Luhan Pharmachem Co., Ltd.

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

Apixaban is an anticoagulant for the prevention of venous thromboembolism and venous thromboembolic events. It is a direct factor Xa inhibitor. Apixaban has been available in Europe since May 2011 and was approved for preventing venous thromboembolism after elective hip or knee replacement. The FDA approved apixaban in December 2012 with an indication of reducing the risk of stroke and dangerous blood clots (systemic embolism) in patients with atrial fibrillation that is not caused by a heart valve problem. The chemical formula is C25H25N5O4, mole mass is 459.497 g/mol.

Apixaban Drug Interaction

Apixaban is a substrate of both CYP3A4 and P-gp. Inhibitors of CYP3A4 and P-gp increase exposure to apixaban and increase the risk of bleeding (e.g., ketoconazole, itraconazole, ritonavir, or clarithromycin). Inducers of CYP3A4 and P-gp decrease exposure to apixaban and increase the risk of stroke (e.g., rifampin, carbamazepine, phenytoin, St. John’s wort). Coadministration of antiplatelet agents, fibrinolytics, heparin, aspirin, and chronic NSAID use increases the risk of bleeding.

APPRAISE-2, a placebo-controlled clinical trial of apixaban in high-risk post-acute coronary syndrome patients treated with aspirin or the combination of aspirin and clopidogrel, was terminated early due to a higher rate of bleeding with apixaban compared to placebo. The rate of ISTH major bleeding was 2.77%/year with apixaban versus 0.62%/year with placebo in patients receiving single antiplatelet therapy and was 5.91%/year with apixaban versus 2.50%/year with placebo in those receiving dual antiplatelet therapy

Precautions Before Using Apixaban

Increased Risk of Stroke with Discontinuation of Apixaban

Discontinuing Apixaban in the absence of adequate alternative anticoagulation

increases the risk of thrombotic events. An increased rate of stroke was observed during the transition from Apixaban to warfarin in clinical trials in patients with nonvalvular atrial fibrillation. If Apixaban must be discontinued for a reason other than pathological bleeding, consider coverage with another anticoagulant.

Bleeding

Apixaban increases the risk of bleeding and can cause serious, potentially fatal, bleeding. Concomitant use of drugs affecting hemostasis increases the risk of bleeding. These include aspirin and other antiplatelet agents, other anticoagulants, heparin, thrombolytic agents, selective serotonin reuptake inhibitors, serotonin norepinephrine reuptake inhibitor, and nonsteroidal anti-inflammatory drugs (NSAIDs).Patients should be made aware of signs and symptoms of blood loss and instructed to report them immediately or go to an emergency room. Apixaban should be discontinued in patients with active pathological hemorrhage.There is no established way to reverse the anticoagulant effect of apixaban, which can be expected to persist for about 24 hours after the last dose, i.e., for about two halflives.

Protamine sulfate and vitamin K would not be expected to affect the anticoagulant activity of apixaban. There is no experience with antifibrinolytic agents (tranexamic acid, aminocaproic acid) in individuals receiving apixaban. There is neither scientific rationale for reversal nor experience with systemic hemostatics (desmopressin and aprotinin) in individuals receiving apixaban. Use of procoagulant reversal agents such as prothrombin complex concentrate, activated prothrombin complex concentrate, or recombinant factor VIIa may be considered but has not been evaluated in clinical studies. Activated oral charcoal reduces absorption of apixaban, thereby lowering apixaban plasma concentration.

Patients with Prosthetic Heart Valves

The safety and efficacy of Apixaban has not been studied in patients with prosthetic heart valves. Therefore, use of Apixaban is not recommended in these patients.

Apixaban side effects

• easy bruising, unusual bleeding (nose, mouth, vagina, or rectum), bleeding from wounds or needle injections, any bleeding that will not stop;
• heavy menstrual periods;
• headache, dizziness, weakness, feeling like you might pass out;
• red, pink, or brown urine;
• black or bloody stools, coughing up blood or vomit that looks like coffee grounds;
• numbness, tingling, or muscle weakness (especially in your legs and feet); or loss of movement in any part of your body.

What should you do if you miss a dose of Apixaban?

If a dose of Apixaban is not taken at the scheduled time, the dose should be taken as soon as possible on the same day and twice daily administration should be resumed. The dose should not be doubled to make up for a missed dose.

• Overdose of Apixaban
• Overdose of apixaban may result in a higher risk of bleeding.

Apixaban Storage

Store at 20°C to 25°C (68°F-77°F); excursions permitted between 15°C and 30°C (59°F-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.