oxychloride .

Clozapine Toxicity Data With Reference

Organism Test Type Route Reported Dose (Normalized Dose) Effect Source
child TDLo oral 4762ug/kg (4.762mg/kg) BEHAVIORAL: ATAXIA
BEHAVIORAL: MUSCLE CONTRACTION OR SPASTICITY)
BEHAVIORAL: ANTIPSYCHOTIC
American Journal of Emergency Medicine. Vol. 14, Pg. 462, 1996.
dog LD50 oral 145mg/kg (145mg/kg) GASTROINTESTINAL: NAUSEA OR VOMITING Farmaco, Edizione Pratica. Vol. 26, Pg. 585, 1971.
guinea pig LD50 oral 510mg/kg (510mg/kg)   Farmaco, Edizione Pratica. Vol. 26, Pg. 585, 1971.
human TDLo oral 5mg/kg/7D-I (5mg/kg) CARDIAC: PULSE RATE INCREASE WITHOUT FALL IN BP Arzneimittel-Forschung. Drug Research. Vol. 22, Pg. 919, 1972.
man TDLo oral 4286ug/kg/11D (4.286mg/kg) GASTROINTESTINAL: "HYPERMOTILITY, DIARRHEA"
BLOOD: CHANGES IN CELL COUNT (UNSPECIFIED)
Journal of Clinical Pyschopharmacology. Vol. 13, Pg. 155, 1993.
man TDLo oral 5357ug/kg/5D- (5.357mg/kg) BEHAVIORAL: "HALLUCINATIONS, DISTORTED PERCEPTIONS"
BEHAVIORAL: ANTIPSYCHOTIC
CARDIAC: PULSE RATE INCREASE WITHOUT FALL IN BP
Journal of Clinical Pyschopharmacology. Vol. 12, Pg. 139, 1992.
man TDLo oral 27mg/kg/13D-I (27mg/kg) AUTONOMIC NERVOUS SYSTEM: "SMOOTH MUSCLE RELAXANT (MECHANISM UNDEFINED, SPASMOLYTIC)"
BEHAVIORAL: "HALLUCINATIONS, DISTORTED PERCEPTIONS"
BEHAVIORAL: ATAXIA
Journal of Clinical Psychiatry. Vol. 55, Pg. 38, 1994.
man TDLo oral 40mg/kg (40mg/kg) BEHAVIORAL: COMA

LUNGS, THORAX, OR RESPIRATION: RESPIRATORY DEPRESSION
VASCULAR: BP LOWERING NOT CHARACTERIZED IN AUTONOMIC SECTION
Veterinary and Human Toxicology. Vol. 41, Pg. 20, 1999.
man TDLo oral 86mg/kg/15D-I (86mg/kg) CARDIAC: PULSE RATE INCREASE WITHOUT FALL IN BP
LUNGS, THORAX, OR RESPIRATION: OTHER CHANGES
British Journal of Psychiatry. Vol. 173, Pg. 440, 1998.
man TDLo oral 270mg/kg/6W-I (270mg/kg) LUNGS, THORAX, OR RESPIRATION: STRUCTURAL OR FUNCTIONAL CHANGE IN TRACHEA OR BRONCHI
BLOOD: AGRANULOCYTOSIS
GASTROINTESTINAL: "HYPERMOTILITY, DIARRHEA"
Annales de Medecine Interne. Vol. 144, Pg. 494, 1993.
man TDLo oral 429mg/kg/60D- (429mg/kg) BEHAVIORAL: MUSCLE CONTRACTION OR SPASTICITY) American Journal of Psychiatry. Vol. 152, Pg. 649, 1995.
man TDLo oral 429mg/kg (429mg/kg) BEHAVIORAL: MUSCLE CONTRACTION OR SPASTICITY)
CARDIAC: PULSE RATE INCREASE WITHOUT FALL IN BP
BEHAVIORAL: COMA
Journal of Toxicology, Clinical Toxicology. Vol. 38, Pg. 325, 2000.
man TDLo oral 2211mg/kg/37W (2211mg/kg) BLOOD: "CHANGES IN SERUM COMPOSITION (E.G., TP, BILIRUBIN, CHOLESTEROL)" Journal of Clinical Pyschopharmacology. Vol. 15, Pg. 287, 1995.
man TDLo oral 3280mg/kg/82W (3280mg/kg) BLOOD: AGRANULOCYTOSIS American Journal of Psychiatry. Vol. 153, Pg. 1503, 1996.
mouse LD50 intraperitoneal 90mg/kg (90mg/kg) BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD
BEHAVIORAL: MUSCLE CONTRACTION OR SPASTICITY)
LUNGS, THORAX, OR RESPIRATION: DYSPNEA
Farmaco, Edizione Pratica. Vol. 26, Pg. 585, 1971.
mouse LD50 intravenous 36500ug/kg (36.5mg/kg) BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY)
LUNGS, THORAX, OR RESPIRATION: RESPIRATORY DEPRESSION
BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD
Kiso to Rinsho. Clinical Report. Vol. 7, Pg. 667, 1973.
mouse LD50 oral 150mg/kg (150mg/kg)   Journal of Medicinal Chemistry. Vol. 23, Pg. 878, 1980.
mouse LD50 subcutaneous 194mg/kg (194mg/kg) BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY)
BEHAVIORAL: EXCITEMENT
BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD
Kiso to Rinsho. Clinical Report. Vol. 7, Pg. 667, 1973.
rat LD50 intramuscular 210mg/kg (210mg/kg)   Farmaco, Edizione Pratica. Vol. 26, Pg. 585, 1971.
rat LD50 intravenous 41600ug/kg (41.6mg/kg) BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD
LUNGS, THORAX, OR RESPIRATION: RESPIRATORY DEPRESSION
BEHAVIORAL: ATAXIA
Kiso to Rinsho. Clinical Report. Vol. 7, Pg. 667, 1973.
rat LD50 oral 251mg/kg (251mg/kg)   Kiso to Rinsho. Clinical Report. Vol. 7, Pg. 667, 1973.
rat LD50 subcutaneous 240mg/kg (240mg/kg) BEHAVIORAL: ALTERED SLEEP TIME (INCLUDING CHANGE IN RIGHTING REFLEX)
BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD
LUNGS, THORAX, OR RESPIRATION: RESPIRATORY DEPRESSION
Kiso to Rinsho. Clinical Report. Vol. 7, Pg. 667, 1973.
women TDLo oral 20mg/kg (20mg/kg) BEHAVIORAL: COMA
BLOOD: LEUKOPENIA
GASTROINTESTINAL: CHANGES IN STRUCTURE OR FUNCTION OF ENDOCRINE PANCREAS
Annals of Internal Medicine. Vol. 121, Pg. 722, 1994.
women TDLo oral 28mg/kg/2W-I (28mg/kg) GASTROINTESTINAL: CHANGES IN STRUCTURE OR FUNCTION OF ENDOCRINE PANCREAS Lancet. Vol. 340, Pg. 251, 1992.
women TDLo oral 96mg/kg/48D-I (96mg/kg) BLOOD: LEUKOPENIA
BLOOD: AGRANULOCYTOSIS
Human Psychopharmacology. Vol. 13, Pg. 583, 1998.
women TDLo oral 104mg/kg/26D- (104mg/kg) BLOOD: EOSINOPHILIA Journal of Clinical Psychiatry. Vol. 59, Pg. 195, 1998.
women TDLo oral 168mg/kg/4W-I (168mg/kg) BLOOD: AGRANULOCYTOSIS Netherlands Journal of Medicine. Vol. 52, Pg. 26, 1998.
women TDLo oral 280mg/kg/5W-I (280mg/kg) LIVER: "HEPATITIS (HEPATOCELLULAR NECROSIS), DIFFUSE"
BLOOD: EOSINOPHILIA
American Journal of Psychiatry. Vol. 150, Pg. 985, 1993.

Clozapine Safety Profile

Hazard Codes: HarmfulXn,IrritantXi
Risk Statements: 22-36/37/38 
R22:Harmful if swallowed. 
R36/37/38:Irritating to eyes, respiratory system and skin.
Safety Statements: 26 
S26: In case of contact with eyes, rinse immediately with plenty of water and seek medical advice.

Clozapine Specification

 Clozapine , its cas register number is 5786-21-0. It also can be called 8-Chloro-11-(4-methyl-1-piperazinyl)-5H-dibenzo[b,e][1,4]diazepine ; Leponex ; and 5H-Dibenzo(b,e)(1,4)diazepine, 8-chloro-11-(4-methyl-1-piperazinyl)- . Many minor though some serious and potentially fatal: the more common include constipation, drooling, muscle stiffness, sedation, tremors, orthostasis, hyperglycemia, and weight gain. Extrapyramidal symptoms may subside somewhat after a person switches from another antipsychotic to Clozapine. Clozapine (CAS NO.5786-21-0) also carries black box warnings for seizures, myocarditis, and "other adverse cardiovascular and respiratory effects." Slow titration of dosing may also decrease the risk for orthostatic hypotension and other adverse cardiovascular side effects. It may have a synergistic effect with the sedating action of other drugs such as benzodiazepines, and thus respiratory depression may result with concomitant use. Care should be taken, especially if the latter drugs are given parenterally.

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