Description: This product is colorless or light yellow transparent liquid. Its chemical name IS hexahydro -1- (5-sulfur-based differences quinoline)-(H)-1 ,4- two azepine hydrochloride.
Pharmacological effects: Inhibit the final stages of myosin light chain phosphorylation in smooth muscle contraction dilation of blood vessels.inhibit the regulation of Rho kinase involved in cell adhesion, cell migration, smooth muscle cell contraction, cytokinesis, thus inhibiting the occurrence and development of atherosclerosis.major expansion in the small arteries (such as the circle of Willis, etc.). Hydrochloric acid fasudil injectionimprove cerebral vasospasm caused by cerebral ischemic symptoms. selectively increase cerebral and coronary blood flow. inhibit the production of free radicals and protect neurons .
Pharmacokinetics: Healthy adults within 30 minutes of continuous intravenous give hydrochloric acid fasudil 0.4mg/kg single plasma unchanged drug concentration in the administration of the end of reached the peak, followed by rapid decay, the elimination half-life of approximately 16 minutes. 2 or 3 times after subarachnoid hemorrhage in patients with repeated intravenous infusion of hydrochloric acid fasudil 30mg, 1st a total of 14 plasma concentration, similar to healthy adults. Rapid intravenous administration of the radiolabeled products in rats and monkeys, the radioactive concentration in the blood after administration to quickly lower. The continuous administration of intravenous blood concentration, since the end of the administration to reduce, about l The disappearance half-life of rats. Four hours, and auc increase with the administration of the amount of increase, a linear relationship with plasma concentrations. After administration rapidly transferred to the organization, higher levels of drugs in the liver, kidney, spleen and intestine. Can also be found to transfer to the brain.After the administration of this product, 80% unchanged unchanged drug and metabolites iso quinoline skeleton l hydroxide combination. The total number of metabolites in rats produces six kinds, five kinds of monkeys. This product is plasma protein binding in vitro approximately 80% in the body is about 34% to 62%. animal experiments show that the product can pass through the placenta and breast milk transfer. 0.2mg/kg and 0.4mg/kg of this product in healthy human experiments, continuous administration of intravenous administration after the disappearance of half-life of approximately 15 minutes.The auc and maximum plasma concentration, along with administration increases.
Indications: Used for the improvement of ischemic cerebrovascular disease symptoms caused by subarachnoid hemorrhage and vasospasm.
Precautions: This product is only intravenous drip to use, not to use other routes of administration; in patients with renal dysfunction, can reduce the dose used, it is recommended each 10mg;hinder the patients may delay the metabolism, the plasma concentration enhancement, may be appropriate to reduce the use of;the use of this product, if found intracranial hemorrhage should be discontinued immediately and appropriate treatment.recommended doses, use of blood pressure lowering effect is minimal, but in the course of medication should be noted that changes in blood pressure and administration of speed: pregnancy or may be pregnant women and lactating women should avoid using.
Adverse reaction: This product is generally well tolerated. In most cases, adverse reactions are minor in nature and is transient in nature. Occasional facial flushing, hypotension, rash. Rare nausea, polyuria, bleeding, leukopenia, abnormal liver function.
