Omarigliptin

• Type 2 Diabetes Mellitus:
  Omarigliptin is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.
• Monotherapy or Combination Therapy:
  Can be used alone or in combination with other antidiabetic agents such as metformin, sulfonylureas, or insulin.
• Off-label Uses:
  Not widely established; ongoing studies evaluating effects on beta-cell preservation and cardiovascular outcomes.

• Route: Oral administration.
• Adults:
• Usual dose is 25 mg once weekly, taken orally with or without food.
• Pediatrics:
• Safety and efficacy not established in patients under 18 years.
• Elderly:
• No dose adjustment required based on age alone.
• Renal Impairment:
• Dose adjustment recommended based on severity:
• Mild to moderate renal impairment: 25 mg once weekly (no adjustment needed).
• Severe renal impairment or end-stage renal disease: dose adjustment to 12.5 mg once weekly may be required.
• Hepatic Impairment:
• No dose adjustment required for mild to moderate hepatic impairment; use with caution in severe hepatic impairment.

Omarigliptin is a selective dipeptidyl peptidase-4 (DPP-4) inhibitor. By inhibiting the DPP-4 enzyme, it prolongs the action of incretin hormones, such as glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). These incretins enhance glucose-dependent insulin secretion from pancreatic beta cells and suppress glucagon release from alpha cells, thereby improving glycemic control.

• Absorption: Well absorbed orally; peak plasma concentration achieved approximately 2–4 hours post-dose.
• Bioavailability: Approximately 73%.
• Distribution: Widely distributed; volume of distribution ~110 L.
• Metabolism: Minimally metabolized; majority excreted unchanged.
• Half-life: Approximately 93 hours, supporting once-weekly dosing.
• Elimination: Primarily renal excretion (~80% unchanged in urine); minor fecal elimination.

• Pregnancy: No adequate, well-controlled studies in pregnant women. Animal studies have not shown fetal harm, but use only if clearly needed.
• Lactation: Unknown if excreted in human milk; caution advised, breastfeeding mothers should consider benefits and risks.

• Antidiabetic agent; Dipeptidyl Peptidase-4 (DPP-4) inhibitor; incretin enhancer.

• Known hypersensitivity to omarigliptin or any of its excipients.
• Type 1 diabetes mellitus or diabetic ketoacidosis (not effective in these conditions).

• Risk of pancreatitis; patients should be monitored for persistent severe abdominal pain.
• Hypersensitivity reactions including anaphylaxis, angioedema, and Stevens-Johnson syndrome have been reported.
• Caution in patients with renal impairment; adjust dose accordingly.
• Monitor for signs of heart failure in patients with pre-existing cardiovascular disease.
• Use caution with concomitant use of other antidiabetic medications to reduce hypoglycemia risk.

• Common:
• Nasopharyngitis, headache, upper respiratory tract infections, arthralgia.
• Less Common:
• Hypoglycemia (especially when combined with insulin or sulfonylureas), diarrhea, abdominal discomfort.
• Rare but Serious:
• Pancreatitis, hypersensitivity reactions, severe skin reactions.

• No significant CYP450 enzyme induction or inhibition; low potential for drug-drug interactions.
• Caution with drugs that may increase hypoglycemia risk (e.g., insulin, sulfonylureas).
• No significant interactions with metformin, pioglitazone, or statins reported.

• Omarigliptin is one of the few DPP-4 inhibitors designed for once-weekly dosing, improving adherence.
• Current diabetes management guidelines recommend DPP-4 inhibitors as second or third-line agents after metformin.
• No recent major safety warnings; ongoing studies assessing cardiovascular safety and beta-cell function preservation.

• Store at controlled room temperature: 20°C to 25°C (68°F to 77°F).
• Protect from moisture and light.
• Keep in original packaging until use.
• Do not freeze.