Emoxipine (1 % solution for injections)
Solutio Emoxipini 1 % pro injectionibus
International nonproprietary name
Emoxipine.
Emoxipine.
Pharmacotherapeutic group
Antiaggregants. Antihypoxants and antioxidants. Angioprotectors, microcirculationcompensators.
Composition of the preparation
1 ml of solution for injections contains 10 mg of emoxipine.
Pharmacological action
Pharmacodynamics
Emoxipine reduces permeability of vascular wall, viscosity and coagulability of blood, agglutination ability of erythrocytes. Increases process of fibrinolysis. Improves microcirculation.
Effectively inhibits free-radical oxidation of biomembranes 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.
Indications
In ophthalmology: central chorioretinal dystrophias, dystrophic changes of retina at high degree myopia, diabetic retinopathy, occlusions of the central vein of retina and its branches, glaucoma, opticoneuropathies of various origin, hemophthalmias, hyphemas, keratites, keratoconus, uveites.
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.
Dosage and method of administration
In patients with central chorioretinal dystrophias, dystrophic changes of retina at high degree myopia, at diabetic retinopathy, occlusion of the central vein of a retina and its branches, glaucoma, opticoneuropathies should be administrated retrobulbarly (parabulbarly) per 0,5-1,0 ml of 1 % solution 1 time a day for 10-15 days (course dose at one eye lesion is 100-150 mg, at bilateral lesion - 200-300 mg); intravenously dropwisely in a dose of 150-300 mg a day 1 time for 5-10 days (5-10 ml of 3 % emoxipine solution is diluted in 200 ml sodium chloride isotonic solution and is introduced with a rate of 20-30 drops in a minute). At hyphemas, keratites, keratoconus, uveites - subconjunctivally per 0,2-0,5 ml of 1 % solution 1 time a day for 10-15 days.
In neurology and neurosurgery emoxipine is administrated intravenously dropwisely in a daily dose of 10 mg/kg for 10-12 days. Before introduction emoxipine is diluted in 200 ml of sodium chloride isotonic solution. Should be introduced with a rate of 20-30 drops in a minute. In the acute period (the first 3-12 hours) of ischemic and hemorrhagic insult should be introduced intra-arterially (inter-carotidly) 1 time a day slowly by bolus dosing of 150-300 mg (5-10 ml 3 % of emoxipine solution per 10 ml of sodium chloride isotonic solution) for the first three days.
In a cardiology the administration is started with intravenous dropwise (20-40 drops in a minute) introductions of 20-30 ml of 3 % emoxipine solution (600-900 mg) in 200 ml of sodium chloride isotonic solution or 5 % glucose solution 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 % 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 2 times a day for 10-15 days in a dose of 150 mg: 5 ml of 3 % emoxipine solution is diluted in 200 ml of sodium chloride isotonic solution and introduced with a rate of 20-30 drops per minute. At acute necrotizing pancreatitis the preparation should be introduced into celiac trunk, in a dose of 150-300 mg for 4-5 days (5-10 ml of 3 % emoxipine solution is diluted in 50-100 ml of sodium chloride isotonic solution and introduced with a rate of 1-2 ml in a minute). In patients with acute pancreatitis at low-invasive interventions under US control and laparoscopies should be introduced as follows: 10 ml of 1 % emoxipine solution is diluted in a syringe by 10 ml of sodium chloride isotonic solution and in regular intervals is infiltrated in parapancreatic cellular tissue and omental bursa, and also should be introduced into cavities after aspiration of pancreatic liquid accumulation.
The treatment by emoxipine, in case of its intravenous and intraarterial introduction, is necessary to carry out under the control of arterial pressure and functional condition of coagulatve andanticoagulative blood systems.
Side effects
In a place of introduction the pain, burning sensation, itch, reddening, hardening of paraorbital tissues, resolving independently are possible at retrobulbar (parabulbar) and subconjunctival introduction; at intravenous introduction - burning sensation in vein; rising of arterial pressure, exaltation or sleepiness can be also marked}. At predisposition to allergic reactions in rare cases an itch and skin redness are observed.
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 medicinal preparations
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
1 % solution in 1 ml ampoules.
