Furosemide is an organic compound with chemical formula CtwelveHelevenClNtwoOfiveS，It is a powerful diuretic, mainly used to treat edema caused by heart, liver, kidney and other diseases.
On October 27, 2017, the list of carcinogens published by the International Agency for Research on Cancer of the World Health Organization (WHO) was preliminarily sorted out for reference, and furosemide was included in the list of category 3 carcinogens.[2]
Chinese name
Furosemide
Foreign name
Furosemide,Frusemide
chemical formula
CtwelveHelevenClNtwoOfiveS
molecular weight
three hundred and thirty point seven four four
CAS login number
54-31-9
EINECS login number
200-203-6
Melting point
220 ℃(Disassembly)
Boiling point
582.1 ℃
Water solubility
Insoluble
Density
1.606 g/cm³
Appearance
White crystalline powder
Flash point
11 ℃
Security description
S7；S16；S22；S36/37/39；S45；S53
Hazard symbol
T
Hazard description
R61
Prescription medicine or not
yes
Main indications
Edema, hypertension, acute pulmonary edema or brain edema
Solubility: soluble in acetone, methanol, dimethylformamide, slightly soluble in ethanol, insoluble in water
Molecular structure data
Molar refractive index: 75.76
Molar volume (cmthree/mol）：205.8
Isotonic specific volume (90.2K): 606.2
Surface tension (dyne/cm): 75.2
Polarization (10-24cmthree）：30.03
Calculate chemical data
Reference value for drainage parameter calculation (XlogP): None
Number of hydrogen bond donors: 3
Number of hydrogen bond receptors: 7
Number of rotatable chemical bonds: 5
Number of tautomers: 4
Topological molecular polar surface area: 131
Number of heavy atoms: 21
Surface charge: 0
Complexity: 481
Number of isotope atoms: 0
Determine the number of atomic structure centers: 0
Number of uncertain atomic structure centers: 0
Determine the number of chemical bond structure centers: 0
Number of uncertain chemical bond structure centers: 0
Number of covalent bond units: 1
Pharmacopoeia information
Announce
edit
source
This product is 2 - [(2-furomethyl) amino] - 5 - (sulfamoyl) - 4-chlorobenzoic acid, calculated as dry product, containing CtwelveHelevenClNtwoOfiveS shall not be less than 99.0%.
character
This product is white or almost white crystalline powder, odorless.
This product is dissolved in acetone, slightly soluble in ethanol, and insoluble in water.
absorption coefficient
Take this product, weigh it precisely, add 0.4% sodium hydroxide solution to dissolve it and dilute it quantitatively to make a solution containing about 10 μ g per 1mL. According to the ultraviolet visible spectrophotometry (general rule 0401), measure the absorbance and absorption coefficient at the wavelength of 271nm（E1%1cm）565~595.
identify
1. Take about 25mg of this product, add 5mL of water, drop sodium hydroxide test solution to dissolve it properly, and add 1-2 drops of copper sulfate test solution to generate green sediment.
2. Take 25mg of this product, put it in a test tube, add 2.5mL of ethanol to dissolve it, drop 2mL of p-dimethylaminobenzaldehyde test solution along the tube wall, and it will turn green and dark red.
3. Take this product, add 0.4% sodium hydroxide solution to make a solution containing about 5 μ g per 1mL, and determine it by ultraviolet visible spectrophotometry (general rule 0401). There is maximum absorption at the wavelength of 228nm, 271nm and 333nm.
4. The infrared absorption spectrum of this product should be consistent with the control spectrum (spectrum set 184 figure).
inspect
Clarity and color of alkaline solution
Take 0.50g of this product, add 5mL of sodium hydroxide test solution to dissolve it, and then add 5mL of water. The solution should be clear and colorless. If it appears turbid, it should not be thicker than No. 2 turbidity standard solution (General Rule 0902 Method 1). If it appears color, it should not be deeper than No. 3 yellow standard solution (General Rule 0901 Method 1).
chloride
Take 2.0g of this product, add 100mL of water, shake fully, filter, take 25mL of filtrate, check according to the law (general rule 0801), and compare with the control solution made of 7.0mL of standard sodium chloride solution, it should not be more concentrated (0.014%).
sulfate
Take 25mL of the remaining filtrate under the above chloride item, and check according to the law (general rule 0801). Compared with the control solution made of 2.0mL of standard potassium sulfate solution, it should not be more concentrated (0.04%).
Related substances
Determine according to the high performance liquid chromatography (general rule 0512), and operate in dark.
Mixed solvent: take 22mL of glacial acetic acid, add acetonitrile water (1:1) to 1000mL, and mix well.
Test solution: take this product, add mixed solvent to dissolve and dilute it to make a solution containing about 1mg per 1mL.
Control solution: Precisely measure an appropriate amount of the test solution and dilute it with mixed solvent to prepare a solution containing 10 μ g per 1mL.
Chromatographic conditions: octadecyl silane bonded silica gel is used as the filler, water tetrahydrofuran glacial acetic acid (70:30:1) is used as the mobile phase, the detection wavelength is 272nm, and the injection volume is 20 μ L.
System applicability requirements: the number of theoretical plates shall not be less than 4000 according to the furosemide peak.
Determination method: Precisely measure the test solution and the reference solution, respectively inject them into the liquid chromatograph, and record the retention time of the chromatogram to three times of the main component peak.
Limit: If there is an impurity peak in the chromatogram of the test solution, the area of a single impurity peak shall not be greater than 0.2 times (0.2%) of the main peak area of the reference solution, and the sum of the areas of each impurity peak shall not be greater than the main peak area of the reference solution (1.0%).
Loss on drying
Take this product, dry it at 105 ℃ to constant weight, and the weight loss shall not exceed 0.5% (general rule 0831).
Ignition residue
Not more than 0.1% (general rule 0841).
heavy metal
Take 0.50g of this product and check it according to the law (General Rule 0821, the third method). The content of heavy metals should not exceed 20 parts per million.
Arsenite
Take 1.0g of this product, add 1g of calcium hydroxide, mix it, add a small amount of water, stir it evenly, heat it with a small fire, burn it until it is completely ashed, cool it, add 5mL of hydrochloric acid and 23mL of water, check according to the law (General Rule 0822, Method 1), and it should meet the requirements (0.0002%).
Assay
Take about 0.5g of this product, weigh it accurately, add 30mL of ethanol, dissolve it at a slight temperature, cool it, add 4 drops of cresol red indicator solution and 1 drop of thymol blue indicator solution, titrate with sodium hydroxide titrant (0.1mol/L) until the solution turns purple red, and correct the titration result with blank test.Every 1mL of sodium hydroxide titrant (0.1mOl/L) is equivalent to 33.07mg CtwelveHelevenClNtwoOfiveS。[3]
Drug description
Announce
edit
classification
Circulating system drugs>antihypertensive drugs>diuretic and antihypertensive drugs
Pharmacodynamics
1. Effect on water and electrolyte excretion: it can increase the excretion of water, sodium, chlorine, potassium, calcium, magnesium, phosphorus, etc.Different from thiazide diuretics, loop diuretics such as furosemide have obvious dose-response relationship.With the increase of the dosage, the diuretic effect was significantly enhanced, and the drug dosage range was large.This kind of drugs mainly inhibit the active reabsorption of NaCl in the thick wall segment of the medullary loop of the renal tubule, resulting in Na in the lumen fluid+、Cl-The concentration increases, while the medullary interstitial fluid Na+、Cl-The decrease of concentration will reduce the osmotic pressure gradient and the concentration function of renal tubules, which will lead to water and Na+、Cl-Increased excretion.Because Na+Decreased reabsorption, distal tubule Na+The concentration increases.Furosemide inhibits Cl reabsorption in thick wall segment of ascending branch of medullary loop of renal tubule-It is believed that there is a chlorine pump in this part, and the research shows that there is a+-K+ATPase related Na+、Cl-Paired transport system, furosemide reduces Na by inhibiting the function of the system+、Cl-Reabsorption of.In addition, furosemide may be able to inhibit Na in proximal tubules and distal tubules+、Cl-And promote the secretion of K by distal tubules+。Furosemide inhibits the effect of Heinz loop on Ca2+、Mg2+Increase Ca due to reabsorption of2+、Mg2+Excretion.Short term medication can increase uric acid excretion, while long-term medication can cause hyperuricemia.
2. Effect on hemodynamics: Furosemide can inhibit the activity of prostaglandin decomposing enzyme, increase the content of prostaglandin E2, and thus has the effect of vasodilation.Expanding renal vessels, reducing renal vascular resistance, and increasing renal blood flow, especially in the deep part of renal cortex, are of great significance in the diuretic effect of furosemide, which is also the theoretical basis for its use in preventing acute renal failure.In addition, unlike other diuretics, loop diuretics do not decrease the glomerular filtration rate when the renal tubular fluid flow increases, which may be related to the decrease of chlorine flowing through the dense spot, thus weakening or blocking the bulb tube balance.Furosemide can dilate the pulmonary volumetric vein, reduce the permeability of pulmonary capillaries, and its diuretic effect can reduce the amount of blood returning to the heart and the end diastolic pressure of the right ventricle, which is helpful to the treatment of acute right heart failure.Furosemide can reduce pulmonary capillary permeability, which provides a theoretical basis for its treatment of adult respiratory distress syndrome.
Pharmacokinetics
The oral absorption rate is 60~70%. Taking food can slow the absorption, but it does not affect the absorption rate and its curative effect.The oral absorption rate of patients with end-stage renal disease decreased to 43~46%.In the case of edema diseases such as congestive heart failure and nephrotic syndrome, the oral absorption rate also decreases due to intestinal wall edema, so drugs should be administered via parenteral route in the above circumstances.It is mainly distributed in extracellular fluid, with an average distribution volume of 11.4% of body weight. The plasma protein binding rate is 91~97%, almost all of which are bound with albumin.The drug can pass through the placental barrier and secrete into milk.After oral administration and intravenous administration, the onset time of the action was 30~60 minutes and 5 minutes, respectively, and the peak time was 1~2 hours and 0.33~1 hour.The duration of action was 6-8 hours and 2 hours respectively.There are great individual differences in the half-life β. The normal person is 30~60 minutes, the anuria patient is 75~155 minutes, and the liver and kidney function is severely damaged at the same time, it is 11~20 hours.The half-life β of neonates was prolonged from 4 to 8 hours due to the poor clearance ability of liver and kidney.88% of the drug is excreted by the kidney in its original form, and 12% is excreted by bile through liver metabolism. The metabolism of patients with impaired renal function increases through liver metabolism.This drug is not cleared by dialysis.
indication
1. Edematous diseases include congestive heart failure, cirrhosis, kidney diseases (nephritis, kidney disease and acute and chronic renal failure caused by various reasons), especially when the effect of other diuretics is poor, the application of this kind of drugs may still be effective.Combined with other drugs to treat acute pulmonary edema and acute brain edema.
2. Hypertension is not the first choice drug for the treatment of primary hypertension in the stepwise therapy of hypertension. However, when thiazide drugs have poor efficacy, especially when accompanied by renal insufficiency or hypertension crisis, this kind of drugs is particularly applicable.
3. The prevention of acute renal failure is used to prevent renal blood perfusion insufficiency caused by various reasons, such as dehydration, shock, poisoning, anesthesia accident and circulatory insufficiency. Timely application can reduce the chance of acute tubular necrosis.
4. Hyperkalemia and hypercalcemia.
5. Dilutive hyponatremia, especially when the blood sodium concentration is below 120 mmol/L.
6. Hypersecretion of antidiuretic hormone (SIADH).
7. Acute drug poisoning, such as barbiturates poisoning.
Usage and dosage
Oral
Common adult consumption:
① Edematous disease: the initial dose is 20~40mg once a day, and 20~40mg is added after 6~8 hours if necessary, until satisfactory diuretic effect appears.The maximum daily dose can reach 600mg, but it should be controlled within 100mg generally, and taken in 2~3 times.Some patients can be reduced to 20-40 mg once, and once every other day (or 20-40 mg a day, 2 to 4 consecutive days a week).
② Hypertension: the initial dose is 40~80mg a day, divided into two times, and the dose should be adjusted as appropriate.
③ Hypercalcemia: 80~120mg a day, divided into 1~3 times.
Commonly used quantity for children
The initial dose of edema disease is 2mg/kg according to body weight. If necessary, 1~2mg/kg is added every 4~6 hours.Newborns should extend the interval of medication.
intravenous injection
Common adult consumption:
① Edematous disease:
a. General dose: the initial dose is 20~40mg, and if necessary, additional dose is added every 2 hours until satisfactory curative effect is achieved.The drug can be administered in several times during the maintenance phase.
b. Acute left heart failure: the initial dose is 40mg, and if necessary, 80mg is added every hour until satisfactory curative effect is achieved.
c. Chronic renal insufficiency: the daily dose is generally 40~120mg.
② Hypertension crisis: the initial dose is 40~80mg. In case of acute left heart failure or acute renal failure, the dosage can be increased as appropriate.
③ Hypercalcemia: 20-80mg once.
Commonly used quantity for children:
Edematous disease: the initial dose is 1mg/kg, and 1mg/kg is added every 2 hours if necessary.The maximum daily dose can reach 6 mg/kg.
Disable and use with caution
1. Cross allergy.People who are allergic to sulfonamides and thiazide diuretics may also be allergic to this drug.
2. This drug can pass through the placental barrier, and pregnant women, especially the first three months of pregnancy, should try to avoid using it.It has no preventive effect on pregnancy induced hypertension syndrome.Animal experiments have shown that this product can cause hydrops in the placenta and renal pelvis, and increase abortion and fetal mortality.
3. This medicine can be secreted through milk, and women in lactation should use it with caution.
4. The half-life of the drug in neonates is obviously prolonged, so the interval of drug use in neonates should be prolonged.
5. The elderly have an increased chance of hypotension, electrolyte disorder, thrombosis and renal function damage when using this drug.
6. Use with caution in the following cases:
① If there is no urine or serious renal function damage, the latter needs to increase the dosage, so the interval between drugs should be extended to avoid ototoxicity and other side effects;
② Diabetes mellitus;
③ Hyperuricemia or gout history;
④ In patients with severe liver function damage, liver coma may be induced due to water electrolyte disorder;
⑤ In acute myocardial infarction, excessive diuresis can induce shock;
⑥ Pancreatitis or a history of this disease;
⑦ People with hypokalemia tendency, especially those who use digitalis or have ventricular arrhythmia;
⑧ Lupus erythematosus, this medicine can aggravate the condition or induce activity;
⑨ Prostate hypertrophy.Hypokalemia, excessive use of digitalis, forbidden for patients with liver coma, and cautious use for patients with advanced cirrhosis.High dose has great ocular toxicity to those with high blood uric acid.
The product can penetrate the placenta, increase the formation of fetal urine, and increase the acid concentration in maternal and fetal serum and amniotic fluid.Therefore, it is necessary for pregnant women to take this product only in the case of heart failure.
Adverse reactions
The common ones are related to water and electrolyte disorders, especially in the case of large dosage or long-term application, such as postural hypotension, shock, hypokalemia, hypochloremia, hypochloremic alkalosis, hyponatremia, hypocalcemia, thirst, fatigue, muscle soreness, arrhythmia, etc.
Rare patients have allergic reactions (including rashes, interstitial nephritis, and even cardiac arrest), blurred vision, yellow vision, photosensitivity, dizziness, headache, anorexia, nausea, vomiting, abdominal pain, diarrhea, pancreatitis, muscle rigidity, etc. Bone marrow suppression leads to granulocytopenia, thrombocytopenic purpura and aplastic anemia, liver function damage, abnormal sensation of fingers and toes,Hyperglycemia, positive urine sugar, aggravated original diabetes, hyperuricemia.Tinnitus and hearing impairment are mostly seen in rapid intravenous injection of large doses (more than 4-5mg per minute), most of which are temporary, and a few are irreversible, especially when used together with other ototoxic drugs.In hypercalcemia, it can cause kidney stones.It has been reported that this drug can aggravate idiopathic edema.It can cause hypokalemia, hypochloremia, decreased blood magnesium, nausea, vomiting, diarrhea, rash, itching, muscle spasm, dizziness, fatigue, lethargy, dry mouth, and temporary deafness if injected too quickly.In individual cases, leukopenia, thrombocytopenia, erythema multiforme, postural hypotension.Long term use may cause gastric and duodenal ulcer, hyperacidemia, gastrointestinal irritation or discomfort, acute pancreatitis, jaundice, and hallucination in individual cases.Intravenous injection may cause cardiac arrest or even death.Cardiovascular system: Furosemide has a short but definite vasodilation effect in addition to diuretic effect.This product can change the venous blood volume and peripheral vascular resistance of patients with kidney damage, resulting in postural hypotension and syncope. When used together with other antihypertensive drugs, the symptoms are more serious.
Endocrine and metabolism: The effect of this product on lipid metabolism is similar to that of thiazide drugs.Furosemide can cause the syndrome of antidiuretic hormone disorder (IADHS). The concentration of antidiuretic hormone (ADH) in patients' plasma increases, the total sodium content of the body is normal, and the total potassium content decreases significantly.If the product is used quickly, it will cause a sharp increase in the secretion of high blood proteasome and aldosterone.Animal experiments show that long-term use of this product leads to thiamine deficiency and damage to heart function.Therefore, attention should be paid to the concentration of thiamine in the blood of patients who use this product for a long time.Similar to thiazide drugs, this product can also lead to high blood uric acid and promote gout, and the frequency and degree of attack are more serious. Older patients may have gout after taking it for 3 months.
Electrolyte and humoral balance: Similar to thiazides, loop diuretics also cause changes in electrolyte balance,
The characteristics and degree of action are different.The incidence is about 23%.
1. Calcium metabolism is different from thiazides. Furosemide does not promote calcium reabsorption in distal renal tubules, but can cause transient hypercalcemia.This product can cause secondary hyperparathyroidism in newborns, resulting in bone calcium loss. The excretion rate of calcium is 10~20 times larger than that of normal children, and there is a risk of formation of kidney stones.There is also the possibility of secondary sepsis.
2. Low blood magnesium. Although this product can increase the renal clearance rate of magnesium, it may not affect the concentration of magnesium in plasma.
3. Liver: Furosemide is very toxic to the liver of animals. In clinical practice, for patients with a history of liver cirrhosis, even taking low doses of this product will accelerate the onset of hepatic encephalopathy. It is better to use spironolactone instead.
4. Digestive system: The incidence of nausea, vomiting and diarrhea is less than 1% under the conventional dosage.However, in case of high dose or uremia, the incidence rate is significantly higher.
5. Urinary system: This product is a strong diuretic.Excessive diuresis and dehydration will cause a temporary decrease in glomerular filtration rate and an increase in blood BUN, which accounts for 8% of adverse reactions.The elderly with enlarged prostate will have acute urinary retention, overflow urinary incontinence and interstitial nephritis.Long term use of this product to treat spontaneous edema will gradually damage renal function, resulting in acute renal failure.
6. Skin: Rashes are common.In case of renal failure, large doses of the product may cause squamous dermatitis and multiple erythroderma, which are rare in other diuretics.
7. Sensory organ: When the blood concentration of the product exceeds 50 μ g/ml, it will cause eye and ear poisoning reactions.Such as glaucoma, vertigo, hearing loss, sometimes irreversible.High blood calcium and the formation of stones in the fetus have also been reported.This product may also cause anaphylactic shock.
Drug interaction
1. Adrenose, mineralocorticoid, adrenocorticotropic hormone and estrogen can reduce the diuretic effect of this drug and increase the chance of electrolyte disorder, especially hypokalemia.
2. Non steroidal anti-inflammatory and analgesic drugs can reduce the diuretic effect of the drug and increase the chance of kidney damage, which is related to the former's inhibition of prostaglandin synthesis and reduction of renal blood flow.
3. When combined with sympathomimetics and anticonvulsants, the diuretic effect is weakened.
4. When used together with clofibrate (antomin), the effects of both drugs are enhanced, and muscle soreness and rigidity may occur.
5. Combined with dopamine, the diuretic effect is strengthened.
6. Alcohol consumption, alcoholic preparations and drugs that can cause blood pressure reduction can enhance the diuretic and antihypertensive effects of the drug;Combined with barbiturates and anesthetics, it is easy to cause orthostatic hypotension.
7. This medicine can reduce uric acid excretion and increase blood uric acid. Therefore, when used in combination with drugs for gout treatment, the dosage of the latter should be properly adjusted.
8. Reduce the efficacy of hypoglycemic drugs.
9. The reduction of the effects of anticoagulants and antifibrinolytic drugs is mainly related to the decrease of blood volume after diuresis, the increase of coagulation factor concentration in blood, and the improvement of liver blood supply and the increase of liver synthetic coagulation factor due to diuresis.
10. This medicine strengthens the effect of non depolarizing muscle relaxants, which is related to the decrease of blood potassium.
11. In combination with amphotericin, cephalosporin, aminoglycosides and other antibiotics, nephrotoxicity and ototoxicity increase, especially when the original kidney is damaged.
When used with antihistamines, the ototoxicity increases, and tinnitus, dizziness, and vertigo are easy to occur.
13. Renal toxicity increased significantly when combined with lithium, which should be avoided as far as possible.
14. After taking chloral hydrate, intravenous injection of this drug can cause sweating, flushing and blood pressure rise, which is related to the increase of thyroxine from the binding state to the free state, leading to the enhancement of catabolism.
15. The combination of sodium carbonate and sodium carbonate increases the chance of hypochlorite alkalosis.
The combined use of thiazides and loop diuretics often leads to serious deterioration of renal function.
This product reduces the clearance rate of aminoglycosides by about 35%, which will increase the risk of eye toxicity and permanent deafness.
The combination of this product with cephalosporins will enhance renal toxicity.
The combination of this product and mannitol will lead to renal failure and strengthen the effect of curare.This product can inhibit the secretion of lithium ions by renal tubules, which may cause lithium poisoning.
Combined use of this product with spironolactone or ACE inhibitor captopril will lead to acute nephrotoxicity and severe hyponatremia.
matters needing attention
1. Minor nausea, diarrhea, drug rash, pruritus, blurred vision and other side effects may occur. Sometimes, standing dizziness, fatigue, fatigue, muscle spasm, thirst may occur. A few cases have leukopenia, and individual cases have thrombocytopenia, erythema multiforme, and orthostatic hypotension.Long term application may cause gastric and duodenal ulcer.
2. Because it can reduce the excretion of uric acid, it can lead to hyperacidemia after multiple applications, and some patients can produce acute gout after long-term application.Use with caution for gout patients.
3. Diabetic patients can increase blood sugar after application;Patients with diabetes should use it with caution.Although its blood glucose rise is far weaker than that of thiazide diuretics, it may still increase blood glucose when combined with hypoglycemic drugs.
4. Due to the rapid and powerful diuretic effect, attention should be paid to the initial dosage to prevent excessive diuresis, which may cause dehydration and electrolyte imbalance.
5. Hepatitis patients are prone to liver coma due to excessive loss of electrolytes (especially K+) after taking it.Use with caution in patients with severe liver dysfunction.
6. When taking large amount of drugs for a long time, the electrolyte concentration in blood should be checked.Patients with obstinate edema are particularly prone to low potassium symptoms. When digitalis or potassium excreting steroids are used at the same time, more attention should be paid to potassium supplementation.
7. At the same time of dehydration, the reversible increase of blood urea nitrogen level can occur. If the creatinine level does not increase significantly and the renal function is not damaged, the product can continue to be used.Use with caution in patients with severe renal insufficiency.
8. During the first month of use, the serum electrolyte, carbon dioxide and blood urea nitrogen levels should be checked regularly.Like other diuretics, when the treatment of kidney disease in progress has increased serum urea nitrogen and oliguria, the drug should be stopped immediately.
9. It can enhance the effect of antihypertensive drugs, so the amount of antihypertensive drugs should be appropriately reduced when combined.
10. Because it is a sulfonamide compound with similar structure to chlorothiazide, which can reduce the reaction of arteries to vasopressin (such as norepinephrine), and can increase the muscle relaxation and paralytic effect of tubocurarine, it should be stopped one week before surgery.
11. It is forbidden for patients with hypokalemia, excessive use of digitalis and liver coma.Patients with advanced cirrhosis should use it with caution.
12. When large doses of intravenous injection are too fast, hearing loss or temporary deafness may occur.It should not be used in combination with aminoglycoside antibiotics, because it is more likely to cause hearing loss.
13. Not for pregnant women.Children should use it with caution.
poisoning
Announce
edit
Furosemide (furosemide) mainly inhibits the effect of medulla and cortex on Cl-And Na+Resorption of, promoting Cl-、Na+、K+And a large amount of water discharged and diuretic.Clinically, it is used to treat cardiac edema, renal edema, cirrhosis ascites, and peripheral edema caused by pulmonary edema, brain edema, acute renal failure or vascular wall disorders.It can be used to accelerate the excretion of poisons in case of drug poisoning.The drug is rapidly absorbed by oral administration. The plasma half-life is 30-70min, about 10% of which is metabolized in the body, and is mainly excreted through the kidney in its original form.The excretion was fast, and there was no obvious retention in the tissue 24 hours later.Oral LD in dogsfifty2g/kg, 0.8g/kg for rabbits and 4.6g/kg for rats.The common dosage is 20mg each time, intramuscular injection or intravenous injection.40mg/d orally.It mainly affects water and salt metabolism, leading to water and electrolyte imbalance and acid-base imbalance.
clinical manifestation
1. Metabolic abnormality
The diuretic effect of this medicine is rapid and powerful, which is easy to cause imbalance of water and electrolyte, dehydration, low blood sodium, low blood potassium, low blood chlorine, low blood magnesium and low chlorine alkalosis.
2. Digestive system
Nausea, vomiting, burning sensation of the mouth and stomach, anorexia, abdominal pain, diarrhea, constipation, large doses can cause gastric and duodenal ulcers and bleeding, acute pancreatitis, jaundice, and liver encephalopathy in patients with cirrhosis.
3. Circulation system
Postural hypotension, syncope, arrhythmia (atrioventricular block was reported in some cases), thromboangiitis, etc.
4. Urinary system
Low back pain, frequent urination, hematuria, oliguria, elevated blood urea nitrogen, urine sugar, hyperuricemia, acute kidney exhaustion, etc.
5. Central nervous system and ototoxicity
There may be headache, dizziness, dizziness, abnormal sensation, tinnitus, hearing loss or temporary deafness, hearing loss.
