Date of approval.
Date of revision.
Acarbose Capsules Instructions
Please read the instructions carefully and use under the guidance of a physician
Drug Name]
Generic name: Acarbose Capsules
Trade name: Bexi
English name: Acarbose Capsules
Hanyu Pinyin: Akabotang Jiaonang
Ingredients
The main ingredient of this product is Acarbose.
Chemical name: O-4,6-dideoxy-4- [[(1S,4R,5S,6S)-4,5,6-trihydroxy-3-(hydroxymethyl)cyclohexen-2-yl]amino]-α-D-glucopyranosyl-(1→4)-O-α-D-glucopyranosyl-(1→4)-D-glucopyranose.
Chemical structure formula.
Molecular formula: C25H43 NO18
Molecular weight: 645.63
【Properties】.
The content of this product is white or off-white powder.
Indications】
In combination with dietary control, it is used for.
(1) Type 2 diabetes mellitus
(2) Lowering postprandial blood glucose in people with low glucose tolerance
Specification
50mg
Dosage]
Swallow the whole capsule immediately before meal, the dose should be individualized.
The recommended dose is 50mg once, 3 times a day, then gradually increase to 100mg once, 3 times a day. In individual cases, the dose may be increased to 200mg 3 times a day. Or as prescribed by the doctor.
If the patient is not effective after 4 to 8 weeks of medication, the dose may be increased. If the patient still has discomfort after adhering to a strict diabetic diet, the dose cannot be increased and sometimes the dose needs to be reduced appropriately, with an average dose of 100mg once, 3 times a day.
Adverse reactions】According to the literature
Adverse reactions were classified according to CIOMS III frequency categories (number of patients in placebo-controlled studies as of February 10, 2006: acarbose N=8595, placebo N=7278) based on clinical studies of adverse drug reactions as follows.
In the same frequency grouping, adverse reaction events were ranked in order of decreasing severity.
Very common Incidence ≥ 10%
Very common Occurrence ≥ 1% < 10%
Occasional Occurrence ≥ 0.1% <1%
Rare Occurrence ≥ 0.01% <0.1%
Unknown Adverse reactions were only identified during post-marketing surveillance (as of December 31, 2005) and the incidence could not be assessed.
Systemic organ classification Very common Common Occasional Rare Unknown Blood and lymphatic system abnormalities Thrombocytopenia Immune system abnormalities Allergic reactions (rash, erythema, urticaria) Vascular abnormalities Edema Gastrointestinal abnormalities Bloating Diarrhea, gastrointestinal and abdominal pain Nausea, vomiting, dyspepsia Incomplete bowel obstruction, intestinal obstruction, cystic pneumatosis of the intestinal wall Liver and biliary abnormalities Elevated liver enzymes Jaundice Hepatitis Skin and subcutaneous tissue disorders Acute Generalized eruptive pustular dermatosis has been reported post-marketing for liver disease, liver function abnormalities and liver injury, and death from fulminant hepatitis has been found in individual patients in Japan, but whether this is related to acarbose is unclear.
Gastrointestinal side effects may be exacerbated if the prescribed diet is not followed.
If severe discomfort persists despite a controlled diet, consult a physician and reduce the dose temporarily or for a long time.
Clinically relevant abnormalities in liver function tests have been observed in individual patients treated with acarbose 150-300 mg daily, but such abnormalities were transient during acarbose treatment (more than 3 times the high limit of normal, refer to the precautions section).
[Contraindications].
1. Contraindicated in persons with hypersensitivity to acarbose and/or inactive ingredients.
2. Contraindicated in patients with chronic gastrointestinal disorders with significant digestive and absorption disturbances, especially inflammatory bowel disease.
3. Contraindicated in patients with disorders that may worsen due to intestinal distention (e.g., gastrocardiac syndrome (Roemheld), severe hernia, intestinal obstruction or tendency to intestinal obstruction, intestinal ulcers).
4. Contraindicated in patients with severe renal impairment (creatinine clearance <25 ml/min).
5. Severe liver disease (severe hepatic insufficiency) and cirrhosis.
6. diabetic ketoacidosis.
Caution】 1.
1. Patients should follow medical advice to adjust the dose and pay strict attention to diet.
2. Asymptomatic elevation of liver enzymes may occur with high doses of this product, therefore, monitoring of liver enzymes should be considered for the first 6 to 12 months of dosing. If elevated liver enzymes are observed, especially if they persist, it may be necessary to reduce the dose or discontinue treatment. Fatal fulminant hepatitis has been reported abroad, but the association with acarbose is unclear.
3. When this product is combined with other hypoglycemic drugs (such as sulfonylureas, metformin or insulin), the possibility of hypoglycemia is increased and the dose of the combined drug should be adjusted. This product can make the breakdown of sucrose to fructose and glucose more slowly, so if acute hypoglycemia occurs, sucrose should not be used, but glucose should be used to correct the hypoglycemic response. Severe hypoglycemia may require intravenous infusion of glucose or injection of glucagon.
4. Temporary failure of glycemic control may occur in diabetic patients with fever, trauma, infection or surgery. Temporary insulin therapy may be necessary in such cases.
5. When treated with acarbose, crude sugar and foods containing crude sugar may easily cause intestinal pain or even diarrhea.
[For pregnant and nursing women].
1. Because of the lack of data from clinical studies on the use of this drug in pregnant women, this product should not be used in women during pregnancy.
2. A small amount of radioactive material was found in the milk of lactating rats after administration of radiolabeled acarbose, and no similar findings have been reported in humans. Even so, it is contraindicated in nursing women because the effect of acarbose in breast milk on the infant cannot be ruled out.
Pediatric Use]
In view of the lack of sufficient information on the efficacy and tolerability of this product in children and adolescents, this product should not be used in patients under 18 years of age.
Geriatric Use
No change in dose or frequency of dosing is necessary for elderly patients over 65 years of age.
Drug Interactions】According to the literature
During treatment with acarbose, sucrose or foods containing sucrose often cause abdominal discomfort and even diarrhea due to increased carbohydrate digestion in the colon.
Certain drugs are prone to hyperglycemia, which may cause failure of glycemic control. Such medications include thiazides, diuretics, glucocorticoids, phenothiazines, thyroid medications, estrogens, birth control pills, phenytoin sodium, niacin, sympathomimetics, calcium channel blockers, and isoniazid. When such drugs are used in patients taking acarbose, blood glucose control should be closely monitored.
Sulfonylureas or insulin may cause hypoglycemia. The combination of acarbose with sulfonylureas or insulin may cause further blood glucose reduction and increase the possibility of hypoglycemia. Cases of hypoglycemic shock have been reported and should be monitored closely. If hypoglycemia occurs, the appropriate dose should be adjusted.
Acarbose can affect the bioavailability of digoxin, so the dose of digoxin needs to be adjusted.
Concomitant use of cauleenamine, intestinal adsorbents (e.g. charcoal) and digestive enzyme preparations containing carbohydrate-degrading enzymes (e.g. amylase, pancreatic enzymes) may diminish the efficacy of acarbose and should therefore be avoided.
Concomitant administration of neomycin and this product may result in a significant decrease in postprandial blood glucose and increase the frequency and severity of gastrointestinal adverse reactions. If symptoms are very severe, a temporary reduction in the dose of this product may be considered.
No interaction has been found with dimethicone oil and simethicone oil.
[Drug Overdose].
If an overdose of acarbose is taken on an empty stomach, gastrointestinal reactions will not occur in general; when an overdose of acarbose is taken together with food or drinks containing carbohydrates (polysaccharides, oligosaccharides, disaccharides), severe gastrointestinal distention and diarrhea will occur, so when an overdose of acarbose is taken avoid drinking or eating foods containing carbohydrates for the next 4 to 6 hours.
Pharmacology and Toxicology
This product is a biosynthetic pseudotetrasaccharide. Animal test results show that this product has an inhibitory effect on the activity of α-glucosidase in the brush border of small intestinal wall cells, which slows down the degradation of polysaccharides, oligosaccharides or disaccharides in the intestine and slows down the degradation and absorption of glucose from carbohydrates into the blood, decreasing the rise of postprandial blood glucose and decreasing the average blood glucose value.
Pharmacokinetics】According to the literature
A study of the pharmacokinetics of 0.2g of radiolabeled acarbose administered orally to healthy volunteers showed that after oral administration of acarbose, 1-2% of the active inhibitor was absorbed through the intestine, plus absorbed products broken down by digestive enzymes and intestinal bacteria, accounting for a total of 35% of the dose administered.
No measurable metabolism of acarbose was observed in vivo, but instead acarbose was broken down by digestive enzymes and intestinal bacteria in the intestinal lumen, and its degradation products were absorbed in the lower part of the small intestine. After oral administration, acarbose and its degradation products are rapidly and completely excreted in the urine, and 51% of the dose is excreted in the feces within 96 hours.
Special Populations
The area under the blood concentration curve (AUC) and maximum concentration (Cmax) of acarbose at steady state were approximately 1.5 times higher in elderly compared to young subjects, but the difference was not statistically significant.
In patients with severe renal insufficiency (creatinine clearance <25 ml/min), the Cmax and AUC of acarbose were 5-fold higher and 6-fold higher than those of subjects with normal renal function.
Storage】Seal and store in a cool and dark place.
Package】Package: Pharmaceutical aluminum foil/polyvinyl chloride solid pharmaceutical rigid tablets, specifications: 50mg×15 capsules/plate×1 plate/box; 50mg×15 capsules/plate×2 plate/box; 50mg×15 capsules/plate×3 plate/box
Expiration date】 18 months
Executive Standard】 Chinese Pharmacopoeia, 2015 Edition, Part II.
Approval number】 State Drug Administration H20020391
【Manufacturing enterprise
Enterprise name: Sichuan Green Leaf Pharmaceutical Co.
Production Address: No. 6 and 8, Section 2, Wangjiang Road, Yutang Town, Longmatan District, Luzhou City
Postal code: 646100
Telephone number: (028)86636527 (sales consulting) (0830)2701406 (quality consulting)
Fax number: (028)86635365 (sales consultation) (0830)2703647 (quality consultation)
Registered address: No. 6 and 8, Section 2, Wangjiang Road, Yutang Town, Longmatan District, Luzhou City
Website: Http://www.scluye.com