Description: The instructions for sibutramine hydrochloride capsules were issued by the State Pharmaceutical Products Supervision and Administration on February 5, 2002 in the Notice on Publishing the Catalogue of Instructions for the Second Batch of Chemicals. The instructions published by the State Administration of Pharmaceutical Products are reference samples for revising the specifications. In case of doubt, the enterprise may propose amendments. Indications should be consistent with the original approval; Adverse reactions, drug interactions and other contents, the instructions provided by the enterprise can not be less than those listed in the sample draft. For empty or incomplete items in the sample manual, enterprises should be required to fill in according to the actual situation, such as product name and specifications.
Drug name
Generic name: sibutramine hydrochloride capsules
Former name:
Commodity name:
Chinese name: sibutramine hydrochloride capsules
Chinese pinyin: Xibuquminɡ Jiɑonɑnɡ
The main component of this product is sibutramine hydrochloride Its chemical name is: (+) n {1 [1 (4 chlorophenyl) cyclobutyl ]3 methyl butyl }N, n dimethylamine hydrochloride monohydrate.
Structural formula:
Molecular formula: C 12H26ClN HCl H2O H2O.
Molecular weight: 334.33
Character; Role; letter
This product is a capsule, and its contents are white or white-like powder.
Pharmacology and toxicology
This product is the main therapeutic drug for obesity. Its main mechanism is to inhibit the reuptake of norepinephrine, serotonin and dopamine and enhance satiety, but it has no obvious effect on the release of norepinephrine, serotonin and dopamine. The study also showed that this product and its amine active metabolites had no obvious anticholinergic, antihistamine and monoamine oxidase inhibitory effects.
pharmacokinetics
Oral absorption is rapid, with an average absorption of at least 77% in a single dose, the peak time of plasma concentration is 1.2 hours, the oral clearance rate is 1750L/h, and the half-life is 1 1 hour. After the first-pass effect in the liver, it is metabolized by cytochrome P450(3A4) isoenzymes in the liver into monomethylidene and bimethylidene metabolites M 1 and M2, which are further hydroxylated and combined to be metabolized into pharmacologically inactive metabolites M5 and M6. The concentrations of drug prototype and its metabolites in plasma were 3%, M 16%, M2 12%, M552% and M627%, respectively. The plasma concentrations of M 1 and M2 reached the peak within 3 ~ 4 hours after taking the drug, and reached a stable state within 4 days after taking the drug, and the concentration was twice that of the single drug. The half-lives of M 1 and M2 are 14 and 16 hours, respectively, and the half-lives remain unchanged after repeated administration. At the therapeutic dose, the binding rates of the original drug M 1 and M2 in human plasma were 97%, 94% and 94% of the plasma concentration, respectively. Oral drugs can be quickly and widely distributed in tissues after being absorbed by intestine, and the concentration is the highest in liver and kidney. About 85% (68% ~ 95%) is excreted in urine and feces after a single dose. M 1 and M2 are mainly excreted by the liver; M5 and M6 are mainly excreted by kidneys, and there is no original component in urine.
indicate
Can be used for treating obesity which cannot be reduced and controlled by diet control and exercise. It is recommended for obese patients with body mass index (BMI) ≥30kg/m2 or ≥28kg/m2 and other risk factors such as diabetes and dyslipidemia.
Note: Body Mass Index (kg/m2) = Weight (kg)/Height Square (m2)
dosage
The recommended dosage is 1 time, 10mg once a day, taken alone in the morning or at the same time with breakfast. If the weight loss is not obvious, the dose can be increased to 15mg/ day after 4 weeks, and it can be reduced to 5mg/ day if the patient cannot tolerate the dose of 10mg/ day. Doses exceeding15mg/day are not recommended.
counteraction
1. Adverse reactions include: dry mouth, anorexia, insomnia, constipation, etc.
2. Other adverse reactions with incidence ≥ 1% include fever, increased heart rate, elevated blood pressure, dyspnea, diarrhea and gastroenteritis.
3. This product can cause abnormal liver function, which often disappears with further treatment, and has a clear dose-response relationship.
4. In addition, limb spasms, increased tension, abnormal thinking, seizures, interstitial nephritis, menstrual disorder and peripheral edema can also be seen; Arthritis, itchy skin, abnormal sensation, amblyopia and other reactions.
taboo
1. Patients treated with monoamine oxidase inhibitor (MAOI).
2. Patients receiving other central appetite suppressants.
3. Patients with anorexia nervosa.
4. Patients who are allergic to the ingredients of this product.
5. Hypertensive patients whose blood pressure cannot be controlled or is not well controlled.
6. Patients with coronary heart disease, heart failure, arrhythmia and stroke.
7. Patients with severe hepatic and renal insufficiency.
Matters needing attention
1. The treatment of obesity should focus on diet control and exercise.
2. Obesity caused by Cushing's syndrome and hypothyroidism should be excluded from the application scope of this product.
3. Patients with a history of hypertension should be used with caution.
4. Because it may increase or aggravate the formation of gallstones, patients with gallstones should use this product with caution.
5. This product can cause pupil dilation, so patients with angle-closure glaucoma should use it with caution.
6. Patients with a history of epilepsy should use it with caution, and patients with epilepsy should stop using it.
7. It may affect judgment, thinking or motor skills.
Medication for pregnant and lactating women
Animal experiments show that this product has teratogenic effect, but no carcinogenic or mutagenic effect has been observed. It is recommended that pregnant women or pregnant women and lactating women do not take this product.
Children's medication
The safety and effectiveness of this product for children under 16 years old have not been established, so it is not recommended for children under 16 years old.
Medication for elderly patients
Due to the decline of heart, kidney and liver function in the elderly, the possibility of drugs for other diseases increases, so the dosage selection of drugs for the elderly should be cautious.
drug interaction
1. This product cannot be used with monoamine oxidase inhibitor (MAOI). Maoi should be stopped for at least 2 weeks before starting treatment with this product; However, before using MAOI, stop using this product for at least 2 weeks.
2. Because this product inhibits serotonin reuptake, it is not suitable for use with other serotonin drugs.
3. Patients who are taking drugs that affect blood pressure and heart rate (such as norephedrine, ephedrine and pseudoephedrine) should use this product with caution.
4. This product has potential interaction with drugs that inhibit cytochrome P450(3A4) metabolism, such as ketoconazole and erythromycin, but the effect is not significant.
excessive
At present, there is no specific antidote for overdose of this product. The treatment methods include general methods to deal with overdose, such as ensuring smooth breathing, monitoring heart and vital signs, and taking symptomatic support treatment. Beta blockers can be used cautiously to control hypertension and tachycardia. The effects of diuresis and hemodialysis have not been confirmed.
standard
5mg (calculated as c12h26cln HCl H2O)
store
Shaded and sealed storage.
term of validity
parcel
Registration authentication number
Production enterprise
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