C98H138N24O33 Bival...

C98H138N24O33 Bivalirudin 128270-60-0

C98H138N24O33 Bivalirudin 128270-60-0

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Bivalirudin 128270-60-0 C98H138N24O33

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Bivalirudin Basic information
Anticoagulants Dosage Adverse reactions and precautions Clinical evaluation Uses
Product Name: Bivalirudin
Synonyms: BIVALIRUDIN;BIVALIRUDIN TRIFLUOROACETATE;Bivalirudin, TFA;BITTERMELONP.E;Human Bivalirudin;Bivalirudin Acetate;Bivalirudin BG 8967, Hirulog, Hirulog I;BG 8967, Hirulog, Hirulog I
CAS: 128270-60-0
MF: C98H138N24O33
MW: 2180.29
EINECS:  
Product Categories: Peptide;API;proteins
Mol File: 128270-60-0.mol
Bivalirudin Structure
 
Bivalirudin Chemical Properties
storage temp.  20°C
color  white to off-white
 
Safety Information
MSDS Information
 
 
Bivalirudin Usage And Synthesis
Anticoagulants Bivalirudin is a kind of synthetic novel anticoagulants. It is the direct, specific and reversible inhibitor of thrombin. It was developed by the Swiss Basset (Biogen) originally. Then it was transferred to the United States Medicines Company, and approved for marketing in the United States in 2000. Its anticoagulant ingredient is a kind of 20 peptides derived from hirudin. Bivalirudin can specifically bind with catalytic site and the anion binding site of whether thrombin that is in the blood circulation or thrombus-bound thrombin, thus directly inhibiting thrombin activity. And its role is characterized by short, reversible. Early clinical studies show that the anticoagulation treatment of bivalirudin is good. And the incidence of bleeding events is low. So its use is safer than traditional heparin therapy. It is mainly used for the prevention of angioplasty interventional treatment of ischemic complications of unstable angina pectoris before and after. 
Bivalirudin has a inhibitory effect on soluble and thrombus-bound thrombin in vitro. That effect cannot be affected by products that are released by platelet, and it can extend plasma activated partial thromboplastin time, thrombin time and prothrombin time of normal human with a dose-dependent manner. It is suitable for percutaneous coronary intervention (PCI) unstable angina. In 2010, domestic PCI operation cases reached 300,000. The annual compound growth rate was over 30%. This showed that sales prospects of bivalirudin after the listing are considerable.
Clinically experiments prove that bivalirudin is more effective than the current mainstream unfractionated heparin/low molecular weight heparin and platelet glycoprotein receptor antagonist in applications around PCI. Especially the risk of bleeding has a significant reduction, and the use safety of anticoagulants is greatly improved: 
1. It can significantly reduce the incidence of bleeding in elective PCI patients. The total clinical outcome risk fell 14%.
2. It does not cause antibody-mediated thrombocytopenia.
3. Reversibly bind with thrombin. Short half-life. Hard to develop ischemic and hemorrhagic complications. 
4. It is not mainly excreted through the kidneys and can be safely used in patients with renal impairment. 
The above information is edited by the chemicalbook of Duan Yalan.
Dosage The first dose 0.75 mg/kg is injected intravenously. Then it is continuously injected intravenously with 1.75 mg/kg per hour by percutaneous coronary intervention. ACT should be monitored after first intravenous injection for 5 minutes. If necessary, 0.3mg/kg bivalirudin is injected again. After percutaneous coronary intervention treatment, it is continued to use for 4h. If necessary, 0.2 mg/kg bivalirudin per hour is continuously injected for 20h. When it is used, using 5mL water for injection to dissolve, and then using 50 mL normal saline to be diluted to 5mg/mL solution.
Adverse reactions and precautions 1. To guard against the occurrence of bleeding, including intracranial hemorrhage, thrombocytopenia. Intravenously injection should stop immediately when a sudden drop in blood pressure and blood volume. 
2. Back pain, headaches, insomnia, anxiety, abdominal pain, diarrhea, nausea, vomiting, low blood pressure can be seen. When serious bivalirudin should be discontinued. Patients with renal dysfunction should reduce its dosage. 
3. Patients allergic to bivalirudin and active bleeding should be banned. Women, infants, breast-feeding women should be careful to use this product.
4. Bivalirudin cannot bind with plasma proteins and red blood cells. When bivalirudin is used with heparin, warfarin, or thrombolytic drugs, it will increase the possibility of bleeding of patients. Once the excessive use, it should be discontinued. The product can be cleared by hemodialysis.
Clinical evaluation In order to prove the efficacy and safety of bivalirudin in the treatment of patients with acute coronary syndrome (ACS), the researchers designed the ACUITY clinical research. 
ACUITY clinical trial was to compare the efficacy and safety of bivalirudin with traditional heparin platelet glycoprotein Ⅱb/Ⅲa inhibitor therapy in high-risk ACS patients. ACUITY results published in a recent issue of the "New England Journal of Medicine" showed that the efficacy of bivalirudin alone is same with traditional anticoagulant drugs. While preventing ischemic events, it can significantly reduce bleeding.
ACUITY trial chooses 13,819 patients from 17 countries with high-risk non-ST segment elevation acute coronary syndrome. Patients were randomly divided into three group: unfractionated heparin or low molecular weight heparin and glycoprotein Ⅱb/Ⅲa inhibitor combination group, bivalirudin and glycoprotein Ⅱb/Ⅲa inhibitor combination group and bivalirudin alone group. The primary endpoint is ischemic composite endpoint occurred in 30 days (death, myocardial infarction or unplanned revascularization due to ischemia), major bleeding events and overall clinical outcomes (the sum of ischemic or serious bleeding events). The results showed that compared with heparin and glycoprotein Ⅱb/Ⅲa inhibitor combination group, the incidence of ischemic events in bivalirudin alone group did not significantly increase (7.8% vs 7.3%;. P = 0.32 ). Bleeding risk decreased 47% (3.0% vs. 5.7%; P <0.001), and the overall clinical outcomes were also improved significantly (10.1% vs.11.7%; P = 0.015). Using bivalirudin alone is not inferior to the combination of heparin and glycoprotein Ⅲb/Ⅲa inhibito. In addition, the combinations of bivalirudin and glycoprotein Ⅱb/Ⅲa inhibitor are also not inferior to heparin and glycoprotein Ⅱb/Ⅲa inhibitors, but no advantage at all.
Stone, the study leader in Columbia University Medical Center Stone, believes that " for high-risk ACS patients with early intervention therapy, bivalirudin is a suitable alternative to heparin or enoxaparin when used with glycoprotein Ⅱb/Ⅲa inhibitors. Compared with the combinations of heparin and glycoprotein Ⅱb/Ⅲa inhibitors or the combinations of bivalirudin and glycoprotein Ⅱb/Ⅲa inhibitor, bivalirudin treatment can make patients to have a more significant net clinical benefit. And event-free survival in 30 days can be improved. "
Uses Alternative medicine as ordinary heparin and platelet glycoprotein IIb/IIIa antagonists.
Definition ChEBI: A synthetic peptide of 20 amino acids, comprising D-Phe, Pro, Arg, Pro, Gly, Gly, Gly, Gly, Asn, Gly, Asp, Phe, Glu, Glu, Ile, Pro, Glu, Glu, Tyr, and Leu in sequence. A congener of hirudin (a naturally occurring drug found in the saliva o the medicinal leech), it a specific and reversible inhibitor of thrombin, and is used as an anticoagulant.

 

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