Physostigmine

Physostigmine Brand Name– Antilirium

What is Physostigmine

Physostigmine is a parenteral and ophthalmic cholinesterase inhibitor. Physostigmine is similar to neostigmine except that it is a tertiary amine while neostigmine is a quaternary amine. This difference may explain the increased activity of physostigmine in the CNS.

Physostigmine most commonly is used as an ophthalmic agent in the treatment of open-angle glaucoma. It has also been used to counteract toxic anticholinergic effects (both central and peripheral) of other drugs which cause anticholinergic toxicity, particularly in overdose situations.

Until recently, physostigmine was used to treat tricyclic antidepressant (TCA) overdose, but it is no longer recommended for this purpose due to its own potentially harmful effects including seizures and life-threatening bradyarrhythmias progressing to asystole.

Physostigmine has been used to treat Alzheimer’s disease and hereditary ataxias. While some improvements were noted in some studies, the drug has not been well established in these diseases.

Extracted physostigmine was first used ophthalmically, for glaucoma, in 1875. It was first synthesized in 1935, and is accepted by the FDA as a pre-1938 drug. A sustained-release form of physostigmine salicylate (Synapton®) has completed phase III investigation for Alzheimer’s disease as of August 1996.

Indications

  • anticholinergic syndrome
  • glaucoma

For antagonism of toxic anticholinergic effects which manifest as the ‘anticholinergic syndrome’

Side Effects

  1. abdominal pain
  2. bradycardia
  3. bronchospasm
  4. confusion
  5. diaphoresis
  6. dyspnea
  7. hyperhidrosis
  8. hypersalivation
  9. hypotension
  10. increased urinary frequency
  11. lacrimation
  12. miosis
  13. muscle paralysis
  14. myasthenia
  15. nausea
  16. palpitations
  17. seizures
  18. vomiting

Monitoring Parameters

  • laboratory monitoring not necessary

Contraindications

  • asthma
  • bradycardia
  • breast-feeding
  • cardiac disease
  • closed-angle glaucoma
  • diabetes mellitus
  • GI obstruction
  • hypotension
  • ileus
  • neonates
  • peptic ulcer disease
  • pregnancy
  • seizure disorder
  • sulfite hypersensitivity
  • urinary tract obstruction

Interactions

  • Ambenonium Chloride
  • Amifampridine
  • Amoxapine
  • Articaine; Epinephrine
  • Atracurium
  • Atropine
  • Atropine; Benzoic Acid; Hyoscyamine; Methenamine; Methylene Blue; Phenyl Salicylate
  • Atropine; Difenoxin
  • Atropine; Diphenoxylate
  • Atropine; Edrophonium
  • Atropine; Hyoscyamine; Phenobarbital; Scopolamine
  • Azelastine; Fluticasone
  • Beclomethasone
  • Benzoic Acid; Hyoscyamine; Methenamine; Methylene Blue; Phenyl Salicylate
  • Benztropine
  • Betamethasone
  • Budesonide
  • Budesonide; Formoterol
  • Bupivacaine
  • Bupivacaine Liposomal
  • Bupivacaine; Lidocaine
  • Chloroprocaine
  • Cholinergic agonists
  • Ciclesonide
  • Cisatracurium
  • Cocaine
  • Corticosteroids
  • Cortisone
  • Deflazacort
  • Dexamethasone
  • Dicyclomine
  • Digoxin
  • Edrophonium
  • Etomidate
  • Fludrocortisone
  • Flunisolide
  • Fluticasone
  • Fluticasone; Salmeterol
  • Fluticasone; Umeclidinium; Vilanterol
  • Fluticasone; Vilanterol
  • Formoterol; Mometasone
  • Fospropofol
  • Glycopyrrolate
  • Glycopyrrolate; Formoterol
  • Halogenated Anesthetics
  • Homatropine; Hydrocodone
  • Hydrocortisone
  • Hyoscyamine
  • Hyoscyamine; Methenamine; Methylene Blue; Phenyl Salicylate; Sodium Biphosphate
  • Indacaterol; Glycopyrrolate
  • Ketamine
  • Levobupivacaine
  • Lidocaine
  • Lidocaine; Prilocaine
  • Mepivacaine
  • Mepivacaine; Levonordefrin
  • Methenamine; Sodium Acid Phosphate; Methylene Blue; Hyoscyamine
  • Methocarbamol
  • Methylprednisolone
  • Mivacurium
  • Mometasone
  • Neostigmine
  • Nonsteroidal antiinflammatory drugs
  • Oxybutynin
  • Pancuronium
  • Prednisolone
  • Prednisone
  • Prilocaine
  • Prilocaine; Epinephrine
  • Procaine
  • Propantheline
  • Propofol
  • Pyridostigmine
  • Quinine
  • Rocuronium
  • Ropivacaine
  • Scopolamine
  • Succinylcholine
  • Tetracaine
  • Triamcinolone
  • Tricyclic antidepressants
  • Trihexyphenidyl
  • Vecuronium
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