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Scutellarin K injection

Function and Efficacy

This product is a cardiac glycoside extracted from the seeds of Convolvulus comfrey. It has high chemical polarity and low lipid solubility. It is a commonly used, efficient, fast-acting, short-acting cardiac glycoside. 1. Positive inotropic effect: This product selectively binds to the Na--K ATPase of the myocardial cell membrane and inhibits the activity of the enzyme, which damages the active coupled transport of Na﹣K inside and outside the myocardial cell membrane, increases the Na concentration in the myocardial cell, and thus makes the NaCa2 exchange on the sarcolemma more active, increases the Ca2 in the cytoplasm, and increases the Ca2 reserves in the sarcoplasmic reticulum. When the myocardium is excited, more Ca2 is released; the Ca2 concentration in the myocardial cell increases, which excites the myocardial contractile protein and increases the myocardial contractility; 2. Negative frequency effect: Due to its positive inotropic effect, the hemodynamic state is improved, and the reflex The increase in sympathetic nerve tone enhances vagal nerve tone, thereby slowing down the heart rate and delaying atrioventricular conduction; 3. Cardiac electrophysiological effects: reducing the autonomy of the sinoatrial node; improving the autonomy of Purkinje fibers; slowing down the conduction velocity of the atrioventricular node and prolonging its effective refractory period, resulting in an increase in latent conduction of the atrioventricular node, which can slow down the ventricular rate of atrial fibrillation or atrial flutter; because this drug shortens the effective refractory period of the atrium, when used for atrial tachycardia and atrial flutter, it may cause an acceleration of the atrial rate and the conversion of atrial flutter to atrial fibrillation; shortening the effective refractory period of Purkinje fibers; 4. Extracardiac effects of cardiac glycosides: Toxic doses of cardiac glycosides can cause central nervous system excitement, headache, dizziness, fatigue and drowsiness, and sometimes neuralgia, pain in the lower 1/3 of the face, similar to trigeminal neuralgia. Vomiting is caused by the stimulation of the emetic chemoreceptor area in the medulla oblongata. In severe cases, abnormal behavior and mental symptoms may occur, especially in the elderly with arteriosclerosis, such as disorientation, aphasia, hallucinations and delirium. Because cardiac glycosides affect the function of the optic nerve, they may even cause retrobulbar optic neuritis and optic nerve disorders such as blurred vision, diplopia and color vision (yellowing or green vision). The stimulation of the central sympathetic nerve by toxic amounts of cardiac glycosides causes excessive sympathetic nerve tension, which is the neurological factor for cardiac glycosides to induce arrhythmias. Cardiac glycosides have a direct contractile effect on human arteries and veins, which is a direct effect of cardiac glycosides on blood vessels; 5 The therapeutic concentration of digitoxin is 15-30ng/ml; the crossover concentration is 25-35ng/ml; the toxic concentration is 35ng/ml; 6 The electrophysiological effect of toxic concentration cardiac glycosides is due to the fact that cardiac glycosides significantly inhibit the Na-KATPase of myocardial cell membrane, increase the accumulation of [Na]i, and significantly reduce [K]i, resulting in a decrease in the maximum diastolic potential of myocardial cell membrane, an increase in autonomy, a decrease in the excitation of the myocardium and Purkinje fibers, a delay in the conduction velocity of the atrioventricular node, Purkinje fibers and myocardium, and varying degrees of atrioventricular conduction block. Toxic doses of cardiac glycosides can also cause excessive Ca2 concentration in myocardial cells, resulting in Ca2 overload, causing the intracellular Ca2 storage to oscillate in the release and reuptake of Ca2. At the same time, the cell membrane permeability to Na increases, stimulating a short inward current, causing delayed depolarization of the myocardial cell membrane, and inducing myocardial triggered activity. This is one of the mechanisms by which toxic doses of cardiac glycosides induce arrhythmias.

Ingredients

This product is a mixture of various glycosides obtained from the dried mature seeds of Strophanthukkombe Oliv, a plant of the Apocynaceae family.

Appearance

This product is a colorless or slightly yellow clear liquid.

Indication

This product is suitable for acute congestive heart failure, especially for patients who are not responsive to digitalis. It can also be used for patients with acute heart failure and atrial fibrillation with normal or slow heart rate.

Usage and Dosage

Intravenous injection: Common dosage for adults: 0.125-0.25 mg for the first dose, add 20-40 ml of isotonic glucose solution and slowly inject (for no less than 5 minutes), repeat 0.125-0.25 mg as needed after 2 hours, total amount 0.25-0.5 mg per day; Maximum dose: 0.5 mg for one intravenous injection, 1 mg per day. After the condition improves, oral digitalis preparations can be used instead. The lethal dose for adults is 10 mg; Common dosage for children: 0.007-0.01 mg/kg based on body weight or 0.3 mg/m2 based on body surface area, half the dose for the first dose, and the rest divided into several equal parts, given at intervals of 0.5-2 hours.

Adverse Reactions

1. Common adverse reactions include: new arrhythmias, poor appetite or nausea, vomiting (stimulation of the medullary center), lower abdominal pain, obvious weakness, and tenderness; 2. Rare reactions include: blurred vision or yellow vision (symptoms of poisoning), diarrhea, and central nervous system reactions such as depression or confusion; 3. Rare reactions include: drowsiness, headache and rash, urticaria (allergic reaction), etc.; 4. Among the manifestations of poisoning, arrhythmias are the most important, and the most common is ventricular premature beats, accounting for about 33% of adverse cardiac reactions. The second is atrioventricular block, paroxysmal or accelerated junctional tachycardia, paroxysmal atrial tachycardia with atrioventricular block, ventricular tachycardia, ventricular fibrillation, sinus arrest, etc. Arrhythmias are more common in children than other reactions.

Precautions

Contraindicated use: 1 Patients poisoned by any cardiac glycoside preparations; 2 Ventricular tachycardia, ventricular fibrillation; 3 Obstructive hypertrophic cardiomyopathy (can still be considered if accompanied by systolic dysfunction or atrial fibrillation); 4 Preexcitation syndrome with atrial fibrillation or flutter; 5 AVB (atrioventricular block) above Ⅱo.

Drug Interactions

1. When used together with amphotericin B, corticosteroids or potassium-losing diuretics such as bumetanide (the product is buturamine) and ethacrynic acid (ethacrynic acid), it may cause hypokalemia and lead to digitalis poisoning; 2. When used together with antiarrhythmic drugs, calcium salt injection, cocaine, pancuronium bromide (Pancuronium Bromide, Pan Kelong, Bahuolang), rauwolfia alkaloids, succinylcholine (Scoline; Suxamethonium Chloride) or adrenergic drugs, arrhythmias may be caused due to additive effects; 3. Digitalized patients with severe or complete atrioventricular block with normal blood potassium should not use potassium salts at the same time. When thiazide diuretics are used together with this product, potassium salts are often required to prevent hypokalemia; 4. Be careful when beta-receptor blockers are used together with this product, as there is a possibility of severe bradycardia in atrioventricular block. However, it does not exclude the use of beta-blockers when digitalis cannot control supraventricular tachyarrhythmia; 5. When used together with quinidine, the blood concentration of this product can be increased by about one-fold, and the degree of increase is related to the dosage of quinidine, and can even reach toxic concentrations; 6. When used together with verapamil, diltiazem, and amiodarone, the blood concentration of cardiac glycosides can be increased due to the reduction of renal and systemic clearance of cardiac glycosides, which can cause severe bradycardia; 7. Spironolactone can prolong the half-life of this product, and the dosage or dosing interval needs to be adjusted, and the blood concentration of this product needs to be monitored; 8. Angiotensin converting enzyme inhibitors and their receptor antagonists can make this product The blood concentration of this product increases; 9 EdrophoniumChloride (Tensilon) combined with this product can cause obvious bradycardia; 10 Indomethacin (Indomethacin) can reduce the renal clearance of this product, prolong the half-life of this product, and there is a risk of poisoning, so the blood concentration and electrocardiogram need to be monitored; 11 When used with heparin, since this product may partially offset the anticoagulant effect of heparin, the dosage of heparin needs to be adjusted; 12 When using this product, intravenous injection of magnesium sulfate should be extremely cautious, especially when intravenous calcium salt is injected, heart conduction block may occur.

Storage

Keep away from light and store in airtight container.

Packaging Specification

1 ml: 0.25 mg

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