Testing Status of Agents at NTP
(Phenothiazine)
CAS NO. 92-84-2
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| 3-Hydroxy-phenothiazine | dog (strain n.p.) | n.p. | n.p. | n.p. | Goodwin (1976; cited by HSDB, 1996) |
| Leucophenothiazone sulfate | mouse (male), rat, hamster (Syrian golden), and gerbil (sex otherwise n.p.) | Phenothiazine (150 mg/kg body weight; 0.75 mmol/kg) was administered via gavage, as a suspension in corn oil. Urine was collected for 24 hours. | n.p. | Leucophenothiazine sulfate accounted for 64.6, 58.1, 11.7, and 55.6% of the administered phenothiazine dose in the 24-hour urine of mice, rats, hamsters, and gerbils, respectively. | Mitchell (1980) |
| Leucothionol | rabbit and dog (strains and sex n.p.) | Rabbits received 3 g (15 mmol) phenothiazine by gavage; dogs received 1.5 or 1.75 g (7.5 or 8.8 mmol) phenothiazine in gelatin capsules. Bile was obtained from rabbits and dogs 6 hours after dosing | n.p. | Leucothionol was detected in rabbit and dog bile, but it was not quantitated. | DeEds and Thomas (1941) |
| human (male) | Urine was obtained from an orchard worker who had a dermal reaction associated with spraying of phenothiazine | n.p. | Leucothionol was detected in urine, but was not quantitated. | DeEds et al. (1940) | |
| human (sex n.p.) | Bile was collected from a patient being treated with phenothiazine for a urinary tract infection. | n.p. | Leucothionol was detected in bile, but it was not quantitated | DeEds and Thomas (1941) | |
| Phenothiazine | n.p. | Phenothiazine was administered orally. The dose was not specified. | n.a. | Approximately 30-50% of the administered dose passed through the alimentary tract unchanged. | Clarke et al. (1981; cited by HS BD, 1996) |
| mouse (female Swiss white) | Phenothiazine (2 mg/kg; 0.01 mmol/kg) was administered orally in olive oil. | n.p. | Approximately 14% of the administered dose was excreted unchanged in urine and feces at 72 hours. | Coats et al. (1976) | |
| mouse (male), rat, hamster (Syrian golden), and gerbil (sex otherwise n.p.) | Phenothiazine (150 mg/kg body weight; 0.75 mmol/kg) wad administered via gavage, as a suspension in corn oil. Urine was collected for 24 hours. | n.p. | Only a small portion of the administered dose was excreted unchanged (urinary phenothiazine accounted for 0.8, 0.2, 0.5, and 0.6% of the administered dose in mice, rats, hamsters, and gerbils, respectively) | Mitchell (1980) | |
| | rabbit and dog (strains n.p.) | Rabbits received 3 g (15 mmol phenothiazine by gavage; dogs received 1.5 or 1.75 g (7.5 or 8.8 mmol) phenothiazine in gelatin capsules. Bile was obtained from rabbits and dogs 6 hours after dosing. | n.p. | Phenothiazine was detected in rabbit and dog bile, but it was not quantitated. | DeEds and Thomas (1941) |
| cattle (female Charolais-Holstein calves) | Calves were drenched with 220 mg phenothiazine/kg body weight (1 mmol/kg) and were killed 24 hours later. | n.p. | Unchanged phenothiazine accounted for ~70% of the administered dose in liver and muscle, 100% in fat and tripe, and ~30% in kidneys. | Bureau of Veterinary Medicine (1972, 1973) | |
| human (sex n.p.) | Bile was collected from a patient being treated with phenothiazine for a urinary tract infection. | n.p. | Phenothiazine was detected in bile, but was not quantitated. | DeEds and Thomas (1941) | |
| Phenothiazine-N-glucuronide | mouse (male), rat, hamster (Syrian golden), and gerbil (sex otherwise n.p.) | Phenothiazine (150 mg/kg body weight; 0.75 mmol/kg) was administered via gavage, as a suspension in corn oil. Urine was collected for 24 hours. | n.p. | Phenothiazine-N-glucuronide accounted for 29.0, 17.4, 85.3, and 28.5% of the administered phenothiazine dose in the 24 hour urine of mice, rats, hamsters, and gerbils, respectively. | Mitchell (1980) |
| Phenothiazine-5-oxide | cattle (female Charolais-Holstein calves) | Calves were drenched with 220 mg phenothiazine/kg body weight (1 mmol/kg) and were killed 24 hours later. | n.p. | Phenothiazine-5-oxide accounted for 16% of the administered dose in liver, ~30% in muscle, ~20% in kidneys, and ~90% in blood. It was not detected in fat or tripe. | Bureau of Veterinary Medicine (1972, 1973) |
| Phenothiazine sulfate | cattle (lactating Holstein-Friesian dairy cows) | Cows were given 100,000 mg phenothiazine (500 mmol/kg; route n.p.) and urine was collected during first 48 hours after dosing. | n.p. | The potassium salt of the ethereal sulfate of 3-hydroxyphenothiazine was detected in urine, but it was not quantitated. | Ellison et al. (1957) |
| n.p. | n.p. | n.p. | Metabolism of phenothiazine occurred in the gut. | Mackison (1981: cited by HSDB, 1996) | |
| Phenothiazine sulfone | mouse (female Swiss white) | Phenothiazine (2 mg/kg; 0.01 mmol/kg) was administered orally in olive oil. | n.p. | Phenothiazine sulfone accounted for 4.7% of the administered dose in urine and feces at 72 hours. | Coates et al. (1976) | Phenothiazine sulfoxide | enzymes of the proglottids (proglottids contain the reproductive organs) of the cestode Moniezia espansa ,and cytosol of intestinal epithelial cells of the nematode Ascaris suum | n.p. | see "System or Species" column. | Enzymes in these systems also metabolized phenothiazine sulfoxides to thioethers under anaerobic conditions. | Dough (1979; cited by HSDB, 1996) |
| guinea pig (adult and neonate Dunkin-Hartley) | Phenothiazine (150 mg/kg; 0.70 mmol/kg) was administered orally or s.c. | n.p. | In orally dosed adults, phenothiazine sulfoxide accounted for 1.8% of the dose in urine; trace amts. were detected in feces. In neonates and adults treated s.c., phenothiazine sulfoxide accounted for 4.0-12.5 and 6.5% of the dose, respectively, in urine; none was detected in feces. | Mitchell and Waring (1979) | |
| mouse (female Swiss white) | Phenothiazine (2 mg/kg; 0.01 mmol/kg) was administered orally in olive oil. | n.p. | Phenothiazine sulfoxide was the primary metabolite detected in urine and feces, accouting for 42-44% of the administered dose at 72 hours. | Coats et al. (1976) | |
| mouse (male), rat, hamster (Syrian golden), and gerbil (sex otherwise n.p.) | Phenothiazine (150 mg/kg body weight; 0.75 mmol/kg) was administered via gavage, as a suspension in corn oil. Urine was collected for 24 hours. | n.p. | Phenothiazine sulfoxide accounted for 1.2, 0.4, 0.8, and 0.5% of the administered phenothiazine dose in in the 24 hours urine of mice, rats, hamsters, and gerbils, respectively. | Mitchell (1980) | |
| rat (male albino) | Phenothiazine (1.5 mg/kg body weight; 0.0075 mmol/kg) was administered via gavage, in corn oil, either once or as 5 daily doses. | n.p. | Phenothiazine sulfoxide accounted for 30% (single dose) or 38% (mulitple doses) of the administered phenothiazine dose in livers of rats 4 hours after treatment. | ICI Americas (1982) | |
| Phenothiazone | mouse (male), rat, hamster (Syrian golden), and gerbil (sex otherwise n.p.) | Phenothiazine (150 mg/kg body weight; 0.75 mmol/kg) was administered via gavage, as a suspension in corn oil. Urine was collected for 24 hours. | n.p. | Phenothiazone accounted for 3.8, 1.5, 0.4, and 1.2% of the administered phenothiazine dose in the 24-hour urine of mice, rats, hamsters, and gerbils, respectively. | Mitchell (1980) |
| mouse (female Swiss white) | Phenothiazine (2 mg/kg; 0.01 mmol/kg) was administered orally in olive oil. | n.p. | Phenothiazone accounted for ~2.7% of the administered dose in urine and feces at 72 hours. | Coates et al. (1976) | |
| cattle (female Charolais-Holstein calves) | Calves were drenched with 220 mg phenothiazine/kg body weight (1 mmol/kg) and were killed 24 hours later. | n.p. | Phenothiazone accounted for <10% of the administered dose in liver and for ~15% of the adminstered dose in kidneys. Phenothiazone was not detected in muscle, fat, tripe, or blood. | Bureau of Veterinary Medicine (1972, 1973) | |
| Thionol | mouse (male), rat, hamster (Syrian golden), and gerbil (sex otherwise n.p.) | Phenothiazine (150 mg/kg body weight; 0.75 mmol/kg) was administered via gavage, as a suspension in corn oil. Urine was collected for 24 hours. | n.p. | Thionol accounted for 4.2, 4.7, 1.3, and 1.7% of the administered phenothiazine dose in the 24-hour urine of mice, rats, hamsters, and gerbils, respectively | Mitchell (1980) |
| rabbit and dog (strains not specified) | Rabbits received 3 g (15 mmol) phenothiazine by gavage; dogs received 1.5 or 1.75 g (7.5 or 8.8 mmol) phenothiazine in gelatin capsules. Bile was obtained from rabbits and dogs 6 hours after dosing | n.p. | Thionol was detected in rabbit and dog bile, but it was not quantitated. | DeEds and Thomas (1941) | |
| human (male) | Urine was obtained from an orchard worker who had a dermal reaction associated with spraying of phenothiazine | n.p. | Thionol was detected in urine, but was not quantitated. | DeEds et al. (1940) | |
| human (sex n.p.) | Bile was collected from a patient being treated with phenothiazine for a urinary tract infection. | n.p. | Thionol was detected in bile, but it was not quantitated | DeEds and Thomas (1941) | |
| Thionol glucuronide | mouse (male), rat, hamster (Syrian golden), and gerbil (sex otherwise n.p.) | Phenothiazine (150 mg/kg body weight; 0.75 mmol/kg) was administered via gavage, as a suspension in corn oil. Urine was collected for 24 hours. | n.p. | Thionol glucuronide accounted for 4.5, 17.7, and 11.9% of the administered phenothiazine dose in the 24-hour urine of mice, rats, hamsters, and gerbils, respectively | Mitchell (1980) |
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