Ozagrel Sodium Injection
Function and Efficacy
This product is a thromboxane (TX) synthase inhibitor, which can prevent prostaglandin H2 (PGH2) from generating thromboxane A2 (TXA2), and promote the transfer of PGH2 derived from platelets to endothelial cells. Endothelial cells are used to synthesize PGI2, thereby improving the abnormal balance between TXA2 and prostaglandin PGI2. Theoretically, it can inhibit platelet aggregation and vasodilation. This product can improve movement disorders in the acute phase of cerebral thrombosis, improve circulatory disorders in the acute phase of cerebral ischemia, and improve abnormal energy metabolism during cerebral ischemia. Animal experiments have shown that intravenous administration can reduce plasma TXB2 levels, reduce the 6-Keto-PGF1?/TXB2 ratio, inhibit platelet aggregation caused by different inducers, and prevent cerebral infarction caused by middle cerebral artery occlusion in rats. The half-inhibitory concentration IC50 of this product for human platelet aggregation is low. Experiments using autologous blood injected into the subarachnoid hemorrhage model showed that continuous intravenous injection of this product has the effects of inhibiting blood TXB2 concentration and cerebral vasoconstriction. Acute toxicity LD50 (mg/kg): 1940 (male), 1580 (female) for intravenous injection in mice; 3800 (male), 3600 (female) for oral administration; 2450 (male), 2100 (female) for subcutaneous administration. 1150 (male), 1300 (female) for intravenous injection in rats; 5900 (male), 5700 (female) for oral administration; 2300 (male), 2250 (female) for subcutaneous administration in rats. 733 (male) for intravenous injection in dogs. Subacute and chronic toxicity: Intravenous injection of this product, except for a slight increase in urine electrolyte excretion in the high-dose group of rats, no other abnormalities were found. The maximum tolerable dose is 125mg/kg for rats and 10-12.5mg/kg for dogs. Other toxicity: The results of reproductive toxicity tests on rats and rabbits showed that at high doses, this product caused toxic symptoms such as suppression of body weight of inbred animals, embryo and fetal death, inhibition of fetal development, and neonatal death. In addition, in the SegⅡ test in rats, it was found that the number of malformed babies with visceral and skeletal abnormalities in the high-dose group increased slightly, and the antigenicity, variability and local irritation tests were all negative. Patients after subarachnoid hemorrhage were given this product for 10 to 14 days in the early postoperative period, and a double-blind test was conducted in the high-dose group (400 mg per day), low-dose group (80 mg per day) and prazepam control group of the drug. The results showed that the effective rate and efficacy of the low-dose group and high-dose group were significantly better than those of the control group. In addition, the frequency of cerebral vasospasm in the high-dose group was also significantly lower than that in the control group.
Ingredients
The main ingredient of this product is: Ozagrel sodium. Its chemical name is: trans-3-[4-(1H-imidazolyl-1-methyl)phenyl]-2-acrylate sodium. Molecular formula: C13H11N2O2Na Molecular weight: 250.23
| Name | Description | Content | CAS NO. | Manufacturer |
|---|---|---|---|---|
| Ozagrel sodiumIngredients |
This product is a thromboxane (TX) synthase inhibitor, which can prevent prostaglandin H2 (PGH2) from generating thromboxane A2 (TXA2), and promote the transfer of PGH2 derived from platelets to endothelial cells. Endothelial cells are used to synthesize PGI2, thereby improving the abnormal balance between TXA2 and prostaglandin PGI2. Theoretically, it can inhibit platelet aggregation and vasodilation. This product can improve movement disorders in the acute phase of cerebral thrombosis, improve circulatory disorders in the acute phase of cerebral ischemia, and improve abnormal energy metabolism during cerebral ischemia. Animal experiments have shown that intravenous administration can reduce plasma TXB2 levels, reduce the ratio of 6-Keto-PGF1α/TXB2, inhibit platelet aggregation caused by different inducers, and prevent cerebral infarction caused by middle cerebral artery occlusion in rats. More |
189224-26-8 | 10 |
Appearance
This product is a colorless transparent liquid.
Indication
Used to treat acute thrombotic cerebral infarction and movement disorders associated with cerebral infarction, and to improve cerebral vasospasm and contraction and concurrent cerebral ischemia symptoms after subarachnoid hemorrhage surgery.
Usage and Dosage
40-80 mg each time, dissolved in an appropriate amount of electrolytes or 5% glucose solution, 1-2 times a day, continuous intravenous drip for 24 hours, 1-2 weeks as a course of treatment. In addition, the dosage can be appropriately increased or decreased according to age and symptoms.
Adverse Reactions
Blood: Due to the tendency of bleeding, observe carefully and stop the administration immediately if abnormalities occur. Liver and kidney: Occasionally, GOT, GPT, and BUN may increase. Digestive system: Occasionally, there may be nausea, vomiting, diarrhea, loss of appetite, and a feeling of fullness. Allergic reactions: Occasionally, urticaria and rash may occur. Stop the administration when they occur. Circulatory system: Occasionally, there may be supraventricular arrhythmia and a decrease in blood pressure. When found, reduce the dose or stop the administration. Others: Occasionally, there may be headache, fever, pain at the injection site, shock, and thrombocytopenia. Serious adverse reactions may include hemorrhagic cerebral infarction, epidural hematoma, intracerebral hemorrhage, gastrointestinal bleeding, subcutaneous bleeding, etc.
Precautions
1. Those who are allergic to this product. 2. Those with cerebral hemorrhage or cerebral infarction and bleeding. 3. Those with severe heart, lung, liver, and kidney dysfunction, such as severe arrhythmia. 4. Those with blood diseases or bleeding tendency. 5. Those with severe hypertension, systolic blood pressure exceeding 26.6kPa (i.e. 200mmHg).
Special Population Medication
Precautions for children: Use with caution in children. Precautions for pregnancy and lactation: Use with caution in pregnant women or women who may become pregnant. Precautions for the elderly: Not yet clear.
Drug Interactions
This product can enhance bleeding tendency when used in combination with antiplatelet aggregation agents, thrombolytic agents and other anticoagulants, so it should be used with caution.
Storage
Keep away from light and store in a sealed container.
Packaging Specification
2ml:40mg
Validity Period
36 months.