Linagliptin (Oral)

Used to reduce blood sugar levels, Linagliptin increases the production of insulin in the pancreas and is used to treat patients who have been diagnosed with type 2 diabetes mellitus.

Overview

Produced by the pancreas, insulin is a hormone which is responsible for the metabolism of fats, proteins and carbohydrates. In order to facilitate this, insulin absorbs glucose and other substances from the patient's blood into specific organs. However, patients with type 2 diabetes do not have sufficient insulin levels in their system. As a result, their blood glucose can reach an abnormally high level and may result in side effects occurring.

Although type 2 diabetes tends to start gradually, symptoms can include fatigue, increased thirst, frequent urination, weight loss, itching of the skin and/or blurred vision. If left untreated, diabetes mellitus can cause serious complications, such as kidney disease, macrovascular problems, diabetic neuropathy and/or diabetic retinopathy. In some cases, untreated diabetes can result in blindness and limb amputations.

When patients are first diagnosed with type 2 diabetes, they may be advised to control their symptoms by making dietary and lifestyle changes. If patients are consuming excessive amounts of sugar, for example, their natural levels of insulin may be unable to process large amounts of glucose effectively. By making changes to their diet and increasing the amount of exercise they do, patients can often control type 2 diabetes well.

If the patient's condition cannot be controlled by dietary and lifestyle changes alone, their hormone levels can be supplemented with a synthetic form of insulin. Alternatively, medications, such as Linagliptin, can be used to reduce the patient's blood glucose levels.

As a dipeptidyl peptidase-4 (DDP-4) inhibitor, it ensures that a hormone, known as incretin, remains in the bloodstream. When incretin is present in the bloodstream, it causes the pancreas to produce more insulin. In addition to this, Linagliptin causes the release of glucagon from the pancreas to be staggered which, in turn, prevents the patient's blood sugar levels from increasing so dramatically.

Although Linagliptin can be used to treat patients with type 2 diabetes, it is ineffective in treating type 1 diabetes. As patients with type 1 diabetes are unable to produce insulin at all, their natural levels of insulin cannot be increased by using a DDP-4 inhibitor and synthetic insulin is required. In cases of type 2 diabetes, however, Linagliptin can be used to increase the levels of naturally produced insulin and to lower the amount of glucose in the patient's blood.

Once the patient's condition is being managed with Linagliptin, the symptoms associated with type 2 diabetes should be relieved. In addition to this, the risk of potential complications arising from type 2 diabetes should be reduced.

Whilst Linagliptin is an effective treatment for type 2 diabetes, it is most effective when it is used in conjunction with dietary and lifestyle changes. If patients are able to enact these changes and adhere to a regular dosing schedule, Linagliptin may be used to manage the patient's condition on a long-term basis.

Conditions Treated

Type 2 diabetes mellitus

Type Of Medicine

Dipeptidyl peptidase-4 (DDP-4) inhibitor

Side Effects

Like most medications, Linagliptin can cause some patients to experience side effects. When patients first start taking Linagliptin, for example, they may notice the following adverse effects:

  • Sore throat
  • Diarrhea
  • Muscle aches
  • Runny or stuffy nose

The above side effects occur most commonly when patients first start using Linagliptin but often decrease over time. If the side effects are mild and short-lived, patients may not require additional medical treatment. However, if the side effects are severe or continuous, patients should obtain medical advice.

Patients will also need to consult their physician straight away if they experience the following side effects when taking Linagliptin:

  • Anxiety
  • Fever
  • Blurred vision
  • Slurred speech
  • Chills
  • Shakiness
  • Cold sweats
  • Seizures
  • Coma
  • Nightmare
  • Confusion
  • Pale, cool skin
  • Nausea
  • Depression
  • Increased hunger
  • Dizziness
  • Headache
  • Fast heartbeat
  • Unusual weakness and tiredness
  • Constipation
  • Bloating
  • Hives, itching or welts
  • Cough
  • Rash on the skin
  • Large, hive-like swelling on the eyelids, tongue, lips, hands, throat, feet, legs or sex organs
  • Pains in the side, abdomen or stomach, may radiate to the back
  • Severe joint pain
  • Loss of appetite
  • Swelling or puffiness around the face, lips, tongue, eyes or of the eyelids
  • Redness of the skin

If patients experience any side effects which are not listed above when using Linagliptin, they should also obtain medical advice.

Dosage

When adult patients are prescribed Linagliptin for the treatment of type 2 diabetes, they are usually advised to take 5mg per day. However, the patient's dose will depend on a number of factors and may be modified by their doctor. In most cases, patients can take Linagliptin with or without food.

As the effects of Linagliptin have not been specifically tested on pediatric patients, children and infants may not be prescribed Linagliptin, even if they have been diagnosed with type 2 diabetes.

It is essential that patients follow a treatment schedule when taking Linagliptin and that they only use the amount of medication which has been prescribed to them. Taking too much Linagliptin, using Linagliptin too often or missing doses of Linagliptin can cause the patient's blood sugar levels to increase or decrease dramatically and the patient may suffer serious side effects as a result.

When patients are prescribed Linagliptin, they are often instructed to adhere to a specific diet plan as well. Patients will need to use the diet plan which has been prescribed to them in order for Linagliptin to be fully effective. Similarly, patients should exercise as their doctor has instructed them to in order for Linagliptin to work properly.

In addition to taking Linagliptin, patients may be advised to test their blood and/or urine sugar levels on a regular basis.

If patients forget to take a dose of Linagliptin, they should take the missed dose as soon as they remember to. However, if their next dose is almost due, patients should skip the missed dose. Patients should not attempt to take an extra dose or a double dose of Linagliptin, even if an earlier dose has been missed.

If patients are unsure how or when to take Linagliptin, they should seek advice from their physician or pharmacist.

Potential Drug Interactions:

As Linagliptin can interact with some other drugs, using Linagliptin in conjunction with the following medications is not usually advisable:

  • Balofloxacin
  • Gatifloxacin
  • Besifloxacin
  • Lanreotide
  • Carbamazepine
  • Mitotane
  • Ciprofloxacin
  • Lomefloxacin
  • Efavirenz
  • Moxifloxacin
  • Pefloxacin
  • Enoxacin
  • Rufloxacin
  • Enzalutamide
  • Pasireotide
  • Sparfloxacin
  • Fleroxacin
  • Phenytoin
  • Thioctic Acid
  • Flumequine
  • Tipranavir
  • Prulifloxacin
  • Fosphenytoin
  • St John's Wort
  • Gemifloxacin
  • Rifabutin
  • Levofloxacin
  • Tosufloxacin
  • Nadifloxacin
  • Pazufloxacin
  • Norfloxacin
  • Primidone
  • Octreotide
  • Rifampin
  • Ofloxacin
  • Rifapentine
  • Oxcarbazepine

In some cases, however, doctors may deem it appropriate to treat the patient with Linagliptin and one of the medications listed above. If so, the patient's dose may be modified or they may be advised to take their medication at a specific time in order to reduce the risk of a drug interaction occurring.

If patients take Linagliptin alongside any of the following medicines, it may increase their risk of developing side effects:

  • Acebutolol
  • Pindolol
  • Atenolol
  • Penbutolol
  • Betaxolol
  • Practolol
  • Bisoprolol
  • Propranolol
  • Carteolol
  • Metoprolol
  • Carvedilol
  • Nebivolol
  • Celiprolol
  • Oxprenolol
  • Esmolol
  • Sotalol
  • Labetalol
  • Nadolol
  • Levobunolol
  • Timolol
  • Metipranolol

Before using Linagliptin, patients should tell their doctor if they are taking any other medicines, supplements or vitamins. Similarly, once patients have started to take Linagliptin, they should obtain medical advice before taking any new medicines, supplements or vitamins.

Warnings

If patients have any other medical conditions, they should inform their physician before Linagliptin is prescribed. Patients should also disclose their medical history to their current doctor before taking Linagliptin. There are some conditions which could affect treatment with this medication and they may include:

  • High levels of ketones and acid in the blood (Diabetic ketoacidosis)
  • Type 1 diabetes
  • Surgery
  • Infection
  • Fever
  • Trauma
  • High levels of triglycerides and fats in the blood (Hypertriglyceridemia)
  • Obesity
  • High levels of cholesterol in the blood (Hypercholesterolemia)
  • Problems with the pancreas

When patients are taking Linagliptin, they may suffer from pancreatitis. Patients should obtain immediate medical help if they develop the following symptoms:

  • Nausea
  • Sudden and severe stomach pain
  • Vomiting
  • Fever
  • Chills
  • Lightheadedness
  • Constipation
  • Loss of appetite

In some cases, Linagliptin could cause patients to develop low blood sugar (hypoglycemia). This is more likely if the patient misses meals, exercises more than usual, is unable to eat due to nausea or vomiting, drinks alcohol and/or takes certain other medications (including other diabetes medications). Symptoms of low blood sugar can include:

  • Blurred vision
  • Anxiety
  • Cold sweats
  • Behavioral changes (including appearing drunk)
  • Pale, cool skin
  • Confusion
  • Excessive hunger
  • Drowsiness
  • Fast heartbeat
  • Difficulty with thinking
  • Nausea
  • Headaches
  • Nervousness
  • Restless sleep
  • Nightmares
  • Shakiness
  • Unusual weakness or tiredness
  • Slurred speech

Although the above symptoms are commonly associated with low blood sugar, everyone can experience different symptoms of hypoglycemia. Patients should learn to recognize their own symptoms of low blood sugar so that they can take action if their blood sugar levels drop. Without effective treatment, low blood sugar can cause serious health problems, such as seizures and a loss of consciousness.

If patients are experiencing symptoms of low blood sugar, they can relieve them by doing any of the following:

  • Eating sugar cubes
  • Consuming a glucose tablet or gel
  • Drinking a non-diet soft drink
  • Dissolving sugar in water and drinking it
  • Drinking fruit juice
  • Consuming honey

When patients are experiencing low blood sugar, they should check their blood sugar levels and seek medical help if necessary. When patients are diagnosed with diabetes, they should be prescribed a glucagon kit. This is a medicine which can be used in emergencies and is normally administered when patients are suffering serious symptoms associated with low blood sugar. Patients should ensure that they carry the kit with them at all times and that they are aware of how to administer glucagon. Patients should also ensure that their family members and close friends are able to administer glucagon in the event of an emergency.

If patients forget to take Linagliptin, eat excessively, do less exercise than usual or have an infection or fever, they may develop high blood sugar (hyperglycemia). The symptoms of hyperglycemia can include:

  • Dry, flushed skin
  • Blurred vision
  • Fruit-like breath odor
  • Dry mouth
  • Increased urination
  • Drowsiness
  • Sleepiness
  • Loss of appetite
  • Stomachache
  • Nausea
  • Unusual thirst
  • Tiredness
  • Vomiting
  • Trouble breathing (may be deep and rapid)
  • Unconsciousness

If patients experience symptoms associated with high blood sugar, they should check their blood sugar levels and contact their physician for advice. If their physician is unavailable, patients should obtain medical advice from another healthcare practitioner.

When patients are prescribed Linagliptin, their doctor may advise them to wear a medical identification bracelet and to carry a medical identification card. This can provide emergency medical technicians with vital information in the event of an emergency.

In some cases, patients can suffer from severe and debilitating joint pain when taking Linagliptin. If patients develop joint pain or discomfort when using this medication, they should notify their physician straight away.

As a category B medicine in terms of pregnancy, patients who are pregnant may be able to take Linagliptin, although a risk of harm to the unborn fetus is still possible. As blood sugar levels can be more difficult to control during pregnancy, patients should be regularly monitored if they are pregnant.

If patients become pregnant when taking Linagliptin, they should notify their physician immediately.

It is not known if Linagliptin is excreted in breast milk or whether it poses a risk to infants if transferred in this way. Due to this, patients may be advised not breastfeed whilst taking Linagliptin and should obtain medical advice before doing so.

In rare cases, Linagliptin may cause patients to develop a serious allergic reaction, including anaphylaxis. A serious allergic reaction can be life-threatening and patients will require emergency medical treatment if they exhibit the following symptoms:

  • Rash on the skin
  • Itching
  • Difficulty swallowing
  • Difficulty breathing
  • Wheezing
  • Hoarseness
  • Swelling of the face, hands, mouth, lips, tongue or throat
  • Hives

Storage

As patients are usually advised to take Linagliptin on a daily basis, they will need to keep a supply of medication at home. However, patients should use caution when storing Linagliptin in the home and should ensure that children and/or pets cannot gain access to it.

In order to store Linagliptin properly, patients should follow the manufacturer's instructions and medication guidelines. In most cases, Linagliptin can be kept at room temperature but should be stored in a closed container. In addition to this, Linagliptin will need to be kept away from moisture, heat and light.

If patients are advised to stop taking Linagliptin or if the medication reaches its use-by date, patients should dispose of it carefully. Medication should not be discarded along with regular household waste as it may pose a risk to other people. Instead, patients should contact their physician's office or pharmacist and access a designated medicine disposal service.

Summary

Although type 2 diabetes can cause serious complications if it is uncontrolled, the condition can often be well-managed with various forms of treatment. If patients continue to exhibit high blood glucose levels, despite making lifestyle and dietary changes, Linagliptin may be used to lower their blood sugar levels.

By causing the pancreas to produce more insulin naturally, the patient's body is able to metabolize a larger amount of glucose and prevent glucose in the patient's blood from increasing to dangerous levels. When Linagliptin is used to increase natural insulin production, additional supplementation with synthetic insulin may not be necessary.

As a result, Linagliptin can be used to reduce the short-term symptoms associated with type 2 diabetes and to reduce the patient's risk of suffering additional health complications, such as kidney disease, diabetic retinopathy and/or diabetic neuropathy.