Medical science is incessantly working towards unravelling the elixir to protect the human race from fatal encounters. This novel idea and rigorous efforts have successfully produced a medicine called Apixaban. Sold as ELIQUIS, Apixaban is an anticoagulant that smoothens the blood flow and reduces the risk of blood clotting.
Patients at a high risk of a heart attack, a stroke or even a pulmonary embolism (blood clot in the lungs) can be fortified with the use of this medicine. Apixaban has been approved by FDA on December 28, 2012 for fighting against atrial fibrillation in patients. For patients who have undergone knee or hip replacements, Apixaban is usually prescribed by the doctor.
Mechanism of action
Blood is the fluid of life. It is the only distributor of oxygen and essential nutrients across the human body and also forces the metabolic wastes out of the system. In the event of an injury, blood tends to coagulate and clot is formed. This process prevents extreme blood loss and protects lives. Blood clotting is a complex process. It not only allows the continuous coagulation, but also remain in the fluid state simultaneously. This process is known as “Clotting Cascade” which is responsible for producing the blood enzyme F(x) or Stuart Prower Factor or Thrombin.
Apixaban tablets target and hinders the activity of Factor Xa and reverses the clotting mechanism. Factor Xa is responsible for converting fibrinogen (soluble form) to fibrin (fibrous form) that produces the clot (also known as thrombus). With the help of Apixaban, the clot formation process is reduced or controlled to prevent any strokes due to blood clotting in the heart.
Dosage and formulation
Usually, doctors recommend the medicine dosage as 5mg to be consumed twice daily. The dosage alters based on patient’s body weight, age, and existing ailments causing resistance to immunity. For elderly patients (age 80 years and above) with kidney ailment, the dosage can be reduced to 2.5mg of Apixaban tablets to be taken two times daily.
Patients already under Apixaban medication must inform their dentist and doctors before undergoing any surgical treatment. Switching to another medication (including herbal medicines) from Eliquis must also be done after consultation with doctor.
When you buy Apixaban, you can refer to the below tablet composition to confirm the originality of the medicine.
- Tablet core: Sodium lauryl sulphate, Anhydrous lactose, Croscarmellose sodium, Microcrystalline cellulose, and magnesium stearate.
- Coat Composition on the Film: Triacetin, Hypromellose, Lactose Monohydrate, red iron oxide (5mg tablets), or yellow iron oxide (2.5mg tablets).
- 2.5 mg tablet: These are yellow, oval tablets adorned with 893 on one side and 2 1/2 on the other.
- 5 mg tablet: They are pink, oval tablets impressed upon with 894 on one side and 5 on the other side.
Chemical name: 1-(4-Methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide.
Molecular formula: C25H25N5O4
Molecular mass: 459.5
A white or a pale-yellow powder Apixaban has a pH ranging between 1.2-6.8. It does not ionize.
Pharmacokinetics or the study of the motion of drug within the body. To attain an efficacious outcome, there were several studies conducted on patients (in different age groups and gender) and already under treatment for atrial fibrillation and cardioembolic strokes. The drug plasma concentration was determined by the high-performance liquid chromatography mass spectrometry analysis.
According to the test outcome, it is learnt that Apixaban has a high absorption (or bioavailability) rate in the blood (~50%). When consumed orally it is soaked up by the gastrointestinal tract, especially in proximal parts of small intestine and lower end of the colon. The recommended dosage of this medicine is two times a day for both 2.5 and 5mg doses. Any food product does not retard the absorption of Apixaban.
The maximal concentration of plasma is observed at 3-4-hour onset. As far as pharmacokinetics is concerned, Apixaban demonstrates a linear pharmacokinetics till 10 mg dosage. The enzyme involved in the metabolism of the drug is CYP3A4. The other enzymes playing their part during the drug’s metabolism are CYP1A2, 2C8, 2C9, and 2J2.
Apixaban is eliminated out of the body via urinary and anal tracts. While urinating, the patient usually eliminates 27% of the drug.
To determine the effectiveness and efficacy of Apixaban, several tests and drug-to-drug interactions have been conducted time and again. Drugs under observation were Naproxen, Enoxaparin, Clarithromycin, Rifampin, ASA (or Acetylsalicylic Acid), Atenolol, Famotidine, Clopidogrel, Digoxin, Activated Charcoal, Prasugrel, and others.
The patient can order and buy this drug online. It is proven for being effective and safe when consumed with or without food. The absorption of the drugs is almost the same in both cases.
When Apixaban is accompanied by a herbal medicine such as St. John’s Wort, it usually slows down the plasma concentration of apixaban. Hence, it is advisable to not have an apixaban and herb consumption simultaneously, e.g. CPY3A4 and P-gp.
The laboratory tests are effective in analysing the coagulation parameters or clotting criterion of Apixaban which includes PT (Prothrombin time), INR (International Normalized-Ratio), and PTT (Partial-Thromboplastin Time). In majority of the occasions the dosage prescribed by the doctors is too low to derive any noticeable readings or variables that can help scrutinize the drug’s anticoagulant ability.
Apixaban is not an OTC drug and its usage and administration must be informed to the doctor during the following scenarios:
- In case of pregnant and lactating mothers.
- In case of children or elderly population (above 85 years of age).
- When the patient is already consuming another medication.
- Besides getting proper instructions from the doctor, patients must avoid getting injured that may cause him or her to bleed profusely. Excessive bleeding may lead to loss of life and other fatal disabilities.
- Before the onset of any surgery (dental and otherwise)