Emoxipine (0,5 %solution for infusions)
Solutio Emoxipini 0,5 % pro infusion
International nonproprietary name:
Emoxipine.
Emoxipine.
Structure
1 ml of solution for injections contains 5 mg of emoxipine.
Pharmacological group
Antiaggregants. Antihypoxants and antioxidants. Angioprotectors, microcirculationcompensators.
Pharmacological action
Pharmacodynamics
Emoxipine has beneficial effect on blood coagulation system: inhibits aggregation of thrombocytes, reduces the general index of coagulation, extends blood coagulation time. It stabilizes blood vessels and erythrocytes cell membranes, increases resistance of erythrocytes to mechanical trauma and hemolysis. It possesses angioprotective properties. Improves microcirculation.
The preparation effectively inhibits free-radical oxidation of biomembrane lipids, increases activity of antioxidative enzymes. Stabilizes cytochrome Р-450, possesses antitoxic action. In the extreme situations, accompanied by intensifying of lipid peroxidation and hypoxia, optimizesbioenergetics processes.
The preparation protects eye retina from damaging action of light of high intensity, promotes resorption of intraocular hemorrhages.
Emoxipine reduces signs of cerebral hemodysfunction. It increases brain resistance to hypoxia and ischemia. At disturbances of cerebral circulation (ischemic and hemorrhagic) it promotes correction of vegetative dysfunctions, relieves restoration of brain integrative activity, improves mnemonics functions.
It has hypolipidemic action, reduces synthesis of triglycerides.
The preparation possesses the expressed cardioprotective action. It dilates coronary vessels, reduces ischemic damage of myocardium. At myocardial infarction it limits size of necrosis center, accelerates reparative processes, promotes normalization of myocardium metabolism. In has beneficial effect on clinical course of myocardial infarction, reducing frequency of acute heart failure development. It promotes a regulation of oxidation-reduction system at circulatory insufficiency.
It is effective at conditions, accompanied by lipid peroxidation intensifying (including dermal diseases, glaucoma, etc.).
Pharmakokinetics
At intravenous introduction in a dose of 10 mg/ml the low period of half-elimination is noted (Т1/2 = 18 min that testifies to high rate of preparation elimination from blood). The value of elimination constant is 0,041 min; systemic clearanceСl is 214,8 ml/min; apparent distributionvolume is Vapp. = 5,2 l. The preparation quickly enters into organs and tissues where its deposition and metabolism take place. 5 metabolites of emoxipine, represented by dealkylated and conjugated products of its transformation are found. Emoxipine metabolites are excreted by kidneys. 2-ethyl-6-methyl-3-oxypyridine -phosphate is found in liver in significant quantities.
At pathological conditions, for example, in case of coronary occlusion, emoxipine pharmakokinetics can be changed. The rate of elimination decreases owing to what the bioavailability of the preparation increases. Time of emoxipine discovery in a vascular bed is enlarged that can be bound to its reverse entering from depot, including from ischemic myocardium.
At retrobulbar introduction emoxipine almost instantly appears in blood; within first two hours its concentration sharply decreases and in 24 hours the preparation is absent in blood. In eye tissues the concentration of emoxipine is higher than in a blood.
Indications
In neurology and neurosurgery: hemorrhagic insult, ischemic insult in pool of internal carotidartery and in vertebrobasilar system, transient disturbances of cerebral circulation, chronic failure of cerebral circulation, craniocerebral trauma, accompanied brain contusions; postoperative period in patients with th craniocerebral trauma, operated in occasion of epi-, subdural and intracerebral hematomas combined with brain contusions; pre- and postoperative period in patients with arterial aneurysms and arteriovenous malformations of brain vessels.
In cardiology: acute myocardial infarction, prophylaxis of “ reperfusion syndrome”, unstable stenocardia.
In surgery: acute and chronic pancreatitis, pseudo-tumorous pancreatitis, peritonitis, pre- and the postoperative period in patients with chronic pancreatitis.
Recommended doses and method of administration
In neurology and neurosurgery the emoxipine solution emoxipine for infusions is administrated intravenously dropwisely in a daily dose of 10 mg/kg (2 ml/kg) for 10-12 days. It should be with a rate of 20-30 drops in a minute. In a subsequent changing to intramuscular injections 2-10 ml of 3 % emoxipine solution 2-3 times a day for 20 days.
In a cardiology the administration is started with intravenous dropwise (20-40 drops in a minute) introductions of 120-180 ml of the preparation (600-900 mg of) emoxipine 1-3 times a day for 5-15 days depending on disease course, with the subsequent changing to intramuscular introduction of 2-10 ml of 3 % emoxipine solution 2-3 times a day for 10-30 days.
In patients with acute and chronic pancreatitis in a stage of exacerbation, at peritonitises, before and after deep roentgenotherapy at pseudo-tumorous pancreatitis, at mechanical jaundice of various origin; and also in pre- and postoperative period in patients operated on organs of hepatopancreaticoduodenal zone should be introduced intravenously dropwisely 30 ml of the preparation (150 mg of emoxipine) 2 times a day for 10-15 days. The preparation should be introduced with a rate of 20-30 drops in a minute.
Side effects
Excitation (short-term), sleepiness, rising of arterial pressure, local reactions in the place of introduction (transient burning sensation, itch, pain), headache, pain in a region of heart, allergic reactions (itch, eruption, skin reddiness). In personses with chronic pathology of digestive apparatus organs the nausea, unpleasant sensations in a region of stomach are possible.
Contraindications
Application of the preparation is counter-indicative at individual intolerance, pregnancy.
Safety measures
It is necessary to constantly control a level of arterial pressure and parameters of blood coagulability during treatment.
Interactions with other medical products
a-tocopherol acetate potentiates an antioxidative emoxipine effect.
Emoxipine is not recommended to mix with others injection agents in one syringe.
The form of release
The emoxipine solution for infusions is released in 100 ml in glass bottles for blood, transfusion and infusional preparations.
