Diazoxide: Effects, Usage & Risks

Diazoxide is one of the most important derivatives of benzothiadiazine. The drug finds application as a potassium channel opener for the treatment of hypoglycemia and is taken orally in the form of capsules. The effects of diazoxide include inhibition of the release of insulin.

What is diazoxide?

Diazoxide is an important representative of the group of so-called antihypoglycemics. In human medical literature, this group includes various preparations or active substances that are prescribed for the treatment of a pathogenically decreased concentration of glucose in the blood (so-called hypoglycemia). Chemically, diazoxide is a derivative of benzothiadiazine. As such, diazoxide, also known as diazoxidum, has no diuretic effects. The lipophilic substance is described in pharmacology and chemistry by the molecular formula C 8 – H 7 – C – I – N 2 – O 2 – S . This corresponds approximately to a moral mass of 230.67 g/mol. At room temperature, diazoxide is present as a white crystalline powder. In preparations, the active medical ingredient is usually used in capsules that are taken orally by the patient independently. Preparations containing diazoxide are subject to pharmacy and prescription requirements in the European Union, so it is not permitted to purchase them on one’s own.

Pharmacologic effects on the body and organs

Diazoxide has a strong hyperglycemic effect. This means that the substance leads to increased blood sugar, thus avoiding hypoglycemia. Thus, the effect of diazoxide can be described as the counterpart of a hypoglycemic, or blood sugar-lowering, effect. Through many years of research, it has been proven that the hyperglycemic effects of diazoxide are due to an inhibition of insulin release. The drug can thus also be referred to as an insulin inhibitor. Also, diazoxide is considered a potassium channel opener. In addition, an increase in blood glucose levels is generally thought to have an association with insulin levels. This could be due to an increase in catecholamines.

Medical use and use for treatment and prevention.

Diazoxide is indicated for the treatment of hypoglycemia. In addition, the drug is also used in preparations for the treatment of glycogen storage disease, congenital leucine hypersensitivity, malignant hypertension, and renal insufficiency. Diazoxide is administered orally in the form of capsules and taken by the patient independently after prior prescription by a physician. In the European Union, diazoxide is subject to compulsory pharmacy and medicinal product regulations, which means that a doctor’s prescription is always required. The best-known preparations containing diazoxide include Proglicem (sold in Germany and Switzerland) and Proglycem (sold in the United States).

Risks and side effects

Taking diazoxide does not remain free of risks. The likelihood with which side effects may occur depends on the individual disposition of the patient as well as the particular drug being taken. The use of diazoxide must be completely discontinued if there is a contraindication. This is the case during pregnancy and lactation as well as in cases of cardiac insufficiency and after a heart attack. The drug must also not be administered in cases of known hypersensitivity to diazoxide, as the risks become uncontrollable. Adverse side effects of diazoxide that should be considered include skin reactions (e.g., rash, wheals, redness, or itching), increased blood cholesterol, and the development of dependence. Other undesirable side effects that may occur after taking diazoxide include fever, a general feeling of weakness or malaise, dizziness, restlessness, sleep disturbances, severe fatigue, headache as well as pain in the limbs. In addition, pancreatitis and cardiac arrhythmias are also possible. In addition, disorders of the gastrointestinal tract may occur. After taking diazoxide, these are mainly manifested by diarrhea, constipation, nausea and vomiting, loss of appetite, and abdominal pain.