Bupropion Hydrochloride Tablets

1. Pharmacological effects Bupropion has a weak inhibitory effect on norepinephrine, 5-HT, and dopamine reuptake, but has no such effect on monoamine oxidase. The antidepressant mechanism of this product is still unclear, and may be related to norepinephrine and/or dopaminergic effects. 2. Toxicological effects Genotoxicity: In the Ames test of bupropion, 2 of the 5 strains showed positive results (the mutation rate was 2 to 3 times that of the control group). In 3 in vivo rat bone marrow cytogenetic tests, one test showed an increased chromosome aberration rate. 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 to 11 times and 7 times the maximum recommended human dose, respectively), and no drug-related fetal toxicity was observed. 3. Carcinogenic effect: In long-term administration studies, rats and mice were given bupropion by gavage at doses of up to 300 and 150 mg/kg, respectively (calculated by body surface area, equivalent to 7 times and 2 times the maximum recommended human dose, respectively), for 104 and 96 weeks, respectively. The dose of 100-300 mg/kg can cause rat liver nodular hyperplasia, and it is unclear whether this hyperplasia is a precursor of neoplasm. However, no similar lesions were observed in mice. No increase in the incidence of malignant tumors in the liver and other organs was observed in both studies.

The main ingredient of this product is bupropion.

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

Used to treat depression.

Oral. Start with a low dose, with a starting dose of 75 mg (1 tablet) twice a day (morning and evening); after taking it for at least 3 days, the dose can be gradually increased to 75 mg (1 tablet) 3 times a day (morning, noon, and evening) based on clinical efficacy and tolerance; later, it can be gradually increased to the usual dose of 300 mg per day, 3 times a day (2 tablets in the morning, 1 tablet each in the afternoon and evening). During the dosage increase process, the dose increase within 3 days should not exceed 100 mg per day. As an antidepressant, this product usually takes 4 weeks to show obvious effects. If there is still no obvious effect after several weeks of continuous use, you can consider gradually increasing it to a maximum daily dose of 450 mg, but the maximum dose each time should not exceed 150 mg (2 tablets), and the interval between two doses should not be less than 6 hours.

1. According to foreign literature reports, common adverse events of bupropion are agitation, dry mouth, insomnia, headache/migraine, nausea/vomiting, constipation and tremor. About 10% of the 2,400 subjects (including patients and healthy volunteers) discontinued medication due to adverse events. The most common causes are neuropsychiatric disorders (3.0%), mainly agitation and mental disorders; gastrointestinal disorders (2.1%), mainly nausea and vomiting; nervous system disorders (1.7%), mainly epilepsy, headache and sleep disorders; skin discomfort (1.4%). It is worth noting that some adverse events are caused by dosages above the recommended daily dose. 2. In other open, uncontrolled clinical studies, the following adverse events were also observed, among which common adverse events refer to those with an incidence of at least 1%, occasional adverse events refer to those with an incidence between 0.1% and 1%, and rare adverse events refer to those with an incidence below 0.1%. 1) Common cardiovascular system: edema; Occasionally: chest pain, ECG abnormalities (premature beats, nonspecific ST segment T wave changes), shortness of breath, dyspnea; Rarely: flushing, pallor, phlebitis, myocardial damage. 2) Common skin system: nonspecific rash; Occasionally: hair loss and dry skin; Rarely: hair color changes, hirsutism, acne. 3) Occasionally digestive system: dysphagia, liver damage/jaundice, rectal disease, colitis, gastrointestinal bleeding, intestinal perforation, and gastric ulcer. 4) Common genitourinary system: increased nocturia; Occasionally: vaginal irritation, testicular enlargement, urinary tract infection, erectile pain, delayed ejaculation; Rarely: dysuria, enuresis, urinary incontinence, amenorrhea, ovarian dysfunction, pelvic infection, cystitis, dyspareunia, and ejaculation pain. 5) Rare blood/tumor: lymphatic system diseases, anemia, and pancytopenia. 6) Rare musculoskeletal system: musculoskeletal chest pain. 7) Common in the nervous system: ataxia, epilepsy, muscle spasm, movement disorder, dystonia; Occasionally: mydriasis, vertigo and dysphonia; Rarely: abnormal EEG, abnormal neurological examination, attention impairment, sciatica and aphasia. 8) Common in the neuropsychiatric system: mania/hypomania, decreased libido, hallucinations, sexual dysfunction, depression; Occasionally: memory impairment, split personality, psychosis, dysphonia, emotional instability, paranoia, abnormal thinking, frigidity; Rarely: suicidal tendencies. 9) Common in the oral system: stomatitis; Occasionally: toothache, bruxism, gingival swelling, mucosal edema; Rarely: glossitis. 10) Occasionally in the respiratory system: bronchitis and tachypnea/dyspnea; Rarely: epistaxis, respiratory rhythm disorders, pulmonary embolism. 11) Occasionally in the special senses: visual disorders; Rarely: diplopia. 12) Common non-specific reactions: cold-like symptoms; Occasionally: non-specific pain; Rarely: abnormal body odor, pain related to surgery, infection. 3. Volunteer reports related to bupropion concluded that the following adverse events may not be related to the drug: 1) Generalized joint pain, myalgia, rash with fever, and other symptoms of delayed allergic reactions, which are similar to serum sickness. 2) Cardiovascular hypertension (some cases are more severe), postural hypotension, and third-degree conduction block. 3) Endocrine antidiuretic hormone secretion syndrome, hypoglycemia, hyperglycemia, male breast development, diabetes, and unstable hormone levels. 4) Gastrointestinal esophagitis, hepatitis, and liver damage. 5) Blood lymphatic system ecchymosis, leukocytosis, leukopenia, and thrombocytopenia. 6) Musculoskeletal joint pain, myalgia, muscle stiffness/fever/rhabdomyolysis, and muscle weakness. 7) Neurological coma, delirium, abnormal dreams, and exposure bradykinesia. 8) Stevens-Johnson symptoms on the skin and appendages, angioedema, exfoliative dermatitis and urticaria. 9) Special senses tinnitus.

1. Patients with a history of epilepsy are contraindicated to use this product. 2. Patients who are taking other drugs containing bupropion are contraindicated to use this product. 3. Patients with bulimia or anorexia are contraindicated to use this product. 4. Patients who are allergic to bupropion or any of the ingredients in this product are contraindicated to use this product. 5. Patients who suddenly quit drinking or stop taking sedatives are contraindicated to use this product. 6. It cannot be used in combination with monoamine oxidase (MAO) inhibitors. The interval between taking monoamine oxidase inhibitors and this product should be at least 14 days.

Precautions for children: The clinical study of this product does not include people under 18 years old. Therefore, the safety of the 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, so 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 effects 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 this drug. Precautions for the elderly: There is no significant difference in the safety and effectiveness of this product between elderly patients and young patients, but some elderly patients may be more sensitive to this product and the risk of drug accumulation in the body is increased. Since this product and its metabolites are mainly metabolized by the kidneys, elderly patients should carefully choose the appropriate dose and test renal function at the same time.

1. Drugs metabolized by cytochrome P450IIB6: In vitro tests have shown that bupropion is mainly metabolized by the P450IIB6 isoenzyme, so there is a potential interaction with other drugs that affect the P450IIB6 isoenzyme. 2. Bupropion can be extensively metabolized, so the combination of other drugs will affect its clinical efficacy. For example, some drugs can induce the metabolism of bupropion (carbamazepine, phenobarbital, phenytoin), and some drugs can inhibit the metabolism of bupropion (such as cimetidine). A clinical trial involving 24 healthy volunteers has shown that the concomitant use of cimetidine can affect the pharmacokinetics of bupropion and its active metabolites. After oral administration of 300 mg of this product, whether or not to use 800 mg of cimetidine in combination has no effect on the pharmacokinetics of the original and hydrogenated metabolites, but the AUC and Cmax of threonine hydrogenated bupropion and erythrose hydrogenated bupropion increased by 16% and 32%, respectively. 3. Drugs metabolized by cytochrome P450IID6: Many drugs (including antidepressants, b-blockers, antiarrhythmic drugs and antipsychotic drugs) can be metabolized by CYPIID6. In vitro tests have shown that bupropion and hydroxybupropion are inhibitors of this enzyme. A study involved 15 male subjects, all of whom were extensive metabolizers of the CYPIID6 enzyme. The results showed that taking bupropion 150 mg twice a day and then taking desipramine 50 mg once would increase the Cmax, AUC and half-life of desipramine by approximately 2, 5 and 2.5 times, respectively. Therefore, caution should be exercised when bupropion is used in combination with other drugs metabolized by the CYPIID6 enzyme. These drugs include certain antidepressants (such as nortriptyline, imipramine, desipramine, paroxetine, fluoxetine, sertraline), antipsychotics (such as haloperidol, risperidone, thioridazine), b-blockers (such as metoprolol), IC class antiarrhythmic drugs (such as propafenone, flufenamide), and the minimum dose should be used at the beginning of combined treatment. When patients who are taking bupropion are taking drugs that metabolize CYPIID6 enzymes, they should consider reducing the dose of the original drug, especially those with a narrow therapeutic index. 4. MAO inhibitors: Animal studies have shown that monoamine oxidase inhibitors (MAOIs) phenethylhydrazine can increase the acute toxicity of bupropion. 5. Levodopa: Clinical data show that the incidence of side effects 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. 6. Drugs that lower the seizure threshold: Extreme caution should be exercised when this product is used in combination with drugs that lower the seizure threshold (such as antipsychotics, antidepressants, theophylline, systemic steroids, etc.) or therapies (such as sudden discontinuation of benzodiazepines).

Store at room temperature (10-30°C), sealed, and dry.

75 mg

Tentative 12 months

Venturpharm Pharmaceutical(Hainan)Limited.

• Founded in:

  2004-03-09

• Address:

  No. 279 Nanhai Avenue, Haikou City

• Tax NO.:

  914601007543894388

• Registered Funds:

  194.8706 million yuan

• Email:

  Log in to view