Linagliptin — uses, dosing, side effects & the brands that sell it · pharmaranks
Linagliptin: uses, dosing, side effects & brands
Linagliptin is a dipeptidyl peptidase 4 inhibitor sold in the U.S. under 2 brand and generic names, for type 2 diabetes mellitus. Below: what the FDA label says, every product that contains it, what the pills look like, and its recall record.
By the pharmaranks editorial team·Reviewed against the FDA (openFDA label, NDC Directory & Enforcement) sources·How we research
Key facts
Drug class
Dipeptidyl Peptidase 4 Inhibitor
Treats
Type 2 Diabetes Mellitus
Available as
Tablet
Sold as
2 products — Tradjenta and Linagliptin
Prescription?
Prescription only
Generic available?
Yes
How linagliptin is dosed
From the FDA label for Tradjenta (application NDA201280). Other linagliptin products — different forms, different strengths — are dosed differently. Follow the label for the one you were prescribed.
The recommended dosage of TRADJENTA is 5 mg orally once daily ( 2.1 ) TRADJENTA can be taken with or without food ( 2.1 ) 2.1 Recommended Dosage and Administration The recommended dosage of TRADJENTA is 5 mg taken orally once daily, with or without food.
Linagliptin side effects
The following serious adverse reactions are described below or elsewhere in the prescribing information: Pancreatitis [see Warnings and Precautions (5.1) ] Hypoglycemia with Concomitant Use with Insulin and Insulin Secretagogues [see Warnings and Precautions (5.2) ] Hypersensitivity Reactions [see Warnings and Precautions (5.3) ] Severe and Disabling Arthralgia [see Warnings and Precautions (5.4) ] Bullous Pemphigoid [see Warnings and Precautions (5.5) ] Heart Failure [see Warnings and Precautions (5.6) ] Most common adverse reaction (incidence ≥5% and more often than placebo) was nasopharyngitis ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Boehringer Ingelheim Pharmaceuticals, Inc. at 1-800-542-6257, or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The safety evaluation of TRADJENTA 5 mg once daily in patients with type 2 diabetes mellitus is based on 14 placebo-controlled trials, 1 active-controlled trial, and one trial in patients with severe renal impairment. In the 14 placebo-controlled studies, a total of 3,625 patients were randomized and treated with TRADJENTA 5 mg…
Who shouldn’t take linagliptin
TRADJENTA is contraindicated in patients with hypersensitivity to linagliptin or any of the excipients in TRADJENTA, reactions such as anaphylaxis, angioedema, exfoliative skin conditions, urticaria, or bronchial hyperreactivity have occurred [see Warnings and Precautions (5.3) and Adverse Reactions (6) ]. Hypersensitivity to linagliptin or any of the excipients in TRADJENTA ( 4 , 5.3 )
Every linagliptin product we track (2)
Same active ingredient — different manufacturer, form, price and FDA recall record. That last one is what our independent score measures.
TRADJENTA tablets for oral use contain linagliptin, an inhibitor of the 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 C 25 H 28 N 8 O 2 and the molecular weight is 472.54 g/mol. The structural formula is: Linagliptin is a white to yellowish, not or only slightly hygroscopic solid substance. It is very slightly soluble in water (0.9 mg/mL). Linagliptin is soluble in methanol (ca. 60 mg/mL), sparingly soluble in ethanol (ca. 10 mg/mL), very slightly soluble in isopropanol (<1 mg/mL), and very slightly soluble in acetone (ca. 1 mg/mL). Each film-coated tablet of TRADJENTA contains 5 mg of linagliptin free base and the following inactive ingredients: copovidone, corn starch, magnesium stearate, mannitol, and pregelatinized starch. In addition, the film coating contains the following inactive ingredients: hypromellose, polyethylene glycol, red ferric oxide, talc, and titanium dioxide. Chemical Structure
What kind of drug is linagliptin?
The FDA classifies linagliptin as a dipeptidyl peptidase 4 inhibitor. DPP-4 inhibitors block the enzyme that quickly destroys the body's own gut hormones (incretins like GLP-1). With these hormones lasting longer, the pancreas releases more insulin and less glucagon after meals, which lowers blood sugar. If you are checking whether it is safe to combine with something else, the class is what matters — two drugs from the same class usually should not be stacked.
Can you take linagliptin with other medicines?
It depends on the medicine. We check it against the FDA labels rather than guessing: our interaction checker searches each drug's own label for the other and quotes what it says, naming the section it came from. Run linagliptin against whatever else you take — and remember that a label not naming a drug is not the same as that combination being safe.
What brand names is linagliptin sold under?
We track 2 linagliptin-containing products in the U.S.: Tradjenta and Linagliptin. They are the same active ingredient; they differ in form, manufacturer, price and FDA recall record.
Sources: FDA openFDA drug label, National Drug Code Directory, and Enforcement (recall) database. This page reproduces public FDA data and is not medical advice. Dosing is set by your prescriber.
Linagliptin drug interactions
Strong P-glycoprotein/CYP3A4 inducer: The efficacy of TRADJENTA may be reduced when administered in combination (e.g., with rifampin). Use of alternative treatments is strongly recommended. ( 7.1 ) 7.1 Inducers of P-glycoprotein or CYP3A4 Enzymes Rifampin decreased linagliptin exposure, suggesting that the efficacy of TRADJENTA may be reduced when administered in combination with a strong P-gp or CYP3A4 inducer. Therefore, use of alternative treatments is strongly recommended when linagliptin is to be administered with a strong P-gp or CYP3A4 inducer [see Clinical Pharmacology (12.3) ] . 7.2 Insulin Secretagogues or Insulin Insulin and insulin secretagogues are known to cause hypoglycemia. The risk of hypoglycemia is increased when linagliptin is used in combination with an insulin secretagogue (e.g., sulfonylurea) or insulin. Coadministration of TRADJENTA with an insulin secretagogue (e.g., sulfonylurea) or insulin may require lower dosages of the insulin secretagogue or insulin to reduce the risk of hypoglycemia [see Warnings and Precautions (5.2) ] .
2.5 mg / 500 mg
yellow
oval
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D2;1000M
2.5 mg / 1000 mg
yellow
oval
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D5;1000M
5 mg / 1000 mg
white
oval
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850;LM
2.5 mg / 850 mg
orange
oval
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10;5
10 mg / 5 mg
yellow
triangle
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S75
5 mg
white
round
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500;LM
2.5 mg / 500 mg
yellow
oval
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What forms does linagliptin come in?
Across the brands we track, linagliptin is currently marketed as tablet, per the FDA's National Drug Code Directory. Each form is dosed differently — follow the label for the exact product you were prescribed.
Is there a generic linagliptin?
Yes. Our catalog lists 1 generic linagliptin product alongside the brand versions. A generic has the same active ingredient and must meet the FDA's bioequivalence standard; it usually costs less. Ask your pharmacist which one your plan covers.