Фуросемид

Краткое описание:

Молекулярная формула: C12H11ClN2O5SМолекулярный вес: 330.7Номер CAS: 54-31-9Имена и идентификаторыИ...

Подробное описание

Молекулярная формула: C12H11ClN2O5S

Молекулярный вес: 330.7

Номер CAS: 54-31-9

Имена и идентификаторы

ИмяФуросемид
СинонимыФуросемид
FRUSEMIDE
ФУРОСЕМИД
ФУРОСЕМИД
Фуросемид
ЛАБОТЕСТ-ВВ LT00244801
4-CHLORO-N-FURFURYL-5-SULFAMOYLANTHRANILIC ACID
4-chloro-n-furfuryl-5-sulfamoylanthranilic acid
2-furfurylamino-4-chloro-5-sulfamoylbenzoic acid
2-furfurylamino-4-chloro-5-sulfamoylbenzoic acid
5-(aminosulfonyl)-4-chloro-2-((2-furanylmethyl)amino)benzoic acid
5-[АМИНОСУЛЬФОНИЛ]-4-ХЛОР-2-[(2-ФУРАНИЛМЕТИЛ)АМИНО]БЕНЗОЙНАЯ КИСЛОТА
5-(АМИНОСУЛЬФОНИЛ)-4-ХЛОР-2-[(2-ФУРАНИЛМЕТИЛ)АМИНО]БЕНЗОЙНАЯ КИСЛОТА
CAS54-31-9
EINECS200-203-6
InChIInChI=1/C12H11ClN2O5S/c13-9-5-10(15-6-7-2-1-3-20-7)8(12(16)17)4-11(9)21(14,18)19/h1-5,15H,6H2,(H,16,17)(H2,14,18,19)
InChIKeyZZUFCTLCJUWOSV-UHFFFAOYSA-N

54-31-9 – Физико-химические свойства

Молекулярная формулаC12H11ClN2O5S
Молярная масса330.74
Плотность1.606
Температура плавления220 ° C (разл.) (Лит.)
Болинг Точка582.1 ± 60.0 ° C (прогноз)
Точка возгорания11 ° C
Растворимость водыРастворим в ацетоне, ДМФА или метаноле. Слабо растворим в воде
РастворимостьПрактически нерастворим в воде, растворим в ацетоне, умеренно растворим в этаноле (96%), практически нерастворим в метиленхлориде. Растворяется в разбавленных растворах гидроксидов щелочных металлов.
Внешний видпорошок
ЦветОт белого до кремового
Merck14,4309
рКаpKa 3.8 (неопределенно)
Условия хранения2-8 ° C
СтабильностьСтабильный, но чувствительный к свету, чувствительный к воздуху и гигроскопичный. Несовместим с сильными окислителями.
Показатель преломления1.6580 (оценка)
Физические и химические свойстваПлотность 1.606
температура плавления 220°С
ИспользуйтеИспользуется как мочегонное средство

54-31-9 – Риск и безопасность

Коды рисковR61 – Может причинить вред нерожденному ребенку
Р39/23/24/25 –
R23/24/25 – Токсично при вдыхании, попадании на кожу и проглатывании.
R11 – Легковоспламеняющийся
R36/37/38 – Раздражает глаза, дыхательную систему и кожу.
Описание безопасностиS7 – Держите контейнер плотно закрытым.
S16 – Хранить вдали от источников возгорания.
S36/37 – Надевайте подходящую защитную одежду и перчатки.
S45 – В случае несчастного случая или плохого самочувствия немедленно обратитесь к врачу (по возможности покажите этикетку).
S53 – Избегайте воздействия – перед использованием получите специальные инструкции.
S36/37/39 – Носите подходящую защитную одежду, перчатки и средства защиты глаз/лица.
S22 – Не вдыхайте пыль.
S36 – Носите подходящую защитную одежду.
S26 – При попадании в глаза немедленно промыть большим количеством воды и обратиться к врачу.
Идентификаторы ООНUN 1230 3 / PG 2
WGK Германия3
RTECSCB2625000
Код ТН ВЭД2935904000
ТоксичностьLD50 orally in female, male rats: 2600, 2820 mg/kg (Goldenthal)

Справочная информация

(МАИР) классификация канцерогенов3 (Vol. 50) 1990
Введениеfurosemide is a diuretic, also known as furosemide, developed in 1963 by the former sidehst, clinically used for the treatment of cardiac edema, renal edema, liver cirrhosis ascites, dysfunction or vascular disorders caused by peripheral edema, and can promote the upper urethral calculi discharge. Its diuretic effect is rapid and strong, and it is often used in severe cases where other diuretics are ineffective.
high-efficiency diureticsfurosemide, also known as furanilianic acid, furosemide, furosemide, diuretics, is a role in the ascending branch of the medullary branch of the sulfamide class of highly efficient diuretics, has a strong and short diuretic effect, can increase water, sodium, chlorine, potassium, calcium, magnesium, excretion of phosphate, etc. Clinically used for the treatment of cardiac edema, renal edema, cirrhosis ascites, dysfunction or vascular disorders caused by peripheral edema, and can promote the upper urinary tract calculi excretion. Intravenous administration can treat cerebral edema, and can also accelerate the excretion of toxic substances in the case of cerebral edema. It should be noted that furosemide diuresis, due to the increase in urine Cl-, Na, K, H excretion, the excretion of HCO3-does not increase, long-term repeated use or a large number of drugs can cause low salt syndrome, low chlorine and low potassium base poisoning. In recent years, researchers have found that furosemide aerosol inhalation has obvious Antiasthmatic effect, which is the same as sodium cromoglycate, inhibits the release of allergic mediators, inhibits the release of neurotransmitter acetylcholine and substance P, it may be related to its ability to inhibit the entry of chloride ions into the cell membrane of the respiratory tract. Clinical trials in exercise-induced asthma, antigen-induced immediate and late-onset asthma.
механизм действияfurosemide mainly inhibits the reabsorption of Na and Cl-in the medulla and cortex of the thick ascending branch of the loop, promoting sodium, chloride, the excretion of potassium and affects the formation of hyperosmolality in the renal medulla, interferes with the process of concentration and dilution of urine, increases the volume of urine. This product can inhibit the activity of prostaglandin decomposition enzyme, increase the content of prostaglandin E2, has the effect of expanding blood vessels, has the effect of proximal convoluted tubules and glomerular filtration, and can increase renal blood flow, adjust the blood flow distribution in the kidney, reduce the blood flow of the medulla, increase the blood flow of the surface cortex, promote diuresis, the effect is rapid and strong, and it is used for other cases of ineffective diuretic drugs.
ФармакокинетикаThe oral absorption rate of furosemide is 60% ~ 70%, but it does not affect the absorption rate and its curative effect. The oral absorption rate of patients with end-stage renal disease is reduced to 43% ~ 46%. Congestive heart failure and nephrotic syndrome and other edema diseases, due to intestinal wall edema, oral absorption rate also decreased, so in the above situation should be parenteral route of administration. Mainly distributed in the extracellular fluid, the volume of distribution of the average body weight of 11.4%, plasma protein binding rate of 91% ~ 97%, almost all with albumin binding. The drug can pass through the placental barrier and can be secreted into the milk. The onset time of action after oral and intravenous administration was 30-60 minutes and 5 minutes, respectively, and the peak time was 1-2 hours and 0.33-1 hours. The duration of action was 6-8 hours and 2 hours, respectively. There is a large individual difference in T1/2b, the normal person is 30~60 minutes, anuria patients extended to 75~155 minutes, liver and kidney function at the same time severe damage extended to 11~20 hours. Due to the poor liver and kidney clearance ability, T1/2b was prolonged to 4~8 hours. 88% to the original form of renal excretion, 12% by the liver metabolism by bile excretion. Impaired renal function increased metabolism by the liver. The drug was not cleared by dialysis.
показания(1) edema diseases including congestive heart failure, liver cirrhosis, kidney disease (nephritis, kidney disease and various causes of acute and chronic renal failure), especially when the effect of other diuretics is not good, the application of this class of drugs may still be effective. Combined with other drugs in the treatment of acute pulmonary edema and acute cerebral edema.
(2) hypertension is generally not the first choice for the treatment of essential hypertension, but when the efficacy of thiazide drugs is poor, especially when accompanied by renal insufficiency or hypertensive crisis, this class of drugs is particularly suitable.
(3) prevention of acute renal failure for a variety of reasons lead to insufficient renal blood perfusion, such as water loss, Shock, poisoning, anesthesia accident and circulatory insufficiency, in the correction of hypovolemia and timely application, can reduce the chance of acute tubular necrosis.
(4) hyperkalemia and hypercalcemia.
(5) Diluted hyponatremia, especially when the serum sodium concentration is lower than 120mmol/L.
(6) SIADH.
(7) Acute drug poisoning such as barbiturate poisoning.
побочные эффектыduring the use of furosemide, there may be Nausea, Diarrhea, drug eruption, pruritus, blurred vision and other adverse reactions, sometimes can occur dizziness, Fatigue, fatigue, muscle cramps, thirst, a small number of patients with leukopenia, individual patients with thrombocytopenia, erythema multiforme, orthostatic hypotension, long-term use can cause gastric and duodenal ulcers.
ИспользуйтеThe drug has a strong and short diuretic effect, and is a potent diuretic for the treatment of heart, liver, edema caused by diseases such as kidney, especially the case of no effect on the basal diuretic drugs; Can be used for the treatment of acute pulmonary edema, cerebral edema, acute renal failure and hypertension and other diseases; With the rehydration of the product can promote the toxic non-discharge. The oral LD50 of rats was 2600-2820mg/kg.
use as diuretic
способ производства2, 4-dichlorobenzoic acid (see 12740) is obtained by chlorosulfonation, ammonification and acidification, 4-dichloro-5-sulfamoylbenzoic acid. Furosemide is then prepared by condensation with furfurylamine.
Каталогтоксичными веществами
степень токсичностиотравление
Острая токсичностьПерорально-крыса LD50: 2600 мг/кг; Перорально-мышь LD50: 2200 мг/кг
характеристики опасности воспламеняемостиflammable; Decomposition of toxic nitrogen oxides in fire; sulfur oxide and chloride fumes
Характеристики хранения и транспортировкисклад низкая температура, вентиляция, сухость
огнегасящий агентвода, углекислый газ, сухой порошок, песок

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