Teneligliptin

Teneligliptin

Teneligliptin is a pharmaceutical drug used for the treatment of type 2 diabetes mellitus. It belongs to the class of antidiabetic drugs known as dipeptidyl peptidase-4 (DPP-4) inhibitors or "gliptins."

Unique Structure

Teneligliptin has a unique J-shaped or anchor-locked domain structure, which allows it to potently inhibit the DPP-4 enzyme. This unique structure enhances its potency and selectivity in targeting the DPP-4 enzyme.

Mechanism of Action

Teneligliptin is an amino acid amide and a long-acting, orally bioavailable, pyrrolidine-based DPP-4 inhibitor. It exhibits hypoglycaemic activity by increasing the levels of incretin hormones like glucagon-like peptide-1 (GLP-1). Additionally, teneligliptin may reduce plasma triglyceride levels through a sustained increase in GLP-1 levels.

Teneligliptin Uses

Teneligliptin is a potent oral antidiabetic medication, and its primary use is to manage and control blood sugar levels and ensure their values are within a normal range. Here are some common uses of teneligliptin drug:

• Treatment of Type 2 Diabetes: Teneligliptin is one of the newer antidiabetic medications specifically designed for the treatment of adult-onset or type 2 diabetes mellitus (T2DM). It improves glycemic control by stimulating insulin production and reducing hormones that elevate blood sugar levels, thereby avoiding the risk of hypoglycaemia (low blood sugar) and weight gain.
• Combination Therapy: While teneligliptin can be used as a monotherapy, it is often prescribed in combination with other antidiabetic drugs like metformin. When metformin alone fails to provide the desired glycemic control, doctors add teneligliptin to the treatment regimen. Studies have shown that the combination of teneligliptin and metformin is more effective in reducing HbA1c (glycated haemoglobin) levels compared to metformin combined with glimepiride.
• Glycemic Control: Teneligliptin exhibits better efficacy in reducing HbA1c levels compared to metformin when used as a monotherapy for T2DM. It works by inhibiting the dipeptidyl peptidase-4 (DPP-4) enzyme. This enzyme causes increased levels of incretin hormones like glucagon-like peptide-1 (GLP-1). This mechanism helps lower fasting and post-meal blood sugar levels, leading to improved glycemic control over the long term.
• Renal Impairment: Teneligliptin is a safe choice for patients with renal impairment or even end-stage renal disease. Unlike many other antidiabetic medications, teneligliptin does not require dose modifications in patients with renal complications. A once-daily dosage has proven effective in providing optimal glycemic control for T2DM patients with renal issues.

How to Use Teneligliptin?

Doctors prescribe tab teneligliptin as a single dose once a day (OD) orally with water after meals. Doctors suggest taking teneligliptin at an earlier time of the day. Since the effect is long-lasting with minimal chances of hypoglycemia (less than the normal blood sugar levels), you can safely take it in the evening. Teneligliptin can be a choice of drug when metformin, another first-line antidiabetic, does not give the desired glycemic control. For ideal results, have it after lunch.

Side Effects of Teneligliptin

Teneligliptin, like other medications, can cause side effects in some individuals. While most side effects are mild and easily controllable, it's essential to be aware of them and report any severe or persistent reactions to your doctor. Here are some common side effects associated with teneligliptin medicine:

• Headache
• Hypoglycaemia (low blood sugar levels)
• Upper respiratory tract infections
• Nasopharyngitis (inflammation of the nasal passages & pharynx)
• Constipation
• Gastrointestinal symptoms (e.g., abdominal pain, nausea, diarrhoea)
• Fatigue
• Skin rashes or itching

Rarely, some individuals may experience severe teneligliptin side effects, including:

• Kidney problems: Teneligliptin is generally safe for individuals with renal impairment, but in rare cases, it may cause kidney-related issues. Monitoring kidney function is recommended.
• Allergic reactions: Teneligliptin has been reported to cause allergic reactions in some cases, such as exanthematous drug eruptions (widespread rash) or generalised pruritic maculopapular rashes (itchy, red, raised skin rashes).

Precautions

While teneligliptin is generally well-tolerated, taking certain precautions can ensure safety and efficacy. Here are some key considerations:

• Severe hepatic impairment
• Acute pancreatitis
• Pituitary or adrenal insufficiency
• History of bowel obstruction 
• Cardiovascular conditions, including heart failure, active or history of arrhythmia, QT prolongation, or bradycardia
• Excessive alcohol intake 
• Pregnancy and breastfeeding

How Teneligliptin Works

Teneligliptin is an oral medication that belongs to a drug group called dipeptidyl peptidase-4 (DPP-4) inhibitors. Here's how teneligliptin works:

• Inhibition of DPP-4 Enzyme: Teneligliptin inhibits human plasma DPP-4 activity and recombinant human DPP-4 activity in a concentration-dependent manner. The DPP-4 enzyme breaks down incretin hormones that are released in response to food intake, thus regulating blood glucose levels.
• Incretin Effect: Incretins are hormones that stimulate insulin release from the pancreas. Teneligliptin improves hyperglycaemia (high blood sugar levels) in a glucose-dependent manner by increasing the levels of these incretins. It enhances insulin secretion and reduces glucagon levels, ultimately lowering fasting and post-meal blood glucose levels.
• Reduces Glucagon Secretion: Teneligliptin also suppresses glucagon hormone release, resulting in reduced hepatic glucose production, further helping to lower blood glucose levels.
• Improves Overall Glycemic Control: By increasing insulin secretion & decreasing glucagon release, teneligliptin helps to regulate postprandial (after-meal) blood glucose levels. It improves overall glycemic control in patients with type 2 diabetes, helping them manage this condition effectively.

Can I Take Teneligliptin with Other Medicines?

• Combination with Metformin: Doctors often prescribe teneligliptin in combination with metformin, a first-line medication for T2DM. This combination has been found to be more effective in reducing HbA1c (glycated haemoglobin) levels compared to metformin combined with glimepiride, a sulfonylurea drug.
• Combination with Other Antidiabetic Drugs: Teneligliptin can be combined with metformin and other antidiabetic medications, such as sulfonylureas, thiazolidinediones, or insulin, based on the patient's needs and glycemic control targets.

However, it's essential to monitor blood glucose levels closely when combining teneligliptin with other antidiabetic drugs, as there may be an increased risk of hypoglycaemia (low blood sugar levels).

Dosing information

For adults, the recommended dosage of teneligliptin is 20 mg once daily. If this initial dosage proves insufficient, the doctor may increase it to 40 mg once daily. Teneligliptin should be taken orally with water, either before or after meals.

Conclusion

Teneligliptin is a valuable tool in managing type 2 diabetes, offering effective blood sugar control with a favourable safety profile. While it presents numerous benefits, it's crucial to remember that optimal results come from a holistic approach to diabetes management, including lifestyle modifications and regular medical consultations. As with any medication, potential side effects and interactions should be carefully considered, particularly for individuals with kidney issues or those taking multiple medications. 

FAQs

1. Does teneligliptin cause weight gain?

No, teneligliptin is considered a weight-neutral medication. Clinical studies have shown that teneligliptin does not cause significant weight gain or loss in patients with type 2 diabetes mellitus (T2DM). 

2. Is teneligliptin bad for your kidneys?

Teneligliptin is a safe choice for patients with renal impairment or even end-stage renal disease (ESRD). Unlike many other antidiabetic medications, teneligliptin does not require dose adjustments in patients with kidney-related issues. Studies have shown that teneligliptin provides optimal glycemic control for T2DM patients with renal problems without significant dosage changes.

3. Can my blood sugar levels dip down after taking teneligliptin?

Teneligliptin's risk of hypoglycaemia (low blood sugar levels) is lower than that of other diabetes medications, such as sulfonylureas or insulin. However, hypoglycaemia can still occur, mainly when teneligliptin is used in combination with other antidiabetic drugs or in individuals with renal impairment. 

4. What is the best time to take teneligliptin?

Teneligliptin can be taken at any time of the day, with or without food. However, it is advisable to take it in the earlier part of the day, as the DPP-4 enzyme it inhibits is more active during daytime hours. This timing may help optimise the efficacy of teneligliptin in controlling blood sugar levels.

5. When should one not use teneligliptin?

Teneligliptin is contraindicated (should not be used) in certain situations, including:

• Hypersensitivity or allergic reactions to teneligliptin or any of its components
• Severe ketosis, type 1 diabetes, severe infections, surgery, severe trauma, or diabetic coma
• Patients with advanced liver disease or congestive heart failure
• Pregnancy and breastfeeding 

6. Can I take teneligliptin during pregnancy?

Limited data exist on the use of teneligliptin during pregnancy. However, animal studies have not revealed evidence of teratogenicity (congenital disabilities) or adverse effects on prenatal or postnatal development when administered during organogenesis (development of organs) at doses similar to the maximum recommended clinical dose. Consult your doctor for its pros and cons before using it.