Amaryl M tablets produced in 1 mg and 250 mg, 2 mg, 500 mg variations are a reliable way to lower the sugar concentration in the circulatory system. It is prescribed to people with diabetes. The medicinal composition is quite potent, therefore it is used strictly as prescribed by a specialist and under the supervision of a physician. Self-medication with these pills is prohibited and can lead to undesirable consequences.
Technical information
The instructions to Amaril (2 and 500, 1 and 250 mg) indicate the manufacturer of the drug - the company Sanofi. The same accompanying documentation lists the ingredients used by the pharmaceutical company in the manufacture of the composition. The appearance of the drug is being clarified. Amaril M is available in tablet form. Each copy is painted white and covered with a thin film. The tablets are oval, convex on both sides. One of the surfaces is complemented by engraving.
Each instance contains 1 or 2 mg of the antidiabetic component of glimepiride. The manufacturer used a micronized form of the substance. The second active ingredient is metformin in the form of hydrochloride. There are 250 mg or twice as much per capsule. As additional components, lactose and sodium, magnesium compounds, povidone and cellulose are used. The shell is made using mellose, macrogol, wax and titanium molecules.
The tablet product is packaged in blisters. One plate contains ten capsules. One carton pack contains three blisters.
Pharmacology
Instruction "Amaril M" (2 mg, 500 mg and another release format) is assigned to the orally used drugs of the hypoglycemic group. This is a combination medicine containing biguanide and a third-generation sulfonylurea ingredient. The quality of a pharmaceutical product is determined by the characteristics of its key ingredients. It makes sense to consider separately how metformin, glimepiride affect the human body.
Glimepiride
This compound is contained in each tablet in an amount of 1 or 2 mg. “Amaryl M” precisely due to glimepiride has pronounced hypoglycemic qualities. This ingredient is intended for oral administration. Belongs to the sulfonylurea processing product category. Belongs to the third generation of such a group of pharmaceutical compounds. By means of glimepiride, the production of insulin by beta cells is activated. The release processes of this hormone are becoming more saturated. The substance has an inherent pancreatic effect, that is, glimepiride first of all corrects the pancreas. At the same time, when it is taken, peripheral organic lipid and muscle tissues become more sensitive to endogenous insulin. This effect is called extrapancreatic.
Substances made during the processing of sulfonylureas make the production of insulin inside the body more active. This is due to the blocking of the channels of the potassium, depending on ATP. These are located in the membrane (cytoplasm) of the pancreatic beta cells. Due to glimepiride, contained in one tablet in an amount of 1 or 2 mg, Amaril M inhibits calcium channels, which means that a little more comes into the cell structures of this microelement. A high rate of the substitution reaction was found, which is characteristic of binding to and detaching from the protein structures of beta cells. The reaction proceeds with the participation of protein structures associated with potassium-dependent ATP channels. Specific differences from other sulfonylurea derivatives are observed: the binding location is somewhat different. The described chemical reactions initiate the release of insulin. The mechanism of the process is exocytosis. The volumes of hormone produced are less than those produced under the influence of second-generation sulfonylureas. Since glimepiride has a small stimulation effect, the danger of hypoglycemia during the period of taking the medication is minimized.
Extrapancreatic effect
Amaril M tablets are somewhat similar to the classic sulfonylurea transformation products, but glimepiride has a more pronounced effect on the human body outside the pancreas. When it is taken, insulin resistance is significantly reduced, a more pronounced effect of the antioxidant is observed. This substance is a fairly strong antiaggregant and antiatherogenic product. Processing glucose by lipid structures and muscles proceeds with the use of transport proteins localized in cell membranes. Glucose transport to such tissues in the second type of diabetic disease is a stage of glucose processing limited by speed. Due to the drug, the molecules responsible for the movement of glucose become more active, their number increases. Due to this, sugar is more effectively absorbed by the peripheral tissues of the body.
Observations, the results of which are recorded in the instructions for use of Amaril M (2 mg and 500 mg and another release option), show a relatively weak effect of inhibition of cardiomyocyte calcium channels, depending on ATP. The use of the drug allows you to maintain the ability of the myocardium to adapt to ischemia in aspects of the course of metabolic reactions. The activity of phospholipase C. increases. This leads to a decrease in the calcium content inside the cells of lipids and muscles. Consequently, protein kinase A activity decreases. Such prerequisites are important for the activation of sugar processing processes. At the same time, the elimination of glucose by the liver is inhibited due to an increase in the content of fructose-2,6-bisphosphate inside the cells, an element that can block the process of gluconeogenesis.
Note
The use of Amaril M is accompanied with selective blocking of COX activity. At the same time, the activity of the process of transformation of arachidonic acid into the thromboxane of type A, indispensable for platelet aggregation, decreases. When taking the drug, the concentration of fats decreases and peroxidic fat oxidation decreases. Such processes explain the atherogenic effect of the combined medication.
Glimepiride is able to increase the concentration of alpha-tocopherol produced inside the body. At the same time, the activity of catalase and a number of other substances significant for biochemistry are growing. As a result, the oxidative stress inherent in every person suffering from the second type of diabetic disease is reduced.
Metformin
Metformin, contained in an amount of 250 mg or 500 in Amaril M, is a biguanide that has a hypoglycemic effect on the human body. This is observed if insulin is produced in the body, and is present even when the secretion of the hormone is significantly lower than normal. The ingredient does not affect pancreatic beta cells, does not stimulate the production of an important hormone of the endocrine system. At the moment, doctors could not establish the exact mechanism of influence of this substance on humans. Scientists suggest: a substance can potentiate the insulin effect. Some believe that biguanide increases the effects of insulin on peripheral receptor zones.
Thanks to metformin, the susceptibility of organic tissues to hormonal compounds is growing. This is due to an increase in the number of insulin receptors on the membrane surface of cell structures. Explaining the positive reviews about Amaril M that talk about the effectiveness of the drug (2 mg, 500 mg and another release option), the manufacturer draws attention to the ability of the active ingredient to slow down hepatic gluconeogenesis. At the same time, the activity of the formation of fatty acids decreases. Fat oxidation slows down, the content of triglycerides in the circulatory system decreases. The percentage of concentration of VLDL, LDL is adjusted. In the reviews of specialists, it is noted that due to metformin, appetite is somewhat weakened, and the activity of intestinal absorption of carbon is also reduced. The fibrinolytic qualities of the blood become higher, as it inhibits ITAP.
Kinetics: glimepiride
As you can conclude from the reviews of Amaril M (2 mg, 500 mg and half the dosage), the drug usually shows a rather pronounced effect that cannot be expected for too long. This is due to the kinetics of the active ingredients. Glimepiride, as studies have shown, with repeated use in the amount of 4 mg per day is observed in the maximum concentration in blood plasma on average 2.5 hours after administration. The average value is 309 units. A linear relationship between dosage and maximum concentration in blood serum was revealed. Oral administration is accompanied by absolute bioavailability. Eating does not affect the ability of the substance to be absorbed too much - the rate of this process only slightly slows down.
Reviews claim that the positive qualities of the drug cost the buyer expensive - from 800 to one and a half thousand rubles (this is the pharmacy price). Instructions for use "Amaril M" clarifies the kinetics of glimepiride, through which the medication has a positive effect on the human body, fully justifying its value. Observations showed a rather small volume of distribution of the substance - it does not exceed 9 liters. Ability to enter into strong bonds with whey proteins of more than 99%. Ground clearance is small - less than 50 units. The substance is able to penetrate into breast milk and through the placenta. It passes with difficulty through the blood-brain barrier.
The kinetics of the substance obtained once and twice a day were compared. No significant differences were found. Case-by-case variation is small. The cumulative effect is not installed.
Processing and elimination: glimepiride
Despite the high price, Amaril M reviews (2 mg, 500 mg and 1 mg and 250 mg) are presented as a popular and good drug, since the pharmaceutical product has a pronounced positive effect. To explain it, the manufacturer applies instructions to the medicine that describe the features of what is happening in the body. It specifies the ability of glimepiride to transform in liver cells. The process is accompanied by the generation of two derivatives detected in urine, feces.
The half-life of glimepiride at a concentration inherent in repeated use is estimated at 5-8 hours. After the use of an increased dosage, the period increases slightly. With a single use, 58% of the compound is eliminated with urine in the form of derivatives, about 35% - by the intestinal tract. Glimepiride in active unchanged form was not detected in urine.
The terminal half-life of reaction products is estimated at 3-6 hours.
Special case: glimepiride
According to reviews, the price of Amaril M (2 mg, 500 mg, 1 mg and 250 mg) does not become an obstacle to the acquisition of this tool by a wide range of people, since its effect fully justifies the cost. It is noted in the reviews of doctors that the drug is sometimes prescribed to people with specific deviations in the functionality of internal systems and organs. Studies were conducted to determine the nuances of different situations. The dependence of kinetics parameters on the gender of people has not been established. Doctors say that with renal failure and low creatinine clearance, some increased glimepiride clearance, while the average plasma parameter decreased. It is believed that this is due to an increased elimination rate due to a lower degree of binding to serum proteins. From observations, there was no danger of the cumulative effect of glimepiride in the presence of impaired renal function.
Kinetics: Metformin
For the price of Amarila M (2 mg, 500 mg) in Moscow, which varies between 800-1500 rubles, the buyer receives a reliable combination product that lowers the concentration of sugar in the blood. The effect is largely due to the presence of metformin in the drug. Shortly after oral administration of the capsule, this ingredient is absorbed. Localization of the process - gastrointestinal tract. Bioavailability is estimated at 55% on average. The maximum plasma content is observed after approximately 2.5 hours and varies about 2 units. If you use the medicine while eating, the process slows down, the absorption efficiency decreases.
The ingredient is distributed over organic tissues. It has a low ability to react with plasma proteins. Metformin is characterized by transformation reactions, but they proceed extremely weakly.
The elimination half-life is estimated at 6.5 hours. Elimination is carried out by the renal system. Tests were conducted involving healthy people. The clearance revealed in their course was approximately four times higher than creatinine. This led to the conclusion about the activity of renal tubule secretion. In case of insufficient functioning of the renal system, there is a danger of the cumulative effect of metformin.
About the combination
Acquired for 800-1500 rubles (this is exactly the price in Moscow), Amaril M (2 mg, 500 mg or 250 mg) is a combined preparation, each ingredient of which is formulated in a precisely calibrated dosage to maximize the hypoglycemic effect at the lowest risk . The maximum concentration when using a multicomponent drug corresponds to the parameters inherent in the separate administration of metformin and glimepiride. A dose-dependent increase in the maximum concentration of glimepiride is observed with an increase in its content in the combination drug with a constant amount of metformin.
No specific important differences were identified in safety aspects for different dosage options. Studies have examined the profile of side effects. Comparisons were made of people who used the combined drug with 500 mg of metformin and 1 mg and twice as much glimepiride.
When will it help?
Amarila M (2 mg, 500 mg), indicating high efficacy and rather high price, reports that this medicine is prescribed to people suffering from the second type of diabetic disease. In the accompanying documentation, the manufacturer lists the features of the testimony. The drug is recommended for use in diabetes as an element of a multicomponent course. Patients in the reviews note that for the effect of “Amaril M” it is necessary to combine with a well-thought-out diet, a weight loss program and sufficient physical activity in everyday life.
The medication is used if non-drug methods, as well as the use of only metformin or glimepiride, do not allow achieving high-quality control of glucose in the body. It is indicated if the patient was prescribed a combined dose of metformin and glimepiride.
Admission Rules
Containing active ingredients in the amount of 1 and 250 mg or 2 and 500, "Amaryl M" is prescribed in each case individually. It is necessary to take into account what is the current state of the patient’s body, what concentrations of sugars in the circulatory system should be observed. It is advisable to take the lowest effective dose that is possible in a particular case, this helps to control the metabolism to the right degree. The period of the therapeutic program should be accompanied by a regular check of the sugar content. It is also advisable to control how much glycated hemoglobin is in the circulatory system. Incorrect use and skipping dosages cannot be made up for by increasing the next portion. The actions of a person who forgot to take a pill or made a different mistake should be monitored by a specialist. You should discuss this in advance with your doctor.
The therapeutic course is accompanied by an increase in the quality of control of metabolic processes, while the susceptibility of tissues to pancreatic hormones increases. During the treatment period, it may be necessary to adjust the dosage. As a rule, the need for glimepiride is reduced. To exclude hypoglycemia, it is recommended to regularly reduce the amount of the drug used and to abandon the therapeutic course in a timely manner, if this is necessary.
Frequency and dose
It is recommended to take the medicine once or twice daily. The drug is used with meals.Due to the rather high price of Amarila M (2 mg, 500 mg and other release options), it is important for patients to know which doses and application programs are optimal in order to use the acquisition as efficiently as possible. Metformin is allowed for single use in an amount of not more than a gram. The daily maximum volume is twice as much. Glimepiride per day can be obtained no more than 8 mg. Studies have shown that only in a small percentage of cases it is necessary to consume more than 6 mg of glimepiride per day.
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Undesirable consequences
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According to patients, glimepiride can cause hypoglycemia, vomiting and nausea. Hypoglycemia can be noticed by severe headache and lethargy, sleep disturbance and anxiety. Some patients note that they become aggressive, cannot concentrate, lose their vigilance. Hypoglycemia may be indicated by a decrease in the rate of mental reactions and movements. There is a danger of adrenergic antiglycemic regulation, which is one of the options for the body's response to the approximation of hypoglycemia. At the same time, the medicine can cause temporary visual impairment, pain in the stomach. Some patients complain of stool disorders. There is a risk of hepatitis, cholestasis, thrombocyte, leuko, pancyto, erythrocyto, granulocytopenia. Allergies and increased susceptibility to light are possible.
Metformin can initiate lactic acidosis, disorders in the digestive tract. At the beginning of the therapeutic course, about 3% of patients have a metallic taste in their mouth, which disappears on its own and unpredictably. There is a possibility of violation of the liver tests. Metformin can cause rashes, itching of skin, erythema.
Contraindications
Amaril M is not used if a diabetic disease of the first type is detected, as well as acidosis due to metabolism. Do not use if it is in acute form or in the form of a chronicle. You can not use the drug for ketoacidosis against diabetes, including previously transferred. Contraindications are also precoma and coma due to diabetic causes.
Is there an alternative?
Due to the rather high cost of the pharmaceutical product, the people with whom it is prescribed are often interested in whether substitutions in the pharmacies are effective enough for a particular case. As an analogue of Amaril M, pharmacists can offer Maninil or Siofor. Both of these drugs are significantly cheaper, are prescribed for a diabetic disease. Indications and features of the compositions are such that the replacement prescribed by the doctor for these drugs can be carried out only after consultation with your doctor.
The price of the Amaril M analogue, presented on pharmacy shelves under the name Gliformin, is quite attractive. The cost of one package - from one hundred to two hundred rubles - depends both on the outlet and the number of capsules inside. This drug and the “Amaryl M” in question cannot be considered completely similar, since it contains only metformin. If it is impossible to purchase a combination product, you must first check with your doctor if you can use Gliformin.
Also, Bagomet and Bukarban funds can be considered as analogues of Amaril M (2 mg, 500 mg). The Butamide and Glibenclamide pharmaceutical products have proven themselves well. The latter is especially cheap. To some extent, the following drugs are considered analogues of Amaril M (2 mg, 500 mg):
- Glibutide.
- Glycvidon.
- Gliclazide.
What else is possible?
As an alternative, the medicine “Glipizide” is sometimes suitable. As can be concluded from the indications specified in the instructions for use, the drug “Diabeton” will be an analogue of Amaril for some patients. Sometimes doctors are advised to consider Metformin. Alternatively, they can offer:
- Glibomed.
- "Isodibut."
- "Diagnizide."
Pharmaceutical products Glucofage and Glucovans, Diaformin have a good reputation.
What do patients say?
As noted in the reviews, the price of Amaril M (2 mg, 500 mg and 250 mg) is quite high, and this is the main minus. Not every diabetic who has been recommended this remedy can afford it. Persons taking the drug note its reliability and good effect. It effectively controls the sugar content in the circulatory system, improves the quality of life of people suffering from the second type of diabetic disease. At the same time, many note: taking the drug was accompanied by side effects. Even strict adherence to the recommendations of the manufacturer and the doctor does not completely eliminate some negative feelings.