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
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.
Drug interactions
- Sulfonylurea or insulin: increased risk of hypoglycemia; dose reduction may be needed
Food interactions
Food interactions are not significant.
Contraindications
- Hypersensitivity
Side effects
Common Side Effects:
- Hypoglycemia
- Nasopharyngitis
- Elevated lipase
- Acute pancreatitis
- Intestinal obstruction
- Atrial fibrillation
- Elevated liver enzymes
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.
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
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.
Therapeutic class
Dipeptidyl Peptidase-4 (DPP-4) inhibitor
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.