Physostigmine
- Atc Codes:S01EB05#V03AB19
- CAS Codes:57-47-6#64-47-1#57-64-7
- PHARMGKB ID:57-47-6#64-47-1#57-64-7
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Genes that may be involved
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Anticholium; Germany: Anticholium; Greece: Anticholium, Physostigmine; Italy: Eserina, Fisost.
North America
Canada: Eserinum, Physostigma.
Asia
Japan: Antilirium.
Drug combinations
Chemistry
Physostigmine: C~15~H~21~N~3~O~2~. Mw: 275.35. Pyrrolo[2,3-b]indol-5-ol, 1,2,3,3a,8,8a-hexahydro-1,3a,8-trimethyl-, methylcarbamate (ester), (3aS-cis); (2) 1,2,3,3aβ,8aβ-Hexahydro-1,3a,8-trimethylpyrrolo[2,3-b]-indol-5-yl methylcarbamate. CAS-57-47-6.
Physostigmine Sulfate: (C~15~H~21~N~3~O~2~)~2~ H~2~SO~4~. Mw: 648.77. Pyrrolo[2,3-b]indol-5-ol, 1,2,3,3a,8,8a-hexahydro-1,3a,8-trimethyl-, methylcarbamate (ester), (3aS-cis)-, sulfate (2:1). CAS-64-47-1.
Physostigmine Salicylate: C~15~H~21~N~3~O~2~ C~7~H~6~O~3~. Mw: 413.47. Pyrrolo[2,3-b]indol-5-ol, 1,2,3,3a,8,8a-hexahydro-1,3a,8-trimethyl-, methylcarbamate (ester), (3aS-cis)-, mono(2-hydroxybenzoate).CAS-57-64-7.
Pharmacologic Category
Parasympathomimetic (Cholinergic) Agents; Acetylcholinesterase Inhibitor. Antidotes. (ATC-Code: S01EB05; V03AB19)
Mechanism of action
Inhibits destruction of acetylcholine by acetylcholinesterase, which facilitates transmission of impulses across myoneural junction and prolongs central and peripheral effects of acetylcholine.
Therapeutic use
Reversal of toxic, life-threatening delirium caused by atropine, diphenhydramine, dimenhydrinate, Atropa belladonna (deadly nightshade), or jimson weed (Datura spp).
Pregnancy and lactiation implications
Caution during pregnancy or lactation.
Unlabeled use
Contraindications
Hypersensitivity to physostigmine or any component of the formulation. GI or GU obstruction. Asthma. Gangrene. Diabetes, cardiovascular disease. Any vagotonic state. Co-administration of choline esters and depolarizing neuromuscular-blocking agents.
Warnings and precautions
Patient must have normal QRS interval. Use caution in poisoning with agents known to prolong intraventricular conduction. Overdosage may result in cholinergic crisis. Not intended as first-line agent for anticholinergic toxicity. Use with caution in asthma, in cardiovascular disease, including bradycardia, in diabetes mellitus, and in gangrene. Not intended as first-line agent for Parkinson’s disease. Use with caution in history of seizure disorder. Concomitant administration of choline esters, or of depolarizing neuromuscular-blocking agents (i.e. succinylcholine) contraindicated. Products may contain benzyl alcohol (associated with «gasping syndrome» in neonates). Products may contain sodium bisulfate. Continuous intravenous infusions should never be used. Physostigmine not recommended in tricyclic antidepressant intoxication.