Date of approval:
Date of revision:
Acarbose Tablets Instructions
Please read the instructions carefully and use under the guidance of a physician http://www.newdruginfo.cn/Html/othdrug/4988760256.html
Drug Name]
Generic name: Acarbose Tablets
English name: Acarbose Tablets
Hanyu Pinyin: Akabotang Pian
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: C25H43NO18
Molecular weight: 645.63
Properties
This product is off-white or light yellow tablet.
Indications】
In combination with dietary control, for.
(1) Type 2 diabetes mellitus.
(2) Reduce postprandial blood glucose in people with low glucose tolerance.
Specification
50mg
Dosage and Administration
Swallow the whole tablet immediately before meal or chew it with the first few bites of food, the dose varies from person to person.
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 4-8 weeks of medication, the dose may be increased. If the patient still has discomfort after adhering to a strict diabetic diet, the dose should not be increased, and sometimes the dose should be reduced appropriately, with the average dose being 100mg once, 3 times a day.
Adverse reactions]
According to the frequency of CIOMS category III (number of patients in placebo-controlled studies as of February 10, 2006: acarbose N = 8595; placebo N = 7278), the adverse drug reactions based on clinical studies are as follows.
In the same frequency grouping, adverse reaction events were ranked in order of decreasing severity.
Very common Incidence ≥10%
Common Occurrence ≥1% <10%
Occasional Occurrence ≥0.1% <1%
Rare Occurrence ≥0.01% <0.1%
Unknown Adverse reactions were only identified in 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 Gastrointestinal distention
Diarrhea, gastrointestinal and abdominal pain
Nausea
vomiting
Indigestion Incomplete bowel obstruction, intestinal obstruction, or cystic pneumatosis of the intestinal wall Hepatobiliary abnormalities Elevated liver enzymes Jaundice Hepatitis Skin and subcutaneous tissue disorders Acute generalized eruptive pustular dermatosis There have been post-marketing reports of liver disease, liver function abnormalities, and liver injury, and individual deaths due to fulminant hepatitis have been observed in Japan, but it is not clear whether this is related to acarbose.
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. Hypersensitivity to acarbose and/or inactive ingredients.
2. Contraindicated in patients with chronic gastrointestinal disorders with significant digestive and absorption disorders, 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
Precautions]
1. Patients should follow medical advice to adjust the dose and pay strict attention to diet.
2. Asymptomatic elevation of liver enzymes may occur in high doses of this product. Therefore, monitoring of liver enzymes should be considered for the first 6 to 12 months of use. 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 relationship 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 blood glucose control may occur in diabetic patients during fever, trauma, infection or surgery. Temporary insulin therapy may be necessary in this situation.
5. A meta-analysis from seven placebo-controlled clinical trials on acarbose for type 2 diabetes (2180 patients in total, 1248 on acarbose and 932 on placebo) showed a 24% reduction in the risk of either cardiovascular event and a 64% reduction in the risk of myocardial infarction. Both of these changes were statistically significant.
[Pregnant and lactating women use].
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.
A small amount of radioactive material was found in the milk of lactating rats after administration of radiolabeled acarbose tablets, and no similar findings have been reported in humans. Even so, since the effect of acarbose tablets in breast milk on the infant cannot be ruled out, it is recommended in principle that this product should not be used in nursing women.
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
1. During acarbose treatment, sucrose or foods containing sucrose often cause abdominal discomfort and even diarrhea due to increased carbohydrate enzymes in the colon.
2. Certain drugs can cause an increase in blood glucose, such as thiazides or other diuretics, glucocorticoids, phenothiazines, thyroid preparations, estrogens, oral contraceptives, phenytoin, niacin, sympathomimetics, calcium channel blockers or isoniazid. Blood glucose should be monitored closely if such drugs are used concurrently.
3. Sulfonylureas or insulin may cause hypoglycemia. The combination of acarbose and sulfonylurea or insulin may cause further blood glucose reduction and increase the possibility of hypoglycemia. Cases of hypoglycemic shock have been reported and should be closely monitored. If hypoglycemia occurs, the appropriate dose should be adjusted.
4. In individual cases, acarbose may affect the bioavailability of digoxin, so the dose of digoxin should be adjusted.
5. The efficacy of acarbose may be reduced by cauleenamine, intestinal adsorbents (e.g. charcoal) and digestive enzyme preparations containing carbohydrate-degrading enzymes (e.g. amylase, pancreatic enzymes), so concurrent use should be avoided.
6. 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 the symptoms are very severe, consider temporarily reducing the dose of this product.
7. No interaction with dimethylsilicone oil has been found.
[Drug overdose].
When an overdose of acarbose tablets is taken with food or drinks containing carbohydrates (polysaccharides, oligosaccharides, disaccharides), severe gastrointestinal flatulence and diarrhea can occur; if an overdose of acarbose tablets is taken on an empty stomach, gastrointestinal reactions do not normally occur. When an overdose of Acarbose tablets is taken, avoid drinking or eating carbohydrate-containing foods for the next 4-6 hours.
[Pharmacological Toxicology].
Acarbose is a biosynthetic pseudotetrasaccharide. Animal test results show that it inhibits the activity of α-glucosidase in the brush border of small intestinal wall cells, thus delaying the degradation of polysaccharides, oligosaccharides or disaccharides in the intestine, slowing down the degradation and absorption of glucose from carbohydrates into the blood, reducing the rise of postprandial blood glucose and decreasing the average blood glucose value.
[Pharmacokinetics].
A pharmacokinetic study 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 in vivo was observed or not, instead acarbose is broken down by digestive enzymes and intestinal bacteria in the intestinal lumen and its degradation products are 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 compared to subjects with normal renal function.
Storage】Store under 25℃ under shade and seal.
Package】Packaged in aluminum-plastic blister, 10 tablets/plate, 1 plate/box, 2 plates/box, 3 plates/box.
Expiration date】24 months
【Execution standard
【Approval number】
【Drug marketing license holder】
Company name: Shiyapharm Group Ouyi Pharmaceutical Co.
Registered address: No. 88 Yangzi Road, Shijiazhuang Economic and Technological Development Zone
Postal Code: 052165
Telephone number: 0311-67163660 0311-87886158
Fax number: 0311-87171665
Manufacturer
Company name: Shiyapharm Group Ouyi Pharmaceutical Co.
Address: No. 88 Yangzi Road, Shijiazhuang Economic and Technological Development Zone
Postal Code: 052165
Telephone number: 0311-67163660 0311-87886158
Fax number: 0311-87171665