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Planning for Sick Days, Surgery, and Travel

Diabetes control can be adversely affected by stressful situations related to physical or emotional distress. Health care providers must be able to advise patients with diabetes who become ill with infections, injuries, or other ailments that complicate their diabetes management routine and cause hyperglycemia. Definition of a sick day: A sick day could be caused by a variety of situations, from a common cold to a broken bone to a death in the family. If the patient is thrown off of his/her usual diabetes … Continue reading

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

Pregnancy: Oral hypoglycaemic agents

Commonly, women with type 2 diabetes are taking sulphonylureas and/or metformin prior to conception. Hitherto, these have little place in the management of diabetes in pregnancy, although the use of metformin has been attracting increasing interest in recent years. The main anxiety about sulphonylureas in pregnancy is the possibility of further increasing the degree of fetal hyperinsulinaemia by direct drug-induced stimulation. Sulphonylureas, with the exception of glyburide, cross the placenta and have been implicated as a direct cause of neonatal hypoglycaemia. The long-acting agent chlorpropamide is particularly dangerous and should not be used in the last 4 weeks of gestation. There is no convincing evidence that these drugs are teratogenic. Metformin, … Continue reading

Metformin Hydrochloride

Drug Approvals (British Approved Name Modified, US Adopted Name, rINN) International Nonproprietary Names (INNs) in main languages (French, Latin, and Spanish): Hidrocloruro de metformina; LA-6023 (metformin or metformin hydrochloride); Metformiinihydrokloridi; Metformin Hidroklorur; Metformin hydrochlorid; Metformine, chlorhydrate de; Metformin-hidroklorid; Metforminhydroklorid; Metformini hydrochloridum; Metformino hidrochloridas. C4H11N5,HCI = 165,6. CAS — 657-24-9 (metformin); 1115-70-4 (metformin hydrochloride). ATC — A10BA02. Pharmacopoeias. In China, Europe, Japan, and US. European Pharmacopoeia, 6th ed. (Metformin Hydrochlonde). White or almost white crystals. Freely soluble in water slightly soluble in alcohol practically insoluble in acetone and in dichloromethane. The United States Pharmacopeia 31, 2008 (Metformin Hydrochloride). A white crystalline powder. Freely soluble in … 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: Thiazoudinediones

Thiazolidinediones were developed in Japan and have been available in the United States since March 1997. Today, more than 600,000 people in the United States are being treated with troglitazone. Until recently, troglitazone was the only available member of this group. Troglitazone Brand Name Drug: Rezulin, Resulin or Romozin Troglitazone has been shown to improve peripheral insulin sensitivity (ie, increase peripheral glucose disposal) by an as yet undetermined mechanism. We do know that the drug binds to an intranuclear receptor (PPARgamma), and this complex has been found to function as a transcriptional activator. How PPARgamma activation by troglitazone results in improved insulin sensitivity is not clear. Troglitazone comes in 200-mg and … 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

Current Oral Antidiabetic Therapy: A Summary of Oral Therapy

Type 2 Diabetes: A Summary of Oral Therapy Class of Drug Chemical Structure Effects Toxicity / Side Effects Combination Therapy Sulfonylurea Sulfonic acid-urea nucleus Increases insulin secretion; reduces HgbA1C 1%-2% as monotherapy; glimepiride may have peripheral insulin-sensitizing effects Hypoglycemia Glyburide must be used with caution in the elderly or renally impaired patient; glipizide is safer in the elderly patient Biguanide or thiazolidinediones Biguanide Structurally distinct from sulfonylureas; dimethylimidodicarbonic compound Decreases hepatic glucose output; can cause mild weight loss & reduce triglycerides; reduces HgbA1C 1.5%-2% as monotherapy Risk of lactic acidosis; contra-indicated in patients with renal, hepatic or cardiorespiratory compromise; gastrointestinal irritation Thiazolidinediones, sulfonylurea, benzoic acid derivative Thiazolidinediones Thiazolidinedione-α tocopherol compound Increases … Continue reading

Treating Obesity in Patients with type 2 Diabetes: Antidiabetic Treatments and Weight

Approximately 40% of all type 2 diabetics take a drug from the sulfonylurea class (see TABLE 2) — usually glyburide, glipizide, or chlorpropamide. The sulfonylureas cause the beta-cells of the pancreas to increase insulin secretion. Weight gain is common with sulfonylurea use and ranges from 1.8 to 2.8 kg. Table 2. Antidiabetic Drugs Used to Treat Type 2 Diabetes Drug Mechanism of Action Effect on Weight During Initiation of Therapy up to One Year Potential Side Effects Sulfonylureas Increased insulin secretion by pancreatic beta cells 1.8 to 2.8 kg weight gain Weight gain, hypoglycemia Metformin Decreased hepatic glucose production/enhanced glucosedisposal by skeletal muscle 0.6 to 0.8 kg weight reduction Abdominal bloating, … Continue reading

Insulin Therapy for Type 2 Diabetes

The benefits of intensive glycemic control in patients with type 2 diabetes have focused greater attention on the use of various combinations of insulin and oral antidiabetic drugs (Table 3). Such combinations not only utilize complementary mechanisms of action but also lower doses of both insulin and oral agents, thereby minimizing the risk of adverse effects and enhancing compliance. Combination therapy is indicated for patients who cannot maintain glycemic goals with monotherapy. Table 3 Combinations of Oral Agents and Insulin for the Management of Type 2 Diabetes Expected Decrease Combination FPG (mg/dL) HbA1c (%) Sulfonylureas + insulinMetformin + insulin Acarbose + insulin Glimepiride + insulin* 60 to 8060 to 80 0 … Continue reading

Synonyms of Glyburide:

Apo-Glibenclamide, Glibenclamida [INN-Spanish], Glibenclamide, Glibenclamidum [INN-Latin]

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Therapeutic classes of Glyburide:

Antiarrhythmic Agents, Hypoglycemic Agents, Sulfonylureas

Dosage forms of Glyburide:

Form Route Strength
Tablet Oral 2.5 mg
Tablet Oral 5 mg

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