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  • Notes: Hypoglycemics: Insulin Secretagogues

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    Salsabila HM
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    This document discusses different classes of drugs used to treat type 2 diabetes by stimulating insulin secretion from the pancreas. It describes sulfonylureas, meglitinides, incretin mimetics (GLP-1 receptor agonists), and DPP-4 inhibitors. These drugs work by binding to receptors on pancreatic beta cells to increase insulin secretion in response to rising blood glucose levels. The document provides information on mechanisms of action, clinical uses, drug interactions, side effects and contraindications for these classes of insulin secretagogues.

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    This document discusses different classes of drugs used to treat type 2 diabetes by stimulating insulin secretion from the pancreas. It describes sulfonylureas, meglitinides, incretin mimetics (GLP-1 receptor agonists), and DPP-4 inhibitors. These drugs work by binding to receptors on pancreatic beta cells to increase insulin secretion in response to rising blood glucose levels. The document provides information on mechanisms of action, clinical uses, drug interactions, side effects and contraindications for these classes of insulin secretagogues.

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    24 views6 pages

    Notes: Hypoglycemics: Insulin Secretagogues

    Uploaded by

    Salsabila HM
    This document discusses different classes of drugs used to treat type 2 diabetes by stimulating insulin secretion from the pancreas. It describes sulfonylureas, meglitinides, incretin mimetics (GLP-1 receptor agonists), and DPP-4 inhibitors. These drugs work by binding to receptors on pancreatic beta cells to increase insulin secretion in response to rising blood glucose levels. The document provides information on mechanisms of action, clinical uses, drug interactions, side effects and contraindications for these classes of insulin secretagogues.

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    of 6

    NOTES

    NOTES
    HYPOGLYCEMICS: INSULIN
    SECRETAGOGUES

    Figure 1.1 Sulfonylureas & meglitinides: mechanism of action.

    WHAT ARE THEY?


    Basic information levels), ↓ insulin release (↓ glucose levels)
    ▪ Drugs used to treat high blood glucose → ↓ hypoglycemia risk (compared to
    levels in type 2 diabetes mellitus (DM type sulfonylureas)
    2)
    ▫ Adjunct to diet, exercise

    Key points
    ▪ Only useful if some beta-cell function is
    present
    ▪ GLP-1 agonist effects are glucose
    dependent → ↑ insulin release (↑ glucose

    OSMOSIS.ORG 1
    CLASSIFICATION CLINICAL CONCERNS
    SULFONYLUREAS & MEGLITINIDES ADVERSE EFFECTS
    ▪ Hypoglycemia
    Sulfonylurea (first generation)
    ▫ Incretins/DPP-4 inhibitors: no
    ▪ ChlorproPAMIDE (Diabinese): PO
    hypoglycemia risk unless used with
    ▪ TOLBUTamide (Orinase): PO other hypoglycemics
    ▪ TOLAZamide: PO
    Drug specific adverse-effects
    Sulfonylurea (second generation) ▪ Sulfonylureas: weight gain; gastrointestinal
    ▪ Glimepiride (Amaryl): PO (GI) upset (e.g. nausea); allergic reactions
    ▪ GlipiZIDE (Glucotrol, Glucotrol XL): PO (e.g. rash), Stevens–Johnson syndrome
    ▪ GlyBURIDE (glibenclamide) (Micronase, (rare); disulfiram-like reactions (first
    Glynase): PO generation)
    ▪ Meglitinides: weight gain
    Meglitinides (Glinides) ▪ Incretins: weight loss, ↓ appetite, fatigue; GI
    ▪ Nateglinide (Starlix): PO disturbance (e.g. nausea, vomiting); ↑ risk of
    ▪ Repaglinide: PO pancreatitis
    ▪ DPP-4 inhibitors: GI disturbance;
    Mechanism of action
    headache; nasopharyngitis; mild urinary/
    ▪ Pancreatic effect (beta cells): close ATP- respiratory infections
    sensitive potassium channels (K-ATP
    channels) in beta cells → ↑ intracellular K+
    → cellular depolarization → voltage-gated DISEASE-RELATED CONCERNS
    Ca2+ channels open → Ca2+ influx → insulin ▪ Hepatic/renal impairment: use with caution
    release → ↓ blood glucose levels
    ▪ Extrapancreatic effects (sulfonylureas): ADMINISTRATION
    ↓ hepatic gluconeogenesis; ↑ peripheral
    insulin sensitivity Administration issues
    ▪ Meglitinides: take before meals; do not take
    INCRETINS (GLP-1 RECEPTOR if meal is missed (avoids hypoglycemia)
    AGONISTS)
    ▪ Exenatide (Bydureon): SubQ PREGNANCY/BREASTFEEDING
    ▪ Liraglutide (Saxenda, Victoza): SubQ IMPLICATIONS
    ▪ Pregnancy: insulin secretagogues not
    Mechanism of action recommended
    ▪ Incretin (GLP-1) hormone analogs activate ▪ Breastfeeding: insulin secretagogues not
    GLP-1 receptors → ↑ glucose-dependent recommended
    insulin secretion; ↓ glucagon secretion;
    ↓ rate of gastric emptying; ↑ satiety → ↓
    blood glucose levels CONTRAINDICATIONS
    ▪ Sulfonylureas: type 1 diabetes mellitus (DM
    type 1), diabetic ketoacidosis
    DIPEPTIDYL PEPTIDASE 4 (DPP-4)
    INHIBITORS
    ▪ SAXagliptin (Onglyza): PO
    ▪ SITagliptin (Januvia): PO

    Mechanism of action
    ▪ Inhibits GLP-1 degradation by DPP-4
    → ↑ GLP-1 levels/effects → ↑ glucose-
    dependent insulin secretion; ↓ glucagon
    secretion; ↓ rate of gastric emptying; ↑
    satiety → ↓ blood glucose levels

    2 OSMOSIS.ORG
    Endocrine Hypoglycemics: Insulin Secretagogues

    Figure 1.2 Incretins (GLP-1 receptor agonists): mechanism of action.

    Figure 1.3 Dipeptidyl peptidase (DPP) inhibitors: mechanism of action.

    OSMOSIS.ORG 3
    Figure 1.4 Hypoglycemics: insulin secretagogues: pharmacodynamic interactions.

    4 OSMOSIS.ORG
    Endocrine Hypoglycemics: Insulin Secretagogues

    Figure 1.5 Hypoglycemics: insulin secretagogues: pharmacokinetic interactions.

    OSMOSIS.ORG 5
    Figure 1.6 Hypoglycemics: insulin secretagogues: general adult dosing guidelines.
    *Dose and dosing interval varies depending on individual patient characteristics

    6 OSMOSIS.ORG

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