Fondaparinux
Fondaparinux Uses, Dosage, Side Effects, Food Interaction and all others data.
Fondaparinux, a synthetic pentasaccharide, acts as a selective inhibitor of activated factor X. It works by binding selectively to antithrombin III and potentiates the neutralisation of factor Xa. This will interrupt the blood coagulation cascade and inhibit both thrombin formation and thrombus development.
Fondaparinux binds specifically to the natural anticoagulant factor, ATIII. Binding to ATIII potentiates the neutralizing action of ATIII on Factor Xa 300-times. Neutralization of Factor Xa decreases the conversion of prothrombin to thrombin, which subsequently decreases the conversion of fibrinogen to fibrin (loose meshwork). The decrease in thrombin also decreases the activation of Factor XIII, which decreases the conversion of fibrin in its loose meshwork form to its stabilized meshwork form. Disruption of the coagulation cascade effectively decreases the formation of blood clots. Fondaparinux does not inactivate thrombin (activated Factor II). According to the manufacturer, fondaparinux has no known effect on platelet function. In studies comparing fondaparinux to enoxaparin, decreases in platelet levels were observed in similar numbers of patients from both groups (2-5%) . At the recommended dose, Fondaparinux does not affect fibrinolytic activity or bleeding time. There is no antidote for fondaparinux. Monitoring of the anticoagulant activity of fondaparinux is not generally required. The anti-factor Xa assay may be used to monitor therapy in special populations such as those with renal impairment or who are pregnant. Complete blood count (CBC) and kidney function should be monitored during treatment.
Trade Name | Fondaparinux |
Availability | Prescription only |
Generic | Fondaparinux |
Fondaparinux Other Names | Natural heparin pentasaccharide |
Related Drugs | Xarelto, Eliquis, warfarin, enoxaparin, apixaban, rivaroxaban, heparin, Lovenox, Pradaxa |
Weight | 10mg/0.8ml, 2.5mg/0.5ml, 5mg/0.4ml, 7.5mg/0.6ml, |
Type | Subcutaneous Solution, Subcutaneous |
Formula | C31H53N3O49S8 |
Weight | Average: 1508.263 Monoisotopic: 1506.951330709 |
Protein binding | 94% in vitro protein binding specifically to ATIII |
Groups | Approved, Investigational |
Therapeutic Class | Parenteral anti-coagulants |
Manufacturer | |
Available Country | United States |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Prophylaxis Of Deep Vein Thrombosis- Fondaparinux is used for the prophylaxis of deep vein thrombosis (DVT), which may lead to pulmonary embolism (PE):
- In patients undergoing hip fracture surgery, including extended prophylaxis;
- In patients undergoing hip replacement surgery;
- In patients undergoing knee replacement surgery;
- In patients undergoing abdominal surgery who are at risk for thromboembolic complications.
Treatment Of Acute Deep Vein Thrombosis: Fondaparinux is used for the treatment of acute deep vein thrombosis when administered in conjunction with warfarin sodium.
Treatment Of Acute Pulmonary Embolism: Fondaparinux is used for the treatment of acute pulmonary embolism when administered in conjunction with warfarin sodium when initial therapy is administered in the hospital.
Fondaparinux is also used to associated treatment for these conditions: Acute Pulmonary Embolism, Deep Vein Thrombosis, Non ST Segment Elevation Myocardial Infarction (NSTEMI), ST Elevation Myocardial Infarction (STEMI), Unstable Angina Pectoris, Acute, superficial, symptomatic Vein Thrombosis
How Fondaparinux works
The antithrombotic activity of fondaparinux is the result of ATIII-mediated selective inhibition of Factor Xa. By selectively binding to ATIII, Fondaparinux potentiates (about 300 times) the neutralization of Factor Xa by ATIII. Neutralization of Factor Xa interrupts the blood coagulation cascade and thus inhibits thrombin formation and thrombus development. It is thought that fondaparinux is unlikely to induce thrombocytopenia via a heparin-induced thrombocytopenia (HIT)-like mechanism given its chemical structure . As a result, fondaparinux has been used as an alternative anticoagulant in heparin-induced thrombocytopenia (HIT) patients . However, it is important to note that rare cases of HIT have been reported in patients treated with fondaparinux .
Dosage
Fondaparinux dosage
Superficial vein thrombosis: 2.5 mg once daily for 30-45 days.
Venous thromboembolism:
- 50-100 kg: 7.5 mg once daily;
- >100 kg: 10 mg once daily.
- Treatment duration: 5-9 days, or until oral anticoagulation is established.
Prophylaxis of deep vein thrombosis in abdominal and orthopaedic surgery:2.5 mg once daily, starting 6-8 hr after surgery, continue for at least 5-9 days. In high-risk patients, 6-14 days or up to 32 days in hip fracture.
Side Effects
Hip-fracture, hip-replacement, or knee-replacement surgery: Anaemia, fever, nausea, oedema, constipation, rash, vomiting, insomnia, increased wound drainage, hypokalaemia, UTI, dizziness, purpura, hypotension, confusion, bullous eruption, urinary retention, haematoma, major bleeding, diarrhoea, dyspepsia, post-op haemorrhage, and headache. Treatment of venous thromboembolism: Constipation, headache, insomnia, fever, nausea, UTI, and coughing. Abdominal surgery: Post-op wound infection and haemorrhage, fever, surgical site reaction, anaemia, HTN, pneumonia, vomiting.
Toxicity
As with other anticoagulants, the main concern is increased bleed risk. The risk of hemorrhage may increase with decreased renal function, body mass less than 50 kg, and moderate to severe hepatic function.
Precaution
Patient with increased risk of haemorrhage (e.g. congenital or acquired bleeding disorders, history or active Gl ulceration, intracranial haemorrhage, recent brain, spinal or ophth surgery)
Interaction
Increased risk of bleeding with (e.g. desirudin, fibrinolytic drugs, glycoprotein IIb/IIIa-receptor antagonists, heparin, heparinoids or LMWH).
Food Interaction
- Avoid herbs and supplements with anticoagulant/antiplatelet activity. Examples include ginseng, ginkgo, ginger, and garlic.
Fondaparinux Drug Interaction
Major: aspirin, aspirin, aspirin, aspirin, heparin, heparinModerate: celecoxib, celecoxibUnknown: albuterol / ipratropium, albuterol / ipratropium, polyethylene glycol 3350, polyethylene glycol 3350, acetaminophen, acetaminophen, cyanocobalamin, cyanocobalamin, cholecalciferol, cholecalciferol, ondansetron, ondansetron
Fondaparinux Disease Interaction
Major: bleeding, hepatic impairment, renal disease, valvular heart disease, bacterial endocarditisModerate: thrombocytopenia
Volume of Distribution
- 7 - 11 L (healthy adults), distributed primarily in blood
Elimination Route
100% bioavailability when administered subcutaneously
Half Life
17-21 hours
Elimination Route
In individuals with normal kidney function, fondaparinux is eliminated in urine mainly as unchanged drug.
Pregnancy & Breastfeeding use
Pregnancy Category B. Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies in women in the 1st trimester (and there is no evidence of a risk in later trimesters).
Lactation: Unknown whether drug is excreted in milk; use with caution
Contraindication
Hypersensitivity. Active clinically significant bleeding, acute bacterial endocarditis.
Storage Condition
Store below 25° C. Do not freeze.
Innovators Monograph
You find simplified version here Fondaparinux
Fondaparinux contains Fondaparinux see full prescribing information from innovator Fondaparinux Monograph, Fondaparinux MSDS, Fondaparinux FDA label