Atracurium Besylate is a nondepolarizing skeletal muscle relaxant. Nondepolarizing agents antagonize the neurotransmitter action of acetylcholine by binding competitively with cholinergic receptor sites on the motor end-plate. This antagonism is inhibited, and neuromuscular block reversed, by acetylcholinesterase inhibitors such as neostigmine, edrophonium, and pyridostigmine.

The dose required to produce 95% suppression of the muscle twitch response in balanced anesthesia is 0.11 to 0.26 mg/kg. An initial dose of Atracurium Besylate of 0.4 to 0.5 mg/kg generally produces maximum neuromuscular block within 3 to 5 minutes of injection, with excellent intubation conditions within 2 to 2.5 minutes in most patients. Recovery from neuromuscular block can be expected to begin approximately 20 to 35 minutes after injection, and recovery is usually 95% complete approximately 60 to 70 minutes after injection.

Repeated administration of maintenance doses of Atracurium Besylate has no cumulative effect on the duration of neuromuscular block if recovery is allowed to begin prior to repeat dosing.

The pharmacokinetics of Atracurium Besylate in man are essentially linear within the 0.3 to 0.6 mg/kg dose range.

The elimination half-life Is approximately 20 minutes.

Atracurium Besylate undergoes extensive degradation, and neither kidney nor liver plays a major role in its elimination.

There has been no significant difference in clinical duration and recovery from neuromuscular block observed between elderly and younger patients receiving Atracurium Besylate.

Atracurium Besylate is a less potent histamine releaser than d-tubocurarine or metocurine. Histamine release is minimal with initial Atracurium Besylate doses up to 0.5 mg/kg.

 

ATRACURIUM ELSaad is indicated, as an adjunct to general anesthesia, to facilitate tracheal intubation and to provide skeletal muscle relaxation during surgery or controlled ventilation.

 

Atracurium Besylate is contraindicated in patients known to have a hypersensitivity to it.

 

-ATRACURIUM BESYLATE SHOULD BE USED ONLY BY THOSE SKILLED IN AIRWAY MANAGEMENT AND RESPIRATORY SUPPORT. EQUIPMENT AND PERSONNEL MUST BE IMMEDIATELY AVAILABLE FOR ENDOTRACHEAL INTUBATION AND SUPPORT OF VENTILATION, INCLUDING ADMINISTRATION OF POSITIVE PRESSURE OXYGEN.    

-ANTICHOLINESTERASE REVERSAL AGENTS SHOULD BE IMMEDIATELY  AVAILABLE.                                                            

-DO NOT GIVE ATRACURIUM BESYLATE BY INTRAMUSCULAR ADMINISTRATION

-Atracurium Besylate, should not be mixed with alkaline solutions  in the same syringe or administered simultaneously during intravenous infusion through the same needle.

-Special caution should be exercised in administering Atracurium Besylate to patients in whom substantial histamine release would be especially hazardous (e.g., patients with clinically significant cardiovascular disease) and in patients with any history (e.g., severe anaphylactoid reactions or asthma). In these patients, the recommended initial Atracurium Besylate dose is lower (0.3 to 0.4 mg/kg) than for other patients and should be administered slowly or in divided doses over one minute.

-Since Atracurium Besylate has no clinically significant effects on heart rate in the recommended dosage range. As a result, bradycardia during anesthesia may be more common with Atracurium Besylate than with other muscle relaxants.

-Atracurium Besylate may have profound effects in patients with myasthenia gravis, Eaton-Lambert syndrome, or other neuromuscular diseases in which potentiation of nondepolarizing agents has been noted.

-Precautions should be taken in patients with severe electrolyte disorders or carcinomatosis.

-Reports of malignant hyperthermia have been rare in cases in which Atracurium Besylate has been used. (Atracurium Besylate did not trigger this syndrome).

-Increased doses of nondepolarizing muscle relaxants may be required in burn patients and are dependent on the time elapsed since the burn injury and the size of the burn.

-The safety of Atracurium Besylate has not been established in patients with bronchial asthma.

-Long-Term Use in Intensive Care Unit: There is wide interpatient variability in dosage requirements and dosage requirements may decrease or increase with time.

-Laudanosine, metabolite of Atracurium Besylate produces transient hypotension and, in higher doses, cerebral excitatory effects (generalized muscle twitching and seizures).

-The use of a peripheral nerve stimulator to monitor neuromuscular function is suggested in pediatric patients.

 

Pregnancy: Category C. Atracurium Besylate should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

The possibility of respiratory depression in the newborn infant should always be considered following cesarean section during which a neuromuscular blocking agent has been administered. In patients receiving magnesium sulfate, The dose of Atracurium Besylate should be lowered as indicated.

It is not known whether Atracurium Besylate is excreted in human milk.  

 

Atracurium Besylate was well tolerated and most adverse reactions were suggestive of histamine release: skin flush, erythema, itching, bronchospasm and mild transient hypotension.

Anaphylactic or anaphylactoid responses which, in rare instances, were severe in conjunction with one or more of anesthetic agents.

 

Drugs which may enhance the neuromuscular blocking action of Atracurium Besylate include: enflurane; isoflurane; halothane; aminoglycosides, polymyxins; lithium; magnesium salts; procainamide; and quinidine.

If other muscle relaxants are used during the same procedure, the possibility of a synergistic or antagonist effect should be considered.

The prior administration of succinylcholine does not enhance the duration, but quickens the onset and may increase the depth, of neuromuscular block induced by Atracurium Besylate. Atracurium Besylate should not be administered until a patient has recovered from succinylcholine-induced neuromuscular block.

 

Intravenous injection:

A dose of Atracurium Besylate of 0.3 to 0.6mg/kg  by intravenous injection, provide adequate relaxation for about 15 to 35 minutes.

Endotracheal intubation can usually be accomplished within 90 seconds from the intravenous injection of 0.5 to 0.6 mg/kg.

Full block can be prolonged with supplementary doses of 0.1 to 0.2 mg/kg as required.

Spontaneous recovery from the end of full block occurs in about 35 minutes as measured by the restoration of the tetanic response to 95% of normal neuromuscular function.

The neuromuscular block produced by Atracurium Besylate can be rapidly reversed by standard doses of anticholinesterase agents, such as neostigmine and edrophonium, accompanied by atropine.

Intravenous infusion:

After an initial bolus dose of 0.3 to 0.6 mg/kg, Atracurium Besylate can be used to maintain neuromuscular block during long surgical procedures by administration as continuous infusion at rates of 0.3 to 0.6 mg/kg/hour.

Induced hypothermia to a body temperature of 25˚ to 26˚C reduced the rate of inactivation of Atracurium Besylate, therefore full neuromuscular block may be maintained by approximately half the original infusion rate at these low temperatures.

Atracurium Besylate is compatible with the following infusion solution for the times stated below:

When diluted in these solutions to give Atracurium Besylate concentrations of 0.5 mg/ml and above, the resultant solutions will be stable in daylight for the stated periods at temperatures of up to 30˚C.

The dosage in children over the age of one month is the same as that in adults on a bodyweight basis.

Atracurium Besylate may be used at standard dosage in elderly patients. It is recommended, however, that the initial dose be at the lower end of the range and that it be administered slowly.

Atracurium Besylate may be used at standard dosage at all levels of renal or hepatic function, including endstage failure.

In patients with clinically significant cardiovascular disease, the initial dose of Atracurium Besylate should be administered over a period of 60 seconds.

After an optional initial bolus dose of Atracurium Besylate of 0.3 to 0.6 mg/kg, Atracurium Besylate can be used to maintain neuromuscular block by administration a continuous infusion at rates: 11 and 13 µg/kg/min (0.65-0.78mg/kg/hr). However, there is wide inter-patient variability in dosage requirements. Dosage requirements may change with time. Infusion rates as low as 4.5µg/kg/min (0.27 mg/kg/hr) or as high as 29.5µg/kg/min (1.77 mg/kg/hr) are required some patients.

The rate of spontaneous recovery from neuromuscular block after infusion of Atracurium Besylate is independent of the duration of administration.

In common with all neuromuscular blocking agents, monitoring of neuromuscular function is recommended during the use of Atracurium Besylate in order to individualize dosage requirements.

 

The possibility of overdosage can be minimized by carefully monitoring muscle twitch response to peripheral nerve stimulation. Excessive doses of Atracurium Besylate can be expected to produce enhanced pharmacological effects. Overdosage may increase the risk of histamine release and cardiovascular effects, especially hypotension. If cardiovascular support is necessary, this should include proper positioning, fluid administration, and the use of vasopressor agents if necessary. The patient's airway should be assured, with manual or mechanical ventilation maintained as necessary. Recovery may be facilitated by administration of an anticholinesterase reversing agent such as neostigmine, or pyridostigmine, in conjunction with an anticholinergic agent such as atropine or glycopyrrolate.

 

-ATRACURIUM ELSaad 25 - Injection: A Pack of 1 or 5 or 25 ampoule of 2.5ml.  Each ampoule (2.5 ml) contains Atracurium Besylate 25mg.

-ATRACURIUM ELSaad 50 - Injection: A Pack of 1 or 5 or 25 ampoule of  5ml.  Each ampoule (5 ml) contains Atracurium Besylate 50mg.

 

Store ATRACURIUM ELSaad - Injection at temperature between 2-8°C. Do not freeze. It is estimated that an 8% loss of potency when stored at 30°C for one month.