Gliclazide

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Contents

[edit] BRAND NAMES

[edit] STRUCTURE

Gliclazide.jpg

[edit] MECHANISM OF ACTION

Gliclazide 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.

The half-life of Gliclazide is approximately 10 - 12 hours

[edit] INDICATIONS

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

[edit] DOSAGE

Modified-release tablets 30 mg and Modified-release breakable tablets 60 mg: The recommended starting dose is 30 mg daily, even in elderly patients (over 65 years old). A single daily dose provides effective blood glucose control. The single daily dose may be between 30 mg and 90 mg, or even 120 mg. The daily dose should not exceed 120 mg.

Dose adjustment should be carried out in steps of 30 mg, according to the blood glucose response. Each step should last for at least two weeks.

[edit] CONTRAINDICATIONS

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

[edit] WARNINGS AND PRECAUTIONS

  • Dose reduction may be necessary in patients with renal dysfunction.
  • 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.

[edit] INTERACTIONS

Increase Effect/Toxicity

  • Miconazole: The concomitant use of miconazole and gliclazide is contraindicated (combination increases the risk of hypoglycemia)
  • Phenylbutazone: Increases the hypoglycaemic effect of sulphonylureas (displaces their binding to plasma proteins and/or reduces their elimination). Combination is not recommended.
  • Other antidiabetic agents (insulins, acarbose, metformin): Increases the risk of hypoglycemia. Use with caution
  • Beta blockers: Increases the risk of hypoglycemia. Use with caution
  • Fluconazole: Increases the risk of hypoglycemia. Use with caution
  • ACE inhibitors: Increases the risk of hypoglycemia. Use with caution


Decreased Effect: Danazol, Chlorpromazine, Glucocorticoids, and beta-2 agonist (Ritodrine, salbutamol) causes an increase in blood glucose levels. Use with caution

[edit] PREGNANCY AND LACTATION

  • Pregnancy: Gliclazide is contraindicated in pregnancy. 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 Women: Gliclazide is contraindicated in breast-feeding mothers

[edit] SIDE EFFECTS

The most frequent adverse drug reactions are hypoglycemia and gastrointestinal disturbances (including abdominal pain, nausea, vomiting, dyspepsia, diarrhea, constipation)

Isolated cases of impairment of liver function with cholestasis and jaundice, and hepatitis which can regress after withdrawal of the drug or may lead to life-threatening liver failure have been observed. other serious adverse reactions reported with gliclazide are hypoglycaemic coma, pancytopenia, thrombocytopenia, pyrexia, pancreatitis acute and skin reactions (pruritus and rash).

[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)