Glibenclamide

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[edit] BRAND NAMES

[edit] STRUCTURE

Glibenclamide.jpg

[edit] MECHANISM OF ACTION

Glibenclamide is a second-generation sulfonylurea antidiabetic agent, twice as potent as the related second-generation agent glipizide.

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.

[edit] INDICATIONS

Glibenclamide is used with diet to lower blood glucose levels in patients with diabetes mellitus type II

[edit] DOSAGE

The usual starting dose is 2.5 to 5 mg daily, administered with breakfast or the first main meal. Those patients who may be more sensitive to hypoglycemic drugs (elderly/ malnourished/renal/hepatic insufficiency) should be started at 1.25 mg daily. The usual maintenance dose is in the range of 1.25 to 20 mg daily, which may be given as a single dose or in divided doses. Dosage increases should be made in increments of no more than 2.5 mg at weekly intervals based upon the patient’s blood glucose response

Glynase (Micronized Glibenclamide): The suggested starting dose is 1.5 to 3 mg daily, administered with breakfast or the first main meal. Those patients who may be more sensitive to hypoglycemic drugs (elderly/ malnourished/renal/hepatic insufficiency) should be started at 0.75 mg daily. The usual maintenance dose is in the range of 0.75 to 12 mg daily, which may be given as a single dose or in divided doses (See Dosage Interval Section). Dosage increases should be made in increments of no more than 1.5 mg at weekly intervals based upon the patient’s blood glucose response.

[edit] CONTRAINDICATIONS

  • Known hypersensitivity or allergy to Glibenclamide or other sulphonylureas.
  • Diabetic ketoacidosis, with or without coma. This condition should be treated with insulin.
  • Type I diabetes mellitus.
  • Patients with glucose 6-phosphate dehydrogenase (G6PD) deficiency (Glibenclamide can lead to hemolytic anemia).
  • Patients with significant hepatic or renal insufficiency

[edit] WARNINGS AND PRECAUTIONS

  • Hypoglycemia: All sulfonylureas are capable of producing severe hypoglycemia. s. Hypoglycemia is more likely to occur when caloric intake is deficient, after severe or prolonged exercise, when alcohol is ingested, or when more than one glucose lowering drug is used.

[edit] METABOLISM

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

[edit] INTERACTIONS

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category B (US). Glibenclamide should be used during pregnancy only if clearly needed. ncontrolled 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.
  • Nursing Mothers: Although it is not known whether glyburide is excreted in human milk, some sulfonylurea drugs are known to be excreted in human milk. Because the potential for hypoglycemia in nursing infants may exist, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother. If the drug is discontinued, and if diet alone is inadequate for controlling blood glucose, insulin therapy should be considered.

[edit] SIDE EFFECTS

  • GI: most common are nausea, epigastric fullness, and heartburn. They tend to be dose related and may disappear when dosage is reduced.
  • Skin: Rash (eg, pruritus, erythema, urticaria) and photosensitivity
  • Hepatic: Cholestatic jaundice and hepatitis may occur rarely
  • Hematology: : Leukopenia, agranulocytosis, thrombocytopenia, hemolytic anemia, aplastic anemia, and pancytopenia have been reported with sulfonylureas.
  • Endocrine: Hypoglycemia, hyponatremia
  • Miscellaneous: Disulfiram-like reaction (rare)

[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)