*** CHEMICAL IDENTIFICATION ***
RTECS NUMBER : RN6960000
CHEMICAL NAME : 1-Oxa-6-azacyclopentadecan-15-one,
13-((2,6-dideoxy-3-C-methyl-3-O-methyl-alpha-L-ribo-
hexopyranosyl)oxy)-2-ethyl-3,4,10-trihydroxy-3,5,6,8,
10,12,14-heptamethyl- 11-
((3,4,6-trideoxy-3-(dimethylamino)-beta-D-xylo-hexopy
ranosyl)oxy)-,
(2R-(2R*,3S*,4R*,5R*,8R*,10R*,11R*,12S*,13S*,14R*))-
CAS REGISTRY NUMBER : 83905-01-5
BEILSTEIN REFERENCE NO. : 5387583
LAST UPDATED : 199806
DATA ITEMS CITED : 10
MOLECULAR FORMULA : C38-H72-N2-O12
MOLECULAR WEIGHT : 749.12
COMPOUND DESCRIPTOR : Drug
Reproductive Effector
Human
SYNONYMS/TRADE NAMES :
* Azithromycin
* CP 62993
* XZ 405
*** HEALTH HAZARD DATA ***
** ACUTE TOXICITY DATA **
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Human - man
DOSE/DURATION : 32 mg/kg/9D-I
TOXIC EFFECTS :
Kidney, Ureter, Bladder - changes in tubules (including acute renal failure,
acute tubular necrosis)
Kidney, Ureter, Bladder - changes in both tubules and glomeruli
Kidney, Ureter, Bladder - hematuria
REFERENCE :
AIMEAS Annals of Internal Medicine. (American College of Physicians, 4200
Pine St., Philadelphia, PA 19104) V.1- 1927- Volume(issue)/page/year:
119,636,1993
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Human - man
DOSE/DURATION : 21 mg/kg/3D-I
TOXIC EFFECTS :
Liver - jaundice, cholestatic
Kidney, Ureter, Bladder - other changes in urine composition
Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol)
REFERENCE :
AJMEAZ American Journal of Medicine. (Technical Pub., 875 Third Ave., New
York, NY 10022) V.1- 1946- Volume(issue)/page/year: 102,217,1997
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : >2 gm/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity)
Lungs, Thorax, or Respiration - respiratory depression
Gastrointestinal - nausea or vomiting
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 51,53,1996
TYPE OF TEST : LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE : Intraperitoneal
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 900 mg/kg
TOXIC EFFECTS :
Behavioral - ataxia
Lungs, Thorax, or Respiration - respiratory depression
Gastrointestinal - nausea or vomiting
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 51,53,1996
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 3 gm/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold
Lungs, Thorax, or Respiration - respiratory depression
Gastrointestinal - nausea or vomiting
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 51,53,1996
TYPE OF TEST : LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE : Intraperitoneal
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 400 mg/kg
TOXIC EFFECTS :
Behavioral - ataxia
Lungs, Thorax, or Respiration - respiratory depression
Gastrointestinal - nausea or vomiting
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 51,53,1996
** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 3600 mg/kg/36D-I
TOXIC EFFECTS :
Liver - other changes
Biochemical - Enzyme inhibition, induction, or change in blood or tissue
levels - dehydrogenases
Biochemical - Enzyme inhibition, induction, or change in blood or tissue
levels - transaminases
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 51,53,1996
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Mammal - dog
DOSE/DURATION : 3600 mg/kg/36D-I
TOXIC EFFECTS :
Liver - change in gall bladder structure or function
Liver - changes in liver weight
Endocrine - other changes
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 51,65,1996
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Mammal - dog
DOSE/DURATION : 6100 mg/kg/61D-I
TOXIC EFFECTS :
Kidney, Ureter, Bladder - changes in both tubules and glomeruli
Liver - other changes
Nutritional and Gross Metabolic - weight loss or decreased weight gain
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 51,65,1996
** REPRODUCTIVE DATA **
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE : 1350 mg/kg
SEX/DURATION : female 15-21 day(s) after conception
lactating female 20 day(s) post-birth
TOXIC EFFECTS :
Reproductive - Effects on Newborn - physical
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 51,85,1996
*** END OF RECORD ***