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This three oral anti-hyperglycemic drugs glimepiride, pioglitazone and metformin hydrochloride used in the management of type-2 diabetes (NIDDM).

Glimepiride:

The primary mechanism of action of glimepiride in lowering blood glucose appears to be dependent on stimulating the release of insulin from functioning pancreatic beta cells.

Pioglitazone :

selectively stimulates the nuclear receptor peroxisome proliferatoractivated receptor gamma and to a lesser extent alpha. It modulates the transcription of the insulin-sensitive genes involved in the control of glucose and lipid metabolism in the muscle, adipose tissue, and the liver. As a result, pioglitazone reduces insulin resistance in the liver and peripheral tissues; increases the expense of insulin-dependent glucose; decreases withdrawal of glucose from the liver; reduces quantity of glucose, insulin and glycated haemoglobin in the bloodstream.

Metformin :

It decreases hepatic glucose production, decreases intestinal absorption of glucose, and improves insulin sensitivity by increasing peripheral glucose uptake and utilization. The combination of glimepiride, pioglitazone and metformin sustained-release complements each other and provides better glycemic control in the management of type-2 diabetes and probably in the prevention of its associated macrovascular and microvascular complications.

MK Medicine is a leading pcd franchise provider, contract manufacturer and hospital supplier of WHO-GMP certified Glimepiride 1 mg Metformin 500 mg (SR) Pioglitazone 15 mg Tablet

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Monitoring of renal function :

Metformin is known to be substantially excreted by the kidney and the risk of metformin accumulation and lactic acidosis increases with the degree of impairment of renal function. Thus, patients with serum creatinine levels above the upper limit of normal for their age should not receive this tablet. Before initiation of therapy with this tablet and at least annually thereafter, renal function should be assessed. this tablet should be discontinued if there is evidence of renal impairment.

Use of intravascular iodinated contrast materials:

Radiologic studies involving the use of intravascular iodinated contrast materials (for example, intravenous urogram, intravenous cholangiography, angiography, and computed tomography (CT) scans with intravascular contrast materials) can lead to  acute alteration of renal function and have been associated with lactic acidosis in patients receiving metformin. Therefore, in patients in whom any such study is planned, this tablet should be temporarily discontinued at the time of or prior to the procedure, and withheld for 48 hours subsequent to the procedure and reinstituted only after renal function has been re-evaluated and found to be normal.

Alcohol intake :

Alcohol is known to potentiate the effect of metformin on lactate metabolism. Patients, therefore, should be warned against excessive alcohol intake, acute or chronic, while receiving metformin.

Congestive Heart Failure & other cardiac effects :

Thiazolidinediones, including pioglitazone, which is a component of this tablet, can cause fluid retention in some patients when used alone or in combination with other antidiabetic agents, including insulin. Fluid retention may lead to or exacerbate heart failure. The administration of oral hypoglycemic drugs (tolbutamide) has been reported to be associated with increased cardiovascular mortality as compared to treatment with diet alone or diet plus insulin. In view of close similarities between the oral hypoglycemic drugs, this warning also applies for glimepiride. After initiation of this tablet, and after dose increases, observe patients carefully for signs and symptoms of heart failure (including excessive, rapid weight gain, dyspnea, and/or edema). Heart failure should be managed according to the current standards of care and discontinuation or dose reduction of this tablet must be considered.

Lactic acidosis :

Lactic acidosis is a rare, but serious, metabolic complication that can occur due to metformin accumulation when used alone or in combination with other antihyperglycemic agents; when it occurs, it is fatal in approximately 50% of cases. When metformin is implicated as the cause of lactic acidosis, metformin plasma levels >5 μg/mL are generally found. The reported incidence of lactic acidosis in patients receiving metformin hydrochloride is very low (approximately 0.03 cases/1000 patient-years, with approximately 0.015 fatal cases/1000 patient years). Reported cases have occurred primarily in diabetic patients with significant renal insufficiency often in the setting of multiple concomitant medical/surgical problems and multiple concomitant medications. Patients with congestive heart failure requiring pharmacologic management, in particular those with unstable or acute congestive heart failure who are at risk of hypoperfusion and hypoxemia, are at increased risk of lactic acidosis. Lactic acidosis is a medical emergency that must be treated in a hospital setting. In a patient with lactic acidosis, metformin should be discontinued immediately and general supportive measures promptly instituted. Because metformin hydrochloride is dialyzable, prompt hemodialysis is recommended to correct the acidosis and remove the accumulated metformin.

Hepatic Effects :

In postmarketing experience with pioglitazone, reports of hepatitis and of hepatic enzyme elevations have been received. Very rarely, these reports have involved hepatic failure with and without fatal outcome, although causality has not been established. Hence it is recommended that patients treated with this tablet undergo periodic monitoring of liver enzymes.
The decision whether to continue the patient on therapy with this tablet should be guided by clinical judgment pending laboratory evaluations.

Hypoxic states :

Cardiovascular collapse (shock) from whatever cause, acute congestive heart failure, acute myocardial infarction and other conditions characterized by hypoxemia have been associated with lactic acidosis and may also cause prerenal azotemia. When such events occur in patients receiving this tablet therapy, the drug should be promptly discontinued.

 

Glimepiride:

After oral administration, glimepiride is completely absorbed from the GI tract. Studies have shown significant absorption of glimepiride within 1 hour after administration and peak drug levels (Cmax) at 2 to 3 hours. When glimepiride was given with meals, the mean Tmax (time to reach Cmax) was slightly increased (12%) and the mean Cmax and AUC (area under the curve) were slightly decreased (8% and 9%, respectively).

Pioglitazone:

Following oral administration, in the fasting state, pioglitazone is first measurable in serum within 30 minutes, with peak concentrations observed within 2 hours. Food slightly delays the time to peak serum concentration [3 to 4 hours], but does not alter the extent of absorption.

Metformin sustained release:

The absolute bioavailability of a metformin 500-mg tablet given under fasting conditions is approximately 50-60%. Following a single oral dose of metformin sustained-release, Cmax is achieved within 4-8 hours. Peak plasma levels are approximately 20% lower compared to the same dose of metformin immediate release, however, the extent of absorption (as measured by AUC) is similar to immediate release. Both high and low fat meals had the same effect on the pharmacokinetics of extended release.

Important Notice:- The Database is still under development and may contain inaccuracies. It is not intended as a substitute for the expertise and judgement of your physician, pharmacist or other healthcare professional. It should not be construed to indicate that the use of any medication in any country is safe, appropriate or effective for you. Consult with your healthcare professional before taking any medication.