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Pilocarpine

RTECS #: TK1400000

CAS #: 92-13-7


UPDATE: May 2009 MW: 208.29 MF: C11H16N2O2


NOTE:

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

SYNONYMS:

  1. (+) - Pilocarpine
  2. (3S - cis) - 3 - Ethyldihydro - 4 - ( (1 - methyl - 1H - imidazol - 5 - yl) methyl) - 2 (3H) - furanone
  3. 2 (3H) - Furanone, 3 - ethyldihydro - 4 - ( (1 - methyl - 1H - imidazol - 5 - yl) methyl) - , (3S - cis) -
  4. Imidazole - 5 - butyric acid, alpha - ethyl - beta - (hydroxymethyl) - 1 - methyl - , gamma - lactone
  1. Ocusert P 20
  2. Pilocarpin
  3. Pilokarpol
  4. Syncarpine


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
N/R
N/R N/R N/R


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
intracerebral
rat
lowest published toxic dose: 2.22 µg/kg Behavioral: Fluid intake EJPHAZ 477,123,2003
intracerebral
rat
lowest published toxic dose: 40 µg/kg Gastrointestinal: Changes in structure or function of salivary glands BJMRDK 36,897,2003
intracerebral
rat
lowest published toxic dose: 160 µg/kg Cardiac: Change in rate

Vascular: BP elevation not characterized in autonomic section

Gastrointestinal: Changes in structure or function of salivary glands
BJMRDK 36,897,2003
intraperitoneal
mouse
lethal dose (50 percent kill): 220 mg/kg Nutritional and Gross Metabolic: Body temperature decrease AIPTAK 192,88,1971
intraperitoneal
mouse
lowest published lethal dose: 300 mg/kg Behavioral: Convulsions or effect on seizure threshold JPETAB 308,957,2004
intraperitoneal
rat
lethal dose (50 percent kill): 166 mg/kg N/R NIIRDN 6,APP-16,1982
intraperitoneal
rat
lowest published toxic dose: 10 mg/kg Endocrine: Change in gonadotropins PSEBAA 168,185,1981
intraperitoneal
rat
lowest published toxic dose: 25 mg/kg Nutritional and Gross Metabolic: Body temperature decrease FATOAO 44,40,1981
intraperitoneal
rat
lowest published toxic dose: 1 mg/kg Gastrointestinal: Changes in structure or function of salivary glands BJMRDK 36,897,2003
intraperitoneal
rat
lowest published toxic dose: 4 mg/kg Cardiac: Change in rate

Vascular: BP lowering not characterized in autonomic section

Gastrointestinal: Changes in structure or function of salivary glands
BJMRDK 36,897,2003
intraperitoneal
rat
lowest published toxic dose: 320 mg/kg Gastrointestinal: Changes in structure or function of salivary glands

Behavioral: Tremor

Behavioral: Tetany
BPBLEO 28,1408,2005
intraperitoneal
rat
lowest published lethal dose: 320 mg/kg N/R BPBLEO 28,1408,2005
intraperitoneal
rat
lowest published toxic dose: 350 mg/kg Behavioral: Convulsions or effect on seizure threshold BMECEP 11,113,2003
intravenous
mouse
lethal dose (50 percent kill): 61,900 µg/kg N/R NIIRDN 6,APP-16,1982
intravenous
mouse
lowest published toxic dose: 852 µg/kg Gastrointestinal: Changes in structure or function of salivary glands BJPCBM 145,219,2005
intravenous
rat
lethal dose (50 percent kill): 88,500 µg/kg N/R NIIRDN 6,APP-16,1982
intravenous
rat
lowest published toxic dose: 852 µg/kg Gastrointestinal: Changes in structure or function of salivary glands JPETAB 316,1137,2006
intravenous
rabbit
lowest published lethal dose: 120 mg/kg N/R HBAMAK 4,1386,1935
oral
human
lowest published toxic dose: 1.43 mg/kg Gastrointestinal: Changes in structure or function of salivary glands BJMRDK 35,105,2002
oral
mouse
lethal dose (50 percent kill): 119 mg/kg N/R NIIRDN 6,APP-16,1982
oral
rat
lethal dose (50 percent kill): 402 mg/kg N/R IYKEDH 12,1204,1981
subcutaneous
dog
lowest published toxic dose: 2 mg/kg Behavioral: Change in psychophysiological tests TOXID9 66,263,2002
subcutaneous
human
lowest published lethal dose: 143 µg/kg Behavioral: Coma

Lung, Thorax, or Respiration: Cyanosis

Vascular: BP elevation not characterized in autonomic section
CONEAT 10,8,1949
subcutaneous
mouse
lethal dose (50 percent kill): 90,900 µg/kg N/R NIIRDN 6,APP-16,1982
subcutaneous
rat
lethal dose (50 percent kill): 366 mg/kg N/R NIIRDN 6,APP-16,1982
subcutaneous
rat
lowest published toxic dose: 3 mg/kg Biochemical: Neurotransmitters or modulators (putative): Dopamine at other sites JPETAB 299,782,2001
subcutaneous
rat
lowest published toxic dose: 10 mg/kg Behavioral: Change in psychophysiological tests JPETAB 299,782,2001
subcutaneous
woman
lowest published toxic dose: 1,143 µg/kg Lung, Thorax, or Respiration: Dyspnea

Gastrointestinal: Changes in structure or function of salivary glands

Skin and Appendages: Other: Sweating
AROPAW 105,25,1987
unreported route
man
lowest published lethal dose: 1,912 µg/kg N/R 85DCAI 2,73,1970


OTHER MULTIPLE DOSE DATA AND REFERENCES:

ROUTE/
ORGANISM
DOSE
EFFECT

REFERENCE
intraperitoneal
rat
: 630 mg/kg/21 day- intermittent Olfaction: Change in sensation of smell

Behavioral: Alteration of classical conditioning
EJPHAZ 531,176,2006


REVIEWS:

ORGANIZATION STANDARD
REFERENCE

TOXICOLOGY REVIEW
MUREAV 488,151,2001
TOXICOLOGY REVIEW
TPHSDY 24,5,2003
TOXICOLOGY REVIEW
EMMUEG 43,143,2004
TOXICOLOGY REVIEW
TPHSDY 24,414,2003
TOXICOLOGY REVIEW
REPTED 25,291,2007
TOXICOLOGY REVIEW
HUTOX* -,335,1996


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: X3227;
Number of Industries 1;
Total Number of Facilities 11;
Number of Occupations 2;
Total Number of Employees Exposed 115;
Total Number of Female Employees Exposed 47


STATUS IN FEDERAL AGENCIES:

ORGANIZATION
REFERENCE

EPA TSCA Section 8(b) CHEMICAL INVENTORY


REFERENCES:

CODEN
REFERENCE

85DCAI "Poisoning; Toxicology, Symptoms, Treatments," 2nd ed., Arena, J.M., Springfield, IL, C.C. Thomas, 1970
AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898-
AROPAW Archives of Ophthalmology (Chicago). (AMA, 535 N. Dearborn St., Chicago, IL 60610) New series: V.1-44(3), 1929-50; V.64- 1960-
BJMRDK Brazilian Journal of Medical and Biological Research. (Associacao Brasileira de Divulgacao Cientifica, Faculdade de Medicina de Ribeirao Preto, USP, 141000 Ribeirao Preto, SP, Brazil) V.14- 1981-
BJPCBM British Journal of Pharmacology. (Macmillan Press Ltd., Houndmills, Basingstoke, Hants. RG21 2XS, UK) V.34- 1968-
BMECEP Biorganic & Medicinal Chemistry. (Elsevier Science, The Boulevard, Langford Lane, Kidlington, Oxford OX5 1GB, UK) V.1 1993-
BPBLEO Biological and Pharmaceutical Bulletin. (Pharmaceutical Society of Japan, 2-12-15-201 Shibuya Shibuya-ku, Tokyo 150, Japan) V.16- 1993-
CONEAT Confinia Neurologica. (Basel, Switzerland) V.1-37, 1938-75.
EJPHAZ European Journal of Pharmacology. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1967-
EMMUEG Environmental and Molecular Mutagenesis. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.10- 1987-
FATOAO Farmakologiya i Toksikologiya (Moscow). For English translation, see PHTXA6 and RPTOAN. (V/O Mezhdunarodnaya Kniga, 113095 Moscow, USSR) V.2- 1939-
HBAMAK "Abdernalden's Handbuch der Biologischen Arbeitsmethoden." (Leipzig, Ger. Dem. Rep.)
HUTOX*
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970-
JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10-
MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964-
NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan)
PSEBAA Proceedings of the Society for Experimental Biology and Medicine. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1903/04-
REPTED Reproductive Toxicology. (Pergamon Press Inc., Maxwell House, Fairview Park, Elmsford, NY 10523) V.1- 1987-
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-

FDA-proprietary drug

RTECS Compound Description:
   Drug
   Human Data
   Natural Product

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