The drug adenosine use and contraindications. Adenosine is an effective antiarrhythmic agent

Adenosine is a drug that is used in ophthalmic practice, namely, this agent is intended for the treatment of cataracts. In addition, it is used for some pathological processes occurring in the cardiovascular system (if the patient has paroxysmal supraventricular tachycardia).

What is the effect of adenosine?

Adenosine is considered an endogenous biologically active substance that takes part in many important biochemical processes in the human body. It has an antiarrhythmic effect, mainly has a positive effect in the presence of supraventricular tachyarrhythmias.

In addition, it slows down AV conduction, significantly reduces the automatism of the sinus node, and has a coronary dilating effect. With slow intravenous administration, it can lead to a decrease in blood pressure.

When used topically in ophthalmic practice, adenosine takes part in reparative processes, it is involved in energy metabolism, and in addition, it slows down degenerative changes that can occur directly in the lens.

Due to the vasodilating action, the blood supply to the organ of vision is improved, which helps to remove toxic products, metabolic processes in the intraocular fluid are stimulated. Adenosine relieves inflammation in the conjunctiva, as well as in the cornea and other tissues of the eye.

When used topically, this active substance penetrates the cornea of \u200b\u200bthe eye and is well distributed over all tissues of the organ of vision. The drug is excreted as metabolites through the kidneys.

When combined with dipyridamole, the effect of the drug Adenosine may increase. When combined with caffeine and theophylline, the activity of this agent will be suppressed.

What are the indications for use of Adenosine?

Adenosine is used for intravenous bolus administration when supraventricular tachycardia is being treated. In addition, the tool is used as an aid for diagnostics in cardiological practice, for example, during scintiography, as well as in two-dimensional echocardiography.

And also Adenosine is used in ophthalmology for topical use as a drug for the treatment of cataracts.

What are the contraindications for use of Adenosine?

The conditions when the use of this agent is contraindicated include AV block II and III degrees, and it is also not used for ventricular tachycardia, and besides this, with hypersensitivity to adenosine.

What is the use and dosage of Adenosine?

As an antiarrhythmic drug, this agent is administered to adults as an intravenous bolus in just two seconds at a dosage of 6 mg. If no positive effect appears within a minute, then the dose is doubled, and the injection is repeated in an amount of 12 mg.

For children, this drug is administered as an antiarrhythmic agent in an amount of 50 μg / kg, while the maximum dosage should not exceed 250 μg / kg.

As a diagnostic agent, this drug is also administered intravenously at a dosage of 140 mcg / kg / min for six minutes, but for patients with an increased risk of side effects, infusion is started at low doses.

In ophthalmic practice, the dosage regimen of this active substance depends on the dosage form used. Due to its rapid metabolism, Adenosine does not have a negative effect on the fetus.

What are the side effects of Adenosine?

On the part of the cardiovascular system, when using Adenosine, the instructions for use indicate such effects: blood pressure may increase, facial flushing is possible, the patient will feel discomfort in the chest region, AV conduction is disturbed, there is a decrease in heart rate, that is, the so-called bradycardia occurs ...

From the respiratory system: bronchospasm may occur, and dyspnea is also noted.

From the side of the nervous system: the patient may feel a headache, nervousness and dizziness will join, in addition, paresthesias are noted, as well as double vision.

On the part of the digestive system: after using the drug, an unpleasant metallic taste may appear in the mouth, in addition, nausea occurs.

Other side effects will be excessive sweating, pain in the throat, as well as in the neck and lower jaw.

Local reactions can occur when using the drug in ophthalmic practice, they will be expressed in the form of a short-term sensation of an unpleasant burning sensation in the eye area, and you can also feel a tingling sensation. As for systemic reactions, they are very rare.

special instructions

With extreme caution, Adenosine should be used in patients with sinus bradycardia, in the presence of unstable angina pectoris, in addition, in patients with a history of heart defects diagnosed, there is pericarditis, as well as bronchial asthma.

When using Adenosine, it is necessary to monitor some parameters, in particular, it is necessary to measure pressure, heart rate, and also do an ECG.

Preparations containing adenosine

Oftan katakhrom and Vita-iodurol.

Conclusion

Any treatment of diseases should be carried out only after consultation with a doctor. Do not forget to attend preventive medical examinations in a timely manner in order to timely identify the existing pathological process in the body.

Adenocor (Adenocor).

Composition and form of release

Adenosine. Solution for intravenous administration (in 1 ml - 3 mg, in an ampoule - 6 mg).

pharmachologic effect

Adenosine affects metabolic processes in the myocardium. Gives an antiarrhythmic effect in supraventricular paroxysmal arrhythmias.

Rapid intravenous administration of the drug causes a short-term slowdown in AV conduction, which leads to the restoration of normal sinus rhythm in patients with paroxysmal supraventricular tachycardia.

Indications

Paroxysmal supraventricular tachyarrhythmia (including with Wolff-Parkinson-White syndrome), differential diagnosis of supraventricular tachyarrhythmias (tachycardia with dilation of ORS complexes), diagnostic electrophysiological studies (increased sensitivity, localization of the AV block).

Application

For relief of paroxysmal supraventricular tachyarrhythmia, adenosine is prescribed as a bolus intravenous injection (within 1-5 s) - the initial dose is 3 mg. If the tachyarrhythmia is not stopped within 1-2 minutes, an additional 6 mg of the drug is administered. If there is no effect, another 12 mg of adenosine is administered after 1-2 minutes. The use of large doses is not recommended.

During the execution of diagnostic studies, the drug is prescribed according to the above scheme until diagnostic information is obtained. The drug is intended for use only in a hospital setting where there is a possibility of monitoring the heart rate.

For patients in whom the administration of adenosine was complicated by AV blockade, if it is necessary to re-administer the dose, the dose of the drug should not exceed the initial one.

During pregnancy, the drug is prescribed only for health reasons. It is not recommended to prescribe adenosine to children, since there is insufficient data on the use of the drug in this category of patients.

Side effect

On the central nervous system: often - dizziness, a feeling of fear, blurred vision, headache are possible.
On CVS: pain in the region of the heart, tachycardia, bradycardia, AV block of various degrees.
On PS: nausea.
On DS: dyspnea, hyperventilation. In patients with, in some cases, the introduction of adenosine can provoke bronchospasm.
Others: hot flashes, increased sweating, pain in the arms, back and neck, metallic taste in the mouth.

Contraindications

AV block II and III degree (except for patients with an artificial pacemaker), SSSU (except for patients with an artificial pacemaker).

Overdose

Overdose cases are not described, since the drug is very quickly inactivated.

The mechanism of action of adenosine and its analogs on the heart is largely similar to the influence of the parasympathetic autonomic nervous system. Adenosine through purine receptors blocks adenylate cyclase, disrupts the synthesis of cAMP from ATP and all cAMP-mediated reactions.

Purine receptors are classified into P1 and P2 types according to modern classification.
P1 receptors are more sensitive to adenosine, blocked by methylxanthines (euphilin, caffeine).

P2 receptors are most sensitive to adenine nucleotides (ATP, ADP), are blocked by quinidine, imidazole derivatives (metronizadol, ketoconazole), but not methylxanthines (that is, methylxanthines will only neutralize the effects of adenosine formed after ATP hydrolysis).

Stimulation of purine receptors leads to an increase in the membrane permeability for potassium ions (KAdo), reduces the duration of the action potential, hyperpolarizes the membrane and reduces atrial contractility, similar changes occur in the SU and AV nodes. The amplitude of the action potential and overshoot are also reduced, slow spontaneous depolarization is inhibited, which leads to suppression of the cell's inherent automatism. Such potassium channels (KAdo) are absent in the His-Purkinje system and ventricular cardiomyocytes.

Trigger activity.

• Adenosine does not affect brady-dependent early post-depolarizations, but eliminates catecholamine-mediated early post-depolarization (associated with cAMP-dependent Ca2 + release from the sarcoplasmic reticulum and activation of the Na-Ca pump, as in late post-depolarization).

REMINDER.
The main condition for early post-depolarization is the lengthening of the action potential and the slowing down of the heart rate. Other reasons for the increased resting potential and early post-depolarization are hypokalemia, acidosis, hypocalcemia, ischemia, exposure to sotalol.

• Adenosine eliminates cAMP-dependent late post-depolarization caused by adenylate cyclase activators (catecholamines, beta-adrenomimetics, histamine).

REMINDER.
The main condition for late post-depolarization is an increase in Ca2 + ions in the cell. Catecholamines through adenylate cyclase increase Ca2 + entry into the cell.
An indirect increase in Ca2 + is observed with inhibition of Na-K-ATPase during hypoxia, under the influence of digitalis, as well as solutions that do not contain potassium and sodium. In the latter case, adenosine does not work.

Sinus rhythm response.

• In response to the introduction of adenosine in patients, there is a slowdown of the sinus rhythm with long periods of arrest of the sinus node, indicating the suppression of its automatism. Administration of atropine has no effect on these effects.

• Often, following the appointment of adenosine, reflex sinus tachycardia (dose-dependent effect without tachyphylaxis).

Unlike bradycardia, which is sensitive to methylxanthines, these compounds have no effect on the developed tachycardia. Cyclooxygenase inhibitors Aspirin and Indomethacin partially suppress tachycardia (which indicates a possible role of COX metabolites of arachidonic acid in the genesis of tachycardia).

ATP bolus injection is a simple, practical and effective method of controlling the cardiovascular response to laryngoscopy and tracheal intubation, which manifests itself in the form of excessive blood pressure and sinus tachycardia.

Stopping NZhT.

• The mechanism for stopping a typical AVNRT is to slow down predominantly anterograde conduction along the slow path... In the case of atypical (fast-slow) tachycardia, blockade of the slow pathway also occurs, which in this situation conducts excitation in a retrograde direction.

• With the introduction of adenosine, the development of ventriculoatrial blockade is possible, leading to the relief of pacemaker tachycardia.

Impact on DPP.

• Adenosine usually has no effect on the anterograde conduction along the DPP, however, it can be blocked in those of them that have a long holding time or decremental properties. There are reports of a slowdown in anterograde and retrograde conduction along the Kent's bundle, characterized by a long effective refractory period.

• A correlation was found between the ERP of the Kent beam and the action of ATP:
• in cases where the drug did not change the anterograde and retrograde conduction along the Kent's bundle, the anterograde ERP was always less than 230 ms.
• in cases where the drug only slowed down the conduction along the Kent's beam in the retrograde direction, the anterograde ERP of this pathway always exceeded 280 ms.

VT relief.

• Adenosine and ATP are capable of specifically arresting ventricular tachycardia, which is based on cAMP-mediated trigger activity (adrenergic).

• Adenosine-sensitive ventricular tachycardias, as a rule, occur in a structurally unchanged heart, the ECG has the configuration of a left bundle branch block with a deviation of the electrical axis of the heart to the right (VT from the right ventricular outlet), and they develop almost exclusively under stress or physical exertion ( along with adenosine, it can be stopped by vagal techniques and verapamil).

Myocardial ischemia

• A possible mechanism of the antiarrhythmic action of adenosine on the ventricular myocardium is an improvement in the blood supply to the myocardium in the ischemic zone. This is evidenced by the ability dipyridamole (inhibits the reuptake of adenosine by erythrocytes - increases the concentration of endogenous adenosine) stop, and aminophylline - resume stable non-reciprocal non-automatic catecholamine-dependent ventricular tachycardia.

• Myocardial ischemia is accompanied by the appearance of endogenous adenosine in the intercellular space. If the blood flow in the area of \u200b\u200bthe AV junction is disturbed, for example, due to RCA spasm, bradycardia that is not cleared by atropine but is treatable with adenosine receptor antagonists .

• Dipyridamole potentiates, and aminophylline eliminates conduction changes caused by hypoxia or myocardial ischemia. The negative dromotropic effect of myocardial ischemia is associated with the effect of endogenous adenosine released from cardiomyocytes.

• Endogenous adenosine, released from cardiomycytes during myocardial ischemia or hypoxia, has the same effect on the vascular system as exogenous adenosine.

• When performing a temporary pacemaker in patients with hypoxia or myocardial ischemia, when the content of endogenous adenosis is increased in the intercellular space, the development of severe bradycardia or asystole is possible. In such cases, purine receptor antagonists (aminophylline, caffeine) may be the only effective remedy.

Part of preparations

ATX:

C.01.E.B.10 Adenosine

Pharmacodynamics:

Endogenous biologically active substance that provides:

- antiarrhythmic action (slows down AV conduction, increases the refractoriness of the AV node and decreases the automatism of the sinus node);

- vasodilator - can provoke arterial hypotension, especially with slow intravenous infusion.

Adenosine is characterized by an immediate onset of action, probably as a result of activation of specific adenosine receptors.

Application in ophthalmology is also due to a number of functions:

- participation in reparative processes, which in turn slows down lens degeneration;

- has a vasodilating effect and improves blood supply to the tissues of the eye, which stimulates the synthesis of intraocular fluid and its purification from toxins;

- reduces inflammation in the conjunctiva, cornea and other tissues of the eye;

- has an indirect effect on the recovery of glutathione.

Pharmacokinetics

Adenosine has a fast metabolism, with the participation of circulating enzymes in erythrocytes and vascular endothelial cells, it turns into inactive and adenosine monophosphate, is excreted by the kidneys in the form of metabolites.

In ophthalmology, when applied topically, it easily penetrates the cornea and is distributed in all tissues.

The half-life of adenosine from blood plasma is no more than 1 minute.

Indications:

- relief of paroxysmal supraventricular tachycardia - for bolus IV administration;

- as an auxiliary diagnostic tool when performing two-dimensional echocardiography, scintigraphy - for intravenous infusion;

- cataract.

VII.H25-H28.H26 Other cataracts

VII.H25-H28.H25 Senile cataract

IX.I30-I52.I45.6 Premature arousal syndrome

IX.I30-I52.I47.1 Supraventricular tachycardia

Contraindications:

- AV block II and III degree (except for patients with an artificial pacemaker);

- sick sinus syndrome (except for patients with an artificial pacemaker);

- ventricular tachycardia;

- individual intolerance.

Carefully:

Adenosine is prescribed with caution in patients with unstable angina pectoris, conduction disorders, sinus bradycardia, as well as in patients with hypovolemia, pericarditis, heart defects, bronchial asthma.

Therapy requires regular monitoring of blood pressure, heart rate and ECG.

Method of administration and dosage:

As an antiarrhythmic agent, 6 mg of the drug is injected into / in bolus (within 1-2 seconds). In the absence of effect, 12 mg is administered intravenously in a bolus within 1-2 minutes, if necessary, the administration in the indicated dose is repeated.

For children, the drug is administered intravenously as a bolus at a dose of 50 μg / kg. The dose can be increased by 50 mcg / kg every 2 minutes up to a maximum dose of 250 mcg / kg.

When carrying out diagnostic studies, it is administered intravenously at a dose of 140 μg / kg / min for 6 minutes (the total dose is 840 μg / kg).

At a high risk of side effects, infusion is started at lower doses (from 50 μg / kg / min).

Maximum dose of the drugfor adults is 12 mg.

When using adenosine in ophthalmology, the dosage regimen depends on the dosage form used.

Side effects:

The cardiovascular system: chest discomfort, arterial hypotension, AV-conduction disturbances, facial redness, bradycardia.

Respiratory system: breathing disorder, bronchospasm.

Nervous system: nervousness, dizziness and headache, paresthesia, diplopia.

Digestive system: nausea, metal taste in the mouth.

Local reactions: a burning sensation and tingling of the eyes that occurs when applied topically in ophthalmology.

Others: increased sweating, sore throat, neck and lower jaw.

Interaction:

Concomitant use with dipyridamole can lead to an increase in the action of adenosine.

Concomitant use with caffeine and theophylline can lead to a decrease in the effect of adenosine, which is due to the antagonistic effect of caffeine and theophylline on adenosine receptors.

Special instructions:

It is necessary to strictly observe the dosage of the drug in accordance with the indications for use.

Instructions

Adenosine (Adenosinum) is an antiarrhythmic agent. A drug used for tachycardia.

Tradename

Adenosine.

International non-proprietary name

Adenosine (Adenosinum).

Dosage form and description

The starting material is a white crystalline powder. Let's dissolve in water and practically insoluble in ethanol. Solubility increases with heating and lowering the pH of the solution. Molecular weight 267.24.

Available as a clear aqueous solution for injection.

Composition and form of release

In solution for injection 1%:

• Active substances: adenazine, in 1 ml - 3.0 mg, in an ampoule - 6.0 mg.
• Excipients:water

Pharmacological group

Antiarrhythmic drugs.

Pharmacological properties

Adenosine is an endogenous purine nucleoside capable of simulating many physiological processes in the body.

Pharmacodynamics and pharmacinetics

The drug has a rapid metabolism. The process involves circulating enzymes of vascular endothelial cells and erythrocytes. Deamination is implemented. The active substance is transformed to inactive inosine and adenosine monophosphate.

The agent begins to act immediately after intravenous administration. T 1/2 lasts less than 10 seconds. The metabolites are excreted by the kidneys.

Indications for use

For bolus IV administration: paroxysmal supraventricular tachycardia (including with WPW syndrome).

For intravenous infusion: differential diagnosis of supraventricular tachyarrhythmias (tachycardia with widened QRS complexes), diagnostic electrophysiological studies (determination of the localization of the AV block).

Contraindications

• Hypersensitivity
• AV block II and III degree or sick sinus syndrome (except for patients with an artificial pacemaker)
• Bronchial asthma (risk of bronchospasm).

Application during pregnancy and lactation

During pregnancy, it is permissible in case of extreme necessity (adequate and strictly controlled studies in humans have not been conducted). Since adenosine is an endogenous intermediate in the body, complications are not expected and in the few reports on the use of adenosine in pregnant women, information about complications in the fetus or mother is absent.

It is believed that due to its rapid disappearance from the bloodstream, adenosine does not penetrate into breast milk.

Method of administration and dosage

As an antiarrhythmic agent: for adults - intravenous bolus (within 1-3 s) into the central or large peripheral vein, 6 mg is injected under the control of ECG and blood pressure, if necessary after 1-2 minutes - 12 mg, if there is no effect - through 1-2 minutes repeatedly 12 mg. At any of the stages, the administration is stopped after the arrhythmia is eliminated or the development of high-grade AV block. The maximum single dose for adults is 12 mg.

For those receiving dipyridamole, the initial dose is 0.5-1 mg. Children - 50 mcg / kg. The dose can be increased by 50 mcg / kg every 2 minutes up to a maximum dose of 250 mcg / kg.

As an auxiliary diagnostic agent: IV (infusion) at a dose of 140 mcg / kg / min for 6 minutes (total dose - 840 mcg / kg).

In patients at high risk of side effects, infusion is started at lower doses (from 50 μg / kg / min).

Side effect

With a rapid intravenous bolus

In controlled clinical trials in the United States, the following adverse effects were observed after intravenous administration of adenosine (in the placebo group, all these reactions were noted in less than 1% of cases):

slight dizziness (2%), headache (2%), tingling in the hands, feeling of numbness (1%), nervousness, blurred vision, neck and back pain (less than 1%).

From the side cardiovascular flushed face (18%), palpitations, chest pain, lowering blood pressure (less than 1%).

Shortness of breath (12%), chest pressure (7%), hyperventilation.

From the digestive tract:nausea (3%), metallic taste in the mouth, feeling of constriction in the throat.

Others:increased sweating (less than 1%).

In post-marketing observations, there were cases of new arrhythmias - ventricular and atrial extrasystole, sinus bradycardia, sinus tachycardia, pulse loss (newly arising arrhythmias usually last for several seconds), transient increase in pressure, bronchospasm.

With intravenous infusion

When conducting controlled and uncontrolled clinical trials in the United States after intravenous administration of adenosine (n \u003d 1421), the following adverse effects were observed, which were noted in at least 1% of cases.

Despite the short T1 / 2 of adenosine, in 10.6% of cases, side effects were recorded not at the time of infusion, but several hours after its completion. In 8.4% of cases, the manifestation of side effects coincided with the beginning of the infusion and ended 24 hours after its completion. In many cases, it is not possible to determine if the later side effects are the result of adenosine infusion.

Flushing (44%), chest discomfort (40%), dyspnea (28%), headache (18%), discomfort in the throat, jaw, or neck (15%), gastrointestinal upset (13%) ), dizziness (12%), a feeling of discomfort in the hands (4%), a decrease in the ST segment (3%), AV block I degree (3%), AV block II degree (3%), paresthesia (2%), arterial hypotension (2%), nervousness (2%), arrhythmia (1%).

Side effects of varying severity, noted in less than 1% of patients, included:

• The organism as a whole:a feeling of discomfort in the back and / or in the lower extremities, weakness.
• From the side cardiovascular system and blood (hematopoiesis, hemostasis): non-fatal myocardial infarction, life-threatening ventricular arrhythmia, grade III AV block, bradycardia, palpitations, sweating, T wave changes, arterial hypertension (SBP\u003e 200 mm Hg).
• From the nervous system and sensory organs:drowsiness, emotional lability, tremors, visual impairment.
• From the respiratory system: cough.
• Others: dry mouth, ear discomfort, metallic taste in the mouth, nasal congestion, scotoma, tongue discomfort.

Overdose

Due to the short T1 / 2, adverse events (if they occur) quickly disappear. Competitive adenosine antagonists are caffeine, theophylline, and other methylxanthines.

Interaction with other medicinal products

Dipyridamole enhances the action of adenosine by inhibiting its uptake by cells (dose reduction is recommended). The vasoactive effects of adenosine are attenuated by adenosine receptor antagonists such as methylxanthines, including caffeine and theophylline (higher doses of adenosine or a change in treatment may be necessary). Carbamazepine may worsen adenosine-induced heart block. Caution should be exercised when in / in the introduction of adenosine with other cardiotropic drugs (such as beta-blockers, cardiac glycosides, CCBs), since their effectiveness in such cases has not been systematically evaluated; although no adverse interactions have been noted, an additive or synergistic inhibitory effect on sinoatrial and AV conduction is potentially possible.

special instructions

Administration through central veins reduces the risk of side effects.

Intravenous administration is permissible only in a hospital setting where it is possible to monitor the activity of the heart. For patients in whom the use of a single dose of adenosine is complicated by AV block, additional doses should not be administered.

Storage conditions and shelf life

1 year. Store in a dark place at a temperature of 3-7 ° C.

Conditions of dispensing from pharmacies

Dispensed by prescription

Analogs

Medicines similar in their pharmacotherapeutic properties:

1. Adenocor;
2. Vitakik;
3. Rimecor.

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The patient's condition at the time of taking the drug

How would you assess the condition of the patient who took the drug?

There are only three such states:

1. In a satisfactory condition a person is able to serve himself and take an active part in the conversation. Consciousness is clear. Symptoms of the disease may appear, but this does not interfere with the patient's normal activities.
2. In a state of moderate severity the patient's consciousness is usually clear. But he prefers to be in bed most of the time, most often in a forced position. Vigorous activity increases general weakness and symptoms of the disease. With direct examination, the severity of pathological changes on the part of internal organs and systems is observed.
3. In severe condition consciousness may be absent, confused, or remain clear. The symptoms of the disease are significantly pronounced. The patient is almost constantly in bed, takes active actions with difficulty or with outside help.