Glimepiride

Glimepiride Brand Name– Amaryl

What is Glimepiride

Glimepiride is an oral sulfonylurea. It is a member of the ‘second-generation’ of high potency sulfonylurea agents that include glyburide and glipizide.

Compared to glyburide, glimepiride appears to have less propensity to cause hypoglycemia and is metabolized to metabolites that are weakly active; the pharmacokinetic properties make it an option in this class for the elderly and those with renal dysfunction.

Glimepiride is used as an adjunct to diet to lower blood glucose in adults with type 2 diabetes mellitus (DM), and may be used in combination with other appropriate antidiabetic agents.

Glimepiride is often added to metformin with or without other antidiabetic agents in patients who need further medication to achieve A1C and blood glucose target goals. Metformin is first-line in the treatment of type 2 DM.

In patients with established cardiovascular (CV) disease, heart failure (HF), or chronic kidney disease (CKD), a sodium-glucose co-transporter 2 (SGLT2) inhibitor or glucagon-like peptide-1 receptor agonist (GLP-1 RA) with proven CV benefit and reduction of CKD progression is recommended for add-on therapy, independent of baseline A1C or individualized A1C target.

In patients without indicators of high-risk or established CVD, HF, or CKD, sulfonylureas are an option that as a class generally reduce hemoglobin A1C by 1% to 2%; however, the second-generation agents are preferred over first-generation agents due to a lower risk of hypoglycemia and favorable cost, efficacy, and safety profiles.

Of the second-generation agents, shorter-acting agents, such as glipizide, are preferred in the elderly and those with renal impairment over glyburide. Glimepiride may be an option as well in these patients, due to its favorable pharmacokinetics in these populations.

Disadvantages of sulfonylurea therapy include hypoglycemia (especially in the elderly), weight gain, and frequent loss of efficacy over time; however, the weight gain is relatively modest in large cohort studies and the incidence of severe hypoglycemia is lower than with insulin.

Glimepiride has been studied in pediatric patients 8 years and older with type 2 DM; however, glimepiride has not been superior to metformin monotherapy at A1C lowering and causes weight gain and more hypoglycemic episodes compared to metformin in pediatric patients

Indications

  • type 2 diabetes mellitus

For the treatment of type 2 diabetes mellitus as an adjunct to diet and exercise

Side Effects

  1. agranulocytosis
  2. alopecia
  3. anaphylactic shock
  4. anaphylactoid reactions
  5. angioedema
  6. aplastic anemia
  7. arthralgia
  8. asthenia
  9. blurred vision
  10. cholestasis
  11. dizziness
  12. dysgeusia
  13. dyspnea
  14. elevated hepatic enzymes
  15. erythema
  16. flushing
  17. headache
  18. hemolysis
  19. hemolytic anemia
  20. hepatic failure
  21. hepatitis
  22. hypoglycemia
  23. hyponatremia
  24. hypotension
  25. jaundice
  26. leukopenia
  27. maculopapular rash
  28. myalgia
  29. nausea
  30. pancytopenia
  31. photosensitivity
  32. porphyria
  33. pruritus
  34. purpura
  35. secondary failure
  36. SIADH
  37. Stevens-Johnson syndrome
  38. thrombocytopenia
  39. urticaria
  40. vasculitis
  41. weakness
  42. weight gain

Monitoring Parameters

  • blood glucose
  • glucose-6-phosphate dehydrogenase (G6PD) activity
  • glycosylated hemoglobin A1c (HbA1c)
  • serum creatinine/BUN

Contraindications

  • adrenal insufficiency
  • autonomic neuropathy
  • breast-feeding
  • children
  • diabetic ketoacidosis
  • G6PD deficiency
  • geriatric
  • hepatic disease
  • infection
  • neonates
  • obstetric delivery
  • pregnancy
  • renal disease
  • renal failure
  • renal impairment
  • sulfonamide hypersensitivity
  • sulfonylurea hypersensitivity
  • surgery
  • thyroid disease
  • trauma
  • type 1 diabetes mellitus

Interactions

  • Acebutolol
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  • Acetaminophen; Caffeine; Magnesium Salicylate; Phenyltoloxamine
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