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succinylcholine (Anectine, Flo-Pack, Quelicin, Sucostrin, Myorelaxin)

Tradenames: Anectine, Flo-Pack, Quelicin, Sucostrin. Indications: 1) skeletal muscle relaxation during a) short surgical procedures under general anesthesia [4] b) endoscopic examinations c) orthopedic manipulation d) electroshock therapy e) endotracheal intubation 2) must ALWAYS be used with sedatives, i.e.lorazepam or anesthetic & an analgesic as needed Contraindications: 1) malignant hyperthermia 2) myopathies associated with elevated serum creatinine 3) narrow-angle glaucoma 4) penetrating eye injuries 5) disorders of plasma pseudocholinesterase 6) children & adolescent except for emergency endotracheal intubation Caution: 1) hyperkalemia 2) paraplegia 3) extensive or severe burns 4) dystrophic neuromuscular disease Dosage: 1) 0.6.0-1.5 mg/kg up to 150 mg IV bolus over 10-30 seconds 2) repeat as necessary 3) infusion: 0.5-10 mg/min 4) intermittent dosing: a) 0.3-1.1 mg/kg initial dose b) followed by 0.04-0.07 mg/kg as necessary 5) pediatrics: 2 mg/kg IV preceded by atropine 0.02 mg/kg 6) pretreatment with atropine may reduce the incidence of bradycardia Injection: 20 mg/mL (10 mL). Powder for injection: 500 mg. 1 g. Pharmacokinetics: 1) rapid onset of action (30-60 seconds) 2) duration of action: a) 30 minutes; 2-5 minutes [2] b) determined by rate of diffusion away from motor end plate 3) metabolized rapidly by pseudocholinesterase to a less active metabolite which produces a non-depolarizing neuromuscular block; this metabolite may accumulate causing prolonged apnea 4) 10% excreted unchanged in the urine Adverse effects: 1) common (> 10%) - postoperative stiffness, increased intraocular pressure 2) less common (1-10%) - excessive salivation, tachycardia, bradycardia 3) uncommon (< 1%) - rash, itching, malignant hyperthermia, hypertension, erythema, circulatory collapse, bronchospasm 4) other - tachyphylaxis - muscle fasciculations* - hypotension - increased intragastric pressure - increased side effects noted when K+ levels are decreased or elevated - prolonged post-surgical apnea associated with mutant alleles of BuChE gene (BCHE gene mutation) * initial muscle fasciculations may result in post-operative pain Antidote: neostigmine, give with atropine in glycopyrrolate. Drug interactions: 1) aminoglycosides, tetracyclines, clindamycin: in combination prolong & increase neuromuscular blockade 2) corticosteroids: in combination prolong muscle weakness 3) K+ depleting agents (thiazides, loop diuretics, amphotericin B corticosteroids): increase & prolong neuromuscular paralysis 4) cholinesterase inhibitors: reverse neuromuscular blockade 5) organophosphates: reduce plasma levels of pseudocholinesterase which can can prolonged apnea 6) malignant hyperthermia when used with halothane Laboratory: - BCHE gene mutation - succinylcholine in serum/plasma - succinylcholine in urine Mechanism of action: 1) depolarizing neuromuscular blocking agent 2) skeletal muscle relaxation is produced by decreasing the response to acetylcholine at the myoneural junction 3) blocks access of acetylcholine to the motor end-plate

Interactions

drug interactions

Related

atropine (Atropair, Atropine-Care) glycopyrrolate (Robinul, Cuvposa, Qbrexza) neostigmine (Prostigmin)

General

neuromuscular blocker (paralyzing agent)

Properties

MISC-INFO: elimination route PLASMA pregnancy-category C safety in lactation ?

Database Correlations

PUBCHEM correlations

References

  1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996.
  2. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998 - not on National VA formulary
  3. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  4. Deprecated Reference