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    Amit Kochhar
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    This document classifies and describes the mechanisms of common antidiabetic agents. It outlines 5 main classes: sulfonylureas, biguanides, meglitinide analogues, thiazolidinediones, and alpha-glucosidase inhibitors. Sulfonylureas work by closing ATP-sensitive potassium channels in pancreatic beta cells, stimulating insulin release. Biguanides suppress hepatic gluconeogenesis and enhance glucose disposal in muscle. Meglitinide analogues similarly close potassium channels to stimulate insulin release. Thiazolidinediones are PPAR-gamma agonists that enhance insulin gene transcription and sensitivity. Alpha-glucosidase inhibitors slow carbohydrate digestion and absorption in the small intestine.

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    Classification and mechanism of action of antidiabetics.

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    12. Antidiabetic_0

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    This document classifies and describes the mechanisms of common antidiabetic agents. It outlines 5 main classes: sulfonylureas, biguanides, meglitinide analogues, thiazolidinediones, and alpha-glucosidase inhibitors. Sulfonylureas work by closing ATP-sensitive potassium channels in pancreatic beta cells, stimulating insulin release. Biguanides suppress hepatic gluconeogenesis and enhance glucose disposal in muscle. Meglitinide analogues similarly close potassium channels to stimulate insulin release. Thiazolidinediones are PPAR-gamma agonists that enhance insulin gene transcription and sensitivity. Alpha-glucosidase inhibitors slow carbohydrate digestion and absorption in the small intestine.

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    © All Rights Reserved
    Download as PDF, TXT or read online from Scribd
    Flag for inappropriate content
    23 views5 pages

    Antidiabetic - 0

    Uploaded by

    Amit Kochhar
    This document classifies and describes the mechanisms of common antidiabetic agents. It outlines 5 main classes: sulfonylureas, biguanides, meglitinide analogues, thiazolidinediones, and alpha-glucosidase inhibitors. Sulfonylureas work by closing ATP-sensitive potassium channels in pancreatic beta cells, stimulating insulin release. Biguanides suppress hepatic gluconeogenesis and enhance glucose disposal in muscle. Meglitinide analogues similarly close potassium channels to stimulate insulin release. Thiazolidinediones are PPAR-gamma agonists that enhance insulin gene transcription and sensitivity. Alpha-glucosidase inhibitors slow carbohydrate digestion and absorption in the small intestine.

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    © All Rights Reserved
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    of 5

    http://www.gpatonline.

    com Pharmacology Antidiabetic

    Antidiabetic agents:
    Classification
    1. Sulfonylureas
    I. First generation
    Tolbutamide, Chlorpropamide
    II. Second generation
    Glibenclamide, Glipizide, Gliclazide, Glimepiride
    2. Biguanides
    Phenformin, Metformin
    3. Meglitinide analogous
    Rapeglinide, Nateglinide
    4. Thiazolidinediones
    Rosiglitazone, Pioglitazone
    5. α- Glucosidase inhibitors
    Acarbose, Miglitol

    Tolbutamide

    Chlorpropamide

    Glibenclamide

    Glipizide

    Gliclazide

    Glimepiride

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    http://www.gpatonline.com Pharmacology Antidiabetic

    Phenformin

    Metformin

    Repaglinide

    Nateglinide

    Rosiglitazone

    Pioglitazone

    Miglitol

    Mechanism of Action:

    1. Sulfonylureas:
    Act on the “sulfonylurea receptors” on pancreatic β- cell membrane  causes
    depolarization duedue to reduction in conductance of ATP sensitive K+ channels. 
    lead to enhances Ca+ influx  causes degranulation. (at least 30% functional
    pancreatic β- cell is essential for the action of Sulfonylureas)

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    http://www.gpatonline.com Pharmacology Antidiabetic

    Sulfonylurea’s action on pancreatic β- cell

    Biguanides:

     Major action: Suppress hepatic gluconeogenesis and glucose output from liver.
     Enhance insulin mediated glucose disposal in muscle and fats. biguanides enhance
    GLUT-1 transport from intracellular site to plasma membrane. (Do not affect the
    GLUT -4 which is major glucose transporter in skeletal muscle)
     Interfere with mitochondrial respiratory chain  promote peripheral glucose
    utilization  by enhancing anaerobic glycolysis.
     inhibit intestinal absorption of glucose, hexoses, amino acid and Vit B12

    Meglitinide analogous (non-sulfonylurea):


     It act as analogous manner by binding to sulfonylurea receptors as well as other
    distinct receptors  Closure of ATP dependant K+ channels  lead to depolarization
     causes insulin release.

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    http://www.gpatonline.com Pharmacology Antidiabetic

    Thiazolidinediones:
     Thiaglitazone has been withdrawn due to serious liver toxicity.
     Selective agonist for the nuclear peroxisome proliferator- activated receptors γ
    (PPAR-γ)  Enhance the transcription of several insulin genes  tend to reverse
    insulin resistance by stimulating GLUT-4 expression and translocation.  entry of
    glucose into muscle and fats.

    α- Glucosidase inhibitors:
     α- Glucosidase  final enzymes in the digestion of carbohydrates in the brush border
    of intestine mucosa.  Inhibition of this enzyme by acarbose and maglitol slow
    down and decrease digestion and absorption of the polysaccharides and sucrose.

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    http://www.gpatonline.com Pharmacology Antidiabetic

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