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Fasudil Hydrochloride

Fasudil HCl

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Fasudil Hydrochloride (CAS: 105628-07-7) is a potent Rho-kinase inhibitor and vasodilator. Since it was discovered, it has been used for the treatment of cerebral vasospasm.

Solubility H2O: >200 mg/mL
Identification
Positive reaction
Assay ≥98.5%
Water Acidity PH 4.5-4.6
Moisture content ≤2.5%
Heavy metal ≤20ppm
Residue ignition ≤0.1%
Flashing point 182°C
Residue on ignition ≤0.1%
Outline Fasudil hydrochloride is a novel drug having a wide range of pharmacological effects ,it is first developed by Asahi Kasei Corporation, in June 1995 it was listed for the first time in Japan. It is Ratified by our country in 2001,that Asahi Kasei Corporation imports fasudil hydrochloride injection under the trade name ” Eril.” Its molecular structure is 5-isoquinoline sulfonamide derivative,it is RHO kinase inhibitor, by increasing the myosin light chain phosphatase activity it can dilate blood vessels, reduce the tension of endothelial cells, improve brain microcirculation, and does not produce and aggravate Pirates of the brain blood, and it can antagonize inflammatory cytokines, anti-apoptotic neuroprotective, and promote nerve regeneration. Fasudil hydrochloride has a certain effect on promoting the recovery of nerve function, reducing symptoms and reducing morbidity . at the grassroots level due to the constraints of economic conditions and the level of awareness of the disease, ultra-early thrombolytic therapy can not be achieved, but in order to reduce further progression of the disease within the therapeutic window of time, to rebuild local blood circulation is critical, and Fasudil hydrochloride has significant neuroprotective and therapeutic effects on ischemic cerebrovascular disease, it is worth in clinical use, especially at the grassroots level, to reduce morbidity and improve quality of life.
Pharmacological effects Fasudil hydrochloride is an isoquinoline sulfonamide derivative which can not only inhibit the intracellular calcium ion activity, but also inhibit protein kinase AGC and myosin light chain kinase, which means inhibiting smooth muscle contraction, myosin light chain phosphorylation in the final stage , relaxes vascular smooth muscle, dilates blood vessels. In vitro experiments show that the product can make cerebrovasculara In vitro relax, and it can inhibit the contraction of blood vessels in vitro caused by calcium influx , can inhibit the contraction caused by a variety of different mechanisms of cerebral vasoconstriction drugs, it can inhibit the intracellular calcium, causing vasoconstriction, but it does not reduce the intracellular calcium ion concentration, inhibit the formation of the myosin light chain phosphorylation when blood vessels contract.it is clinically used for improving and preventing cerebral vasospasm after subarachnoid hemorrhage and cerebral ischemic symptoms consequent. Intravenous administration of30mg once, 2 or 3 times one day. The product is in the early application after subarachnoid hemorrhage , the general application of 2 weeks is appropriate. When administered ,in the GS or 50 ~ 100mLNS dilution intravenous infusion, each infusion time is 30 minutes. Renal dysfunction patients need appropriate reduction, for example, once 10mg. Adverse reactions after use may be intracranial hemorrhage, gastrointestinal bleeding, pulmonary hemorrhage, epistaxis, subcutaneous bleeding, consciousness disorders. There is alsoliver abnormal function. Occasionally low blood pressure, anemia, leukopenia, abnormal renal function, urine, skin rash, fever. Patients with Intracranial hemorrhage and intracranial hemorrhage may occur, hypotension patients are disabled. Patients with Preoperative diabetes, cerebral arteriosclerosis trunk, with severe disturbance of consciousness, subarachnoid hemorrhage with cerebral vascular disorders, liver and kidney dysfunction, patients over 70 years of age, pregnant women, children should use with caution. Lactating women should stop breast-feeding. Intravenous infusion of the drug is the only way allowed.
Application Cardiovascular drugs for improving ischemic cerebrovascular disease symptoms caused by cerebral vasospasm after subarachnoid hemorrhage.
Usage vasodilator, potent Rho-kinase inhibitor

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