Quinethazone

289.73858

289.74

200-801-7

759904

DTXSID9023548

Fibrous crystals from 50% acetone|WHITE TO YELLOWISH WHITE, CRYSTALLINE POWDER

C - Cardiovascular system

109.67000

0.49

Fibrous crystals or white powder. (NTP, 1992)

1.4±0.1 g/cm3

250-252 °C

1.582

0.15g/L(25 ºC)

ODORLESS

BITTER TASTE

IT DIFFERS CHEMICALLY FROM THE BENZOTHIAZIDE TYPE ONLY IN REPLACEMENT OF SULFUR ATOM BY CARBON

Insoluble in water.

Amides and Imides

NONH for all modes of transport

Stable. Combustible. Incompatible with strong oxidizing agents.

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).

Flash point data for this chemical are not available; however, it is probably combustible. (NTP, 1992)

Fires involving this chemical may be controlled with a carbon dioxide, dry chemical or Halon extinguisher. (NTP, 1992)

SMALL SPILLS AND LEAKAGE: If you spill this chemical, dampen the solid spill material with 5% ammonium hydroxide, then transfer the dampened material to a suitable container. Use absorbent paper dampened with 5% ammonium hydroxide to pick up any remaining material. Your contaminated clothing and the absorbent paper should be sealed in a vapor-tight plastic bag for eventual disposal. Wash all contaminated surfaces with 5% ammonium hydroxide followed by washing with a soap and water solution. Do not reenter the contaminated area until the Safety Officer (or other responsible person) has verified that the area has been properly cleaned. STORAGE PRECAUTIONS: You should store this material in a refrigerator. (NTP, 1992)

RECOMMENDED RESPIRATOR: Where the neat test chemical is weighed and diluted, wear a NIOSH-approved half face respirator equipped with an organic vapor/acid gas cartridge (specific for organic vapors, HCl, acid gas and SO2) with a dust/mist filter. (NTP, 1992)

MANY DIABETIC PT REGULATED BY CHLORPROPAMIDE OR OTHER SULFONYLUREAS EXHIBIT IMPAIRED DIABETIC CONTROL WHEN ANY THIAZIDE DIURETIC IS ADDED TO DRUG REGIMEN. /QUINETHAZONE/...SHOULD BE EXPECTED TO INTERACT IN A SIMILAR MANNER.|PT RECEIVING /THIAZIDES & RELATED DIURETICS/...MAY DEVELOP ELECTROLYTE DISTURBANCES...WHICH MAY ENHANCE CARDIOTOXICITY OF DIGITALIS. /QUINETHAZONE/...CAN CAUSE HYPOKALEMIA, & MAY BE EXPECTED TO INTERACT WITH CARDIAC GLYCOSIDES.|THIAZIDES ENHANCE ANTIHYPERTENSIVE ACTION OF GUANETHIDINE... /QUINETHAZONE/...SHOULD BE EXPECTED TO INTERACT WITH GUANETHIDINE ALSO.|/QUINETHAZONE/...MAY ENHANCE NEUROMUSCULAR BLOCKADE PRODUCED BY TUBOCURARINE...|For more Interactions (Complete) data for QUINETHAZONE (20 total), please visit the HSDB record page.

Used to treat hypertension.

Diuretics, Sulfamyl|A QUINAZOLINE DERIVATIVE WITH DIURETIC & ANTIHYPERTENSIVE ACTIONS SIMILAR TO THIAZIDES. ... AVAILABLE CLINICAL EVIDENCE INDICATES THAT ITS SITE, MECHANISM & DURATION OF ACTION, ELECTROLYTE EXCRETION PATTERN, THERAPEUTIC ACTIONS, & UNTOWARD EFFECTS ARE SIMILIAR TO THOSE OF CHLOROTHIAZIDE & RELATED AGENTS.|MOST OF THE THIAZIDES ARE GIVEN IN DIVIDED DAILY DOSES FOR TREATMENT OF HYPERTENSION, BUT A SINGLE DAILY DOSE MAY BE PREFERABLE FOR THE MOBILIZATION OF EDEMA FLUID. ... THE ACTION OF QUINETHAZONE...MAY PERSIST UP TO 24 HR.|Initial antihypertensive agents Diuretics...hydrochlorothiazide or chlorthalidone is generally preferred; used in most clinical trials /from table/|For more Therapeutic Uses (Complete) data for QUINETHAZONE (8 total), please visit the HSDB record page.

PLASMA POTASSIUM CONCN SHOULD BE DETERMINED PERIODICALLY IN PT WHO RECEIVE THIAZIDE DIURETICS FOR EXTENDED PERIODS. /BENZOTHIADIAZIDES/|... Long-term effects include slight decrease in extracellular fluid volume ... /from table/|May suppress lactation ... /Thiazide diuretics; from table/|Many experts consider diuretics contraindicated in pregnancy except for patients with heart disease, since they do not prevent or alter course of toxemia and may decrease placental perfusion. /Chlorothiazide; from table/|For more Drug Warnings (Complete) data for QUINETHAZONE (9 total), please visit the HSDB record page.

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

Quinethazone is a thiazide diuretic used to treat hypertension. It inhibits 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.)

...RAPIDLY ABSORBED FROM GI TRACT...

As a diuretic, quinethazone 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 quinethazone 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 quinethazone 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 CARBONIC ANHYDRASE INACTIVATION. ...HAVE PARALLEL DOSE-RESPONSE CURVES & COMPARABLE MAX CHLORURETIC EFFECTS. /BENZOTHIADIAZIDES/|RENAL ACTIONS OF THIAZIDE DIURETICS DECR EXTRACELLULAR FLUID & PLASMA VOL, CARDIAC OUTPUT, & TOTAL EXCHANGEABLE SODIUM IN INDIVIDUALS WITHOUT ANY EVIDENCE OF CARDIAC FAILURE. ...SODIUM & WATER DEPLETION...BASIS FOR ANTIHYPERTENSIVE EFFECT. ...DIURETIC THIAZIDES RELAX PERIPHERAL ARTERIOLAR SMOOTH MUSCLE. /BENZOTHIADIAZIDES/|Decreased plasma volume and decreased extracellular fluid volume; decreased cardiac output initially, followed by decreased total peripheral resistance with normalization of cardiac output ... /from table/|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/|For more Mechanism of Action (Complete) data for QUINETHAZONE (7 total), please visit the HSDB record page.

SYMPTOMS: Symptoms of exposure to this compound may include allergies, skin rashes, thirst, epigastric pain, anorexia, gastric irritation, nausea, vomiting, diarrhea, constipation, photosensitivity, dryness, headache, muscle spasm, weakness, inflammation of the salivary gland, loss of libido, paresthesia, acute pancreatitis, pneumonitis, jaundice and other blood disorders. Other symptoms include cramping, hyperglycemia, glycosuria, vertigo, xanthopsia, leukopenia, thrombocytopenia, agranulocytosis, aplastic anemia, purpura, urticaria, necrotizing angiitis and restlessness. ACUTE/CHRONIC HAZARDS: This chemical may cause skin irritation. (NTP, 1992)

EYES: First check the victim for contact lenses and remove if present. Flush victim's eyes with water or normal saline solution for 20 to 30 minutes while simultaneously calling a hospital or poison control center. Do not put any ointments, oils, or medication in the victim's eyes without specific instructions from a physician. IMMEDIATELY transport the victim after flushing eyes to a hospital even if no symptoms (such as redness or irritation) develop. SKIN: IMMEDIATELY flood affected skin with water while removing and isolating all contaminated clothing. Gently wash all affected skin areas thoroughly with soap and water. If symptoms such as redness or irritation develop, IMMEDIATELY call a physician and be prepared to transport the victim to a hospital for treatment. INHALATION: IMMEDIATELY leave the contaminated area; take deep breaths of fresh air. If symptoms (such as wheezing, coughing, shortness of breath, or burning in the mouth, throat, or chest) develop, call a physician and be prepared to transport the victim to a hospital. Provide proper respiratory protection to rescuers entering an unknown atmosphere. Whenever possible, Self-Contained Breathing Apparatus (SCBA) should be used; if not available, use a level of protection greater than or equal to that advised under Protective Clothing. INGESTION: DO NOT INDUCE VOMITING. If the victim is conscious and not convulsing, give 1 or 2 glasses of water to dilute the chemical and IMMEDIATELY call a hospital or poison control center. Be prepared to transport the victim to a hospital if advised by a physician. If the victim is convulsing or unconscious, do not give anything by mouth, ensure that the victim's airway is open and lay the victim on his/her side with the head lower than the body. DO NOT INDUCE VOMITING. IMMEDIATELY transport the victim to a hospital. (NTP, 1992)

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

CLINICAL TOXICITY...USUALLY RESULTS FROM UNEXPECTED HYPERSENSITIVITY. CASES HAVE BEEN REPORTED WITH PURPURA, DERMATITIS WITH PHOTOSENSITIVITY, DEPRESSION OF FORMED ELEMENTS OF BLOOD, & NECROTIZING VASCULITIS. /BENZOTHIADIAZIDES/

quinethazone

DETECTION IN BIOLOGICAL FLUIDS BY CHROMATOGRAPHY & UV ABSORPTION @ 254 NM.|DETERMINATION OF SULFONAMIDE DIURETICS BY ELECTRON-CAPTURE GAS CHROMATOGRAPHY.

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