This chapter will be most useful after having a basic understanding of the material in Chapter 43, Endocrine Pancreas and Pharmacotherapy of Diabetes Mellitus and Hypoglycemia in Goodman & Gilman’s The Pharmacological Basis of Therapeutics, 12th Edition. In addition to the material presented here, the 12th Edition includes:
A detailed discussion of the regulation of blood glucose
A description of pancreatic islet cell physiology and the synthesis and processing of insulin
A discussion of the signaling pathway that is activated by insulin resulting in its effects on target cells
A description of the pathogenesis of type 1 and type 2 diabetes
Drugs that are in development for type 2 diabetes
Table 43-5 Properties of Insulin Preparations
Understand the mechanisms of action of insulin and the oral antidiabetic drugs.
Describe the components for management of the diabetic patient including the goals of therapy.
Describe the pharmacotherapeutic options for the treatment of patients with type 1 or type 2 diabetes.
Learn about the adverse effects of insulin and the oral antidiabetic drugs.
Understand the treatment of hypoglycemia.
DRUGS INCLUDED IN THIS CHAPTER
Acarbose (PRECOSE, others)
Bromocriptine (CYCLOSET, not yet available in the United States for treatment of diabetes)
Gliclazide (DIAMICRON, others, unavailable in the United States)
Glipizide (GLUCOTROL, others)
Glyburide (Glibenclamide; MICRONASE, DIABETA, others)
Insulin aspart (NOVOLOG)
Insulin determir (LEVEMIR)
Insulin glargine (LANTUS)
Insulin glulisine (APIDRA)
Insulin lispro (HUMALOG)
Insulin protamine hagedorn (NPH, insulin isophane)
Metformin (GLUCOPHAGE, others)
Vidagliptin (GALVUS, ZOMELIS, JAIRA, not available in the United States)
Voglibose (VOGLIB, not available in the United States)
MECHANISMS OF ACTION INSULIN AND ORAL ANTIDIABETIC DRUGS ||Download (.pdf) MECHANISMS OF ACTION INSULIN AND ORAL ANTIDIABETIC DRUGS
|DRUG CLASS ||DRUGS ||MECHANISM OF ACTION |
|Insulin ||Insulin ||Insulin binds to a plasma membrane receptor that initiates a cascade of signaling events, which results in glucose utilization and glycogen synthesis (see Figure 30-1) |
|Biguanides ||Metformin ||Increases the activity of AMP-dependent protein kinase (AMPK); activated AMPK stimulates fatty acid oxidation, glucose uptake, and nonoxidative metabolism, and it reduces lipogenesis and gluconeogenesis; the net result is increased glycogen storage in skeletal muscle, lower rates of hepatic glucose production, increased insulin sensitivity, and lower blood glucose concentrations |
|Insulin Secretagogues—Sulfonylureas || |
|Stimulate insulin release by binding to a specific site on the β cell KATP channel complex and inhibiting its activity (see Figure 30-2) |
|Insulin Secretagogues—Nonsulfonylureas || |
|Stimulates insulin release by closing KATP channels in pancreatic β cells (see Figure 30-2) |
|Thiazolidinediones || |
|Ligands for the peroxisome proliferation activating receptor γ (PPARγ) that are involved in the regulation of genes related to glucose and lipid ...|