hydroflumethiazide

Names

[ CAS No. ]:
135-09-1

[ Name ]:
hydroflumethiazide

[Synonym ]:
EINECS 205-173-8
Robezon
Spandiuril
Saluron
MFCD00057316
hydroflumethyazide
Glomerulin
hydroflumenthiazide
Diurometon
hydroflumethiazide
Flutizide
Hidroflumetiazid
Diuredemina
Hidroalogen

Biological Activity

[Description]:

Hydroflumethiazide (Methforylthiazidine) is an orally active and potent thiazide diuretic. Hydroflumethiazide possesses the ability to directly stimulate A cell secretion in the normal and alloxan diabetic pancreas[1][2][3].

[Related Catalog]:

Research Areas >> Endocrinology

Signaling Pathways >> Others >> Others

Research Areas >> Metabolic Disease

[References]

[1]. Selvaag E, et al. Phototoxicity to sulphonamide derived oral antidiabetics and diuretics. Comparative in vitro and in vivo investigations. In Vivo. 1997 Jan-Feb;11(1):103-7.

[2]. Brørs O, et al. Pharmacokinetics of a single oral dose of hydroflumethiazide in health and in cardiac failure.-. Eur J Clin Pharmacol. 1978 Nov 9;14(1):29-37.

[3]. Hermansen K, et al. Effects of a thiazide diuretic (hydroflumethiazide) and a loop diuretic (bumetanide) on the endocrine pancreas: studies in vitro. Metabolism. 1985 Aug;34(8):784-9.

Chemical & Physical Properties

[ Density]:
1.678g/cm3

[ Boiling Point ]:
531.6ºC at 760 mmHg

[ Melting Point ]:
272-273ºC

[ Molecular Formula ]:
C₈H₈F₃N₃O₄S₂

[ Molecular Weight ]:
331.29200

[ Flash Point ]:
275.3ºC

[ Exact Mass ]:
330.99100

[ PSA ]:
135.12000

[ LogP ]:
3.34280

[ Vapour Pressure ]:
2.2E-11mmHg at 25°C

[ Index of Refraction ]:
1.55

[ Storage condition ]:
Refrigerator

MSDS

Click to get detail MSDS

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: DK9625000

CHEMICAL NAME :: 2H-1,2,4-Benzothiadiazine-7-sulfonamide, 3,4-dihydro-6-(trifluoromethyl)-, 1,1-dioxide

CAS REGISTRY NUMBER :: 135-09-1

BEILSTEIN REFERENCE NO. :: 0342692

LAST UPDATED :: 199712

DATA ITEMS CITED :: 4

MOLECULAR FORMULA :: C8-H8-F3-N3-O4-S2

MOLECULAR WEIGHT :: 331.31

WISWESSER LINE NOTATION :: T66 BSWM EM DHJ HXFFF ISZW

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >10 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: 6,629,1982

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 6280 mg/kg

TOXIC EFFECTS :: Peripheral Nerve and Sensation - spastic paralysis with or without sensory change Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - other changes

REFERENCE :: JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 134,273,1961

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 750 mg/kg

TOXIC EFFECTS :: Peripheral Nerve and Sensation - spastic paralysis with or without sensory change Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - other changes

REFERENCE :: JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 134,273,1961

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

ROUTE OF EXPOSURE :: Parenteral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1182 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold

REFERENCE :: FMXXAJ French Medicament Patent Document. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Discontinued. Volume(issue)/page/year: #80M

Safety Information

[ Symbol ]:

GHS08

[ Signal Word ]:
Danger

[ Hazard Statements ]:
H317-H334

[ Precautionary Statements ]:
P261-P280-P284-P304 + P340-P342 + P311

[ Personal Protective Equipment ]:
dust mask type N95 (US);Eyeshields;Faceshields;Gloves

[ Hazard Codes ]:
Xn,Xi

[ Risk Phrases ]:
R42/43

[ Safety Phrases ]:
S36

[ RIDADR ]:
NONH for all modes of transport

[ WGK Germany ]:
2

[ RTECS ]:
DK9625000

[ HS Code ]:
2935009090

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Customs

[ HS Code ]: 2935009090

[ Summary ]:
2935009090 other sulphonamides VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:35.0%

Articles

Do thiazides reduce intestinal oxalate absorption?: a study in vitro using rabbit colon.

Clin. Sci. 86(3) , 353-7, (1994)

1. The purpose of the present study was to examine the effects of various diuretics on intestinal oxalate transport. Transmural oxalate fluxes were measured across isolated, short-circuited tissue seg...

Comparative effects of LN 5330 and diazoxide on insulin release and 86Rb+ permeability in perifused rat islets of Langerhans.

Biochem. Pharmacol. 42(4) , 787-91, (1991)

The benzothiadiazine derivative LN 5330 (chloro-7 trifluoromethyl-6 benzothiadiazine-1,2,4-dioxide-1,1) has been shown to inhibit insulin secretion and calcium uptake. The present study was carried ou...

Metabolic effects of propranolol and hydroflumethiazide treatment in Kenyans with mild to moderate essential hypertension.

East Afr. Med. J. 70(11) , 696-700, (1993)

In a prospective single-blind comparative trial, sixty newly diagnosed mild to moderate hypertensives were randomly assigned to either propranolol or hydroflumethiazide monotherapy. Baseline fasting s...