Methyclothiazide

360.24

360.24

205-172-2

R6KDH2S0SX|R00UUL4SRN

760078|110431

DTXSID6023313

Crystals form alcohol and water|White or practically white, crystalline powder

C - Cardiovascular system

2935904000

126

0.6

Solid

1.6122 (rough estimate)

225 °C

597.9±60.0 °C(Predicted)

315.4±32.9 °C

1.6000 (estimate)

8.24e-01 g/L

Store below 40 deg C (104 deg F), preferably between 15 and 30 deg C (59 and 86 deg F), unless otherwise specified by manufacturer. Store in a well-closed container.

2.93E-14mmHg at 25°C

Odorless or has slight odor.

TASTELESS

9.4None

9.4|pKa = 9.4

Chars slightly below 220 °C and decomposes at 220 °C

NONH for all modes of transport

Commercially available methyclothiazide tablets have an expiration date of 5 yr following the date of manufacture.

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.

The Approved Drug Products with Therapeutic Equivalence Evaluations List identifies currently marketed prescription drug products, incl methylclothiazide, approved on the basis of safety and effectiveness by FDA under sections 505 of the Federal Food, Drug, and Cosmetic Act.

Acute oral toxicity (LD50): >4000 mg/kg [Rat]. Symptoms of overdosage include electrolyte imbalance and signs of potassium deficiency such as confusion, dizziness, muscular weakness, and gastrointestinal disturbances.

Many diabetic patients regulated by chlorpropamide or other sulfonylureas exhibit impaired diabetic control when any thiazide diuretic is added to the drug regimen. ... This drug interaction may occur with acetohexamide, tolazamide, and tolbutamide. /thiazide diuretics/|Thiazides enhance the antihypertensive action of guanethidine, allowing the dose of guanethidine to be reduced and decr the incidence of adverse reactions. ... Bethanidine and debrisoquin are chemically and Pharmacologically related to guanethidine and may be expected to interact with hydrochlorothiazide. /thiazide diuretics/|Chlorothiazide and other thiazide diuretics enhance the cardiotoxic and neurotoxic effects of lithium and these drugs should not be administered concurrently. /thiazide diuretics/|...Disruption of uricosuric therapy by admin of diuretic which increases plasma uric acid levels (thiazides) ... /thiazide diuretics/|For more Interactions (Complete) data for METHYCLOTHIAZIDE (16 total), please visit the HSDB record page.

LD50 Rat ip 2000 mg/kg|LD50 Mouse ip 870 mg/kg|LD50 Mouse iv 400 mg/kg

For use in the management of hypertension either as the sole therapeutic agent or to enhance the effect of other antihypertensive drugs in the more severe forms of hypertension. Also used as adjunctive therapy in edema associated with congestive heart failure, hepatic cirrhosis, and corticosteroid and estrogen therapy.

Diuretics, Thiazide|Thiazides...may be used to control edema associated with premenstrual tension and to reduce fluid retention following administration of corticosteroids or estrogens. /thiazide diuretics/|Indications include edema associated with congestive heart failure, hepatic cirrhosis with ascites, corticosteroid and estrogen therapy, and some forms of renal function impairment including nephrotic syndrome, acute glomerulonephritis, and chronic renal failure. /Included in US product labeling; Thiazide diuretics/|Thiazide diuretics are indicated either alone or as adjunctive therapy in the treatment of hypertension. /Included in US product labeling; Thiazide diuretics/|For more Therapeutic Uses (Complete) data for METHYCLOTHIAZIDE (10 total), please visit the HSDB record page.

Because hypokalemia accelerates glucose intolerance, fall in serum potassium level can aggravate diabetes. Diuretic therapy may cause pronounced hypokalemia in presence of incr mineralocorticoid activity due to primary adrenal disease...or corticosteroid therapy. /thiazide diuretics/|Reversible elevation of blood urea nitrogen level may occur... This prerenal azotemia is caused by decrease in renal blood flow and glomerular filtration rate secondary to reduction in blood volume induced by diuretic. ...thiazides may directly depress renal blood flow. /thiazide diuretics/|Necrotizing vasculitis of skin and kidney has occurred in elderly patients, but its relationship to thiazides is still unproved. /thiazide diuretics/|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. /thiazide diuretics/|For more Drug Warnings (Complete) data for METHYCLOTHIAZIDE (19 total), please visit the HSDB record page.

3. 3= Moderately toxic: probable oral lethal dose (human) 0.5-5 g/kg, between 1 oz and 1 pint for 70 Kg person (150 lb). /thiazide diuretics/

Methyclothiazide, a diuretic-antihypertensive agent, is a member of the benzothiadiazine (thiazide) class of drugs. Methyclothiazide has a per mg natriuretic activity approximately 100 times that of the prototype thiazide, chlorothiazide. At maximal therapeutic dosages, all thiazides are approximately equal in their diuretic/natriuretic effects. Like other benzothiadiazines, methyclothiazide also has antihypertensive properties, and may be used for this purpose either alone or to enhance the antihypertensive action of other drugs.

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.)

Rapidly absorbed following oral administration.|Thiazides are absorbed from GI tract and owe their usefulness largely to their effectiveness by oral route. Absorption is relatively rapid. Most agents show demonstrable diuretic effect within hr after oral administration. /thiazide diuretics/|In general, thiazides with relatively long durations of action show proportionately high degrees of both binding to plasma proteins and reabsorption by renal tubules. ... Drug passes readily through placental barrier to fetus. All thiazides probably undergo active secretion in proximal tubule. /thiazide diuretics/|Methyclothiazide is absorbed from the GI tract. Little information is available on the extent of absorption and the distribution of methyclothiazide in the body. Methyclothiazide is excreted unchanged in urine.

Methyclothiazide is excreted unchanged in urine.

Methyclothiazide appears to block the active reabsorption of chloride and possibly sodium in the ascending loop of Henle, altering electrolyte transfer in the proximal tubule. This results in excretion of sodium, chloride, and water and, hence, diuresis. As a diuretic, methyclothiazide 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 methyclothiazide 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 methyclothiazide 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.|Acute admin of thiazides increases the excretion of uric acid. However, uric acid excretion is reduced following chronic admin... . The acute effects of inhibitors of Na+-Cl- symport on Ca2+ excretion are variable; when admin chronically, thiazide diuretics decr Ca2+ excretion. The mechanism is unknown but may involve increased proximal reabsorption due to volume depletion as well as direct effects of thiazides to incr Ca2+ reabsorption in the /distal convoluted tubule/. Thiazide diuretics may cause a mild magnesuria by a poorly understood mechanism, and there is increasing awareness that long-term use of thiazide diuretics may cause magnesium deficiency, particularly in the elderly. /Thiazide diuretics/|Thiazides inhibit reabsorption of sodium and ...chloride in distal segment. ... As /a/ class...have important action on excretion of potassium that results from increased secretion of cation by distal tubule. ... Glomerular filtration rate may be reduced by thiazides, particularly with iv admin for exptl purposes. /thiazide diuretics/|Nature of chemical interaction between thiazides and specific renal receptors responsible for chloruretic effect is not known; no critical enzymatic reactions have been identified. /thiazides/|Thiazide diuretics increase urinary excretion of sodium and water by inhibiting sodium reabsorption in the early distal tubules. They increase the rate of delivery of tubular fluid and electrolytes to the distal sites of hydrogen and potassium ion secretion, while plasma volume contraction increases aldosterone production. The increased delivery and increase in aldosterone levels promote sodium reabsorption at the distal tubules, thus increasing the loss of potassium and hydrogen ions. /Thiazide diuretics/|The antidiuretic effect of thiazide diuretics is a result of mild sodium and water depletion leading to increased reabsorption of glomerular filtrate in the proximal renal tubule and reduced delivery of tubular fluid available for excretion. /Thiazide diuretics/

Basic treatment: Establish a patent airway. Suction if necessary. Watch for signs of respiratory insufficiency and assist ventilations if needed. Administer oxygen by nonrebreather mask at 10 to 15 L/min. Monitor for pulmonary edema and treat if necessary ... . Monitor for shock and treat if necessary ... . Anticipate seizures and treat if necessary ... . For eye contamination, flush eyes immediately with water. Irrigate each eye continuously with normal saline during transport ... . Do not use emetics. For ingestion, rinse mouth and administer 5 ml/kg up to 200 ml of water for dilution if the patient can swallow, has a strong gag reflex, and does not drool ... . Cover skin burns with dry sterile dressings after decontamination ... . /Poison A and B/|Advanced treatment: Consider orotracheal or nasotracheal intubation for airway control in the patient who is unconscious, has severe pulmonary edema, or is in respiratory arrest. Positive pressure ventilation techniques with a bag valve mask device may be beneficial. Monitor cardiac rhythm and treat arrhythmias as necessary ... . Start an IV with D5W /SRP: "To keep open", minimal flow rate/. Use lactated Ringer's if signs of hypovolemia are present. Watch for signs of fluid overload. Consider drug therapy for pulmonary edema ... . For hypotension with signs of hypovolemia, administer fluid cautiously. Watch for signs of fluid overload ... . Treat seizures with diazepam (Valium) ... . Use proparacaine hydrochloride to assist eye irrigation ... . /Poison A and B/

Methyclothiazide

Aquatensen: tablets 5 mg; Enduron: tablets: 2.5 & 5 mg.

Analyte: methyclothiazide; matrix: chemical identification; procedure: infrared absorption spectrophotometry with comparison to standards|Analyte: methyclothiazide; matrix: chemical identification; procedure: ultraviolet absorption spectrophotometry with comparison to standards|Analyte: methyclothiazide; matrix: chemical identification; procedure: fuse with sodium hydroxide; ammonia fumes produced turn moistened red litmus paper blue; fused mixture responds to the sulfite test|Analyte: methyclothiazide; matrix: chemical purity; procedure: titration with silver nitrate using eosin Y as indicator|For more Analytic Laboratory Methods (Complete) data for METHYCLOTHIAZIDE (7 total), please visit the HSDB record page.

Method for determination of methylclothiazide in urine by liquid chromatography.

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