Active Ingredients

Β-Acetyldigoxin – Effect, Application & Risks


B-acetyldigoxin is a cardiac glycoside used in cardiac insufficiency . It has multiple positive effects on the heart . As a so-called prodrug, it is first converted into the active form digoxin in the body.

B-acetyldigoxin is one of the so-called glycosides. Glycosides are made up of a combination of sugar-like building blocks and non-sugar components. This creates complicated molecules that act as important active ingredients in the organism. Digoxin is produced in the body from β-acetyldigoxin , which is the actual active ingredient. β-acetyldigoxin still contains an acetyl group, which is removed during conversion to digoxin.

In the human organism, digoxin acts as a hormone . β-acetyldigoxin is obtained from certain types of foxgloves . Pharmacologically, it represents a so-called prodrug, which is deacetylated in the intestinal mucosa . This produces the actual heart-active active ingredient digoxin.

The use in cardiac insufficiency is intended to relieve the heart. Heart activity is more effective. In this way, cardiovascular activity is generally supported and ineffective heart functions are weakened. This allows the heart to concentrate more effectively on life-sustaining functions.

Five to ten percent of digoxin is metabolized in the liver . The rest is excreted unchanged via the kidneys. β-acetyldigoxin is more biologically available than digoxin. Therefore, instead of digoxin, this glycoside is first administered, which is still being converted in the body in preparation for the effect.

Pharmacological action

The actual cardioactive digoxin develops positive inotropic, negative chronotropic, negative dromotropic and positive bathmotropic effects on the heart. Overall, the heartbeat is optimized so that the lower cardiac output produces effective effects. Positive inotropic effects denote the ability of the heart to contract . In this case, the ability of the heart to contract is increased. This affects the contraction amplitude and the rate at which the contraction increases.

With the positive inotropic effect, the active influx of potassium ions into the cell and the simultaneous efflux of sodium ions out of the cell are inhibited. The higher concentration of sodium ions in the cell in turn inhibits calcium ejection from the cell. An increased concentration of calcium ions increases the contractility of muscles , especially the heart muscle .

The next effect of cardiac glycosides, the negative chronotropic effect, is the reduction of the heart’s beating rate . The combination of these two effects means focusing on fewer but more effective heartbeats. In the subsequent mode of action, the negative dromotropic effect, the excitation conduction of the heart is slowed down. Finally, the positive bathochromic effect lowers the threshold for heart excitability.

Medical Application & Use

A-acetyldigoxin is used in chronic heart failure that is already in stage 3 or even 4. It is said to strengthen the heart in the case of cardiac insufficiency. Furthermore, the heart rate should be reduced in certain forms of accelerated cardiac activity. In addition to manifest and chronic heart failure, permanent forms of paroxysmal atrial flutter and atrial fibrillation should also be treated.

The combination of the four different modes of action ensures that the heart is relieved, which now produces a stable cardiac performance with less force, but still effectively. As a result, the cardiac output can even be increased again somewhat, so that some patients can return to a higher cardiac output level. However, the ranges between positive and negative effects are often very narrow, which means that the medication needs to be dosed precisely.

Risks & side effects

However, B-acetyldigoxin or the actual active ingredient digoxin should be used with caution. In the case of certain diseases and disorders, the application is even counterproductive. A use of the drug is excluded in an AV block of the II. and III. degree, hypercalcemia (too much calcium in the blood), hyperkalemia , hypokalemia or bradycardia (low heart rate). Also with an enlargement of the heart, with carotid sinus syndrome, with special forms of cardiac arrhythmias , with aneurysms or with ventricular tachycardia, the result of heart attacksor medication, the use of cardiac glycosides is prohibited.

Of course, a ban on use also applies to existing hypersensitivity to cardiac glycosides. Contraindications also apply to pregnancy and lactation . To date, no complications have been observed when using β-acetyldigoxin in pregnancies. To be on the safe side, however, the drug should not be used in the first three months of pregnancy.

Side effects such as nausea , vomiting and loss of appetite , occasional headaches , insomnia , tiredness and, more rarely, indigestion , nightmares , confusion , depression or psychoses were observed relatively frequently when β-acetyldigoxin was used .

Rare side effects include the development of gynecomastia (breast gland enlargement), skin rash or blood platelet drop . The side effects also depend on the form in which the medication is administered. The interaction with other drugs must also be considered. Thus, intravenous administration of calcium increases the toxicity of β-acetyldigoxin. Diuretics or laxatives can lead to potassium or magnesium deficiencies. In this case, too, the use of β-acetyldigoxin is counterproductive.

Various drugs also reduce the effectiveness of cardiac glycosides or can even trigger cardiac arrhythmias in combination with these. These include drugs to lower blood pressure such as reserpine , drugs to relax muscles such as succinylcholine, tricyclic antidepressants, asthma drugs or drugs to increase potency.

Simultaneous intake with absorbent substances such as activated charcoal or kaolin pectin against diarrhea , cholesterol-lowering drugs or antacids (acid binders) inhibit absorption by the body and thereby weaken the effect. Finally, there is still a risk of allergic reactions to the drug in individual cases.

Lisa Newlon
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Hello! I am Lisa Newlon, and I am a medical writer and researcher with over 10 years of experience in the healthcare industry. I have a Master’s degree in Medicine, and my deep understanding of medical terminology, practices, and procedures has made me a trusted source of information in the medical world.