Product name: Visteon
Alias: risperidone tablets
English name: Risperidone tablets
Chinese Pinyin: Li Peitong Pian
Edit this instruction
It can be used to treat acute and chronic schizophrenia, as well as obvious positive symptoms (such as hallucination, delusion, thinking disorder, hostility and doubt) and obvious negative symptoms (such as slow response, apathy, social apathy and lack of speech) in other mental states. It can also relieve emotional symptoms related to schizophrenia (such as depression, guilt and anxiety). For patients with effective treatment in acute phase, this product can continue to play its clinical effect in maintenance period.
Edit this paragraph specification
At present, there are two forms of vestibular bone: 1) tablets: 1mg X 20 tablets/box, 2mg X 20 tablets/box; 2) Oral liquid: 30ml/ bottle (1ml= 1mg). Vestibular bone oral liquid was listed in China in early 2004, which is a new antipsychotic drug at present.
Edit this paragraph character.
The chemical name of risperidone is 3-[2-[4-(6- fluoro-1, 2- benzisoxazole -3- yl)-1- piperidinyl] ethyl]-6,7,8,9-tetrahydro -2- methyl -4H- pyridine. The molecular formula is C23H27FN4O2 and the molecular weight is 4 10.49.
1 mg tablets are white film-coated tablets, which are white after removing the coating; 2 mg tablets are light orange film-coated tablets, which are white after coating is removed.
Storage/expiration date15-30 c seal. Valid for 3 years.
Pharmacological effects of editing this paragraph
This product is a benzoisoxazole derivative and a new generation of antipsychotics. Risperidone, its active ingredient, is a selective monoamine antagonist with unique properties. It has high affinity for 5-HT2 receptor and dopamine D2 receptor. Risperidone can also bind to α 1- adrenoceptor, but has low affinity to H 1- histamine receptor and α2- adrenoceptor. Risperidone does not bind to cholinergic receptors. Risperidone is a potent D2 antagonist, which can improve the positive symptoms of schizophrenia, but compared with classical antipsychotics, it causes less motor function inhibition and tension syncope. The antagonistic balance between serotonin and dopamine in the central system can reduce the possibility of extrapyramidal side effects and extend its therapeutic effect to negative symptoms and emotional symptoms of schizophrenia.
Edit the pharmacokinetics of this paragraph
Risperidone can be completely absorbed after oral administration, and the blood concentration reaches the peak within 1-2 hours, and the absorption is not affected by food. This product can be rapidly distributed in the body, and the distribution volume is 1-2 L/Kg. In plasma, risperidone binds to albumin and α 1 acidic glycoprotein. The plasma protein binding rate of risperidone is 88%, and that of 9- hydroxyrisperidone is 77%. In vivo, risperidone is metabolized by CYP 2D6 to 9- hydroxyrisperidone, which has similar pharmacological effects to risperidone. Risperidone and 9- hydroxyrisperidone * * * together constitute the antipsychotic effective components of this product, and another metabolic pathway of risperidone in the body is N- dealkylation. The elimination half-life of risperidone is about 3 hours, and that of 9- hydroxyrisperidone and other active metabolites is 24 hours. Most patients reach the steady state of risperidone within 1 day and 9- hydroxyrisperidone after 4-5 days. In the therapeutic dose range, the plasma concentration of risperidone is directly proportional to the dose. After 1 week, 70% of the drugs were excreted in urine and 14% in feces. 35-45% of drugs excreted in urine are risperidone and 9- hydroxyrisperidone, and the rest are inactive metabolites. Single dose study showed that the plasma concentration of risperidone in elderly patients and patients with renal insufficiency was higher and the clearance rate was slower. The plasma concentration of risperidone in patients with hepatic insufficiency is normal. The pharmacokinetics of active metabolites such as risperidone and 9- hydroxyrisperidone in children are similar to those in adults.
Edit this paragraph of toxicology research.
Acute toxicology:
Oral LD50: 82.65438 0 mg/kg in male mice; (female) 63. 1 mg/Kg. Rat (male)113 mg/kg; (Female) 56.6 mg/kg. Dog (male and female) 18.3 mg/kg.
Long-term toxicology:
Long-term oral toxicology study of rats with 12 months showed that risperidone was well tolerated, and the only observed effect (changes in reproductive tract and breast) was prolactin-mediated change, which was related to the antagonistic characteristics of dopamine D2 receptor, an antipsychotic drug. 12 month dog tube feeding study showed that the non-toxic dose of risperidone was 0.3 1 mg/Kg.
Reproductive toxicity: The results of reproductive toxicology research in rats show that risperidone has no teratogenic effect and embryonic toxicity at any test dose.
Mutagenic effect: Studies show that risperidone has no potential mutagenic risk.
Carcinogenicity test: Carcinogenicity studies show that risperidone may enhance the tumorigenicity mediated by prolactin in rodents. Similar prolactin-mediated effects are also seen in other dopamine -D2 antagonists. Facts have proved that this discovery has almost no clinical significance.
Edit the usage and dosage of this paragraph.
Those who switch from other antipsychotics to this product: When starting to use, the original antipsychotics should be gradually stopped. If the patient originally used long-acting antipsychotics, this product can be used instead of the next course of treatment. The use of anti-Parkinson's drugs should be re-evaluated periodically.
Adults: 65438+ 0 times a day or twice a day. The initial dose is 1 mg, and the dose is gradually increased to 2-4 mg per day in about 1 week, and can be gradually increased to 4-6 mg per day in the second week. After that, this dose can be kept unchanged or further adjusted according to individual circumstances. Generally speaking, the best dosage is 2-6 mg per day. The daily dose is generally not more than 10 mg.
Patients with kidney disease and liver disease: It is recommended that the initial dose be 0.5 mg twice a day. According to individual needs, the dosage can be gradually increased to 1-2 mg twice a day.
Edit this adverse reaction
Extensive clinical experience (including long-term application) shows that this product is well tolerated. In many cases, it is difficult to distinguish adverse events from symptoms of underlying diseases. The adverse events reported when using this product are as follows:
Common adverse reactions include insomnia, anxiety, agitation and headache. Children and adolescents have more sedative reactions than adults, but they are mild and transient.
Rare or rare adverse reactions include drowsiness, fatigue, dizziness, decreased attention, constipation, dyspepsia, nausea/vomiting, abdominal pain, blurred vision, abnormal erection of penis, erectile difficulty, ejaculation weakness, sexual apathy, urinary incontinence, rhinitis, rash and other allergic reactions.
Compared with other traditional antipsychotics, this product causes fewer extrapyramidal symptoms. However, in some cases, the following extrapyramidal symptoms also appeared, such as tremor, rigidity, salivation, bradykinesia, akathisia and acute dystonia. It can be eliminated by reducing the dose or giving anti-Parkinson's drugs. Occasionally tardive dyskinesia.
Occasionally there are symptoms of (postural) hypotension, (reflex) tachycardia or hypertension.
Like traditional antipsychotic drugs, there are occasional reports of mental patients suffering from water poisoning, bradykinesia, malignant syndrome related to antipsychotic drugs, abnormal body temperature and convulsions caused by excessive drinking or inappropriate secretion of SIADH.
Like traditional antipsychotics, it may lead to a dose-related increase in plasma prolactin levels. The symptoms of elevated prolactin levels are galactorrhea, breasts of men and women, menstrual disorder and amenorrhea.
There are reports of weight gain, edema and elevated liver enzyme levels.
Occasionally, malignant syndrome, body temperature disorder and convulsion may occur.
There are reports of cerebrovascular adverse events (including cerebrovascular accidents and temporary ischemic attacks).
There is a case report of decreased neutrophil and/or platelet count.
Rare report of hyperglycemia and diabetes aggravation.
Notes for editing this paragraph
Because this product has α receptor blocking effect, hypotension may occur at the initial stage of medication. For patients with known cardiovascular diseases (such as heart failure, myocardial infarction, abnormal conduction, dehydration, hypovolemia or cerebrovascular diseases), this product should be used with caution, and the dosage should be gradually increased according to the recommended dosage (see usage and dosage). If hypotension occurs, the dosage should be reduced.
Like all other drugs with dopamine receptor antagonist properties, this product may also cause tardive dyskinesia, which is characterized by rhythmic involuntary movements mainly in the tongue and face. It is reported that the appearance of extrapyramidal symptoms is a risk factor for the development of tardive dyskinesia. Compared with other traditional antipsychotics, this product causes fewer extrapyramidal symptoms, so the risk of tardive dyskinesia is lower than that of similar drugs. If you have symptoms of tardive dyskinesia, consider stopping all antipsychotics.
It has been reported that taking traditional antipsychotic drugs will lead to malignant syndrome, which is characterized by high fever, muscle rigidity, trembling, disturbance of consciousness and increased creatine phosphokinase level. At this time, all antipsychotic drugs including this product should be stopped.
For the special dosage recommended for elderly patients, patients with liver disease, patients with kidney disease or patients with dementia, please refer to the section [Usage and Dosage].
Because antipsychotic drugs containing this product may increase the risk of malignant syndrome or Parkinson's symptoms related to antipsychotic drugs in patients with Lewy body dementia or Parkinson's disease, doctors should weigh the advantages and disadvantages when prescribing.
In patients with Alzheimer's disease (age range 73-97 years old; The average age is 85 years old), the incidence of cerebrovascular adverse events (including cerebrovascular accidents and transient ischemic attacks) in the drug group is higher than that in the placebo group.
Traditional antipsychotics will lower the threshold of epilepsy, so patients with epilepsy should use this product with caution.
Patients taking this product should avoid overeating to avoid gaining weight.
This product has an impact on activities that need vigilance. Therefore, patients are advised not to drive or operate machines during the treatment period until they know the sensitivity of patients to drugs.
Medication for pregnant and lactating women
It is not clear whether this product is safe for pregnant women. Animal experiments show that risperidone has no direct toxicity to reproduction, and only some indirect prolactin and central nervous system mediated effects are observed. This product has no teratogenic effect. For pregnant women, it is necessary to weigh the pros and cons to decide whether to take this product. Animal experiments show that risperidone and 9- hydroxyrisperidone are excreted through animal milk. At the same time, human experiments also prove that this product will be excreted through breast milk, so women who take this product should not breastfeed.
Children's medication
For schizophrenia, there is still insufficient clinical experience for children under 1.5 years old.
At present, there is not enough clinical experience of children under 5 years old for behavioral disorders such as conduct disorder.
Medication for elderly patients
It is suggested that the initial dose is 0.5 mg each time, twice a day, and the dose can be adjusted according to individual needs. The range of dose increase is 0.5 mg each time, twice a day, until 1 times 1-2 mg twice a day. Risperidone is well tolerated by the elderly.
drug interaction
The risk of combining this product with other drugs has not been systematically evaluated. In view of the effect of this product on the central nervous system, it should be used with caution when combined with other drugs that act on the central nervous system.
This product can antagonize the effects of levodopa and other dopamine agonists.
Carbamazepine and other liver enzyme inducers can reduce the plasma concentration of active ingredients in this product. Once the use of carbamazepine or other liver enzyme inducers is stopped, the dosage of this product should be re-determined and reduced if necessary.
Phenothiazine antipsychotics, tricyclic antidepressants and some β -blockers will increase the plasma concentration of this product, but will not increase the plasma concentration of its antipsychotic active components. Amitriptyline does not affect the pharmacokinetic parameters of risperidone or its antipsychotic active components. Cimetidine and ranitidine can increase the bioavailability of risperidone, but have little effect on its antipsychotic active components. Fluoxetine and paroxetine (CYP 2D6 inhibitor) can increase the plasma concentration of this product, but have little effect on the plasma concentration of its antipsychotic active components. When starting or stopping the combination with fluoxetine or paroxetine, the doctor should re-determine the dose of this product. Erythromycin (CYP 3A4 inhibitor) does not affect the pharmacokinetic parameters of risperidone or its antipsychotic active components. The pharmacokinetic parameters of cholinesterase inhibitors galanthamine and donepezil or their antipsychotic active components have no significant effect.
When taken together with other high-protein binding drugs, there is no clinical exchange of plasma proteins.
This product has no significant effect on the pharmacokinetic parameters of lithium, sodium valproate or digoxin.
Food does not affect the absorption of this product.
excessive
When there are symptoms of acute overdose, we should consider whether there are other factors caused by the combination of drugs. Generally speaking, the reported symptoms and signs of overdose are caused by the extension of its pharmacological action, including drowsiness and sedation, tachycardia and hypotension, and extrapyramidal symptoms. It has been reported that patients take more than 360 mg of this product, and the existing evidence shows that this product has a wide range of safety. A rare report of QT interval prolongation caused by drug overdose. If the rescue is excessive, keep the airway unobstructed, ensure sufficient oxygen and good ventilation, and give gastric lavage (intubate if the patient loses consciousness), activated carbon and laxatives, and immediately carry out cardiovascular monitoring, including continuous ECG monitoring, and find possible arrhythmia. There is no specific medicine for this product. Therefore, appropriate supportive therapy should be taken. Hypotension and circulatory failure can be corrected by intravenous infusion or sympathomimetic drugs Once severe extrapyramidal symptoms appear, anticholinergic drugs should be given, and strict medical monitoring and guardianship should continue until the patient recovers.
Frequently asked questions about editing this paragraph
What's the difference between 1.Vestibone and other antipsychotics? Vestibone is the first antipsychotic drug with a brand-new structure designed according to the requirements of ideal drugs, and it is a serotonin and dopamine antagonist with a unique balance mechanism. Its characteristic is that it is effective for both positive and negative symptoms of schizophrenia, especially for negative symptoms, which makes up for the defects of traditional drugs. The side effects are mild, and it does not affect the work and study of patients after taking the medicine, which is helpful for patients to return to society. From 65438 to 0995, risperidone has been the first antipsychotic drug in the world.
2. How does Visteon exert its curative effect? Psychotic symptoms are thought to be caused by the imbalance of brain chemicals (serotonin and dopamine). Visteon can adjust the balance of related chemicals in the brain, thus improving symptoms.
3. When did Visteon come into effect? The onset time of antipsychotic drugs varies with the condition, course of disease and individual differences. Usually antipsychotic drugs take effect in 2-4 weeks, and risperidone takes effect a little faster, but it may take several weeks to achieve full efficacy. Be patient and give Visteon enough time to play its role. After the drug takes effect, we should continue to go to the hospital for regular review and take Visteon on time according to the doctor's advice to prevent the recurrence of the disease. If you feel physical and emotional changes, please tell the doctor in time. When necessary, the doctor can improve the therapeutic effect by adjusting the dose. You shouldn't stop taking Visteon or increase or decrease the dose without consulting your doctor.
4. Will Visteon have any side effects? Any medicine will have some side effects. It has been eleven years since Visteon was listed, and it has been used by more than 10 million people around the world. In the past eleven years, it has been found that some people will have some side effects, such as insomnia, anxiety, dizziness, dry mouth and so on. These side effects usually gradually decrease or disappear after taking medicine for a period of time. Visteon rarely causes serious adverse physical reactions.
5. What dosage forms does 5.Vestone currently have? At present, there are two dosage forms of Visteon: 1) tablets: 1mg X 20 tablets/box, 2mg X 20 tablets/box; 2) oral liquid: 30ml/ bottle (1ml= 1mg). Visteon oral liquid was made in early 2004.
6. Can Weishitong oral liquid be taken with all drinks? Weishitong oral liquid can be taken with non-alcoholic beverages, such as drinking water, fruit juice, skim milk, coffee or food (such as porridge), but it should be avoided with tea, cola or alcoholic beverages.
7. What mental diseases can Visteon treat? Weishitong can be used to treat acute and chronic schizophrenia, as well as obvious positive and negative symptoms of other mental states. It can also relieve the emotional symptoms related to schizophrenia. Patients who are effective in acute phase can continue to play a clinical role in maintenance treatment.
8. Does vestibular bone have the function of preventing recurrence? Yes, Vestibone is the only new antipsychotic drug approved by FDA for long-term treatment and prevention of recurrence.
9. How long will it take for Visteon? Schizophrenia needs full treatment. The treatment of the whole course includes 8- 10 weeks of acute phase, 6 months of consolidation period and longer maintenance period. In the acute phase, the doctor will add the drug to the effective dose within 1-2 weeks, and continue the treatment at this dose for 6-8 weeks in order to control the symptoms to the greatest extent. After the symptoms are relieved, you should continue to treat with the original drug and dosage for at least 3-6 months, consolidate the curative effect, and then enter maintenance treatment. The time of maintenance treatment varies according to the condition: for the first-onset and slow-onset patients, the time of maintenance treatment needs at least 1-5 years; For patients with recurrent attacks, frequent fluctuations or incomplete remission, long-term medication should be taken.
10. Should we reduce the amount of Visteon after the symptoms are relieved? Because of the large dosage and serious side effects of traditional antipsychotics, the maintenance dose is lower than the therapeutic dose, which is generally about 1/2 of the therapeutic dose. New antipsychotics such as risperidone are safer. In order to better prevent recurrence, the dose should not be reduced in the maintenance treatment stage.
1 1. How to take Visteon for adults 1 time a day or twice a day? The initial dose was 1mg/ day, and it was increased to 2-4mg/ day within one week; It can be gradually increased to 4-6mg/ day in the second week. After that, this dose can be kept unchanged or further adjusted according to individual circumstances. Generally speaking, the optimal dosage is 2 mg -6 mg/day.
12. What should children pay attention to when taking risperidone? For children with schizophrenia, attention should be paid to starting from a low dose and gradually increasing the dose: the initial dose is 0.5mg~ 1mg/ day, which is taken orally twice. Then increase the dose by 0.5mg or 1mg every 3-4 days until the effective dose is reached, and the maximum dose shall not exceed 6mg/ day. For children/adolescents with oppositional defiant behavior disorder, a small dose is usually used. The recommended initial dose is 0.25mg(ml)/ day, 1 time/day; Teenagers 0.5mg(ml)/ day. The dosage should be slow, 0.25mg once, once a day 1 time, and the dosage will be increased the fastest the next day. The optimal dosage for children/adolescents is 1.5mg/d or 3mg/d respectively. Weishitong oral liquid is colorless and odorless, can be mixed with food and beverage, and the dosage adjustment is accurate and convenient, which is more suitable for children/teenagers.
13. Precautions for elderly patients taking Vestone? Elderly patients should pay attention to slowly increasing the dose of vestibular bone: the initial dose is generally 0.25-0.5 mg (ml) once, twice a day. The range of dose increase is 0.5mg per day, taken twice. The fastest dose increase was the next day. The ideal dose for most patients is 1-2 mg/day. Weston oral liquid is flexible and convenient to add medicine and easy to swallow, which is more suitable for elderly patients.
14. What should I pay attention to if I switch from other drugs to Visteon? When switching from other antipsychotics to risperidone, the original antipsychotics should be gradually stopped. Generally, all the original antipsychotics are reduced within 1 ~ 2 weeks, and risperidone is used at the same time, which is generally increased to 2mg within 1 week, and the dose range is 1-2mg/ week, and gradually reaches the therapeutic dose of 2-6mg/ day. At the beginning of dressing change, anticholinergic drugs and sedatives can be used together for a short time. Outpatients should reduce the dose and increase the dose of fluoxetine. When the long-term injection is changed to fluoxetine, it should be changed to fluoxetine in the scheduled next injection cycle. Patients who use clozapine should reduce the dose more slowly. Replace 1-2 diapers every day. The doctor will make a suitable dressing change plan for you according to your situation. Please let me know in time if you have any discomfort.
Chinese name of medicine: Weishitong
English name of drug: risperidone.
Drug category: antipsychotic drugs
instruction for (drug) use
Alias risperidone
Indications Acute and chronic schizophrenia, positive and negative symptoms of various mental states, can also be used to relieve emotional symptoms related to schizophrenia.
Dosage and Usage The initial dosage is 1-2mg/ day, and it will be increased to 4-6mg/ day within 3-7 days, with the dosage of 1-2mg/ day each time. The optimal dosage is 4-6mg/ day, which can be maintained or further adjusted. The first attack, the elderly and patients with liver and kidney diseases halved.
/kloc-children under 0/5, pregnant women and lactating women are prohibited.
Adverse reactions: insomnia, agitation, fatigue and constipation. Occasionally postural hypotension.
Precautions: Use with caution in patients with cardiovascular diseases.
Drug interaction can antagonize the action of levodopa and dopamine agonist, and amide azine and liver enzyme inducer can reduce the plasma concentration of active components of the drug. Phenothiazine, tricyclic antidepressants and β -blockers can increase the plasma concentration of the drug.
Specification tablets 1 mgx 20 tablets. 2mgx 20 tablets.