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Physostigmine

RTECS #: TJ2100000

CAS #: 57-47-6

UPDATE: May 2009 MW: 275.39 MF: C15H21N3O2


NOTE:

TABLE OF CONTENTS:
  1. SYNONYMS:
  2. REPRODUCTIVE EFFECTS DATA:
  3. ACUTE TOXICITY DATA:
  4. OTHER MULTIPLE DOSE DATA:
  5. REVIEWS:
  6. NIOSH DOCUMENTATION AND SURVEILLANCE:
  7. STATUS IN FEDERAL AGENCIES:
  8. REFERENCES:

SYNONYMS:

  1. ( - ) - Physostigmine
  2. CS 58525
  3. Carbamic acid, methyl - , ester with eseroline
  4. Eserine
  5. Eserolein, methylcarbamate (ester)
  1. Fysostigmin (Czech)
  2. MCV 4484
  3. NIH 10421
  4. Physostol


SKIN AND EYE IRRITATION DATA AND REFERENCES:

ROUTE/
ORGANISM 		DOSE
EFFECT

 REFERENCE
N/R
 N/R N/R N/R


MUTATION DATA AND REFERENCES:

SYSTEM TEST ROUTE/
ORGANISM/
TISSUE 		DOSE REFERENCE
N/R N/R N/R N/R


REPRODUCTIVE EFFECTS DATA AND REFERENCES:

ROUTE/
ORGANISM 		DOSE
EFFECT

 REFERENCE
intraperitoneal
mouse 		lowest published toxic dose: 50 µg/kg (13 day pregnant) Reproductive: Effects on newborn: Biochemical and metabolic

Reproductive: Effects on newborn: Behavioral 		FEPRA7 31,596,1972
intraperitoneal
rat 		lowest published toxic dose: 333 µg/kg (1 day male) Reproductive: Effects on fertility: Mating performance (e.g., # sperm positive females per # females mated; # copulations per # estrus cycles) ANENAG 24(Suppl 3),1,1963


TUMORIGENIC DATA AND REFERENCES:

ROUTE/
ORGANISM 		DOSE
EFFECT

 REFERENCE
N/R
 N/R N/R N/R


ACUTE TOXICITY DATA AND REFERENCES:

ROUTE/
ORGANISM 		DOSE
EFFECT

 REFERENCE
intramuscular
mouse 		lethal dose (50 percent kill): 330 µg/kg N/R JMCMAR 33,577,1990
intramuscular
rat 		lowest published toxic dose: 0.15 mg/kg Behavioral: Anticonvulsant EKFAE9 60,16,1997
intramuscular
rabbit 		lethal dose (50 percent kill): 2,200 µg/kg Biochemical: Enzyme inhibition, induction, or change in blood or tissue levels: True cholinesterase DCTODJ 3,319,1980
intraperitoneal
mouse 		lethal dose (50 percent kill): 644 µg/kg Behavioral: Muscle contraction or spasticity

Lung, Thorax, or Respiration: Dyspnea

Lung, Thorax, or Respiration: Cyanosis 		FATOAO 43,717,1980
intraperitoneal
mouse 		lowest published toxic dose: 3.5 mg/kg Brain and Coverings: Other degenerative changes

Biochemical: Enzyme inhibition, induction, or change in blood or tissue levels: True cholinesterase 		EKFAE9 57,13,1994
intraperitoneal
mouse 		lowest published toxic dose: 0.2 mg/kg Peripheral Nerve and Sensation: Fasciculations

Biochemical: Enzyme inhibition, induction, or change in blood or tissue levels: True cholinesterase 		FATOAO 55,13,1992
intraperitoneal
mouse 		lowest published toxic dose: 0.1 mg/kg Behavioral: Alteration of classical conditioning

Behavioral: Change in psychophysiological tests 		PSCHDL 176,66,2004
intraperitoneal
rat 		lethal dose (50 percent kill): 2 mg/kg N/R ARZNAD 22,1926,1972
intraperitoneal
rat 		lowest published toxic dose: 0.5 mg/kg Behavioral: Alteration of operant conditioning FATOAO 50,27,1987
intraperitoneal
rat 		lowest published toxic dose: 0.1 mg/kg Behavioral: Alteration of classical conditioning JOPSEQ 19,149,2005
intraperitoneal
rat 		lowest published toxic dose: 100 µg/kg Biochemical: Enzyme inhibition, induction, or change in blood or tissue levels: Hepatic microsomal mixed oxidase (dealkylation, hydroxylation, etc.) TOXID9 66,314,2002
intraperitoneal
rabbit 		lethal dose (50 percent kill): 2,470 µg/kg N/R ABMHAM (Suppl),226,1984
intravenous
cat 		lethal dose (50 percent kill): 660 µg/kg N/R JPETAB 88,39,1946
intravenous
human 		lowest published toxic dose: 5.8 µg/kg Brain and Coverings: Changes in circulation

Behavioral: Change in psychophysiological tests 		NEROEW 25,555,2001
intravenous
human 		lowest published toxic dose: 8 µg/kg Gastrointestinal: Changes in structure or function of salivary glands

Endocrine: Other changes

Blood: Changes in serum composition (e.g. TP, bilirubin, cholesterol) 		NEROEW 26,672,2002
intravenous
man 		lowest published toxic dose: 7.1 µg/kg Brain and Coverings: Changes in surface EEG

Gastrointestinal: Nausea or vomiting 		CLPTAT 67,538,2000
intravenous
man 		lowest published toxic dose: 0.7 mg/kg Brain and Coverings: Changes in surface EEG EJCPAS (),A51,1999
intravenous
mouse 		lethal dose (50 percent kill): 400 µg/kg N/R JPETAB 58,337,1936
intravenous
rabbit 		lethal dose (50 percent kill): 500 µg/kg N/R 85IXA4 -,452,1948
oral
human 		lowest published toxic dose: 20 mg/kg Behavioral: Coma

Lung, Thorax, or Respiration: Dyspnea

Gastrointestinal: Nausea or vomiting 		34ZIAG -,475,1969
oral
man 		lowest published toxic dose: 12 mg/kg/60 day- intermittent Behavioral: Muscle contraction or spasticity NEURAI 37,345,1987
oral
mouse 		lethal dose (50 percent kill): 3 mg/kg N/R 85IXA4 -,452,1948
oral
rat 		lethal dose (50 percent kill): 4,500 µg/kg N/R USXXAM #5302593
oral
rabbit 		lethal dose (50 percent kill): 11,200 µg/kg Biochemical: Enzyme inhibition, induction, or change in blood or tissue levels: True cholinesterase DCTODJ 3,319,1980
oral
woman 		lowest published toxic dose: 40 µg/kg/5 day- intermittent Vascular: BP elevation not characterized in autonomic section AJPSAO 143,910,1985
oral
woman 		lowest published toxic dose: 3,920 µg/kg/2 week- intermittent Behavioral: Muscle contraction or spasticity NEURAI 37,345,1987
parenteral
mouse 		lethal dose (50 percent kill): 600 µg/kg N/R USXXAM #5306825
subcutaneous
dog 		lowest published lethal dose: 1,138 µg/kg Behavioral: Muscle contraction or spasticity

Gastrointestinal: Changes in structure or function of salivary glands

Gastrointestinal: Ulceration or bleeding from large intestine 		FEPRA7 5,184,1946
subcutaneous
mouse 		lethal dose (50 percent kill): 740 µg/kg Peripheral Nerve and Sensation: Flaccid paralysis without anesthesia (usually neuromuscular blockage)

Behavioral: Muscle weakness 		JPETAB 123,121,1958
subcutaneous
mouse 		lethal dose (50 percent kill): 0.87 mg/kg N/R EKFAE9 57,13,1994
subcutaneous
mouse 		lowest published toxic dose: 0.28 mg/kg Behavioral: Muscle contraction or spasticity EKFAE9 57,13,1994
subcutaneous
pigeon 		lowest published lethal dose: 450 µg/kg N/R HBAMAK 4,1289,1935
subcutaneous
rat 		lowest published lethal dose: 1 mg/kg N/R USXXAM #5318967
subcutaneous
rat 		lowest published toxic dose: 0.1 mg/kg Behavioral: Tremor

Behavioral: Change in motor activity (specific assay) 		PSCHDL 158,273,2001
subcutaneous
rat 		lowest published toxic dose: 0.25 mg/kg Brain and Coverings: Other degenerative changes

Gastrointestinal: Other changes

Blood: Other changes 		TOXID9 60,245,2001
subcutaneous
rat 		lowest published toxic dose: 0.25 mg/kg Biochemical: Enzyme inhibition, induction, or change in blood or tissue levels: True cholinesterase TOXID9 60,245,2001
subcutaneous
rat 		lowest published toxic dose: 1 mg/kg Behavioral: Tremor

Behavioral: Somnolence (general depressed activity) 		FCTOD7 45,70,2007
subcutaneous
rat 		lowest published toxic dose: 1 mg/kg Gastrointestinal: Changes in structure or function of salivary glands FCTOD7 45,70,2007
subcutaneous
rat 		lowest published toxic dose: 1 mg/kg Musculoskeletal: Other changes FCTOD7 45,70,2007
subcutaneous
rat 		lowest published toxic dose: 0.1 mg/kg Brain and Coverings: Recordings from specific areas of CNS NRTXDN 29,87,2008
subcutaneous
rat 		lowest published toxic dose: 0.5 mg/kg Brain and Coverings: Other degenerative changes

Nutritional and Gross Metabolic: Body temperature decrease

Biochemical: Enzyme inhibition, induction, or change in blood or tissue levels: True cholinesterase 		NRTXDN 29,87,2008
subcutaneous
rabbit 		lethal dose (50 percent kill): 3 mg/kg N/R 85IXA4 -,452,1948
unreported route
mammal (species unspecified) 		lethal dose (50 percent kill): 600 µg/kg N/R USXXAM #5409948
unreported route
man 		lowest published lethal dose: 882 µg/kg N/R 85DCAI 2,73,1970
unreported route
mouse 		lethal dose (50 percent kill): 0.6 mg/kg N/R USXXAM #5306825


OTHER MULTIPLE DOSE DATA AND REFERENCES:

ROUTE/
ORGANISM 		DOSE
EFFECT

 REFERENCE
intraperitoneal
rat 		lowest published toxic dose: 1 mg/kg/10 day- intermittent Behavioral: Alteration of operant conditioning CYLPDN 23,477,2002
subcutaneous
rat 		lowest published toxic dose: 0.2 mg/kg/2 day- intermittent Behavioral: Tremor

Behavioral: Change in motor activity (specific assay) 		PSCHDL 158,273,2001


REVIEWS:

ORGANIZATION STANDARD
REFERENCE
TOXICOLOGY REVIEW
TPHSDY 23,426,2002
TOXICOLOGY REVIEW
ENTOX* -,588,2005
TOXICOLOGY REVIEW
HUTOX* -,301,1996


STANDARDS AND REGULATIONS:

ORGANIZATION STANDARD
REFERENCE
N/R N/R N/R


NIOSH DOCUMENTATION AND SURVEILLANCE:

ORGANIZATION STANDARD or SURVEY
REFERENCE
National Occupational Exposure Survey 1983 National Occupational Exposure Survey 1983: Hazard Code: X4159;
Number of Industries 1;
Total Number of Facilities 7;
Number of Occupations 1;
Total Number of Employees Exposed 103;
Total Number of Female Employees Exposed 52


STATUS IN FEDERAL AGENCIES:

ORGANIZATION
REFERENCE
EPA TSCA Section 8(b) CHEMICAL INVENTORY
Used as an anticholinesterase inhibitor
EPA TSCA Section 8(d) unpublished health/safety studies
EPA TSCA TEST SUBMISSION (TSCATS) DATA BASE, JANUARY 2001


REFERENCES:

CODEN
REFERENCE
34ZIAG "Toxicology of Drugs and Chemicals," Deichmann, W.B., New York, Academic Press, Inc., 1969
85DCAI "Poisoning; Toxicology, Symptoms, Treatments," 2nd ed., Arena, J.M., Springfield, IL, C.C. Thomas, 1970
85IXA4 "Structure et Activite Pharmacodyanmique des Medicaments du Systeme Nerveux Vegetatif," Bovet, D., and F. Bovet-Nitti, New York, S. Karger, 1948
ABMHAM Archives Belges de Medecine Sociale, Hygiene, Medecine du Trevail et Medecine Legale. (Quartier Esplanade no.6, 1010 Brussels, Belgium) V.4- 1946-
AJPSAO American Journal of Psychiatry. (American Psychiatric Assoc., Circulation Dept., 1400 K St., NW, Washington, DC 20005) V.78- 1921-
ANENAG Annales d'Endocrinologie. (Masson Editeur, 120 Blvd. Saint-Germain, F-25280 Paris Cedex 06, France) V.1- 1939-
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951-
CLPTAT Clinical Pharmacology and Therapeutics. (American Society for Clinical Pharmacology and Therapeutics, St. Louis Mo Mosby-Year Book) V.1- 1960-
CYLPDN Zhongguo Yaoli Xuebao. Acta Pharmacologica Sinica. Chinese Journal of Pharmacology. (China International Book Trading Corp., POB 2820, Beijing, Peop. Rep. China) V.1- 1980-
DCTODJ Drug and Chemical Toxicology. (Marcel Dekker, 270 Madison Ave., New York, NY 10016) V.1- 1977/78-
EJCPAS European Journal of Clinical Pharmacology. (Springer-Verlag New York, Inc., Service Center, 44 Hartz Way, Secaucus, NJ 07094) V.3- 1970-
EKFAE9 Eksperimental'naya i Klinicheskaya Farmakologiya. Experimental and Clinical Pharmacology. (Mezhdunarodnaya Kniga, ul. B. Yakimanka, 39, 117049 Moscow, Russia) V.55- 1992-
ENTOX* Encyclopedia of Toxicology: Reference Book, Elsevier, 2005
FATOAO Farmakologiya i Toksikologiya (Moscow). For English translation, see PHTXA6 and RPTOAN. (V/O Mezhdunarodnaya Kniga, 113095 Moscow, USSR) V.2- 1939-
FCTOD7 Food and Chemical Toxicology. (Pergamon Press Inc., Maxwell House, Fairview Park, Elmsford, NY 10523) V.20- 1982-
FEPRA7 Federation Proceedings, Federation of American Societies for Experimental Biology. (Bethesda, MD) V.1-46, 1942-87.
HBAMAK "Abdernalden's Handbuch der Biologischen Arbeitsmethoden." (Leipzig, Ger. Dem. Rep.)
HUTOX*
JMCMAR Journal of Medicinal Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB POB 57136, West End Stn., Washington, DC 20037) V.6- 1963-
JOPSEQ Journal of Psychopharmacology (Oxford). (Oxford University Press, Great Clarendon St., Oxford OX2 6DP, UK) V.1- 1987-
JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10-
NEROEW Neuropsychopharmacology. (Elsevier Science, 655 Avenue of the Americas, New York, NY 10010) V.1- 1987-
NEURAI Neurology. (Modern Medicine Pub., Inc., 1 E. First St., Duluth, MN 55802) V.1- 1951-
NRTXDN Neurotoxicology. (Intox Press, Inc., POB 34075, Little Rock, AR 72203) V.1- 1979-
PSCHDL Psychopharmacology (Berlin). (Springer-Verlag New York, Inc., Service Center, 44 Hartz Way, Secaucus, NJ 07094) V.47- 1976-
TOXID9 Toxicologist. (Soc. of Toxicology, Inc., 475 Wolf Ledge Parkway, Akron, OH 44311) V.1- 1981-
TPHSDY Trends in Pharmacological Sciences. (Elsevier Science Pub. Co., Inc., 52 Vanderbilt Ave., New York, NY 10017) V.1- 1979-
USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231)

Used as an anticholinesterase inhibitor

RTECS Compound Description:
   Agricultural Chemical
   Drug
   Reproductive Effector
   Human Data
   Natural Product

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