Benzthiazide

431.94

431.94

202-061-0

1TD8J48L61

755902

DTXSID4022658

C65254

Crystals from acetone.|FINE, WHITE, CRYSTALLINE POWDER

2935009090

161

1.7

Solid

1.4176 (rough estimate)

231-232 °C

1.6100 (estimate)

2.8mg/L(room temperature)

Intravenous-rat LD50: 422 mg/kg; Intravenous-mouse LD50; 410 mg/kg

Ventilated, low temperature and dry; combustible with warehouse food; burning produces toxic nitrogen oxides, sulfur oxides and chloride fumes

CHARACTERISTIC

BITTER TASTE

6None

6

186.7 Ų [M+H]+ [CCS Type: TW, Method: calibrated with polyalanine and drug standards]

NONH for all modes of transport

2

42/43

26-36

DK8400000

Xn

Ventilated, low temperature and dry; stored separately from food materials in warehouse

STABLE IN BOTH LIGHT & AIR

P261-P280-P342 + P311

H317-H334

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.

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).

|Danger|H317 (100%): May cause an allergic skin reaction [Warning Sensitization, Skin]|P261, P272, P280, P285, P302+P352, P304+P341, P321, P333+P313, P342+P311, P363, and P501|Aggregated GHS information provided by 90 companies from 2 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

highly toxic

Symptoms of overdose include nausea, vomiting, fatigue, urinary problems and drowsiness.

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/|...HYPOKALEMIA MAY INTENSIFY ACTION OF NEUROMUSCULAR BLOCKING AGENTS. ... POTASSIUM-DEPLETING DIURETICS ARE KNOWN TO CAUSE HYPOKALEMIA & MAY ENHANCE THIS EFFECT. /DIURETICS/|...CARDIAC GLYCOSIDE & DIURETIC; DIURETIC-INDUCED HYPOKALEMIA POTENTIATES CARDIOTOXICITY OF GLYCOSIDE. /DIURETICS/|For more Interactions (Complete) data for BENZTHIAZIDE (21 total), please visit the HSDB record page.

LD50 MOUSE ORAL GREATER THAN 5000 MG/KG|LD50 RAT ORAL GREATER THAN 10000 MG/KG|LD50 DOG ORAL GREATER THAN 5000 MG/KG|RABBIT INTRAVENOUS 410 MG/KG|For more Non-Human Toxicity Values (Complete) data for BENZTHIAZIDE (6 total), please visit the HSDB record page.

30%

For the treatment of high blood pressure and management of edema.

Diuretics, Thiazide|IT IS ABOUT 10 TIMES AS POTENT ON MG BASIS AS CHLOROTHIAZIDE.|THIAZIDE DRUGS...USUALLY FIRST DRUG TO BE EMPLOYED IN TREATMENT OF HYPERTENSION. SINCE THIAZIDES INDUCE ONLY LIMITED (10%) REDN IN BLOOD PRESSURE THEY ARE USEFUL EITHER IN MILD CASES OF HYPERTENSION OR AS ADJUNCTIVE THERAPY TO OTHER DRUGS. /THIAZIDE DIURETICS/|THIAZIDE DIURETICS ARE EFFECTIVE AS ADJUNCTIVE THERAPY IN EDEMA ASSOC WITH CONGESTIVE HEART FAILURE, HEPATIC CIRRHOSIS, & CORTICOSTEROID & ESTROGEN THERAPY, AS WELL AS EDEMA DUE TO VARIOUS FORMS OF RENAL DYSFUNCTION...& SEVERE EDEMA DUE TO PREGNANCY. /THIAZIDE DIURETICS/|For more Therapeutic Uses (Complete) data for BENZTHIAZIDE (8 total), please visit the HSDB record page.

THEY SHOULD...BE USED WITH CAUTION IN PT WITH IMPAIRED LIVER FUNCTION. /THIAZIDE DIURETICS/|PERIODIC SERUM ELECTROLYTE DETERMINATION SHOULD BE DONE ON ALL PATIENTS IN ORDER TO DETECT ELECTROLYTE IMBALANCE SUCH AS HYPONATREMIA, HYPOCHLOREMIC ALKALOSIS, & HYPOKALEMIA. /THIAZIDE DIURETICS/|THIAZIDE DIURETICS ARE CONTRAINDICATED IN ANURIA, PATIENTS HYPERSENSITIVE TO THESE & OTHER SULFONAMIDE DRUGS, & IN OTHERWISE HEALTHY PREGNANT WOMEN WITH OR WITHOUT MILD EDEMA. ...SHOULD BE USED WITH CAUTION IN PT WITH RENAL DISEASE, SINCE THEY MAY PPT AZOTEMIA. /THIAZIDE DIURETICS/|CLINICAL TOXICITY...USUALLY RESULTS FROM UNEXPECTED HYPERSENSITIVITY. CASES OF...PURPURA, DERMATITIS WITH PHOTOSENSITIVITY, DEPRESSION OF FORMED ELEMENTS OF BLOOD, & NECROTIZING VASCULITIS HAVE BEEN REPORTED. /THIAZIDE DIURETICS/|For more Drug Warnings (Complete) data for BENZTHIAZIDE (8 total), please visit the HSDB record page.

3. 3= MODERATELY TOXIC: PROBABLE ORAL LETHAL DOSE (HUMAN) 0.5-5 G/KG, BETWEEN 1 OZ & 1 PINT FOR 70 KG PERSON (150 LB). /BENZOTHIADIAZIDE 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.

Absorbed in the digestive tract.|DIURESIS OCCURS WITHIN 2 HR & LASTS 12-18 HR.|THIAZIDES ARE ABSORBED FROM GI TRACT & OWE THEIR USEFULNESS LARGELY TO THEIR EFFECTIVENESS BY ORAL ROUTE. ABSORPTION IS RELATIVELY RAPID. MOST AGENTS SHOW DEMONSTRABLE DIURETIC EFFECT WITHIN HR AFTER ORAL ADMIN. /THIAZIDE DIURETICS/|IN GENERAL, THIAZIDES WITH RELATIVELY LONG DURATIONS OF ACTION SHOW PROPORTIONATELY HIGH DEGREE OF BINDING TO PLASMA PROTEINS & ARE REABSORBED BY RENAL TUBULES. ... DRUG PASSES READILY THROUGH PLACENTAL BARRIER TO FETUS. ALL THIAZIDES PROBABLY UNDERGO ACTIVE SECRETION IN PROXIMAL TUBULE. /THIAZIDE DIURETICS/|DISTRIBUTED IN EXTRACELLULAR SPACE & /CROSSES/ PLACENTA /& APPEARS IN CORD BLOOD/. ONSET OF DIURETIC ACTION...2 HR...PEAK EFFECT...3 TO 6 HR...APPROX DURATION OF /ACTION OF SINGLE DOSE 12-18 HR/. EXCRETED BY GLOMERULAR FILTRATION & ACTIVE SECRETION IN PROXIMAL TUBULE /HUMAN, ORAL/.|ONSET OF HYPOTENSIVE ACTION...3 TO 4 DAYS, &...ACTION DISSIPATES...1ST WK AFTER DISCONTINUING CHRONIC THERAPY. /APPEARS/ IN MILK OF NURSING MOTHERS /HUMAN, ORAL/.

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/|For more Mechanism of Action (Complete) data for BENZTHIAZIDE (11 total), please visit the HSDB record page.

Thiazide diuretic overdose should be treated by immediate evacuation of the stomach followed by supportive symptomatic treatment and monitoring of serum electrolyte concentrations and renal function. /Thiazide diuretic/

ASYMPTOMATIC HYPERURICEMIA OCCURS FREQUENTLY DURING PROLONGED TREATMENT. ACUTE ATTACK OF GOUT MAY BE PPT IN PATIENTS WITH HISTORY OF GOUT OR IN THOSE WITH RENAL FAILURE, BUT IS OBSERVED ONLY RARELY IN PATIENTS WITHOUT THESE DISABILITIES.|ADVERSE EFFECTS...HYPERSENSITIVITY (...RASH, URTICARIA...FEVER, RESPIRATORY DISTRESS, ANAPHYLACTIC REACTIONS)...GLYCOSURIA...MUSCLE SPASM, WEAKNESS, RESTLESSNESS, BLURRED VISION, & HEMATURIA... /THIAZIDE DIURETICS/|May suppress lactation, but compatible /SRP: with breast feeding/. /Thiazide diuretics, from table/

benzothiazide

DOSAGE FORMS- TABLETS NF: 50 MG.

THIN-LAYER CHROMATOGRAPHY.|AOAC Method 973.74. Thiazide in Drugs. Spectrophotometric Method. Applicable to benzthiazide, chlorothiazide, methylclothiazide, hydrochlorothiazide, and hydroflumethiazide.

DETERMINATION OF BENZTHIAZIDE IN URINE BY LIQUID CHROMATOGRAPHY.

Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients