Adenozin

Each ml contains Adenosine 3 mg/ml, 2 ml.
Chemical Name: 6-Amino-9-β-D-ribofuranosyl-9H-purine; 9-β-D-Ribofuranosyladenine.
Adenosine is Endogenous nucleoside.

Other Cardiac Preparations. ATC Code: C01EB10.
Pharmacology: Pharmacodynamics: Endogenous nucleoside with peripheral vasodilator/antiarrhythmic effect.
Antiarrhythmic Drug: Adenosine is a purine nucleoside which is present in all cells of the body.
Adenosine administered by intravenous injection slows conduction through the AV node. This action can interrupt re-entry circuits involving the AV node and restore normal sinus rhythm in patients with paroxysmal supraventricular tachycardia. Once the circuit has been interrupted, the tachycardia stops and normal sinus rhythm is re-established. One acute interruption of the circuit is usually sufficient to arrest the tachycardia.
Pharmacokinetics: It is impossible to study adenosine in classical pharmacokinetic studies. It is present in various forms in all cells of the body where it plays an important role in energy production and utilization systems. An efficient salvage and recycling system exists in the body, primarily in the erythrocytes and blood vessel endothelial cells. The half-life in vitro is estimated to be less than 10 seconds.
Onset of action: rapid. Duration: very brief.

Treatment Indications: Conversion to a normal sinus rhythm of paroxysmal supraventricular tachycardias, including those associated with accessory by-pass tracts (Wolff-Parkinson-White Syndrome).
Diagnostic Indications: Aid to diagnosis of broad or narrow complex supraventricular tachycardias. Although adenosine injection will not convert atrial flutter, atrial fibrillation or ventricular tachycardia to sinus rhythm, the slowing of AV conduction helps diagnosis of atrial activity.
Sensitisation of intra-cavitary electrophysiological investigations.

Recommended Dose: Dosage and Method of Administration: Adenosine injection is intended for hospital use only with monitoring and cardio respiratory resuscitation equipment available for immediate use.
Method of Administration: It should be administered by intravenous (IV) bolus injection according to the ascending dosage schedule as follows. To be certain the solution reaches the systemic circulation administer either directly into a vein or into an IV line. If given into an IV line it should be injected as proximally as possible, and followed by a rapid saline flush.
Adenosine Injection should only be used when facilities exist for cardiac monitoring. Patients who develop high-level AV block at a particular dose should not be given further dosage increments.
Posology: Adults: Initial Dose: 3 mg given as a rapid intravenous bolus (over 2 seconds).
Second Dose: If the first dose does not result in elimination of the supraventricular tachycardia within 1 to 2 minutes, 6 mg should be given also as an intravenous bolus.
Third Dose: If the second dose does not result in elimination of the supraventricular tachycardia within 1 to 2 minutes 12mg should be given also as an intravenous bolus. Additional or higher doses are not recommended.
Pediatric Population: Less than 50 kg: Initial dosage: 0.05 - 0.1mg/kg as an intravenous bolus given centrally or peripherally.
Second Dose: If conversion of PSVT does not occur within 1 - 2 minutes, additional bolus injections can be administered at incrementally higher doses, increasing the amount given by 0.05 - 0.1 mg/kg. Continue this process until sinus rhythm is established or a maximum single dose of 0.3 mg/kg (up to 12 mg) is used.
Maximum dose: 0.3mg/kg single dose (up to 12mg).
Diagnostic Dose: The previously mentioned ascending dosage schedule should be employed until sufficient diagnostic information has been obtained.
Method of Administration: Intravenous injection only.

Overdose and treatment: Over dosage would cause severe hypotension, bradycardia or asystole. The half-life of adenosine in blood is very short (< 10 seconds), and side effects (when they occur) would quickly resolve. Administration of IV aminophylline or theophylline may be needed. Pharmacokinetic evaluation indicates that methyl xanthines are competitive antagonists to adenosine and that therapeutic concentrations of theophylline block its exogenous effects.

Adenosine injection is contraindicated for patients presenting: Known hypersensitivity to adenosine or to any of the excipients; Sick sinus syndrome, second or third degree Atrio-Ventricular (AV) block (except in patients with a functioning artificial pacemaker); Severe hypotension.

Due to the possibility of transient cardiac arrhythmias arising during conversion of the supra ventricular tachycardia to normal sinus rhythm, administration should be carried out in a hospital setting with monitoring and cardio-respiratory resuscitation equipment available for immediate use if necessary. During administration, continuous ECG monitoring is necessary as life-threatening arrhythmia might occur. Hypotension is possible when large doses of adenosine are administered by continuous IV infusion. Discontinue infusion in patients who develop persistent or symptomatic hypotension.
Adenosine should be used with caution in patients with recent myocardial infarction, severe heart failure, or in patients with minor conduction defects (first degree A-V block, bundle branch block) that could be transiently aggravated during infusion. Adenosine should be used with caution in patients with atrial fibrillation or flutter and especially in those with an accessory by-pass tract since particularly the latter may develop increased conduction down the anomalous pathway.
Cardiac denervation in patients who have undergone cardiac transplantation reportedly may enhance sensitivity to the bradycardic effects of adenosine.
Adenosine does not require renal or hepatic function for therapeutic effect or inactivation, so renal or hepatic dysfunction would not be expected to alter its effectiveness or tolerability.
Use adenosine with caution in patients with obstructive lung disease not associated with bronchoconstriction (eg. bronchitis, emphysema), and avoid use in patients with bronchoconstriction or bronchospasm (eg. asthma). Discontinue adenosine in any patient who develops severe respiratory difficulties.
Use in Children: The safety and efficacy of adenosine in children aged 0-18 years old have not been established.

Pregnancy: Category C.
There are no or limited amount of data from the use of adenosine in pregnant women. Animal studies are insufficient with respect to reproductive toxicity. Adenosine is not recommended during pregnancy unless the physician considers the benefits to outweigh the potential risks.
Lactation: It is unknown whether adenosine metabolites are excreted in human milk. In addition, the serum half-life is so short that it is unlikely that any of the drug will pass into human milk. Adenosine Injection should not be used during breast-feeding.

Cardiovascular: Facial flushing (18%), chest pain, hypotension, palpitations (less than 1%).
CNS: Headache, light-headedness (2%), dizziness, numbness, tingling in arms (1%), apprehension (less than 1%).
GI: Nausea (3%), metallic taste, pressure in groin, tightness in throat (less than 1%).
Musculoskeletal: Heaviness in arms, neck/back pain (less than 1%).
Respiratory: Dyspnea (12%), hyperventilation (less than 1%).
Miscellaneous: Chest pressure (7%), blurred vision, burning sensation, head pressure, sweating (less than 1%).

Dipyridamole inhibits adenosine cellular uptake and metabolism, and potentiates the action of adenosine. Asystole has been reported following concomitant administration. It is therefore suggested that adenosine injection should not be administered to patients receiving dipyridamole; if use of adenosine injection is essential, dipyridamole should be stopped 24 hours before hand, or the dose of adenosine should be greatly reduced.
Theophylline and other xanthenes (methylxanthines) are competitive adenosine antagonists and should be avoided for 24 hours prior to use of adenosine. Food and drinks containing xanthines (tea, coffee, chocolate and cola) should be avoided for at least 12 hours prior to use of adenosine injection or larger doses of adenosine may be required. Adenosine may interact with drugs tending to impair cardiac conduction.

Store below 30°C. Do not refrigerate.

Cardiac Drugs

C01EB10 - adenosine ; Belongs to the class of other cardiac preparations.

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