Digoxin elixir
Function and Efficacy
At therapeutic doses, it has: 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 impairs the active coupled transport of Na﹣K inside and outside the myocardial cell membrane, increases the concentration of Na in myocardial cells, and thus makes the Na+-Ca2+ exchange on the sarcolemma active, increasing the amount of Ca2+ in the cytoplasm; the Ca2+ reserves in the sarcoplasmic reticulum also increase, and when the myocardium is excited, more Ca2+ is released; the concentration of Ca2+ in myocardial cells increases, and the excitement of myocardial contractile proteins is enhanced, thereby increasing myocardial contractility. 2. Negative frequency effect: Due to its positive inotropic effect, it increases the cardiac output of the failing heart, improves hemodynamics, eliminates the reflex increase of sympathetic nerve tension, and enhances vagal nerve tension, thereby slowing down the heart rate and delaying atrioventricular conduction. In addition, at low doses, it increases the sensitivity of the sinoatrial node to vagal impulses, which can enhance its effect of slowing down the heart rate. Due to its negative frequency effect, the diastole is relatively prolonged, which is beneficial to increase myocardial blood supply; large doses can directly inhibit the sinoatrial node, atrioventricular node and His bundle, resulting in sinus bradycardia and varying degrees of atrioventricular conduction block. 3 Through direct effects on myocardial electrical activity and indirect effects on the vagus nerve, it reduces the autonomy of the sinoatrial node; improves the autonomy of Purkinje fibers; slows down the conduction velocity of the atrioventricular node, prolongs its effective refractory period, and leads to an increase in the 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; shortens the effective refractory period of Purkinje fibers.
Ingredients
The chemical name of this product is: 3beta;-[[O-2, O-dideoxy-beta;-D-core-hexopyranosyl-(1rarr;4)-O-2, 6-dideoxy-beta;-D-core-hexopyranosyl-(1rarr;4)-2, 6-dideoxy-beta;-D-core-hexopyranosyloxy]-12beta;, 14beta;-dihydroxy-5beta;-cardiosteroid-20(22)ene lactone. Its molecular formula: C41H64O14. Molecular weight: 780.95.
Appearance
Slightly yellow clear liquid; sweet and slightly mellow taste.
Indication
1. For acute and chronic heart failure. It has good effects on heart failure caused by hypertension, valvular disease (except for severe simple type II valvular stenosis or aortic stenosis), and congenital heart disease, especially for heart failure with atrial fibrillation and rapid ventricular rate; it has poor effects on heart failure caused by cor pulmonale, severe myocardial ischemia, active myocarditis, and extramyocardial mechanical factors; it has poor effects on heart failure secondary to severe anemia, hypothyroidism, and vitamin B1 deficiency; 2. It is used to control the ventricular rate and supraventricular tachycardia in patients with atrial fibrillation and atrial flutter with rapid ventricular rate.
Usage and Dosage
Clinical application is 0.125-0.5mg equivalent elixir: 2.5ml-10ml, once a day. For patients with acute and severe heart failure who have not used digitalis preparations within two weeks, one or several loading doses can be given appropriately, 0.125-0.5mg equivalent elixir each time, once every 6-8 hours, with a total dose of 0.75mg-1.0mg equivalent elixir. Digoxin elixir 10ml: 0.5mg; 30ml: 1.5mg; 100ml: 5mg (mainly used for children). Elixir is a sweet dilute alcohol solution for oral administration. Elixir contains aromatics, sweeteners and ethanol. The ethanol content is mostly between 5% and 40%, ethanol is volatile, and the concentration increases; because elixir contains alcohol and glycerin, the cost is relatively high, and it is rarely used in China.
Adverse Reactions
1. Common adverse reactions include: new arrhythmias, poor appetite or nausea, vomiting, lower abdominal pain, weakness, and flabbyness. 2. Rare reactions include: blurred vision or color vision (poisoning symptoms such as xanthoopia, etc.), diarrhea, depression or confusion. 3. Rare reactions include: drowsiness, headache and rash, urticaria (allergic reaction). 4. Among the manifestations of digitalis poisoning, arrhythmias are the most important, and the most common is ventricular premature beats, accounting for about 33% of cardiac reactions. The second is atrioventricular block, paroxysmal or accelerated junctional tachycardia, paroxysmal atrial tachycardia with atrioventricular block, ventricular tachycardia, sinus arrest, ventricular fibrillation, etc. Arrhythmias are more common in children than other reactions, but ventricular arrhythmias are less common than in adults.
Precautions
1. Used in combination with calcium injection; 2. Poisoning by any cardiac glycoside preparation; 3. Ventricular tachycardia, ventricular fibrillation; 4. Obstructive hypertrophic cardiomyopathy (can still be used if accompanied by systolic dysfunction or atrial fibrillation); 5. Preexcitation syndrome with atrial fibrillation or flutter. Use with caution in the following conditions: (1) hypokalemia; (2) incomplete atrioventricular block; (3) hypercalcemia; (4) hypothyroidism; (5) ischemic heart disease; (6) myocardial infarction; (7) myocarditis; (8) renal impairment; (9) alcohol allergy.
Special Population Medication
Precautions for children: This experiment has not been conducted and there is no reliable reference. Precautions for pregnancy and lactation: This experiment has not been conducted and there is no reliable reference. Precautions for the elderly: This experiment has not been conducted and there is no reliable reference.
Drug Interactions
1. When used in combination with amphotericin B, corticosteroids or potassium-losing diuretics such as bumetanide and ethacrynic acid, digitalis poisoning may occur due to hypokalemia. 2. When used in combination with antacids (especially magnesium trisilicate) or antidiarrheal adsorbents such as kaolin, pectin, colestyramine and other anion exchange resins, sulfasalazine or neomycin, and para-aminosalicylic acid, the absorption of digitalis cardiac glycosides may be inhibited. 3. When used in combination with antiarrhythmic drugs, calcium salt injections, cocaine or adrenaline-mimetic drugs, arrhythmias may occur. 4. Digitalized patients with severe or complete atrioventricular block and normal blood potassium should not use potassium salts at the same time, but hypokalemia should be prevented when thiazide diuretics are used in combination with this product. 5. The combination of beta-blockers and this product may cause severe bradycardia due to atrioventricular block. However, it does not rule out the use of beta-blockers for supraventricular tachyarrhythmias where digitalis cannot control the ventricular rate. 6. When used with quinidine, the blood concentration of this product can be increased by about one-fold. When the two drugs are used together, the dose of digoxin should be reduced by 1/2 to 1/3. 7. When used with verapamil, diltiazem, and amiodarone, it can cause severe bradycardia. 8. Spironolactone can prolong the half-life of this product. 9. Angiotensin-converting enzyme inhibitors and their receptor antagonists can increase the blood concentration of this product. 10. Indomethacin can prolong the half-life of this product, and blood concentration and electrocardiogram need to be monitored. 11. When used with heparin, it can partially offset the anticoagulant effect of heparin, and the dose of heparin should be adjusted. 12. Intravenous magnesium sulfate should be used with extreme caution during digitalization, as heart block may occur. 13 Erythromycin can increase the absorption of this product in the gastrointestinal tract.
Storage
Keep in a light-proof and airtight container.
Packaging Specification
5E-05
Validity Period
Tentative 48 months
Manufacturer
Beijing China Resources HI-TECH NATURAL Pharmaceutical Co., Ltd.
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Founded in:
1997-07-23 -
Address:
No. 11, Guishui South Street, Yanqing Town, Yanqing District, Beijing -
Tax NO.:
91110229103055813A -
Registered Funds:
87.4934 million yuan -
Email: