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

Current Oral Antidiabetic Therapy: Benzoic Acid Derivatives

Repaglinide Brand Name Drug: Prandin in the U.S., GlucoNorm in Canada, NovoNorm elsewhere Benzoic acid derivatives are the most recent addition to the list of treatment options for type 2 diabetes. In 1998, the FDA approved the first agent in this class, repaglinide. Benzoic acid derivatives are similar to sulfonylureas in that they are insulin secretagogues. However, they differ in that they bind to a different receptor on the beta cell membrane. Also, in contrast to sulfonylureas, benzoic acid derivatives do not cause direct exocytic insulin release in the absence of glucose stimulation. The true benefit of these agents stems from the fact that they have a short duration of action. … Continue reading

Eric’s expanding waistline

• review the features of type 2 diabetes mellitus; • outline common changes in the vasculature associated with diabetes; • summarize renal, ocular and neuronal complications of poorly controlled diabetes; • explain the uses of biguanide, sulfonylurea and thiazolidinedione drugs in the management of type 2 diabetes. His workmates had started to tease Eric about his expanding waistline; the overalls he wore to work would no longer fasten round his middle. In fact, Eric was only too aware that his weight had increased by about 40 lb in the last three years to 200 lb, mostly as a result of daily takeaways and drinking copious amounts of beer each night … Continue reading

Few Antidiabetic Drugs

Buformin (US Adopted Name, rINN) Drug Nomenclature Synonyms: Buformina; DBV; W-37 USAN: Buformin INN: Buformin [pINN (en)] INN: Buformina [pINN (es)] INN: Buformine [pINN (fr)] INN: Buforminum [pINN (la)] INN: Буформин [pINN (ru)] Chemical name: 1-Butylbiguanide Molecular formula: C6H15N5 =157.2 CAS: 692-13-7 (buformin); 1190-53-0 (buformin hydrochloride) ATC code: A10BA03 Profile Buformin is a biguanide antidiabetic. It has been given orally in the treatment of type 2 diabetes mellitus in doses of up to 300 mg daily. Buformin is also used as the hydrochloride. Proprietary Preparations Czech Republic: Adebit † Silubin- † … Continue reading

Biguanide Antidiabetics

Antidiabeticos biguanfdicos Adverse Effects Gastrointestinal adverse effects including anorexia, nausea, vomiting, and diarrhoea may occur with bigua-nides patients may experience taste disturbance and there may be weight loss. Absorption of various substances including vitamin B12 may be impaired. Skin reactions have been reported rarely. Hypoglycaemia is rare with a biguanide given alone, although it may occur if other contributing factors or drugs are present. Lactic acidosis, sometimes fatal, has occurred with biguanides, primarily with phenformin. When it has occurred with metformin most cases have been in patients whose condition contra-indicated the use of the drug, particularly those with renal impairment. Phenformin has been implicated … Continue reading

Diabetic emergencies

Hypoglycaemia The most frequent complication of insulin therapy is hypoglycaemia and patients taking insulin need to be educated about its cause, symptoms, and treatment. Most patients can recognise the early warning signs of hypoglycaemia and by taking sugar immediately can prevent more serious symptoms developing. Comatose patients need to be given intravenous glucose or, if this is not practicable, subcutaneous, intramuscular, or intravenous glucagon (although glucose is still required if mere is no response within 10 minutes). Hypoglycaemia can also develop in patients taking oral antidiabetics, notably the sulfonylureas. Some patients report loss of the warning signs of hypoglycaemia after transferring from animal to human insulin and these … Continue reading

Gliquidone

(British Approved Name, rINN) Drug Nomenclature International Nonproprietary Names (INNs) in main languages (French, Latin, Russian, and Spanish): Synonyms: ARDF-26; Glikidon; Glikidoni; Gliquidona; Gliquidonum BAN: Gliquidone INN: Gliquidone [rINN (en)] INN: Gliquidona [rINN (es)] INN: Gliquidone [rINN (fr)] INN: Gliquidonum [rINN (la)] INN: Гликвидон [rINN (ru)] Chemical name: 1-Cyclohexyl-3-{4-[2-(3,4-dihydro-7-methoxy-4,4-dimethyl-1,3-dioxo-2(1H)-isoquinolyl)ethyl]benzenesulphonyl}urea Molecular formula: C27H33N3O6S =527.6 CAS: 33342-05-1 ATC code: A10BB08 Read code: y02Xh Pharmacopoeias. In British and China British Pharmacopoeia 2008 (Gliquidone). A white or almost white powder. Practically insoluble in water slightly soluble in alcohol and in methyl alcohol soluble in acetone freely soluble in dimethylforma-mide. Adverse Effects, Treatment, and Precautions As for sulfonylureas … 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

Glimepiride

Drug Approvals (British Approved Name, US Adopted Name, rINN) INNs in other languages (French, Latin, and Spanish): Synonyms: Glimepirid; Glimepirida; Glimepiridi; Glimepiridum; Hoe-490 BAN: Glimepiride USAN: Glimepiride INN: Glimepiride [rINN (en)] INN: Glimepirida [rINN (es)] INN: Glimépiride [rINN (fr)] INN: Glimepiridum [rINN (la)] INN: Глимепирид [rINN (ru)] Chemical name: 1-({p-[2-(3-Ethyl-4-methyl-2-oxo-3-pyrroline-1-carboxamido)ethyl]phenyl}sulfonyl)-3-(trans-4-methylcyclohexyl)urea Molecular formula: C24H34N4O5S =490.6 CAS: 93479-97-1 ATC code: A10BB12 Read code: y0ASD Pharmacopoeias. In Europe and US. European Pharmacopoeia, 6th ed. (Glimepiride). A white to almost white powder. It exhibits polymorphism. Practically insoluble in water slightly soluble in dichloromethane soluble in dimethylformamide very slightly soluble in methyl alcohol. The United States Pharmacopeia 31, … Continue reading

Gliclazide

Drug Approvals (British Approved Name, rINN) International Nonproprietary Names (INNs) in main languages (French, Latin, and Spanish): Synonyms: Gliclazida; Gliclazidum; Gliklatsidi; Gliklazid; Gliklazidas; Glyclazide; SE-1702 BAN: Gliclazide INN: Gliclazide [rINN (en)] INN: Gliclazida [rINN (es)] INN: Gliclazide [rINN (fr)] INN: Gliclazidum [rINN (la)] INN: Гликлазид [rINN (ru)] Chemical name: 1-(3-Azabicyclo[3.3.0]oct-3-yl)-3-tosylurea; 1-(3-Azabicyclo[3.3.0]oct-3-yl)-3-p-tolylsulphonylurea Molecular formula: C15H21N3O3S =323.4 CAS: 21187-98-4 ATC code: A10BB09 Read code: y02XY Pharmacopoeias. In China, and Europe. European Pharmacopoeia, 6th ed. (Gliclazide). A white or almost white powder. Practically insoluble in water slightly soluble in alcohol sparingly soluble in acetone freely soluble in dichloromethane. Adverse Effects, Treatment, and Precautions As for sulfonylureas … Continue reading