Date of approval: 05/01/2007
Modification date: October 01, 2010
Modification date: December 01, 2015
Modification date: xxxxx xx xx
Sulpiride tablets instructions
Please read the instructions carefully and use under the guidance of a physician
Pheochromocytoma, pituitary prolactin adenoma, hypertensive patients, patients with severe cardiovascular disease and severe liver disease, and those who are allergic to this product are prohibited.
Drug Name
Generic name: Sulpiride Tablets
English name: Sulpiride Tablets
Hanyu Pinyin: Shubili Piɑn
Ingredients
The main ingredient of this product is Shubili.
Chemical name: N-[(1-ethyl-2-pyrrolidinyl)methyl]-2-methoxy-5-(aminosulfonyl)benzamide.
Chemical structure formula.
Molecular formula: C15H23N3O4S
Molecular weight: 341.42
Properties
This product is a film-coated tablet, which appears white or off-white after removing the coating.
Indications
Used for schizophrenia. It has some effect on depression symptoms. Other uses include anti-vomiting.
Specification
100mg
Dosage]
Take orally. For the treatment of schizophrenia, the starting dose is 100mg (1 tablet) once, 2~3 times a day, gradually increasing to a therapeutic dose of 600~1200mg (6~12 tablets) a day, and the maintenance dose is 200~600mg (2~6 tablets) a day. To stop vomiting, 100~200mg (1~2 tablets) once, 2~3 times a day. children over 6 years old should start with small doses and increase the dose slowly according to the adult dose conversion.
Adverse reactions
Serious Adverse Reactions
Neuroblocker malignant syndrome (<0.1%)
It may cause neural blocker malignant syndrome. When patients develop symptoms such as motor inability, muteness, muscle tonicity, dysphagia, tachycardia, blood pressure fluctuation, sweating, etc., followed by fever, drug administration should be stopped immediately and appropriate measures should be taken for systemic supportive treatment, such as physical cooling and hydration. The onset of this condition is most often accompanied by elevated white blood cells and elevated serum CPK. In addition, decreased renal function accompanied by elevated myoglobin may sometimes be observed.
In addition, cases of persistent high fever, impaired consciousness, respiratory distress, circulatory failure, dehydration, and then progression to acute renal insufficiency and eventual death have been reported clinically.
Convulsions (<0.1%)
Convulsive symptoms may occur and the drug should be discontinued when they occur.
Prolonged QT interval, ventricular tachycardia (<0.1%)
Because prolonged QT interval and ventricular tachycardia (including tip-twist type) may occur, patients should be monitored closely while taking the drug, and when they develop abnormalities, the drug should be stopped immediately and appropriate therapeutic measures should be taken.
Hepatic insufficiency, jaundice (<0.1%)
Because hepatic impairment accompanied by elevated AST (GOT), ALT (GPT), γ-GTP and ALP and jaundice may occur, patients should be closely monitored when administering the drug, and when they develop abnormalities, the drug should be discontinued immediately and appropriate therapeutic measures should be taken.
Late-onset dyskinesia (<0.1%)
Because long-term administration of this product may cause involuntary movements in the perioral region, etc., which may persist even if the administration is stopped, patients should be monitored closely when administering the drug, and when they develop abnormalities, the drug should be discontinued immediately and appropriate therapeutic measures should be taken.
Granulocyte deficiency, leukopenia (<0.1%)
Because of the possibility of granulocyte deficiency and leukopenia, patients should be monitored closely when administering the drug, and when they develop abnormalities, the drug should be discontinued immediately and appropriate therapeutic measures should be taken.
Pulmonary embolism, deep vein embolism formation (<0.1%)
Antipsychotic drugs have been reported to cause thromboembolic diseases such as pulmonary embolism and venous thrombosis, so patients should be closely monitored when administering the drugs, and when patients are observed to have symptoms such as shortness of breath, chest pain, pain in the extremities and edema, the administration of the drugs should be stopped and appropriate therapeutic measures should be taken.
Other adverse reactions
If the following adverse reactions occur, appropriate measures such as reducing the dosage or stopping the drug should be taken when necessary.
0.1~5%<0.1% Cardiovascular system*1 Decreased blood pressure abnormal electrocardiogram, increased blood pressure, chest tightness, tachycardia Extrapyramidal reactions*2 Parkinson’s syndrome (tremor, myotonia, salivation, etc.), movement disorders (tongue movement disorder, speech disorder, neck muscle spasm, eye rotation, gaze spasm, swallowing difficulty, etc.), inability to sit still Endocrine system*3 Breast overflow, feminization of male breast , menstrual abnormalities, ejaculatory disorders breast swelling, erectile dysfunction psychoneurological system sleep disorders, restlessness, agitation, sleepiness, headache, heavy head, dizziness, hallucinations, excitement, mania, manic state, numbness, ataxia amnesia, dullness, wandering, hyperactivity, weakened inhibition, apathy digestive system nausea, vomiting, dry mouth, constipation, loss of appetite, abdominal discomfort diarrhea, heartburn, abdominal pain, over-appetite Liver Elevated AST (GOT), ALT (GPT), ALP Skin*4 Itchy rash Eyes Visual impairment, cold, heavy feeling in the eyes, flickering eyes Other*5 Weight gain, edema, weakness, lethargy, difficulty urinating, loss of libido Urinary frequency, lumbago, stiff shoulder muscles, dryness, fever, sweating, nasal congestion *1: Because ECG changes may occur with sharply increased doses, they should be be administered with caution.
*2: If such symptoms occur, the dose should be reduced and concomitant anti-Parkinsonian medication should be administered.
*3: should be closely observed and administered with caution because such symptoms may occur
*4: medication should be discontinued if such symptoms occur.
*5: Medication should be discontinued in case of edema.
[Contraindication].
This product is contraindicated in the following cases.
Persons with a history of hypersensitivity to any of the components of this product.
Patients with pituitary prolactin adenoma (prolactinoma).
Patients with suspected pheochromocytoma (which may trigger hypertensive emergencies).
Patients with hypertension, severe cardiovascular disease and severe liver disease.
[Caution].
It should be used with caution in the following patients.
(1) Patients with cardiovascular disease, hypotension, and suspected such disease (risk of exacerbating symptoms)
(2) Patients with prolonged QT interval (may aggravate QT interval prolongation)
(3) Patients prone to QT interval prolongation (may precipitate QT interval prolongation)
(1) Patients with significant bradycardia
(2) Patients with hypokalemia, etc.
(4) Patients with renal insufficiency (may cause drug accumulation)
(5) Patients with Parkinson’s disease (may aggravate extrapyramidal symptoms)
(6) Patients with physical failure accompanied by dehydration and malnutrition (may induce nerve blocker malignant syndrome)
(7) The elderly (see [geriatric use] for details)
(8) Children (see [Children’s medication] for details)
(9) All antipsychotics should be discontinued for the development of delayed-onset movement disorder.
(10) The appearance of allergic rash and malignant symptom groups should be immediately discontinued and treated accordingly.
(11) Use with caution for basal ganglion lesions, Parkinson’s syndrome, and severe central nervous depression.
(12) The dosage should be reduced in patients with hepatic and renal insufficiency.
(13) Use with caution in patients with epilepsy.
Important basic precautions
(1) Because this product may cause side effects such as abnormal endocrine function (increased prolactin levels) and extrapyramidal symptoms, the effectiveness and safety of the drug should be fully weighed before it is actually given.
(2) Since drowsiness and dizziness may result from taking this product, patients should be careful not to engage in dangerous operations related to the operation of machinery, such as driving a car, while taking this product.
(3) Since this product has anti-emetic effect, it may mask the symptoms of vomiting caused by other drug poisoning, intestinal obstruction, brain tumor, etc.
(4) Since adverse reactions of thromboembolic diseases such as pulmonary embolism and venous embolism have been reported with antipsychotic drugs, extra caution should be exercised in patients with risk factors such as physical inappropriateness, prolonged bed rest, obesity, and dehydration.
Other precautions
In clinical trials of elderly patients with dementia-related psychotic disorders (unapproved indications) conducted in 17 foreign clinical trial centers, mortality rates were reported to be 1.6 to 1.7 times higher in the atypical antipsychotic treatment group than in the placebo group. In addition, epidemiological findings from foreign countries have shown that typical antipsychotics are associated with increased drug-related mortality as well as atypical antipsychotics.
[For pregnant and lactating women].
(1) The safety of this product during pregnancy has not been established. In women who are pregnant or likely to become pregnant, this product should be used only if the benefits of the drug outweigh the risks. The use of antipsychotics during pregnancy has been reported to cause withdrawal symptoms and extrapyramidal reactions such as neonatal lactation disorder, drowsiness, dyspnea, tremor, hypotonia and irritability.
(2) Women who are breastfeeding should not take this drug, and if they must use it, they should avoid breastfeeding. (This product has been reported to be secreted through breast milk). (See [Pharmacokinetics]).
[Pediatric Use].
Use with caution.
For Elderly]
This product is mainly excreted by the kidneys, but the elderly usually have varying degrees of renal hypofunction, so there may be a risk of persistently high blood levels, so attention should be paid to the occurrence of adverse reactions (extrapyramidal reactions, etc.) during administration, and the dose and dosing interval should be observed when administering the drug.
Elderly patients should start with small doses and increase the dose slowly.
Drug Interactions]
Precautions for combined drug use
Drug name Clinical symptoms – Treatment measures Mechanism – Risk factors Drugs known to cause prolongation of QT interval
Promethazine, pimozide, etc. may have serious side effects such as QT interval prolongation and ventricular arrhythmias, etc. Since sulpiride and these drugs have the effect of prolonging the QT interval, the QT interval prolongation may be enhanced when combined with digitalis drugs
Digoxin and digitalis toxin may mask the symptoms of nausea, vomiting and loss of appetite caused by the saturation concentration of digitalis, which originate from the antiemetic effect of benzamide
Gastroflucan, Tebrile, etc.
Phenothiazines
Chlorpromazine, etc.
Butyrylbenzenes
Haloperidol, etc. are more likely to cause endocrine dysfunction and extrapyramidal reactions because these drugs have antidopamine effects, and their combined use enhances the antidopamine effect Central nervous system depressants
Barbiturate derivatives.
Narcotic drugs have a synergistic effect on CNS depression both of which have CNS depressant effects dopamine agonists
L-dopa, etc. may have antagonistic effects on each other because of the antidopamine effect of this product Alcohol
(alcohol consumption) may enhance its inhibitory effect on the central nervous system Both have inhibitory effects on the central nervous system
Drug overdose]
Symptoms of poisoning.
CNS symptoms: Severe impairment of consciousness, ranging from drowsiness and inattention to lethargy and finally coma. Pupil narrowing and dull reaction to light can be found during examination. It is also accompanied by central hypothermia.
Cardiovascular system symptoms: postural hypotension, increased heart rate, fine pulse count, and occasional arrhythmia, leading to hypovolemic shock in severe cases.
Hematologic symptoms: neutropenia, allergic purpura.
Treatment: gastric lavage, catheterization, fluid infusion. And give symptomatic treatment and maintenance treatment (infusion, etc.) according to the condition.
Pharmacology and Toxicology
1.Anti-psychotic effect
This product is a benzamide antipsychotic, characterized by selective blockade of dopamine (DA2) receptors in the limbic system of the midbrain, with less effect on other transmitter receptors, lighter anticholinergic effect, no significant sedative and anti-excitatory agitation effect.
2.Antidepressant effect
Although this product has not been shown to have a conventional tricyclic antidepressants to inhibit the reuptake of biogenic amines (rats), but considering that it has an antileptic effect (monkeys), so it is believed that this product has antidepressant effects.
3. It also has strong antiemetic and gastric juice inhibition effects.
Pharmacokinetics]
Absorption and excretion
The peak concentration (0.31μg/ml) was reached 2 hours after a single oral dose of 100mg in healthy adults, and the blood concentration was 0.13μg/ml after 8 hours. the urinary excretion rate was 23.9% 24 hours after administration.
Lactation
The concentration of sulpiride in breast milk was 0.97μg/ml 2 hours after the administration of 50mg orally twice daily in lactating women.
Storage
Store under shade and seal.
Package
Packed in plastic bottle, 100 tablets/bottle.
Expiration date
24 months
【Execution standard
Approval number】
State Drug Certificate H32023126
Drug marketing license holder
Name
Name: Jiangsu Tianshili Diyi Pharmaceutical Co.
Registered Address: No. 168, West Chaoyang Road, Qingpu Industrial Park, Huai’an City
Postal Code: 223002
Contact: 0517-83803757
Fax
Fax: 0517-83803898
Web
Address: www.taslydiyi.com
Manufacturer
Company name: Jiangsu Tianshi Li Diyi Pharmaceutical Co.
Address: No. 168, Chaoyang West Road, Qingpu Industrial Park, Huai’an City, Jiangsu Province
Postal Code: 223002
Telephone number: 0517-83803757
Fax number: 0517-83803898
Tianshili Group free service phone number: 8008189818 (landline); 4006189818
Web
Address: www.taslydiyi.com