Home Medicines Sitagliptin: effect, areas of application, side effects

Sitagliptin: effect, areas of application, side effects

by Josephine Andrews
Published: Last Updated on 384 views

Sitagliptin belongs to the class of oral antidiabetics. As a so-called DPP-4 inhibitor, the active ingredient blocks the enzyme dipeptidyl peptidase-4. This indirectly increases the release of the blood sugar-lowering hormone insulin. This benefits people whose body cells respond less to normal insulin levels or whose body releases too little insulin after a meal. Here you can read everything interesting about sitagliptin: effect, application and possible interactions and side effects.

How sitagliptin works

DPP-4 inhibitors such as sitagliptin inhibit the enzyme dipeptidyl peptidase-4 and in this way indirectly stimulate the release of insulin if carbohydrates are supplied with food (food-dependent effect). Because of this mechanism of action, sitagliptin, like other DPP4 inhibitors, very rarely leads to hypoglycaemia .

After eating, the ingested food is broken down into its building blocks in the gastrointestinal tract, including sugar. This is absorbed into the blood via the intestinal mucosa – the blood sugar level rises. As a result, the pancreas releases insulin. The hormone causes the body’s cells to absorb sugar from the blood in order to use it for energy production. This is how the blood sugar level drops again.

As early as the middle of the last century, the assumption was made that the body releases insulin via a signal from the intestine before the sugar is absorbed into the blood. This effect probably serves to prepare the body for a quick utilization of the incoming sugar and thus to avoid high blood sugar spikes.

The assumption was confirmed with the discovery of the so-called incretin effect. The incretin effect describes that the cells of the mucous membrane of the small intestine release a peptide hormone into the blood during the passage of food, which causes insulin to be released even before a large part of the food components have been absorbed into the blood.

The two hormones “glucose-dependent insulinotropic peptide” (GIP) and “glucagon-like peptide 1” (glucagon-like peptide, GLP-1) are mainly responsible for this . These hormones are secreted by the intestines and stimulate the production of insulin in the pancreas. However, they are broken down again after just a few minutes and thus lose their effect.

In type 2 diabetics , the amount of insulin released is relatively too small to keep blood sugar levels under control. Sitagliptin blocks the enzyme that breaks down GLP-1, called dipeptidyl peptidase-4. GLP-1 can therefore have a longer effect – the insulin release lasts longer, so that the blood sugar level in diabetics, which is elevated after a meal, can normalize again.

intake, degradation and excretion

Once ingested, sitagliptin is rapidly absorbed in the gut, reaching peak blood levels in one to four hours. It is hardly broken down in the body and is mostly excreted unchanged in the urine. After an average of eight to 14 hours, half of the administered amount of active substance has left the body again.

When is sitagliptin used?

The oral antidiabetic sitagliptin is approved for type 2 diabetics for whom a change in eating habits and increased exercise are not enough to improve blood sugar levels .

The drug can be used on its own (monotherapy) or in combination with one or two other oral blood glucose -lowering drugs (e.g. metformin and/or an SGLT-2 inhibitor such as ertugliflozin and/or a sulfonylurea such as glibenclamide ).

If multiple therapy cannot lower blood sugar sufficiently, sitagliptin can also be combined with insulin injections.

Since diabetes is a long-term condition, oral antidiabetic drugs such as sitagliptin must be taken continuously.

How sitagliptin is used

Sitagliptin is taken as a tablet once a day with a glass of water and with or without food. Usually, adults take 100 milligrams of sitagliptin once a day in the morning.

If you forget a pill, you can take it later on the same day. If you only notice the missed dose the next day, you should continue with the normal daily dosage and never take two tablets at the same time.

In moderate to severe renal impairment, the elimination of sitagliptin may be impaired. The active ingredient can then accumulate in the body. The doctor will therefore adjust the dosage of the drug accordingly.

What are the side effects of sitagliptin?

During therapy with sitagliptin, symptoms such as headaches and low blood sugar levels affect up to one in ten to a hundred people. Dizziness and constipation also occasionally occur with sitagliptin.

If other drugs that affect blood sugar levels are taken in addition to sitagliptin, other digestive tract symptoms are possible, such as diarrhea, vomiting, nausea, flatulence and dry mouth. Taking sulfonylureas or insulin at the same time increases the likelihood of low blood sugar.

Acute inflammation of the pancreas (pancreatitis) can occur in rare cases during treatment with sitagliptin. Possible signs of this are sudden onset and persistent severe abdominal pain that radiates in the form of a belt to the back.

If you experience such symptoms, you should consult a doctor.

What should be considered when taking sitagliptin?


Sitagliptin should not be taken if there is a known hypersensitivity to the active ingredient.


The antidiabetic sitagliptin shows hardly any relevant interactions with other drugs.

Combining sitagliptin with the heart drug digoxin can slightly increase its blood levels. Since digoxin has a narrow therapeutic window (ie can become rapidly toxic in the event of an overdose), the patient may need to be closely monitored.

Sitagliptin can cause low blood sugar (hypoglycaemia) . The signs of this (such as cold sweats, tremors, feeling unwell) may be masked by beta-blockers taken at the same time (e.g. for high blood pressure).

age restriction

Sitagliptin is approved for the monotherapy or combination therapy of type 2 diabetes from the age of 18 years.

pregnancy and breast feeding period

To be on the safe side, pregnant and breastfeeding women should not take sitagliptin, as the safety and benefits of an application have not been sufficiently documented.

Insulin is the drug of choice for diabetes that requires medical treatment during pregnancy and breastfeeding.

How to get sitagliptin medication

Drugs with the active ingredient sitagliptin require a prescription in Germany, Austria and Switzerland in any dosage and pack size and are therefore only available in pharmacies upon presentation of a doctor’s prescription.

Since when is sitagliptin known?

Since the discovery of the GLP-1-degrading enzyme DPP-4 in 1967, there have been suggestions that inhibiting this enzyme could have a positive effect on the blood sugar levels of type 2 diabetics. The first DPP-4 inhibitors were discovered in the late 1980s and 1990s.

Since then, work has been done to optimize the effect of these drugs. Sitagliptin was developed from 1999 and approved in the USA in 2006 and in Germany in 2007.

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