Flumethiazide

329.278

329.28

205-717-4

3PA0CDS0M5

44626

DTXSID60163862

CRYSTALS

2935009090

135.45000

2.93080

1.6578 (estimate)

305.4-307.8 °C (decomp)

560.0±60.0 °C(Predicted)

1.673

1.05g/L(room temperature)

UNSTABLE IN ALKALINE SOLN, CONVERSION TO PRECURSOR ALPHA,ALPHA,ALPHA-TRIFLUORO-3-AMINO-4,6-DISULFAMOYLTOLUENE; DECOMP @ 305.4-307.8 °C

TUBULAR TRANSPORT OF THIAZIDES MAY BE INHIBITED BY PROBENECID. /BENZOTHIADIAZIDES/|USE OF ENTERIC-COATED COMBINATIONS OF POTASSIUM CHLORIDE & THIAZIDE HAS BEEN ASSOC WITH HIGH INCIDENCE OF ULCERATION OF DISTAL JEJUNUM OR ILEUM. IT IS PREFERABLE TO PRESCRIBE PALATABLE SOLN OF POTASSIUM CHLORIDE... /BENZOTHIADIAZIDES/|...THIAZIDE DIURETICS HAVE BEEN PRESCRIBED IN COMBINATION WITH ALDOSTERONE ANTAGONIST OR OTHER POTASSIUM-SPARING DIURETIC IN ORDER TO OBTAIN ADDITIVE DIURETIC EFFECT WITH MAINTENANCE OF POTASSIUM BALANCE. /BENZOTHIADIAZIDES/

...AVAILABLE AS TABLETS FOR ORAL ADMIN. ...GIVEN IN DIVIDED DAILY DOSES FOR TREATMENT OF HYPERTENSION, BUT SINGLE DAILY DOSE MAY BE PREFERABLE FOR MOBILIZATION OF EDEMA FLUID. ... LESS COMMON USAGES...INCL TREATMENT OF DIABETES INSIPIDUS & MGMNT OF HYPERCALCIURIA IN PT WITH...URINARY CALCULI... /BENZOTHIADIAZIDES/|THIAZIDES HAVE THEIR GREATEST USEFULNESS AS DIURETICS IN MGMNT OF EDEMA OF CHRONIC CARDIAC DECOMPENSATION. EDEMA DUE TO CHRONIC HEPATIC OR RENAL DISEASE ALSO RESPONDS FAVORABLY. WHEN EMPLOYED IN HYPERTENSIVE DISEASE, WITH OR WITHOUT OVERT EDEMA, THESE AGENTS HAVE HYPOTENSIVE ACTION... /BENZOTHIADIAZIDES/

PLASMA POTASSIUM CONCN SHOULD BE DETERMINED PERIODICALLY IN PT WHO RECEIVE THIAZIDE DIURETICS FOR EXTENDED PERIODS. ...TO AVOID NEGATIVE POTASSIUM BALANCE, THIAZIDES ARE OFTEN PRESCRIBED IN COMBINATION WITH POTASSIUM CHLORIDE. /BENZOTHIADIAZIDES/|WHEN CARDIAC DECOMPENSATION OR HYPERTENSION IS ACCOMPANIED BY SIGNIFICANT IMPAIRMENT OF RENAL FUNCTION, THIAZIDES SHOULD BE ADMIN WITH CAUTION BECAUSE OF THEIR CAPACITY TO AGGRAVATE RENAL INSUFFICIENCY.

THIAZIDES ARE ABSORBED FROM GASTROINTESTINAL TRACT & OWE THEIR USEFULNESS LARGELY TO THEIR EFFECTIVENESS BY ORAL ROUTE. ABSORPTION IS RELATIVELY RAPID. ... DRUG PASSES READILY THROUGH PLACENTAL BARRIER TO FETUS. ... MOST COMPD ARE RAPIDLY EXCRETED WITHIN 3-6 HR. /BENZOTHIADIAZIDES/

INHIBITION OF CARBONIC ANHYDRASE DECR CONCN OF HYDROGEN ION AVAILABLE FOR EXCHANGE. DECR HYDROGEN-ION CONCN LEADS TO NATRIURESIS & THEREFORE DIURESIS. USE OF CARBONIC ANHYDRASE INHIBITOR DOES NOT GREATLY ALTER CHLORIDE EXCRETION. HOWEVER, THERE MAY BE MARKED POTASSIUM LOSS WITH RESULTING HYPOKALEMIA. /DIURETICS/|DOMINANT ACTION OF THIAZIDES IS TO INCR RENAL EXCRETION OF SODIUM & CHLORIDE & ACCOMPANYING VOL OF WATER. UNLIKE BOTH MERCURIALS & CARBONIC ANHYDRASE INHIBITORS, ACTION OF THIAZIDES IS VIRTUALLY INDEPENDENT OF ACID-BASE BALANCE. THIAZIDES ALSO EVOKE SIGNIFICANT AUGMENTATION OF POTASSIUM EXCRETION... /BENZOTHIADIAZIDES/|THIAZIDES ARE...SECRETED INTO TUBULAR FLUID BY ACTIVE PROCESS LOCATED IN PROXIMAL SEGMENT. ... THIAZIDES INHIBIT REABSORPTION OF SODIUM & ITS ATTENDANT ANION, CHLORIDE, IN DISTAL SEGMENT. ... AUGMENTED EXCRETION OF.../POTASSIUM/ RESULTS FROM ITS INCR SECRETION BY DISTAL TUBULE. /BENZOTHIADIAZIDES/

CLINICAL TOXICITY IS RELATIVELY RARE & USUALLY RESULTS FROM UNEXPECTED HYPERSENSITIVITY. CASES HAVE BEEN REPORTED WITH PURPURA, DERMATITIS WITH PHOTOSENSITIVITY, DEPRESSION OF FORMED ELEMENTS OF BLOOD, & NECROTIZING VASCULITIS... /BENZOTHIADIAZIDES/|PLASMA URIC ACID IS FREQUENTLY ELEVATED & IN SUSCEPTIBLE PT MAY BE ASSOCIATED WITH ATTACKS OF GOUT. ... MANY OBSERVERS HAVE NOTED CORRELATION WITH HYPOKALEMIA & ALKALOSIS. INCR CONCN OF BLOOD AMMONIA HAVE BEEN REPORTED. /BENZOTHIADIAZIDES/|IN PT...WITH HYPERTENSIVE DISEASE & DECR RENAL RESERVE, MANIFESTATIONS OF RENAL INSUFFICIENCY MAY BE AGGRAVATED AFTER INTENSIVE OR PROLONGED COURSES OF THIAZIDES THAT LEAD TO EXCESSIVE DEPLETION OF FLUID & ELECTROLYTE. /BENZOTHIADIAZIDES/|IN CIRRHOSIS OF LIVER, DETERIORATIONG OF MENTAL FUNCTION, INCL ONSET OF COMA, HAS BEEN ATTRIBUTED TO THIAZIDE THERAPY. ... CHOLESTATIC HEPATITIS HAS ALSO BEEN REPORTED. THIAZIDES MAY INDUCE HYPERGLYCEMIA & AGGRAVATE PREEXISTING DIABETES MELLITUS. /BENZOTHIADIAZIDES/

Ademol

MOST COMPD OF THIS GROUP ARE ANALOGS OF 1,2,4-BENZOTHIADIAZINE-1,1-DIOXIDE... AS GROUP THEY CAN BE DESIGNATED AS "BENZOTHIADIAZIDE," OR "THIAZIDE," DIURETICS. /BENZOTHIADIAZIDES/

CHROMATOGRAPHY, THIN-LAYER; GENEST, K & CG FARMILO, J CHROMATOGR 6, 347 (1961).

GENERAL SAMPLE, SPECTROPHOTOMETRY; PILSBURY, VB & JV JACKSON, J PHARM PHARMACOL, 18, 713 (1966). BLOOD, SPECTROPHOTOMETRY; POUTSIAKA, JW ET AL, J PHARMACOL EXP THER, 128, 405 (1960).