betrixaban

Action and Spectrum

Actions and Spectrum: 

Actions: 

betrixaban works by directly inhibiting the activity of factor Xa, a crucial enzyme involved in the blood clotting cascade. By inhibiting factor Xa, betrixaban prevents the formation of thrombin, a clotting enzyme responsible for converting fibrinogen into fibrin. Fibrin is the protein that forms the meshwork of a blood clot, and by blocking its production, betrixaban helps prevent blood clot formation. betrixaban has a long half-life, which means is active inside the body for longer. This allows for once-daily dosing, providing continuous anticoagulation with a single daily dose. 

Spectrum: 

The spectrum of betrixaban refers to the range of conditions for which it is indicated. Betrixaban is currently approved for venous thromboembolism (VTE) prophylaxis. It is done in adult patients hospitalized for an acute medical illness and at risk for thromboembolic complications due to restricted mobility. It is not indicated for treating existing blood clots or use in patients with atrial fibrillation.

Drug Interaction

Adverse Reaction

Frequency defined 

1-10% 

Non-major bleeding (2.45%) 

Hematuria (2%) 

Epistaxis (2%) 

<1% 

Major bleeding (0.67%) 

Intracranial hemorrhage (0.05%) 

GI bleeding (0.51%) 

Fatal bleeding (0.03%) 

Black Box Warning

Black Box Warning: 

A spinal or epidural hematoma occurs in patients who have received neuraxial anesthesia or spinal puncture.  

This condition can result in permanent or long-term paralysis.

Contraindication / Caution

Contraindication/Caution: 

Contraindications 

• Hypersensitivity 
• Active pathological bleeding 

Cautions 

• Increased risk of bleeding 
• Renal impairment 
• Hepatic impairment 
• Drug interactions 
• Pregnancy  
• Breastfeeding 

Pregnancy / Lactation

Pregnancy consideration:  

No data is available regarding the administration of the drug during pregnancy. 

Breastfeeding warnings:  

No data is available regarding the excretion of drug in breast milk. 

Pregnancy category: 

Category A: well-controlled and satisfactory studies show no risk to the fetus in the first or later trimester. 

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: No data is available for the drug under this category. 

Pharmacology

Pharmacology: 

betrixaban is a direct factor Xa inhibitor, which means it acts by directly inhibiting the activity of factor Xa, a crucial enzyme in the blood clotting cascade. By inhibiting factor Xa, betrixaban prevents the conversion of prothrombin to thrombin, which is necessary for forming fibrin, the protein that forms blood clots. 

Pharmacodynamics: 

The pharmacodynamics of betrixaban refers to its effects on the body and how it interacts with its target, factor Xa, and the clotting cascade. Here are the key pharmacodynamic aspects of betrixaban: 

betrixaban exerts its anticoagulant effect by blocking the production of thrombin and fibrin, thereby inhibiting the formation of blood clots. By reducing the generation of thrombin, betrixaban helps prevent the development of thromboembolic events, such as deep vein thrombosis (DVT) and pulmonary embolism (PE). 

Pharmacokinetics: 

Absorption 

The bioavailability is 34% 

The time to achieve peak effect is 3-4 hours 

Distribution 

Protein-bound is 60% 

The volume of distribution of betrixaban is 32 L/kg 

Metabolism 

betrixaban is extensively metabolized in the liver through various enzymatic reactions, including oxidation and conjugation. The main metabolic pathway involves oxidation mediated by the CYP3A4 enzyme. 

Elimination and Excretion 

The half-life is 19-27 hours 

The drug is excreted 85% in feces and 11% in urine. 

Adminstartion

Administration: 

betrixaban is typically administered orally in the form of tablets. The recommended betrixaban dosage may vary depending on the indication and individual patient factors. It is essential to follow the prescribing instructions provided by healthcare professionals and the specific dosing regimen outlined in the product labeling. betrixaban is taken by mouth with water. The tablets should take as a whole and not crushed, chewed, or split unless specifically instructed by the healthcare provider. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: betrixaban 

Pronounced: be-TRIX-a-ban 

Why do we use betrixaban? 

betrixaban is a medication that belongs to direct oral anticoagulants (DOACs) or non-vitamin K antagonist oral anticoagulants (NOACs). betrixaban is typically prescribed for patients who have undergone orthopedic surgery, such as hip or knee replacement surgery