Bupropion Hydrochloride Sustained Release Tablets

Pharmacological action: Bupropion has a weak inhibitory effect on the uptake of norepinephrine, 5-HT and dopamine, but has no such effect on monoamine oxidase. Toxicological studies: Genetic toxicity: Two of the five strains showed positive results in the Ames test of bupropion (the mutation rate was 2-3 times that of the control group). In three in vivo rat bone marrow cytogenetic tests, one test showed an increased rate of chromosome aberrations. Reproductive toxicity: Rats were given bupropion orally up to 300 mg/kg, and no damage to fertility was observed. Pregnant rats and rabbits were given bupropion at doses of up to 450 mg/kg and 150 mg/kg, respectively (calculated by body surface area, equivalent to 7-11 times and 7 times the maximum recommended human dose, respectively), and no drug-related fetal toxicity was observed. Carcinogenic effect: In long-term administration studies, rats and mice were given bupropion by gavage at doses of up to 300 mg/kg and 150 mg/kg (7 times and 2 times the maximum recommended human dose, respectively, calculated by body surface area) for 104 and 96 weeks. The dose of 100 mg/kg to 300 mg/kg can cause rat liver nodular hyperplasia. It is not clear whether this hyperplasia is a precursor of neoplasm, but similar lesions were not observed in mice. No increase in the incidence of malignant tumors in the liver and other organs was observed in both studies.

(±)-1-(3-Chlorophenyl)-2-[(1,1-dimethylethyl)amino]-1-propanone hydrochloride

This product is a film-coated tablet, which appears white or off-white after removing the film coating.

Used to treat depression.

1. Oral administration. Take 150 mg (1 tablet) once a day for 3 consecutive days from the beginning of medication. Increase to twice a day after the 4th day, 150 mg (1 tablet) each time. The recommended dose of this product is 300 mg (2 tablets) a day, taken twice, with an interval of more than 8 hours between the two doses. Like other antidepressants, the best antidepressant effect of this product may not be shown until the 4th week or even longer. If there is no significant improvement after several weeks of clinical use of 300 mg per day, consider increasing the dose to 400 mg per day. Usually, acute depression requires continuous drug treatment for several months or even longer. Due to limited evidence, it is not clear whether the maintenance treatment dose of this product is consistent with the recommended effective dose. The necessity of taking the drug should be re-evaluated regularly when taking it for a long time. 2. For the use of patients with liver and kidney damage, please refer to the contents of [Precautions].

According to the results of foreign and domestic clinical studies, the adverse reactions of bupropion hydrochloride sustained-release tablets include: loss of appetite or anorexia, dry mouth, facial flushing, sweating, tinnitus, tremor, abdominal pain, agitation, anxiety, dizziness, insomnia, myalgia, palpitations, pharyngitis or frequent urination, nausea and vomiting, constipation, blurred vision, and headache. Common adverse reactions that lead to discontinuation of the drug include: facial flushing, nausea, agitation, and migraine. Less common adverse reactions include: diarrhea, bitter taste in the mouth, stomach discomfort, stomach pain, increased salivation, skin symptoms, and weight gain.

The following patients are prohibited from using this product: 1. Patients with epileptic seizures; 2. Patients using other drugs containing bupropion; 3. Patients currently or previously diagnosed with bulimia or anorexia, because it may induce epileptic seizures; 4. Patients cannot be used in combination with monoamine oxidase (MAO) inhibitors. When stopping monoamine oxidase inhibitors and taking this product, the interval should be at least 14 days; 5. Patients who are allergic to bupropion or the ingredients of this product; 6. Patients who suddenly stop drinking or stopping sedatives.

Precautions for children: The clinical study of this product does not include people under 18 years old. Therefore, the effectiveness and safety of this drug for children has not been determined. Precautions for pregnancy and lactation: There is currently no sufficient controlled research data on the use of this product by pregnant women to prove the safety of this product. Therefore, pregnant women should not use it. If it must be used, the pros and cons should be fully weighed. Bupropion and its metabolites can be secreted through breast milk. Considering the potential impact of this product on infants, it should not be used by breastfeeding women. If it must be used, the necessity of this product for the mother should be fully evaluated to determine whether to stop breastfeeding and use the drug. Precautions for the elderly: 1. In the clinical study of bupropion sustained-release tablets (anti-depression and smoking cessation studies), approximately 6,000 patients were over 65 years old, including 47 over 75 years old. In addition, several hundred elderly patients over 65 years old participated in the study of bupropion ordinary tablets (anti-depression). There is no significant difference in the safety and effectiveness of this product between elderly patients and young patients. However, some elderly patients may be more sensitive to this product. 2. Pharmacokinetic studies of single-dose administration have shown that the distribution of bupropion and its metabolites in the elderly and young is similar. Other pharmacokinetic studies have shown that the risk of bupropion and its metabolites accumulating in the body increases after taking the drug in elderly patients. 3. Bupropion is metabolized to active metabolites in the liver, which are ultimately eliminated through renal metabolism. The toxicity of metabolites in patients with impaired renal function will be higher. Therefore, elderly patients should carefully choose the appropriate dose and monitor renal function at the same time.

1. Drugs metabolized by cytochrome P450ⅡB6: In vitro tests have shown that bupropion is mainly metabolized by cytochrome P450ⅡB6 isoenzymes, so there is a potential interaction with other drugs that affect cytochrome P450ⅡB6 isoenzymes. 2. MAO inhibitors: Animal studies have shown that monoamine oxidase inhibitor (MAOI) phenelzine can increase the acute toxicity of bupropion. 3. Levodopa: Clinical data show that the incidence of adverse reactions may increase after the simultaneous use of bupropion and levodopa. Patients taking levodopa should be cautious when taking this product at the same time, starting with the minimum dose and then gradually increasing the dose. 4. Drugs that lower the threshold of epilepsy: Extreme caution should be used when this product is used in combination with drugs that lower the threshold of epilepsy (such as antipsychotics, antidepressants, theophylline, systemic steroids, etc.) or therapies (such as sudden discontinuation of benzodiazepines). 5. Nicotine transdermal patch: Clinical studies have shown that the combined use of bupropion sustained-release tablets and nicotine transdermal patches has a higher incidence of emergency therapeutic hypertension. Therefore, blood pressure should be closely monitored when the two are used in combination.

Keep in a light-proof and airtight container.

0.15g

Tentatively 24 months.

Jiangsu Kanion Pharmaceutical Co., Ltd.

• Founded in:

  1996-05-08

• Address:

  Lianyungang Economic and Technological Development Zone Jiangning Industrial City

• Tax NO.:

  91320700138997640W

• Registered Funds:

  581.797452 million yuan

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