Trelagliptin-100

Trelagliptin - 100

Trelagliptin- 100 mg

Trelagliptin is a pharmaceutical drug used for the treatment of diabetes mellitus.

  • By inhibiting dipeptidyl-peptidase-4 (DPP-4) activity that neutralizes glucagon-like peptide-1 (GLP-1) Trelagliptin increases by secreting from the intestine into the blood when there is stimulation after oral intake of food GLP-1 promotes insulin secretion by the pancreas by dependence on blood concentrations and glucose Concentration.

Pharmacokinetics:

  • Mean plasma concentrations of trelagliptin were 20.00 ng / ml at week 4 and 21.60 ng / ml at week 4. Analysis of patients receiving and not receiving hemodialysis revealed that trelagliptin plasma concentrations are 23.4 ng / ml and 10.12 ng / ml over 4 weeks. And 25.09 ng / ml and 11.94 ng / ml at week 12 respectively.

Pharmacodynamics:

  • The DPP-4 enzyme is involved in inactivating the insulin hormone glucagon such as peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), which aid in the regulation of glucose homeostasis by increasing insulin biosynthesis and secretion. Inhibiting glucagon secretion. Thus, treatment with DPP-4 inhibitors by inhibiting the DPP-4 enzyme increases insulin levels under hyperglycaemic conditions. Trelagliptin is a potent inhibitor of DPP-4, and in an in vitro study in human plasma, the concentration required to produce 50% inhibition (IC50) was 1.3 nmol / L, with trelagliptin with 5.3 nmol / L with alogliptin.

Precautions:

  • Hypoglycemia: The risk of hypoglycemia may be increased by concomitant use of tregliptin and sulfonylureas or insulin preparations. Therefore, a reduction in the dose of sulfonyluria or insulin preparations when used in combination with tregliptin should be considered to reduce the risk of hypoglycemia.
  • Acute pancreatitis: Acute pancreatitis is associated with other DPP-4 inhibitors. After the initiation of tralagliptin, patients should be carefully observed for signs and symptoms of pancreatitis. If pancreatitis is suspected, tregliptin should be discontinued immediately and proper management should be initiated.

Side effects:

  • Hypersensitivity to trilagliptin or any of its components; Patients with severe renal impairment or end-stage renal failure on dialysis. Hypoglycemia: The risk of hypoglycemia may be increased by concomitant use of tregliptin and sulfonylureas or insulin preparations.

Dosage:

  • Typically, for adults, 100 mg trelagliptin is given orally once a week. The score line is not intended for dose adjustment. Do not break or crush the tablet.

Over dosage:

  • There is insufficient information regarding overdose in humans. The highest dose of trilagliptin administered in a clinical trial was a single dose of 800 mg for healthy subjects. In a fully QT / QTc study with single administration in trelagliptin 200 mg or 800 mg in healthy subjects, prolonged QT was observed in the trelagliptin 800 mg group. Triagliptin is moderately diazable; after 4 hours of hemodialysis, approximately 9.2% of the drug was removed.

Warning:

  • Hypoglycemia: The risk of hypoglycemia may be increased by concomitant use of trelagliptin and sulfonylureas or insulin preparations. Therefore, a reduction in the dose of sulfonyluria or insulin preparations when used in combination with trelagliptin should be considered to reduce the risk of hypoglycemia.
  • Acute pancreatitis: Acute pancreatitis is associated with other DPP-4 inhibitors. After the initiation of trelagliptin, patients should be carefully observed for signs and symptoms of pancreatitis. If pancreatitis is suspected, tregliptin should be discontinued immediately and proper management should be initiated.

Duration of action:

  • During periods of high blood sugar (at least 180 mg / dL), postprandial and 24-h data obtained by CGM showed that both trogliptin and alloglyptin suppressed hyperglycemia. This effect was maintained for 8 days following the administration of once-weekly tragalagliptin.

Drug- drug interaction:

  • No clinically meaningful interaction (with both medication and food) was observed, and there was no need for dose adjustment of tragalagliptin or other concomitantly administered drugs. Trigliptin is primarily excreted by the kidneys. The cytochrome (CYP) metabolism related to P450 is negligible. No significant drug – drug interactions were observed with testing of CYP-substrates.

Adverse reaction:

  • Hypersensitivity (rash, pruritus), atrial fibrillation, liver (increased ALT, AST, – increased GTP), urinary blood positive, nasopharyngitis, increased lipase, increased amylase.

Pregnancy:

  • To date no clinical studies have been conducted to evaluate trelagliptin in pregnant or lactating subjects. trelagliptin should not be given to women who are or may be pregnant, unless the expected therapeutic benefit is thought to outweigh any potential risk.

Fertility:

  • In a fertility study in mice, no adverse effects on early fetal development, mating, or male / female fertility were observed at doses up to 1000 mg / kg.

Contraindications:

  • Hypersensitivity to trelagliptin or any of its components
  • Patients with severe renal impairment or end-stage renal failure on dialysis

Breast feeding:

  • It is unknown if tralagliptin is excreted in human milk.