150915-40-5 Usage
Tirofiban hydrochloride monohydrate
Tirofiban is an anti-angina drug, it is successfully developed by the United States Merck company , Patent Number is EP 478363, and in 1998 it was sold in the United States, the trade name is Aggrastat,it is clinically used in treating acute coronary syndromes, including unstable angina or non-Q-wave myocardial infarction, and percutaneous transluminal coronary angioplasty (PTCA) or atherosclerotic plaque excision patients with in combination with heparin.
Drugs currently used in clinical are mainly tirofiban hydrochloride injections under the tradename Xin Weining, it is a reversible non-peptide platelet surface glycoprotein (GP) Ⅱb/Ⅲa receptor antagonist, it can competitively inhibit combination of fibrinogen and platelet (GP) Ⅱb/Ⅲa receptor . Intravenous injection is a dose-dependent inhibition of outside human platelet aggregation, prolonged bleeding time,and thrombosis caused by ADP, collagen, arachidonic acid,thromboxane analog U46619 and thrombin.
In healthy volunteers ,they are injected in routinely recommended doses, the peak plasma concentration is similar to that of steady-state plasma concentrations during the infusion ,T1/2 is 2h. Within 0.01~25 μg/ml dose range, PPB of this product is 65%, independent of concentration. Free drug accounts for 35% in plasma, Vd is 22~42 L. In healthy volunteers, CL is 213~314 ml/min, the renal clearance rate is 39%-69% of plasma clearance.
[Usage ]
(1) tirofiban hydrochloride monohydrate in combination with heparin is used in treating acute coronary syndromes, including unstable angina or non-Q-wave myocardial infarction, and percutaneous transluminal coronary angioplasty (PTCA) or atherectomy artery surgery patients.
(2) to give this product 0.4μg/(kg · min) bolus, 300 min, followed by a maintenance dose of 0.1μg/(kg · min). Unstable angina or non-Q-wave myocardial infarction patients need an infusion of 48~108 h. Row PTCA or atherectomy arterial patients need to continue infusion 12~24 h after surgery.
The above information is edited by the lookchem of Tian Ye.
Precautions
1. Adverse reactions: The most common adverse reactions are fever, or bleeding complications; other visible adverse reactions are nausea, headache, rash or urticaria, systemic reactions visible is reduction in platelet count.
2. Disable: allergy to the drug, the use of tirofiban in patients with thrombocytopenia occurring, there is active bleeding or bleeding constitution history before 30 days, history of intracranial hemorrhage, nearly a month of stroke or brain hemorrhage stroke, intracranial tumors, aneurysms, arteriovenous malformations, vital organs, surgery or severe trauma requiring surgical treatment, patients with aortic dissection, pericarditis, severe hypertension.
3. caution: recent (1 year) bleeding in patients, with coagulopathy, platelet disorder, or a history of thrombocytopenia, platelet count less than 150 × 109/L patients who have a history of cerebrovascular disease (1 year) , with recent subdural extracapsular surgery, nearly a month having a major surgery or a history of severe physical trauma, dissecting aneurysm, hemorrhagic retinal diseases, chronic hemodialysis patients.
Uses
Different sources of media describe the Uses of 150915-40-5 differently. You can refer to the following data:
1. Acute coronary syndrome (angina pectoris, myocardial infarction, surgery hydrant).
Tirofiban hydrochloride monohydrate is a potent non-peptide, glycoprotein IIb/IIIa inhibitor. It can prevent platelet aggregation and thrombosis.
2. A specific nonpeptide platelet fibrinogen receptor (GPIIb/IIIa) antagonist. An antithrombotic used in the treatment of unstable angina
3. Tirofiban is a specific nonpeptide platelet fibrinogen receptor (GPIIb/IIIa) antagonist. Tirofiban is an antithrombotic used in the treatment of unstable angina.
4. Tirofiban hydrochloride monohydrate has been used as an αIIbβ3 integrin (glycoprotein IIb/IIIa) inhibitor for mouse induced pluripotent stem cell (iPSC) culture.
Chemical Properties
White Solid
Biochem/physiol Actions
Tirofiban hydrochloride is a potent non-peptide, glycoprotein IIb/IIIa inhibitor. Blocks platelet aggregation and thrombus formation.
Check Digit Verification of cas no
The CAS Registry Mumber 150915-40-5 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,5,0,9,1 and 5 respectively; the second part has 2 digits, 4 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 150915-40:
(8*1)+(7*5)+(6*0)+(5*9)+(4*1)+(3*5)+(2*4)+(1*0)=115
115 % 10 = 5
So 150915-40-5 is a valid CAS Registry Number.
InChI:InChI=1/C23H37NO5S.ClH.H2O/c1-2-3-16-30(27,28)18-21(23(25)26)17-20-7-9-22(10-8-20)29-15-5-4-6-19-11-13-24-14-12-19;;/h7-10,19,21,24H,2-6,11-18H2,1H3,(H,25,26);1H;1H2/t21-;;/m0../s1
150915-40-5Relevant articles and documents
Preparation of tirofiban hydrochloride
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Paragraph 0026; 0027, (2019/04/26)
The invention relates to a method for preparing tirofiban hydrochloride. The method adopts N-butyl sulfonyl-L-imidate and 3-butyne-1-alcohol as starting materials, condensation reaction is carried outto obtain O-3-alkynylbutyl-N-butyl sulfonyl-L-complex amino acid ester and the product is subjected to Sonogashira coupling reaction with 4-halogenated pyridine to obtain N-butyl sulfonyl-O-(4-(pyridine-4-goup)3-butyne-1-group)-L-complex amino acid ester. The preparation of the tirofiban hydrochloride is then completed through hydrogenation reaction and hydrochloric acid salifying.
