AMARYL ® is a Glimepiride-based drug.
THERAPEUTIC GROUP: Oral hypoglycemic agents - Sulfonamides, urea derivatives
Indications AMARYL ® - Glimepiride
AMARYL ® is indicated as a pharmacological aid useful for the treatment of type II diabetes, in case of therapeutic failure of non-pharmacological strategies such as diet, physical activity and lifestyle.
Mechanism of action AMARYL ® - Glimepiride
The therapeutic action of AMARYL ® is guaranteed by its active ingredient Glimepiride, belonging to the pharmacological category of sulfonamides.
Taken orally, it is in fact absorbed at the gastrointestinal level, reaching its maximum plasma concentration in just two and a half hours, and persisting in the bloodstream for a period of between 5 and 8 hours.
Once its activity is terminated, it is metabolized by liver enzymes belonging to the cytochrome family and eliminated largely through the faeces, and to a small extent through the urine.
The hypoglycemic efficacy of glimepiride is determined by the concomitant presence of intrapancreatic and extrapancreatic mechanisms.
More precisely, the former, which occur at the level of pancreatic Beta cells, promote the endogenous secretion of insulin, acting on a specific potassium channel, responsible for the "wave of depolarization useful for ensuring the calcium-mediated release of insulin, while the" extrapancreatic action takes the form of an increase in insulin efficacy on muscle and adipose tissue, which is necessary to improve glucose uptake and inhibit hepatic glycogenolysis and gluconeogenesis processes.
Studies carried out and clinical efficacy
1. GLIMEPIRIS AND ATHEROSCLEROSIS
Diabetes Res Clin Pract. 2011 Jan 21.
Effects of glimepiride and glibenclamide on carotid atherosclerosis in type 2 diabetic patients.
Katakami N, Kaneto H, Matsuhisa M, Shimomura I, Yamasaki Y.
Recent and very interesting study that has shown how the maximum annual thickening of the medial intima of the carotid artery in type II diabetic patients can be significantly reduced by taking glimepiride as a hypoglycemic agent. THERAPY
2. COMBINED: METFORMIN AND GLIMEPIRIDE
Am J Ther. 2011 Feb 15.
Evaluation of Efficacy and Tolerability of Glimepiride and Metformin Combination: A Multicentric Study in Patients with Type-2 Diabetes Mellitus, Uncontrolled on Monotherapy with Sulfonylurea or Metformin.
Pareek A, Chandurkar NB, Salkar HR, Borkar MS, Tiwari D.
Patients with type II diabetes, with fasting glucose greater than 140 mg / dL and Hb1Ac greater than 7% were treated for 12 weeks with a combination of metformin and glimepiride. The data suggest the greater efficacy of the combined treatment in improving glycemic control, also significantly reducing the values of glycosylated hemoglobin, without clinically relevant side effects.
3. THERAPY WITH GLIMEPIRIS: METABOLIC AND CARDIOVASCULAR ASPECTS
Diabetes Res Clin Pract. 2010 Apr; 88: 71-5. Epub 2009 Dec 31.
Effects of Glimepiride on metabolic parameters and cardiovascular risk factors in patients with newly diagnosed type 2 diabetes mellitus.
Xu DY, Zhao SP, Huang QX, Du W, Liu YH, Liu L, Xie XM.
Administration of glimepiride for 12 weeks in patients with type II diabetes has been shown to rapidly reduce fasting blood glucose levels, stabilize glycemic control, improve lipoprotein metabolism, reduce insulin resistance and improve fibrinolytic activity. .
Method of use and dosage
AMARYL ® 1, 2, 3, 4 and 6 mg tablets of Glimepiride: the formulation of the correct therapeutic dosage of Glimepiride cannot ignore the metabolic situation of the diabetic patient and the blood glucose levels measured. Therefore, the initial dosage, which is that of a 1 mg daily tablet taken either at breakfast or during the main meal, may be sufficient to ensure good glycemic control or require an increase proportional to the metabolic decompensation recorded.
In the case of combined therapies with metformin or insulin, it is always recommended to start with the lowest dosages, to gradually increase them until a good glycemic control is achieved.
Medical supervision is of fundamental importance, both in the initial choice of the appropriate dosage and in the prolonged and constant monitoring of therapy.
AMARYL ® warnings - Glimepiride
The correct therapeutic approach to the type II diabetic patient should include dietary and health treatment before pharmacological treatment, useful for improving the general as well as metabolic state of health.
The wrong dosage of AMARYL ® could be accompanied by the presence of hypoglycemic crises punctuated by side effects such as tiredness, headache, hunger, reduced alertness and reaction time, drowsiness and loss of consciousness for which it would be necessary to intervene quickly with oral administration of simple carbohydrates.
For this reason it is very important that the correct dosage is formulated by the doctor after a "careful evaluation of the dietary habits, the physio-pathological conditions of the patient and the laboratory parameters and that the entire therapeutic plan is monitored by periodic blood chemistry checks.
The use of sulfonylureas could also be associated with haemolytic crises in patients with G6PD enzyme deficiency, and with important side effects in patients with impaired hepatic and renal function.
AMARYL ® contains lactose, therefore its intake is not recommended in patients with lactase enzyme deficiency or glucose / galactose malabsorption.
The risk of hypoglycaemia could reduce the patient's perceptive abilities, making it dangerous to use machines or drive vehicles, and for this reason it is very important to pay attention to the warning symptoms of hypoglycemia.
PREGNANCY AND BREASTFEEDING
Although glycemic control during pregnancy is particularly useful for the correct development of the fetus, the administration of glimepiride is contraindicated due to the presence of potential side effects.
Therefore, one should resort to taking drugs with a higher safety profile and better characterized such as insulin.
Given the possible secretion of the unchanged active ingredient in breast milk, it would be advisable to avoid breastfeeding during therapy, in order to reduce the important risk of hypoglycaemia in the infant.
Interactions
The hepatic metabolism of glimepiride supported by the CYP2C9 enzyme subjects the active substance to the risk of important alterations of its pharmacokinetic properties.
Active ingredients such as phenylbutazone, azapropazone and oxyphenbutazone, insulins and other oral ntidiabetic products such as metformin, salicylates and para-amino-salicylic acid, anabolic steroids and male sex hormones, chloramphenicol, some long-acting sulphonamides, tetracycline, clarinet antibiotics and chlarin coumarins, fenfluramine, fibrates, ACE inhibitors, Fluoxetine, MAO-inhibitors, Allopurinol, probenecid, sulfinpyrazone, Sympatholytics, cyclophosphamide, trophosphamide and ifosfamidi, miconazole, fluconazole, pentoxifylline and tritoqualine concentrating enzyme, could inhibit the above-mentioned efficacy of the glimepiride.
On the contrary, inducer of the CYP2C9 enzyme such as estrogens and progestogens, diuretics, glucorticoids, thyroid stimulants, adrenaline, nicotinic acid, laxatives, phenytoin, barbiturates could increase the metabolism of glimepiride, also significantly reducing the therapeutic efficacy of AMARYL ®
Alcohol, beta-blockers and H2-antagonists, on the other hand, could unpredictably alter the hypoglycemic action of this medicine.
Contraindications AMARYL ® - Glimepiride
AMARYL ® is contraindicated in type I diabetic patients, keto acidosis and diabetic coma and in patients with impaired liver and kidney function.
Individuals with known hypersensitivity to the active substance or other sulfonylureas or sulfonamides should refrain from taking this medicine.
Undesirable Effects - Side Effects
The various clinical trials and post-marketing experience seem to agree on the excellent tolerability of AMARYL ® and on the absence of clinically relevant side effects.
In fact, episodes such as alterations in haematochemical parameters, disorders of the gastrointestinal tract, neurological or vision disorders and dermatological manifestations and not due to hypersensitivity to the active ingredient have been very rare.
However, it is important to remember that the long half-life of the drug could lead to an accumulation of the active ingredient, increasing the risk of hypoglycaemia in case of repeated administration. For this reason it is preferable to administer AMARYL in a single intake.
Note
AMARYL ® can only be sold under medical prescription.
The information on AMARYL ® - Glimepiride published on this page may be out of date or incomplete. For a correct use of this information, see the Disclaimer and useful information page.
