RTECS:UY5770000 The Registry of Toxic Effects of Chemical Substances

2 - Pyrrolidinone, 1 - ethyl - 4 - (2 - morpholinoethyl) - 3,3 - diphenyl - , monohydrochloride, monohydrate

RTECS #: UY5770000

CAS #: 7081-53-0

UPDATE: March 1996 MW: 433.04 MF: C₂₄H₃₀N₂O₂•ClH•H₂O

NOTE:

TOXICITY DATA HAVE NOT BEEN EVALUATED. OMISSION OF A SUBSTANCE OR NOTATION DOES NOT IMPLY ANY RELIEF FROM REGULATORY RESPONSIBILITY.

TABLE OF CONTENTS:

SYNONYMS:

REPRODUCTIVE EFFECTS DATA:

ACUTE TOXICITY DATA:

OTHER MULTIPLE DOSE DATA:

NIOSH DOCUMENTATION AND SURVEILLANCE:

REFERENCES:

SYNONYMS:

1 - Ethyl - 4 - (2 - morpholinoethyl) - 3,3 - diphenyl - 2 - pyrrolidinone hydrochloride hydrate

AHR - 619

Doxapram hydrochloride monohydrate

Doxapram hydrochloride hydrate

Stimulexin

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: 864 mg/kg (7-12 day pregnant) Reproductive: Effects on fertility: Post- implantation mortality (e.g., dead and/or resorbed implants per total number of implants)

Reproductive: Effects on fertility: Litter size (e.g., # fetuses per litter; measured before birth)

Reproductive: Effects on embryo or fetus: Fetotoxicity (except death, e.g., stunted fetus) OYYAA2 8,229,1974
intraperitoneal
mouse lowest published toxic dose: 864 mg/kg (7-12 day pregnant) Reproductive: Specific developmental abnormalities: Musculoskeletal system OYYAA2 8,229,1974

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
intraperitoneal
mouse lethal dose (50 percent kill): 153 mg/kg Behavioral: Convulsions or effect on seizure threshold

Behavioral: Excitement

Lung, Thorax, or Respiration: Respiratory stimulation TXAPA9 13,242,1968
intraperitoneal
rat lethal dose (50 percent kill): 174 mg/kg Behavioral: Convulsions or effect on seizure threshold

Behavioral: Excitement

Lung, Thorax, or Respiration: Respiratory stimulation TXAPA9 13,242,1968
intravenous
dog lethal dose (50 percent kill): 40 mg/kg N/R TXAPA9 18,185,1971
intravenous
man lowest published toxic dose: 41 mg/kg/24 hour- continuous Liver: Hepatitis (hepatocellular necrosis), diffuse PGMJAO 61,833,1985
intravenous
mouse lethal dose (50 percent kill): 85 mg/kg Behavioral: Convulsions or effect on seizure threshold

Behavioral: Excitement

Lung, Thorax, or Respiration: Respiratory stimulation TXAPA9 13,242,1968
intravenous
rat lethal dose (50 percent kill): 72 mg/kg Behavioral: Convulsions or effect on seizure threshold

Behavioral: Excitement

Lung, Thorax, or Respiration: Respiratory stimulation TXAPA9 13,242,1968
oral
dog lethal dose (50 percent kill): 150 mg/kg N/R 27ZQAG -,225,1972
oral
mouse lethal dose (50 percent kill): 270 mg/kg Behavioral: Convulsions or effect on seizure threshold

Behavioral: Excitement

Lung, Thorax, or Respiration: Respiratory stimulation TXAPA9 13,242,1968
oral
rat lethal dose (50 percent kill): 261 mg/kg N/R TXAPA9 18,185,1971
subcutaneous
mouse lethal dose (50 percent kill): 312 mg/kg N/R NIIRDN 6,504,1982
subcutaneous
rat lethal dose (50 percent kill): 312 mg/kg Behavioral: Convulsions or effect on seizure threshold

Behavioral: Excitement

Lung, Thorax, or Respiration: Respiratory stimulation TXAPA9 13,242,1968

OTHER MULTIPLE DOSE DATA AND REFERENCES:
ROUTE/
ORGANISM DOSE
EFFECT

REFERENCE
intraperitoneal
rat lowest published toxic dose: 4,050 mg/kg/5 week- intermittent Behavioral: Food intake (animal)

Behavioral: Muscle weakness OYYAA2 8,1365,1974
intraperitoneal
rat lowest published toxic dose: 14,040 mg/kg/26 week- intermittent Behavioral: Muscle weakness

Blood: Normocytic anemia OYYAA2 8,1381,1974

REVIEWS:
ORGANIZATION STANDARD
REFERENCE

N/R N/R N/R

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: X5346;
Number of Industries 1;
Total Number of Facilities 35;
Number of Occupations 2;
Total Number of Employees Exposed 644;
Total Number of Female Employees Exposed 433

STATUS IN FEDERAL AGENCIES:
ORGANIZATION
REFERENCE

N/R

REFERENCES:
CODEN
REFERENCE

27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972
NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan)
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967-
PGMJAO Postgraduate Medical Journal. (Blackwell Scientific Pub. Ltd., POB 88, Oxford, UK) V.1- 1925-
TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959-

Used as a respiratory stimulant

FDA-proprietary drug

RTECS Compound Description:
   Drug
   Reproductive Effector
   Human Data

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SYNONYMS:
1 - Ethyl - 4 - (2 - morpholinoethyl) - 3,3 - diphenyl - 2 - pyrrolidinone hydrochloride hydrate AHR - 619 Doxapram hydrochloride monohydrate	Doxapram hydrochloride hydrate Stimulexin

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: 864 mg/kg (7-12 day pregnant)	Reproductive: Effects on fertility: Post- implantation mortality (e.g., dead and/or resorbed implants per total number of implants) Reproductive: Effects on fertility: Litter size (e.g., # fetuses per litter; measured before birth) Reproductive: Effects on embryo or fetus: Fetotoxicity (except death, e.g., stunted fetus)	OYYAA2 8,229,1974
intraperitoneal mouse	lowest published toxic dose: 864 mg/kg (7-12 day pregnant)	Reproductive: Specific developmental abnormalities: Musculoskeletal system	OYYAA2 8,229,1974

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
intraperitoneal mouse	lethal dose (50 percent kill): 153 mg/kg	Behavioral: Convulsions or effect on seizure threshold Behavioral: Excitement Lung, Thorax, or Respiration: Respiratory stimulation	TXAPA9 13,242,1968
intraperitoneal rat	lethal dose (50 percent kill): 174 mg/kg	Behavioral: Convulsions or effect on seizure threshold Behavioral: Excitement Lung, Thorax, or Respiration: Respiratory stimulation	TXAPA9 13,242,1968
intravenous dog	lethal dose (50 percent kill): 40 mg/kg	N/R	TXAPA9 18,185,1971
intravenous man	lowest published toxic dose: 41 mg/kg/24 hour- continuous	Liver: Hepatitis (hepatocellular necrosis), diffuse	PGMJAO 61,833,1985
intravenous mouse	lethal dose (50 percent kill): 85 mg/kg	Behavioral: Convulsions or effect on seizure threshold Behavioral: Excitement Lung, Thorax, or Respiration: Respiratory stimulation	TXAPA9 13,242,1968
intravenous rat	lethal dose (50 percent kill): 72 mg/kg	Behavioral: Convulsions or effect on seizure threshold Behavioral: Excitement Lung, Thorax, or Respiration: Respiratory stimulation	TXAPA9 13,242,1968
oral dog	lethal dose (50 percent kill): 150 mg/kg	N/R	27ZQAG -,225,1972
oral mouse	lethal dose (50 percent kill): 270 mg/kg	Behavioral: Convulsions or effect on seizure threshold Behavioral: Excitement Lung, Thorax, or Respiration: Respiratory stimulation	TXAPA9 13,242,1968
oral rat	lethal dose (50 percent kill): 261 mg/kg	N/R	TXAPA9 18,185,1971
subcutaneous mouse	lethal dose (50 percent kill): 312 mg/kg	N/R	NIIRDN 6,504,1982
subcutaneous rat	lethal dose (50 percent kill): 312 mg/kg	Behavioral: Convulsions or effect on seizure threshold Behavioral: Excitement Lung, Thorax, or Respiration: Respiratory stimulation	TXAPA9 13,242,1968

OTHER MULTIPLE DOSE DATA AND REFERENCES:
ROUTE/ ORGANISM	DOSE	EFFECT	REFERENCE
intraperitoneal rat	lowest published toxic dose: 4,050 mg/kg/5 week- intermittent	Behavioral: Food intake (animal) Behavioral: Muscle weakness	OYYAA2 8,1365,1974
intraperitoneal rat	lowest published toxic dose: 14,040 mg/kg/26 week- intermittent	Behavioral: Muscle weakness Blood: Normocytic anemia	OYYAA2 8,1381,1974

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: X5346; Number of Industries 1; Total Number of Facilities 35; Number of Occupations 2; Total Number of Employees Exposed 644; Total Number of Female Employees Exposed 433

REFERENCES:
CODEN	REFERENCE
27ZQAG	"Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972
NIIRDN	Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan)
OYYAA2	Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967-
PGMJAO	Postgraduate Medical Journal. (Blackwell Scientific Pub. Ltd., POB 88, Oxford, UK) V.1- 1925-
TXAPA9	Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959-