QUELICIN (Page 4 of 5)

8.4 Pediatric Use

Safety and effectiveness of succinylcholine chloride have been established in pediatric patient age groups, neonate to adolescent. Because of a risk of ventricular dysrhythmias, cardiac arrest, and death from hyperkalemic rhabdomyolysis in pediatric patients, reserve the use of QUELICIN in pediatric patients for emergency intubation or instances where immediate securing of the airway is necessary, e.g., laryngospasm, difficult airway, full stomach, or for intramuscular use when a suitable vein is inaccessible [see Warnings and Precautions (5.1)].

Intravenous bolus administration of QUELICIN in pediatric patients (including infants) may result in profound bradycardia or, rarely, asystole. The incidence and severity of bradycardia is higher in pediatric patients than adults [see Warnings and Precautions (5.6)].

The effective dose of QUELICIN in pediatric patients may be higher than that predicted by body weight dosing alone [see Dosage and Administration (2.3)].

8.5 Geriatric Use

Clinical studies of QUELICIN did not include sufficient numbers of subjects aged 65 years and over to determine whether they respond differently from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients.

In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.

10 OVERDOSAGE

Overdosage with QUELICIN may result in neuromuscular block beyond the time needed for surgery and anesthesia. This may be manifested by skeletal muscle weakness, decreased respiratory reserve, low tidal volume, or apnea. The primary treatment is maintenance of a patent airway and respiratory support until recovery of normal respiration is assured. Depending on the dose and duration of QUELICIN administration, the characteristic depolarizing neuromuscular block (Phase I) may change to a block with characteristics superficially resembling a non-depolarizing block (Phase II) [see Warnings and Precautions (5.8)].

11 DESCRIPTION

QUELICIN (Succinylcholine Chloride Injection, USP) is a sterile, nonpyrogenic solution to be used as a short-acting, depolarizing neuromuscular blocker for intravenous or intramuscular use. QUELICIN contains succinylcholine chloride as the active pharmaceutical ingredient.

Succinylcholine Chloride, USP is chemically designated C14 H30 Cl2 N2 O4 and its molecular weight is 361.31. The chemical name of succinylcholine chloride is ethanaminium, 2,2′-[(1,4-dioxo-1,4 butanediyl)bis(oxy)]bis[N,N,N-trimethyl-], dichloride. Succinylcholine chloride 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. It has the following structural formula:

Chemical Structure
(click image for full-size original)

QUELICIN 1,000 mg/10 mL (100 mg/mL) is intended for single-dose administration and contains no preservative. Each 1 mL of QUELICIN 1,000 mg/10 mL (100 mg/mL) single-dose fliptop vials contains: 100 mg of succinylcholine anhydrous (equivalent to 113.27 mg of Succinylcholine Chloride, USP), and sodium hydroxide and hydrochloric acid as pH adjusters in water for injection. The pH of the solution is between 3.0 and 4.5, with an osmolarity of 0.830 mOsm/mL (calc.).

QUELICIN 200 mg/10 mL (20 mg/mL) is intended for multiple-dose administration and contains preservative. Each 1 mL of QUELICIN 200 mg/10 mL (20 mg/mL) multiple-dose fliptop vials contains: 20 mg of succinylcholine anhydrous (equivalent to 22.65 mg of Succinylcholine Chloride, USP), 1.8 mg of methylparaben and 0.2 mg of propylparaben as preservatives, 4.65 mg of sodium chloride as iso-osmotic agent, and sodium hydroxide and hydrochloric acid as pH adjusters in water for injection. The pH of the solution is between 3.0 and 4.5, with an osmolarity of 0.338 mOsm/mL (calc.).

12 CLINICAL PHARMACOLOGY

12.1 Mechanism of Action

Succinylcholine is a depolarizing neuromuscular blocker. 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.

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.

12.2 Pharmacodynamics

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. Tachyphylaxis occurs with repeated administration [see Warnings and Precautions (5.8)]. The transition from Phase I to Phase II block has been reported in 7 of 7 patients studied under halothane anesthesia after an accumulated dose of 2 to 4 mg/kg succinylcholine (administered in repeated, divided doses). The onset of Phase II block coincided with the onset of tachyphylaxis and prolongation of spontaneous recovery. In another study, using balanced anesthesia (N2 O/O2 /narcotic-thiopental) and succinylcholine infusion, the transition was less abrupt, with great individual variability in the dose of succinylcholine required to produce Phase II block. Of 32 patients studied, 24 developed Phase II block. Tachyphylaxis was not associated with the transition to Phase II block, and 50% of the patients who developed Phase II block experienced prolonged recovery [see Warnings and Precautions (5.8)].

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 Warnings and Precautions (5.1, 5.4, 5.6), Use in Specific Populations (8.4)]. These effects are enhanced by halogenated anesthetics.

Succinylcholine causes an increase in intraocular pressure immediately after its injection and during the fasciculation phase, and increases which may persist after onset of complete paralysis [see Warnings and Precautions (5.7)].

Succinylcholine may cause increases in intracranial pressure immediately after its injection and during the fasciculation phase [see Warnings and Precautions (5.11)].

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 with normal clinical usage.

Succinylcholine has no effect on consciousness, pain threshold or cerebration [see Warnings and Precautions (5.14)].

Succinylcholine has no direct action on the uterus or other smooth muscle structures.

12.3 Pharmacokinetics

Elimination

Succinylcholine levels were reported to be below the detection limit of 2 µg/mL after 2.5 minutes of an intravenous bolus dose of 1 or 2 mg/kg in 14 anesthetized patients.

Metabolism

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.

Excretion

About 10% of the drug is excreted unchanged in the urine.

Specific Populations

Pediatric Patients

Due to the relatively large volume of distribution in the pediatric patient versus the adult patient, the effective dose of QUELICIN in pediatric patients may be higher than that predicted by body weight dosing alone [see Dosage and Administration (2.3)].

All MedLibrary.org resources are included in as near-original form as possible, meaning that the information from the original provider has been rendered here with only typographical or stylistic modifications and not with any substantive alterations of content, meaning or intent.

This site is provided for educational and informational purposes only, in accordance with our Terms of Use, and is not intended as a substitute for the advice of a medical doctor, nurse, nurse practitioner or other qualified health professional.

Privacy Policy | Copyright © 2022. All Rights Reserved.