Ozagrel sodium

CBNumber： CB62131047
Name： OZAGREL SODIUM
MF： C13H11N2NaO2
MW： 250.23
CAS： 189224-26-8

Thromboxane (TXA) synthase inhibitors:
Ozagrel sodium is the sodium salt form of the antiplatelet aggregating agent Ozagrel. It is a thromboxane (TXA) synthase inhibitor, which can selectively inhibit thromboxane synthase and inhibit TXA synthesis, thereby inhibiting the production and promotion of TXA2 The production of prostacyclin (PGI2) has the effect of anti-platelet aggregation and relieving vasospasm. Can inhibit cerebral embolism and cerebral vasospasm. After a single intravenous injection, the blood disappears quickly, and the steady-state blood concentration is reached after continuous administration for 2 hours.

Pharmacological effects:
Ozagrel sodium is a thromboxane synthase inhibitor, which can inhibit the production of TXA2, so it has anti-platelet accumulation and vasodilation effects. Animal experiments showed that intravenous administration can reduce the level of plasma TXB2 and the ratio of Keto-PGF12/TXB2, inhibit platelet aggregation caused by different inducers, and prevent cerebral infarction caused by middle cerebral artery in rats.

Pharmacokinetics:
After intravenous infusion, the plasma concentration-Chemicalbook time curve conformed to the two-compartment open model, with T1/2β of 1.22±0.44h, Vd of 2.32±0.62l/kg, and AUC of 0.47±0.08μg·hr/nl. The Cl is 3.25±0.82l/h/kg, the longest half-life of the subjects is 1.93h, and the blood concentration can be measured 3h after drug withdrawal. After 24 hours of drug withdrawal, almost all the drugs were excreted in urine.

Indications:
For the treatment of acute thrombotic cerebral infarction, subarachnoid hemorrhage after vasospasm associated with movement disorders and the improvement of symptoms complicated by cerebral ischemia.

Dosage:
Improve cerebral thrombosis (acute phase): 40-80 mg, dissolved with an appropriate amount of electrolyte or GS, intravenously for 2 hours, bid, for 1-2 weeks. Improve cerebral vasospasm and accompanying cerebral ischemia symptoms after subarachnoid hemorrhage surgery: 80 mg, qd, continuous intravenous infusion for 24 hours, for 2 consecutive weeks. The dose can be appropriately increased or decreased according to age and symptoms. This information was edited by Chemicalbook Xiaonan (2015-10-12).