Amaryl (Glimepiride)

$ 111.94$ 283.00

Category: Diabetes
Commercial name: Amaryl
Active ingredient: Glimepiride
Production form: Pills
Available dosage: 2 mg, 4mg

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Description

Amaryl (Glimepirid). Dosage, Side Effects, Interactions

Amaryl (Glimepirid) is an antidiabetic from the active substance group of sulfonylureas.

Amaryl (Glimepirid) is an insulinotropic oral antidiabetic that belongs to the group of sulfonylureas . The active ingredient is only effective if the body’s own insulin production is still partially functional. It is used for the symptomatic treatment of type 2 diabetes mellitus when the basic therapy consisting of diet, physical activity and weight reduction alone is not sufficient. As a rule, glimepiride is used as monotherapy, but the active substance can also be combined with metformin in type 2 diabetics of normal weight . In the case of secondary insufficiency of the beta cells of the pancreas, a combination with insulin or incretin mimetics is also possible.

Application type

Glimepiride is available in oral tablet form. In addition to drug therapy, the basis of diabetes treatment is an adequate diet, regular physical activity and regular checks of blood and urine values.

How Amaryl (Glimepirid) works

Type 2 diabetes is characterized by a reduced response of the body’s cells to insulin in combination with a functional impairment of the pancreatic beta cells. Because of this, the physiological insulin-dependent lowering of the glucose level is reduced and the blood sugar level of the patients is increased. Glimepiride stimulates the release of insulin from pancreatic beta cells independent of blood glucose levels. When blood sugar levels are high, glucose is taken up by the beta cells via so-called GLUT2 transporters. Oxidation processes lead to increased ATP formation, which leads to the closing of ATP-dependent potassium channels. Glimepiride binds to these potassium channels, reducing the likelihood that they open. The cells depolarize and as a result voltage-gated calcium channels open. The incoming calcium in turn promotes the exocytosis of insulin and thus the reduction of blood sugar levels.

Glimepiride also has extrapancreatic effects: the active ingredient improves insulin sensitivity of peripheral tissues, reduces hepatic insulin uptake and increases the number of active glucose transporters in muscle and fat cell membranes. This increases insulin levels and stimulates glucose uptake. Furthermore, glimepiride appears to have inhibitory effects on hepatic glucose production.

 

Pharmacokinetics

Absorption

Glimepiride is rapidly and completely absorbed from the gastrointestinal tract. Food has no relevant influence on absorption. Peak plasma levels are reached after about 2.5 hours. At physiological pH, the active substance is 90% in the ionic form, which binds to the target, the potassium channel of the beta cells.

Distribution

The volume of distribution of glimepiride is small at 8.8 L and approximately the same as that of albumin. The active ingredient has a very high plasma protein binding of over 99% and crosses the blood-brain barrier to a small extent.

Metabolism

Glimepiride is metabolised by CYP2C9 . The hydroxy metabolite, while active, contributes only marginally to the overall effect.

Elimination

Elimination is 58% renal and 35% via the faeces. The clearance is quite low at 48 ml/min. Only a very small proportion of the active substance (< 1%) is eliminated unchanged. The half-life is 5 to 8 hours, but the pancreatic beta cells can only be addressed again after some time after maximum stimulation.

Dosage of Amaryl (Glimepirid)

The dosage of glimepiride depends on the results of blood and urine sugar determinations of the patients. The tablets are swallowed whole with some liquid once a day. The administration takes place immediately before or with the first main meal. The dosage of glimepiride depends on the results of the blood and urine sugar determinations of the patient. The tablets are swallowed whole with some liquid once a day. The dose is given immediately before or with the first main meal.

Usually the starting dose is 1 mg glimepiride daily. If the metabolism cannot be satisfactorily adjusted with this, the dose is gradually increased. An increase to 2, 3 or 4 mg glimepiride per day is possible within one to two weeks. The recommended maximum dose is 6 mg daily, an improved effect can only be achieved with high doses in individual cases.

If the metabolism cannot be adequately adjusted with glimepiride, insulin can also be administered under strict medical supervision. The glimepiride dose remains the same and the insulin dose is adjusted accordingly.

If glimepiride is used in combination with metformin, the metformin dose is maintained while the glimepiride dose is slowly increased to the maximum.

A dose adjustment of glimepiride may also be necessary in the following cases:

  • Changed weight
  • Changes in lifestyle that favor hyper- or hypoglycemia
  • Long-term glimepiride therapy, since an improvement in the metabolic status with increased insulin sensitivity is possible with glimepiride

Side effects of Amaryl (Glimepirid)

The following side effects may occur rarely (≥ 1/10,000 to < 1/1,000) during therapy with glimepiride:

  • Taste disturbances, gastrointestinal complaints
  • Increased appetite and weight gain
  • hair loss
  • Hypoglycemia, especially in elderly patients and alcohol abuse
  • Blood disorders such as leukpenia, thrombocytopenia, granulocytopenia, agranulocytosis, erythropenia, haemolytic anemia and pancytopenia 

Interactions

Numerous interactions are possible in therapy with glimepiride. For example, the effective levels can be influenced by CYP2C9 inhibitors such as fluconazole (AUC increased approximately 2-fold) or inducers such as rifampicin . Patients with glucose-6-phosphate dehydrogenase deficiency are at risk of hemolytic anemia.

The following active substances can increase the blood sugar-lowering effect of glimepiride and thus lead to an increased risk of hypoglycaemia:

  • Phenylbutazone , Azapropazone , Oxyphenbutazone
  • Insulin and oral antidiabetics
  • salicylates and p-aminosalicylates
  • Anabolic steroids and male sex hormones
  • chloramphenicol , long-acting sulfonamides, tetracyclines , quinolone antibiotics, clarithromycin
  • Vitamin K antagonists
  • fenfluramine
  • disopyramid
  • fibrates
  • ACE inhibitors
  • Fluoxetine , MAO inhibitor
  • allopurinol , probenecid , sulfinpyrazone
  • sympatholytics
  • cyclophosphamide , trofosfamide , ifosfamide
  • miconazole , fluconazole
  • Pentoxifylline (high dose parenteral)
  • tritoqualine

The following active substances can weaken the blood-sugar-lowering effect of glimepiride and thus lead to increased blood-sugar levels

  • estrogens and progestins
  • Saluretics, thiazide diuretics , acetazolamide
  • Thyroid stimulating agents, glucocorticoids
  • phenothiazine derivatives, chlorpromazine
  • Adrenaline, sympathomimetics
  • Nicotinic acid (high dose) and derivatives
  • Laxatives (for long-term use)
  • phenytoin , diazoxide
  • glucagon , barbiturates, rifampicin

Alcohol, H2 antagonists , beta- blockers , clonidine and reserpine can either increase or decrease the hypoglycaemic effect.

Sympatholytics such as beta-blockers, clonidine, guanethidine and reserpine can suppress signs of adrenergic hypoglycemia counter-regulation.

 

Contraindications

The following contraindications should be noted when treating with glimepiride:

  • Hypersensitivity to glimepiride, other sulfonylureas or sulfonamides
  • Type 1 diabetes mellitus
  • diabetic coma
  • ketoacidosis
  • Severe kidney and liver dysfunction
  • pregnancy and lactation

Pregnancy

There are no adequate data on the use of glimepiride in pregnant women. Animal experiments have shown evidence of reproductive toxicity, which is probably related to the hypoglycaemic effect. Since untreated diabetes during pregnancy increases the teratogenic risk, a switch from glimepiride to insulin should take place.

 

Lactation

There is a high probability that glimepiride passes into breast milk and there is therefore a risk of hypoglycaemia in the infant. On the one hand, this could be shown in rats, on the other hand, other sulfonylureas are also excreted in breast milk. Therefore, breast-feeding is not recommended during therapy with glimepiride.

 

Driving ability

Patients with frequent episodes of hypoglycaemia should be advised to take precautions when driving, as hypoglycaemia may reduce concentration and responsiveness.

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Additional information

Dosage

2 mg, 4 mg

Quantity

30, 60, 90, 120, 180

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