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Chapter: Clinical Anesthesiology: Clinical Pharmacology: Cholinesterase Inhibitors & Other Pharmacologic Antagonists to Neuromuscular Blocking Agents

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Cholinesterase Inhibitors: Pyridostigmine

Pyridostigmine is structurally similar to neostig-mine except that the quaternary ammonium is incorporated into the phenol ring.

PYRIDOSTIGMINE

Physical Structure

Pyridostigmine is structurally similar to neostig-mine except that the quaternary ammonium is incorporated into the phenol ring. Pyridostigmine shares neostigmine’s covalent binding to acetylcho-linesterase and its lipid insolubility.

Dosage & Packaging

Pyridostigmine is 20% as potent as neostigmine and may be administered in doses up to 0.25 mg/kg (a total of 20 mg in adults). It is available as a solu-tion of 5 mg/mL.

Clinical Considerations

The onset of action of pyridostigmine is slower (10–15 min) than that of neostigmine, and its duration is slightly longer (>2 h). Glycopyrrolate (0.05 mg per 1 mg of pyridostigmine) or atropine

(0.1 mg per 1 mg of pyridostigmine) must also be administered to prevent bradycardia. Glyco-pyrrolate is preferred because its slower onset of action better matches that of pyridostigmine, again resulting in less tachycardia.

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