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Glimepiride is a hypoglycemic drug for oral use - a derivative of the sulfonylurea of the new (third) generation. Glimepiride acts mainly by stimulating the secretion and release of insulin from the beta cells of the pancreas (pancreatic action). Like other sulfonylurea derivatives, this effect is based on an increase in the response of beta cells of the pancreas to physiological stimulation with glucose, while the amount of secreted insulin is much less than with the action of traditional sulfonylurea derivatives. The least stimulating effect of glimepiride on insulin secretion provides a lower risk of hypoglycemia. In addition to this, glimepiride has an extra pancreatic action - the ability to improve the sensitivity of peripheral tissues (muscle, fat) to the action of its own insulin, to reduce insulin absorption by the liver; inhibits glucose production in the liver. Glimepiride selectively inhibits cyclooxygenase and reduces the conversion of arachidonic acid to thromboxane A2, which promotes platelet aggregation, thus exerting an antithrombotic effect.
Glimepiride contributes to the normalization of lipids, reduces the level of small aldehyde in the blood, which leads to a significant reduction in lipid peroxidation, it contributes to the anti-atherogenic effect of the drug.
Glimepiride increases the level of endogenous α-tocopherol, the activity of catalase, glutathione peroxidase and superoxide dismutase, which helps reduce the severity of oxidative stress in the patient’s body, which is constantly present in diabetes mellitus type 2.
The drug is indicated for the treatment of type 2 diabetes mellitus with the ineffectiveness of the previously prescribed diet and exercise.
With the ineffectiveness of monotherapy with glimepiride, it can be used in combination therapy with metformin or insulin.
The active substance is glimepiride - 4 mg;
Excipients: lactose monohydrate 150.80 mg, corn starch 4.66 mg, sodium carboxymethyl starch 10.00 mg, povidone 6.00 mg. polysorbate 1.34 mg, talc 2.00 mg, magnesium stearate 1.20 mg, iron dye (E 172) 0.30 mg;
Glimepiride is marketed under different brands and generic names, and comes in different dosage forms:
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Dosage and Administration
The drug is administered orally. The initial and maintenance doses of Glimepiride are set individually based on the results of regular monitoring of glucose concentration in the blood.
Initial dose and dose selection
At the beginning of treatment, 1 mg of glimepiride is prescribed once a day. When an optimal therapeutic effect is achieved, it is recommended to take this dose as a maintenance. In the absence of glycemic control, the daily dose should be gradually increased under regular control of the concentration of glucose in the blood (at intervals of 1-2 weeks) to 2 mg, 3 mg or 4 mg per day. Doses over 4 per day are effective only in exceptional cases. The maximum recommended daily dose is 6 mg. Use in combination with metformin
In the absence of glycemic control in patients taking metformin, concomitant therapy with glimepiride may be initiated. While maintaining the dose of metformin at the same level, treatment with Glimepiride begins with a minimum dose, and then the dose gradually increases depending on the desired level of glycemic control, up to the maximum daily dose. Combination therapy should be carried out under close medical supervision.
Use in combination with insulin
In cases where it is not possible to achieve glycemic control by taking the maximum dose of Glimepiride, in monotherapy or in combination with the maximum dose of metformin, a combination of Glimepiride with insulin is possible. In this case, the last dose of Glimepirida assigned to the patient remains unchanged. In this case, insulin treatment begins with a minimum dose, with the possible subsequent gradual increase in its dose under the control of glucose concentration in the blood. Combined treatment requires mandatory medical supervision.
The time and frequency of taking the daily dose is determined by the doctor, taking into account the patient's lifestyle. As a rule, the appointment of a daily dose in a single dose immediately before or during a hearty breakfast or the first main meal is sufficient. Glimepirida pills taken whole, without chewing, with a sufficient amount of liquid (about 0.5 cups). It is very important not to skip meals after taking Glimepirida.
Duration of treatment
As a rule, treatment with glimepiride can be long.
Transfer of the patient from another oral hypoglycemic drug to glimepiride.
When transferring a patient from another oral hypoglycemic drug to Glimepiride, the initial daily dose of the latter should be 1 mg (even if the patient is transferred to Glimepiridt from the maximum dose of another oral hypoglycemic drug). Any increase in the dose of Glimepiride should be carried out in stages in accordance with the above recommendations. It is necessary to take into account the effectiveness, dose and duration of action of the hypoglycemic agent used. In some cases, especially when taking hypoglycemic drugs with a long half-life (for example, chlorpropamid), it may be necessary to temporarily (within a few days) discontinue treatment in order to avoid an additive effect that increases the risk of hypoglycemia.
Transfer of a patient from insulin to glimepiride
In exceptional cases, when insulin therapy is performed in patients with type 2 diabetes mellitus, when compensating for the disease and when the secretory function is intact (3-cells of the pancreas, insulin can be replaced by Glimepiride. The translation should be carried out under close medical supervision. minimum dose of 1 mg.
Metabolism:development of hypoglycemic reactions. These reactions mainly occur shortly after taking the drug, and they are not always easy to stop.
From the organs of vision:during treatment (especially at the beginning), a transient decrease in vision due to a change in glucose concentration in the blood may be observed.
On the part of the digestive system:increased activity of liver enzymes, cholestasis, jaundice, hepatitis (up to the development of liver failure).
From the hemopoietic system:thrombocytopenia (moderate to severe), leukopenia, hemolytic or aplastic anemia, erythrocytopenia, granulocytopenia, agranulocytosis and pancytopenia.
On the part of the digestive system:nausea, vomiting, feeling of heaviness or discomfort in the epigastrium, abdominal pain, diarrhea, very rarely leading to discontinuation of treatment.
Allergic reactions:appearance of urticaria symptoms (itching, skin rash). Such reactions are, as a rule, moderately pronounced, but can progress, accompanied by a drop in blood pressure, dyspnea, up to the development of anaphylactic shock. If symptoms of urticaria appear, consult a doctor immediately. Possible cross-allergy with other sulfonylurea derivatives, sulfonamides, or similar substances, the development of allergic vasculitis is also possible.
In exceptional cases:
Other side effects:may develop photosensitivity, hyponatremia.
Since certain side effects, such as: severe hypoglycemia, serious changes in the blood picture, severe allergic reactions, liver failure, can under certain circumstances pose a threat to life, if undesirable or severe reactions develop, the patient should immediately inform the attending physician and Do not continue taking the drug without recommending it.
Carefully - conditions requiring the transfer of the patient to insulin therapy (extensive burns, severe multiple injuries, extensive surgical interventions); adrenal insufficiency; thyroid disease (hypothyroidism, thyrotoxicosis); impaired absorption of food and drugs in the gastrointestinal tract, including intestinal obstruction, intestinal paresis; infectious fever; alcoholism; in the first days of treatment (increased risk of hypoglycemia); with an increased risk of hypoglycemia; with intercurrent diseases during treatment or with a change in the patient's lifestyle (change in diet and meal times, increase or decrease in physical activity).
Glimepiride is metabolized by cytochrome P450 2S9 (CYP2C9). With simultaneous use with CYP2C9 isoenzyme inducers, for example, rifampicin, it is possible to reduce the hypoglycemic action of glimepiride and increase the risk of developing hypoglycemia if they are canceled without dose adjustment of glimepiride. When used simultaneously with CYP2C9 isoenzyme inhibitors, for example, fluconazole, the hypoglycemic effect of glimepiride can be increased and the risk of hypoglycemia and side effects of glimepiride can increase, and its hypoglycemic action can be reduced if they are canceled without dose adjustment of glimepiride. Strengthening hypoglycemic action and the associated development of hypoglycemia associated with this can be observed with simultaneous use of ages with insulin or other oral hypoglycemic drugs, metformin, inhibitors of angiotensin-converting enzyme (ACE), allopurinol, anabolic steroids, and male reproductive hormones, antiferromatin inhibitors (ACE), allopurinol, anabolic steroids, and male reproductive hormones, antifungal inhibitors (ACE), allopurinol, anabolic steroids, and male reproductive hormones. tropic and isophosphamide, fenfluramine, disopyramide, fibrates, fluoxetine, sympatholytic (guanetidine), inhibitors of Noamine Oxidase (MAO), miconazole, fluconazole, pentoxifylline (when parenterally administered with Pec, in high doses,), phenylbutazone, azapropazone, oxyphenbutazone, zapicidium, quinolone, salicylates, and aminosalicylic acid, sulfinpyrazone, and his / her zyphinbutazone.The weakening of the hypoglycemic action and the associated increase in the concentration of glucose in the blood can be observed with the simultaneous use of glimepiride with acetazolamide, barbiturates, glucocorticosteroids, glucagon, laxatives (with long-term use), nicotinic acid (in high doses) and nicotinic acid derivatives, estrogen and prostate, nicotinic acid, in long-term use, nicotinic acid (in high doses) and derivatives of nicotinic acid, estrogen and prostate, nicotinic acid, in estrogen and prostate and nicotinic acid , phenothiazines, chlorpromazine, phenytoin, rifampicin, thyroid hormones, lithium salts. H2-histamine receptor blockers, clonidine and reserpine, are able to both potentiate and weaken the hypoglycemic effect of glimepiride. Under the influence of such sympatholytic agents, such as beta-blockers, clonidine, guanetidine and reserpine, the weakening or absence of clinical signs of hypoglycemia is possible. Against the background of glimepiride intake, the effect of coumarin derivatives may be enhanced or weakened. With simultaneous use with drugs that inhibit bone marrow hematopoiesis, the risk of myelosuppression increases. Single or chronic drinking can both strengthen and weaken the hypoglycemic effect of glimepiride.
Pregnancy and Lactation
Glimepiride is contraindicated for use in pregnant women. In the case of a planned pregnancy or if the pregnancy occurs, the woman should be transferred to insulin therapy.
Since glimepiride seems to penetrate into breast milk, it should not be given to women during lactation. In this case, it is necessary to switch to insulin therapy or stop breastfeeding.
Glimepiride should be taken in recommended doses and at the scheduled time. Errors in the use of the drug, for example, skipping a dose, can never be eliminated by the subsequent intake of a higher dose. The doctor and the patient should discuss in advance the measures to be taken in case of such errors (for example, skipping the drug or eating) or in situations where it is impossible to take the next dose of the drug at the scheduled time. The patient should immediately inform the doctor in the event of receiving too high a dose of the drug.
If a patient has developed a hypoglycemic reaction while taking 1 mg of glimepiride per day, this indicates that in this patient normalization of blood glucose levels can be achieved with a single diet.
Upon reaching compensation for type 2 diabetes, insulin sensitivity is increased. In this regard, the need for glimepiride may decrease during the treatment process. To avoid the development of hypoglycemia, it is necessary to temporarily reduce the dose or cancel Glimepiride. Dose adjustment should also be carried out when the patient's body weight changes, when their lifestyle changes, or when other factors appear that increase the risk of developing hypo- or hyperglycemia. Adequate diet, regular and sufficient exercise and, if necessary, weight loss are just as important for achieving optimal control of blood glucose levels as regular Glimepiride intake.
Clinical symptomshyperglycemia(inadequate reduction in blood glucose) are: increased frequency of urination, severe thirst, dry mouth and dry skin. In the first weeks of treatment, the risk of hypoglycemia may increase, which requires particularly careful monitoring of the patient. With Glimepiride treatment, with an irregular meal or skipping a meal, it may develophypoglycemia.Its possible symptoms are: headache, hunger, nausea, vomiting, fatigue, drowsiness, sleep disturbances, anxiety, aggression, concentration, attention and reaction disorders, depression, confusion, speech and visual disturbances, aphasia, tremor, paresis, sensory disturbances, dizziness, delirium, cerebral seizures, confusion or loss of consciousness, including coma, shallow breathing, bradycardia. In addition, as a result of the adrenergic feedback mechanism, sweating, anxiety, tachycardia, high blood pressure, angina pectoris, and heart rhythm disturbances can occur.Factors contributing to the development of hypoglycemia include:
- unwillingness or (especially in old age) insufficient ability of the patient to cooperate with the doctor;
- inadequate, irregular meals, skipping meals, fasting, changes in the usual diet;
- imbalance between exercise and carbohydrate intake;
- drinking alcohol, especially when combined with skipping meals;
- impaired renal function;
- severe liver dysfunction;
- Glimepiride overdose;
- some uncompensated diseases of the endocrine system that affect carbohydrate metabolism (for example, dysfunction of the thyroid gland, pituitary or adrenal insufficiency);
- simultaneous use of drugs that enhance the action of glimepiride.
The physician should be informed of the above factors and episodes of hypoglycemia, since they require particularly strict monitoring of the patient. If there are such factors that increase the risk of hypoglycemia, you should adjust the dose of glimepiride or the entire treatment regimen. This must also be done in the case of an intercurrent disease or a change in the lifestyle of the patient.
Symptoms of hypoglycemia may be smoothed out or absent altogether in elderly patients, in patients suffering from vegetative neuropathy or receiving simultaneous treatment with β-blockers, clonidine, reserpine, guanethidine or other sympatholytic agents. Hypoglycemia can almost always be quickly stopped by taking carbohydrates immediately (glucose or sugar, for example, in the form of a piece of sugar, sweet fruit juice or tea). In this regard, the patient should always carry with him at least 20 g of glucose (4 pieces of sugar). Sweeteners are ineffective in the treatment of hypoglycemia.
From the experience of using other sulfonylurea drugs, it is known that, despite the initial success in stopping hypoglycemia, it is possible to relapse. In this regard, continuous and careful observation of the patient is necessary. Severe hypoglycemia requires immediate treatment under the supervision of a physician, and under certain circumstances, hospitalization of the patient.
If a patient suffering from diabetes is treated by different doctors (for example, during his stay in hospital after an accident, with illness on weekends), he must inform them about his illness and prior treatment.
During treatment with glimepiride, regular monitoring of liver function and peripheral blood pattern (especially the number of leukocytes and platelets) is required.
In stressful situations (for example, in case of trauma, surgery, infectious diseases involving fever), it may be necessary to temporarily transfer the patient to insulin therapy.
There is no experience of using Glimepiride in patients with severe hepatic and renal dysfunction or patients on hemodialysis. Patients with severe impaired renal function and liver are shown to be transferred to insulin therapy.
During treatment with glimepiride, regular monitoring of blood glucose and glycated hemoglobin concentration is necessary.
At the beginning of treatment, when switching from one drug to another, or when taking Glimepirida on an irregular basis, there may be a decrease in the concentration of attention and speed of psychomotor reactions of the patient, due to hypo- or hyperglycemia. This may adversely affect the ability to drive vehicles or to control various machines and mechanisms.
Symptoms:hypoglycemia (nausea, vomiting and epigastric pain, anxiety, tremor, visual disturbances, impaired coordination, drowsiness, coma and convulsions).Treatment:if the patient is conscious - induction of vomiting, heavy drinking, activated charcoal and laxative. In case of severe overdose, intravenous bolus administration of a dextrose solution (50 ml of a 40% solution), then an infusion of a 10% solution. Constant monitoring of the patient, maintenance of vital functions and control of the glucose concentration in the blood are necessary (repetition of episodes of hypoglycemia is possible). Further treatment is symptomatic.
- Beta Cell Response to Oral Glimepiride Administration During and Following a Hyperglycaemic Clamp in NIDDM Patients
- A rapid and highly sensitive method for the determination of glimepiride in human plasma by liquid chromatography–electrospray ionization tandem mass spectrometry: application to a pre-clinical pharmacokinetic study
- ChemInform Abstract: Glimepiride.
- Total Synthesis of cis and trans-Hydroxyglimepiride: Active Metabolite of Glimepiride.
- Lower incidence of severe hypoglycaemia in patients with type 2 diabetes treated with glimepiride versus glibenclamide
- Multi-objective optimization strategy based on desirability functions used for electrophoratic separation and quantification of rosiglitazone and glimepiride in plasma and formulations
- Determination of the interaction between glimepiride and hyperbranched polymers in solid dispersions
- A discriminating dissolution method for glimepiride polymorphs
- Direct separation and quantitative determination of glimepiride isomers by high performance liquid chromatography
- Fast HPLC method for the determination of glimepiride, glibenclamide, and related substances using monolithic column and flow program
- Formulation and biological evaluation of glimepiride–cyclodextrin–polymer systems
- Implication of inclusion complexation of glimepiride in cyclodextrin–polymer systems on its dissolution, stability and therapeutic efficacy
- Microparticle size control and glimepiride microencapsulation using spray congealing technology
- Hyperbranched poly(esteramides) as solubility enhancers for poorly water-soluble drug glimepiride
- Pharmacokinetics of glimepiride and cytochrome P450 2C9 genetic polymorphisms
- Determination of glimepiride in human plasma by liquid chromatography–electrospray ionization tandem mass spectrometry
- Determination of glimepiride in human plasma using semi-microbore high performance liquid chromatography with column-switching
- HPLC study of glimepiride under hydrolytic stress conditions
- LC determination of glimepiride and its related impurities
- LC–UV–PDA and LC–MS studies to characterize degradation products of glimepiride
- Effect of gemfibrozil on the pharmacokinetics and pharmacodynamics of glimepiride
- Total synthesis of cis and trans-hydroxyglimepiride: active metabolite of glimepiride
- Simultaneous determination of the sulphonylurea glimepiride and its metabolites in human serum and urine by high-performance liquid chromatography after pre-column derivatization
- Analysis of glimepiride by using derivative UV spectrophotometric method