Amynil stimulates the insulin release from pancreatic β-cells and reduces glucose output from the liver. It also increases insulin sensitivity at peripheral target sites.
Amynil is used for an adjunct to diet to lower the blood glucose in patients with non-insulin-dependent diabetes mellitus (type 2 diabetes) whose hyperglycemia cannot be controlled by diet, physical exercise and weight reduction.
Amynil is also used for use in combination with Insulin to lower blood glucose in patients whose hyperglycaemia can not be controlled by diet and exercise or in conjunction with an oral hypoglycaemic agent.
Amynil is also used to associated treatment for these conditions: Type 2 Diabetes Mellitus
|Glimepiride Other Names||Glimepirida, Glimépiride, Glimepiride, Glimepiridum|
|Weight||1 mg, 2mg|
Plasma protein binding of glimepiride is greater than 99.5%.
|Manufacturer||Globex Pharmaceuticals Ltd|
|Last Updated:||June 23, 2021 at 11:21 am|
In principle, the dosage of Amynil is governed by the desired blood sugar level. The dosage of Amynil must be the lowest which is sufficient to achieve the desired metabolic control.
The initial and the maintenance doses are set based on the results of regular checking of glucose in blood and urine. Monitoring of glucose levels in blood and urine also serves to detect either primary or secondary failure of therapy.
Initial dose and dose titration: Usual initial dose is 1 mg once daily. If necessary, the daily dose can be increased. Any increase can be based on regular blood sugar monitoring, and should be gradual, i.e., at intervals of one to two weeks and carried out step wise at follows: 1 mg-2 mg-3 mg-4 mg-6 mg.
Dose range in patients with well controlled diabetes: Usual dose range in patients with well controlled diabetes is 1 to 4 mg daily.
Distribution of doses: Timing and distribution of doses are decided by the physician, in consideration of the patient's current life style. Normally, a single daily dose is sufficient. This should be taken immediately before a substantial breakfast or - if none is taken - immediately before the first main meals. It is very important not to skip meals after taking the drug.
Secondary dosage adjustment: As the control of diabetes improves, sensitivity to insulin increases; therefore, Amynil requirement may fall as treatment proceeds. To avoid hypoglycaemia, timely dose reduction or cessation of Amynil therapy must be considered.A dose adjustment must also be considered whenever the patient's weight or life style changes, or other factors arise which cause an increased susceptibility to hypo- or hyperglycaemia.
Changeover from other oral antidiabetics to Amynil: There is no exact dosage relationship between Amynil and other oral blood sugar lowering agents. When substituting Glimepride for other such agents, the initial daily dose is 1 mg; this applies even in changeover from the maximum dose of other oral blood sugar lowering agents. Any dose increase should be in accordance with guideline given above in initial dose and dose titration.
Consideration must be given to the potency and duration of action of the previous blood sugar lowering agent. It may be necessary to interrupt treatment to avoid additive effects which would increase the risk of hypoglycaemia.
Diaryl tablet must be swallowed without chewing and with sufficient amount of liquid (approximately ½ glass).
Hypoglycaemia, temporary visual impairment, nausea, vomiting, diarrhoea, abdominal pain, urticaria & fall in blood pressure.
In the initial weeks of treatment, the risk of hypoglycaemia may be increased and necessitates careful monitoring. If such risk is present it may be necessary to adjust the dosage of Amynil. Hypoglycaemia can almost always be promptly controlled by immediate intake of carbohydrates (glucose or sugar, e.g., sugar sweetened fruit juice or sugar sweetened tea)
Potentiation of the blood-sugar-lowering effect may occur with Insulin and other oral anti-diabetics, ACE inhibitors, Allopurinol, anabolic steroids and male sex hormones, Chloramphenicol, coumarin derivatives, Fluoxetine, MAO inhibitors, Miconazole, Para-aminosalicyclic acid, Pentoxifylline (high dose parenteral), Phenylbutazone, Oxyphenbutazone, quinolones, salicylates, sulphonamides, tetracyclines, β blockers.
Weakening of the blood-sugar-lowering effect may occur with Acetazolamide, barbiturates, corticosteroids, Diazoxide, diuretics, Epinephrine and other sympathomimetic agents, laxative, oestrogens and progestogens, phenothiazines, Phenytoin, Rifampicin, and thyroid hormones.
H2 -receptor antagonists, Clonidine and Reserpine may lead to either potentiation or weakening of the blood-sugar-lowering effect.
Both acute and chronic alcohol intake may potentiate or weaken the blood-sugar-lowering action of Amynil unpredictably.
- Avoid alcohol. Acute and chronic alcohol intake may unpredictably affect the glucose-lowering action of glimepiride.
- Take with food. The manufacturer recommends administration with the first meal of the day.
Volume of Distribution
Following intravenous dosing in healthy subjects, the volume of distribution was 8.8 L (113 mL/kg).
The elimination half-life of glimepiride is approximately 5 to 8 hours, which can increase up to 9 hours following multiple doses.
A single-dose, crossover, dose-proportionality (1, 2, 4, and 8 mg) study in normal subjects and from a single- and multiple-dose, parallel, dose proportionality (4 and 8 mg) study in patients with type 2 diabetes (T2D) were performed. In these studies, the total body clearance was 52.1 +/- 16.0 mL/min, 48.5 +/- 29.3 mL/min in patients with T2D given a single oral dose, and 52.7 +/- 40.3 mL/min in patients with T2D given multiple oral doses. Following intravenous dosing in healthy subjects, the total body clearance was 47.8 mL/min.
Pregnancy & Breastfeeding use
Pregnancy: Amynil must not be taken during pregnancy; a changeover to Insulin is necessary. Patients planning a pregnancy must inform their physician, and should be shifted to Insulin.
Lactation: Ingestion of Amynil with breast milk may harm the child. Therefore, Amynil must not be taken by lactating women. Either a changeover or a complete discontinuation of breast-feeding is necessary.
Amynil is not suitable for the treatment of insulin dependent (type-I) diabetes mellitus, or of diabetic pre-coma or coma. Amynil must not be used in patients hypersensitive to Amynil or other sulphonylureas.
Pediatric use: Safety and effectiveness in pediatric patients have not been established.
Geriatric use: No overall differences in safety or effectiveness were observed between elderly and adult subjects, but greater sensitivity of some older individuals cannot be ruled out. The drug is known to be substantially excreted by the kidney, and the risk of toxic reactions to this drug may be greater in patients with impaired renal function. Because elderly patients are more likely to have decreased renal function, care should be taken in dose selection, and it may be useful to monitor renal function.
Use in renal insufficiency: A starting dose of 1 mg glimepiride may be given to NIDDM patients with kidney disease, and the dose may be titrated based on fasting blood glucose levels.
Use in hepatic insufficiency: No studies were performed in patients with hepatic insufficiency. Adverse reactions: Hypoglycemia. Adverse events, other than hypoglycemia, are dizzines, asthenia, headache, and nausea.
Accidental or intentional overdose may cause severe and prolonged hypoglycemia which may be life-threatening. In case of overdosage with Amynil, a doctor must be notified immediately. At the first signs of hypoglycemia, the patient must immediately take sugar, preferably glucose, unless a doctor has already started care.
Store at 25° C.