Generic
Trelagliptin
2 brands available in the market
At a glance
Trelagliptin is indicated for type 2 diabetes mellitus when the first line treatment of metformin is not achieving the expected glycemic goals.
Description
Trelagliptin inhibits dipeptidyl peptidase 4 (DPP-4) activity, increasing GLP-1 blood concentration and promoting glucose-dependent insulin secretion from the pancreas.
Indications
- Type 2 diabetes mellitus
Therapeutic class
Dipeptidyl Peptidase-4 (DPP-4) inhibitor
Pharmacological class
DPP-4 Inhibitor
Pharmacology
Trelagliptin selectively inhibits human plasma DPP-4 activity (IC50: 4.2 nmol/l). It inactivates GLP-1, increasing active GLP-1 concentration, which promotes glucose-dependent insulin secretion and improves glucose tolerance.
Mechanism of action
Inhibits DPP-4, increasing GLP-1 and insulin secretion.
Dosage
Adult Dose (Oral):
- 100 mg tablet once weekly
- Moderate renal impairment (CrCl 30-<50): 50 mg once weekly
Administration
- Take once weekly on the same day each week
- May be taken with or without food
Missed dose
If you miss a dose, take it as soon as you remember and continue with a newly decided schedule; do not double the dose.
Side effects
Common Side Effects:
- Hypoglycemia
- Nasopharyngitis
- Elevated lipase
- Acute pancreatitis
- Intestinal obstruction
- Atrial fibrillation
- Elevated liver enzymes
Precautions & warnings
- Caution in moderate kidney function disease
- Caution in hypoadrenalism or hypopituitarism
- Caution in malnutrition, irregular eating patterns, starvation, vigorous exercise
- May cause hypoglycemia when used with other diabetes medication
- Consider reducing dose of sulfonylurea or insulin when used in combination
Contraindications
- Hypersensitivity
Drug interactions
- Sulfonylurea or insulin: increased risk of hypoglycemia; dose reduction may be needed
Food interactions
Food interactions are not significant.
Use in pregnancy
Use in Pregnancy: Safety not established; use only after risk-benefit evaluation.
Pregnancy Category: C — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Not recommended; discontinue breastfeeding if drug must be administered.
Pediatric use
Safety not established in children under 13 years
Geriatric use
Caution advised in elderly due to reduced kidney function
Renal / hepatic impairment
Renal Impairment: Moderate (CrCl 30-<50): 50 mg once weekly; Severe (eGFR <30): contraindicated
Hepatic Impairment: Limited information
Overdose effects
Symptoms: Hypoglycemia, QT elongation (at 800 mg dose).
Treatment: Supportive; correct hypoglycemia with sucrose.
Storage conditions
Store at 25°C; excursions permitted to 15-30°C. Dispense in original container to protect from high humidity and light; keep out of reach of children.