Glucobay® (Glucobay®)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceAcarboseAcarbose
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  • Glucobay®
    pills inwards 
    Bayer Pharma AG     Germany
    • Dosage form: & nbsppills
    Composition:

    Each tablet contains:

    Active substance: acarbose 50 mg or 100 mg,

    Excipients: silicon dioxide colloidal anhydrous 0.25 mg or 0.50 mg, magnesium stearate 0.50 or 1.00 mg, corn starch 54.25 or 108.50, microcrystalline cellulose 30 mg or 60 mg, respectively.

    Description:

    50 mg tablets- white or white with a yellowish hue round biconvex tablets with engraving of the brand marking (Bayer's cross) on one side and dosage of "G 50" on the reverse.

    Tablets 100 mg - white or white with a yellowish tinge, oblong biconvex tablets with a risk on both sides, on one side an engraving indicating the dosage - "G 100".

    Pharmacotherapeutic group:Hypoglycemic agent for oral administration
    ATX: & nbsp

    A.10.B.F.01   Acarbose

    Pharmacodynamics:

    The active substance Glucobay® - acarbose, is a pseudotetrasaccharide of microbial origin. Acarbose acts at the level of the gastrointestinal tract, suppressing the activity of small intestine enzymes (α-glucosidase), which participate in the cleavage of di-, oligo- and polysaccharides. As a result, there is a dose-dependent delay in the digestion of carbohydrates, followed by delayed release and absorption of glucose,which is formed during the breakdown of carbohydrates. In this way, acarbose delay and reduce postprandial increase in the concentration of glucose in the blood. Due to a more balanced absorption of glucose from the intestine, the average concentration and its diurnal fluctuations in the blood decrease. In the case of an increase in the concentration of glycosylated hemoglobin, acarbose reduces its level.

    In patients with impaired glucose tolerance (NTG *), the regular administration of acarbose leads to a 25% reduction in the risk of developing type 2 diabetes. In addition, it was found that they significantly reduced the incidence of cardiovascular diseases (by 49%) and myocardial infarction (by 91%).

    The use of acarbose in type 2 diabetes reduces the risk of cardiovascular disease by 24%, and myocardial infarction by 64%.

    * IGT is defined as plasma glucose levels after 2 hours after eating in the range from 7.8 to 11.1 mmol / L (140-200 mg / dl) glucose level while fasting - from 5.6 to 7.0 mmol / l ( 100-1125 mg / dL).

    Pharmacokinetics:

    Suction. About 35% of the administered dose is absorbed in the form of metabolites, less 2% - in an active form.Metabolised in the gastrointestinal tract, mainly by intestinal bacteria and, only partially, by digestive enzymes with the formation of at least 13 compounds in the form of sulfate, methyl and glucuronic conjugates. One metabolite, the product of the cleavage of the glucose molecule in acarbose, has the ability to inhibit alpha-glucosidase. After taking Glucoboy® inside, there are 2 peaks of the maximum concentration of acarbose in the blood plasma, which averaged 52.2 ± 15.7 μg / L and 586.3 + 282.7 μg / L and are observed through 1,1 + 0,3 hours and 20.7 + 5.2 hours, respectively. The appearance of the second peak is due, apparently, to the absorption of products of bacterial decay from the deep sections of the small intestine. In patients with renal insufficiency (creatinine clearance <25 mL / min / 1.73 square meters) Cmah increases 5 times, in the elderly it increases 1.5 times. Bioavailability is 1-2%.

    Distribution: volume distribution of 0.32 l / kg body weight.

    Excretion: the half-life for the distribution and elimination phase is 3.7 + 2.7 hours and 9.6 + 4.4 hours, respectively; 51% of the active substance is excreted through the intestine; 1.7% in unchanged form and in the form of an active metabolite and 34% in the form of metabolites through the kidneys.

    Indications:

    - Treatment of type 2 diabetes mellitus in combination with diet therapy (in the form of monotherapy or in combination with other hypoglycemic drugs, including insulin)

    - Prevention of type 2 diabetes mellitus in patients with impaired glucose tolerance in combination with diet and exercise

    Contraindications:

    - Hypersensitivity to any component of the drug

    - Age under 18 years old

    - Chronic intestinal diseases that occur with severe digestion and absorption disorders

    - Conditions that are accompanied by flatulence (Remkheld's syndrome, large hernias, intestinal stenosis, intestinal ulcers)

    - Pregnancy and lactation

    - Severe renal insufficiency (creatinine clearance <25 mL / min)

    Carefully:

    Pfever, infectious diseases, injuries, surgical interventions. Since the reception of the drug may asymptomatic increase in the level of "liver" enzymes, then during the first 6-12 months of treatment, it is recommended to control the level of these enzymes; usually with the abolition of Glucobia®, their activity is normalized.

    Pregnancy and lactation:

    Since there is no data on the use of Glucobia® during pregnancy and lactation, it is not recommended for use in pregnant and lactating women.

    Dosing and Administration:

    Glucobaya ® tablets are effective only if they are taken immediately before eating whole, without chewing, with a small amount of liquid or chewing with the first portion of food.

    The optimal dose of the drug is selected by the attending physician individually for each patient, since its effectiveness and tolerability vary.

    Combination therapy in combination with diet in patients with type 2 diabetes mellitus

    The initial dose is 1 tablet of 50 mg 3 times a day or 1/2 tablets of 100 mg 3 times a day. In the future, the dose should be increased to an average daily dose of 300 mg per day (2 tablets 50 mg 3 times daily or 1 tablet 100 mg 3 times a day).

    In some cases, if necessary, the dose of the drug can be increased to 200 mg 3 times a day.

    The dose should be increased at intervals of 4-8 weeks if patients in the previous dose did not receive the required clinical effect.

    If the patient, despite strict adherence to diet, increased flatulence and diarrhea, then further increase in the dose should be stopped, and in some cases reduced.The average daily dose of the drug is 300 mg per day.

    Prevention of type 2 diabetes in patients with impaired glucose tolerance in combination with diet and exercise

    The initial dose is 50 mg once daily (50 mg tablets or 1/2 tablets of 100 mg once a day). Within 3 months, the initial dose gradually rises to the recommended therapeutic dose of 100 mg 3 times a day (2 tablets of 50 mg or 1 tablet of 100 mg 3 times a day)

    Patients of advanced age (over 65 years): no dose adjustment is required.

    Children: the use is contraindicated.

    Liver failure: no dose adjustment is required.

    Side effects:

    Data on the incidence of side effects of Glucobay® were obtained from clinical studies and post-marketing reports. Undesirable phenomena are distributed according to the frequency of occurrence in accordance with the following gradation: very often - ≥1/10, often - ≥ 1/100 <1/10, infrequently - ≥ 1/1000 <1/100, rarely - ≥ 1/10000 <1/1000. Within each group, adverse events are presented in descending order of severity. Undesirable phenomena detected during post-marketing monitoring, and for which the incidence rate can not be estimated, are indicated in italics.

    On the part of the circulatory system and lymphatic system: thrombocytopenia - frequency of onset is unknown;

    From the cardiovascular system: edema is rare;

    From the immune system: allergic reactions (rash, erythema, exanthema, urticaria) - the incidence is unknown;

    From the digestive system: flatulence - very often, diarrhea, abdominal pain - often, nausea, vomiting, indigestion - rarely, obstruction or partial obstruction of the intestine, cystic pneumatosis of the intestine - the frequency of occurrence is unknown.

    From the hepatobiliary system: increased activity of "hepatic" enzymes (including transaminases, alkaline phosphatase and gamma-glutamyltransferase) - infrequently, jaundice - rarely, hepatitis - the frequency of occurrence is unknown.

    Also, mainly from Japan, there were reports reported as clinical and / or laboratory signs of impaired liver function and liver damage.

    Some cases of fulminant hepatitis with a fatal outcome took place in Japan. Their relationship with Glucobay® is unclear. If the prescribed diet is not followed, side effects from the gastrointestinal tract can be intensified.

    If adverse events occur, despite strict adherence to the prescribed diet, specialist consultation and temporary or permanent dose reduction are necessary.

    In rare cases, patients receiving the recommended daily dose of Glucobaya®, equal to 150-300 mg / day, there were clinically significant deviations in the parameters of functional liver tests (three times the upper limit of the norm). These changes can be short-term and transitory and disappear on their own against the backdrop of continued treatment with Glucobam®.

    Overdose:

    If a high dose of Glucobaya is obtained with food and / or beverages containing carbohydrates (di-, oligo-, polysaccharides), an overdose may be accompanied by the appearance of flatulence and diarrhea. In case of an overdose for the next 4-6 hours, food or drinks containing carbohydrates should be excluded from the diet.

    When Glucobaya® is taken in an increased dose outside the connection with food intake, the development of symptoms from the intestinal side is not expected.

    Interaction:

    Sucrose and sucrose-containing foods when combined with Glucobam ® cause unpleasant sensations in the abdomen up to diarrhea, which is caused by increased fermentation of carbohydrates in the intestine. Kolestyramine, intestinal adsorbents and preparations containing digestive enzymes, can affect the effectiveness of Glucobaya® when used simultaneously with it. In combination with dimethicone / simethicone interaction reactions are not observed. In some cases, Glucobay® changes the bioavailability of digoxin, which may require dose adjustment of digoxin. Derivatives of sulfonylureas, insulin, metformin increase the hypoglycemic effect of acarbose. Drugs that cause hyperglycemia, such as thiazide diuretics, glucocorticosteroids, phenothiazine, estrogens, oral contraceptives, isoniazid, a nicotinic acid, phenytoin, adrenomimetics, thyroid hormones, blockers of "slow" calcium channels, significantly reduce the activity of acarbose (possibly the development of decompensation of diabetes mellitus).

    The combined use of Glucobaya® and oral neomycin can lead to an excessive decrease in postprandial glycemia, and also increase the incidence and severity of gastrointestinal side effects. In case of serious side effects, it is advisable to consider the possibility of a temporary reduction in the dose of Glucobaya®.

    Special instructions:

    Strict adherence to the anti-diabetic diet is mandatory when using Glucobaya®. Without consultation with a doctor, you can not cancel the drug yourself, as the drug can be canceled with an increase in blood glucose levels. In the case of non-compliance with a prescribed diet, adverse reactions from the intestine may increase. If the symptoms increase, despite strict adherence to the diet, it is necessary to consult a doctor and reduce the dose of the drug for a short or long period.

    Glucobay ® has a hypoklikemic effect, but does not cause hypoglycemia in patients who, as a therapy, are prescribed only to follow a diet without taking hypoglycemic preparations.

    If Glucobay® joins the therapy with insulin or preparations containing sulfonylurea or metformin, then, due to a decrease in the need for these drugs, hypoglycemia may develop, in rare cases down to hypoglycemic coma, which requires a reduction in their dose.

    It should be borne in mind. That Glucobay® slows the conversion of sucrose into fructose and glucose, so sucrose can not be used to stop acute hypoglycemia. In these cases, glucose should be administered.

    It is not recommended to combine Glucobay® with colestyramine, intestinal adsorbents and preparations containing digestive enzymes. When combined with digoxin, it may be necessary to adjust the dose of the latter.

    An identification card for a patient suffering from diabetes should be marked with Glucobay®.

    Effect on the ability to drive transp. cf. and fur:

    Effects on the ability to drive / drive Glucobay® does not render.

    Form release / dosage:Tablets of 50 mg and 100 mg.
    Packaging:For 15 tablets in Al / PP blister, 2 or 8 blisters together with instructions for use in a cardboard pack.
    Storage conditions:At a temperature of no higher than 30 ° C. Keep out of the reach of children.
    Shelf life:3 years. Do not use after the expiration date.
    Terms of leave from pharmacies:On prescription
    Registration number:П N012033 / 01
    Date of registration:31.05.2010
    Expiration Date:Unlimited
    The owner of the registration certificate:Bayer Pharma AGBayer Pharma AG Germany
    Manufacturer: & nbsp
    Representation: & nbspBAYER, AOBAYER, AO
    Information update date: & nbsp01.05.2017
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