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Oral Diabetic Medications

Posted on June 28, 2021 | No Comments on Oral Diabetic Medications

Type 2 diabetes mellitus is a blood sugar disorder due to a relative lack of insulin or the lack of insulin effectiveness, also known as insulin resistance, or both. Insulin is the hormone that lowers blood sugar. Patients with type 2 diabetes often respond well to oral medications, especially early in the disease process, unlike those with type 1 diabetes. As the disease progresses, the oral agents may become less and less effective and at some point the patient may require insulin therapy (injections). It is also possible to start treatment with insulin even in type 2 diabetes.

Contrary to what some people might think, the first drug to be effectively used for diabetes is not an oral agent, but rather, insulin. Oral antidiabetic agents currently available in the market can be broadly classified into three groups according to the mechanism of action. These can be given alone or in combination, or together with insulin. The first group of drugs works by increasing the amount of insulin released into the blood. These should be taken before a meal. It should be clarified that there is no change in the amount of insulin produced. There are two subgroups.

The sulfonylurea drugs comprise the first subgroup of insulin-releasers. Tolbutamide,introduced in 1956,was one of the earliest sulfonylureas. Other drugs in this category include chlorpropamide, glibenclamide (known as glyburide in the United States), glipizide, gliclazide, and glimepiride. Almost all of them have generic versions. Their most common adverse effect is hypoglycemia or low blood sugar. The second subgroup is known as the miglitinides (repaglinide and nateglinide), a drug class that was introduced in 1998. Because they are newer, they are more expensive. There is however, a lesser chance of hypoglycemia with miglitinides compared with sulfonylureas. In general, miglitinides have an earlier onset of action and shorter duration of action when compared with most sulfonylureas.

The second group of drugs works by increasing the effectiveness of insulin. These are called insulin sensitizers since they make the body more sensitive to the effects of insulin. There are again two subgroups. The first subgroup is the biguanides. There is only one drug in this subgroup, metformin, and generic preparations are common. Metformin has been in the market since the late 1970s. In addition to its effect on improving the body’s response to insulin, it also has some anorectic* effect and can cause weight loss. Adverse effects are usually gut-related, such as diarrhea and flatulence (stomach gas). Caution must be exercised if one has heart failure, liver or kidney disease.These conditions increase the production or decrease the elimination of acids, leading to the accumulation of acids in the body.

The second subgroup of insulin sensitizers is called thiazolidinediones (TZD). These drugs end with the suffix -glitazone. They act mainly by helping insulin function properly in the fat and muscle.They also help lower sugar production by the liver. Three drugs have been introduced since 1998, namely, troglitazone, rosiglitazone and pioglitazone. Unfortunately, troglitazone was withdrawn from the market because of unacceptable serious adverse effects on the liver. Although the two other TZDs are much less toxic to the liver, they still have to be monitored. Another known side effect is edema*. It can present as swelling of the legs, ankles and feet or as accumulation of fluid in the lungs, the latter being less common.

The third group of drugs is formed by the alpha-glucosidase inhibitors (AGI).There are two drugs in this class, acarbose and voglibose.They slow down the absorption of carbohydrates by the gastrointestinal tract*. The main side effect is also gastrointestinal, namely, flatulence (stomach gas). It must be emphasized that AGIs generally do not reduce the absorption of carbohydrates, just the rate of absorption. If one can temper the rise of blood glucose after a meal or postprandial glucose, the overall control of blood sugar will improve. The AGIs and the miglitinides generally help lower post-meal blood sugars. Both fasting and postprandial glucose are important in diabetes management.

Prior to the 1990s, there were only two classes of oral anti-diabetic agents, the sulfonylureas and biguanides. The available drugs have increased since that time. There are exciting drugs in the horizon – some oral, some injectible and others, inhaled. Diabetic patients can now lead near-normal lives. Not only is the choice of medications unprecedented, the availability of generic equivalents for some of these drugs have helped bring down the cost of diabetes care.

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