Sulfonylureas: Effects, Uses & Risks

The term sulfonylurea is used to describe various drugs that are used as part of a therapy for diabetes mellitus. Sulfonylureas are used as blood glucose-lowering agents in the control of type 2 of the disease. The drugs achieve this effect by increasing the secretion of insulin. Consequently, sulfonylureas are antidiabetic agents.

What are sulfonylureas?

Sulfonylureas are important antidiabetic agents used to control type 2 diabetes mellitus (often called sugar diabetes in common parlance). Use in type 1 is not indicated. The drugs should be distinguished from the group of glinides. Although these have a similar mechanism of action to sulfonylureas, they have important differences in terms of their action profile. In pharmacology and chemistry, sulfonylureas can be described by the molecular formula C 24 – H 3 – N 4 – O 5 – S . The standard application of sulfonylureas is the regulation of blood glucose levels. After ingestion, the drugs influence the insulin content so that a relevant lowering of blood glucose is achieved. Since sulfonylureas are only taken orally, they are considered oral antidiabetics. They play an important role in the course of therapy. In the Federal Republic of Germany and other EU countries, the drugs are subject to pharmacy and prescription requirements. Acquisition is thus possible only after prior prescription by a physician.

Pharmacological effects on the body and organs

Sulfonylureas act by stimulating the potassium channels of pancreatic beta cells, which increases their activity. This excitation results in increased production of insulin. Because of the increased insulin release, the insulin content in the blood increases, resulting in a noticeable lowering of blood glucose. Sulfonylureas are considered potassium channel blockers due to their influence on the potassium channel. The effects are achieved by mimicking an increased concentration of ATP. Since sulfonylurea only increases the body’s own production of insulin, the therapy requires a functioning pancreas. The treated person must still be able to produce sufficient amounts of insulin. Since the term sulfonylurea is a collective term under which various active ingredients are grouped, there are some differences between the individual substances. However, the differences are limited to the speed and duration of the onset of action. The most common sulfonylureas include the drugs gliclazide, tolbutamide, glimepiride, glibenclamide and glibornuride. Which agent is used is determined by the individual characteristics of each case.

Medical use and use for treatment and prevention.

The use of sulfonylureas has been well established in human medicine for the treatment of type 2 diabetes mellitus. The first preparations came on the market as early as 1956. Today, sulfonylureas are primarily used in monopreparations. These are drugs that rely exclusively or primarily on one active ingredient. However, a combination with other active ingredients such as metformin is also possible. Prescription is only for the treatment of type 2 diabetes, but the prerequisite is always that the pancreas must be able to function properly. Otherwise, other preparations must be administered. Sulfonylureas are taken orally in the form of film-coated tablets. Various preparations are on the market in the European Union. All sulfonylureas are subject to pharmacy and prescription requirements because of the risk of side effects. Consequently, they may only be purchased after a prescription has been issued in a licensed pharmacy. It is essential to follow the doctor’s instructions when taking the product. Thus, it may be necessary in particular to coordinate the intake of the preparations with the daily meals.

Risks and side effects

Sulfonylureas are not free of risks and side effects. However, safety of use is guaranteed unless there is a contraindication. This is the case, for example, during pregnancy and lactation. In such cases, they should not be taken. The same applies to patients with severe liver or kidney damage. There is also a contraindication in type 1 diabetes mellitus due to lack of efficacy.Since sulfonylureas have an effect on blood glucose levels, interactions with other medications must be taken into account. The attending physician must always be informed about all preparations taken. Adverse interactions are possible with oral contraceptives or thyroid hormones, for example. These lead to reduced efficacy. The effect of sulfonylureas can also be enhanced by taking beta blockers or insulin. Furthermore, interactions with thiazide diuretics, MAO inhibitors, salicylates and sulfonamides are possible. Furthermore, attention must be paid to side effects. Here, priority should be given to the possibility of hypoglycemia caused by the insulin. The likelihood of this side effect occurring is greater with substances with a long duration of action, such as glibenclamide, than with active substances with a short duration of action, such as tolbutamide. Other side effects of sulfonylureas include alcohol intolerance, gastrointestinal symptoms (nausea, vomiting, diarrhea), general malaise, and anemia. In addition, treatment with sulfonylureas usually results in weight gain of about 2 kg.