Antidiabetic Agents

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Antidiabetic drugs are a group of drug structurally unrelated to sulfonylureas and are effective when used in combination with insulin or sulfonylureas. These drugs include alpha-glucosidase inhibitors, biguanides, dipeptidyl peptidase-4 (DPP-4) inhibitors, human amylin, incretin mimetics, meglitinides, and thiazolidinediones.

Antidiabetic Agents: Generic and Brand Names

Here is a table of commonly encountered other antidiabetic agents, their generic names, and brand names:

  • Alpha-glucosidase inhibitors
    • acarbose miglitol (Precose, Glyset)
  • Biguanides
    • metformin (Glucophage)
  • Dipeptidyl peptidase-4-inhibitors
    • linagliptin (Tradjenta)
    • saxagliptin (Onglyza)
    • sitagliptin (Januvia)
  • Human amilyn
    • pramlintide acetate (Symlin)
  • Incretin mimetics
    • exanatide (Baraclude)
    • liraglutide (Victoza)
  • Meglitinides
    • nateglinide (Starlix)
    • repaglinide (Prandin)
  • Thiozolidinediones
    • pioglitazone (Actos)
    • rosiglitazone (Avandia)

Therapeutic Action

The desired and beneficial action of other antidiabetic agents:

  • Alpha-glucosidase inhibitors acarbose and miglitol inhibit alpha-glucosidase, an enzyme that breaks down glucose for absorption. Therefore, they delay the absorption of glucose. They have only a mild effect on glucose levels and do not enhance insulin secretion. They are associated with severe hepatic toxicity and GI distress.
  • Biguanide metformin decrease the production and increases the uptake of glucose. It is effective in lowering blood glucose and does not cause hypoglycemia as the sulfonylureas do. It has been associated with development of lactic acidosis and GI distress.
  • Meglitinides nateglinide and repaglinide are newer agents that act like sulfonylureas to increase insulin release.
  • Synthetic human amylin pramlintide works to modulate gastric emptying after a meal to cause a feeling of fullness or satiety. It also prevents the postmeal rise in glucagon that usually elevates glucose levels. Human amylin is a hormone produced by beta cells in the pancreas that is important in regulating postmeal glucose levels. It should not be used when patient is unable to eat.
  • Incretin mimetics exenatide and liraglutide mimic the effects of GLP-1: enhancement of glucose-dependent insulin secretion by the beta cells in the pancreas, depression of elevated glucagon secretion, and slowed gastric emptying to help moderate and lower blood glucose levels.
  • DPP-4 inhibitors lina-, saxa-, and sitagliptin slow the breakdown of GLP-1 to prolong the effects of increased insulin secretion, decreased glucagon secretion, and slowed GI emptying.
  • Thiazolidinediones pioglitazone and rosiglitazone decrease insulin resistance.

Indications

Other antidiabetic agents are indicated for the following medical conditions:

  • Biguanide metformin is approved for use in children 10 years of age and older. It is also being used in the treatment of women with polycystic ovarian syndrome (PCOS).
  • Meglitinides nateglinide and repaglinide are used to lower postprandial glucose levels because they are rapid-acting and with a very short half-life. They are taken just before meals.
  • Thiazolidinediones pioglitazone and rosiglitazone are used in combination with insulin, metformin, and sulfonylureas in patients with insulin resistance.
  • Bromocriptine, a dopamine agonist used to treat Parkinson’s disease was approved in 2009 as a CNS approach to treat type 2 diabetes.

Pharmacokinetics

Here are the characteristic interactions of other antidiabetic agents and the body in terms of absorption, distribution, metabolism, and excretion:

RouteOnsetPeakDuration
OralSlow2-2.5 h10-16 h
T1/2: 6.2 h and then 17 h
Metabolism: liver
Excretion: urine

Contraindications and Cautions

The following are contraindications and cautions for the use of agents to control blood glucose level:

  • Allergy to sulfonylureas and other antidiabetic agents. Avoid hypersensitivity reactions
  • Type 1 diabetes. These patients do not have functioning beta cells and would have no benefit from the drug.
  • Pregnancy and lactation. Potential adverse effect on the fetus or neonate.

Adverse Effects

Use of other antidiabetic agents may result to these adverse effects:

  • Common adverse effects include hypoglycemia, lactic acidosis, GI upset, nausea, anorexia, diarrhea, heartburn, and allergic skin reaction.
  • Pioglitazone is strongly linked with an increased risk of bladder cancer if it is used for over 1 year.
  • Rosiglitazone is linked with increased risk of cardiovascular problems.

Interactions

The following are drug-drug interactions involved in the use of other antidiabetic agents:

  • decreased excretion with drugs that acidify urine

Nursing Considerations

Nursing considerations are the same with sulfonylureas.

Practice Quiz: Antidiabetic Agents

Here are some practice questions for this study guide. Please visit our nursing test bank page for more NCLEX practice questions.

1. Which of the following exerts its effect by inhibiting the enzyme that breaks down glucose for absorption?

A. Miglitol
B. Metformin
C. Pramlintide
D. Linagliptin

1. Answer: A. Miglitol

The enzyme that breaks down glucose for absorption is called alpha glucosidase. Drugs under alpha glucosidase inhibitors include acarbose and miglitol.

2. This antidiabetic agent works best in patients with insulin resistance.

A. Biguanides
B. Dipeptidyl peptidase-4 inhibitors
C. Thiazolidinediones
D. Meglitinides

2. Answer: C. Thiazolidinediones

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Thiazolidinediones pioglitazone and rosiglitazone work by decreasing insulin resistance.

3. This antidiabetic drug is also used in women with polycystic ovarian syndrome.

A. Acarbose
B. Metformin
C. Rosiglitazone
D. Nateglinide

3. Answer: B. Metformin

4. Which antidiabetic agent works by modulating gastric emptying after a meal to cause a feeling of fullness?

A. Incretin mimetics
B. Meglitinides
C. Human amylin
D. Biguanides

4. Answer: C. Human amylin

Synthetic human amylin pramlintide works to modulate gastric emptying after a meal to cause a feeling of fullness or satiety. It also prevents the postmeal rise in glucagon that usually elevates glucose levels. Human amylin is a hormone produced by beta cells in the pancreas that is important in regulating postmeal glucose levels. It should not be used when patient is unable to eat.

5. Use of pioglitazone for over a year is linked with which condition?

A. Loss of effectiveness of the drug
B. Bladder cancer
C. Esophageal cancer
D. Kidney failure

5. Answer: B. Bladder cancer

Pioglitazone is strongly linked with an increased risk of bladder cancer if it is used for over one year.

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References and Sources

References and sources for this pharmacology guide for Antidiabetic Agents:

  • Karch, A. M., & Karch. (2011). Focus on nursing pharmacology. Wolters Kluwer Health/Lippincott Williams & Wilkins. [Link]
  • Katzung, B. G. (2017). Basic and clinical pharmacology. McGraw-Hill Education.
  • Lehne, R. A., Moore, L. A., Crosby, L. J., & Hamilton, D. B. (2004). Pharmacology for nursing care.
  • Smeltzer, S. C., & Bare, B. G. (1992). Brunner & Suddarth’s textbook of medical-surgical nursing. Philadelphia: JB Lippincott.
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Iris Dawn is a nurse writer in her 20s who is on the constant lookout for latest stories about Science. Her interests include Research and Medical-Surgical Nursing. She is currently furthering her studies and is seriously considering being a student as her profession. Life is spoiling her with spaghetti, acoustic playlists, libraries, and the beach.
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