INTRODUCTION.
Apixaban(ELIQUIS) is an oral anticoagulant for the treatment of venous thromboembolic events. It is a
direct factor Xa inhibitor.
BIOCHEMICAL PROPERTIES
It is chemically described as 1-(4methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl)phenyl]-4,5,6,7tetrahydro-1H-pyrazolo[3,4c]pyridine-3-carboxamide. Its molecular formula is C25H25N5O4, which
corresponds to a molecular weight of 459.5.
Apixaban is a white to pale-yellow powder. At physiological pH (1.2–6.8), apixaban does not ionize; its
aqueous solubility across the physiological pH range is ~0.04 mg/mL.
MECHANISM OF ACTION.
It is an anticoagulant that works by blocking the action of factor Xa. Factor Xa is an important protein in
the coagulation cascade that causes blood to clot. Reducing the action of factor Xa reduces the ability of
blood to clot.
DOSING AND ADMINISTRATION
Apixaban (eliquis) tablets are available for oral administration in strengths of 2.5 mg and 5 mg of
apixaban with the following inactive ingredients: anhydrous lactose, microcrystalline cellulose,
croscarmellose sodium, sodium lauryl sulfate, and magnesium stearate. The film coating contains
lactose monohydrate, hypromellose, titanium dioxide, triacetin, and yellow iron oxide (2.5 mg tablets)
or red iron oxide (5 mg tablets).
The usually recommended dose is 5 mg by mouth twice daily. The dose for individuals 80 years or older,
weighing less than or equal to 60 kg, or with reduced kidney function is 2.5 mg twice daily.
INDICATIONS.
1. Reduction Of Risk Of Stroke And Systemic Embolism In Nonvalvular Atrial Fibrillation: The
recommended dose of ELIQUIS for most patients is 5 mg taken orally twice daily.
2. Prophylaxis Of Deep Vein Thrombosis Following Hip Or Knee Replacement Surgery: The
recommended dose of ELIQUIS is 2.5 mg taken orally twice daily. The initial dose should be
taken 12 to 24 hours after surgery. In patients undergoing hip replacement surgery, the
recommended duration of treatment is 35 days. In patients undergoing knee replacement
surgery, the recommended duration of treatment is 12 days.
CONTRAINDICATIONS.
ELIQUIS is contraindicated in patients with the following conditions:
1.Active pathological bleeding
2.Severe hypersensitivity reaction to ELIQUIS (e.g., anaphylactic reactions)
PRECAUTIONS
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Increased Risk Of Stroke With Discontinuation Of ELIQUIS In Patients With Nonvalvular Atrial
Fibrillation Spinal/Epidural Anesthesia Or Puncture
Patients with Prosthetic Heart Valves
Pregnancy, (category B),labour and delivery
Nursing mothers
Pediatric age group
Geriatric age group
End stage renal disease patients maintained with haemodialysis
SIDE EFFECTS: (though rare)
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Blood in the eyes
blood in the urine
bloody or black, tarry stools
bruising or purple areas on the skin
confusion
constipation
coughing up blood
decreased alertness
difficulty swallowing
dizziness
fainting
fast heartbeat
headache
hives
itching
joint pain or swelling
nausea and vomiting
nosebleeds
puffiness or swelling of the eyelids or around the eyes, face, lips, or tongue
redness of the eye
severe stomach pain
shortness of breath
skin rash
tightness in the chest
unusual tiredness or weakness
vomiting of blood or material that looks like coffee grounds
DRUG INTERACTIONS.
Blood levels of apixaban are increased by drugs that reduce the activity of the liver enzymes that break
down apixaban. The dose of apixaban should be reduced to 2.5 mg twice daily if combined with drugs
that reduce the activity of these enzymes. Examples include ketoconazole (Nizoral, Extina, Xolegel,
Kuric), itraconazole (Sporanox), ritonavir (Norvir), and clarithromycin (Biaxin, Biaxin XL)
Drugs that increase the breakdown of apixaban reduce its blood levels and its effectiveness. Examples
include carbamazepine (Tegretol, Tegretol XR, Equetro, Carbatrol), rifampin, St. John's Wort, and
phenytoin (Diantin, Dilantin-125. They should not be combined with apixaban.
Administration of other drugs that also can prevent clotting will increase the risk of bleeding during
treatment with apixaban. Examples include aspirin, heparin, chronic use of NSAIDs, and drugs that
breakdown blood clots (fibrinolytics).
CONCLUSION
Apixaban is a relatively new oral anticoagulant, which is still being studied for use in various clinical
scenarios, but it has however been shown to be superior to warfarin in preventing stroke or systemic
embolism in patients with atrial fibrillation. It also causes less bleeding and lower mortality.