Teneligliptin + Metformin

Teneligliptin + Metformin is an Anti-diabetic Agent belonging to the pharmacological class of Dipeptidyl peptidase-4 (DPP-4) inhibitors and biguanides.

Teneligliptin+ Metformin has been approved as a treatment for type 2 diabetes mellitus, helping to control blood sugar levels blood sugar levels by stimulating insulin resistance and enhancing the body's response to insulin.

Teneligliptin is rapidly absorbed after oral administration. It undergoes minimal metabolism and is excreted primarily unchanged in the urine. Metformin is absorbed in the upper small intestine, doesn't undergo metabolism, and is excreted unchanged in the urine.

Teneligliptin + Metformin side effects commonly include diarrhoea, nausea, vomiting, upset stomach, and headache.

Teneligliptin + Metformin is available as a tablet for convenient administration.

Teneligliptin+ Metformin is available in India, the United States, Canada, the United Kingdom, Germany, France and Australia.

Teneligliptin + Metformin is an Anti-diabetic Agent belonging to the pharmacological class of Dipeptidyl peptidase-4 (DPP-4) inhibitors and biguanides.

Teneligliptin: Teneligliptin inhibits DPP-4, which slows down the inactivation of incretins such as GLP-1 and GIP. As part of glucose homeostasis, incretins are released throughout the day and are increased after meals. Depending on glucose concentrations, reduced inhibition of incretins boosts insulin production and decreases glucagon release. Reduced glycosylated haemoglobin (HbA1c) is one marker for how effectively blood glucose control is generally improved due to these effects.

Metformin: Metformin decreases hepatic glucose production, reduces glucose absorption in the intestine and improves insulin sensitivity (increases peripheral glucose uptake and utilization).

Synergistic Benefits: Metformin and Teneligliptin work synergistically to help manage type 2 diabetes. Metformin, also known as biguanide, works by reducing the amount of glucose that the liver can make, slowing down the absorption of glucose in the intestines, and increasing the body's sensitivity to insulin. A dipeptidyl peptidase-4 inhibitor called teneligliptin increases insulin release from the pancreas and decreases hormones that raise blood sugar. This reduces blood sugar levels after meals and during fasting. When combined, they provide better control of blood sugar.

Teneligliptin+ Metformin is available in oral tablets.

Tablets: To be swallowed whole with water/liquid. Do not chew, crush or break it.

As the physician recommends, take the medication orally once daily before meals or generally with a meal.

Teneligliptin+ Metformin can be used in the following health conditions:

Teneligliptin: Teneligliptin inhibits the dipeptidyl peptidase-4 (DPP-4) enzyme to be inhibited, which raises the levels of active incretin for longer. Incretin hormones, such as GLP-1 and GIP, increase insulin synthesis and release from the pancreatic beta cells and lower glucagon secretion from pancreatic alpha cells, hence regulating glucose homeostasis. Hepatic glucose synthesis is reduced when glucagon secretion is reduced. The DPP-4 enzyme rapidly inactivates incretin hormones, but under normal physiological conditions, the gut releases them throughout the day and releases more of them in response to a meal.

Metformin: Metformin improves glucose tolerance by lowering basal and postprandial plasma glucose. It exerts its effect by decreasing hepatic glucose production by inhibiting gluconeogenesis and glycogenolysis, delaying intestinal glucose absorption, and increasing insulin sensitivity by increasing peripheral glucose uptake and utilization.

It is advised to treat type 2 diabetes with teneligliptin with metformin in addition to a healthy diet and regular exercise. Patients for whom Metformin alone is not an efficient means of controlling their diabetes are prescribed Teneligliptin plus Metformin. This medication helps the body return to normal by increasing insulin sensitivity. It is especially recommended that metformin drugs be taken frequently so that the medication releases into the body progressively.

The combination should only be administered to patients who have not improved sufficiently with either of the following treatments:

Orally: Teneligliptin+ Metformin is available as a tablet that can be taken orally.

It is advised to administer once daily during breakfast or the first main meal and avoid breaking, crushing, dissolving, or chewing pills; swallow them whole with a glass of water. It is best to take it regularly at a fixed time each day following the physician's prescribed schedule for regular and evenly spaced intervals because the dose and duration of therapy are individualized per specific conditions to achieve the most effective and successful treatment outcome.

The dosage and duration of treatment should be as per the treating physician's clinical judgment.

Teneligliptin+ Metformin is available in the form of Oral tablets.

The recommended dose is one tablet PO once daily, with adjustments made based on response and tolerability, not exceeding the maximum daily dose of 40 mg Teneligliptin and 2000 mg Metformin Extended-Release.

Teneligliptin+ Metformin should be used in treating type 2 diabetes mellitus, along with appropriate dietary restrictions.

Teneligliptin+Metformin is usually taken with meals to lower the risk of gastrointestinal (GI) side effects and to ensure proper absorption.

Limit or avoid alcohol while taking Teneligliptin and Metformin, as alcohol can potentiate the risk of hypoglycemia (low blood sugar).

Limit foods like chips, crisps, pastries, biscuits, and samosas that contain saturated fat, often known as hidden consumption fats. For regular cooking, use oils high in omega-3 fatty acids. For frying, one can use safflower oil, rice bran oil, mustard oil, palm oil, and groundnut oil. For a healthier diet, selecting low-fat dairy products like fat-free milk, cheese, and yoghurt is also advised.

The dietary restriction should be individualized as per patient requirements.

Teneligliptin+ Metformin may be contraindicated under the following conditions:-

When an allergic reaction occurs, people may feel tightness in their chest, swelling, rashes on their skin, and hives, among other symptoms. It is only advisable to modify dosage with a medical provider's advice. The product should only be used by directions. Patients are counselled to follow a prescribed diet and partake in regular physical activity.

Patients should be informed about any warning signs and symptoms of hypoglycemia as well as appropriate treatment options. When using prescription or over-the-counter medications, herbal products or supplements, trying to conceive, breastfeeding, pregnancy, allergies, or other health conditions, caution is suggested. When taking Teneligliptin + Metformin, metformin accumulation can lead to lactic acidosis, a rare but metabolic severe condition.

The adverse reactions related to Teneligliptin+ Metformin can be categorized as:-

The clinically relevant drug interactions of Teneligliptin+ metformin are briefly summarized here:

The most common side effects of Teneligliptin+ Metformin include:

Teneligliptin+ Metformin should be prudent in the following group of special populations.

Category B pregnancy (FDA): Possibly acceptable. Research on animals has either not indicated any danger, but human studies have yet to be conducted, or research on animals has shown some risk but not human risk.

The use of teneligliptin and metformin combination therapy in pregnant women is not well-established enough. Unknown is the possible risk to humans. As such, this product should be used exclusively when necessary and only if the prospective benefit outweighs the potential risk to the developing fetus.

Teneligliptin excretion in human milk is unclear; however, metformin can be excreted in human milk in small concentrations. Excretion of both metformin and teneligliptin has been observed in milk from animal studies (rats). Some teneligliptin+Metformin combinations are not advised to be used while breastfeeding due to the possibility of neonatal hypoglycemia. Breastfeeding mothers should stop while this product is administered if medication therapy is required.

As per FDA, safety and effectiveness in the pediatric population have yet to be established.

For older patients, dose modifications are typically not required. Use this medication with caution in older individuals and routinely check their renal function because metformin is excreted through the kidney and tends to decrease renal function (physiological hypofunction).

Usually, a lower dose should be given to patients with poor renal function. Usually, there is no need to change the dose if the GFR is greater than 60 ml/min. Patients with a GFR of less than 30 milliliters per minute should refrain from taking metformin preparations.

Hepatic impairment: Contraindicated.

There have been reports of lactic acidosis in people treated with metformin who have hepatic impairment.

The physician should be vigilant about the knowledge pertaining to the identification and treatment of overdosage of Teneligliptin+ Metformin.

Overconsumption of Teneligliptin+ Metformin could lead to severe hypoglycemia (low blood sugar), gastrointestinal disturbances, and lactic acidosis.

There is no specific antidote or treatment for excessive intake of Teneligliptin+ Metformin. However, immediate medical attention is essential. Teneligliptin+ Metformin should be terminated immediately when an overdose is suspected or if any unusual symptoms occur after intake. Activated charcoal may be administered to limit further absorption of the drugs.

For hypoglycemia (low blood sugar), consume a source of rapidly absorbed carbohydrates such as glucose tablets, sugar, or honey. Gastrointestinal disturbances can be managed through supportive measures, including hydration and antiemetic medications. Lactic acidosis, a rare but severe complication, may require intensive medical intervention, such as intravenous fluids and correction of metabolic imbalances.

Hemodialysis may be considered in severe cases to remove the drugs from the bloodstream. Patients should be closely observed for any signs of lactic acidosis, a rare but potentially life-threatening complication, and treated accordingly.

Teneligliptin: Teneligliptin inhibits DPP-4, which results in lower glucagon levels, more robust insulin response to glucose, and higher levels of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP).

Metformin: Metformin is an antihyperglycemic medication that lowers basal and postprandial plasma glucose levels in people with type 2 diabetes, improving their glucose tolerance. Its pharmacologic modes of action are distinct from those of other oral antihyperglycemic medication groups. Metformin increases peripheral glucose uptake and utilization, which lowers intestinal glucose absorption, reduces hepatic glucose synthesis, and enhances insulin sensitivity. Metformin, unlike sulfonylureas, does not result in hyperinsulinemia or hypoglycemia in either type 2 diabetes patients or healthy persons. Metformin medication does not alter insulin secretion, although it may reduce the plasma insulin response throughout the day and insulin levels while fasting.

Teneligliptin: Teneligliptin's pharmacokinetics are unaffected by food, and is 87% bioavailable when taken orally. Teneligliptin takes two hours to reach its maximal plasma concentration.

Metformin: Slowly and incompletely absorbed from the gastrointestinal tract. Food slightly delays and decreases the extent of absorption. Absolute bioavailability: 50-60%. Time to peak plasma concentration: 2-3 hours (immediate-release); 7 hours, range: 4-8 hours (extended-release).

Bioavailability: 50-60% (Metformin [fasted])

Teneligliptin: Volume of distribution: Approx 198 L. Plasma protein binding: 38%

Metformin: Concentrates in the liver, kidney and gastrointestinal tract. It crosses the placenta and then enters breast milk (small amounts). Volume of distribution: 654 ± 358 L.

Protein-bound: Negligible (Metformin)

Teneligliptin: Teneligliptin is mostly not metabolized; 79% of the dosage is eliminated as the parent molecule, unaltered, in the urine. Cytochrome p450(CYP)3A4 and, to a lesser degree, CYP2C8 mediate minor metabolic pathways. Eighteen hours later, 211 per cent of the dose was still present. Of the remaining metabolites, 2% were N-sulfated to the M1 metabolite, 6% were oxidatively desaturated and cyclized to the M2 metabolite, <1% were glucuronidated at an unknown site to the M3 metabolite, <1% were carbamoylated and glucuronidated to the M4 metabolite, 6% were oxidatively saturated and cyclized to the M5 metabolite, and 2% were hydroxylated at an unknown site to the M6 metabolite. The cis isomer of a metabolite is called M2, while the trans isomer is called M5 of the same metabolite.

Metformin: Excreted unchanged in the urine and did not undergo specific hepatic metabolism (no metabolites have been found in humans) or biliary excretion.

Teneligliptin: Teneligliptin excretes as its unaltered parent molecule in the urine in approximately 79% of cases. 13% of the dosage is excreted in the faeces and 87% in the urine.

Metformin: With a plasma elimination half-life of roughly 6.2 hours, 90% of the absorbed medication is excreted via the renal pathway during the first 24 hours following oral administration. The elimination half-life of blood is roughly 17.6 hours, indicating that the erythrocyte bulk could constitute a distribution compartment.

Enhanced Glycemic Control: Metformin raises insulin sensitivity, whereas teneligliptin increases insulin secretion and lowers glucagon levels. When combined, They help improve the regulation of blood glucose.

Combining the drugs at lower doses may minimize individual drug side effects, promoting better tolerability and adherence to the treatment regimen.Some studies suggest potential cardiovascular benefits associated with Teneligliptin use.