Oral agents for glucose management

Five classes of oral pharmaceutical agents for the treatment of type 2 diabetes have been approved in the United States by the Food and Drug Administration (FDA). In general, there is no clinical evidence of superiority of a particular drug over another in elderly patients. Knowledge of pharmacokinetics, side effects, and potential interactions allow for a safe use of these drugs in older patients with diabetes. Two classes of drugs, the sulfonylureas and the meglitinides improve glucose levels by stimulating insulin secretion from pancreatic β-cells. Other agents target different mechanisms in the underlying pathogenesis of the disease, such as the reduction of carbohydrate absorption (a-glucosidase inhibitors) and improvement in insulin … Continue reading

Glipizide

(British Approved Name, US Adopted Name, rINN) Drug Nomenclature International Nonproprietary Names (INNs) in main languages (French, Latin, Russian, and Spanish): Synonyms: CP-28720; Glipitsidi; Glipizid; Glipizida; Glipizidas; Glipizidum; Glydiazinamide; K-4024 BAN: Glipizide USAN: Glipizide INN: Glipizide [pINN (en)] INN: Glipizida [pINN (es)] INN: Glipizide [pINN (fr)] INN: Glipizidum [pINN (la)] INN: Глипизид [pINN (ru)] Chemical name: 1-Cyclohexyl-3-{4-[2-(5-methylpyrazine-2-carboxamido)ethyl]benzenesulphonyl}urea Molecular formula: C21H27N5O4S =445.5 CAS: 29094-61-9 ATC code: A10BB07 Read code: y02Xb Pharmacopoeias. In China, Europe, and US. European Pharmacopoeia, 6th ed. (Glipizide). A white or almost white crystalline powder. Practically insoluble in water and in alcohol very slightly soluble in acetone and in dichloromethane. It … Continue reading

Glibenclamide

Drug Approvals (British Approved Name, rINN) International Nonproprietary Names (INNs) in main languages (French, Latin, and Spanish): Glibenclamida; Glibenclamidum; Glibenklamid; Glibenklamidas; Glibenklamidi; Glybenclamide; Glybenzcyclamide; Glyburide (US-AN); HB-419; U-26452 C23H28CIN305S = 494.0. CAS — 10238-21-8. ATC — A10BB01. Note. The name glibornuride has frequently but erroneously been applied to glibenclamide. Pharmacopoeias. In China, Europe, International, Japan, and US. European Pharmacopoeia, 6th ed. (Glibenclamide). A white or almost white, crystalline powder. Practically insoluble in water slightly soluble in alcohol and in methyl alcohol sparingly soluble in dichloromethane. The United States Pharmacopeia 31, 2008 (Glyburide). Store in airtight containers. Adverse Effects, Treatment, and Precautions As for … Continue reading

Current Oral Antidiabetic Therapy: Sulfonylureas

These agents are derivatives of sulfonic acid and urea, and produce their effects by binding to receptors on the surface of pancreatic beta cells. The binding of sulfonylureas results in depolarization of the cell membrane, the influx of calcium ions, and subsequent release of insulin. The sulfonylureas were developed in 1954 and continue to be the most widely prescribed oral agents for the treatment of type 2 diabetes. Early evidence of associated increased cardiovascular morbidity has not been reproduced, and today sulfonylureas are considered relatively safe agents that have proven effective over long-term use. Sulfonylureas: First-Generation Sulfonylureas consists of two groups or generations of agents. The first-generation agents are … Continue reading

Type 2 Diabetes: Antidiabetic Agents

All patients with type 1 diabetes are dependent on exogenous insulin administration, whereas patients with type 2 diabetes have a relative, not an absolute, insulin deficiency. If monitoring and lifestyle changes alone do not produce adequate glucose control of type 2 diabetes, oral antidiabetic agents will be prescribed. Diet, exercise, and optimal use of oral antidiabetic agents (alone or in combination) may be enough to counteract insulin resistance and thus achieve effective glycemic control. However, due to progressive pancreatic b-cell deterioration, many patients with type 2 diabetes eventually become unable to produce sufficient insulin. In such cases daily insulin self-injections will be needed. Oral antidiabetic drugs fall … Continue reading