Buy Fondaparinux (Arixtra)

Fondaparinux (Arixtra), a synthetic pentasaccharide that selectively inhibits factor Xa, is the latest heparin analog to reach the U.S. market. Fondaparinux blocks the activity of certain clotting substances in the blood. Fondaparinux is known as a "blood thinner" (anticoagulant). It is a drug similar to heparin that works by blocking certain natural substances in the blood that cause clotting. Fondaparinux is used to treat serious blood clots in the legs or lungs. This drug may also be used to prevent blood clots after certain surgeries with an increased risk of blood clots such as hip fracture, abdominal, knee or hip replacement. If untreated, blood clots can travel to the lungs, heart, or brain, causing serious (possibly fatal) breathing problems, heart attack, or stroke.

Fondaparinux (brand name in U.S. is Arixtra) is also used together with warfarin (Coumadin, Jantoven) to treat DVT, including pulmonary embolism. You should not use fondaparinux if you have active bleeding, severe kidney disease, an infection in the lining of your heart, or low platelets in your blood after testing positive for a certain antibody. Fondaparinux can cause you to bleed more easily. Call your doctor at once if you have signs of bleeding such as: bleeding gums, nosebleeds, heavy menstrual periods or abnormal vaginal bleeding, blood in your urine, bloody or tarry stools, coughing up blood or vomit that looks like coffee grounds.

How Fondaparinux work?

Fondaparinux acts exclusively against factor Xa—it does not affect thrombin. Fondaparinux does not require monitoring. Fondaparinux (Arixtra) differs from standard heparin and LMWH in several ways. In particular, it does not come from animal sources. Instead, this drug is a synthetic version of the active site of the heparin molecule and is an even smaller molecule than LMWH. Heparin blocks both thrombin and factor Xa, whereas LMWH has relatively more activity against factor Xa and relatively less activity against thrombin. Blood clotting can be a problem when blood flow is disturbed in any way. Fondaparinux is an anticoagulant: it prevents the blood from coagulating (clotting). The active ingredient fondaparinux sodium, stops one of the substances (factors) that are involved in the clotting of blood, factor Xa. When this is blocked, no thrombin (another factor) can be produced, and no clot can be formed. By using Fondaparinux after surgery, the risk of a blood clot forming is greatly reduced. By reducing blood clots, Fondaparinux can also help the flow of blood to the heart to be maintained in patients with angina or who are having a heart attack.

Cost-effectiveness of fondaparinux versus other anticoagulants

Fondaparinux is a well established synthetic anticoagulant that inhibits thrombus formation by interrupting the blood coagulation cascade through antithrombin IIIA-mediated selective inhibition of factor Xa. Acute coronary syndrome (ACS) refers to a spectrum of life-threatening cardiac diseases usually due to coronary artery plaque rupture, subsequent thrombin generation plaque activation and thrombus formation. Organization to Assess Strategies in Acute Ischemic Syndromes Investigators decided to trial randomized 20000 patients to fondaparinux or enoxaparin. The trial data showed that fondaparinux is protective against all clinical events observed in the trial. The model showed that over 180 days, fondaparinux dominates enoxaparin. Based on trial data, it has been proven that fondaparinux dominates enoxaparin (less costly and more effective). As the conclusions, in the hospital setting, fondaparinux is cost-effective when compared to enoxaparin.

How to use Fondaparinux?

Fondaparinux is usually given every day until your bleeding condition improves. Follow all directions on your prescription label and read all medication guides or instruction sheets. Use the medicine exactly as directed. Fondaparinux is injected under the skin. A healthcare provider may teach you how to properly use the medication by yourself. Read and carefully follow any Instructions for Use provided with your medicine. Do not use fondaparinux if you don't understand all instructions for proper use. Ask your doctor or pharmacist if you have questions. You should be sitting or lying down during the injection. Do not inject fondaparinux into a muscle or a vein. Prepare your injection only when you are ready to give it. Do not use if the medicine has changed colors or has particles in it. Call your pharmacist for new medicine. Your care provider will show you where on your body to inject fondaparinux. Use a different place each time you give an injection. Do not inject into the same place two times in a row. Fondaparinux can make it easier for you to bleed, even from a minor injury. Seek medical attention if you have bleeding that will not stop. If you need surgery, dental work, or a medical procedure, tell the doctor or dentist ahead of time that you are using this medication. If you need anesthesia, you may need to stop using fondaparinux for a short time.

Read the Patient Information Leaflet if available from your pharmacist before you start using fondaparinux and each time you get a refill. If you have any questions, ask your doctor or pharmacist. Before using, check this product visually for particles or discoloration. If either is present, do not use the liquid. Do not mix any other medication in the same injection. Before injecting each dose, clean the injection site with rubbing alcohol. Change the injection site each time to lessen injury under the skin. To minimize bruising, do not rub the injection site after a shot. Use a needle and syringe only once and then place them in a puncture-proof "sharps" container. Follow state or local laws about how to dispose of this container.

Fondaparinux Off Label Uses

Fondaparinux has been also proposed as a treatment for COVID-19, because of its anti-inflammatory and anti-viral properties]. Fondaparinux can be an attractive drug in this setting, as it is not associated with heparin-induced thrombocytopenia, a fearful side effect of heparin treatment reported in a non-negligible part of COVID-19 patients, which is associated with a worse prognosis.

In acutely patients with COVID-19, anticoagulant thromboprophylaxis with fondaparinux over anticoagulant thromboprophylaxis with unfractionated heparin (UFH) is suggested; and also recommended anticoagulant thromboprophylaxis with LMWH, fondaparinux or UFH over anticoagulant thromboprophylaxis with a direct oral anticoagulant (DOAC). In addition, it is likely that many of these patients will be receiving concomitant therapy (antiviral agents or other investigational treatments) that can significantly affect the pharmacodynamics of and thus bleeding risk associated with the DOACs.

Dosage

This medication is given by injection under the skin of the stomach as directed by your doctor, usually once daily. If you are using this medication at home, learn all preparation and usage instructions from your health care professional and the product package. Do not inject into a muscle. The dosage and length of treatment are based on your medical condition and response to treatment. The dosage may also be based on your weight. Use this medication regularly to get the most benefit from it. To help you remember, use it at the same time each day.

When treating a blood clot, another blood thinner is usually started within 3 days after you start using fondaparinux. Your doctor will direct you to use both of these medications until the warfarin is working well. Do not stop either of these medications until your doctor directs you to stop.

To prevent blood clots due to surgery, your doctor may direct you to start using this medication after surgery, such as 6 to 8 hours after knee or hip replacement surgery, and continue for several days. Follow your doctor's directions closely. Starting this medication too soon after surgery may increase the risk of serious bleeding.

Usual Adult Dose for Deep Vein Thrombosis

Dosage is based on patient's weight:

• Under 50 kg: 5 mg subcutaneously once a day
• 50 to 100 kg: 7.5 mg subcutaneously once a day
• Over 100 kg: 10 mg subcutaneously once a day
• Duration of therapy: At least 5 days, until INR of 2 to 3 achieved with warfarin

Usual Adult Dose for Pulmonary Embolism

Dosage is based on patient's weight:

• Under 50 kg: 5 mg subcutaneously once a day
• 50 to 100 kg: 7.5 mg subcutaneously once a day
• Over 100 kg: 10 mg subcutaneously once a day
• Duration of therapy: At least 5 days, until INR of 2 to 3 achieved with warfarin

Usual Adult Dose for Deep Vein Thrombosis Prophylaxis after Abdominal Surgery

2.5 mg subcutaneously once a day after hemostasis is established, starting no sooner than 6 to 8 hours after surgery
Duration of therapy: 5 to 9 days

Usual Adult Dose for Deep Vein Thrombosis - Prophylaxis

2.5 mg subcutaneously once a day after hemostasis is established, starting no sooner than 6 to 8 hours after surgery
Duration of therapy: 5 to 9 days

Usual Adult Dose for Deep Vein Thrombosis Prophylaxis after Hip Replacement Surgery

2.5 mg subcutaneously once a day after hemostasis is established, starting no sooner than 6 to 8 hours after surgery
Duration of therapy: 5 to 9 days

Usual Adult Dose for Deep Vein Thrombosis Prophylaxis after Knee Replacement Surgery

2.5 mg subcutaneously once a day after hemostasis is established, starting no sooner than 6 to 8 hours after surgery
Duration of therapy: 5 to 9 days

Renal Dose Adjustments

CrCl less than 30 mL/min: Contraindicated
CrCl 30 to 50 mL/min: Use with caution

Discontinue immediately if patient develops severe renal impairment.

Liver Dose Adjustments

Mild to moderate hepatic impairment: No adjustment recommended
Severe hepatic impairment: Observe closely for signs of bleeding

Dose Adjustments

Patients weighing less than 50 kg: Contraindicated for DVT prophylaxis; use with caution for DVT/pulmonary embolism treatment
Discontinue if platelet count falls below 100,000/mm(3)

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution, Subcutaneous, as sodium:

Generic: 2.5 mg/0.5 mL (0.5 mL); 5 mg/0.4 mL (0.4 mL); 7.5 mg/0.6 mL (0.6 mL); 10 mg/0.8 mL (0.8 mL)

Solution, Subcutaneous, as sodium [preservative free]:

Arixtra: 2.5 mg/0.5 mL (0.5 mL); 5 mg/0.4 mL (0.4 mL); 7.5 mg/0.6 mL (0.6 mL); 10 mg/0.8 mL (0.8 mL)

Generic: 2.5 mg/0.5 mL (0.5 mL); 5 mg/0.4 mL (0.4 mL); 7.5 mg/0.6 mL (0.6 mL); 10 mg/0.8 mL (0.8 mL)

Side Effects

Fondaparinux can cause you to bleed more easily. Call your doctor at once if you have signs of bleeding such as:

• easy bruising or bleeding (nosebleeds, bleeding gums, heavy menstrual bleeding
• pain, swelling, or drainage from a wound or where a needle was injected in your skin
• bleeding from wounds or needle injections, any bleeding that will not stop
• headaches, dizziness, weakness, feeling like you might pass out
• urine that looks red, pink, or brown; or
• bloody or tarry stools, coughing up blood or vomit that looks like coffee grounds.
• a light-headed feeling, like you might pass out
• low potassium level - leg cramps, constipation, irregular heartbeats, fluttering in your chest, increased thirst or urination, numbness or tingling, muscle weakness or limp feeling
• low red blood cells (anemia) - pale skin, unusual tiredness, feeling light-headed or short of breath, cold hands and feet
• low potassium - leg cramps, constipation, irregular heartbeats, fluttering in your chest, increased thirst or urination, numbness or tingling, muscle weakness or limp feeling
• low red blood cells (anemia) - pale skin, feeling light-headed or short of breath, rapid heart rate, trouble concentrating; or
• bleeding, bruising
• sleep problems (insomnia)
• rash, blisters
• dizziness, confusion; or
• minor bleeding, rash, itching, or oozing where the medicine was injected.

Get emergency medical help if you have signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat. Also seek emergency medical attention if you have symptoms of a spinal blood clot: back pain, numbness or muscle weakness in your lower body, or loss of bladder or bowel control.

Precautions

Before using fondaparinux, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients (such as dry natural rubber/latex in the needle cover on the prefilled syringe), which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

Before using fondaparinux, tell your doctor or pharmacist your medical history, especially of: infection in the heart (bacterial endocarditis), current serious bleeding (such as bleeding ulcer), low platelet count because of antiplatelet antibody, bleeding/blood problems (such as low blood count/platelets), a past blood-clotting problem because of heparin (heparin-induced thrombocytopenia), a certain eye problem (diabetic retinopathy), high blood pressure, kidney disease, seizures, stomach/intestinal problems (such as recent ulcers, colitis), stroke, recent spinal procedures or puncture, spine problems (such as spinal deformity), recent surgery (especially on the eye, brain, or spine), low body weight (less than 50 kilograms).

Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products). Limit alcohol while taking this drug because it may increase the risk of stomach bleeding. To lower the chance of getting cut, bruised, or injured, use caution with sharp objects like razors and nail cutters, and avoid activities such as contact sports. Older adults may be more sensitive to the side effects of this drug, especially bleeding. During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor. If you become pregnant or think you may be pregnant, tell your doctor right away.

Epidural or spinal hematomas may occur in patients who are anticoagulated with low molecular weight heparins (LMWH), heparinoids, or fondaparinux sodium, and are receiving neuraxial anesthesia or undergoing spinal puncture. These hematomas may result in longterm or permanent paralysis. Consider these risks when scheduling patients for spinal procedures. Factors that can increase the risk of developing epidural or spinal hematomas in these patients include: use of indwelling epidural catheters concomitant use of other drugs that affect hemostasis, such as nonsteroidal antiinflammatory drugs (NSAIDs), platelet inhibitors, or other anticoagulants a history of traumatic or repeated epidural or spinal puncture Optimal timing between administration of fondaparinux and neuraxial procedures is not known. Recommendations: Monitor patients frequently for signs and symptoms of neurologic impairment. If neurologic compromise is noted, urgent treatment is necessary Consider the benefits and risks before neuraxial intervention in patients anticoagulated or to be anticoagulated for thromboprophylaxis.

Easy to use

Fondaparinux is the first selective inhibitor of the coagulation factor Xa which is commercially avaliable for clinical use. It has been approved for the prevention of venous thromboembolism in patients undergoing orthopedic surgery and for the initial therapy of venous thromboembolism. In summary, fondaparinux is a new antithrombin that is an efficient, safe, and easy to use in treatment for STEMI patients, particularly those not undergoing primary PCI. All in all, medical professionals are hopeful fondaparinux will be the first in a new wave of antithrombotic agents. It's a welcome new addition to antithrombotic armamentarium because it appears that fondaparinux is more effective than previous agents. It's easy to use, has a predictable response, and does not cause thrombocytopenia.

Risks and Benefits

What are the benefits of Fondaparinux?

Fondaparinux is safe and relatively inexpensive, does not require routine monitoring, and is likely to be favored in settings without routine mechanical coronary reperfusion. Some large randomized trials show an advantage of a simple fondaparinux regimen over other antithrombotic regimens in acute coronary syndrome patients, with or without STEMI, among subjects not intended for primary PCI. Fondaparinux reduced death, myocardial infarction, stroke, or major bleeding by 22% compared with enoxaparin. Even in those undergoing early PCI (i.e. within the first 24 h), there was a 24% relative risk reduction in favour of fonda- parinux. Fondaparinux achieve significant reductions in the extension of superficial thrombophlebitis into the deeper venous systems and the rate of recurrence in general, as well as to reduce the symptoms of venous thromboembolism.

Fondaparinux was at least as effective as the comparators in all of the studies that looked at the prevention of VTE and treatment of DVT and PE. The overall rate of thrombotic events in patients treated with Fondaparinux was significantly less than in patients treated with placebo or enoxaparin (for patients undergoing leg surgery), and was similar to that seen with enoxaparin (treatment of DVT), dalteparin or unfractionated heparin. Fondaparinux was more effective than placebo in reducing the overall occurrence of VTE or death in patients with superficial-vein thrombosis. While there was one VTE or death for every 100 patients taking Fondaparinux, there were six for every hundred taking placebo. Fondaparinux was at least as effective as enoxaparin in preventing death or an ischaemic event in patients with unstable angina or myocardial infarction without ST-segment elevation, with around 5% of the patients in each group had died or had an ischaemic event after nine days. In the study of myocardial infarction with ST-segment elevation, Fondaparinux reduced the risk of death or another heart attack by 14% after 30 days, compared to standard care. However, these results were insufficient to show whether Fondaparinux was more effective than unfractionated heparin or not.

What is the risk associated with Fondaparinux?

As with other anticoagulant medicines, the most common side effect of Fondaparinux is bleeding. Fondaparinux should not be used in people who may be hypersensitive (allergic) to fondaparinux sodium or any of the other ingredients, who might be bleeding already, who have acute bacterial endocarditis (an infection of the heart) or have severe kidney problems.