Quelicin

Quelicin

suxamethonium

Manufacturer:

Hospira

Distributor:

Hospira
Full Prescribing Info
Contents
Succinylcholine chloride.
Description
Succinylcholine chloride is a sterile, nonpyrogenic solution to be used as a short-acting, depolarizing, skeletal muscle relaxant. The solutions are intended for IM or IV use.
Succinylcholine chloride USP is C14H30CI2N2O4 and has a molecular weight of 361.31.
Succinylcholine chloride is a diquaternary base consisting of the dichloride salt of the dichloride ester of succinic acid. It is a white, odorless, slightly bitter powder and very soluble in water. It is incompatible with alkaline solutions but relatively stable in acid solutions. Solutions of succinylcholine lose potency unless refrigerated.
Solutions intended for multiple-dose administration contain methylparaben 0.18% and propylparaben 0.02% as preservatives.
Solutions intended for single-dose administration contain no preservatives. Products not requiring dilution (muitiple-dose fliptop vial and Abboject syringe) contain sodium chloride to render isotonic. It may contain sodium hydroxide and/or hydrochloric acid for pH adjustment. The pH is 3.6 (3-4.5).
Sodium chloride (NaCl) is a white crystalline compound freely soluble in water.
Action
Pharmacology: Succinylcholine is a depolarizing skeletal muscle relaxant. Like 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 (<1 min after IV administration) and with single administration lasts approximately 4-6 min.
Succinylcholine is rapidly hydrolyzed by plasma pseudocholinesterase to succinyl monocline (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. The paralysis following administration of succinylcholine is selective, initially involving the levator muscles of the eyelids and in sequence the muscles of mastication, limb muscles, abdominal muscles, muscles of the glottis and finally the intercostals and diaphragm.
Onset and duration of action may be altered by use of other medications eg, anticholinesterases, depolarizing or nondepolarizing muscle relaxants, dehydration, electrolyte imbalance, certain nonpenicillin antibiotics, procaine-type local anesthetics. Neuromuscular blockade with succinylcholine is potentiated by quinine, magnesium salts and prolonged by hypokalemia or hypocalcemia.
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).
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 children (see Use in children under Precautions). These effects are enhanced by cyclopropane and 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).
As with other neuromuscular blocking agents, the potential for releasing histamine is present following succinylcholine administration. Signs and symptoms of histamine mediated release eg, 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.
Indications/Uses
Adjunct to general anesthesia and to facilitate tracheal intubation to provide skeletal muscle relaxation during surgery or mechanical ventilation.
It may be employed to reduce the intensity of muscle contractions of pharmacologically- or electrically-induced convulsions.
Dosage/Direction for Use
The dosage of succinylcholine should be individualized and should always be determined by the clinician after careful assessment of the patient (see Warnings).
Adults: Short Surgical Procedures: The average dose required to produce neuromuscular blockade and to facilitate tracheal intubation is succinylcholine chloride injection 0.6 mg/kg given IV. The optimum dose will vary among individuals and may be from 0.3-1.1 mg/kg for adults.
Following administration of doses in this range, neuromuscular blockade develops in about 1 min; maximum blockade may persist for about 2 min, after which recovery takes place within 4-6 min. However, very large doses may result in more prolonged blockade. A test dose of 5-10 mg may be used to determine the sensitivity of the patient and the individual recovery time (see Precautions).
Long Surgical Procedures: The dose of succinylcholine administered by infusion depends upon the duration of the surgical procedure and the need for muscle relaxation. The average rate for an adult ranges between 2.5 and 4.3 mg/min.
Solutions containing from succinylcholine 1-2 mg/mL have commonly been used for continuous infusion. The more dilute solution (1 mg/mL) is probably preferable from the standpoint of ease of control of the rate of administration of the drug and, hence, of relaxation. This IV solution containing 1 mg/mL may be administered at a rate of 0.5-10 mg/min (0.5-10 mL/min) to obtain the required amount of relaxation. The amount required per minute will depend upon the individual response as well as the degree of relaxation required. Avoid overburdening the circulation with a large volume of fluid. It is recommended that neuromuscular function be carefully monitored with a peripheral nerve stimulator when using succinylcholine by infusion in order to avoid overdose, detect development of phase II block, follow its rate of recovery, and assess the effects of reversing agents (see Precautions).
Intermittent IV injections of succinylcholine may also be used to provide muscle relaxation for long procedures. An IV injection of 0.3-1.1 mg/kg may be given initially, followed, at appropriate intervals, by further injections of 0.04-0.07 mg/kg to maintain the degree of relaxation required.
Children: The dose for infants and children ranges from 1-2 mg/kg of body weight.
Intramuscular Use: If necessary, succinylcholine may be given IM to infants, older children or adults when a suitable vein is inaccessible. A dose of up to 3-4 mg/kg may be given, but not more than 150 mg total dose should be administered by this route. The onset of effect of succinylcholine given IM is usually observed in about 2-3 min.
Overdosage
Overdosage with succinylcholine may result in prolonged respiratory depression or apnea. Treatment is primarily supportive through maintenance of ventilation and oxygenation until return of adequate spontaneous ventilation.
In those instances where phase II block can be demonstrated by post-tetanic facilitation and fade of successive stimuli, small repeated doses of neostigmine or edrophonium preceded by atropine may be used to antagonize the block.
It should be kept in mind that the block may outlast the antagonist and careful observation for recurrence of neuromuscular blockade should be maintained in an environment and by persons capable of providing intubation and artificial ventilation.
Contraindications
Known hypersensitivity to succinylcholine chloride, genetically determined disorders of plasma pseudocholinesterase and myopathies associated with elevated creatinine phosphokinase values.
Patients after the acute phase of injury following major burns, multiple trauma, extensive denervation of skeletal muscle, or upper motor neuron injury unless clinical circumstances require immediate securing of the airway (see Warnings).
Warnings
Succinylcholine should only be used by adequately trained individuals familiar with its actions, characteristics and hazards.
Succinylcholine should not be administered unless facilities for intubation, artificial respiration and administration of oxygen therapy are instantaneously available.
There have been rare reports of acute rhabdomyolysis with hyperkalemia followed by ventricular dysrhythmias, cardiac arrest and death after the administration of succinylcholine to apparently healthy children who were subsequently found to have undiagnosed skeletal muscle myopathy, most frequently Duchenne's muscular dystrophy.
Great caution should be observed if succinylcholine is administered to patients during the acute phase of injury following major burns, multiple trauma, extensive denervation of skeletal muscle or upper motor neuron injury (see Contraindications). The risk of hyperkalemia in these patients increases over time and usually peaks at 7-10 days after the injury. The risk is dependent on the extent and location of the injury.
Caution should also be observed in patients with preexisting hyperkalemia and those who are paraplegic, who have suffered spinal cord injury or have degenerative or dystrophic neuromuscular disease, as such patients tend to become severely hyperkalemic when succinylcholine is given.
Succinylcholine administration has been associated with acute onset of fulminant hypermetabolism of skeletal muscle known as malignant hyperthermic crisis. This frequently presents as intractable spasm of the jaw muscles which may progress to generalized rigidity, increased oxygen demand, tachycardia, tachypnea and profound hyperpyrexia. Successful outcome depends on recognition of early signs eg, inappropriate response to initial administration of succinylcholine for endotracheal intubation or failure of tachycardia to respond to deepening anesthesia. Skin mottling, rising temperature and coagulopathies occur late in the course of the hypermetabolic process. Confirmation of the diagnosis requires discontinuance of anesthesia, attention to increased oxygen consumption, correction of metabolic acidosis, support of circulation, assurance of adequate urinary output and institution of measures to control rising temperature. Dantrolene sodium IV is recommended as an adjunct to supportive measures in the management of this problem. Consult literature references or the dantrolene prescribing information for additional information about the management of malignant hyperthermic crisis.
Special Precautions
General: When succinylcholine is given over a prolonged period, the characteristic depolarization block of the myoneural junction may change to a nondepolarizing block which results in prolonged respiratory depression or apnea. Under such circumstances, small repeated doses of neostigmine or edrophonium preceded by atropine may act as antagonists. A nerve stimulator may be used to ascertain the type of neuromuscular blockage. If a depolarization block is present, both fast (tetanic) and slow (twitch) rates of nerve stimulation are well sustained and post-tetanic facilitation is absent. If a nondepolarizing block is present, there is post-tetanic facilitation and "fade" of successive stimuli on both fast (tetanic) and slow (twitch) rates of nerve stimulation.
Succinylcholine should be employed with caution in patients with fractures as the muscle fasciculations may cause additional trauma.
Muscle fasciculations and hyperkalemia can be reduced by administering a small dose of a nondepolarizing relaxant prior to succinylcholine, but if other relaxants are to be used during the same procedure, the possibility of a synergistic or antagonistic effect should be considered.
The administration of succinylcholine may cause a rise in intraocular tension. Succinylcholine should be used with caution during intraocular operations and in patients with glaucoma.
Succinylcholine should be used with caution in patients with cardiovascular, hepatic, pulmonary, metabolic or renal disorders.
Intravenous as well as IM injections (single or repeated) of succinylcholine have been associated with myoglobinemia and myoglobinuria, especially in children. Injection of small doses of nondepolarizing agents eg, tubocurarine, before injecting succinylcholine has been used to reduce severity of muscle fasciculations, and also has been noted to decrease the incidence of myoglobinuria.
The action of succinylcholine may be altered by electrolyte imbalance, body temperature, the use of antibiotics other than the penicillin group, some carcinomas or renal disease.
Reduced Plasma Cholinesterase Activity: A low level of plasma pseudocholinesterase may be associated with a prolonged paralysis of respiration following the use of succinylcholine. Low levels of this enzyme are often found in patients with severe liver disease or cirrhosis, severe anemia, severe malnutrition, severe dehydration, exposure to neurotoxic insecticides, those receiving antimalarial drugs or those with a recessive hereditary trait. Succinylcholine should be administered with extreme care to such patients and doses should be minimal. If low plasma pseudocholinesterase activity is suspected, a small test dose of succinylcholine 5-10 mg may be administered or relaxation may be produced by the cautious administration of 0.1% IV drip. Drugs which either inhibit plasma pseudocholinesterase (eg, neostigmine) or compete with succinylcholine for the enzyme (as does IV procaine) should not be given concurrently with succinylcholine.
Carcinogenicity, Mutagenicity & Impairment of Fertility: There have been no long-term studies performed in animals to evaluate carcinogenic potential.
Use in pregnancy: Pregnancy Category C: Teratogenic Effects: Animal reproduction studies have not been conducted with succinylcholine chloride. It is also not known whether succinylcholine can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. Succinylcholine should be given to a pregnant woman only if clearly needed.
Labor and Delivery: Succinylcholine is used in labor and delivery for muscle relaxation to treat such conditions as laryngospasm and to facilitate intubation during general anesthesia. Succinylcholine has no direct action on the uterus or other smooth muscle structures. Since succinylcholine is highly ionized and has low fat solubility, it does not readily cross the placenta.
Use in lactation: It is not known whether succinylcholine is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised following succinylcholine administration to a nursing woman.
Use in children: As in adults, the incidence of bradycardia in children is higher following the 2nd dose of succinylcholine. The incidence and severity of bradycardia is higher in children than adults. Pre-treatment with anticholinergic agents eg, atropine, may reduce the occurrence of bradyarrhythmias.
Use In Pregnancy & Lactation
Use in pregnancy: Pregnancy Category C: Teratogenic Effects: Animal reproduction studies have not been conducted with succinylcholine chloride. It is also not known whether succinylcholine can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. Succinylcholine should be given to a pregnant woman only if clearly needed.
Labor and Delivery: Succinylcholine is used in labor and delivery for muscle relaxation to treat such conditions as laryngospasm and to facilitate intubation during general anesthesia. Succinylcholine has no direct action on the uterus or other smooth muscle structures. Since succinylcholine is highly ionized and has low fat solubility, it does not readily cross the placenta.
Use in lactation: It is not known whether succinylcholine is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised following succinylcholine administration to a nursing woman.
Adverse Reactions
Adverse reactions to succinylcholine consist primarily of an extension of its pharmacological actions. Profound muscle relaxation may occur resulting in respiratory depression to the point of apnea. Hypersensitivity, including anaphylaxis, to succinylcholine may exist in rare instances.
The following additional adverse reactions have been reported: Bradycardia (frequently noted after a 2nd IV injection of 2% solution in children), tachycardia, hypertension, hypotension, cardiac arrest, malignant hyperthermia, increased intraocular pressure, muscle fasciculation, postoperative muscle pain and excessive salivation.
Caution For Usage
Only freshly prepared solutions of succinylcholine should be used. Solution remaining after completion of the operative schedule for the day should be discarded.
Succinylcholine is rapidly hydrolyzed, quickly loses potency and may cause a precipitate to form when mixed with alkaline solutions of other drugs. Preferably, succinylcholine should be separately injected and should not be mixed in the same syringe nor administered simultaneously through the same needle with solutions of short-acting barbiturates eg, Pentothal (Thiopental Sodium Injection, USP) or other drugs which have an alkaline pH. If such mixtures are used at all, they must be given within a few minutes after they are prepared.
Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration whenever solution and container permit. Solutions which are not clear and colorless should not be used.
Storage
Store in refrigerator 2°-8°C (36°-46°F).
The multi-dose vials are stable for up to 14 days at room temperature without significant loss of potency.
ATC Classification
M03AB01 - suxamethonium ; Belongs to the class of choline derivative agents used as peripherally-acting muscle relaxants.
Presentation/Packing
Inj (vial) 20 mg/mL x 10 mL.
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