Luhan Pharmachem Co., Ltd.

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LINAGLIPTIN

Luhan Pharmachem Co., Ltd. supplies Linagliptin bulk active pharmaceutical ingredient (API) to the pharmaceutical industry. Our Linagliptin is manufactured by cGMP compliant facility. Welcome to contact us for further details including current DMF status for the product and up to date regulatory status of the manufacturing facility. We look forward to assisting you with your research and development projects.

What is Linagliptin?

Linagliptin is an orally-active inhibitor of the dipeptidyl peptidase-4 (DPP-4) enzyme. Linagliptin is described chemically as 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 empirical formula is C25H28N8O2 and the molecular weight is 472.54 g/mol. 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 (

Linagliptin is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus when treatment with both linagliptin and metformin is appropriate.

Linagliptin Drug Interaction

Inducers of P-glycoprotein and CYP3A4 Enzymes

Rifampin decreased linagliptin exposure, suggesting that the efficacy of linagliptin may be reduced when administered in combination with a strong P-gp inducer or CYP 3A4 inducer.

Precautions Before Using Linagliptin
  • Lactic acidosis: Warn against excessive alcohol use. Linagliptin is not recommended in hepatic impairment or hypoxic states and is contraindicated in renal impairment. Ensure normal renal function before initiating and at least annually thereafter.
  • There have been postmarketing reports of acute pancreatitis, including fatal pancreatitis. If pancreatitis is suspected, promptly discontinue linagliptin.
  • Temporarily discontinue linagliptin in patients undergoing radiologic studies with intravascular administration of iodinated contrast materials or any surgical procedures necessitating restricted intake of food and fluids.
  • Hypoglycemia: When used with a sulfonylurea (SU), a lower dose of the SU may be required to reduce the risk of hypoglycemia.
  • Macrovascular outcomes: No conclusive evidence of macrovascular risk reduction with linagliptin or any other antidiabetic drug
Linagliptin side effects
  • Adverse reactions reported in ?5% of patients treated with linagliptin and more commonly than in patients treated with placebo are nasopharyngitis and diarrhea.
  • Hypoglycemia
Linagliptin Overdosage

During controlled clinical trials in healthy subjects, with single doses of up to 600 mg of linagliptin (equivalent to 120 times the recommended daily dose), there were no dose-related clinical adverse drug reactions. There is no experience with doses above 600 mg in humans.

Linagliptin Storage

Store at 25°C (77°F); excursions permitted to 15°-30°C (59°-86°F) [see USP Controlled Room Temperature]

Disclaimer:

Information on this page is provided for general information purposes. You should not make a clinical treatment decision based on information contained in this page without consulting other references including the package insert of the drug, textbooks and where relevant, expert opinion. We cannot be held responsible for any errors you make in administering drugs mentioned on this page, nor for use of any erroneous information contained on this page.

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