New Antidiabetes Oral

Posted by: rizkyp13 on: Januari 18, 2009

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Sitagliptin (INN; previously identified as MK-0431, trade name Januvia) is an oral antihyperglycemic (anti-diabetic drug) of the dipeptidyl peptidase-4 (DPP-4) inhibitor class, Sitagliptin being the only 2nd Generation DPP4 inhibitor currently available. This enzyme-inhibiting drug is used either alone or in combination with other oral antihyperglycemic agents (such as metformin or a thiazolidinedione) for treatment of diabetes mellitus type 2. The benefit of this medicine is its lower side-effects (e.g., less hypoglycemia, less weight gain) in the control of blood glucose values. Exenatide/Byetta is an alternative drug that also works with the incretin system.

Adverse effects
In clinical trials, adverse effects were as common with sitagliptin (whether used alone or with metformin or pioglitazone) as they were with placebo, except for extremely rare nausea and common cold-like symptoms..[2] There is no significant difference in the occurrence of hypoglycemia between placebo and sitagliptin.[2]

History
Sitagliptin was approved by the U.S. Food and Drug Administration (FDA) on October 17, 2006[3] and is marketed in the US as Januvia by Merck & Co. On April 2, 2007, the FDA approved an oral combination of sitagliptin and metformin marketed in the US as Janumet.

Mechanism

See also: Dipeptidyl peptidase-4 inhibitors

Sitagliptin works to competitively inhibit the enzyme dipeptidyl peptidase 4 (DPP-4). This enzyme breaks down the incretins GLP-1 and GIP, gastrointestinal hormones that are released in response to a meal.[4] By preventing GLP-1 and GIP inactivation, GLP-1 and GIP are able to potentiate the secretion of insulin and suppress the release of glucagon by the pancreas. This drives blood glucose levels towards normal. As the blood glucose level approaches normal, the amounts of insulin released and glucagon suppressed diminishes thus tending to prevent an “overshoot” and subsequent low blood sugar (hypoglycemia) which is seen with some other oral hypoglycemic agents.

Source : wikipedia.org