Physostigmine

SOLNS SHOULD BE KEPT WELL CLOSED IN LIGHT-RESISTANT, ALKALI-FREE GLASS CONTAINER& USED WITHIN A WK. /PHYSOSTIGMINE SALICYLATE/

Store below 40 °C (104 °F), preferably between 15 and 30 °C (59 and 86 °F), unless otherwise specified by manufacturer. Store in a tight, light-resistant container. Protect from freezing. /Physostigmine salicylate ophthalmic solution USP/

Packaging and storage: Store below 40 °C ( 104 °F), preferably between 15 and 30 °C (59 and 86 °F), unless otherwise specified by manufacturer. Store in a tight container. Protect from freezing. /Physostigmine sulfate ophthalmic ointment USP/

Packaging and storage: Store below 40 °C (104 °F), preferably between 15 and 30 °C (59 and 86 °F), unless otherwise specified by manufacturer. Protect from light. Protect from freezing. /Physostigmine salicylate USP/

For more Storage Conditions (Complete) data for PHYSOSTIGMINE (6 total), please visit the HSDB record page.

This is a carbamate pesticide. As for other carbamate pesticides, avoid breathing dusts, and fumes from burning materials. Keep upwind. Avoid bodily contact with the material. Wash away any material which may have contacted the body with copious amounts of water or soap and water. (EPA, 1998)

0.41 [mg/m3]

4.5 [mg/m3]

27 [mg/m3]

For emergency situations, wear a positive pressure, pressure-demand, full facepiece self-contained breathing apparatus (SCBA) or pressure- demand supplied air respirator with escape SCBA and a fully-encapsulating, chemical resistant suit. (EPA, 1998)

ACTIONS OF ANTICHOLINESTERASE AGENTS ON AUTONOMIC EFFECTOR CELLS & ON CORTICAL & SUBCORTICAL SITES IN CNS, WHERE RECEPTORS ARE LARGELY OF MUSCARINIC TYPE, ARE BLOCKED BY ATROPINE. /ANTI-CHOLINESTERASE AGENTS/

VARIOUS ACTIONS OF ANTI-CHOLINESTERASE AGENTS ON SKELETAL MUSCLE ARE AUGMENTED BY EPINEPHRINE OR EPHEDRINE ... & BLOCKED BY D-TUBOCURARINE. /ANTICHOLINESTERASEAGENTS/

SUFFICIENT CONCN OF ... PHYSOSTIGMINE ... PREVENTS ALKYLPHOSPHORYLATION OF ACETYLCHOLINESTERASE BY DIISOPROPYLFLUORO PHOSPHATE OCCUPATION OF ACTIVE SITES OF /CHOLINESTERASE/ ENZYME BY THE SHORTER ACTING DRUG PREVENTS ... ALKYLPHOSPHORYLATION BY ORGANOPHOSPHORUS CMPD ... IN VITRO & IN VIVO.

TOXOGONIN GIVEN 15 MIN PRIOR TO ADMIN OF PHYSOSTIGMINE CAUSED REDN IN TOXICITY TO MICE OF PHYSOSTIGMINE. PRALIDOXIME MESYLATE ALSO CAUSED SLIGHT REDN.

For more Interactions (Complete) data for PHYSOSTIGMINE (9 total), please visit the HSDB record page.

Physostigmine, an indirect-acting parasympathomimetic agent, is an alkaloid usually obtained from the dried ripe seeds of Physostigma venenosum.

FROM CALABAR BEANS, THE SEEDS OF THE VINE PHYSOSTIGMA VENENOSUM BALF, LEGUMINOSAE.

GI SYMPTOMS OCCUR EARLIEST AFTER INGESTION, & INCL ANOREXIA, NAUSEA & VOMITING, ABDOMINAL CRAMPS, & DIARRHEA. WITH PERCUTANEOUS ABSORPTION OF LIQ, LOCALIZED SWEATING & MUSCULAR FASCICULATION IN IMMEDIATE VICINITY ARE GENERALLY EARLIEST MANIFESTATIONS. /ANTI-CHOLINESTERASE AGENTS/

EFFECTS ON CNS INCL CONFUSION, ATAXIA, SLURRED SPEECH, LOSS OF REFLEXES, CHEYNE-STOKES RESPIRATION, GENERALIZED CONVULSIONS, COMA, & CENTRAL RESP PARALYSIS. ... TIME OF DEATH AFTER SINGLE ACUTE EXPOSURE ... 5 MIN TO NEARLY 24 HR, DEPENDING UPON DOSE, ROUTE ... CAUSE OF DEATH ... RESP FAILURE ... /&/ SECONDARY CARDIOVASCULAR COMPONENT. /ANTI-CHOLINESTERASE AGENTS/

AFTER LOCAL EXPOSURE TO VAPORS OR ... INHALATION, OCULAR PAIN & RESP EFFECTS GENERALLY APPEAR FIRST. OCULAR ... INCL MARKED MIOSIS, OCCULAR PAIN, CONJUNCTIVAL CONGESTION, DIMINISHED VISION, CILIARY SPASM, & BROW ACHE. IN ADDITION TO RHINORRHEA AND HYPEREMIA OF THE UPPER RESP TRACT, RESP EFFECTS CONSIST OF "TIGHTNESS" IN CHEST & WHEEZING RESP, CAUSED BY ... BRONCHOCONSTRICTION & INCR BRONCHIAL SECRETION. /ANTI-CHOLINESTERASE AGENTS/

NICOTINIC ACTIONS @ NEUROMUSCULAR JUNCTIONS OF SKELETAL MUSCLE ... FATIGABILITY & GENERALIZED WEAKNESS, INVOLUNTARY TWITCHINGS ... SEVERE WEAKNESS & PARALYSIS; A CENTRAL COMPONENT OF ACTION CONTRIBUTES TO SOME OF THESE EFFECTS. THE MOST SERIOUS CONSEQUENCE ... IS PARALYSIS OF RESPIRATORY MUSCLES. /ANTI -CHOLINESTERASE AGENTS/

For more Human Toxicity Excerpts (Complete) data for PHYSOSTIGMINE (18 total), please visit the HSDB record page.

Drug-Induced Liver Injury Severity and Toxicity (DILIst)

physostigmine

DILI Negative

Intravenous

DOI:10.1016/j.drudis.2019.09.022

INJECTING 0.05 TO 15.0 MG INTO THE YOLK SAC DURING THE FIRST 12 DAYS OF INCUBATION PRODUCED SEVERE VERTEBRAL DEFECTS AND MICROMELIA IN CHICKS. /ANOTHER EXPT/ USED 0.05 MG AT 26 HR TO PRODUCE BRACHYMELIA AND SPINA BIFIDA IN THE CHICK.

Two consecutive im doses of physostigmine (300 ug/kg, at 0 and 120 min) were given to male Sprague Dawley rats and the effects on acetylcholine, choline, the activity of choline acetyltransferase, and the release of acetylcholine from slices of caudate nucleus were studied. Peak inhibition of cholinesterase was moderate (65%) at 15 min after the first physostigmine administration. The time course and extent of inhibition of cholinesterase after the first and second administration of physostigmine followed a similar pattern. Fifteen min after the second administration of physostigmine, inhibition of cholinesterase was 60%; the activity recovered to control levels at 120 min. After the first administration of physostigmine, levels of acetylcholine incr by 70%. The peak value of acetylcholine was reached at 15 min. Acetylcholine returned almost to control levels at 60 min after treatment. The incr in the level of acetylcholine in brain seen with the second administration of physostigmine was of the same order and duration as that seen after the first administration.

Recommended treatment for physostigmine overdose includes: Maintenance of open airway (possible suction of bronchial secretions); use of assisted respiration. Monitoring of cardiac function. Intravenous administration of atropine sulfate in doses of 2 to 4 mg; may be repeated every 3 to 10 minutes, if necessary to control muscarinic effects. Intravenous administration of pralidoxime chloride at a rate of 50 to 100 mg per minute, to counteract ganglionic and skeletal muscle effects. Treatment of convulsions or shock as appropriate.

Manufacturers, packers, and distributors of drug and drug products for human use are responsible for complying with the labeling, certification, and usage requirements as prescribed by the Federal Food, Drug, and Cosmetic Act, as amended (secs 201-902, 52 Stat. 1040 et seq., as amended; 21 U.S.C. 321-392).

Releases of CERCLA hazardous substances are subject to the release reporting requirement of CERCLA section 103, codified at 40 CFR part 302, in addition to the requirements of 40 CFR part 355. Physostigmine is an extremely hazardous substance (EHS) subject to reporting requirements when stored in amounts in excess of its threshold planning quantity (TPQ) of 100/10,000 lbs.

MEDICATION

MEDICATION (VET):

PHYSOSTIGMINE IS GENERALLY USED AS SALICYLATE OR SULFATE SALT; SALICYLATE HAS ADVANTAGE OF BEING LESS DELIQUESCENT ... ADDITION OF FEW GRAINS BORIC ACID TO SOLN OF SALT ... INHIBIT FORMATION OF RED DECOMP PRODUCT ... .

PHYSOSTIGMINE, USP (ESERINE), PHYSOSTIGMINE SALICYLATE, USP, & PHYSOSTIGMINE SULFATE, USP ARE AVAILABLE AS CRYSTALLINE POWDERS FOR COMPOUNDING ORAL & PARENTERAL PREPN IN SUITABLE DOSAGE FORMS.

PHYSOSTIGMINE SALICYLATE (ANTILIRIUM) IS AVAILABLE AS A SOLUTION (1 MG/ML) FOR INJECTION. PHYSOSTIGMINE SULFATE OPHTHALMIC OINTMENT (0.25%) & PHYSOSTIGMINE SALICYLATE OPHTHALMIC SOLUTION (0.25% & 0.5%), ARE ALSO AVAILABLE.

Ophthalmic solution (as the salicylate), 0.25% and 0.5%. Ophthalmic ointment (as the sulfate), 0.25%. Ampules and syringes (as the salicylate), 1 mg/ml.

For more Formulations/Preparations (Complete) data for PHYSOSTIGMINE (8 total), please visit the HSDB record page.

Pyrrolo[2,3-b]indol-5-ol, 1,2,3,3a,8,8a-hexahydro-1,3a,8-trimethyl-, 5-(N-methylcarbamate), (3aS,8aR)-: ACTIVE

THE VIABILITY OF THE CONDITIONED FLAVOR AVERSION TEST AS A BEHAVIORAL INDEX OF THE TOXICITY OF PHYSOSTIGMINE WAS EVALUATED IN A SERIES OF THREE EXPERIMENTS. IT WAS CONCLUDED THAT THE FLAVOR AVERSION TEST IS A SIMPLE AND SENSITIVE BEHAVIORAL MEASURE OF TOXICITY.

Available as the salicylate and sulfate.