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BY Dr Truc |

January 30, 2023

DPP-4 Inhibitors: A Breakthrough in Diabetes Treatment?

DPP-4 Inhibitors - Diabetes Treatment Blog -FEATURE

Table of Contents

DPP-4 is a protein that is associated with type 2 diabetes. Studies have shown that people who have a higher level of this in their blood have a higher risk of developing the disease.

On the other hand, DPP-4 inhibitors are drugs that can lower the level of DPP-4 in your blood and may help prevent type 2 diabetes from developing.

Increasing numbers of people across the globe are suffering from type-2 diabetes mellitus. Diabetes is a serious disease affecting over 23 million American adults and children (roughly 8% of the total population).

What is DPP-4?

Dipeptidyl peptidase 4 (DPP-4) is an important enzyme that controls many body functions, such as eating, digestion, immune response, pain perception, and growth. This enzyme is present in all organs and the blood. It starts or stops these processes by removing two amino acid peptides from a variety of peptides and proteins.

DPP-4 Inhibitors - Diabetes Treatment Blog

What are DPP-4 inhibitors?

An oral diabetes drug class that is relatively new is the DPP-4 inhibitors. The drug is also referred to as gliptin and can be prescribed to diabetics who have failed to respond well to other diabetes medications, like metformin and sulphonylurea.

DPP-4 inhibitors are a class of prescription medicines used with diet and exercise to control high blood sugar in adults with type 2 diabetes. FDA-approved includes sitagliptin, saxagliptin, linagliptin, and alogliptin. They are available as single-ingredient products and in combination with other diabetes medicines such as metformin.

There are five DPP-4 inhibitors in the market today: sitagliptin, saxagliptin, linagliptin, alogliptin (in the United States and Europe), and vildagliptin (only available in Europe). Four more gliptins: teneligliptin, anagliptin, omarigliptin, and trelagliptin, are only approved in the Japanese and Korean markets.

Table of Comparison of currently marketed DPP-4 inhibitors

How do DPP-4 inhibitors work?

DPP-4 inhibitors work by raising levels of insulin after eating, which lowers blood sugar levels. An essential function of insulin is to transport sugar from the blood into the tissues, where it can produce energy and maintain blood sugar levels.

What is Type 2 diabetes?

Type 2 diabetes mellitus is a disorder that affects how your body uses glucose (sugar); it can also impact how it stores and processes other forms of energy such as fat.

All cells require sugar for your body to function normally, and insulin helps transport sugar into your cells. Type 2 diabetes occurs when the body stops responding to normal or even high insulin levels. Over time, the pancreas (an organ in the abdomen) cannot produce enough insulin. When you are overweight, especially if you have fat stored in your liver and stomach, your body requires more insulin. High blood sugar (glucose) levels can lead to serious complications if left untreated.

With lifestyle changes, type 2 diabetes can usually be controlled. However, some people also require medication.

Symptoms of Type 2 diabetes

Frequent thirst.

The kidneys work overtime to eliminate sugar when it builds up in the blood. The process causes your tissues to lose fluids, which makes you dehydrated, leading you to feel thirsty.

Constant hunger.

When you have diabetes, glucose can’t reach your cells, so you feel hungry even after eating.

Frequent urination.

When you have too much sugar in your system, your kidneys work to get rid of it, resulting in more frequent peeing.

Drying of the mouth.

Dehydration and frequent urination can also cause your mouth to dry out.

Losing weight without trying.

Besides losing sugar from peeing a lot, you also lose calories. This might lead to you losing weight even though you’re eating normally.

Fatigue

A body that can’t use food for energy may feel weak and tired. You may also feel this way if you’re dehydrated.

Blurred Vision

You may have trouble focusing when you have high blood sugar.

Loss of Consciousness

Your blood sugar levels could get too low after exercising, skipping a meal, or taking too many medications, and these could cause you to pass out.

A wound or infection that does not heal.

Your body may have difficulty healing when your blood sugar is high.

Red, swollen, tender gums.

You could develop infections in your gums, resulting in receding of the gumline. Your teeth may also become loose.

Man drinking water

Who should take DPP-4 inhibitors?

DPP-4 inhibitors are not considered initial therapy for most patients with type 2 diabetes. Initial therapy in most patients should begin with diet, weight reduction, exercise, and metformin (in the absence of contraindications).
  • DPP-4 inhibitors should not be used in place of metformin and sulphonylureas. Instead, they are best used together. It is considered an add-on drug therapy for patients who are inadequately controlled on metformin, a thiazolidinedione, or sulfonylurea.
  • In patients with kidney disease or diabetes, DPP-4 inhibitors are not recommended.
  • People with type 2 diabetes are prescribed this as a second or third line of treatment.
  • Certain medications include antibiotics, antifungals, antiplatelets, proton pump inhibitors (PPIs), selective serotonin reuptake inhibitors (SSRIs), thiazide diuretics, or warfarin, DPP-4 inhibitors can cause liver damage and death.

Benefits of DPP-4 inhibitors for treating diabetes

DPP-4 inhibitors work by blocking the action of DPP-4, an enzyme that destroys the hormone incretin. Incretin helps the body produce more insulin only when needed and reduces the amount of glucose produced by the liver when it is not required.

Potential benefits include:

  • Weight loss
  • Renoprotective effects
  • Decreasing blood glucose levels
  • Lowering of BP
Old woman with a wound

What are the side effects of DPP-4 inhibitors?

  1. Healthcare professionals should consider DPP-4 inhibitors as a possible cause of severe joint pain, and discontinue the drug if necessary.
  2. When type 2 diabetes occurs in adults, diet and exercise are used along with DPP-4 inhibitors to lower blood sugar levels. Type 2 diabetes can lead to severe complications, including blindness, damage to nerves and kidneys, and heart disease.
  3. Other ‌side effects, besides severe joint pain, include inflammation of the pancreas, low blood sugar when combining this class of medicines with other prescription medicines prescribed to treat diabetes, and allergic reactions.
  4. The most common adverse reactions occurring in 5% of patients after taking DPP-4 inhibitors were: upper respiratory tract infection, nasopharyngitis, headache with sitagliptin and upper respiratory tract infection, urinary tract infection, and headache with saxagliptin.
  5. The most common adverse reactions occurring in 5% of patients after taking DPP-4 inhibitors were: upper respiratory tract infection, nasopharyngitis, headache with sitagliptin and upper respiratory tract infection, urinary tract infection, and headache with saxagliptin.

How do DPP-4 inhibitors treat type 2 diabetes?

This class of medicines, dipeptidyl peptidase-4 (DPP-4) inhibitors, includes sitagliptin (brand name: Januvia), saxagliptin (brand name: Onglyza), linagliptin (brand name: Tradjenta), alogliptin (brand name: Nesina), and vildagliptin (brand name: Galvus). Vildagliptin is available in some countries but not in the United States.

These medicines lower blood sugar levels by increasing the amount of insulin being released from the pancreas after eating a meal. They can be given alone to people who cannot tolerate the first-line medicine (metformin) or other medicines. They can be given together with other oral medications if blood sugar levels are still higher than the goal. These medicines do not cause hypoglycemia or changes in body weight. There have been rare reports of joint pain, pancreatitis, and severe skin reactions. DPP-4 inhibitors are expensive.

Takeaway

DPP-4 inhibitors are a type of oral medication used in the treatment of type 2 diabetes. These drugs work by increasing the levels of active incretins in the body, which in turn helps to regulate insulin secretion and glucose levels. DPP-4 inhibitors have been shown to be effective and well-tolerated in clinical trials, and they offer a safe and convenient alternative to traditional diabetes medications.