Definition of prostacyclin
Prostacyclin, a derivative of arachidonic acid, associated with prostaglandins, contains a secondary five – membered ring, is an inhibitor of platelet aggregation. Which can improve the damage of the brain and spinal cord nerve regeneration, and a strong vasodilator effect, is a can inhibit thrombosis drugs. Can be used to treat certain cardiovascular diseases, such as cardiopulmonary bypass, hemodialysis, etc. as antiplatelet drugs to prevent hypercoagulable state.
An overview of prostacyclin
Prostacyclin, medicinal named epoprostenol, can improve the damage of the brain and spinal cord nerve regeneration, prostacyclin is anti-thromboxane antagonist, its synthesis can promote the reduction of thrombosis.
Prostacyclin (PGI2) antithrombotic substances, mainly by endothelial cell synthesis, with a strong vasodilator effect and anti-platelet aggregation, prostacyclin generation or reduction may play an important role in xenograft thrombosis process.
The formation mechanism of prostacyclin
Prostacyclin is produced by the action of prostacyclin synthase in vascular microparticles, which is the main product of peroxidic metabolism in the vessel wall. The main synthesis site in the body is vascular endothelial cells.
Prostacyclin is extremely unstable in aqueous solution at 220 °C its activity disappears within 10 min and its hydrolyzate is 6-PGF1.
Application of prostacyclin
Prostacyclin has a strong dilation of blood vessels and antiplatelet aggregation. The mechanism of diastolic blood vessels may be through the cAMP pathway blocking calcium influx process.
Can be used to treat certain cardiovascular diseases (such as cardiopulmonary bypass, hemodialysis, etc.) as antiplatelet drugs to prevent hypercoagulable state.
Also used for severe peripheral vascular disease (such as Renault disease), ischemic heart disease, primary pulmonary hypertension and platelet wasting disease.
An adverse effect of prostacyclin
The use of prostacycines common adverse reactions are low blood pressure, heart rate, facial flushing, headache, etc., the incidence increased with the dose increased. Can also have stomach cramps, nausea, vomiting, stomach discomfort, blood sugar, lethargy, chest pain and so on.
Precautions for using prostacyclin
1, bleeding tendency disabled.
2, intravenous infusion rate of more than 10μg / kg per minute, there may be headache, abdominal discomfort, high blood sugar, etc., more than 20μg / kg, there may be blood pressure, heart rate, and even fainting.
Prostacyclin and aspirin and other antithrombotic effects of the role of action on the blood vessels in the cells, it can not only expand small blood vessels, but also inhibit platelet aggregation, antithrombotic, inhibit the release of inflammatory mediators, anti-remodeling.
3, ellarella has anti-platelet and diastolic blood vessels, it can prevent thrombosis. The mechanism of the former may be due to activation of adenylate cyclase, and platelet cAMP concentration caused by increased.
According to the precursors of alcohol instability, in vivo rapid decomposition of 6 a ketone-PGF1αt for 2-3 minutes, the metabolites more stable, but the biological activity is very weak.
A related study of prostacyclin
On October 14, 2012, the Japan Science and Technology Agency and the Osaka University announced that Osaka University researchers found that the release of prostacyclin from mice with multiple sclerosis increased the regeneration of the brain and spinal nerve Ability, and in the experiment by enhancing the role of prostacyclin to improve the symptoms of mice.
Japanese scientific research institutions, said multiple sclerosis is the brain and spinal cord inflammation caused by central nervous system damage caused by a difficult condition, clinical manifestations of hand and foot paralysis, decreased vision and other symptoms. Previously, it was thought that once the central nervous system of the mammal was damaged, it was difficult to recover, one of the reasons is that the axonal regeneration capacity is low. New research for the first time that the blood vessels have the role of improving nerve regeneration, on the basis of this is expected to develop for multiple sclerosis and other central nervous system injury of new molecular targeted drugs.
Pharmacological effects of prostacyclin
Prostacyclin can inhibit platelet aggregation by increasing cAMP in platelets, the strongest among anticoagulants found. Prostacyclin through the pulmonary circulation is not metabolized to prevent thrombosis during cardiopulmonary bypass; higher doses can platelet clot depolymerization, skin bleeding time to extend 2 times; can reduce platelet procoagulant effect and reduce its heparin And factor release. Prostacyclin can inhibit the accumulation and release of platelets induced by ADP, collagen, arachidonic acid and so on, and has depolymerization.
Application of prostacyclin in the treatment
The current clinical application of prostacyclin preparations include intravenous epoprostenol, subcutaneous injection of treprostinil, oral preparation of prostaglandin, inhalation preparations iloprost. Prostacyclin is a metabolite of arachidonic acid, mainly produced by vascular endothelial cells, is a powerful vasodilator. Prostacyclin and its receptor, the activation of adenylate cyclase, the intracellular cyclic adenosine monophosphate concentration increased, and thus play a role in vasodilator. Studies have shown that prostacyclin still inhibit platelet aggregation, vascular smooth muscle proliferation.