Luhan Pharmachem Co., Ltd.

Luhan pharmachem Co., Ltd. supplies Dabigatran Etexilate Mesylate bulk active pharmaceutical ingredient (API) to the pharmaceutical industry. Our Dabigatran Etexilate Mesylate 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 Dabigatran Etexilate Mesylate?

The chemical name for dabigatran etexilate mesylate, clinic a direct thrombin inhibitor, is ?-Alanine, N-[[2-[[[4-[[[(hexyloxy)carbonyl]amino]iminomethyl] phenyl]amino]methyl]-1-methyl-1H-benzimidazol-5-yl]carbonyl]-N-2-pyridinyl-,ethyl ester, methanesulfonate. The empirical formula is C34H41N7O5 • CH4O3S and the molecular weight is 723.86 (mesylate salt), 627.75 (free base).

Dabigatran etexilate mesylate is a yellow-white to yellow powder. A saturated solution in pure water has a solubility of 1.8 mg/mL. It is freely soluble in methanol, shop slightly soluble in ethanol, and sparingly soluble in isopropanol.

Dabigatran is used to prevent strokes in those with atrial fibrillation due to causes other than heart valve disease, and at least one additional risk factor for stroke (congestive heart failure, hypertension, age, diabetes, and prior stroke), and to prevent the formation of blood clots in the veins in adults who have had an operation to replace a hip or knee.

Dabigatran Etexilate Mesylate Drug Interactions
The concomitant use of Dabigatran etexilate mesylate with P-gp inducers (e.g., sales rifampin) reduces exposure to dabigatran and should generally be avoided.

P-gp inhibition and impaired renal function are the major independent factors that result in increased exposure to dabigatran. Concomitant use of P-gp inhibitors in patients with renal impairment is expected to produce increased exposure of dabigatran compared to that seen with either factor alone.

The concomitant use of Dabigatran etexilate mesylate and P-gp inhibitors in patients with severe renal impairment (CrCl 15-30 mL/min) should be avoided.

Precautions before using Dabigatran Etexilate Mesylate

Increased Risk of Stroke with Discontinuation of Dabigatran etexilate mesylate

Discontinuing Dabigatran etexilate mesylate in absence of adequate alternative anticoagulation increases the risk of thrombotic events. If Dabigatran etexilate mesylate must be discontinued for a reason other than pathological bleeding, consider coverage with another anticoagulant.

Risk of Bleeding

Dabigatran etexilate mesylate increases the risk of bleeding and can cause significant and, sometimes, fatal bleeding. Promptly evaluate any signs or symptoms of blood loss (e.g., a drop in hemoglobin and/or hematocrit or hypotension). Discontinue Dabigatran etexilate mesylate in patients with active pathological bleeding.

Risk factors for bleeding include the concomitant use of other drugs that increase the risk of bleeding (e.g., anti-platelet agents, heparin, fibrinolytic therapy, and chronic use of NSAIDs). Dabigatran etexilate mesylate’s anticoagulant activity and half-life are increased in patients with renal impairment.

A specific reversal agent for dabigatran is not available. Hemodialysis can remove dabigatran; however the clinical experience supporting the use of hemodialysis as a treatment for bleeding is limited. Activated prothrombin complex concentrates (aPCCs, e.g., FEIBA), or recombinant Factor VIIa, or concentrates of coagulation factors II, IX or X may be considered but their use has not been evaluated in clinical trials. Protamine sulfate and vitamin K are not expected to affect the anticoagulant activity of dabigatran. Consider administration of platelet concentrates in cases where thrombocytopenia is present or long-acting antiplatelet drugs have been used.

Thromboembolic and Bleeding Events in Patients with Prosthetic Heart Valves

The safety and efficacy of Dabigatran etexilate mesylate in patients with bileaflet mechanical prosthetic heart valves was evaluated in the RE-ALIGN trial, in which patients with bileaflet mechanical prosthetic heart valves (recently implanted or implanted more than three months prior to enrollment) were randomized to dose adjusted warfarin or 150, 220, or 300 mg of PRADAXA twice a day. Therefore, the use of Dabigatran etexilate mesylate is contraindicated in patients with mechanical prosthetic valves.

Effect of P-gp Inducers and Inhibitors on Dabigatran Exposure

The concomitant use of Dabigatran etexilate mesylate with P-gp inducers (e.g. rifampin) reduces exposure to dabigatran and should generally be avoided.

P-gp inhibition and impaired renal function are the major independent factors that result in increased exposure to dabigatran. Concomitant use of P-gp inhibitors in patients with renal impairment is expected to produce increased exposure of dabigatran compared to that seen with either factor alone.

Dabigatran Etexilate Mesylate Side effects

Most common adverse reactions (>15%) are gastritis-like symptoms and bleeding.

Dabigatran Etexilate Mesylate Storage

Store at 25°C (77°F); excursions permitted to 15°-30°C (59°-86°F).

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.