Linagliptin

Generic name: linagliptin
Brand name: Tradjenta
Dosage form: oral tablet (5 mg)
Drug class: Dipeptidyl peptidase 4 inhibitors

Medically reviewed by  A Ras MD.

What is linagliptin used for?

Linagliptin is a prescription medicine that is used to lower blood sugar in patients with high blood sugar (diabetes).

Description

GLYXAMBI tablets for oral use contain: empagliflozin and linagliptin.

 

Empagliflozin

Empagliflozin is an inhibitor of the sodium-glucose co-transporter 2 (SGLT2).

The chemical name of empagliflozin is D-Glucitol,1,5-anhydro-1-C-[4-chloro-3-[[4-[[(3S)-tetrahydro-3-furanyl]oxy]phenyl]methyl]phenyl]-, (1S).

The molecular formula is C23H27ClO7 and the molecular weight is 450.91. The structural formula is:

Chemical Structure

Empagliflozin is a white to yellowish, non-hygroscopic powder. It is very slightly soluble in water, sparingly soluble in methanol, slightly soluble in ethanol and acetonitrile, soluble in 50% acetonitrile/water, and practically insoluble in toluene.

 

Linagliptin

Linagliptin is an inhibitor of the dipeptidyl peptidase-4 (DPP-4) enzyme.

The chemical name of linagliptin is 1H-Purine-2,6-dione, 8-[(3R)-3-amino-1-piperidinyl]-7-(2-butyn-1-yl)-3,7-dihydro-3-methyl-1-[(4-methyl-2-quinazolinyl)methyl]-

The molecular formula is C25H28N8O2 and the molecular weight is 472.54. The structural formula is:

Chemical Structure

Linagliptin is a white to yellowish, not or only slightly hygroscopic solid substance. It is very slightly soluble in water. Linagliptin is soluble in methanol, sparingly soluble in ethanol, very slightly soluble in isopropanol, and very slightly soluble in acetone.

 

GLYXAMBI

GLYXAMBI tablets are available in two dosage strengths containing 10 mg or 25 mg empagliflozin in combination with 5 mg linagliptin. The inactive ingredients of GLYXAMBI are the following: Tablet Core: mannitol, pregelatinized starch, corn starch, copovidone, crospovidone, talc and magnesium stearate. Coating: hypromellose, mannitol, talc, titanium dioxide, polyethylene glycol and ferric oxide, yellow (10 mg/5 mg) or ferric oxide, red (25 mg/5 mg).

Mechanism of Action

GLYXAMBI

GLYXAMBI contains: empagliflozin, a sodium-glucose co-transporter 2 (SGLT2) inhibitor, and linagliptin, a dipeptidyl peptidase-4 (DPP-4) inhibitor.

Empagliflozin

Sodium-glucose co-transporter 2 (SGLT2) is the predominant transporter responsible for reabsorption of glucose from the glomerular filtrate back into the circulation. Empagliflozin is an inhibitor of SGLT2. By inhibiting SGLT2, empagliflozin reduces renal reabsorption of filtered glucose and lowers the renal threshold for glucose, and thereby increases urinary glucose excretion.

Linagliptin

Linagliptin is an inhibitor of DPP-4, an enzyme that degrades the incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). Thus, linagliptin increases the concentrations of active incretin hormones, stimulating the release of insulin in a glucose-dependent manner and decreasing the levels of glucagon in the circulation. Both incretin hormones are involved in the physiological regulation of glucose homeostasis. Incretin hormones are secreted at a low basal level throughout the day and levels rise immediately after meal intake. GLP-1 and GIP increase insulin biosynthesis and secretion from pancreatic beta cells in the presence of normal and elevated blood glucose levels. Furthermore, GLP-1 also reduces glucagon secretion from pancreatic alpha cells, resulting in a reduction in hepatic glucose output.

Before taking linagliptin, tell your doctor:

  • If you are allergic to linagliptin; any part of this medicine; or any other drugs, foods, or substances. Tell your doctor about the allergy and what signs you had.
  • If you have any of these health problems: Acidic blood problem or type 1 diabetes.

This is not a list of all drugs or health problems that interact with linagliptin.

Tell your doctor and pharmacist about all of your drugs (prescription or OTC, natural products, vitamins) and health problems. You must check to make sure that it is safe for you to take linagliptin with all of your drugs and health problems. Do not start, stop, or change the dose of any drug without checking with your doctor.

What are some things I need to know or do while I take linagliptin?

  • Tell all of your health care providers that you take linagliptin. This includes your doctors, nurses, pharmacists, and dentists.
  • Do not drive if your blood sugar has been low. There is a greater chance of you having a crash.
  • Check your blood sugar as you have been told by your doctor.
  • Have blood work checked as you have been told by the doctor. Talk with the doctor.
  • It may be harder to control blood sugar during times of stress such as fever, infection, injury, or surgery. A change in physical activity, exercise, or diet may also affect blood sugar.
  • Talk with your doctor before you drink alcohol.
  • Follow the diet and workout plan that your doctor told you about.
  • Tell your doctor if you are pregnant, plan on getting pregnant, or are breast-feeding. You will need to talk about the benefits and risks to you and the baby.

How is linagliptin best taken?

Use linagliptin as ordered by your doctor. Read all information given to you. Follow all instructions closely.

  • Take with or without food.
  • Keep taking linagliptin as you have been told by your doctor or other health care provider, even if you feel well.

What do I do if I miss a dose?

  • Take a missed dose as soon as you think about it.
  • If it is close to the time for your next dose, skip the missed dose and go back to your normal time.
  • Do not take 2 doses at the same time or extra doses.

What are the side effects of linagliptin that I need to call my doctor about immediately?

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

  • Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
  • Low blood sugar can happen. The chance may be raised when linagliptin is used with other drugs for diabetes. Signs may be dizziness, headache, feeling sleepy or weak, shaking, fast heartbeat, confusion, hunger, or sweating. Call your doctor right away if you have any of these signs. Follow what you have been told to do for low blood sugar. This may include taking glucose tablets, liquid glucose, or some fruit juices.
  • Severe and sometimes deadly pancreas problems (pancreatitis) have happened with linagliptin. This could happen at any time during treatment. Signs of pancreatitis include very bad stomach pain, very bad back pain, or very upset stomach or throwing up. Call your doctor right away if you have any of these signs.
  • Drugs like this one may cause joint pain that can be very bad and disabling. Call your doctor right away if you have very bad joint pain or any joint pain that does not go away.
  • A skin reaction called bullous pemphigoid has happened with drugs like this one. Sometimes, people have had to go to the hospital. Call your doctor right away if you have blisters or if your skin starts to break down.
  • Heart failure has happened in people taking drugs like this one. Tell your doctor if you have ever had heart failure or kidney problems. Call your doctor right away if you feel very tired or you have shortness of breath, a big weight gain, or swelling in the arms or legs.

What are some other side effects of linagliptin?

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

  • Sore throat.
  • Runny or stuffy nose.
  • Cough.
  • Diarrhea.

These are not all of the side effects that may occur. If you have questions about side effects, call your doctor. Call your doctor for medical advice about side effects.

You may report side effects to the FDA at 1-800-332-1088. You may also report side effects at https://www.fda.gov/medwatch.

If overdose is suspected:

If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

How do I store and/or throw out linagliptin?

  • Store at room temperature.
  • Store in a dry place. Do not store in a bathroom.
  • Keep all drugs in a safe place. Keep all drugs out of the reach of children and pets.
  • Throw away unused or expired drugs. Do not flush down a toilet or pour down a drain unless you are told to do so. Check with your pharmacist if you have questions about the best way to throw out drugs. There may be drug take-back programs in your area.

Label

PRINCIPAL DISPLAY PANEL – 10 MG/5 MG BOTTLE LABEL

  • NDC 0597-0182-90
  • Glyxambi®
  • (empagliflozin and
    linagliptin tablets)
  • 10 mg/5 mg
  • DISPENSE WITH ACCOMPANYING MEDICATION GUIDE
  • 90 tablets
    Rx only
  • Boehringer
    Ingelheim
    Lilly
PRINCIPAL DISPLAY PANEL - 10 mg/5 mg Bottle Label

PRINCIPAL DISPLAY PANEL – 25 MG/5 MG BOTTLE LABEL

  • NDC 0597-0164-90
  • Glyxambi®
  • (empagliflozin and
    linagliptin tablets)
  • 25 mg/5 mg
  • DISPENSE WITH ACCOMPANYING MEDICATION GUIDE
  • 90 tablets
    Rx only
  • Boehringer
    Ingelheim
    Lilly
PRINCIPAL DISPLAY PANEL - 25 mg/5 mg Bottle Label

SRC: NLM .

 

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