Endocrinology Book

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Second Generation SulfonylureaAka: Insulin Secretagogue, Sulfonylurea, Glipizide, Glyburide

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  1. See Also
    1. First Generation Sulfonylurea
    2. Oral Hypoglycemic Agents
  2. Indications: Type II Diabetes Mellitus (early, phase 1-2)
    1. Better effect in lean patients
    2. Consider when Hemoglobin A1C <9%
    3. Second-line to Metformin in most patients
    4. Consider as first-line in specific cohorts
      1. Consider when post-prandial glucose 200 to 300 mg/dl
      2. Consider when Type II with polyuria, polydipsia
  3. Contraindication
    1. Sulfa allergy (applies to sulonylureas)
    2. Renal and liver dysfunction
      1. Use caution with sulfonylureas
      2. Repaglinide or Nateglinide may be preferred here
  4. Mechanism
    1. Pancreatic beta cell stimulation for Insulin release
    2. Secretagogues do not burn out the beta cells sooner
  5. Dosing Pearls
    1. Use Long acting agents
    2. Increase dose every 1-2 weeks until adequate response
    3. No response in 25-30% of Type II Diabetics
    4. Never combine secretagogues
      1. They all have same site of activity
      2. If one does not work, then all will not work
  6. Preparations
    1. Glimepiride (Amaryl)
      1. Start: 1-2 mg PO qd
      2. Usual: 4 mg PO qd
      3. Maximum: 8 mg PO qd
      4. Advantages
        1. More rapid onset with longer duration
        2. Lower Incidence of Hypoglycemia
        3. Preferred of class for Coronary Artery Disease
    2. Glipizide (Glucotrol)
      1. Start: 5 mg PO qd
      2. Usual: 10-20 mg PO qd
      3. Maximum: 20 mg PO bid
    3. Glipizide Extended Release (Glucotrol XL)
      1. Start: 5 mg PO qd
      2. Usual: 5-10 mg PO qd
      3. Maximum: 20 mg PO qd
      4. Advantages: Least expensive sulfonylurea
    4. Glyburide (DiaBeta, Micronase)
      1. Start: 2.5 to 5 mg PO qd
      2. Usual: 5-20 mg PO qd
      3. Maximum: 20 mg PO qd
    5. Glyburide Micronized (Glynase, PresTab)
      1. Start: 1.5 to 3 mg PO qd
      2. Usual: 3-12 mg PO qd
      3. Maximum: 12 mg PO qd
  7. Adverse Effects
    1. Weight gain
    2. Hypoglycemia
  8. References
    1. Defronzo (1999) Ann Intern Med 131:281
    2. Luna (1999) Prim Care 26:895

Glyburide (C0017628)

Definition (MSH)An antidiabetic sulfonylurea derivative with actions similar to those of chlorpropamide.
Definition (CSP)N-4-beta-(2-methoxy-5-chlorobenzamido) -ethylbenzosulfonyl-N'- cyclohexylurea; hypoglycemic used against non-insulin dependent diabetes mellitus; thought to act by increasing insulin receptor expression in target tissues.
Definition (NCI)A member of the second generation of the sulfonylurea hypoglycemic agents. Glyburide inhibits the ATP-sensitive potassium channels on the beta-cell membrane, thereby preventing potassium efflux leading to membrane depolarization and subsequent calcium influx. The increased intracellular levels of calcium induce insulin secretion from functioning beta-cells of the pancreatic islet tissue and leads to a lowering in blood glucose levels.
ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
EnglishGlibenclamide, Glybenclamide, Glybenzcyclamide, Glyburide, GLYBURIDE PREPARATION, Gyburide
Spanishglibenclamida, glibenzciclamida, gliburida
CreditsDerived from the NIH UMLS (Unified Medical Language System)


Glipizide (C0017642)

Definition (MSH)An oral hypoglycemic agent which is rapidly absorbed and completely metabolized.
Definition (CSP)1-cyclohexyl-3-(p-(2-(5-methyl pyrazinecarboxamido) ethyl) phenyl) sulfonylurea; a typical member of the sulfonylurea family of type II (NIDDM) antidiabetic drugs.
Definition (NCI)A member of the second generation of the sulfonylurea hypoglycemic agents. Glipizide inhibits the ATP-sensitive potassium channels on the beta-cell membrane, thereby preventing potassium efflux leading to membrane depolarization and subsequent calcium influx. The increased intracellular calcium levels induce insulin secretion from functioning beta-cells of the pancreatic islet tissue and reduces blood glucose levels.
ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
EnglishGlidiazinamide, Glipizide, GLIPIZIDE PREPARATION, Glipizide product, Glydiazinamide, Glypidizine
Spanishglidiacinamida, glidiazinamida, glipicida, glipizida
CreditsDerived from the NIH UMLS (Unified Medical Language System)


Sulfonylurea Compounds (C0038766)

Definition (CSP)compounds of the type R-SO2-NHCONH-; when R=Ph, these are a group of hypoglycemic agents which enhance insulin secretion by beta cells and insulin sensitivity in target tissue, and so are effective in type II (noninsulin-dependent) diabetes mellitus.
ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
EnglishSulfonylurea, Sulfonylurea and its derivatives, Sulfonylurea Compounds, SULFONYLUREA CPDS, Sulfonylurea product, Sulfonylureas, Sulphonylurea, Sulphonylurea and its derivatives, Sulphonylurea compounds, Sulphonylurea product
Spanishsulfonilurea, sulfonilurea y derivados
CreditsDerived from the NIH UMLS (Unified Medical Language System)



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