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Toxicity Effects

CAS Registry Number: 389-08-2

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

Names 1

  • 1-Ethyl-1,4-Dihydro-7-Methyl-4-Oxo-1,8-Naphthyridine-3-Carboxylic Acid (9ci)
  • Nalidixic acid

Human Toxicity Excerpts

  • Acute toxicity from nalidixic acid may be manifested by toxic psychoses, convulsions, increased intracranial pressure, or metabolic acidosis. Vomiting, nausea, and lethargy may also occur. Because of the rapid excretion of nalidixic acid, such reactions are usually short-lived, persisting only 2-3 hours.[McEvoy, G.K. (ed.). American Hospital Formulary Service - Drug Information 97. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 1997 (Plus Supplements)., p. 594] **PEER REVIEWED**
  • Human systemic effects: convulsions, hyperglycemia, sweating, and blood changes in children.[Lewis, R.J. Sax's Dangerous Properties of Industrial Materials. 9th ed. Volumes 1-3. New York, NY: Van Nostrand Reinhold, 1996., p. 1536] **PEER REVIEWED**

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Non-Human Toxicity Excerpts

  • ...prolonged use of the drug /in dogs and cats/ has caused retinal degeneration leading to blindness in some cases.[McEvoy, G.K. (ed.). American Hospital Formulary Service - Drug Information 97. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 1997 (Plus Supplements)., p. 593] **PEER REVIEWED**
  • Nalidixic acid causes lameness in immature dogs due to permanent damage of the cartilage of weight-bearing joints.[USP Convention. USPDI - Drug Information for the Health Care Professional. 17th ed. Volume I. Rockville, MD: Convention, Inc., 1997. (Plus Updates)., p. 2092] **PEER REVIEWED**

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Human Toxicity Values

  • None found

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Non-Human Toxicity Values

  • LD50 MOUSE INTRAVENOUS 0.176 G/KG[The Merck Index. 9th ed. Rahway, New Jersey: Merck & Co., Inc., 1976., p. 826] **PEER REVIEWED**
  • LD50 MOUSE ORAL 3.3 G/KG[The Merck Index. 9th ed. Rahway, New Jersey: Merck & Co., Inc., 1976., p. 826] **PEER REVIEWED**
  • LD50 MOUSE SUBCUTANEOUS 0.5 G/KG[The Merck Index. 9th ed. Rahway, New Jersey: Merck & Co., Inc., 1976., p. 826] **PEER REVIEWED**
  • LD50 Rat oral 1160 mg/kg[Lewis, R.J. Sax's Dangerous Properties of Industrial Materials. 9th ed. Volumes 1-3. New York, NY: Van Nostrand Reinhold, 1996., p. 1536] **PEER REVIEWED**

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Absorption, Distribution And Excretion

  • ...rapidly absorbed from the GI tract, with essentially the entire dose being absorbed.[McEvoy, G.K. (ed.). American Hospital Formulary Service - Drug Information 97. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 1997 (Plus Supplements)., p. 593] **PEER REVIEWED**
  • ABSORPTION & ELIMINATION RATES OF NALIDIXIC ACID WERE SHOWN TO BE LOW IN NEWBORN CHILDREN COMPARED WITH ADULTS, & ADULT VALUES WERE NOT OBTAINED UNTIL ABOUT THIRD YR OF LIFE. RELATIVE DISTRIBUTION VOL, HOWEVER, WERE SIMILAR IN BOTH AGE GROUPS.[The Chemical Society. Foreign Compound Metabolism in Mammals. Volume 2: A Review of the Literature Published Between 1970 and 1971. London: The Chemical Society, 1972., p. 437] **PEER REVIEWED**
  • ABSORPTION EFFICIENCY & RATE OF ELIMINATION OF...NALIDIXIC ACID...DECR IN PT WITH SHIGELLOSIS. POOR ABSORPTION WAS GENERALLY OBSERVED IN YOUNGER PT WITH MARKED DIARRHEA BUT THERE WAS NO READY EXPLANATION FOR DELAYED EXCRETION.[The Chemical Society. Foreign Compound Metabolism in Mammals Volume 3. London: The Chemical Society, 1975., p. 169] **PEER REVIEWED**
  • Elimination: Renal - 2 to 3% excreted unchanged. 13% as active metabolite and more than 80% as inactive metabolites; rapidly and almost completely excreted within 24 hours; active drug does not accumulate in patients with impaired renal function, but inactive metabolites accumulate and may be toxic. Fecal - Approximately 4%.[USP Convention. USPDI - Drug Information for the Health Care Professional. 17th ed. Volume I. Rockville, MD: Convention, Inc., 1997. (Plus Updates)., p. 2092] **PEER REVIEWED**
  • IN RATS & MICE ORAL DOSES ARE RAPIDLY ABSORBED WITH PEAK BLOOD CONCN ABOUT 1 HR LATER. ...ELIMINATION IS VIA KIDNEYS, PEAKING @ ABOUT 6TH HR. 80% OF ADMIN DOSE IS ELIMINATED IN 1ST 8 HR. IN DOGS HIGHLY EFFECTIVE CONCN APPEAR IN URINE WITHIN 2-3 HR AFTER ORAL ADMIN.[Rossoff, I.S. Handbook of Veterinary Drugs. New York: Springer Publishing Company, 1974., p. 375] **PEER REVIEWED**
  • Parent drug and active metabolite are distributed to most tissues, especially to the kidneys and to urine; serum concentrations are low; traces of drug cross the placenta. Excreted in breast milk. Drug does not penetrate into prostatic fluid.[USP Convention. USPDI - Drug Information for the Health Care Professional. 17th ed. Volume I. Rockville, MD: Convention, Inc., 1997. (Plus Updates)., p. 2092] **PEER REVIEWED**
  • Rapidly and almost completely absorbed from the gastrointestinal tract; bioavailability is approximately 96%. Absorption may be delayed if taken with antacids.[USP Convention. USPDI - Drug Information for the Health Care Professional. 17th ed. Volume I. Rockville, MD: Convention, Inc., 1997. (Plus Updates)., p. 2092] **PEER REVIEWED**

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Metabolism/Metabolites

  • Nalidixic acid is partially metabolized in the liver to hydroxynalidixic acid and the glucuronic acid conjugates of nalidixic acid and hydroxynalidixic acid. The drug is also partially metabolized to the dicarboxylic acid derivative; there is some evidence suggesting that this metabolite is formed in the kidney.[McEvoy, G.K. (ed.). American Hospital Formulary Service - Drug Information 97. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 1997 (Plus Supplements)., p. 593] **PEER REVIEWED**
  • WHEN NALIDIXIC ACID...IS INGESTED BY MAN, IT IS PARTLY EXCRETED AS FREE... /ACID/ BUT MUCH BIGGER PROPORTION IS EXCRETED AS MONOGLUCURONIDE...& CONSIDERABLE FRACTION AS 7-HYDROXYMETHYL METABOLITE...TOGETHER WITH SMALLER AMT OF LATTER IN CONJUGATED FORM. 3,7-DICARBOXYLIC ACID...IS MINOR METABOLITE.[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. 205] **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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