Apixaban
An oral direct factor Xa inhibitor used to prevent stroke in atrial fibrillation and to prevent and treat deep vein thrombosis and pulmonary embolism.
Drug card
- How it works
- Binding factor Xa directly, so less thrombin is made
- Used for
- Preventing stroke in nonvalvular atrial fibrillation
- Preventing DVT after hip or knee replacement; treating DVT
- Treating pulmonary embolism and preventing its return
- Known for
- Bleeding (gums, nose, bruising, urine, gut)
- Its name
- -xaban means a direct factor Xa inhibitor
Study it as a flashcard, and it comes back before you forget it.
Mechanism of action
How does apixaban work?
A selective, direct inhibitor of free and clot-bound factor Xa and of prothrombinase activity that needs no antithrombin. Thrombin generation falls, and with it thrombin-driven platelet aggregation. It is metabolized mainly by CYP3A4 and carried by P-gp, and the kidneys handle only about 27% of its clearance.
Like other direct factor Xa inhibitors: They bind factor Xa themselves, with no need for antithrombin, and block it both free in the blood and inside the prothrombinase complex. Less prothrombin is converted to thrombin, so less fibrin is laid down and clots grow less. They have no direct effect on platelets, but they reduce the platelet aggregation that thrombin would trigger.
Uses
What is apixaban used for?
- Preventing stroke in nonvalvular atrial fibrillation
- Preventing DVT after hip or knee replacement; treating DVT
- Treating pulmonary embolism and preventing its return
Side effects
Side effects of apixaban
- Bleeding (gums, nose, bruising, urine, gut)Known forSerious
- Spinal or epidural hematoma after spinal proceduresSerious
- Clots and stroke if stopped earlySerious
- Anemia
- Nausea
- Allergic reactions, including rash
- Anaphylactic reactionsSerious
- Abnormal liver tests
Known for marks what an exam expects you to know it for.
Watch for
Cautions and what sets it apart
- Drugs that strongly inhibit both CYP3A4 and P-gp (ketoconazole, itraconazole, ritonavir) raise its levels: reduce the dose or avoid them.
- Not recommended in severe liver impairment (Child-Pugh C), with prosthetic heart valves, or in triple-positive antiphospholipid syndrome.
- Clotting tests (PT, INR, aPTT) are not useful for monitoring it; its effect persists for a day or more after the last dose.
- Spinal or epidural procedures (boxed warning): a hematoma can cause long-term or permanent paralysis.
Good to know: In the main atrial fibrillation trial (ARISTOTLE) it caused less major and less intracranial bleeding than warfarin.
Remember it
A way to remember it
Xa marks the spot: these drugs go straight for factor Xa, with no antithrombin needed.
Heparins reach factor Xa only through antithrombin. These drugs bind factor Xa themselves, both free and inside the prothrombinase complex, so less thrombin is made.
Written for biofideX
Its name
-xaban means direct factor Xa inhibitor
Rivaroxaban, apixaban and edoxaban are taken by mouth and block factor Xa directly. Fondaparinux (-parinux) also targets factor Xa, but indirectly.
- Every drug name stem
Its class
Direct factor Xa inhibitors
Other direct factor Xa inhibitors with a card:
Easily mixed up with heparins, direct thrombin inhibitors and vitamin K antagonists.
Sources
Checked against
Written for biofideX in plain words, after checking these references:
For learning pharmacology, not for treatment decisions: no doses are given, and a prescriber, pharmacist or the product's own label is the word on any one patient. Spotted a mistake? Tell us and we'll correct it.
Blood clots and cholesterol
Apixaban is one of 19 drugs practiced together here: their classes, how they work, what they treat and what they're known for.
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