TENEBLU Film-coated tablet Ref.[51008] Active ingredients: Teneligliptin

General

Teneligliptin is not a substitute for insulin in insulin-requiring patients. Teneligliptin should not be used in patients with type 1 diabetes or for the treatment of diabetic ketoacidosis.

Hypoglycaemia

Sulphonylureas such as gliclazide, glipizide, or glimepiride are known to cause hypoglycaemia. Patients receiving teneligliptin in combination with a sulphonylurea may be at risk for hypoglycaemia. Therefore, a lower dose of sulphonylurea may be considered to reduce the risk of hypoglycaemia.

Hypoglycemia may also occur in patients with adrenal insufficiency, malnutrition, starved state, irregular dietary intake, insufficient dietary intake or hyposthenia, vigorous muscular movement, or in patient with excessive alcohol consumption.

Pancreatitis

Acute pancreatitis has been observed in post marketing studies. Further, acute pancreatitis is also reported with similar molecules such as vildagliptin. Thus, teneligliptin should not be used in patients with history of acute pancreatitis. In case a patient develops acute pancreatitis, teneligliptin should be immediately discontinued and consult treating physician.

Hepatic Impairment

Teneligliptin should be administered with caution in patient with severe hepatic dysfunction as safety has not been established in these patients.

Heart Failure

Teneligliptin should be administered with caution in patient with heart failure (NYHA class III-IV) as there is no usage experience and safety has not been established.

Abdominal Surgery

Use teneligliptin with caution in patient with history of abdominal surgery or intestinal obstruction as there is risk of intestinal obstruction.

QT Prolongation

QT prolongation may occur in patients having arrhythmia such as severe bradycardia or having its history, patient having heart disease such as congestive heart failure, and patient having hypokalemia.

Arthralgia

There have been post marketing reports of severe and disabling arthralgia in patients taking DPP-4 inhibitors. The time to onset of symptoms following initiation of drug therapy varied from one day to years. Patients experienced relief of symptoms upon discontinuation of the medication. A subset of patients experienced a recurrence of symptoms when restarting the same drug or a different DPP-4 inhibitor. Consider DPP-4 inhibitors as a possible cause for severe joint pain and discontinue drug if appropriate.

Ketoconazole

Teneligliptin is metabolized by CYP3A4 and is a weak substrate of P-glycoprotein. Ketoconazole is an inhibitor of CYP3A4 and P-glycoprotein. Exposure to teneligliptin, when administered in combination with ketoconazole, was less than twice the exposure to teneligliptin alone, which suggests that drugs that inhibit CYP3A4 (such as ketoconazole) are unlikely to increase the teneligliptin concentration in the plasma. Thus, teneligliptin can be administered with ketoconazole.

Antidiabetic Drugs

No clinically relevant drug-drug interactions were observed when teneligliptin was co-administered with metformin, canagliflozin, glimepiride, or pioglitazone in healthy volunteers; therefore, no dose adjustment of teneligliptin is required when it is coadministered with these drugs. Furthermore, teneligliptin did not affect the pharmacokinetic properties of metformin, canagliflozin, glimepiride, or pioglitazone.

Drugs Affecting Glycemic Control

Teneligliptin should be used with caution with drugs that can enhance the blood glucose lowering effect (e.g., β-blockers, MAO inhibitors, etc.) or attenuate the blood glucose lowering effect (like steroids, thyroid hormones, etc.).

No studies on the effects on the ability to drive and use machines have been performed. Patients who experience dizziness as an adverse reaction should avoid driving vehicles or using machines. Further, patients should be cautioned about the risk of hypoglycaemia especially when teneligliptin is co-administered with sulphonylurea and/or insulin.

The most common adverse reactions reported with teneligliptin are hypoglycemia and constipation. Other adverse reactions reported with the use of teneligliptin may include:

General: Fatigue, headache, dizziness, pyrexia.

Gastrointestinal Disorders: Intestinal obstruction, abdominal bloating, abdominal discomfort, nausea, vomiting, abdominal pain, flatulence, stomatitis, gastric polyps, colon polyps, duodenal ulcer, reflux esophagitis, diarrhea, loss of appetite, acute pancreatitis.

Liver: Increased AST (SGOT), increased ALT (SGPT), and increased γ-GTP

Kidney and Urinary System: Proteinuria, positive ketone bodies in urine.

Skin and Subcutaneous Tissue Disorders: Eczema, rash, itching, allergic dermatitis.

Respiratory System: Allergic rhinitis, nasopharyngitis, pneumonia.

Laboratory Investigations: Increase in serum levels of one or more of the followingamylase, lipase, CPK, potassium, uric acid.

None known.

The safety of teneligliptin in pregnant women has not been established. Teneligliptin should be used in pregnant women or in women who may possibly be pregnant only if the expected therapeutic benefits outweigh the possible risks associated with treatment.

It is unknown whether teneligliptin is excreted in human milk. But, animal studies (rat) have shown excretion of teneligliptin in milk. Thus, breast-feeding must be discontinued during administration of this product in lactating women.

Safety and efficacy of teneligliptin in children and adolescents have not been established. Thus, TENEBLU Tablets are not recommended for use in paediatric patients.

Dose adjustments are usually not necessary for elderly patients. But, as elderly patients often have physiological hypofunction, teneligliptin should be administered with caution in them.

As determined from the pharmacokinetic characteristics of teneligliptin, the extent of increase in the exposure level of teneligliptin in patients with renal impairment will not pose any significant safety risk. Teneligliptin can be used in diabetes patients with renal impairment, including those on hemodialysis, without the need for dose adjustment.

As determined from the pharmacokinetic characteristics of teneligliptin, the extent of increase in the exposure level of teneligliptin in patients with mild to moderate hepatic impairment will not pose any significant safety risk. Thus, no dose adjustment is recommended in mild to moderate hepatic impaired patients. There is no clinical experience of using teneligliptin in severe hepatic dysfunction patients.