Glimepiride

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Contents

[edit] BRAND NAMES

  • International: Amaryl
  • Palestine: Amiran

[edit] STRUCTURE

Glimepiride.jpg

[edit] MECHANISM OF ACTION

Glimepiride is a second-generation sulfonylurea antidiabetic agent. Second-generation sulfonylureas are both more potent and have shorter half-lives than the first-generation sulfonylureas.

Sulfonylureas appears to lower the blood glucose acutely by stimulating the release of insulin from the pancreas, an effect dependent upon functioning beta cells in the pancreatic islets.

Sulfonylureas likely bind to ATP-sensitive potassium-channel receptors on the pancreatic cell surface, reducing potassium conductance and causing depolarization of the membrane. Depolarization stimulates calcium ion influx through voltage-sensitive calcium channels, raising intracellular concentrations of calcium ions, which induces the secretion, or exocytosis, of insulin.

Good metabolic control over 24 hours can be achieved with a single dose of Glimepiride

[edit] INDICATIONS

Glimepiride is used as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus

[edit] DOSAGE

  • The usual initial dose is 1mg once daily. If necessary, the daily dose can be increased. Any increase should be based on regular blood sugar monitoring, and should be gradual, i.e., at intervals of one to two weeks, and carried out stepwise, as follows: 1mg - 2mg - 3mg - 4mg - 6mg, and in exceptional cases 8mg.
  • Administer with breakfast or first meal of the day.
  • Use 1 mg starting dose and titrate slowly in patients at increased risk for hypoglycemia (e.g., elderly, patients with renal impairment)

[edit] CONTRAINDICATIONS

  • Hypersensitivity to Glimepiride or other sulphonylureas
  • Diabetic ketoacidosis, with or without coma. This condition should be treated with insulin.
  • Type I diabetes mellitus.
  • Pregnancy and lactation
  • Patients with glucose 6-phosphate dehydrogenase (G6PD) deficiency (sulfonylurea agents can lead to hemolytic anemia).

[edit] WARNINGS AND PRECAUTIONS

  • Hypoglycemia: All sulfonylureas are capable of producing severe hypoglycemia. Hypoglycemia is more likely to occur when caloric intake is deficient, after severe or prolonged exercise, when alcohol is ingested, when more than one glucose lowering drug is used, in elderly patients, and in patients with impaired hepatic or renal function. Some cases may be severe and prolonged. Hospitalisation may be necessary and glucose administration may need to be continued for several days. Hypoglycemia may be difficult to recognize in elderly patients and in patients receiving beta-blockers. In people with type 2 diabetes, glimepiride was associated with fewer episodes of severe hypoglycemia than glibenclamide (Daonil, Euglucon) in routine clinical use.

[edit] METABOLISM

  • Glimepiride is metabolized by the enzyme cytochrome P450 2C9 (CYP2C9)

[edit] INTERACTIONS

  • Miconazole: Severe hypoglycemia can occur when Glimepiride and oral miconazole are used concomitantly.
  • CYP2C9 Inhibitors : Fluconazole may inhibit the metabolism of glimepiride, causing increased plasma concentrations, which may lead to hypoglycemia.

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category C (US). Glimepiride should be given to a pregnant woman only if the potential benefits justify the potential risk to the patient and fetus. Uncontrolled diabetes (gestational or not) is associated with a higher incidence of congenital abnormalities and perinatal mortality. Blood glucose control should be optimal around the time of conception to reduce the risk of congenital malformations. Insulin is the drug of choice for controlling diabetes mellitus during pregnancy.
  • Nursing Mothers: a decision should be made whether to discontinue nursing or discontinue Glimepiride, taking into account the importance of Glimepiride to the mother.

[edit] SIDE EFFECTS

Common adverse reactions in clinical trials (≥5% and more common than with placebo) include hypoglycemia, headache, nausea, and dizziness

[edit] RELATED LINKS

Understanding Type 2 Diabetes
A simple explanation of what diabetes is

[edit] BIBLIOGRAPHY

[edit] REFERENCES

Diabetes (Antidiabetic drugs)
Insulin Secretagogues (drugs that increase insulin release from pancreas) Sulfonylureas Chlorpropamide (Diabinese)   Glibenclamide or Glyburide (Diabeta, Micronase, Glynase, Daonil, Euglycon)   Gliclazide (Diamicron)   Glimepiride (Amaryl, Solosa)   Glipizide (Glucotrol, Minidiab, Glibenese)   Gliquidone (Glurenorm)
Meglitinides Repaglinide (Prandin, Novonorm)   Nateglinide (Starlix)
Dipeptidyl peptidase-4 inhibitors Linagliptin (Trajenta)   Saxagliptin (Onglyza)   Sitagliptin (Januvia)   Vildagliptin (Galvus)
Incretin mimetics (GLP-1 agonists and analogs) Exenatide (Byetta)   Liraglutide (Victoza)   Lixisenatide (Lyxumia)   Dulaglutide (Trulicity)
Insulin Sensitizers (drugs that decrease insulin resistance)
Biguanides Metformin (Glucophage)
Thiazolidinediones Pioglitazone (Actos)
Drugs that retard the digestion and absorption of carbohydrates in the small intestine
Alpha-glucosidase inhibitors Acarbose (Glucobay, Precose)
Drugs that reduce glucose absorption in the kidney and increase glucose excretion in the urine
Sodium glucose cotransporter 2 (SGLT2) inhibitors Canagliflozin (Invokana)   Dapagliflozin (Farxiga)   Empagliflozin (Jardiance, Glyxambi, Synjardi)
Insulin and insulin analogs
Intermediate acting insulins Insulin lispro protamine (Humalog BASAL)   Isophane human insulin : Human insulin protamine (NPH) (Humulin I, Protaphane)
Long-acting insulins‎ Insulin detemir (Levemir)   Insulin glargine (Lantus)
Fast-acting insulins‎ Regular insulin : Insulin (Human recombinant) (Actrapid, Humulin R)
Ultra-rapid-acting insulins‎‎ Insulin aspart (Novorapid)   Insulin glulisine (Apidra)   Insulin lispro (Humalog)   Insulin human (Inhalation Powder) (Afrezza)
Premixed insulin‎‎‎ (ultra-rapid-acting + intermediate acting Insulin aspart / Insulin aspart protamine (Novomix)   Insulin lispro / Insulin lispro protamine (Humalog Mix)
Inhaled Insulin Insulin human (Inhalation Powder) (Afrezza)
Combination therapy
Sulfonylurea + Metformin Glibenclamide / Metformin (Bieuglicon M, Diaglimet, Glibomet, Gliconorm, Glicorest, Suguan M)
Thiazolidinedione + Metformin Pioglitazone / Metformin (Competact, Glubrava)
Thiazolidinedione + Sulfonylurea Pioglitazone / Glimepiride (Tandemact)
Dipeptidyl peptidase-4 inhibitors + Metformin Linagliptin / Metformin (Jentadueto)   Sitagliptin / Metformin (Efficib, Janumet, Velmetia)   Vildagliptin / Metformin (Eucreas)