AMARYL ® - Glimepiride

AMARYL ® is a drug based on Glimepiride.

THERAPEUTIC GROUP: Oral hypoglycemic agents - Sulfonamides, derivatives of urea

IndicationsAction mechanismStudies and clinical effectiveness Usage and dosage instructionsWarnings Pregnancy and lactationInteractionsContraindicationsUndesirable effects

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 gastro-intestinal level, reaching maximum plasma concentration in just two and a half hours, and persisting in the circulatory stream for a period between 5 and 8 hours.

Once its activity is over, it is metabolized by liver enzymes belonging to the cytochromes family and largely eliminated through the faeces, and in small part through the urine.

The hypoglycemic efficacy of glimepiride is determined by the concomitant presence of intrapancreatic and extrapancreatic mechanisms.

More precisely, the former, which are carried out at the level of pancreatic Beta cells, promote the endogenous insulin secretion, acting on a specific channel with Potassium, responsible for the wave of depolarization useful for guaranteeing the calcium-mediated release of insulin, while the extrapancreatic action takes the form of increased insulin efficacy in muscle and fat tissue, necessary to improve glucose uptake and inhibit hepatic glycogenolysis and gluconeogenesis processes.

Studies carried out and clinical efficacy

1. GLIMEPIRIDE AND ATEROSCLEROSIS

Recent and very interesting study that has shown how the maximum annual thickening of the carotid medial intimate habit in type II diabetic patients, can be significantly reduced by taking glimepiride as a hypoglycemic agent. THERAPY

2. COMBINED: METFORMIN AND GLIMEPIRIDE

Patients with type II diabetes with fasting blood glucose above 140 mg / dL and Hb1Ac above 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, significantly reducing also the values of glycosylated hemoglobin, without clinically relevant side effects.

3. THERAPY WITH GLIMEPIRIDE: METABOLIC AND CARDIOVASCULAR ASPECTS

Administration of glimepiride for 12 weeks in patients with type II diabetes has been shown to be useful in rapidly reducing fasting blood glucose levels, stabilizing glycemic control, improving lipoprotein metabolism, reducing insulin resistance and improving fibrinolytic activity .

Method of use and dosage

AMARYL ® tablets of 1, 2, 3, 4 and 6 mg of Glimepiride: the formulation of the correct therapeutic dosage of Glimepiride, cannot disregard the metabolic situation of the diabetic patient and the measured blood glucose levels. Therefore the initial dosage which is that of a daily tablet of 1 mg taken either at breakfast or during the main meal, could be sufficient to guarantee a good glycemic control or require an increase proportional to the registered metabolic decompensation.

In the case of therapies combined with metformin or insulin, it is always recommended to start from the lowest dosages, to gradually increase them until good glycemic control is obtained.

Medical supervision is of fundamental importance, both in the initial choice of the appropriate dosage, and in the prolonged and constant monitoring of the therapy.

Warnings AMARYL ® - Glimepiride

The correct therapeutic approach to the type II diabetic patient, should foresee, before the pharmacological treatment, the dietetic and healthy one useful for the improvement of the general state of health as well as metabolic.

The incorrect dosage of AMARYL ® could be accompanied by the presence of hypoglycemic crises marked by side effects such as fatigue, headache, hunger, reduced alertness and time of reactions, drowsiness and loss of consciousness for which it would be necessary to intervene rapidly 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 dietary habits, physio-pathological conditions of the patient and laboratory parameters and that the whole treatment plan is monitored by periodic blood chemistry checks.

The use of sulfonylureas could also be associated with haemolytic seizures in patients with G6PD enzyme deficiency, and with major side effects in patients with reduced liver and kidney function.

AMARYL ® contains lactose, therefore its use 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 machinery or driving vehicles; for this reason it is very important to pay attention to the warning symptoms of hypoglycemia.

PREGNANCY AND BREASTFEEDING

Although the control of glycaemia 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 as insulin.

Given the possible secretion of the active ingredient in breast milk, it would be good to avoid breastfeeding during therapy, in order to reduce the significant risk of hypoglycemia in the infant.

Interactions

The hepatic metabolism of glimepiride supported by the enzyme CYP2C9 puts the active principle at risk of significant alterations in its pharmacokinetic properties.

Active ingredients such as phenylbutazone, azapropazone and ossifenbutazone, insulins and other oral ntidiabetic products such as metformin, salicylates and para-amino-salicylic acid, anabolic steroids and male sex hormones, chloramphenicol, some sulfonamides with protracted action, tetracyclines, quinolone antibiotics and clarithromycin, anticoagulants coumarin, fenfluramine, fibrates, ACE inhibitors, Fluoxetine, MAO inhibitors, Allopurinol, probenecid, sulfinpyrazone, simpaticolitici, cyclophosphamide, trophosphamide and ifosphamides, miconazole, fluconazole, pentoxifylline and tritoqualine, could inhibit the aforementioned enzyme by increasing blood concentrations hypoglycemic agent of glimepiride.

In contrast to inducer of the CYP2C9 enzyme such as estrogens and progestins, diuretics, glucorticoids, thyroid stimulants, adrenaline, nicotinic acid, laxatives, phenytoin, barbiturates, they could increase the metabolism of glimepiride, thus significantly reducing the therapeutic efficacy of AMARYL ®

Alcohol, beta-blockers and H2-antagonists could unpredictably alter the hypoglycemic action of this medicine.

Contraindications AMARYL ® - Glimepiride

AMARYL ® is contraindicated in patients with type I diabetes, keto acidosis and diabetic coma and in patients with impaired hepatic and renal function.

Individuals with known hypersensitivity to the active ingredient 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 changes in blood chemistry parameters, disorders of the gastrointestinal tract, neurological or vision disorders, and dermatological manifestations that are 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 hypoglycemia in case of repeated administrations. For this reason it is preferred to administer AMARYL in a single assumption.