Строфант - Strophanthus
For medical purposes mainly used 3 type strophanthus: Van strofant, Strophanthus Strophanthus bristly and smooth, which is a perennial tropical tree vines up to 4 m, families kutrovыh (Apocynaceae). With the purpose of treatment using mature seeds, from which the drug-strophanthin K.
The chemical composition of strophanthus
The seeds contain strophanthus cardiac glycoside - strophanthin. Depending on the plant species distinguish K-strophanthin and C-strophanthin (uaʙain). Besides, Combe strophanthus seeds contain K-strofantozid, cymarin, cimarol, glûkocimarol, gelvetikozid, glyukogelvetikozid, perilocimarin, emitsiarin. The seeds strophanthus bristly found K-strofantozid, cymarin, saponins, mix, trigonelline and fatty oils, and seeds smooth strophanthus, in addition to the C-strophanthin, Found resin, fixed oil, saponins, trigonelline and choline.
Chemically Strophanthin is a steroidal glycoside, Genin (aglycone) which is strofantidin, as part of the sugar (glycolic) represented by D-cymarose and D-glucose. Genin - the main carrier of cardiac glycosides cardiotonic activity - involves a complex nucleus tsiklopentapergidrofenantrena and unsaturated five-membered lactone ring with C17.
The pharmacological properties of drugs strophanthus
Strophanthin fairly well studied experimentally. Its biological activity is in the range 43000-58000 ICE, or CUD 5800-7100. In experiments on different kinds of animals in isolated hearts and hearts in situ K-strophanthin-β increases the amplitude of cardiac contractions, It increases the tone of the heart muscle and slows the heart rate. In toxic doses strophanthin causes cardiac arrest in systole.
Under the influence of the drug on ECG changes the duration of the cardiac cycle due to the shortening of the systolic and diastolic lengthening periods. Besides, found, that K-β-strophanthin slightly increases blood pressure, increases the amplitude of the pulse wave.
In the experimental heart failure action strophanthin manifested mainly in the increase of shock and cardiac output, in enhancing the level of myocardial contractility in combination with an elongation diastole, which creates the most economical mode of cardiac activity, providing favorable conditions for the recovery of energy resources.
Cardiac action strophanthin, as well as other cardiac glycosides, develop without increasing myocardial oxygen consumption, that is the main positive point in therapy. Influenced strophanthin decreases venous stasis, decreases venous pressure and total peripheral resistance. As a result, improves blood circulation, oxygenation of the heart and other organs, increased diuresis, disappear or decrease swelling.
The positive inotropic effect strophanthin largely determined by its direct action on the heart myotropic. Bradycardic impact glycoside developed by enhancing vagal tone; improve reflexes mechanoreceptors sinoaortalnoy zone caused by them due to the increase in blood pressure during systole, and as a result of the slowing of the pulse atrioventricular bundle.
The mechanism of action of cardiac glycosides cardiac, including strophanthin, is not fully understood. Currently, however, believe, that cardiac glycosides increase the content of ionized calcium, which, interacting protein troponin, activates the heart muscle contractile protein actomyosin, thereby increasing the power and heart rate. There is evidence about the direct effect of cardiac glycosides on actomyosin, as well as the stimulating effect strophanthin on energy metabolism in the myocardium and potassium-sodium exchange in the cell. As a result, the content of sodium ions inside the cell increases, and potassium ions - decreases, which leads to corresponding changes in myocardial contractility.
We also study the possibility of exposure of cardiac glycosides on the exchange of catecholamines in heart.
The use of drugs in medicine strophanthus
Strofantin - Highly efficient and fast-glycoside. When administered intravenously, car- diotonicheskoe its effect manifests itself either immediately or after 3-10 minutes, It reaches its maximum after 30-90 minutes and lasts for a day or more longer.
Strofantin, However, pretty quickly completely eliminated from the body. First 24 h stands approximately 7/8 Introducion dose. Therefore cumulative properties strophanthin mild. If ingestion is ineffective strophanthin, because it is poorly absorbed and rapidly destroyed in the gastrointestinal tract. Provided strophanthin mainly kidneys unchanged.
Apply strophanthin for acute cardiovascular disease, including soil acute myocardial infarction; in severe forms of chronic circulatory failure II and stage III, especially after failure of treatment with digitalis. Strophanthin optimal therapeutic effect is manifested in the heart dilatation.
Leveraging the reduction of myocardial, drug sosobstvuet greater expulsion of blood from the heart cavities. Weakly pronounced effect on the system strophanthin vagus nerve and conduction system of the heart allows its use in heart failure as a normal heart rate, and at bradisistolicheskoy atrial fibrillation, slow atrioventricular conduction.
Side effect. If overdose appear nausea, vomiting, diarrhea, various types of arrhythmia, often the type of ventricular bigeminy, dissociation rate, electric alternation, parasistolija, ventricular tachycardia. Less developed severe bradycardia, violation atrioventriku- polar conductivity. Besides, cardiac glycosides can cause muscle weakness, Headache, allergic skin rashes, mental disorders (hypererethism, hallucinations), visual impairment, color perception and other phenomena.
To eliminate the toxic effects dose should be reduced, increase the intervals between doses of the drug. Recommended drip intravenous potassium chloride. To eliminate the arrhythmia, does not disappear after application of potassium, prescribed Inderal (propranolol) orally at a dose of 10-30 mg 3 once a day. Apply also preparations, binding calcium ions (tetatsin lime, disodium edetate), unithiol. To mitigate the effect of the vagus nerve on the heart used atropine, for removing flicker, and ventricular fibrillation - electrical stimulation.
Contraindications. Strophanthin contraindicated in significant organic changes in the heart muscle and blood vessels, as well as acute infectious myocarditis, endokardite, a pronounced cardiosclerosis. Caution should be used strophanthin patients with incomplete atrioventricular block, thyrotoxicosis, and together with calcium and hypoglycemia.
Formulations, Dosage and administration of drugs strophanthus
Tincture strophanthus (Tincture Strophanthi). Available in concentration 1:10 on 70 % alcohol; Biological activity 1 ml 180-220 LED, or 24-28 CUD. Administered orally in chronic heart failure stage I. Assign an adult to 5-8 drops, children - depending on the age of 1 to 5 drops 2-4 times daily. The highest single dose for adults 10 drops (0,2 ml), daily - 20 drops (0,4 ml).
Strophanthin-K (Strophanthin-K). The white crystalline powder, it is soluble in water, is more soluble in alcohol. Available in capsules in the form 0,05 % solution, Biological Activity 1 ml solution equals 22-29 ICE, or 2.9-3.5 CUD. Enter intravenous slowly (for 5-6 min) or drop by 0.5-1 ml (0,250.5 mg) 10-20 ml 5 %, 20 % or 40 % glucose solution and isotonic sodium chloride solution 1 time (rarely 2 times) per day.
Sometimes appointed strophanthin intramuscularly. To eliminate the pain (due to the pronounced irritant effect of the drug previously administered 5 ml 2 % Novocaine.
It takes care and accuracy in dose selection, and indications for use. Previously patients received other cardiac glycosides, before using strophanthin need to take a break: After slabokumuliruyuschihsya glycosides - about 5 days, after drugs with a strong cumulative effect - within 10-14 days.
The highest single dose strophanthin For adult admission 0,0005 g (0,5 mg), daily - 0,001 g (1 mg) or correspondingly 1 and 2 ml 0,05 % solution.