Tenelia Teneligliptin Hydrobromide Tablets

1. Indications and Usage
Monotherapy:
Indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.
Combination Therapy:
Indicated in combination with metformin hydrochloride when diet and exercise plus metformin alone do not provide adequate glycemic control.
Contraindications:
Patients with hypersensitivity to teneligliptin or any component of the product.
Patients with severe ketosis, diabetic coma or pre-coma, or type 1 diabetes mellitus.
Patients with severe infections, during the pre- and post-operative periods, or with severe trauma.
2. Dosage and Administration
Route of Administration:
Oral Use ONLY.
Recommended Dosage:
Initial Dose: The recommended dose for adult patients with type 2 diabetes is 20 mg taken orally once daily.
Titration: If glycemic control is inadequate after a sufficient period of observation, the dose may be increased to 40 mg once daily.
Administration Instructions:
Can be administered without regard to meals. Food intake does not significantly affect the overall absorption (AUC), though it may delay the time to peak concentration (Tmax).
3. Mechanism of Action
DPP-4 Inhibition:
Teneligliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor. It possesses a unique J-shaped structure that anchors strongly to DPP-4, resulting in potent inhibition.
Incretin Effect Enhancement:
By inhibiting DPP-4 activity, teneligliptin prevents the degradation of glucagon-like peptide-1 (GLP-1). This increases the plasma concentration of active GLP-1, which stimulates glucose-dependent insulin secretion from pancreatic beta cells and suppresses glucagon release from alpha cells, thereby lowering blood glucose levels.
4. Safety and Warnings
Hypoglycemia Risk:
Hypoglycemia may occur, especially when used in combination with insulin or sulfonylureas. A dose reduction of insulin or sulfonylureas should be considered when initiating teneligliptin. Caution is advised in patients with pituitary/adrenal insufficiency, malnutrition, irregular eating habits, or excessive alcohol intake.
Gastrointestinal Complications:
Severe constipation, abdominal distension, persistent abdominal pain, and vomiting may occur; these can be symptoms of intestinal obstruction. Discontinue the drug if suspected.
Acute Pancreatitis:
Persistent, severe abdominal pain accompanied by vomiting requires immediate discontinuation of the drug and appropriate management.
Interstitial Lung Disease:
Cough, dyspnea, fever, or abnormal lung sounds require prompt investigation (e.g., chest X-ray, CT). Discontinue the drug if interstitial pneumonia is suspected.
Bullous Pemphigoid:
Blisters or erosions on the skin warrant consultation with a dermatologist and potential discontinuation of therapy.
QT Prolongation:
QT interval prolongation has been reported at supratherapeutic doses (e.g., 160 mg/day); caution is advised.
5. Adverse Reactions
Most Common:
Hypoglycemia (approx. 2.6%) and constipation (approx. 0.9%).
Other Reported Reactions:
Gastrointestinal: Abdominal discomfort, nausea, diarrhea, flatulence, appetite decreased.
Hepatic: Elevated AST, ALT, γ-GTP, ALP.
Dermatological: Rash, pruritus, eczema, allergic dermatitis.
Renal/Urinary: Proteinuria, occult blood in urine.
Musculoskeletal: Arthralgia.
General: Fatigue, peripheral edema, dizziness.
6. Drug Interactions
Insulin and Insulin Secretagogues:
Concomitant use with insulin or sulfonylureas increases the risk of hypoglycemia.
CYP3A4 and FMO Substrates:
Teneligliptin is primarily metabolized by CYP3A4 and Flavin-containing Monooxygenases (FMO1/FMO3). It has weak inhibitory effects on CYP2D6, CYP3A4, and FMO.
7. Pharmaceutical Information
Chemical Composition:
Active Ingredient: Teneligliptin Hydrobromide Hydrate.
Available Strength: 20 mg (based on teneligliptin).
Excipients: Mannitol, corn starch, hydroxypropyl cellulose, silicon dioxide, magnesium stearate, hypromellose, titanium dioxide, macrogol 400, red ferric oxide.
Storage:
Store at room temperature in a tightly closed container, protected from light and moisture.