Digitalis glycoside tablets
Function and Efficacy
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, increases the amount of Ca2 in the cytoplasm, and increases 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 and delaying atrioventricular conduction. 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. Due to its negative frequency effect, the diastole period is relatively prolonged, which is beneficial to increase myocardial blood supply; large doses (usually close to the toxic dose) can directly inhibit the sinoatrial node, atrioventricular node and His bundle to present sinus bradycardia and varying degrees of atrioventricular conduction block; 3 Cardiac electrophysiological effects: 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 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 the atrium, 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; shortens the effective refractory period of Purkinje fibers.
Ingredients
Digitoxin
| Name | Description | Content | CAS NO. | Manufacturer |
|---|---|---|---|---|
| DigitoxinIngredients |
1. Positive inotropic effect: selectively binds to Na--K-ATPase on myocardial cell membrane, inhibits its activity, increases Ca2 concentration in myocardial cells, and thus enhances myocardial contractility; 2. Negative frequency effect: improves hemodynamic state, slows heart rate, delays atrioventricular conduction, and can directly inhibit the cardiac conduction system at high doses; 3. Cardiac electrophysiological effect: reduces sinoatrial node autonomy, increases Purkinje fiber autonomy, slows atrioventricular node conduction velocity, and may change arrhythmia characteristics. More |
71-63-6 | 1 |
Appearance
This product is white tablets.
Indication
It is mainly used for congestive heart failure. Because of its slow and lasting effect, it is suitable for long-term use by patients with chronic heart failure. It is especially suitable for patients with congestive heart failure accompanied by renal impairment.
Usage and Dosage
1 Common dosage for adults: total digitalization amount is 0.7-1.2 mg, 0.05-0.1 mg is given orally every 6-8 hours. The maintenance dose is 0.05-0.1 mg per day; 2 Common dosage for children: Digitalization is given three times or every 6 hours according to the following doses. Premature infants or full-term newborns, according to body weight 0.022 mg/kg or according to body surface area 0.3-0.35 mg/㎡; 2 weeks to 1 year old, according to body weight 0.045 mg/kg; 2 years old and above, according to body weight 0.03 mg/kg; 3 Maintenance dose is 1/10 of the total digitalization amount, once a day.
Adverse Reactions
1. Common adverse reactions include: new arrhythmias, poor appetite or nausea, vomiting (stimulation of the medullary center), lower abdominal pain, weakness, etc.; 2. Rare reactions include: blurred vision or yellow vision (symptoms of poisoning), 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, 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. New
Precautions
1. Poisoning by any cardiac glycoside preparation; 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.
Special Population Medication
Precautions for children: Newborns have uncertain tolerance to this product, and their renal clearance is reduced. Premature infants and immature infants are sensitive to this product, and the dosage must be reduced according to their degree of immaturity. Infants over 1 month old need a slightly larger dosage than adults based on body weight or body surface area. Precautions for pregnancy and lactation: ① This product can pass through the placenta, so the maternal dosage may increase in the late pregnancy, and the dosage must be gradually reduced 6 weeks after delivery; ② This product can be excreted into breast milk, and lactating women must weigh the pros and cons when using it.
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, cholestyramine (cholestyramine) and other anion exchange resins, sulfasalazine or neomycin, and para-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 injection 1. When this product is used together with antacids, cocaine, pancuronium bromide (PancuroniumBromide, Pankelong, Bahuolang), rauwolfia alkaloids, succinylcholine (Scoline; SuxamethoniumChloride) or adrenergic drugs, arrhythmias may occur due to additive effects; 2. Digitalized patients with severe or complete atrioventricular block and normal blood potassium should not use potassium salts at the same time, but when thiazide diuretics are used with this product, potassium salts are often required to prevent hypokalemia; 3. The use of beta-receptor blockers with this product may cause severe bradycardia due to atrioventricular block, which should be taken seriously. However, 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 digitalis is discontinued, its blood concentration continues to rise. This is because quinidine replaces digitalis from tissue binding and reduces its distribution volume. When the two drugs are used together, the dosage of digitalis should be reduced by 1/2-1/3; 7 When used together with verapamil, diltiazem, and amiodarone, the blood concentration of digitalis can be increased due to the reduction of the renal and systemic clearance rate, 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 (EdrophoniumChloride, Tensilon) and this product can cause obvious bradycardia when used together; 11 Indomethacin (Indometacin) 12 When used together with heparin, this product may partially offset the anticoagulant effect of heparin, so the dosage of heparin needs to be adjusted; 13 During digitalization, intravenous use of magnesium sulfate should be very cautious, especially when calcium salts are injected intravenously at the same time, as heart block may occur; 14 Erythromycin can increase the absorption of this product in the gastrointestinal tract due to changes in the gastrointestinal flora; 15 Metoclopramide (Maxolon) reduces the bioavailability of digitalis by about 25% due to the promotion of intestinal motility. Propanedi increases the bioavailability of digitalis by about 25% due to its inhibition of intestinal peristalsis; 16 During the use of cardiac glycosides, or within 7 days after discontinuation, avoid the use of epinephrine, ephedrine and their similar drugs, because these drugs may increase the toxicity of cardiac glycosides; 17 Reserpine can increase the toxic reaction of digitalis to the heart, causing arrhythmias, and increase the excretion of digitalis glycosides, so caution should be exercised when using the two together with reserpine.
Storage
Keep sealed.
Packaging Specification
0.1 mg
Validity Period
36 months