Description

Simple

A medication or "blood thinner" used to prevent blood clots and blocked blood vessels, as well as other events, such as stroke, in various cardiovascular conditions.

Clinical

An anticoagulant used for the prophylaxis of stroke and systemic embolism in nonvalvular atrial fibrillation, and deep vein thrombosis(DVT) leading to pulmonary embolism(PE), including in patients after a hip or knee replacement surgery.

Overview

Apixaban is an oral, direct, and highly selective factor Xa (FXa) inhibitor of both free and bound FXa, as well as prothrombinase, independent of antithrombin III for the prevention and treatment of thromboembolic diseases[Label,2]. It is marketed under the name Eliquis[Label,3]. Apixaban was approved by the FDA on December 28, 2012[3].

Pharmacology

Indication

Apixaban is indicated for reducing the risk of stroke and systemic embolism in patients who have nonvalvular atrial fibrillation, prophylaxis of deep vein thrombosis(DVT) leading to pulmonary embolism(PE) in patients after a hip or knee replacement surgery, and treatment of DVT and PE to reduce the... Read more

Pharmacodynamic

Apixaban selectively inhibits factor Xa in its free and bound forms, independant of antithrombin III[Label]. Apixaban also inhibits prothrominase[Label]. These effects prevent the formation of a thrombus[Label].

Mechanism of action

Apixaban selectively inhibits factor Xa in its free and bound forms, independant of antithrombin III[Label]. Apixaban also inhibits prothrominase[Label]. These effects prevent the formation of a thrombus[Label].

Absorption

Apixaban is approximately 50% bioavailable[Label] though other studies report 43-46% oral bioavailability[ Read more

Protein binding

92-94%[Label].

Volume of distribution

Approximately 21L[Label].

Clearance

3.3L/h[Label] though other studies report 4876mL/h[ Read more

Half life

12.7±8.55h[Label, Read more

Route of elimination

56% of an orally administered dose is recovered in the feces and 24.5-28.8% of the dose is recovered in the urine[label, Read more

Toxicity

Animal studies have shown an increased risk of maternal bleeding during pregnancy but no increase in fetal malformations or fetal or maternal deaths[Label]. It is unknown if this animal data also translates to humans so apixaban should only be used in pregnancy if the benefits outweigh the risks[Lab... Read more

Adverse Effects

Contraindications

  • Route:
    • Oral
  • Dose Form:
    • Tablet
  • Hypersensitivity:
    • true
  • Sex Group: all
  • Regions: US
  • Route:
    • Oral
  • Dose Form:
    • Tablet
  • Regions: US
  • Patient Conditions:
      • Name: Active pathological bleeding
      • Drugbank Id: DBCOND0107496

Food Interactions

  • Alfalfa, Anise, Bilberry may increase the adverse effects of apixaban.
  • Grapefruit juice may increase apixaban serum concentration.
  • St. John's wort will likely decrease apixaban serum concentration. Avoid combination if possible.

Interactions

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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
(1,2,6,7-3H)Testosterone
(1,2,6,7-3H)Testosterone may increase the anticoagulant activities of Apixaban.
(R)-warfarin
Apixaban may increase the anticoagulant activities of (R)-warfarin.
(S)-Warfarin
Apixaban may increase the anticoagulant activities of (S)-Warfarin.
1-Testosterone
1-Testosterone may increase the anticoagulant activities of Apixaban.
18-methyl-19-nortestosterone
18-methyl-19-nortestosterone may increase the anticoagulant activities of Apixaban.
3,5-Diiodotyrosine
3,5-Diiodotyrosine may increase the anticoagulant activities of Apixaban.
4-hydroxycoumarin
Apixaban may increase the anticoagulant activities of 4-hydroxycoumarin.
4-Hydroxytestosterone
4-Hydroxytestosterone may increase the anticoagulant activities of Apixaban.
5beta-dihydrotestosterone
5beta-dihydrotestosterone may increase the anticoagulant activities of Apixaban.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
The risk or severity of bleeding and hemorrhage can be increased when 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline is combined with Apixaban.
Abatacept
The metabolism of Apixaban can be increased when combined with Abatacept.
Abciximab
Apixaban may increase the anticoagulant activities of Abciximab.
Abemaciclib
The serum concentration of Apixaban can be increased when it is combined with Abemaciclib.
Abiraterone
The metabolism of Apixaban can be decreased when combined with Abiraterone.
Acalabrutinib
The metabolism of Apixaban can be decreased when combined with Acalabrutinib.
Acebutolol
The serum concentration of Apixaban can be increased when it is combined with Acebutolol.
Aceclofenac
The risk or severity of bleeding and hemorrhage can be increased when Aceclofenac is combined with Apixaban.
Acemetacin
The risk or severity of bleeding and hemorrhage can be increased when Acemetacin is combined with Apixaban.
Acenocoumarol
Apixaban may increase the anticoagulant activities of Acenocoumarol.
Acetaminophen
The serum concentration of Apixaban can be increased when it is combined with Acetaminophen.
3 References
  1. 1 . Raghavan N, Frost CE, Yu Z, He K, Zhang H, Humphreys WG, Pinto D, Chen S, Bonacorsi S, Wong PC, Zhang D: Apixaban metabolism and pharmacokinetics after oral administration to humans. Drug Metab Dispos. 2009 Jan;37(1):74-81. doi: 10.1124/dmd.108.023143. Epub 2008 Oct 2.PubMed: 18832478
  2. 2 . Granger CB, Alexander JH, McMurray JJ, Lopes RD, Hylek EM, Hanna M, Al-Khalidi HR, Ansell J, Atar D, Avezum A, Bahit MC, Diaz R, Easton JD, Ezekowitz JA, Flaker G, Garcia D, Geraldes M, Gersh BJ, Golitsyn S, Goto S, Hermosillo AG, Hohnloser SH, Horowitz J, Mohan P, Jansky P, Lewis BS, Lopez-Sendon JL, Pais P, Parkhomenko A, Verheugt FW, Zhu J, Wallentin L: Apixaban versus warfarin in patients with atrial fibrillation. N Engl J Med. 2011 Sep 15;365(11):981-92. doi: 10.1056/NEJMoa1107039. Epub 2011 Aug 27.PubMed: 21870978
  3. 3 . FDA Drug Approval Package: Apixaban Link