Fasudil Hydrochloride Injection
Function and Efficacy
Fasudil hydrochloride is a protein kinase inhibitor, i.e., an intracellular calcium ion antagonist. The contraction of vascular smooth muscle is due to the significant increase in the concentration of Ca2 in smooth muscle cells, which activates key enzymes. When CA2 reaches a certain concentration, it binds to the CA2-binding protein calmodulin, activates myosin light chain phosphorylase, phosphorylates myosin light chain, and causes muscle contraction. During subarachnoid hemorrhage, various vasoconstrictor substances released from blood vessels participate in vasospasm, and ultimately cause vasoconstriction through myosin light chain phosphorylation. Fasudil hydrochloride dilates blood vessels and inhibits vasospasm by blocking the final stage of the vasoconstriction process, myosin light chain phosphorylation. Acute toxicity: The LD50 of oral administration in mice and rats is 273.9 mg/kg for male mice and 277.3 mg/kg for female mice; 335 mg/kg for male rats and 348 mg/kg for female rats. The LD50 of intravenous administration in mice is 69.5 mg/kg. Subacute toxicity: rats and monkeys were intravenously administered for 1 month, and the non-toxic dose was 12.5 mg/kg for rats and 3.125 mg/kg for monkeys. Chronic toxicity: rats and monkeys were intravenously administered for 6 months, and the non-toxic dose was 9 mg/kg for rats and 3.125 mg/kg for monkeys. Mutagenicity experiment: The bacterial reverse mutation experiment and the rodent micronucleus test were both negative. The mammalian cell chromosome test proved that it was non-mutagenic in vivo. Reproductive toxicity test: The toxicity study of reproduction and development of rats before and early pregnancy and rat fetuses during organ formation was conducted at doses of 1.56, 6.25, 25 and 1.6, 8.0, 40 mg/kg respectively. The results showed that the 25 mg/kg dose group caused a decrease in the number of corpora lutea and implantation before and early pregnancy; the 40 mg/kg dose group could slightly inhibit the weight gain of the secondary generation, but had no teratogenic effect, and had no effect on other reproductive capacity and various observation indicators of the secondary generation.
Ingredients
Fasudil hydrochloride.
| Name | Description | Content | CAS NO. | Manufacturer |
|---|---|---|---|---|
| Fasudil hydrochlorideIngredients |
Fasudil hydrochloride is a protein kinase inhibitor, i.e., an intracellular calcium ion antagonist, which dilates blood vessels and inhibits vasospasm by blocking the final stage of vasoconstriction (myosin light chain phosphorylation). More |
105628-07-7 | 54 |
Indication
Improvement of symptoms of ischemic cerebrovascular disease caused by cerebral vasospasm after subarachnoid hemorrhage.
Usage and Dosage
Adults should take 2-3 times a day, 30 mg each time, diluted with an appropriate amount of electrolyte solution and then intravenously dripped, each time taking 30 minutes. This product should be administered early after subarachnoid hemorrhage surgery and used for 2 weeks.
Adverse Reactions
1. Since this product dilates blood vessels, it may cause hypotension, facial flushing, reflex tachycardia and bleeding. 2. The use of this product may sometimes cause an increase in GOT and GPT, and sometimes cause rash, dysuria or polyuria, belching, vomiting, headache, fever, decreased consciousness level and respiratory depression.
Precautions
1. Patients who are bleeding, especially those with intracranial hemorrhage and hypotension, are contraindicated to use this product. 2. This product can only be used by intravenous drip, and cannot be injected into the spinal cavity.
Drug Interactions
1. Aleviatin injection, Bitashimin (Vc) injection, Puremarin for intravenous injection, Arepiati (phenytoin sodium) will immediately change color or become turbid when used with this product, and it is strictly forbidden to use. 2. Drugs that need to be used quickly after being used with this product include: Cefotiam for intravenous injection, Buroakuto, and Fulumarin. Because the above drugs often change color or have low permeability when used with this product, they should be used quickly after being used.
Storage
Store at room temperature. Valid for 3 years.
Packaging Specification
2ml:30mg
Manufacturer
Chengdu Easton Bio Pharmaceuticals Co., Ltd.
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Founded in:
2009-06-01 -
Address:
No. 8, Xiyuan Avenue, Chengdu Hi-tech Zone -
Tax NO.:
91510100689030428K -
Registered Funds:
176.532256 million yuan -
Website:
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Email: