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Antidiabetic agent

This document provides an overview of antidiabetic agents including insulin and oral medications used to treat type 2 diabetes. It discusses the aims of diabetes management including achieving near-normal glycemia to prevent short and long-term complications. It then describes the types of insulin including rapid, short, intermediate and long-acting varieties. The document also summarizes the classes of oral medications including their mechanisms of action, efficacy, side effects and examples of drugs from each class. Combination therapy approaches are briefly outlined.

Health & Medicine◦
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ANTIDIABETIC AGENTS By Sara Sami Yuzuncu Yil University 2015
Aims of management • To achieve near normal glycaemia - Short term- to prevent symptoms of hyper & hypo - Long term- to prevent complications • Good quality of life, near normal life expectancy
Insulin Human Insulin : • Do not contain measurable amounts of proinsulin or contaminants. • Diminished antibody • Less allergic reactions • Less lipodystrophy • Preferred in gestational diabetes
Types of Insulin • Short acting - Soluble / Neutral insulin Insulin aspart Insulin lispro Insulin glulisin • Intermediate acting – Isophane or NPH • Long acting - Insulin Zinc suspension new insulin analogue - Glargine Detemir • Biphasic- mixture of short and intermediate Biphasic lispro Biphasic Isophane
Types of Insulin Insulin Lispro Aspart Neutral/ regular Isophane ultratard Glargine Onset 10-20′ 30′ 1h 4h 2-4h Peak 1h 1-3h 4-6h 6-18h peak less Duration 3-5h 4-8h 8-14h 24h 20-24h
Soluble insulin / neutral /clear • Names - Human actrapid/ Humulin S • Species- Bovine, porcine, human • Following s/c injection Onset of action – 30 min Peak- 1-3 hours Duration- 4-8 hours • Only insulin suitable for intravenous route –plasma half life < 5 min, required continuous infusion • Used in diabetes Ketoacidosis
Sites of injections - Subcutaneous • Thighs • Upper buttocks • Abdomen • Arms Important to rotate the site Rate of absorption may be significantly different – faster from arm and abdomen than from thigh and buttock
Routes of Administration • Subcutaneous for long term regular use • Intravenous infusion in acute conditions- diabetes Ketoacidosis, Perioperative period, Hyperosmolar Nonketotic state ONLY NEUTRAL/ CLEAR INSULIN CAN BE USED • Continuous subcutaneous insulin infusion via pump – neutral • Intraperitoneal – Peritoneal dialysis patients • Inhaled insulin- experimental
Side effect of insulin • Hypoglycaemia • Weight gain- anabolic hormone • Lipohypertrophy- injection to same site • Insulin oedema • Transient deterioration in retinopathy • Insulin neuritis – actively regenerating neurone, uncommon • Postural hypotension
Example injections Short acting Short acting Short acting Intermediate/long acting breakfast lunch dinner breakfast lunch dinner bedtime bedtime injections Biphasic insulin Biphasic insulin
Rules qnever stop insulin qmonitor more frequently qmaintain your hydration qCheck for ketones qKnow when & how to call for help
Different types of Insulin Preparations: Type Appearance Onset (hr) Peak (hr) Duration (hr) RAPID ACTING Insulin lispro Clear 0.2-0.3 1-1.5 3-5 Insulin aspart Clear 0.2-0.3 1-1.5 3-5 Insulin Glulisin Clear 0.2-0.4 1-2 3-5 SHORT ACTING Regular (soluble) insulin Clear 0.5-1 2-3 6-8 INTERMEDIATE ACTING Insulin zinc suspension or Lente Cloudy 1-2 8-10 20-24 NPH or isophane Insulin Cloudy 1-2 8-10 20-24 LONG ACTING Insulin Glargine and Insulin detemir Clear Glargine: 2-4 Detemir: 1-4 _ _ Glargine: 24 Detemir: 20-24
Oral Medications to Treat Type 2 Diabetes
Major Classes of Medications sensitize the body to insulin +/- control hepatic glucose production stimulate the pancreas to make more insulin slow the absorption of CH Thiazolidinediones Biguanides Sulfonylureas Meglitinides Alpha-glucosidase inhibitors
Sites of action of Antidiabetics
Thiazolidinediones • ↓ insulin resistance by making muscle and adipose cells more sensitive to insulin. They also suppress hepatic glucose production. • Efficacy • Enhance glucose and lipid metabolism through action on Peroxisome Proliferator Activated Receptor (PPAR–γ) • by increasing the GLUT 4 glucose transporters –↓ fasting plasma glucose ~1.9-2.2 mmol/L –6 weeks for maximum effect
• Other Effects – Weight gain, oedema – Hypoglycemia (if taken with insulin or agents that stimulate insulin release) – Improves HDL cholesterol and plasma triglycerides ; usually LDL neutral • Medications in this Class: pioglitazone (Actos), rosiglitazone (Avandia), troglitazone (Rezulin) - taken off market due to liver toxicity]
Biguanides • Biguanides ↓ hepatic glucose production and increase insulin- mediated peripheral glucose uptake. • Efficacy – Decrease fasting plasma glucose 60-70 mg/dl (3.3-3.9 mmol/L) • Other Effects – Diarrhea and abdominal discomfort – Lactic acidosis if improperly prescribed – Cause small decrease in LDL cholesterol level and triglycerides – No specific effect on blood pressure – No weight gain, with possible modest weight loss – Contraindicated in patients with impaired renal function – Medications in this Class: metformin (Glucophage), metformin hydrochloride extended release (Glucophage XR)
Metformin (Glucophage) : • It does not cause hypoglycemia. • It produces a significant ↓ TG and LDL, and ↑HDL. • There is a serious concern about lactic acidosis especially in patients with kidney disease.
Sulfonylureas • Sulfonylureas increase endogenous insulin secretion • Efficacy – Decrease fasting plasma glucose 3.3-3.9 mmol/L • Other Effects – Hypoglycemia – Weight gain – No specific effect on plasma lipids or blood pressure – Generally the least expensive class of medication • Medications in this Class: – First generation : chlorpropamide , tolazamide, acetohexamide , tolbutamide – Second generation : glyburide , glipizide – Third generation : Glimiperide
Sulfonylureas
Sulfonylureas Adverse effects : • Hypoglycemia • Cholestatic jaundice • Weight gain • Cross placenta – fetal hypoglycemia. • Chlorpropamide : It can cause water retention by ↑ release of ADH (SIADH) • Disulfiram-like reaction with alcohol.
Meglitinides • stimulate insulin secretion (rapidly and for a short duration) in the presence of glucose. • Efficacy – ↓ peak postprandial glucose – ↓ plasma glucose 3.3-3.9 mmol/L • Other Effects – Hypoglycemia (may be less than with sulfonylureas if patient has a variable eating schedule) – Weight gain – No significant effect on plasma lipid levels – Safe at higher levels of serum Cr than sulfonylureas • Medications in this Class: repaglinide , nateglinide
Alpha-glucosidase Inhibitors • Alpha-glucosidase inhibitors block the enzymes that digest starches in the small intestine • It reduces absorption of glucose after meals • Efficacy – ↓ peak postprandial glucose 2.2-2.8 mmol/L – ↓ fasting plasma glucose 1.4-1.7 mmol/L • Other Effects – Flatulence or abdominal discomfort – No specific effect on lipids or blood pressure – No weight gain – Contraindicated in patients with inflammatory bowel disease or cirrhosis • Medications in this Class: acarbose , miglitol
Efficacy of Monotherapy with Oral Diabetes Agents
Anti-diabetic drugs Glucagon like Peptide : GLP-1 analog : Xenatide : (Byetta) : • GLP is an incretin released from the small intestine which increase the glucose dependent insulin secretion. • Xenatide suppress glucagon release and reduce appetite • It is administered by SC injection.
Anti-diabetic drugs Glucagon like Peptide : GLP-1 analog : Xenatide : (Byetta) :
Anti-diabetic drugs Dipeptidyl peptidase 4 (DPP-4) inhibitors: SITAGLIPTIN (januvia) Xenatide (Byetta) inj Sitagliptin (januvia)
Anti-diabetic drugs • Sitagliptin (Januvia) is an oral anti- diabetic drug. • It inhibit the dipeptidyl peptidase 4 (DPP- 4), an enzyme which inactivates the incretins GLP-1 and GIP, that are released in response to a meal. • It potentiates the secretion of insulin and suppress the release of glucagon by the pancreas.
Endocrine pancreas Glucagon : • It has positive inotropic action and chronotropic action on the heart. • It acts by stimulation of glucagon receptors and not through beta 1 receptors. • This is the basis for using glucagon in beta blocker overdose.
Treatment of Type 2 Diabetes Diagnosis Therapeutic Lifestyle Change Combination Therapy - Oral Drug with Insulin Combination Therapy - Oral Drugs Only Monotherapy
Sulfonylurea + Biguanide Glyburide + Metformin - Glucovance Glipizide + Metformin - Metaglip Thiazolidinedione + Biguanide Rosiglitazone + Metformin - Avandamet Fixed Combination Pills Combination Therapy for Type 2 Diabetes
Combination Therapy for Type 2 Diabetes Biguanides Insulin Sulfonylureas Alpha-glucosidase Inhibitors Meglitinide Thiazolidinediones www.freelivedoctor.com
Special circumstances • Intercurrent illness • Peri-operative period • Pregnancy • Childhood and adolescents • Others- travelling across time zones Exercise Alcohol Driving
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