Product Name: Tirofiban hydrochloride monohydrate
Synonym: TIROFIBAN, HYDROCHLORIDE HYDRATE;Tirofiban HCl;TirofibanHcl142373-60-2/;N-(Butylsulfonyl)-O-[4-(4-piperidynyl)butyl]-L-tyrosine, Hydrochloride Hydrate;(2S)-2-(Butylsulfonylamino)-3-[4-[4-(4-piperidyl)butoxy]phenyl]propanoic acid hydrochloride hydrate;N-(Butylsulfonyl)-O-(4-(4-piperidinyl)butyl)-L-tyrosine monohydrochloride monohydrate;Tirofiban hydrochloride monohydrate;Tirofiban hcl Monohydrate
Product Category: Cardiovascular APIs;Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals;API
Melting Point: 135-137°C
Storage Temp.: -20°C Freezer
Solubility: DMSO: >12mg/mL at warmed to 60°C
Color: white to beige
Optical Activity: [α]/D -10 to -18° (c=1, MeOH)
Hazard Codes: Xi
Risk Statements: 36/37/38
Safety Statements: 26-37-45
WGK Germany: 3
Tirofiban Hyderochloride 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.
(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.
Precaution: 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: 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.
Chemical Property: White Solid
Uses: A specific nonpeptide platelet fibrinogen receptor (GPIIb/IIIa) antagonist. An antithrombotic used in the treatment of unstable angina
Uses: Tirofiban is a specific nonpeptide platelet fibrinogen receptor (GPIIb/IIIa) antagonist. Tirofiban is an antithrombotic used in the treatment of unstable angina.