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    Oral Hypoglycemic Drugs2

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    علي الطياري
    1. There are several types of oral hypoglycemic drugs used to treat diabetes including sulfonylureas, biguanides, insulin sensitizers, and alpha-glycosidase inhibitors. Each drug class works through a different mechanism of action such as increasing insulin secretion, increasing glucose uptake in cells, or decreasing carbohydrate absorption. 2. Sulfonylureas are further divided into first and second generation drugs. They carry risks of hypoglycemia, weight gain, and other side effects. Biguanides like metformin decrease glucose levels and are useful for obese patients but can cause gastrointestinal issues. Insulin sensitizers improve insulin sensitivity and are used to overcome resistance. 3. All oral hyp

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    Oral Hypoglycemic Drugs2

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    علي الطياري
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    1. There are several types of oral hypoglycemic drugs used to treat diabetes including sulfonylureas, biguanides, insulin sensitizers, and alpha-glycosidase inhibitors. Each drug class works through a different mechanism of action such as increasing insulin secretion, increasing glucose uptake in cells, or decreasing carbohydrate absorption. 2. Sulfonylureas are further divided into first and second generation drugs. They carry risks of hypoglycemia, weight gain, and other side effects. Biguanides like metformin decrease glucose levels and are useful for obese patients but can cause gastrointestinal issues. Insulin sensitizers improve insulin sensitivity and are used to overcome resistance. 3. All oral hyp

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    1. There are several types of oral hypoglycemic drugs used to treat diabetes including sulfonylureas, biguanides, insulin sensitizers, and alpha-glycosidase inhibitors. Each drug class works through a different mechanism of action such as increasing insulin secretion, increasing glucose uptake in cells, or decreasing carbohydrate absorption. 2. Sulfonylureas are further divided into first and second generation drugs. They carry risks of hypoglycemia, weight gain, and other side effects. Biguanides like metformin decrease glucose levels and are useful for obese patients but can cause gastrointestinal issues. Insulin sensitizers improve insulin sensitivity and are used to overcome resistance. 3. All oral hyp

    Copyright:

    © All Rights Reserved
    Download as PDF, TXT or read online from Scribd
    Download as pdf or txt
    42 views4 pages

    Oral Hypoglycemic Drugs2

    Uploaded by

    علي الطياري
    1. There are several types of oral hypoglycemic drugs used to treat diabetes including sulfonylureas, biguanides, insulin sensitizers, and alpha-glycosidase inhibitors. Each drug class works through a different mechanism of action such as increasing insulin secretion, increasing glucose uptake in cells, or decreasing carbohydrate absorption. 2. Sulfonylureas are further divided into first and second generation drugs. They carry risks of hypoglycemia, weight gain, and other side effects. Biguanides like metformin decrease glucose levels and are useful for obese patients but can cause gastrointestinal issues. Insulin sensitizers improve insulin sensitivity and are used to overcome resistance. 3. All oral hyp

    Copyright:

    © All Rights Reserved
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    Oral hypoglycemic drugs Dr. Fahmy M.

    Al-Wasei

    Oral hypoglycemic drugs


    Diabetes is a disease that affects your body’s ability to produce or use insulin.
    Insulin is a hormone. When your body turns the food you eat into energy (also called sugar or
    glucose), insulin is released to help transport this energy to the cells. Insulin acts as a “key.” Its
    chemical message tells the cell to open and receive glucose.
    If you produce little or no insulin, or are insulin resistant, too much sugar remains in your
    blood. Blood glucose levels are higher than normal for individuals with diabetes.
    There are two main types of diabetes: Type 1 and Type 2.
    Type 1 diabetes
    When you are affected with Type 1 diabetes, your pancreas does not produce insulin .
    Type 1 diabetes, once called juvenile diabetes, is often diagnosed in children or teens .
    However, it can also occur in adults . This type accounts for 5-10 percent of people with
    diabetes.
    Type 2 diabetes occurs when the body does not produce enough insulin, which is called insulin
    resistance . Type-2 diabetes is commonly called “adult-onset diabetes” since it is diagnosed
    later in life, generally after the age of 45. It accounts for 90-95 percent of people with diabetes .
    In recent years, Type-2 diabetes has been diagnosed in younger people, including children,
    more frequently than in the past.

    Gestational diabetes occurs during pregnancy and affects about 18 percent of all pregnancies .
    Gestational diabetes usually goes away after pregnancy, but once you've had gestational
    diabetes, your chances are higher that it will happen in future pregnancies .
    In some women pregnancy uncovers Type 1 or Type 2 diabetes and these women will need to
    continue diabetes treatment after pregnancy.
    Another form is prediabetes .
    This condition causes a person’s blood sugar levels to be higher than normal but not high
    enough to be diagnosed with diabetes .
    The American Diabetes Association estimates that there are 84.1 million Americans that have
    pre-diabetes in addition to the 30.3 million with diabetes.

    Normal Diabetes
    — Fasting blood sugar 80-99 mg/dl 126 mg/dl and above
    — Random blood sugar 80-139 mg/dl 200 mg/dl and above
    — 2 hour glucose tolerance test 80-139 mg/dl 200 mg/dl and above

    — What causes diabetes?


    — Genetics, lifestyle and environment can be causes of diabetes.
    — Eating an unhealthy diet, being overweight or obese and not exercising enough may play a
    role in developing diabetes, particularly Type 2 diabetes. Type 1 diabetes is caused by an
    autoimmune response.
    The body’s immune system attacks and destroys the insulin producing beta cells in the
    pancreas.

    Oral hypoglycemic drugs


    1. Insulin secretagogues
    a. Sulfonylureas
    b. Other ( Repaglinide & Nateglinide)
    2. Biguanides
    3. Insulin sensitizers
    4. Alpha- Glycosidase inhibitors

    1
    Oral hypoglycemic drugs Dr. Fahmy M. Al-Wasei

    1. Sulfonylureas
    Pharmacological actions
    - Decrease blood glucose: 1- increase insulin secretion
    2- increase uptake of glucose by target cells
    3- decrease glucagon secretion
    4- increase the process of glycolysis (break down of
    glucose)
    Potency Onset Duration
    1st Generation
    Tolbutamide Low Rapid Short
    Acetohexamide Low Intermediate Intermediate
    Chlorpropamide Low Slow Long
    2nd Generation
    Glipizide High v. rapid Short
    Cliclazide Intermediate Intermediate Intermediate
    Glibenclamide High Slow Long

    First generation >> low potency >> is used for mild hyperglycemia
    Second generation >> high potency >> is used for severe DM

    Adverse effects of sulfonylaureas


    -Gastrointestinal: pain & abdominal discomfort
    -Hematological : Granulocytosis & Anemia
    -Liver : increase in liver enzymes (GOT & AST)
    -Syndrome of inappropriate ADH (Hyponatremia)
    -Hypoglycemia
    -Weight gain

    2- BIGUANIDES
    Actions :
    - Decrease plasma glucose by :
    1- ↑ glucose uptake into cells  increase its metabolism
    2- potenciate effect of insulin on tissue receptors

    Advantages :
    - No weight gain BCz they produce anorexia
    - No hypoglycemia ( Euoglaycemia = normal glucose level)
    - Suitable for obese patients

    Clinical value of BIGUANIDES


    - initial therapy in diabetes with obesity
    - in combination with SULFONYLUREAS in whom sulfonylureas alone are inadequate.
    Examples of BIGUANIDES :
    - Metformin ( is the most commonly used )
    - Phenformin
    - Buformin
    Adverse Effects :
    - GI (most common : anorexia & abdominal pain & diarrhea)
    - Vit B12 Malabsorption
    - Lactic Acidosis ( Phenformin)
    3- Insulin Sensetizers

    2
    Oral hypoglycemic drugs Dr. Fahmy M. Al-Wasei

    Examples :
    - Rosiglitazone
    - Pioglitazone
    Actions : ( increase receptor sensitivity )
    They diminish insulin resistance by :
    - Increase glucose uptake into cells
    - Increase cell glucose metabolism
    Clinical value of Insulin-sensitizers
     In combination with other oral hypoglycemics or insulin to overcome insulin resistance.

    Adverse effects:
     Edema, fluid retention
     Anemia, due to effect on bone marrow
     Weight gain
     Abdominal pain
     Elevation of liver enzymes, BCZ all these agents are metabolized in liver.

    4. α-Glycosidase Inhibitors
    This enzyme is found in the stomach & intestine
    Used to increase absorption of glucose by binding monosacharides into olysaccharides

    Example: Acarbose
    Used in obese patients for weight control, also in postprandial hyperglycemia
    It has no effect on FBS (Fasting Blood Sugar)

    Action: Decrease CHO (carbohydrate) absorption.

    Clinical Value: Combined with diet control in mild postprancial hyperglycemia.

    Adverse effects: GI (most common): Abdominal pain, flatulence and diarrhea.

    Hypoglycemia
    Symptoms:
    Central : dizziness , confusion
    Peripheral : tremors , sweating , hunger, palpitation ( sypathatic )

    Some drugs may mask these symptoms associated with hypoglycemia, such as β-blockers.
    Hence diabetic patients suffering from \hypertension should not be given
    Β-blockers. If given , the patient may go into severe hypoglycemia, which may proceed into
    coma, without manifestations.

    Death might occur.

    in DM 1- over dose of insulin


    2- fasting
     3- skipped meal
     4- insulinoma

    Two types of hypoglycemia :


    1- acute hypoglycemia seen in diabetic patients
    2- chronic hypoglycemia seen in insulinoma patients

    3
    Oral hypoglycemic drugs Dr. Fahmy M. Al-Wasei

    Treatment:
     Glucose (Oral, IV).
     Glucagon. (1mg I.M. in unconsciousness)
     Diazoxide (chronic hypoglycemia).

    Drug-Drug interaction:
    1- Drug reduce the efficacy of antidiabetics ( treatment failure )
    - β-adrenergic agonist
    - diazoxide
    - corticosteroids
    - phenytoin
    - diuretics ( thiazide, furosemide)
    - oral contraceptives
    - thyroid hormones

    2- Drugs increase th efficacy of antdiabetics ( hypoglycemia )


    - sulphonamides
    - salicylates
    - coumarins
    - microsomal enzyme inhibitors

    N.B. 1st 3 drugs displace the oral hypoglycemic agents in plasma.


    N.B. 4th one increase in the level of oral hypoglycemic in plasma.

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