polythiazide (200 mg)

Names

[ CAS No. ]:
346-18-9

[ Name ]:
polythiazide (200 mg)

[Synonym ]:
Polythiazide
Polythiazidum
Politiazida
Nephril
P-2525
Renese
Drenusil

Biological Activity

[Description]:

Polythiazide is a potent and orally active thiazide diuretic agent that has antihypertensive effect. Polythiazide can decrease edema and decrease blood pressure. Polythiazide also has phototoxicity[1][2][3].

[Related Catalog]:

Research Areas >> Cardiovascular Disease

Signaling Pathways >> Others >> Others

[In Vitro]

Polythiazide (500 μM, 1 min) induces significant phototoxic NHIK 3025 cell death under Bluelight 2000 apparatus (Ex: 325 nM)[2].

[In Vivo]

Polythiazide (oral gavage, 10 mg/kg, daily for 5 days) Increased plasma cholesterol levels in Cholesterol-fed C57BL/cdJ mouse[3]. Polythiazide (Oral administration, 0.4 mg/k g) shows diuretic and saluretic effects in hypertensive dogs and rats[1]. Animal Model: Cholesterol-fed C57BL/cdJ mice[3] Dosage: 10 mg/kg Administration: Oral gavage, daily for 5 days Result: Caused approximately 13% rise in total plasma cholesterol levels, and increased non-HDL lipoprotein fraction. Animal Model: Hypertensive dogs[1] Dosage: 0.4 mg/kg Administration: Oral administration, daily for 5 days Result: Increased in excretion of sodium and chloride. Animal Model: Hypertensive rats[1] Dosage: 0.05, 0.1, 0.2, 0.4 mg/k g Administration: Oral administration, twice a day for 3 days. Result: Displayed natriuretic and chloruretic effects.

[References]

[1]. A SCRIABINE, et al. Pharmacological studies with polythiazide, a new diuretic and antihypertensive agent. Proc Soc Exp Biol Med. 1961 Aug-Sep;107:864-72.

[2]. E Selvaag, et al. Phototoxicity due to sulphonamide derived oral antidiabetics and diuretics: investigations in a cell culture model. Photodermatol Photoimmunol Photomed. 1996 Feb;12(1):1-6.

[3]. M N Krupp, et al. Effects of doxazosin and other antihypertensives on serum lipid levels and lipoprotein lipase in the C57BR/cdJ mouse. J Cardiovasc Pharmacol. 1989;13 Suppl 2:S11-8; discussion S18-9.

Chemical & Physical Properties

[ Density]:
1.598g/cm3

[ Boiling Point ]:
580.1ºC at 760mmHg

[ Melting Point ]:
202.5°

[ Molecular Formula ]:
C₁₁H₁₃ClF₃N₃O₄S₃

[ Molecular Weight ]:
439.88200

[ Flash Point ]:
304.7ºC

[ Exact Mass ]:
438.97100

[ PSA ]:
151.63000

[ LogP ]:
4.59280

[ Index of Refraction ]:
1.566

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: DK9275000

CHEMICAL NAME :: 2H-1,2,4-Benzothiadiazine-7-sulfonamide, 6-chloro-3,4-dihydro-2-methyl- 3-(((2,2,2-trifluoroethyl)thio)methyl)-, 1,1-dioxide

CAS REGISTRY NUMBER :: 346-18-9

LAST UPDATED :: 199709

DATA ITEMS CITED :: 6

MOLECULAR FORMULA :: C11-H13-Cl-F3-N3-O4-S3

MOLECULAR WEIGHT :: 439.90

WISWESSER LINE NOTATION :: T66 BSWN EM DHJ C1 D1S1XFFF HG ISZW

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 300 ug/kg/5D-I

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - coma Nutritional and Gross Metabolic - other changes

REFERENCE :: AJMEAZ American Journal of Medicine. (Technical Pub., 875 Third Ave., New York, NY 10022) V.1- 1946- Volume(issue)/page/year: 70,1163,1981

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >10 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: YAKUD5 Gekkan Yakuji. Pharmaceuticals Monthly. (Yakugyo Jihosha, Inaoka Bldg., 2-36 Jinbo-cho, Kanda, Chiyoda-ku, Tokyo 101, Japan) V.1- 1959- Volume(issue)/page/year: 21,775,1979

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 400 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: 29ZVAB "Handbook of Analytical Toxicology," Sunshine, I., ed., Cleveland, OH, Chemical Rubber Co., 1969 Volume(issue)/page/year: -,97,1969

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >5 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,793,1982

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >5 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: YAKUD5 Gekkan Yakuji. Pharmaceuticals Monthly. (Yakugyo Jihosha, Inaoka Bldg., 2-36 Jinbo-cho, Kanda, Chiyoda-ku, Tokyo 101, Japan) V.1- 1959- Volume(issue)/page/year: 21,775,1979

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 450 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: 29ZVAB "Handbook of Analytical Toxicology," Sunshine, I., ed., Cleveland, OH, Chemical Rubber Co., 1969 Volume(issue)/page/year: -,97,1969

Related Compounds

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