Pharmacopeia

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Field NEOSTIGMINE
Neurology & Sedation · Neurology & Sedation · Level 2
SUGAMMADEX
Neuromuscular · Neuromuscular · Level 2
Mechanism of action

reversible acid transferring cholinesterase inhibitor that binds to the esteratic site of AChE and is hydrolyzed but at a much slower rate than Ach. Leads to increase in Ach in the synapse.

Encapsulates steroid portion of aminosteroid molecules. The binding leads to a decrease of free drug in the central compartment, leading to a diffusion gradient away from the NMJ.
Median time to recovery 90 seconds

Physiological effects

CVS: Bradycardia. In high doses a central effect may precipitate hypotension

Resp: Bronchoconstriction in asthmatic. Increased bronchial secretion

Renal: Increased ureteric peristalsis leading to involuntary micturition

GIT:
- Salivation
- Increased LOS tone and GIT motility (cramps)
- N/V
- Increased gastric acid output

CNS: Miosis and failure to accommodate

Other: Sweating and lacrimation

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Absorption

Poorly absorbed orally (bioavailability 1%)

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Distribution

Highly ionized so does not cross BBB

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Protein binding

10% PB

Not protein bound

Volume of distribution

Vd 0.5-1L/Kg

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Metabolism

- Predominantly plasma esterases
- Some hepatic metabolism with biliary excretion

None

Excretion

65% renally excreted

95% unaltered in urine

Half-life

T1/2= 15-80min (increased in renal failure)

T1/2 is 1.8 hours

Adverse Effects Toxicity

(SLUDGE-BM)
- Salivation
- Lacrimation
- Urination
- Diaphoresis
- GI upset
- Emesis
- Bradycardia and bronchoconstriction
- Miosis

- Prolongs suxamethonium duration of action

1. Anaphylaxis
2. Fluclox can displace aminosteroids from Sugammadex

Chemical Pharmaceutics

Carbamate ester Acetylcholinesterase inhibitor

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Class Group

Cholinesterase Inhibitor

Neuromuscular - Miscellaneous

Indications Uses

- Reversal of NDMR (0.05mg/kg)
- Myasthenia gravis (PO 15-30mg)
- Urinary retention
- Paralytic ileus

1. Reversal of NMB by aminosteroid NMBA (Rocuronium>vecuronium>>pancuronium)

Introduction —

Cyclodextrin Selective Relaxant Binding Agent

Legacy Cicm Level

Level 2

Level 3

Presentation

PO or IV (IV preparations may contain glycopyrolate)

Clear colourless or pale yellow solution for injection
Contains 100mg/ml of y-Cyclodextrin Sugammadex

Route And Dose —

4mg/kg for deep block
2mg/kg for shallow block
16mg/kg for rescue reversal in RSI CICO scenario