Insulin Secretagogues

Insulin secretagogues cause the pancreas to secret insulin

Insulin secretagogues are those drugs or things that when present in the body, will cause the pancreas to secret insulin.

Diabetes is a disease which is characterized by an unregulated level of blood sugar. Two hormones which regulate the level of blood glucose are insulin and glucagon. In the case of diabetes, insulin regulation of blood sugar is not working properly. The person might have smaller amounts of insulin released from the pancreas. Another option is that tissues in the human body do not react to normal levels of glucose. Both of these mechanisms lead to increased blood sugar levels.

There are several types of drugs for diabetes treatment. Insulin secretagogues are a type of insulin drugs which increase the release of insulin from the pancreas. These secretagogues bind to the pancreas cells and stimulate them to release insulin in higher concentration. There are two types of insulin secretagogues drugs which are FDA approved, sulfonylureas (SFUs) and glinides.


Sulfonylureas were first drugs for diabetes treatment. They are divided into two generations. Tolbutamide and Chlorpropamide are representatives of first generation of sulfonylureas. Second generation are Glibenclamide, Glipizide, Gliclazide, Gliquidone, and Loperamide. They absorb very well in gastrointestinal tract after intake. Sulfonylureas treat diabetes using several mechanisms. They work as secretagogues and increase release of insulin from pancreas cells. They do not increase insulin synthesis, they only help in releasing already formed insulin. But also they decrease level of serum glucagon which prevents glucose synthesis and release. Another mechanism is increasing the response of body tissues and organs on insulin. On that way they will take the excess of glucose and decrease glucose serum level. 

The side effect of tolbutamide is skin rash and symptoms of low blood sugar. Another side effects of sulfonylurea are redness of the face, thrombocytopenia, leukopenia, weight gain. They should be avoided in case you have liver or kidney damage.


Glinides are the second category of insulin secretagogues. Repaglinide and nateglinide are representatives of glinides.They work quickly after taking them, so it is important to take them right before a meal. If you take insulin secretagogues and skip a meal you are risking to get symptoms of low blood sugar (hypoglycemia). The most common symptoms are dizziness, confusion, hunger, shaky hands. The secretagogues can also be combined with other types of diabetes drugs. 

They are medicines which are capable of reducing glucose serum level effectively and quickly. However, they should be used with precaution because of their capability to cause lowering of glucose serum level quickly and cause symptoms of low blood sugar.

Other categories of drugs

Dipeptidyl peptidase 4 inhibitors - DPP-4s (saxagliptin, sitagliptin, linagliptin) stimulate the release of insulin from pancreatic cells. They are used together with other types of diabetes medicines. They are also easy to use, because they can be taken as a pill. On the other hand, using of Incretin mimetics is a bit more complicated because they are used as injections. They are also combined with other diabetes medications. Agonists at the Glucagon-Like Peptide-1 Receptor act as a incretin. They will increase secretion of insulin by stimulating pancreatic beta cells. This type of medicines will work only in presence of glucose. They will also decrease the release of glucagon.

Sodium-glucose transporter 2 inhibitors - SGLT2s (canagliflozin - Invokana) is also used as injections and in combination with other drugs. Amylin mimetics increase the release of insulin and it is used together with insulin. The downside of amylin mimetics is that they are used as injections.

Thiazolidinediones are a group pf medicine which are used for treatment of insulin resistance. But it will also stimulate pancreatic beta cells. 

Natural Insulin Secretagogues

Besides these two categories of drugs, there are natural remedies which help in insulin release. Their usage is widely spread in some cultures, especially in Asia and Africa. Research have found that some plants stimulate insulin secretion. Babhul or Acacia arabica causes hypoglycemic effects. It can be used in form of powdered seed. Garlic is a herb which is commonly used worldwide. It has many positive effect on human health. One of them is hypoglycemic effect. Garlic stimulates release of insulin from beta cells of pancreas. Garlic has also significant positive effect on reducing levels of cholesterol. Indian gooseberry, also known as jamun is another natural remedy which increases the release of insulin from the pancreas. Seeds and pulp are commonly used. For seeds it takes longer period of time (24 hours) to start with hypoglycemic effect. Fenugreek is another herb which stimulates secretion of insulin from pancreatic cells. It is widely spread in southeast Asia and it is used in form of plant extract.


Insulinoma is benign tumor of the pancreas. They are built out of pancreatic beta cells which produce insulin. Patients which suffer from insulinoma will have an extra amount of insulin in their blood. Their main complaints will be the symptoms of hypoglycemia.


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