ベンズチアジド

log Kow = 1.31 at pH 6.5

1.7

1.73

BITTER TASTE

CHARACTERISTIC

Crystals from acetone.

FINE, WHITE, CRYSTALLINE POWDER

PRACTICALLY INSOL IN WATER, SOL IN ALKALINE SOLN

FREELY SOL IN DIMETHYLFORMAMIDE; SLIGHTLY SOL IN ACETONE; PRACTICALLY INSOL IN ETHER & CHLOROFORM

1.29e-02 g/L

Breast Feeding; Lactation; Milk, Human; Antihypertensive Agents; Thiazide Diuretics

FDA approved drugs -> Active ingredient

FDA approved drugs -> Active ingredient

210-211

231 to 232 °C

Melting point also reported as 238 to 239 °C.

Danger

H317 (100%): May cause an allergic skin reaction [Warning Sensitization, Skin]

P233, P260, P261, P271, P272, P280, P284, P302+P352, P304+P340, P321, P333+P317, P342+P316, P362+P364, P403, and P501 (click each P-code to see the statement)

Aggregated GHS information provided per 91 reports by companies from 2 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Manufacturers, packers, and distributors of drug and drug products for human use are responsible for complying with the labeling, certification, and usage requirements as prescribed by the Federal Food, Drug, and Cosmetic Act, as amended (secs 201-902, 52 Stat. 1040 et seq., as amended; 21 U.S.C. 321-392).

SRP: At the time of review, criteria for land treatment or burial (sanitary landfill) disposal practices are subject to significant revision. Prior to implementing land disposal of waste residue (including waste sludge), consult with environmental regulatory agencies for guidance on acceptable disposal practices.

MANY DIABETIC PATIENTS REGULATED BY CHLORPROPAMIDE OR OTHER SULFONYLUREAS EXHIBIT IMPAIRED DIABETIC CONTROL WHEN ANY THIAZIDE DIURETIC IS ADDED TO DRUG REGIMEN. /THIAZIDE DIURETICS/

CONCURRENT ADMIN OF THIAZIDE DIURETICS & MONOAMINE OXIDASE INHIBITORS MAY INCR HYPOTENSION. /THIAZIDE DIURETICS/

Benzthiazide is used to treat hypertension and edema. Like other thiazides, benzthiazide promotes water loss from the body (diuretics). They inhibit Na⁺/Cl^- reabsorption from the distal convoluted tubules in the kidneys. Thiazides also cause loss of potassium and an increase in serum uric acid. Thiazides are often used to treat hypertension, but their hypotensive effects are not necessarily due to their diuretic activity. Thiazides have been shown to prevent hypertension-related morbidity and mortality although the mechanism is not fully understood. Thiazides cause vasodilation by activating calcium-activated potassium channels (large conductance) in vascular smooth muscles and inhibiting various carbonic anhydrases in vascular tissue.

As a diuretic, benzthiazide inhibits active chloride reabsorption at the early distal tubule via the Na-Cl cotransporter, resulting in an increase in the excretion of sodium, chloride, and water. Thiazides like benzthiazide also inhibit sodium ion transport across the renal tubular epithelium through binding to the thiazide sensitive sodium-chloride transporter. This results in an increase in potassium excretion via the sodium-potassium exchange mechanism. The antihypertensive mechanism of benzthiazide is less well understood although it may be mediated through its action on carbonic anhydrases in the smooth muscle or through its action on the large-conductance calcium-activated potassium (KCa) channel, also found in the smooth muscle.

...BENZOTHIADIIDIDES HAVE DIRECT EFFECT ON RENAL TUBULAR TRANSPORT OF SODIUM & CHLORIDE...INDEPENDENT OF ANY EFFECT ON CARBONIC ANHYDRASE. /THIAZIDE DIURETICS/

...BENEFICIAL EFFECTS /OF THIAZIDES/ APPEAR TO RESULT FROM ALTERED SODIUM BALANCE. ...INITIATION OF TREATMENT...CARDIAC OUTPUT IS DECR & BLOOD VOL... DIMINISHED. ...CHRONIC THERAPY CARDIAC OUTPUT RETURNS TO NORMAL, PERIPHERAL VASCULAR RESISTANCE FALLS &...SMALL REDN IN EXTRACELLULAR WATER & PLASMA VOL. /THIAZIDE DIURETICS/

/DOMINANT ACTION OF THIAZIDES IS TO INCR/ RENAL EXCRETION OF SODIUM & CHLORIDE & ACCOMPANYING VOL OF WATER. ...VIRTUALLY INDEPENDENT OF ACID-BASE BALANCE. ... EVOKE SIGNIFICANT AUGMENTATION OF POTASSIUM EXCRETION. THEY VARY WIDELY IN THEIR POTENCY AS INHIBITORS OF CARBONIC ANHYDRASE. /THIAZIDE DIURETICS/

UNILATERAL RENAL INTRA-ARTERIAL INJECTION OF THIAZIDES PRODUCES A UNILATERAL DIURETIC RESPONSE, INDICATING A DIRECT RENAL ACTION. ...THIAZIDES...ACTIVELY SECRETED IN PROXIMAL TUBULE. ... DEPENDING ON THIAZIDE, ITS DOSAGE & SOLUTES MEASURED, ITS ACTION ON ELECTROLYTE TRANSPORT MAY OR MAY NOT BE BLOCKED. /THIAZIDE DIURETICS/