Clozapine Powder API CAS 5786-21-0

What is Clozapine ?

The appearance of Clozapine powder is light yellow crystalline powder. Odorless. Tasteless. Insoluble in water. Clozapine was withdrawn from the market in 1976 due to neutropenia. Later research proved that this product had a good effect on drug-resistant schizophrenia, and it was listed again in Sweden and the United States in 1989 and 1990. This product is a non-classical antipsychotic drug, which can selectively block the DA receptor in the limbic system of midbrain and has little effect on the DA receptor in the substantia nigra striatum. It has weak blocking effect on D2 receptor, strong blocking effect on D1 receptor, antagonistic effect on D4 receptor and strong blocking effect on 5-HT2 receptor. Therefore, it has a strong antipsychotic effect, while EPS is rare and will not cause rigidity reaction. Because Clozapine can directly inhibit the ascending activation system of midbrain reticular structure, it has a powerful sedative and hypnotic effect.
Clozapine powder API is used for schizophrenia, and has good curative effect on hallucinations, delusions and adolescence. Besides being effective for positive symptoms such as agitation, hallucinations and delusions,CLOZAPINE also has a good effect on negative symptoms. Because this product is different from the classical antipsychotics in blocking DA receptor, HF-1854 may be effective to switch to this product for some patients with poor curative effect of classical antipsychotics. It can also be used for manic episode and improving obstinate sleep disorder.
In addition, Asaleptin also has anticholinergic effect, NE blocking effect, sympathetic nerve blocking effect, muscle relaxation effect and antihistamine effect.

Product name	Clozapine
CAS	5786-21-0
structural formula	C18H19ClN4
molecular weight	326.82
EINECS	227-313-7
melting point	182-185°C
boiling point	482.71°C (rough estimate)
Acidity coefficient (pKa)	3.70, 7.60(at 25℃)
density	1.1327 (rough estimate)
Storage condition	2-8°C

What is the pharmacokinetics of Clozapine ? 

Food has no effect on the absorption rate and degree of Clozapine, and the bioavailability varies greatly among individuals, with an average of about 50% ~ 60%, which has the first-pass effect of the liver. After liver metabolism, 80% of them appear in urine and feces as metabolites, and the main metabolites are N- demethylclozapine and N- oxide of clozapine. Under the same dose and weight, the serum drug concentration of female patients is significantly higher than that of male patients, and the renal clearance rate and drug metabolism are significantly reduced in the elderly. Clozapine powder API can be secreted from milk and can pass through the blood-brain barrier.

What is the use and efficacy of Clozapine  ?

 

 

Clozapine is the earliest second-generation antipsychotic used in psychiatry. Multiple receptor antagonists play an antipsychotic role mainly by inhibiting the central serotonin 2 receptor.
1. Clozapine powder API can be used for acute and chronic madness. It is used to treat trance, inverted soul and dream, sadness and crying, palpitation, limb fatigue, sudden onset, sudden rage and ignorance, glare and other symptoms.
2. LEPONEX can be used for various mad diseases caused by various reasons. Such as impatience, or destroying houses and hitting people, or crying and laughing, emotional anxiety, tension, and sometimes mania.

3. HF-1854 can be used for behavioral disorders with mental retardation. For example, speech development is slow, expression ability is poor, thinking and understanding are slow, and abstract and generalization ability is lacking. Perception is slow and the range of perception is narrow, so it is difficult to distinguish the small differences in shape, size and color of objects. Lack of concentration and narrow attention span. Poor memory, slow memorization and inaccurate reproduction. Childish, immature, emotionally unstable, lacking self-control and impulsive. Often timid, withdrawn, shy, shrinking, etc. Uneven body shape, uncoordinated movement, poor flexibility, or excessive activity, destruction, aggression or other bad behavior.
4. Asaleptin can be used for drug or alcohol dependence withdrawal syndrome. Such as acute tremor, emotional excitement, easy to jump, nausea, vomiting and sweating. Once drinking alcohol, the symptoms disappear immediately, otherwise it lasts for several days. What's more, there are temporary illusions, hallucinations, visual distortion and unclear pronunciation. Finally, there may be seizures or delirium tremens.
5. It can be used for insomnia. Clozapine powder API is suitable for all kinds of insomnia, such as dreaminess, forgetfulness, limb fatigue and mental fatigue.

 Product Specification

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