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Description
It contains; sitagliptin and metformin. Sitagliptin, an orally-active inhibitor of the dipeptidyl peptidase-4 (DPP-4) enzyme, used as an oral hypoglycemic agent in Type II diabetes mellitus. Dipeptidyl peptidase-4 (DPP-4) is an enzyme that acts to inactivate glucagon like peptide-1(GLP-1). When sitagliptin inhibits DPP-4 then levels of GLP-1 will increase that results in increased insulin release from the body after taking meals and in this way glucose tolerance by the body will increase. For adult patients with type 2 diabetes mellitus, sitagliptin is indicated to improve glycemic control as an adjunct to diet and exercise. Used in patients that show inadequate glycemic control by diet and exercise alone and for whom metformin is inappropriate due to contraindications or intolerance. Metformin (N, N-dimethylbiguanide) belongs to the biguanide class of antidiabetic drugs (containing two linked guanidine rings). This drug has a major clinical advantage that it does not induce hypoglycemia or weight gain with remarkable cardiovascular safety. Metformin is also used for the treatment of polycystic ovary disease, diabetic nephropathy, and gestational diabetes. Metformin acts via both AMP-activated protein kinase (AMPK)-dependent and AMPK-independent mechanisms; by inhibiting mitochondrial respiration and inhibiting mitochondrial glycerophosphate dehydrogenase, and a mechanism involving the lysosome. Metformin acts directly or indirectly on the liver in order to reduce glucose production, and acts on the gut to increase glucose utilization. At the molecular level, metformin acts to inhibit the mitochondrial respiratory chain in the liver, which results in activation of AMPK, enhances insulin sensitivity (via effects on fat metabolism) and lowers cAMP, and reduces the expression of gluconeogenic enzymes. Metformin shows AMPK-independent effects on the liver that results in inhibition of fructose-1,6-bisphosphatase by AMP.
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Ingredients
Metformin, Sitagliptin
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Dosage Form
Tablet
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Uses
Diabetes Type 2
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Dosage
Dose must be taken according to the doctor’s advice only; doses given below are suggested as supportive literature for better understanding in some areas of requirements. Adult dose: For patients who were previously taking metformin alone: 100mg sitagliptin along with previously taken dose of metformin once in a day. If a patient was taking 850mg or 1000mg of metformin daily then he may start with taking 50mg of sitagliptin and 850mg or 1000mg of metformin. The formulation of tablets in this case should be; 50mg(sitagliptin)/850mg(metformin) or 50mg(sitagliptin)/1000mg(metformin) per day. The dose should be not more than 100mg sitagliptin and 2000mg metformin daily. For the patient who was previously taking sitagliptin alone: he may start with 100mg of sitagliptin and 1000mg of metformin once a day. The dose should be not more than 100mg sitagliptin and 2000mg metformin daily.
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In case of Overdose
In case of overdose with this drug consult your doctor first, he may take the usual supportive measures, e.g., he may remove unabsorbed material from the gastrointestinal tract, employ clinical monitoring and take supportive therapy as dictated by the patient's clinical status. Sitagliptin is modestly dialyzable. It is not known if Sitagliptin can be dialyzable by peritoneal dialysis or not. Metformin overdose can cause hypotension.
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Missed Dose
In case you missed any dose, take the next dose as soon as you remember, but don't double your next dose to compensate for the missed one.
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How To Use
Take it orally as advised by the physician.
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When Not to Use
Do not use it in case of hypersensitivity to Sitagliptin. Not suitable for use in type I diabetes mellitus or for the treatment of diabetic ketoacidosis. Metformin should not be used in case of hypersensitivity to the drug, metabolic acidosis, chronic heart, failure, myocardial infarction, diabetic ketoacidosis, severe renal disease, abnormal creatinine clearance resulting from shock, septicemia and lactation.
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Side Effects
Hypersensitivity Reactions Hypoglycemia Headache Dizziness Constipation Vomiting Acute Pancreatitis Pruritus Angioedema Rash Urticaria Cutaneous Vasculitis Exfoliative Skin Conditions Myalgia Back Pain Arthropathy.
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Precautions & Warnings
After initiation of Sitagliptin, patients should be observed carefully for signs and symptoms of pancreatitis (inflammation of pancreas). If pancreatitis is suspected, Sitagliptin should promptly be discontinued and appropriate management should be initiated. Assess renal function prior to initiation of this drug. If metformin-associated lactic acidosis is suspected, general supportive measures should be taken in a hospital setting, along with immediate discontinuation of this medicine.
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Food Interactions
Do not use grapefruit with sitagliptin or metformin. Taking grapefruit along with this medicine could increase the accumulation of metformin in the liver and in result increases the risk of lactic acidosis. Taking metformin with a meal can reduce the chances of developing an upset stomach or gastric discomfort.
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Storage/Disposal
If you are diabetic, go for the following tests: Glucose Tolerance Test, Blood sugar test, Blood Glucose Fasting Test