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    Anti Diabetik A Oral: Dr. Theodorus, Mmedsc Staf Bagian Farmakologi FK Unsri

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    - Sulfonylureas work by stimulating insulin secretion from the pancreatic beta cells by closing ATP-sensitive potassium channels. They become less effective if beta cell function declines. Common side effects include hypoglycemia and weight gain. - Biguanides like metformin increase glucose uptake in muscle and inhibit glucose production and absorption to lower blood glucose levels. They may cause gastrointestinal side effects. - Thiazolidinediones improve insulin sensitivity in muscle, adipose tissue and liver by activating PPARγ receptors. They reduce hepatic glucose output and increase glucose disposal. - DPP-4 inhibitors like gliptins enhance the effects of incretin hormones by inhibiting their breakdown, stimulating insulin secretion and suppressing glucagon levels in

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    Anti Diabetik A Oral: Dr. Theodorus, Mmedsc Staf Bagian Farmakologi FK Unsri

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    22 views35 pages
    - Sulfonylureas work by stimulating insulin secretion from the pancreatic beta cells by closing ATP-sensitive potassium channels. They become less effective if beta cell function declines. Common side effects include hypoglycemia and weight gain. - Biguanides like metformin increase glucose uptake in muscle and inhibit glucose production and absorption to lower blood glucose levels. They may cause gastrointestinal side effects. - Thiazolidinediones improve insulin sensitivity in muscle, adipose tissue and liver by activating PPARγ receptors. They reduce hepatic glucose output and increase glucose disposal. - DPP-4 inhibitors like gliptins enhance the effects of incretin hormones by inhibiting their breakdown, stimulating insulin secretion and suppressing glucagon levels in

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    Anti Diabetika Oral

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    - Sulfonylureas work by stimulating insulin secretion from the pancreatic beta cells by closing ATP-sensitive potassium channels. They become less effective if beta cell function declines. Common side effects include hypoglycemia and weight gain. - Biguanides like metformin increase glucose uptake in muscle and inhibit glucose production and absorption to lower blood glucose levels. They may cause gastrointestinal side effects. - Thiazolidinediones improve insulin sensitivity in muscle, adipose tissue and liver by activating PPARγ receptors. They reduce hepatic glucose output and increase glucose disposal. - DPP-4 inhibitors like gliptins enhance the effects of incretin hormones by inhibiting their breakdown, stimulating insulin secretion and suppressing glucagon levels in

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    22 views35 pages

    Anti Diabetik A Oral: Dr. Theodorus, Mmedsc Staf Bagian Farmakologi FK Unsri

    Uploaded by

    Poppy
    - Sulfonylureas work by stimulating insulin secretion from the pancreatic beta cells by closing ATP-sensitive potassium channels. They become less effective if beta cell function declines. Common side effects include hypoglycemia and weight gain. - Biguanides like metformin increase glucose uptake in muscle and inhibit glucose production and absorption to lower blood glucose levels. They may cause gastrointestinal side effects. - Thiazolidinediones improve insulin sensitivity in muscle, adipose tissue and liver by activating PPARγ receptors. They reduce hepatic glucose output and increase glucose disposal. - DPP-4 inhibitors like gliptins enhance the effects of incretin hormones by inhibiting their breakdown, stimulating insulin secretion and suppressing glucagon levels in

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    ANTI DIABETIK A

    ORAL
    dr. Theodorus, MMedSc
    Staf Bagian Farmakologi
    FK Unsri
    • Stimulate insulin secretion

    • Cause hypoglycaemia  stimulate appetite and leads


    to weight gain

    • Only effective if β-cells are functional

    • Block ATP-sensitive K + channels in β-cells


    Mechanism of Insulin Secretion
    KATP
    Channel
    Glucose ATP

    + - -
    Metabolism Binding

    Sulfonylurea
    - Voltage

    Insulin Ca trigger
    Ca i Passive flux
    Secretion Ca
    Channel

    + +
    Sulfonylurea
    VDCC or VDCC
    KATP KATP
     ATP
    Ca2+
    K+

    Depolarization

    Resting celll Stimulated cell


    3 Pancreas : Insulin secretion
    Sulfonylureas  Insulin secretion
    SULFONILUREA
    1. Generasi I :
    Carbutamide
    Tolbutamide
    Chlorpropamide
    2. Generasi II :
    Glyburide
    Glipizide
    3. Generasi III :
    Glimepiride
    Mechanism of action ≈ Thiazolidinediones
    SULFONILUREA

    • SIDE EFFECTS
    • Hypoglicemic reactions including coma
    • Particularly, elderly patients with impaired hepatic or renal function
    • Glyburide=chlorpropamide > glipizide > tolbutamide
    • Nausea and Vomiting
    • Aplastic and hemolytic anemia
    • Hypersensitivity and dermatological reactions
    SULFONIL UREA

    • CONTRAINDICATIONS
    • Hypersensitivity
    • Diabetic keto acidosis

    • DRUG INTERACTION
    • Clofibrate, dicumarol, salysilates displace the sulfonyl ureas
    from binding site
    SECRETAGOGUE LAIN
    MEGLITINIDES :
    1.Repaglinide
    2.Meglitinide
    3.Nateglinide
    BIGUANIDE (METFORMIN)

    • Increase glucose uptake in striated muscle


    • Inhibit hepatic glucose output & intestinal glucose
    absorbtion
    • Cause anorexia  assist in weight loss
    • Are used with sulphonylurea when these have
    ceased to work adequately
    • Reduction of total cholesterol, LDL cholesterol &
    trigliceride
    • Increase HDL cholesterol concentration
    2. Muscle and adipose tissue :
    Glucose uptake
    Metformin  glucose utilization

    4. Liver : Hepatic
    Glucose Output
    Metformin  HGO
    METFORMIN

    • DRUG INTERACTION
    • Cimetidine and furosemide increased yhe metformin plasma
    • Alcohol potentiate the effect of metformin
    1. Intestine : glucose absorption
    Acarbose  glucose absorbtion secondary
    to  digestion of carbohydrate

    2. Muscle and adipose


    Tissue : glucose uptake
    ACARBOSE

    • SIDE EFFECTS: usually during the first week of therapy; most


    commonly mild-to-moderate GI tracts such as flatulantce,
    diarrhea, and abdominal discomport
    • CONTRAINDICATION:
    - Hypersensitifity
    - Diabetic ketoacidosis
    - Cirrhosis
    THIAZOLIDINEDIONES

    • Antidiabetic agents that increase insuline sensitivity


    through the modulation of several processes
    • These agents affect:
    - insulin receptor kinase activity
    - insulin receptor phosphorylation
    - insulin receptor numbers
    - hepatic glucose metabolism
    • May activate PPAR-γ (Peroxisome Proliferator –
    Activated Receptor) in adipose tissue, skeletal
    muscle and liver
    Liver : Hepatic Glucose
    Output
    Thiazolidinediones  HGO

    Improve β –
    cell function
    Proteins involve in glucose
    lipid metabolism

    Thiazolidinedione PPAR Υ RXR

    mRNA
    Response
    elements
    Gene transcription

    Promoter Coding Region

    Nucleus

    Thiazolidinediones activate nuclear receptors, resulting in expression


    of proteins involved inglucose and lipid metabolism
    TZD

    • CONTRAINDICATION
    - Hypersensitivity
    - Liver disease
    - Pregnancy category C
    - Nursing woman
    • DRUG INTERACTION
    - May induce drug metabolism by CYP3A4:
    Consider this when prescribing with others CYP3A4
    substrate such as CCB, cisapride, steroid and HMG-
    CoA reductase inhibitors
    GLIPTINE
    • DPP-4 inhibitors (Dipeptidyl peptidase-4)
    • Linagliptin, sitagliptin, and saxagliptin

    Mechanism of action: enhance and prolong


    the action of incretin hormones by
    competitively antagonizing the enzyme DPP-
    4
    gliptin

    Pharmakokinetics
    • Rapidly absorbed after oral administration, with
    peak plasma concentration occuring in 1- 4 hours
    • Bioavaibility is more than 87%
    • 79% is excreted unchanged in the urine, primarily
    via renal excretion
    • Only slightly is metabolized by using CYP3A4 and
    CYP2C6 in liver
    gliptin

    CONTRINDICATION
    • DM type 1
    • Hipersensitivity
    • Pregnancy

    • SIDE EFFECTS
    • Upper respiratory tract infection
    • Headache, nausea
    • Hypersensitivity reaction
    gliptin
    DRUG INTERACTION:
    • Alpha adrenergic agonist, isoniazid, antipsychotic
    first generation reduced it’s effect
    • Etanol and quinolone enhanced it’s effect

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