Islets of Hope for persons with diabetes

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Source:  edited for content, from Wikipedia.com


Drug dictionaries & information

NIH - Generic and Brand

Int'l, Generic and Brand
RX List

Street Drug Slang


Insulin information

History of Insulin

Types of Insulin


Drugs prescribed for endocrine problems include the following:

androgen, antiandrogen, gonadotropin, corticosteroid, growth hormone, insulin, antidiabetic (sulfonylurea, biguanide/metformin, thiazolidinedione, insulin), thyroid hormones, antithyroid drugs, calcitonin, diphosponate, vasopressin analogues


References

Article Source:  Wikipedia.com (our edited version, reprinted with permission)

Lebovitz HE. Therapy for Diabetes Mellitus and Related Disorders. 4th edition. Alexandria:American Diabetes Association, 2004.

Holland, Norman & Adams, Michael Patrick. Core Concepts in Pharmacology. Pearson Education, Inc. New Jersey. 2003.

Salpeter SR, Greyber E, Pasternak GA, Salpeter EE. Risk of fatal and nonfatal lactic acidosis with metformin use in type 2 diabetes mellitus. Arch Intern Med 2003;163:2594-602. PMID 14638559.

UK Prospective Diabetes Study (UKPDS) Group. Effect of intensive blood-glucose control with metformin on complications in overweight patients with type 2 diabetes (UKPDS 34). Lancet 1998;352:854-65. PMID 9742977.

Witters LA. The blooming of the French lilac. J Clin Invest 2001;108:1105-1107. DOI 10.1172/JCI200114178.

Zhou G, Myers R, Li Y, Chen Y, Shen X, Fenyk-Melody J, Wu M, Ventre J, Doebber T, Fujii N, Musi N, Hirshman MF, Goodyear LJ, Moller DE. Role of AMP-activated protein kinase in mechanism of metformin action. J Clin Invest 2001;108:1167-1174. DOI 10.1172/JCI200113505.

 

 

islets of hope diabetes medical library                                          main Treatment Options page
Treatment options - diabetes medications

Diabetes medications by drug classification


Mini site index
Anti-diabetes drugs
Alpha glucosidase inhibitors
Biguanides
Incretin mimetic
Meglitinides
Oral Insulin
Sulfonylureas
Thiazolidinediones
Experimental agents

Also, see
Diabetes Medications for individual drug information
BYETTA (exenatide)

Types of insulin
   

   


Anti-diabetes drugs

An anti-diabetic drug or oral hypoglycemic agent is used to treat diabetes mellitus. They usually work by lowering the glucose levels in the blood. There are different types of anti-diabetic drugs, and their use depends on the nature of the diabetes, age and situation of the person, as well as other factors.

Insulin and exenatide are the only non-oral antidiabetic drugs. Insulin is the mainstay of treatment in Type I diabetes, in which insulin production is impaired. In Type II diabetes, Insulin is used when oral medication has become ineffective. Exenatide is a new injectible medication approved in 2005 in the US by the FDA to treat diabetes mellitus type 2.  


Incretin mimetic

Exenatide (also Exendin-4, marketed as Byetta) is the first of a new class of medications approved for the treatment of type 2 diabetes. It is to be used in conjunction with oral medications such as metformin and/or a sulfonylurea to improve glucose control. The medication is injected twice per day using a specially designed pen. The typical human response is both an improvement of the release of internal insulin by the pancreas and suppression of pancreas glucagon release, behaviors more typical of individuals without blood sugar control problems. In the presence of exenatide, these responses are greater when the blood sugar is elevated.  Also, see our complete section on BYETTA.  

   


Sulfonylureas

Sulfonylurea derivatives are a class of antidiabetic drugs that are used in the management of diabetes mellitus type 2 ("adult-onset"). They act by increasing insulin release from the beta cells in the pancreas.  Sulfonylureas were the first widely used oral hypoglycemic medications. They are insulin secretagogues, triggering insulin release by direct action on the KATP channel of the pancreatic beta cells.

Sulfonylureas bind strongly to plasma proteins. Sulfonylureas are only useful in type II diabetes, as they work by stimulating endogenous release of insulin. They work best with patients over 40 years old, who have had diabetes mellitus for under ten years. They can not be used with type I diabetes, or diabetes of pregnancy. They can be safely used with biguanides and glitazones. The toxicity of these drugs on the whole is relatively low.

Seven types of these pills have been marketed in North America. Four, known as "first-generation" drugs, have been in use for some time, but not all remain available. Seven "second-generation" drugs, are now more commonly used. They are stronger than first-generation drugs and have fewer side effects.

Members in this class include:

  • First-generation agents
    • Tolbutamide (Orinase)
    • Acetohexamide (Dymelor)
    • Tolazamide (Tolinase)
    • Chlorpropamide (Diabinese)
  • Second-generation agents
    • Glipizide (Glucotrol)
    • Glyburide (Diabeta, Micronase, Glynase)
    • Glimepiride (Amaryl)
    • Gliclazide
    • Glibenclamide
    • Glimepiride
    • Gliquidone

   


Meglitinides

Meglitinides are related to sulfonylureas. The amplification of insulin release is shorter and more intense, and they are take with meals to boost the insulin response to each meal.

Members of the class include:

  • Repaglinide (Prandin) - The max dosage is 16mg/day. Take this drug 0 to 30 minutes prior before eating a meal. If a meal is skipped, then the medication should also be skipped.
  • Nateglinide (Starlix) - The max dosage is 360 mg/day, usually 120 mg three times a day (TID). It also follows the same recommendations as Repaglinide.

Adverse reactions include weight gain and hypoglycemia.

   


Biguanides

Biguanides reduce hepatic glucose output. Although it must be used with caution in patients with impaired liver or kidney function, metformin (Glucophage) has become the most commonly used agent for type 2 diabetes in children and teenagers.  It is also used in the treatment of insulin resistance and polycystic ovarian syndrome (PCOS).

  • Metformin (Glucophage)
  • Phenformin (DBI): used in 1960-1980s, withdrawn due to lactic acidosis risk.

History

The class of biguanide originates from the French lilac (Galega officinalis), a plant known for several centuries to improve the symptoms of diabetes mellitus (Witters 2001).

   


Thiazolidinediones

Thiazolidinediones, also known as "glitazones," bind to PPARγ, a type of nuclear regulatory protein involved in transcription of numerous genes regulating glucose and fat metabolism. They act as "insulin sensitizers" without increasing insulin secretion.  The medication class of thiazolidinedione was introduced in the late 1990s as an adjunctive therapy for diabetes mellitus (type II) and related diseases.

Members of the class include:

Troglitazone (sold under the name Rezulin) was withdrawn from the market due to an increased incidence of drug-induced hepatitis in patients who were using the drug. It is now common practice that liver enzymes are monitored during the first year of treatment with the "newer" thiazolidinediones.

Experimental agents include MCC-555, a powerful antidiabetic agent and the early non-marketed thiazolidinedione ciglitazone.

There is now some interest in the partial PPAR gamma activators, telmisartan, which may provide similar benefits to the thiazolidinediones, but without the side effects associated with this class of drugs.

Uses

The only registered use of the thiazolidinediones is in diabetes mellitus type 2.

It is being investigated experimentally in polycystic ovary syndrome (PCOS) and non-alcoholic steatohepatitis (NASH).

Several forms of lipodystrophy cause insulin resistance, which has responded favorably to thiazolidinediones.

Side-effects and contraindications

The withdrawal of troglitazone has led to concerns of other thiazolidinediones increasing the risk of hepatitis. Guidelines now mention that for the first year of thiazolidinedione therapy, a two- or three-monthly check of liver enzymes is conducted to ascertain that no liver damage is occurring.

The main side-effect of all thiazolidinediones is fluid retention, leading to edema and potentially aggravating heart failure. Therefore, thiazolidinediones cannot be prescribed in patients with decreased ventricular function (NYHA grade III and IV heart failure).

   


Alpha glucosidase inhibitors

Alpha glucosidase inhibitors are "diabetes pills" but not technically hypoglycemic agents because they do not have a direct effect on insulin secretion or sensitivity. These agents slow the digestion of starch in the small intestine, so that glucose from the starch of a meal enters the bloodstream more slowly, and can be matched more effectively by an impaired insulin response or sensitivity. These agents are effective by themselves only in the earliest stages of impaired glucose tolerance, but can be helpful in combination with other agents in type 2 diabetes.

These medications are rarely used in the United States because of the severity of their side effects (flatulence and bloating). They are more commonly prescribed in Europe.

   


Experimental agents

Many other potential drugs are currently in investigation by pharmaceutical companies. Some of these are simply newer members of one of the above classes, but some work by novel mechanisms. For example, at least one compound that enhances the sensitivity of glucokinase to rising glucose is in the stage of animal research.  

   


Oral insulin

The basic appeal of oral hypoglycemic agents is that most people would prefer a pill to an injection. Unlike all the oral drugs described in this article, insulin is a protein. Protein hormones, like meat proteins, are digested in the stomach and gut.

However, the potential market for an oral form of insulin is enormous and many laboratories have attempted to devise ways of moving enough intact insulin from the gut to the portal vein to have a measurable effect on blood sugar. One can find several research reports over the years describing promising approaches or limited success in animals, and limited human testing, but as of 2004, no products appear to be successful enough to bring to market.

 

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Page Updated 09/02/2006