0Drugs | Leading Online Medicine Index & Healthcare Portal

Generic Name

Sitagliptin + Metformin Hydrochloride
Therapeutic Class: Anti Diabetic

Indications:
Sitagliptin + Metformin HCl is a dipeptidyl peptidase-4 (DPP-4) inhibitor and biguanide combination product indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus when treatment with both Sitagliptin and Metformin extended-release is appropriate.

Presentation:
Sitagliptin + Metformin HCl 50/500 : Each extended-release tablet contains Sitagliptin Phosphate Monohydrate INN 64.25 mg eq. to Sitagliptin 50mg & Metformin HCl BP 500 mg.
Sitagliptin + Metformin HCl 50/1000 : Each extended-release tablet contains Sitagliptin Phosphate Monohydrate INN 64.25 mg eq. to Sitagliptin 50 mg & Metformin HCl BP 1000 mg.

Description:
Sitagliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor, which exerts its action by slowing the inactivation of incretin hormones. Incretin hormones, including glucagon-like peptide-1(GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), are released by the intestine throughout the day and levels are increased in response to a meal. These hormones are rapidly inactivated by the enzyme, DPP-4. The incretins are part of an endogenous system involved in the physiologic regulation of glucose homeostasis. When blood glucose concentrations are normal or elevated, GLP-1 and GIP increase insulin synthesis and release from pancreatic beta cells by intracellular signalling pathways involving cyclic AMP. GLP-1 also lowers glucagon secretion from pancreatic alpha cells, leading to reduced hepatic glucose production. The pharmacologic mechanism of action of Metformin is different from other classes of oral antihyperglycemic agents. Metformin decreases hepatic glucose production, decreases intestinal absorption of glucose, and increases peripheral glucose uptake and utilization.

Dosage & Administration:
May adjust the dosing based on effectiveness and tolerability while not exceeding the maximum recommended daily dose of 100 mg Sitagliptin and 2000 mg Metformin extended-release.
Administer once daily with a meal preferably in the evening. Gradually escalate the dose to reduce the gastrointestinal side effects due to Metformin. Maintain the same total daily dose of Sitagliptin and Metformin when changing between Sitagliptin + Metformin HCl, without exceeding the maximum recommended daily dose of 2000 mg Metformin extended-release.
Swallow whole. Never split, crush or chew.

Side Effects:

• The most common adverse reactions reported in ≥5% of patients simultaneously started on Sitagliptin and Metformin and more commonly than in patients treated with placebo were diarrhoea, upper respiratory tract infection, and headache.
•  Adverse reactions reported in ≥5% of patients treated with Sitagliptin in combination with Sulfonylurea and Metformin and more commonly than in patients treated with placebo in combination with Sulfonylurea and Metformin were hypoglycemia and headache.
• Hypoglycemia was the only adverse reaction reported in ≥5% of patients treated with Sitagliptin in combination with insulin and Metformin and more commonly than in patients treated with placebo in combination with insulin and Metformin.

Precautions:
Do not use the combination of Sitagliptin + Metformin HCl in patients with hepatic disease. Before initiating the combination and at least annually thereafter, assess renal function and verify as normal. May need to discontinue the combination and temporarily use insulin during periods of stress and decreased intakes of fluids and food, such as fever, trauma, infection, or surgery.

Use in Pregnancy & Lactation:

• There are no adequate and well-controlled studies in pregnant women with Sitagliptin + Metformin HCl or its individual components; therefore, the safety of Sitagliptin + Metformin HCl in pregnant women is not known. Sitagliptin + Metformin HCl should be used during pregnancy only if clearly needed.
• It is not known whether Sitagliptin or Metformin are excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Sitagliptin + Metformin HCl is administered to a nursing woman.

Interaction:
Carbonic anhydrase inhibitors should be used with caution treated with Sitagliptin + Metformin HCl, as the risk of lactic acidosis may increase.
Careful patient monitoring and dose adjustment of Sitagliptin + Metformin HCl and/or the interfering drug are recommended in patients taking cationic medications that are excreted via the proximal renal tubular secretory system.

Overdose:
Sitagliptin
There is no experience with doses above 800 mg in clinical studies. In the event of an overdose, it is reasonable to employ the usual supportive measures, e.g., remove unabsorbed material from the gastrointestinal tract, employ clinical monitoring (including obtaining an electrocardiogram), and institute supportive therapy as indicated by the patient's clinical status.
Prolonged hemodialysis may be considered if clinically appropriate. It is not known if sitagliptin is dialyzable by peritoneal dialysis.
Metformin Hydrochloride
Overdose of Metformin Hydrochloride has occurred, including ingestion of amounts greater than 50 grams. Hypoglycemia was reported in approximately 10% of cases, but no causal association with Metformin Hydrochloride has been established. Lactic acidosis has been reported in approximately 32% of Metformin overdose cases. Hemodialysis may be useful for the removal of accumulated drug from patients in whom Metformin overdose is suspected.

Storage:

Store in a cool and dry place. Protect from light and moisture. Keep out of the reach of children