Digoxin tablets
Function and Efficacy
At therapeutic doses: 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, impairing the active coupled transport of Na-K inside and outside the myocardial cell membrane, increasing the concentration of Na in myocardial cells, thereby activating the NaCa2 exchange on the sarcolemma, increasing the Ca2 in the cytoplasm, and increasing the Ca2 reserve in the sarcoplasmic reticulum. When the myocardium is excited, more Ca2 is released; the increase in the concentration of Ca2 in myocardial cells excites myocardial contractile proteins, thereby increasing myocardial contractility; 2. Negative frequency effect: Due to its positive inotropic effect, it increases the cardiac output of the failing heart, improves the hemodynamic state, eliminates the reflex increase of sympathetic nerve tension, and enhances the vagus nerve tension, thereby slowing down the heart rate. In addition, at low doses, it increases the sensitivity of the sinoatrial node to vagus nerve impulses, which can enhance its effect of slowing down the heart rate. Large doses (usually close to the toxic dose) can directly inhibit the sinoatrial node, atrioventricular node and His bundle, resulting in sinus bradycardia and varying degrees of atrioventricular conduction block; 3 Cardiac electrophysiological effects: Reduce the autonomy of the sinoatrial node through direct effects on myocardial electrical activity and indirect effects on the vagus nerve; Improve the autonomy of Purkinje fibers; Slow down the conduction velocity of the atrioventricular node, prolong its effective refractory period, resulting in increased latent conduction of the atrioventricular node, which can slow down the ventricular rate of atrial fibrillation or atrial flutter; Since this drug shortens the effective refractory period of atrial heart, when used for atrial tachycardia and atrial flutter, it may lead to acceleration of the atrial rate and conversion of atrial flutter to atrial fibrillation; shorten the effective refractory period of Purkinje fibers.
Ingredients
The chemical name of this product is: 3beta;-[[O-2,6-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. Molecular formula: C41H64O14 Molecular weight: 780.95.
Appearance
This product is white tablets.
Indication
1. Used for acute and chronic heart failure such as hypertension, valvular heart disease, congenital heart disease, etc. It is especially suitable for heart failure with atrial fibrillation accompanied by rapid ventricular rate; it has poor efficacy for heart failure caused by cor pulmonale, severe myocardial ischemia, active myocarditis and extracardiac factors such as severe anemia, hypothyroidism and vitamin B1 deficiency; 2. Used to control the ventricular rate and supraventricular tachycardia of patients with atrial fibrillation and atrial flutter accompanied by rapid ventricular rate.
Usage and Dosage
Common dosage for adults. Oral: commonly used 0.125-0.5 mg, once a day, steady-state blood concentration can be reached in 7 days; if the rapid loading dose is reached, 0.25 mg can be administered every 6-8 hours, with a total dose of 0.75-1.25 mg/day; maintenance dose, once a day 0.125-0.5 mg. Common dosage for children. Oral: total amount of this product, premature infants 0.02-0.03 mg/kg; newborns under 1 month old 0.03-0.04 mg/kg; 1 month to 2 years old, 0.05-0.06 mg/kg; 2-5 years old, 0.03-0.04 mg/kg; 5-10 years old, 0.02-0.035/kg; 10 years old or above, according to the common dosage for adults; the total amount of this product is given in 3 times or every 6-8 hours. The maintenance dose is 1/5 to 1/3 of the total amount, divided into 2 times, once every 12 hours or once a day. In infants and young children (especially premature infants), the dose should be carefully titrated and the blood drug concentration and electrocardiogram should be closely monitored. In recent years, studies have shown that digoxin can reach a stable concentration in the body after 6 to 7 days of daily administration of a fixed dose and exert its full effect. Therefore, for patients with mild conditions but prone to poisoning, daily administration of 5.5 mg/kg can also achieve satisfactory therapeutic effects and reduce the incidence of poisoning.
Adverse Reactions
1 Common adverse reactions include: proarrhythmic effects, poor appetite or nausea, vomiting (stimulation of the medullary center), lower abdominal pain, abnormal weakness, weakness; 2 Rare reactions include: blurred vision or color vision, such as yellow vision, green vision, diarrhea, central nervous system reactions such as depression or confusion; 3 Rare reactions include: drowsiness, headache and rash, urticaria (allergic reaction); 4 Among the manifestations of digitalis poisoning, proarrhythmia is the most important, and the most common is ventricular premature beats, accounting for about 33% of proarrhythmic adverse reactions. The second is atrioventricular block, paroxysmal or accelerated junctional tachycardia, paroxysmal atrial tachycardia with atrioventricular block, ventricular tachycardia, sinus arrest, ventricular fibrillation, etc.
Precautions
1. Combined with calcium injection; 2. Poisoning by any digitalis preparation; 3. Ventricular tachycardia, ventricular fibrillation; 4. Obstructive hypertrophic cardiomyopathy (can still be considered if accompanied by systolic dysfunction or atrial fibrillation); 5. Preexcitation syndrome with atrial fibrillation or flutter.
Special Population Medication
Precautions for children: 1. Children's tolerance to this product is uncertain, and their renal clearance is reduced; 2. Children and immature children are sensitive to this product, and the dosage should be reduced according to their degree of immaturity. In terms of body weight or body surface area, the dosage for infants over 1 month old is slightly larger than that for adults. Precautions for pregnancy and lactation: This product can pass through the placenta, so the maternal dosage may increase in the late pregnancy, and the dosage must be reduced 6 weeks after delivery. This product can be excreted into breast milk, and lactating women must weigh the pros and cons when using it. Precautions for the elderly: Elderly people with impaired liver and kidney function, reduced apparent distribution volume, or electrolyte imbalance have low tolerance to this product and must reduce the dosage.
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 can cause hypokalemia and lead to digitalis poisoning; 2. When used together with antacids (especially magnesium trisilicate) or antidiarrheal adsorbents such as white clay, pectin, colestyramine (cholestyramine) and other anion exchange resins, sulfasalazine or neomycin, and aminosalicylic acid, it can inhibit the absorption of digitalis cardiac glycosides and lead to a weakening of the effect of cardiac glycosides; 3. When used together with antiarrhythmic drugs, calcium salt injections , cocaine, pancuronium bromide (PancuroniumBromide, Pankelong, Bahuolang), rauwolfia ine, succinylcholine (Scoline; SuxamethoniumChloride) or adrenergic drugs when used together, arrhythmias may occur due to additive effects; 4. Patients with severe or complete atrioventricular block and normal blood potassium should not use potassium salts at the same time with digitalis, but when thiazide diuretics are used with this product, potassium salts are often required to prevent hypokalemia; 5. The use of beta-receptor blockers with this product may cause severe bradycardia due to atrioventricular block, which should be taken seriously. But it does not rule out the use of beta-blockers for supraventricular tachyarrhythmias where digitalis cannot control the ventricular rate; 6. When used together with quinidine, the blood concentration of this product can be increased by about one-fold. The degree of increase is related to the dosage of quinidine and can even reach toxic concentrations. Even if digoxin is discontinued, its blood concentration continues to rise. This is because quinidine replaces digoxin from tissue binding and reduces its distribution volume. When the two drugs are used together, the dosage of digoxin should be reduced by 1/2-1/3; 7 When used together with verapamil, diltiazem, and amiodarone, the blood concentration of digoxin can be increased due to the reduction of the renal and systemic clearance rate of digoxin, which can cause severe bradycardia; 8 Spironolactone can prolong the half-life of this product, and the dose or dosing interval needs to be adjusted, and the blood concentration of this product should be followed up and monitored; 9 Angiotensin converting enzyme inhibitors and their receptor antagonists can increase the blood concentration of this product; 10 EdrophoniumChloride (Tensilon) and this product can cause obvious bradycardia when used together; 11 Indomethacin (Indome 12. When used with heparin, this product may partially offset the anticoagulant effect of heparin, so the dosage of heparin needs to be adjusted; 13. When using magnesium sulfate intravenously during digitalization, extreme caution should be exercised, especially when calcium salts are also injected intravenously, as heart block may occur; 14. Erythromycin can increase the absorption of this product in the gastrointestinal tract by changing the gastrointestinal flora; 15. Metoclopramide (Maxolon) reduces the bioavailability of digoxin by about 25% due to promoting intestinal motility. Propane increases the bioavailability of digoxin by about 25% due to inhibiting intestinal peristalsis.
Storage
Keep tightly closed.
Packaging Specification
0.25mg
Validity Period
36 months
Manufacturer
Sanofi (Hangzhou) Pharmaceuticals Co., Ltd.
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Founded in:
1995-11-30 -
Address:
No. 325, Jiangling Road, Binjiang District, Hangzhou City, Zhejiang Province -
Tax NO.:
91330100609136127P -
Registered Funds:
$28.8 million -
Website:
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Email: