Nothing Special   »   [go: up one dir, main page]
Scribd Logo
Upload

Welcome to Scribd!

  • 38 views

    Oral Hypoglycemics or Anti-Diabetic Drugs

    Uploaded by

    Reema Razzak
    The document discusses various classes of oral hypoglycemic drugs used to treat Type 2 Diabetes. It describes: 1) Insulin secretagogues like sulfonylureas and meglitinides that stimulate insulin release from the pancreas. 2) Insulin sensitizers like biguanides (e.g. metformin) and thiazolidinediones (e.g. pioglitazone) that increase tissue sensitivity to insulin. 3) Other classes that include alpha-glucosidase inhibitors, incretin mimetics like GLP-1 agonists, and DPP-4 inhibitors that increase insulin secretion. The mechanisms of action, pharmacokinetics, uses,

    Copyright:

    © All Rights Reserved
    Download as PPTX, PDF, TXT or read online from Scribd

    Oral Hypoglycemics or Anti-Diabetic Drugs

    Uploaded by

    Reema Razzak
    38 views24 pages
    The document discusses various classes of oral hypoglycemic drugs used to treat Type 2 Diabetes. It describes: 1) Insulin secretagogues like sulfonylureas and meglitinides that stimulate insulin release from the pancreas. 2) Insulin sensitizers like biguanides (e.g. metformin) and thiazolidinediones (e.g. pioglitazone) that increase tissue sensitivity to insulin. 3) Other classes that include alpha-glucosidase inhibitors, incretin mimetics like GLP-1 agonists, and DPP-4 inhibitors that increase insulin secretion. The mechanisms of action, pharmacokinetics, uses,

    Original Description:

    Original Title

    Oral Hypoglycemics

    Copyright

    © © All Rights Reserved

    Available Formats

    PPTX, PDF, TXT or read online from Scribd

    Did you find this document useful?

    Is this content inappropriate?

    The document discusses various classes of oral hypoglycemic drugs used to treat Type 2 Diabetes. It describes: 1) Insulin secretagogues like sulfonylureas and meglitinides that stimulate insulin release from the pancreas. 2) Insulin sensitizers like biguanides (e.g. metformin) and thiazolidinediones (e.g. pioglitazone) that increase tissue sensitivity to insulin. 3) Other classes that include alpha-glucosidase inhibitors, incretin mimetics like GLP-1 agonists, and DPP-4 inhibitors that increase insulin secretion. The mechanisms of action, pharmacokinetics, uses,

    Copyright:

    © All Rights Reserved
    Download as PPTX, PDF, TXT or read online from Scribd
    Download as pptx, pdf, or txt
    38 views24 pages

    Oral Hypoglycemics or Anti-Diabetic Drugs

    Uploaded by

    Reema Razzak
    The document discusses various classes of oral hypoglycemic drugs used to treat Type 2 Diabetes. It describes: 1) Insulin secretagogues like sulfonylureas and meglitinides that stimulate insulin release from the pancreas. 2) Insulin sensitizers like biguanides (e.g. metformin) and thiazolidinediones (e.g. pioglitazone) that increase tissue sensitivity to insulin. 3) Other classes that include alpha-glucosidase inhibitors, incretin mimetics like GLP-1 agonists, and DPP-4 inhibitors that increase insulin secretion. The mechanisms of action, pharmacokinetics, uses,

    Copyright:

    © All Rights Reserved
    Download as PPTX, PDF, TXT or read online from Scribd
    Download as pptx, pdf, or txt
    of 24

    Oral Hypoglycemics or

    Anti-Diabetic Drugs
    Patients with Type 2 Diabetes have two physiological defects:

    1. Abnormal insulin secretion.

    2. Resistance to insulin action in target tissues associated with decreased number of insulin receptors.

    Oral hypoglycemic drugs:

    Insulin secretagogues
    • Sulfonylurea drugs
    • Meglitinides

    Insulin sensitizers
    • Biguanides
    • Thiazolidinediones

    2
    Oral hypoglycemic drugs:

    Insulin secretagogues
    • Sulfonylurea drugs
    • Meglitinides

    Insulin sensitizers
    • Biguanides
    • Thiazolidinediones

    3
    Others:
    • Alpha glucosidase inhibitors
    • Gastrointestinal hormones:
    Incretin(GLP-1) mimetics
    Dipeptidyl peptidase-4 (DPP-4)inhibitors

    4
    Insulin secretagogues
    Are drugs which increase the amount of insulin
    secreted by the pancreas.
    Include:
    • Sulfonylureas
    • Meglitinides

    5
    Mechanism of action of sulfonylureas:
    Stimulate insulin release from functioning B cells by
    blocking of ATP-sensitive K channels depolarization
    and opening of voltage- dependent calcium channels
    increase in intracellular calcium in the beta cells,
    which stimulates insulin release.

    6
    Pharmacokinetics of sulfonylureas:

    • Orally, well absorbed.


    • Reach peak concentration after 2-4 hr.
    • All are highly bound to plasma proteins.
    • Duration of action is variable.

    7
    Pharmacokinetics of sulfonylureas:

    • Metabolized in liver
    • Excreted in urine (elderly and renal disease)
    • Cross placenta, stimulate fetal β-cells to
    release insulin → fetal hypoglycemia at
    birth.

    8
    Uses of sulfonylureas

    Type 2 Diabetes:
    monotherapy or
    in combination with other antidiabetic drugs.

    9
    Unwanted Effects:
    1. Hyperinsulinemia & Hypoglycemia
    2. Weight gain due to increase in appetite

    10
    Meglitinides
    E.g. Repaglinide are rapidly acting insulin
    secretagogues.

    11
    Pharmacokinetics of meglitinides:

    • Orally, well absorbed.


    • Very fast onset of action, peak 1 h.
    • short duration of action (4 h).
    • Metabolized in liver and excreted in bile.
    • Taken just before each meal (3 times/day).

    12
    Uses of Meglitinides
    Type II diabetes:
    Monotherapy or in combination with other
    antidiabetic drugs.
    Patients allergic to sulfur or sulfonylureas.

    Adverse effects of Meglitinides

    • Hypoglycemia.
    • Weight gain.
    13
    Insulin sensitizers
    Are drugs which increase the sensitivity of
    target organs to insulin.

    Include
    • Biguanides(e.g. Metformin)
    • Thiazolidinediones(e.g. Pioglitazone)

    14
    Metformin(Glucophage):

    Mechanism of action of metformin

    • Does not stimulate insulin release.


    • Increases liver, muscle & adipose tissues
    sensitivity to insulin & increase peripheral
    glucose utilization.
    • Inhibits gluconeogenesis.
    • Impairs glucose absorption from GIT.

    15
    Pharmacokinetics of metformin:

    Orally.
    Not bound to serum protein.
    Not metabolized.
    Excreted unchanged in urine.

    16
    Uses:
    overweight patients with type 2 diabetes, as
    monotherapy or in combination with other
    anti diabetics.

    Advantages:
    • No risk of hypoglycemia
    • No weight gain
    • Improvement of lipid profile
    • Inexpensive

    17
    Adverse effects of metformin:
    • GIT disturbances: nausea, vomiting, diarrhea
    • Interference with vitamin B12 absorption (long term
    use).
    • Metallic taste in the mouth

    Contraindications of metformin:

    • Renal disease.
    • Liver disease.
    • Alcoholism.
    • Cardiopulmonary dysfunction.
    • Pregnancy.
    18
    Pioglitazone
    Mechanism of action:

    Increase sensitivity of target tissues to insulin.


    Increase glucose uptake and utilization in muscle and
    adipose tissue.

    Pharmacokinetics:
    Orally (once daily dose).
    Highly bound to plasma albumins (99%)
    Slow onset of activity
    Half life 3-4 h
    Metabolized in liver .
    Excreted in urine & bile
    19
    Uses of Pioglitazone
    Type II diabetes with insulin resistance.
    Used either alone or in combination with other anti
    diabetics.
    No risk of hypoglycemia when used alone.

    Adverse effects:

    • Hepatotoxicity (liver function tests for 1st year of


    therapy).
    • Fluid retention (Edema).
    • Congestive heart failure.
    • Mild weight gain.

    20
     α-GLUCOSIDASE INHIBITORS:
    • Mechanism of Action:

    Decrease carbohydrate GI absorption by inhibiting


    brush border alpha glucosidase.

    Contraindicated:
    • Inflammatory bowel disease
    • Severe liver dysfunction

    Side-Effects:
    • Abdominal cramps
    • Diarrhea
    21
    Incretin mimetics:
    Incretins are hormones secreted from intestine in response to
    food, carried through circulation to beta cells.
    Stimulate insulin secretion & decrease in glucagon secretion.

    Incretins as:
    GLP-1 (glucagon-like peptide-1).

    GLP-1Inactivated by dipeptidyl peptidase-4 (DPP-4).

    22
    Glucagon- like peptide-1 agonists:
    Therapy of patients with type 2 diabetes who are not
    controlled with oral medicine.

    Adverse effects:
    Nausea & vomiting (most common).
    Abdominal pain, decreased appetite & fatigue.

    Dipeptidyl peptidase-4 inhibitors (DPP- 4 inhibitors):


    Type 2 DM as an adjunct to diet & exercise as a
    monotherapy or in combination with other antidiabetic drugs.

    Adverse effects:
    Nausea, abdominal pain, diarrhea.

    23
    Thanks!

    24

    You might also like