Trichlormethiazide

380.66

380.66

205-118-8

757368|61560

DTXSID7023699

CRYSTALS FROM METHANOL + ACETONE + WATER|WHITE, CRYSTALLINE POWDER

C - Cardiovascular system

2935904000

135

0.6

Solid

1.748

270 °C (decomp)

631.3±65.0 °C(Predicted)

335.6±34.3 °C

1.6000 (estimate)

4.15e-01 g/L

Trichlormethiazide tablets should be stored in well-closed containers at a temperature less than 40 deg C, preferably between 15-30 deg C.

7.62E-16mmHg at 25°C

LD50 orally in rats: >20000 mg/kg (Goldenthal)

ODORLESS OR HAS SLIGHT CHARACTERISTIC ODOR

8.6None

8.6|PKA: 8.6

DECOMP AT 266-273 °C, ALSO REPORTED AS 248-250 °C

Ⅲ

2811

2

42/43

36

DK8925000

Xn

LIGHT-SENSITIVE, BUT STABLE IN AIR & HEAT

P261-P280-P284-P304 + P340-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 (97.44%): 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 40 companies from 3 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Oral Rat LD50 = 5600 mg/kg, oral Mouse LD50 = 2600 mg/kg

MANY DIABETIC PATIENTS REGULATED BY CHLORPROPAMIDE OR OTHER SULFONYLUREAS EXHIBIT IMPAIRED DIABETIC CONTROL WHEN ANY THIAZIDE DIURETIC IS ADDED TO DRUG REGIMEN. /THIAZIDE DIURETICS/|...DRUGS SUCH AS...THIAZIDE DIURETICS...WHICH INCR URINARY PH, MAY SERVE TO INCR LIPID SOLUBILITY & TUBULAR REABSORPTION OF QUINIDINE & THUS PROLONG ITS THERAPEUTIC EFFECTS. /THIAZIDE DIURETICS/|...THIAZIDE DIURETICS ENHANCE CARDIOTOXIC & NEUROTOXIC EFFECTS OF LITHIUM & THESE DRUGS SHOULD NOT BE ADMINISTERED CONCURRENTLY. /THIAZIDES/|THIAZIDES ENHANCE ANTIHYPERTENSIVE ACTION OF GUANETHIDINE, ALLOWING DOSE OF GUANETHIDINE TO BE REDUCED & DECR INCIDENCE OF ADVERSE REACTIONS, PARTICULARLY ORTHOSTATIC & EXERCISE-ASSOC HYPOTENSION. /THIAZIDES/|For more Interactions (Complete) data for TRICHLORMETHIAZIDE (24 total), please visit the HSDB record page.

LD50 RAT ORAL 5600 MG/KG|LD50 Rat iv 920 mg/kg|LD50 Mouse oral 2600 mg/kg|LD50 Mouse ip 540 mg/kg|LD50 Mouse iv 750 mg/kg

Used in the treatment of oedema (including that associated with heart failure) and hypertension.

Antihypertensive Agents; Diuretics, Thiazide|ORALLY EFFECTIVE & LONG-ACTING DIURETIC & ANTIHYPERTENSIVE OF THIAZIDE CLASS. ... ON MG BASIS, IT IS APPROX 250 TIMES MORE ACTIVE THAN 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 TRICHLORMETHIAZIDE (11 total), please visit the HSDB record page.

TRICHLORMETHIAZIDE...COULD BE GIVEN LESS FREQUENTLY /THAN MOST OF THIAZIDES/, SINCE...DURATION OF ACTION LONGER THAN 24 HR.|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 PATIENTS WITH RENAL DISEASE, SINCE THEY MAY PPT AZOTEMIA. /THIAZIDE DIURETICS/|PLASMA POTASSIUM CONCN SHOULD BE DETERMINED PERIODICALLY IN PATIENTS WHO RECEIVE THIAZIDE DIURETICS FOR EXTENDED PERIODS. /THIAZIDE DIURETICS/|For more Drug Warnings (Complete) data for TRICHLORMETHIAZIDE (11 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/

Trichloromethiazide is indicated as adjunctive therapy in edema associated with congestive heart failure, hepatic cirrhosis, and corticosteroid and estrogen therapy. Trichloromethiazide has also been found useful in edema due to various forms of renal dysfunction such as nephrotic syndrome, acute glomer-ulonephritis, and chronic renal failure. Trichloromethiazide is also indicated in the management of hypertension either as the sole therapeutic agent or to enhance the effectiveness of other antihypertensive drugs in the more severe forms of hypertension. Like other thiazides, Trichloromethiazide 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.

Agents that inhibit SODIUM CHLORIDE SYMPORTERS. They act as DIURETICS. Excess use is associated with HYPOKALEMIA. (See all compounds classified as Sodium Chloride Symporter Inhibitors.)|Agents that promote the excretion of urine through their effects on kidney function. (See all compounds classified as Diuretics.)|Drugs used in the treatment of acute or chronic vascular HYPERTENSION regardless of pharmacological mechanism. Among the antihypertensive agents are DIURETICS; (especially DIURETICS, THIAZIDE); ADRENERGIC BETA-ANTAGONISTS; ADRENERGIC ALPHA-ANTAGONISTS; ANGIOTENSIN-CONVERTING ENZYME INHIBITORS; CALCIUM CHANNEL BLOCKERS; GANGLIONIC BLOCKERS; and VASODILATOR AGENTS. (See all compounds classified as Antihypertensive Agents.)

Trichlormethiazide is absorbed from the GI tract. Little information is available on the extent of absorption and the fate of trichlormethiazide in the body, although it is believed to be excreted principally as unchanged drug in urine.|MOST CMPD ARE RAPIDLY EXCRETED WITHIN 3-6 HR. /THIAZIDE DIURETICS/|DIURESIS OCCURS WITHIN 2 HR, REACHES PEAK IN 6 HR, & LASTS MORE THAN 24 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/

Half-life is 2-7 hr. /From table/

Trichlormethiazide seemingly appears to inhibit the active reabsorption of chloride in the ascending loop of Henle. Additionally, it may also do the same for sodium. These actions subsequently alter electrolyte transfer in the proximal tubule. This results in excretion of sodium, chloride, and water and, hence, diuresis. As a diuretic, Trichloromethiazide 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 Trichloromethiazide 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 Trichloromethiazide 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.|...BENZOTHIADIAZIDES HAVE DIRECT EFFECT ON RENAL TUBULAR TRANSPORT OF SODIUM & CHLORIDE...INDEPENDENT OF ANY EFFECT ON CARBONIC ANHYDRASE. /THIAZIDE DIURETICS/|THIAZIDES INHIBIT REABSORPTION OF SODIUM &...CHLORIDE IN DISTAL SEGMENT. ... AS CLASS...HAVE IMPORTANT ACTION ON EXCRETION OF POTASSIUM THAT RESULTS FROM INCR SECRETION OF CATION BY DISTAL TUBULE. ... GLOMERULAR FILTRATION RATE MAY BE REDUCED BY THIAZIDES, PARTICULARLY WITH IV ADMIN FOR EXPTL PURPOSES. /THIAZIDE DIURETICS/|...MAY DECR EXCRETION OF URIC ACID IN MAN, THUS INCR ITS CONCN IN PLASMA. HYPERURICEMIC EFFECT RESULTS PRIMARILY FROM INHIBITION OF TUBULAR SECRETION OF URATE. ... UNLIKE MOST OTHER NATRIURETIC AGENTS...DECR RENAL EXCRETION OF CALCIUM RELATIVE TO THAT OF SODIUM... /ENHANCE/ EXCRETION OF MAGNESIUM... /THIAZIDE DIURETICS/|NATURE OF CHEM INTERACTION BETWEEN THIAZIDES & SPECIFIC RENAL RECEPTORS RESPONSIBLE FOR CHLORURETIC EFFECT IS NOT KNOWN; NO CRITICAL ENZYMATIC REACTIONS HAVE BEEN IDENTIFIED. /THIAZIDE DIURETICS/|For more Mechanism of Action (Complete) data for TRICHLORMETHIAZIDE (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/

STUDY OF LIVER DAMAGE DURING TREATMENT WITH TRICHLORMETHIAZIDE IN A MIDDLE AGED PATIENT.|May suppress lactation, but compatible /SRP: with breast feeding/. /Thiazide diuretics, from table/

Aquazide

TABLETS NF: 2 & 4 MG.|METAHYDRIN, NAQUA. MARKET PREPN (TABLETS) 2 & 4 MG.

2H-1,2,4-Benzothiadiazine-7-sulfonamide, 6-chloro-3-(dichloromethyl)-3,4-dihydro-, 1,1-dioxide: ACTIVE

DETECTION OF THIAZIDE DIURETICS IN URINE BY REVERSED-PHASE LIQUID CHROMATOGRAPHY WITH DETECTION BY ULTRAVIOLET ABSORPTION.

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