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Created January 27, 2022, last updated almost 3 years ago.
Collection: 151, Score: 697, Trend score: 0, Read count: 1129, Articles count: 13, Created: 2022-01-27 01:23:35 UTC. Updated: 2022-01-27 01:44:51 UTC.Notes
Suxamethonium chloride (suxamethonium, succinylcholine or sux) is a depolarising muscle relaxant that produces rapid-onset, short-duration, deep muscle relaxation. First identified in 1906 and used medically in 1951, it is one of the oldest anaesthesia drugs still widely used. Due to its unique properties and low cost, it remains on the World Health Organisation's List of Essential Medicines
A. Physiochemistry
- (CH3)3-N-CH2CH2-OCO-CH2CH2-OCO-CH2CH2-N-(CH3)3
- pH 3.5
- Shelf life 3 years at 4°C, though only 'months' at 20°C.
B. Pharmacokinetics
- Dose - ED95 0.5 mg/kg, IV 1.5 mg/kg, IM 2.5-4 mg/kg.
- Absorption - IM, IV.
- Distribution - >0.2 L/kg; crosses placenta slightly but little effect on foetus.
- Protein binding ?
- Onset 30s IV, 2-3 min IM; Offset 3-5 min.
- Metabolism - PChE to succinylmonocholine (5% activity) & choline -> succinic acid & choline.
- tß½ 5 minutes
C. Pharmacodynamics
- Mechanism - binds to alpha subunit of nicotinic ACh receptor, producing persistent depolarisation (phase 1 & phase 2 blocks).
- CNS - ⇡ intra-ocular pressure (4-8 mmHg rise), ⇡ intra-celebral pressure (to 30 mmHg at 2-4 min).
- CVS - arrhythmias (both bradycardia & tachycardia possible), ⇡ systolic blood pressure, (both negative inotropic and chronotropic effects).
- Resp - 'sux apnoea' pharmacogenetic diversity (94% normal, 3.8% heterozyg (10 min duration of effect), <1% homozog (1-2h duration))
- Renal - hyperkalaemia due to K+ release from muscle; beware in neuromuscular conditions, denervation, and extensive burns.
- GIT - ⇡ intragastric pressure, ⇡ secretions, salivation.
- SEs - anaphylaxis, malignant hyperthermia, sux apnoea, muscle pains, masseter spasm.
Daniel Jolley
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Collected Articles
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Severe life-threatening hyperkalaemia may occur following administration of suxamethonium during certain periods after burns, neurological injuries, and in certain other conditions. Although this response is well-known, there is disagreement about when it may occur. This review describes the normal hyperkalaemic response to suxamethonium, the factors affecting it, the conditions in which it may be exaggerated, and the periods of high risk.
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Pure suxamethonium chloride does not produce in vitro contracture of skeletal muscle from swine which are susceptible to malignant hyperpyrexia (MH), but does induce MH in vivo. It is suggested that suxamethonium chloride induces MH because the fasciculations which it causes lead to an increase in the myoplasmic calcium concentration.