ANECTINE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ANECTINE (ANECTINE).
Depolarizing neuromuscular blocker; mimics acetylcholine at nicotinic receptors at the neuromuscular junction, causing sustained depolarization and receptor desensitization.
| Metabolism | Hydrolyzed by plasma pseudocholinesterase (butyrylcholinesterase) to succinylmonocholine and choline; minor hepatic metabolism. |
| Excretion | Renal: 10-15% unchanged; hepatic: rapid hydrolysis by plasma pseudocholinesterase (butyrylcholinesterase) to succinylmonocholine and succinic acid; <2% biliary; <2% fecal |
| Half-life | 2-5 minutes (pseudocholinesterase hydrolysis); terminal half-life of succinylmonocholine ~30-60 minutes; clinical duration of apnea determined by rapid initial hydrolysis |
| Protein binding | 30-50% (primarily to albumin); low binding to other proteins |
| Volume of Distribution | 0.3-0.6 L/kg; corresponds to extracellular fluid volume; higher in neonates (0.4-0.7 L/kg) |
| Bioavailability | IV: 100%; IM: 80-100% (rapid absorption); oral: negligible (<1%) due to first-pass hydrolysis |
| Onset of Action | IV: 30-60 seconds; IM: 2-3 minutes |
| Duration of Action | IV: 4-6 minutes (succinylcholine dose-dependent: 1-1.5 mg/kg produces paralysis for 5-10 minutes; clinical duration of neuromuscular block); prolonged in pseudocholinesterase deficiency or with anticholinesterases |
1-1.5 mg/kg IV bolus for intubation; maintenance infusion: 2.5-4.3 mg/min IV; alternatively, 3-4 mg/kg IM for intubation.
| Dosage form | INJECTABLE |
| Renal impairment | No specific GFR-based dose adjustment recommended; use with caution in renal impairment due to prolonged effect. |
| Liver impairment | No specific Child-Pugh based adjustment; use with caution in hepatic impairment due to reduced pseudocholinesterase activity. |
| Pediatric use | Neonates: 2 mg/kg IV; Infants and children: 1-2 mg/kg IV; maintenance infusion: 0.5-1 mg/kg/min IV. |
| Geriatric use | Reduce initial dose (e.g., 0.6 mg/kg IV) due to decreased pseudocholinesterase activity; monitor for prolonged paralysis. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ANECTINE (ANECTINE).
| Breastfeeding | Excretion into breast milk is unknown. Because of its rapid metabolism and short half-life, systemic absorption by the infant is unlikely. Caution is advised. M/P ratio not available. |
| Teratogenic Risk | ANECTINE (succinylcholine) is a short-acting depolarizing neuromuscular blocker. Available data do not indicate an increased risk of major birth defects or miscarriage. Animal reproduction studies have not been well-conducted. Transplacental passage is limited. Use in pregnancy only if clearly needed. |
| Fetal Monitoring |
■ FDA Black Box Warning
Risk of cardiac arrest from hyperkalemia in undiagnosed skeletal muscle myopathies, especially in children and adolescent males with Duchenne muscular dystrophy. Use alternative agents in patients with known myopathies or elevated plasma creatine kinase.
| Serious Effects |
Personal or familial history of malignant hyperthermia, known hypersensitivity to succinylcholine, skeletal muscle myopathies (e.g., Duchenne muscular dystrophy), acute narrow-angle glaucoma, and patients with atypical plasma pseudocholinesterase.
| Precautions | Risk of malignant hyperthermia, bradycardia or asystole, especially with repeated doses; hyperkalemia in patients with burns, trauma, neuromuscular disease, or denervation; increased intraocular and intragastric pressure; prolonged paralysis in patients with atypical pseudocholinesterase; caution in patients with electrolyte imbalances, renal failure, or pulmonary hypertension. |
| Food/Dietary | No known food interactions. However, grapefruit juice may alter metabolism by inhibiting pseudocholinesterase? (theoretical, not clinically established). Enteral nutrition should be held during paralysis due to aspiration risk. |
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| Monitor maternal vital signs and oxygen saturation. Fetal heart rate should be monitored if used during cesarean delivery. Assess for prolonged neuromuscular blockade due to pseudocholinesterase deficiency. |
| Fertility Effects | No known effects on fertility. No human or animal data available regarding impairment of fertility. |
| Clinical Pearls | ANECTINE (succinylcholine) is a depolarizing neuromuscular blocker with rapid onset (30-60 seconds) and short duration (5-10 minutes). Avoid in patients with atypical pseudocholinesterase deficiency (risk of prolonged paralysis), hyperkalemia risk (e.g., burns, denervation, crush injuries), and malignant hyperthermia susceptibility. Use with caution in patients with myasthenia gravis (resistance). Always have resuscitation equipment available. Bradycardia is common with repeated doses; atropine may be considered in children. |
| Patient Advice | This medication causes complete paralysis and you will be unable to breathe on your own; a machine will breathe for you. · You may experience muscle fasciculations (twitching) before paralysis. This is normal. · You will remain awake during paralysis unless other anesthetics are given; you will not remember the procedure. · Tell your doctor if you have a personal or family history of malignant hyperthermia (severe fever with muscle breakdown). · Disclose any use of medications that affect potassium levels (e.g., digoxin, diuretics) or previous reactions to succinylcholine. |