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Apixaban belongs to a group of drugs known as factor Xa inhibitors. It is a Novel Oral Anticoagulants, which acts by inhibiting the action of a natural chemical that promotes blood clot formation. It is used to prevent strokes and blood clots in persons with atrial fibrillation that is not caused by a heart valve condition. Apixaban was authorized by the FDA on December 28, 2012.
BRAND NAMES:
Eliquis – It contains the active ingredient of Apixaban. It is available in the form of tablets used to prevent and treat blood clots.
MECHANISM OF ACTION:
Apixaban is an oral, reversible and Specific active site inhibitor of FXa. It does not require antithrombin III to exert antithrombotic action. Apixaban inhibits the activities of both free and clot-bound FXa and Although apixaban does not directly affect platelet aggregation, it does indirectly prevent thrombin-induced platelet aggregation. Apixaban reduces thrombin production and thrombus formation by blocking FXa.
PHARMACOKINETICS:
Absorption: Apixaban's absolute bioavailability is around 50% for doses up to 10 mg. The bioavailability of the medicine remains unchanged when consumed with food. Apixaban's peak plasma concentration is typically obtained 3 to 4 hours after treatment.
Distribution:Apixaban has a volume of distribution of about 21 liters and a plasma protein binding of about 87%.
Metabolism:The enzyme CYP3A4 is mainly responsible for the metabolism of apixaban. The amount of apixaban that is excreted in urine and feces as metabolites is around 25% of the oral dosage.
Excretion:Apixaban is eliminated via urine and feces, with an apparent half-life of 12 hours after oral treatment.
PHARMACODYNAMICS:
Apixaban specifically inhibits factor Xa in both free and bound forms, independently of antithrombin III. Additionally, apixaban inhibits prothrombinase. These effects stop a thrombus from forming.
DOSAGE AND ADMINISTRATION:
Apixaban comes as a tablet to take by orally. It is usually taken once or twice a day with food as directed by the physician.
Apixaban is available in the form of tablet with the strengths of 2.5 mg and 5mg.
DRUG INTERACTIONS:
Drug interactions of Apixaban may includes
- Fungal Infections – Ketoconazole or itraconazole
- Tuberculosis drugs – Rifampin
- HIV drugs – Ritonavir
- Seizure Drugs – Carbamazepine
- Non-Steroidal Anti-Inflammatory Drugs- Ibuprofen, Naproxen
CONTRAINDICATIONS:
Apixaban is a highly effective anticoagulant, but it is not suitable for everyone. Contraindications of Apixaban are Active pathological bleeding and severe hypersensitivity to Eliquis.
SIDE EFFECTS:
Side effects of Apixaban may include
- Bleeding gums
- Red, pink or brown urine
- Headache
- Rash
- Feeling dizzy
- Chest pain
- Nosebleeds
- Joint pain
OVERDOSE:
Symptoms of overdose may include the following
Symptoms may include unusual bleeding or brushing, red, brown, or pink urine, and coughing up or vomiting blood or coffee grounds.
An overdose can cause severe anticoagulant effects, resulting in uncontrolled bleeding that may necessitate emergency treatment with reversal medications such as Andexanet alfa.
TOXICITY :
Bleeding is the main hazard linked to Apixaban. Apixaban functions as an anticoagulant by preventing Factor Xa from participating in the coagulation cascade, which lowers the blood's capacity to clot. Although this helps to reduce thromboembolic events, it greatly raises the risk of bleeding, which can be fatal.
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