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Quelicin (Succinylcholine Chloride) - Description and Clinical Pharmacology

 
 



This drug should be used only by individuals familiar with its actions, characteristics and hazards.

DESCRIPTION

Quelicin (Succinylcholine Chloride Injection, USP) is a sterile, nonpyrogenic solution to be used as a short-acting, depolarizing, skeletal muscle relaxant. See HOW SUPPLIED for summary of content and characteristics of the solutions. The solutions are for I.M. or I.V. use.

Succinylcholine Chloride, USP is chemically designated C14H30Cl2N2O4 and its molecular weight is 361.31.

It has the following structural formula:

 

Succinylcholine is a diquaternary base consisting of the dichloride salt of the dicholine ester of succinic acid. It is a white, odorless, slightly bitter powder, very soluble in water. The drug is incompatible with alkaline solutions but relatively stable in acid solutions. Solutions of the drug lose potency unless refrigerated.

Solution intended for multiple-dose administration contains 0.18% methylparaben and 0.02% propylparaben as preservatives (List No. 6629). Product not requiring dilution (multiple-dose fliptop vial) contains sodium chloride to render isotonic. May contain sodium hydroxide and/or hydrochloric acid for pH adjustment. pH is 3.6 (3.0 to 4.5). See table in HOW SUPPLIED for characteristics.

Sodium Chloride, USP, chemically designated NaCl, is a white crystalline compound freely soluble in water.

CLINICAL PHARMACOLOGY

Succinylcholine is a depolarizing skeletal muscle relaxant. As does acetylcholine, it combines with the cholinergic receptors of the motor end plate to produce depolarization. This depolarization may be observed as fasciculations. Subsequent neuromuscular transmission is inhibited so long as adequate concentration of succinylcholine remains at the receptor site. Onset of flaccid paralysis is rapid (less than one minute after intravenous administration), and with single administration lasts approximately 4 to 6 minutes.

Succinylcholine is rapidly hydrolyzed by plasma cholinesterase to succinylmonocholine (which possesses clinically insignificant depolarizing muscle relaxant properties) and then more slowly to succinic acid and choline (see PRECAUTIONS ). About 10% of the drug is excreted unchanged in the urine. Succinylcholine levels were reported to be below the detection limit of 2 µg/mL after 2.5 minutes of an IV bolus dose of 1 or 2 mg/kg in fourteen (14) anesthetized patients.

The paralysis following administration of succinylcholine is progressive, with differing sensitivities of different muscles. This initially involves consecutively the levator muscles of the face, muscles of the glottis and finally the intercostals and the diaphragm and all other skeletal muscles.

Succinylcholine has no direct action on the uterus or other smooth muscle structures. Because it is highly ionized and has low fat solubility, it does not readily cross the placenta.

Tachyphylaxis occurs with repeated administration (see PRECAUTIONS ).

Depending on the dose and duration of succinylcholine administration, the characteristic depolarizing neuromuscular block (Phase I block) may change to a block with characteristics superficially resembling a non-depolarizing block (Phase II block). This may be associated with prolonged respiratory muscle paralysis or weakness in patients who manifest the transition to Phase II block. When this diagnosis is confirmed by peripheral nerve stimulation, it may sometimes be reversed with anticholinesterase drugs such as neostigmine (see PRECAUTIONS ). Anticholinesterase drugs may not always be effective. If given before succinylcholine is metabolized by cholinesterase, anticholinesterase drugs may prolong rather than shorten paralysis.

Succinylcholine has no direct effect on the myocardium. Succinylcholine stimulates both autonomic ganglia and muscarinic receptors which may cause changes in cardiac rhythm, including cardiac arrest. Changes in rhythm, including cardiac arrest, may also result from vagal stimulation, which may occur during surgical procedures, or from hyperkalemia, particularly in pediatric patients (see PRECAUTIONS:   Pediatric Use ). These effects are enhanced by halogenated anesthetics.

Succinylcholine causes an increase in intraocular pressure immediately after its injection and during the fasciculation phase, and slight increases which may persist after onset of complete paralysis (see WARNINGS ).

Succinylcholine may cause slight increases in intracranial pressure immediately after its injection and during the fasciculation phase (see PRECAUTIONS ).

As with other neuromuscular blocking agents, the potential for releasing histamine is present following succinylcholine administration. Signs and symptoms of histamine mediated release such as flushing, hypotension and bronchoconstriction are, however, uncommon in normal clinical usage.

Succinylcholine has no effect on consciousness, pain threshold or cerebration. It should be used only with adequate anesthesia (see WARNINGS ).

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