Antipsychotic Drugs API CAS 106266-06-2 Risperidone for Sale


Product Name: Risperidone
Synonyms:RISPERDAL;RISPERIDAL;RISPERIDONE
CAS:106266-06-2
MF:C23H27FN4O2
MW:410.48
Product Categories: Active Pharmaceutical Ingredients;API;APIs;Risperidone;
Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals;API's;Dopamine receptor;Heterocycles;Pharmaceutical raw material;Antibiotics
Melting point: 170C
Fp: 9
Storage temp.: Room temp
Chemical Properties: Crystalline Solid
Purity: 99%
Package:1kg/25kg/package
Uses: neuroprotectant, inhibitory neurotransmitter, GABA agonist
Uses: for the treatment of schizophrenia in adults and in adolescents, ages 13 to 17, and for the short-term treatment of manic or mixed episodes of bipolar I disorder in children and adolescents ages 10 to 17. May also be used to manage symptoms of inappropria.
Uses: A combined serotonin (5-HT2) and dopamine (D2) receptor antagonist.


Risperidone Description

Characters: 1mg Risperidone tablets are white film-coated tablets, after removing the coating,they are white; 2mg Risperidone tablets are pale orange film-coated tablets,after removing the coating, they are white.

Pharmacological characteristics: this product is benzisoxazole derivative,it is a new generation of antipsychotics. Its active ingredient Risperidone  is a selective monoamine antagonist with unique properties, it has a high affinity with the serotonin 5-HT2 receptors and the dopamine D2 receptors. Risperidone can also be combined with 1-adrenergic receptors, and it can combine with the histamine H1-receptors and 2-adrenoceptors  with lower affinity. Risperidone can not combine with cholinergic receptors. Risperidone is a potent D2 antagonist, which can improve the positive symptoms of schizophrenia, but inhibition of motor function, as well as catalepsy caused by it are lesser than classical antipsychotics. Balance of serotonin and dopamine antagonism of the central nervous systemcan can reduce the potential for extrapyramidal side effects, and  expand its role in the treatment of negative symptoms and affective symptoms of schizophrenia.

Pharmacokinetic characteristics: after oral administration,Risperidone can be completely absorbed and the peak of plasma concentration is reached within 1-2 hours, and its absorption is not affected by food. In vivo, Risperidone is metabolized to 9-hydroxy portion-Risperidone, which has similar pharmacological effects to Risperidone. this product can be quickly distributed in the body, Risperidone plasma protein binding rate is 88%, 9-hydroxy-Risperidone plasma protein binding rate is 77%. the drug elimination half-life is about three hours, antipsychotic active ingredient elimination half-life is 24 hours. most patients reach a steady state of Risperidone in a day, and after 4-5 days,they reach the 9-hydroxy-risperidone homeostasis. One week after treatment, 70% of the drug  is excreted in urine and 14% of the drug is through fecal excretion, 35-45% of the section of urinary excretion are Risperidone and 9-hydroxy-risperidone, the remaining is non-active metabolite. Elderly patients and patients with renal insufficiency have higher plasma concentrations of Risperidone, so they have slower clearance.


Benefits and side effects

Risperidone advantages:
(1)it is effective not only for positive symptoms, but also  effective for negative symptoms, it can also improve cognitive disorders, thereby improving the patient's condition as a whole.
(2) adverse reactions of the drug is light,it  produces fewer extrapyramidal side effects.
(3)it is easy to adjust the dose, for most patients, the dose is 2~6mg/d, which can produce a therapeutic effect.
(4) for some poor therapeutic effect of conventional antipsychotics or intolerant patients, Risperidone may produce better results.
(5)Compliance of patients  greatly increases during the period of medication.
(6) foreign research shows, Risperidone  can reduce the expenses of patients and reduce the overall expenditure of the patients, and thus more in line with the principles of health economics.

Risperidone side effects:
Risperidone common adverse reactions: insomnia, anxiety, agitation, headache; rare adverse reactions are: drowsiness, fatigue, dizziness, decreased attention, constipation, indigestion, nausea, vomiting, abdominal pain, blurred vision, priapism, erectile dysfunction, weak ejaculation, sexual apathy, urinary incontinence, rhinitis, rash and other allergic reactions. Risperidone can cause extrapyramidal side effects, tremors, rigidity, salivation, bradykinesia, akathisia, acute dystonia, orthostatic hypotensionlactation,lactation, gynecomastia, menstrual disorders, amenorrhea can occur occasionally, Risperidone can also cause weight gain, edema, and increased liver enzymes and so on.


Uses

1. It has antagonism effect on 5HT2 receptors and D2 receptors. It is used for acute and chronic schizophrenia.
2. Antipsychotic drugs.