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Toxicity Effects

CAS Registry Number: 968-81-0

Selected toxicity information from HSDB, one of the National Library of Medicine's databases. 2.

Names 1

  • 4-Acetyl-N-((Cyclohexylamino)Carbonyl)Benzenesulfonamide
  • Acetohexamide
  • Dymelor

Human Toxicity Excerpts

  • Coma or altered mental status is generally the most important presenting sign in the majority (90%) of patients who have ingested excessive doses of the sulfonylureas ... /Sulfonylurea/[Ellenhorn, M.J., S. Schonwald, G. Ordog, J. Wasserberger. Ellenhorn's Medical Toxicology: Diagnosis and Treatment of Human Poisoning. 2nd ed. Baltimore, MD: Williams and Wilkins, 1997., p. 723] **PEER REVIEWED**
  • HYPOGLYCEMIC REACTIONS, INCL COMA, MAY OCCUR. WHILE THEY ARE USUALLY NOT SEVERE, SEVERAL FATALITIES HAVE BEEN REPORTED.[Goodman, L.S., and A. Gilman. (eds.) The Pharmacological Basis of Therapeutics. 5th ed. New York: Macmillan Publishing Co., Inc., 1975., p. 1521] **PEER REVIEWED**

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Non-Human Toxicity Excerpts

  • ACETOHEXAMIDE STIMULATED ENZYMES IN LIVER HOMOGENATES OF NORMAL & ALLOXAN-DIABETIC RATS. APPARENTLY DRUG INTERFERES WITH HEPATIC PROTEIN BIOSYNTHESIS & GLUCONEOGENESIS. ORAL.[ABDEL-KHALEK A ET AL; J EGYPT MED ASSOC 61(1-2) 11 (1978)] **PEER REVIEWED**
  • BIOASSAY CONDUCTED BY ADMINISTERING TEST CHEMICAL IN FEED TO FISCHER 344 RATS & B6C3F1 MICE FOR 103 WK. APPARENTLY ACETOHEXAMIDE WAS NOT CARCINOGENIC FOR EITHER SPECIES.[BIOASSAY OF ACETOHEXAMIDE FOR POSSIBLE CARCINOGENICITY; REPORT DHEW/PUB/NIH-78-850, NCI-CG-TR-50, PB-284673 (1977)] **PEER REVIEWED**
  • SULFONYLUREAS FOUND TERATOGENIC IN ANIMALS. /FROM TABLE, SULFONYLUREAS/[Casarett, L.J., and J. Doull. Toxicology: The Basic Science of Poisons. New York: MacMillan Publishing Co., 1975., p. 322] **PEER REVIEWED**

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Human Toxicity Values

  • None found

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Non-Human Toxicity Values

  • None found

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Absorption, Distribution And Excretion

  • ...5 DAYS AFTER ORAL DOSE...TO RATS. 86% WAS EXCRETED IN 24-HR URINE & 9% IN 48-HR FECES. RESULTS INDICATED RAPID ABSORPTION & EXCRETION...[The Chemical Society. Foreign Compound Metabolism in Mammals. Volume 1: A Review of the Literature Published Between 1960 and 1969. London: The Chemical Society, 1970., p. 64] **PEER REVIEWED**
  • ACETOHEXAMIDE IS RAPIDLY ABSORBED, & MAX HYPOGLYCEMIC ACTIVITY IS OBSERVED ABOUT 3 HR AFTER INGESTION. TOTAL DURATION OF ACTION IS 12-24 HR. MUCH OF ACTIVITY IS ASCRIBABLE TO METABOLITE, HYDROXYHEXAMIDE, WHICH HAS PLASMA T/2 OF ABOUT 6 HR...ACETOHEXAMIDE, HAS PLASMA T/2 OF 1.3 HR.[Goodman, L.S., and A. Gilman. (eds.) The Pharmacological Basis of Therapeutics. 5th ed. New York: Macmillan Publishing Co., Inc., 1975., p. 1521] **PEER REVIEWED**
  • AFTER ADMIN OF ACETOHEXAMIDE (30 MG/KG, IV) TO DOGS, MAX PLASMA CONCN OF ACTIVE METABOLITE HYDROXYHEXAMIDE WAS REDUCED IN 3 HR & STABLE SEVERAL HR. ACETOHEXAMIDE PLASMA LEVEL DECR LINEARLY. PLASMA PROTEIN BINDING WAS 80% FOR ACETOHEXAMIDE & 63% FOR HYDROXYHEXAMIDE.[RAYMOND Y; ANN PHARM FR 36(11-12) 593 (1978)] **PEER REVIEWED**
  • AFTER ADMIN OF ACETOHEXAMIDE (30 MG/KG, IV) TO DOGS, RENAL CLEARANCE OF METABOLITE HYDROXYHEXAMIDE WAS DOUBLED BY CHANGING URINARY PH FROM ACIDIC TO ALKALINE.[RAYMOND Y; ANN PHARM FR 36(11-12) 593 (1978)] **PEER REVIEWED**
  • Excreted (percentage)...60 /from table/[Ellenhorn, M.J., S. Schonwald, G. Ordog, J. Wasserberger. Ellenhorn's Medical Toxicology: Diagnosis and Treatment of Human Poisoning. 2nd ed. Baltimore, MD: Williams and Wilkins, 1997., p. 722] **PEER REVIEWED**
  • IN PERSONS WITH NORMAL RENAL & HEPATIC FUNCTION, MORE THAN 80% IS EXCRETED, LARGELY AS METABOLITES, IN 24 HR.[Goodman, L.S., and A. Gilman. (eds.) The Pharmacological Basis of Therapeutics. 5th ed. New York: Macmillan Publishing Co., Inc., 1975., p. 1521] **PEER REVIEWED**
  • TIME OF PEAK CONCN AFTER ORAL DOSE: 3 HR /FROM TABLE/[Miller, R. R., and D. J. Greenblatt. Handbook of Drug Therapy. New York: Elsevier North Holland, 1979., p. 688] **PEER REVIEWED**
  • When administered near term, acetohexamide crosses the placenta and may persist in the neonatal serum for several days.[Briggs, G.G, R.K. Freeman, S.J. Yaffe. A Reference Guide to Fetal and Neonatal Risk. Drugs in Pregnancy and Lactation. 4th ed. Baltimore, MD: Williams & Wilkins 1994., p. 8] **PEER REVIEWED**

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Metabolism/Metabolites

  • Active metabolite greater than parent drug. Metabolite excreted, in part, by kidney. /from table/[Young, L.Y., M.A. Koda-Kimble (eds.). Applied Therapeutics. The Clinical Use of Drugs. 6th ed. Vancouver, WA., Applied Therapeutics, Inc. 1995., p. 48-37] **PEER REVIEWED**
  • HYDROXYHEXAMIDE...MAJOR METABOLITE OF ACETOHEXAMIDE...IN HUMANS, HAS L-CONFIGURATION. ...CONTRIBUTES SIGNIFICANTLY TO HYPOGLYCEMIC RESPONSE THAT FOLLOWS ADMIN...[The Chemical Society. Foreign Compound Metabolism in Mammals. Volume 1: A Review of the Literature Published Between 1960 and 1969. London: The Chemical Society, 1970., p. 221] **PEER REVIEWED**
  • PRINCIPAL ROUTE OF METABOLIC DEGRADATION IN MAN...REDUCTION OF P-ACETYL GROUP TO /1-[(P-ALPHA-HYDROXYETHYLBENZENE)SULFONYL]-3-CYCLOHEXYLUREA WHICH/ EXHIBITS HYPOGLYCEMIA IN MAN & OTHER ANIMALS. &...MAY PROLONG HYPOGLYCEMIC ACTIVITY OF ACETOHEXAMIDE /ORAL/[American Society of Hospital Pharmacists. Data supplied on contract from American Hospital Formulary Service and other current ASHP sources., p. 1964] **PEER REVIEWED**
  • Sulfonylureas are rapidly absorbed from the gastrointestinal tract, transported in the blood in highly protein-bound complexes, and subjected to extensive hepatic metabolism (except for chlorpropamide). Wide variation exists among the sulfonylureas in hepatic metabolism and remnal clearance, factors that tend to alter the steady-state serum levels. Metabolites may be active, so there may be a variation between the plasma half-life of the parent drug and the degree of hypoglycemia encountered. /Sulfonylurea/[Ellenhorn, M.J., S. Schonwald, G. Ordog, J. Wasserberger. Ellenhorn's Medical Toxicology: Diagnosis and Treatment of Human Poisoning. 2nd ed. Baltimore, MD: Williams and Wilkins, 1997., p. 722] **PEER REVIEWED**

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Tsca Test Submissions

  • None found

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Footnotes

1 Source: the NTP's CEBS database.

2 Source: the National Library of Medicine's Hazardous Substance Database, 02/28/2017.

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