Teneligliptin tablets are considered as a monotherapy in addition to serious diet and exercise to improve glycemic control in adults having type II diabetes mellitus(T2DM).
Composition:
Each Teneligliptin Hemipentahydrobromide Hydrate film-coated tablet containsTeneligliptin Hemipentahydrobromide Hydrate equivalent to 20 mg Teneligliptin and qs excipents.
It is an orally-active inhibitor of the dipeptidyl peptidase (DPP – 4) enzyme. Its chemical name is {(2S,4S)-4-[4-(3-Methyl-1-phenyl-1H-pyrazol-5-yl) piperazin-1-yl] pyrrolidin-2-yl} (1,3-thiazolidin-3-yl) methanone hemipentahydrobromide hydrate and molecular formula is C22H30N6OS.2½HBr.xH2O and its molecular weight is 628.86.
Teneligliptin is a DPP – 4 inhibitor which is known to exert its actions in patients suffering form type II diabetes by slowing the inactivation of incretin hormones and increasing concentration of active intact hormones and thereby prolonging the action of these hormones. These hormones are rapidly inactivated by the enzyme, DPP-4.
The incretins are component of an endogenous system that is included in the physiologic regulation of glucose homeostasis. When blood glucose concentrations are normal or elevated, insulin synthesis is increased by GLP-1 & GIP and they release from pancreatic beta cells by intracellular signaling path that includes cyclic AMP. GLP-1 also lowers glucagon secretion from pancreatic alpha cells, which leads to decreased hepatic glucose production. By increasing active incretin levels, teneligliptin raises the insulin release and reduces glucagon levels in the circulation in a glucose-dependent way.
Teneligliptin in India is in the middle of the intense price war. India’s gliptin market is growing at around 60% annually where out of 68 million diabetics in India, around 1.85 million are on Gliptin therapy to manage the type II diabetes. So, manufacturers are on the run to decrease the prices of Teneligliptintablets.
Teneligliptin is contra-indicated with the following type of patients:
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If the patient is hypersensitive to teneligliptin or any components in the formulation.
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Patients with Type I diabetes, severe ketosis diabetic coma or history of diabetic coma.
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Patients with severe infection, surgery or severe trauma
Precautions and Warnings:
Teneligliptin tablets should be carefully administered in the patients having following problems:
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Advanced Liver failure
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Congestive heart failure
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Pituitary or Adrenal Insufficiency, Poor nutritional state, Starvation, irregular diet intake, intense muscle movement or excessive alcohol intake.
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Abdominal surgery or a history of bowel obstruction.
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Arryhthmia, severe bradycardia or its history, congestive heart failure or patients with low serum potassium, congenital prolonged QT syndrome
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Patients using insulin secretagogue
This drug should be taken cautiously with the drugs which can enhance blood glucose lowering effect such as steroids, thyroid hormones etc.
Reactions:
The most common reactions noticed with Teneligliptin are constipation and hypoglycemia. Other adverse reactions reported are as follows:
Kidney and Urinary system: Urine ketone-positive, Proteinuria
Gastrointestinal Disorders: Abdominal bloating, Intestinal obstruction, nausea, gastric polyps, stomatitis, flatulence, abdominal pain, colon polyps, duodenal ulcer, diarrhea, reflux esophagitis, loss of appetite, acute pancreatitis
Skin and Subcutaneous Tissue Disorders: Rash, Itching, Eczema, Allergic dermatitis
Investigations: Increase in ALT, AST, ALP and y-GTP
Others: Increased serum potassium, increased CPK, fatigue, allergic rhinitis, elevation of serum uric acid.
Usually, 20 mg of Teneligliptin dosage is advised orally once daily and in event of an overdose, it is recommended to employ the supportive measures like removing unabsorbed material from gastrointestinal tract and employing clinical monitoring of the patient.
