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    Anti Diabetic Drugs

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    manj99
    This document discusses various classes of antidiabetic drugs including insulin, sulfonylureas, meglitinides, biguanides, thiazolidinediones, alpha-glucosidase inhibitors, incretin analogues, and dipeptidyl peptidase-4 inhibitors. It provides details on their mechanisms of action, pharmacokinetics, uses, and adverse effects. For Mr. Ramesh, who is newly diagnosed with type 2 diabetes, overweight, and has increased LDL, an appropriate drug would be metformin or a thiazolidinedione to address his insulin resistance and lipid issues.

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    Anti Diabetic Drugs

    Uploaded by

    manj99
    199 views54 pages
    This document discusses various classes of antidiabetic drugs including insulin, sulfonylureas, meglitinides, biguanides, thiazolidinediones, alpha-glucosidase inhibitors, incretin analogues, and dipeptidyl peptidase-4 inhibitors. It provides details on their mechanisms of action, pharmacokinetics, uses, and adverse effects. For Mr. Ramesh, who is newly diagnosed with type 2 diabetes, overweight, and has increased LDL, an appropriate drug would be metformin or a thiazolidinedione to address his insulin resistance and lipid issues.

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    This document discusses various classes of antidiabetic drugs including insulin, sulfonylureas, meglitinides, biguanides, thiazolidinediones, alpha-glucosidase inhibitors, incretin analogues, and dipeptidyl peptidase-4 inhibitors. It provides details on their mechanisms of action, pharmacokinetics, uses, and adverse effects. For Mr. Ramesh, who is newly diagnosed with type 2 diabetes, overweight, and has increased LDL, an appropriate drug would be metformin or a thiazolidinedione to address his insulin resistance and lipid issues.

    Copyright:

    Attribution Non-Commercial (BY-NC)
    Download as PPT, PDF, TXT or read online from Scribd
    Download as ppt, pdf, or txt
    199 views54 pages

    Anti Diabetic Drugs

    Uploaded by

    manj99
    This document discusses various classes of antidiabetic drugs including insulin, sulfonylureas, meglitinides, biguanides, thiazolidinediones, alpha-glucosidase inhibitors, incretin analogues, and dipeptidyl peptidase-4 inhibitors. It provides details on their mechanisms of action, pharmacokinetics, uses, and adverse effects. For Mr. Ramesh, who is newly diagnosed with type 2 diabetes, overweight, and has increased LDL, an appropriate drug would be metformin or a thiazolidinedione to address his insulin resistance and lipid issues.

    Copyright:

    Attribution Non-Commercial (BY-NC)
    Download as PPT, PDF, TXT or read online from Scribd
    Download as ppt, pdf, or txt
    of 54

    ANTIDIABETIC DRUGS

    Dr. Manjunatha.C.H Asst. Professor, Dept. of Pharmacology

    LEARNING OBJECTIVES
    At the end of the class the students should be able to mention various classes of antidiabetic drugs Explain their mechanism of action

    Choose appropriate drug for management of Diabetes

    OUTLINE
    INTRODUCTION VARIOUS ANTIDIABETIC DRUGS INSULIN ORAL ANTIDIABETIC DRUGS

    Mr.ramesh, 45 yr old accountant, has been newly diagnosed of DM type 2. he weighs 100 kilos and has increased increased LDL. Which group of antidiabetic drug would be appropriate in his case?

    INTRODUCTION

    Diabetes mellitus (DM) type 1 and type 2 Persistently elevated plama glucose leads to various micro and macrovascular complications

    ANTIDIABETIC DRUGS
    INSULIN AND ORAL ANTIDIABETIC DRUGS InsulinHuman and animal insulin and their analogues

    Oral antidiabetic drugs Sulfonylureas Meglitinides Biguanides thiazolidinediones

    Others -Glucosidase inhibitor Incretin analogues Dipeptidyl peptidase-4 inhibitors

    INSULIN

    SOURCES OF INSULIN
    Bovine and pork insulin Human insulinsProduced by modification of porcine insulin or by recombinant DNA technology

    Advantages of human insulinDiminished antibody production Less allergic reactions Less lipodystrophy

    Insulin analoguesInsulin lispro Insulin aspart Insulin glargine

    INSULIN RECEPTOR AND MECHANISM OF ACTION

    ACTIONS OF INSULIN
    Target cells-liver, skeletal muscles and adipose tissue Reduction in blood glucose Transit of amino acids and potassium into cells

    Enhances protein synthesis Inhibits lipolysis

    PHARMACOKINETICS
    Naturally insulin secreted- enters liver through portal vein and then to systemic circulation When administered (SC or IV) both liver and other organs receive the same concentration

    Route- Subcutaneous, Inhalational Intravenous

    Plasma t1/2 is 5-9 mins INSULIN DELIVERY SYSTEMS Syringes Insulin pens External infusion Implantable pumps

    Various insulin preparations


    ULTRASHORT-ACTINGInsulin lispro

    Insulin aspart
    SHORT-ACTING Soluble insulin

    INTERMEDIATE ACTINGIsophane (NPH) insulin Lente insulin

    LONG ACTINGUltralente insulin Insulin glargine Insulin detemir

    Strength of insulin-100u/ml Chemical assay using HPLC has replaced bioassay.

    Insulin regimens
    FLEXIBLE Multiple injections of short-acting and single night time dose of long-acting insulin CONVENTIONALTwo injections a day of biphasic insulin(combination of short and long-acting insulins)

    Adverse effects
    Mainly because of overdose Hypoglycemia- coma and convulsions and even death Lipodystrophy- rare with purified insulin and patient education to rotate injection site

    USES
    Diabetes mellitus Hyperkalemia Testing of anterior pituitary function

    ORAL ANITDIABETIC DRUGS


    NO ROLE IN TYPE 1 DM SOME (30%)ENDOGENOUS INSULIN SECRETION MUST FOR THEIR ACTION Two major groups-Hypoglycemic drugs and Antihyperglycemic drugs

    Hypoglycemic drugs
    SULFONYLUREAS (2nd generation)Glibenclamide Glipizide Gliclazide glimipiride

    MOA Increase insulin secretion and decease glucagon secretion Inhibition of ATP-sensitive potassium channels- increased amount of insulin released

    Increase only pulsatile secretion Increased insulin and somatostatin- decreased glucagon (normalize insulin glucagon ratio) Extra-pancreatic- insulin sensitization

    PHARMACOKINETICS Orally well absorbed

    ADVERSE EFFECTS- Hypoglycemia, skin rashes, nausea , vomiting , cholestasis and blood dyscrasias

    DRUG INTERACTIONS Decrease effectiveness- thiazide diuretics, corticosteroids, estrogen Increase effectiveness- ACE inhibitors, sulfonamides, salicylates and NSAIDs

    INDICATIONS First line therapy in type 2 DM Used as monotherapy or in combination with metformin or thiazolidinediones

    MEGLITINIDES
    Repaglinide Nateglinide

    MOA- similar to sulfonylureas


    PHARMACOKINETICSt1/2- 1-1.5, short and rapid acting

    Orally well absorbed Taken before food Completely metabolized in liver in 4hrs.

    ADVERSE EFFECTS Hypoglycemia-less frequent Dizziness, dyspepsia, arthralgia

    ANTIHYPERGLYCEMIC DRUGS
    BIGUANIDE-

    metformin MOA- Not completely known

    AMPK activation

    Suppresses hepatic glucose output Enhance insulin mediated glucose uptake Reduced intestinal glucose absorption

    PHARMACOKINETICS- well absorbed, not metabolized


    t1/2 1.5 to 3 hrs

    ADVERSE EFFECTS- abdominal pain, anorexia, metallic taste

    INDICATIONS First-line therapy for type 2 DM Particularly appropriate- obese diabetics with insulin resistance and hyperlipidemia Single or in combination with sulfonylureas

    THIAZOLIDINEDIONES
    Rosiglitazone Pioglitazone

    MOA- Stimulate PPAR-- enhances transcription of several insulin responsive genes.

    Suppression of hepatic gluconeognesis Insulin sensitizing action- stimulates GLUT-4 expression and translocation Activation of genes regulating FA metabolism and lipogenesis in adipose tissue Pioglitazone lowers serum TGs and raises HDL

    PHARMACOKINETICS t 3-5 hrs Metabolized in Liver

    ADVERSE REACTIONS Usually well tolerated Weight gain and edema Headache, myalgia, hepatic dysfunction

    DRUG INTERACTIONFailure of oral contraception due to pioglitazone therapy Ketoconazole inhibits pioglitazone metabolism

    INDICATIONS Mainly used to supplement sulfonylureas or biguanides and in case of insulin resistance. Particularly in patients with insulin resistance

    OTHERS
    -Glucosidase inhibitors- Acarbose, Miglitol Inhibits alpha glucosidase- prevents digestion of polysaccharides and sucrose. Postprandial glycaemia is reduced Taken at the beginning of meal

    Mild hyperglycemic and used mainly as adjuvant in obese diabetics Flatulence , abdominal discomfort and loose stools

    INCRETIN ANALOGUES- Exenatide GLP-1 enhances insulin release in response to raised plasma glucose concentration Adjunctive therapy in type 2 DM

    DIPEPTIDYL PEPTIDASE (DPP) 4 INHIBITORS Sitagliptin and Vildagliptin DDP 4 breaksdown GLP-1 and its inhibition improves glucose control

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