Introduction to furosemide

Contents 1 Pinyin 2 English Reference 3 National Essential Medicines 4 Overview 5 Furosemide Pharmacopoeia Standard 5.1 Product Name 5.1.1 Chinese Name 5.1.2 Chinese Pinyin 5.1.3 English Name 5.2 Structural Formula 5.3 Molecular Formula and Molecular Weight 5.4 Source (name), content (potency) 5.5 Properties 5.5.1 Melting point 5.5.2 Absorption coefficient 5.6 Identification 5.7 Inspection 5.7.1 Clarity and color of alkaline solution 5.7.2 Chloride 5.7.3 Sulfate 5.7.4 Related substances 5.7.5 Weight loss on drying 5.7.6 Residue on ignition 5.7.7 Heavy metals 5.7.8 Arsenic salt 5.8 Content determination 5.9 Category 5.10 Storage 5.11 Preparation 5.12 Version 6 Furosemide instructions 6.1 Drug name 6.2 English name 6.3 Alias ??of furosemide 6.4 Classification 6.5 Dosage form 6.6 Pharmacological effects of furosemide 6.7 Pharmacokinetics of furosemide 6.8 Indications of furosemide 6.9 Contraindications of furosemide 6.10 Precautions 6.11 Adverse reactions of furosemide 6.12 Usage and dosage of furosemide 6.13 Interactions between furosemide and other drugs 6.14 Expert comments 7 Furosemide poisoning 7.1 Clinical manifestations 7.2 Treatment 8 References attached: * Other versions of furosemide related drug instructions 1 Pinyin

fū sāi mǐ 2 English Reference

frusemide [Xiangya Medical Professional Dictionary]

furosemide [Landau Chinese-English Dictionary]

DiuralFurosemide [Xiangya Medical Professional Dictionary] 3 National Essential Medicines

National essential drug retail price guidance information related to furosemide

Serial number essential drug

Catalog serial number drug name dosage form specification unit retail index

Price Category Notes 868 127 Furosemide Tablets 20mg*100 Box (Bottle) 5.2 Chemical Drugs and Biological Products Part* 869 127 Furosemide Tablets 20mg*10 Box (Bottle) 0.57 Chemical Drugs and Biological Products Part 870 127 Furosemide tablets 20mg*20 box (bottle) 1.1 Chemical drugs and biological products part 871 127 Furosemide tablets 20mg*50 box (bottle) 2.7 Chemical drugs and biological products part 872 127 Furosemide injection 20mg: 2ml bottle (tube) 0.52 Chemicals and biological products* 873 127 Furosemide injection 20mg (lyophilized powder) Bottle (tube) 3.5 Chemicals and biological products 874 127 Furosemide injection 40mg (lyophilized powder) bottle ( Branch) 6 Chemicals and biological products

Note:

1. Those marked with "*" in the remarks column in the table are representative products.

2. If the representative dosage form specifications in the table are marked with "△" in the remarks column, the prices of the representative dosage form specifications and related specifications with a clear price difference relationship are provisional prices. 4 Overview

Furosemide is a diuretic, a white or off-white crystalline powder; odorless and almost tasteless. It mainly inhibits the reabsorption of Cl and Na+ in the medullary part of the ascending branch of the medullary loop and cortex of the kidney, and promotes the excretion of large amounts of Cl, Na+, K+ and water to act as a diuretic. It is clinically used to treat cardiac edema, renal edema, liver cirrhosis ascites, pulmonary edema, cerebral edema, acute renal failure or peripheral edema caused by blood vessel wall disorders. In case of drug poisoning, it can be used to accelerate the excretion of poison. It mainly affects water and salt metabolism, leading to disorders of water and electrolyte balance and acid and salt balance.

5 Furosemide Pharmacopoeia Standard 5.1 Product name 5.1.1 Chinese name

Furosemide 5.1.2 Chinese Pinyin

Fusa1ml 5.1.3 English name

Furosemide 5.2 Structural formula 5.3 Molecular formula and molecular weight

C12H11ClN2O5S? 330.75 5.4 Source (name), content (potency)

This product is 2[(2furanmethyl)amino]5(aminosulfonate) Acyl) 4-chlorobenzoic acid. Calculated as dry product, the content of C12H11ClN2O5S shall not be less than 99.0%. 5.5 Properties

This product is a white or off-white crystalline powder; odorless and almost tasteless.

This product is soluble in acetone, slightly soluble in ethanol, and insoluble in water. 5.5.1 Melting point

The melting point of this product (Appendix VI C of Pharmacopoeia Part 2, 2010 Edition) is 208~213℃, and it decomposes when melted. 5.5.2 Absorption coefficient

Take this product, weigh it accurately, add 0.4% sodium hydroxide solution to dissolve and quantitatively dilute it to make a solution containing about 10 μg per 1ml, and measure it by UV-visible spectrophotometry ( According to the 2010 edition of Pharmacopoeia Part II, Appendix IV A), the absorbance is measured at a wavelength of 271 nm, and the absorption coefficient ( ) is 565 to 595. 5.6 Identification

(1) Take about 25 mg of this product, add 5 ml of water, add sodium hydroxide test solution dropwise to dissolve it, add 1 to 2 drops of copper sulfate test solution, and a green precipitate will form.

(2) Take 25 mg of this product and place it in a test tube. Add 2.5 ml of ethanol to dissolve it. Then add 2 ml of p-dimethylaminobenzaldehyde test solution dropwise along the wall of the tube. It will appear green and gradually change to deep red.

(3) Take this product, add 0.4% sodium hydroxide solution to make a solution containing about 5 μg per 1ml, and measure it according to UV-visible spectrophotometry (2010 edition of Pharmacopoeia, Part 2, Appendix IV A) , with maximum absorption at wavelengths of 228nm, 271nm and 333nm.

(4) The infrared light absorption spectrum of this product should be consistent with the control spectrum (Figure 184 of "Drug Infrared Spectrum Collection"). 5.7 Check the clarity and color of 5.7.1 alkaline solution

Take 0.50g of this product, add 5ml of sodium hydroxide test solution to dissolve, then add 5ml of water. The solution should be clear and colorless; if it is turbid, dissolve it with Compared with the No. 2 turbidity standard solution (2010 edition of Pharmacopoeia, Part II, Appendix IX B), it shall not be more concentrated; if color develops, it shall not be compared with the yellow No. 3 standard colorimetric solution (2010 edition of Pharmacopoeia, Part II, Appendix IX A, Method 1). Deeper. 5.7.2 Chloride

Take 2.0g of this product, add 100ml of water, shake it thoroughly, and filter; take 25ml of the filtrate, check it according to the law (Appendix VIII A of the 2010 edition of Pharmacopoeia Part 2), and compare it with the standard chlorination Compared with the control solution made from 7.0 ml of sodium solution, it must not be more concentrated (0.014%). 5.7.3 Sulfate

Take 25ml of the remaining filtrate under the above chloride item, check it according to the law (Appendix VIII B of Part II of the 2010 edition of the Pharmacopoeia), and compare it with the control solution made of 2.0ml of standard potassium sulfate solution. No more concentrated (0.04%). 5.7.4 Related substances

Avoid light operation. Take this product, add mixed solvent (take 22ml of glacial acetic acid, add acetonitrile-water (1:1) to 1000ml, mix), dissolve and dilute to make a solution containing approximately 1mg per 1ml, as the test solution; precise measurement Take an appropriate amount and quantitatively dilute it with the above mixed solvent to prepare a solution containing 10 μg per 1 ml. Use it as a control solution for testing according to the high performance liquid chromatography method (2010 edition of Pharmacopoeia, Appendix V D), and use octadecylsilane to bond the silica gel. Use water-tetrahydrofuran-glacial acetic acid (70:30:1) as the mobile phase, and the detection wavelength is 272nm. The theoretical plate number is not less than 4000 based on the furosemide peak. Inject 20 μl of the control solution into the liquid chromatograph. , adjust the detection sensitivity so that the peak height of the main component chromatographic peak is approximately 20% of the full scale, then accurately measure 20 μl each of the test solution and the control solution, and inject them into the liquid chromatograph respectively, and record the chromatogram until the main component peak is retained. 3 times the time, 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 control solution, and the sum of the peak areas of each impurity shall not be greater than the main peak area of ??the control solution (1.0 %). 5.7.5 Weight loss on drying

Take this product and dry it to constant weight at 105°C. The weight loss shall not exceed 0.5% (Appendix VIII L of the 2010 edition of the Pharmacopoeia). Residues

must not exceed 0.1% (2010 edition of Pharmacopoeia, Part II, Appendix VIII N) 5.7.7 Heavy metals

Take 0.50g of this product and inspect according to law (2010 edition of Pharmacopoeia, Part II, Appendix VIII). H Third Law), the content of heavy metals shall not exceed 20 parts per million.

5.7.8 Arsenic salt

Take 1.0g of this product, add 1g of calcium hydroxide, mix, add a small amount of water, stir evenly, first heat over low heat, then blanch until completely ashes, let cool, add hydrochloric acid 5ml and 23ml of water, check according to the law (Appendix VIII J, Method 1 of Part II of the Pharmacopoeia 2010), and it should comply with the regulations (0.0002%). 5.8 Content determination

Take about 0.5g of this product, weigh it accurately, add 30ml of ethanol, dissolve it at a slight temperature, let it cool, add 4 drops of cresol red indicator solution and 1 drop of thymol blue indicator solution. Titrate with sodium hydroxide titrant (0.1 mol/L) until the solution turns purple, and correct the titration results with a blank test. Each 1ml of sodium hydroxide titrant (0.1mol/L) is equivalent to 33.07mg of C12H11ClN2O5S. 5.9 Category

Diuretics. 5.10 Storage

Protect from light and seal. 5.11 Preparations

(1) Furosemide Tablets? (2) Furosemide Injection? (3) Compound Furosemide Tablets Version 5.12

"The People's Republic of China and Chinese Pharmacopoeia 2010 Edition 6 Furosemide Instructions 6.1 Drug Name

Furosemide 6.2 English Name

Furosemide 6.3 Alias ??of Furosemide

Furosemide; Diuretic acid; Furosemide; Diuretic acid; Ascites; Ascites; Fulo tablets; Furosemide; Frusemide; Lasix; Frusemide 6.4 Classification

Circulatory system drugs> Antihypertensive drugs> Diuretic and antihypertensive drugs 6.5 dosage forms

1. Tablets: 20mg per tablet; 40mg.

2. Injection: 20mg (2ml). 6.6 Pharmacological effects of furosemide

Furosemide is a short-acting and powerful sulfonamide diuretic. It acts on the thick ascending branch of the medullary loop and works by inhibiting the active reabsorption of Cl- and the passive reabsorption of Na. Due to the reduced reabsorption of NaCl, the osmotic concentration of the renal medullary interstitium decreases, the concentration function decreases, and the urine output increases. Furosemide can dilate arterioles and reduce peripheral resistance, thereby reducing the burden on the left heart. It also rapidly reduces blood volume and blood return volume through its powerful diuretic effect, thereby reducing the burden on the left heart. Furosemide inhibits the reabsorption of Na+ and Cl- in the medullary and cortical parts of the ascending branch of the medullary loop, promoting the excretion of large amounts of Na+, Cl-, K+ and water. It also blocks the reabsorption of Mg2+ and Ca2+ by the renal tubules. Increases the excretion of Mg2+ and Ca2+, and its natriuretic effect is stronger than that of thiazide diuretics. Furosemide can dilate renal blood vessels, increase renal blood flow, and adjust renal blood flow distribution. 6.7 Pharmacokinetics of furosemide

After oral administration, it is rapidly absorbed in the gastrointestinal tract but incompletely. The bioavailability is 50% to 75%. It takes effect in about 30 minutes. The time to reach peak plasma drug concentration is 1h, the effect lasts 4h. It takes effect 5 minutes after intravenous injection. The urinary Na+ excretion within 30 minutes can be up to 25 times that before administration, and the urinary output within 24 hours can reach 8-10L. The plasma half-life is 0.2~0.25h. In cases of renal insufficiency, the half-life can be extended to 10 hours, and the plasma protein binding rate is 95% to 99%. However, in patients with uremia and renal disease, the protein binding rate is reduced. The distribution concentration in the liver is high, and about 1/3 is excreted from the bile into the intestine through the liver and excreted in the feces. Only small amounts are metabolized in the liver. Furosemide is partially metabolized in the body (10%). The main metabolite is the furylmethyl derivative 2-amino-4-chloro-5-sulfamoylbenzoic acid. It is excreted by the kidneys as the original drug and a small amount of metabolites. In cases of renal insufficiency, it can be Excreted in feces via bile. Most of it is secreted into the lumen by the proximal convoluted tubule epithelium and excreted unchanged from the body. The half-life is about 2 hours, and can be extended to 10 hours in patients with advanced age, renal insufficiency or uremia. Because the drug is excreted quickly, repeated administration is less likely to cause accumulation. 6.8 Indications of furosemide

It is used for various types of edema in the heart, liver, and kidneys, as well as acute pulmonary edema, heart failure, renal failure, and toxic excretion hypercalcemia. When the patient's renal filtration rate is low (less than 10ml per minute) or chlorthalidone is ineffective, furosemide still has a diuretic effect. Its action is not affected by changes in the acid-binder balance. Adjuvant treatment of hypertensive crisis. 6.9 Contraindications of furosemide

1. Appropriate supplementation of potassium salt is appropriate during long-term use, and is contraindicated in patients with hypokalemia.

2. Furosemide can be excreted in breast milk and has teratogenic effects. It is contraindicated in pregnant and breastfeeding women.

3. It is prohibited for patients with hepatic encephalopathy. 6.10 Precautions

1. Use with caution in patients with severe liver and kidney dysfunction, diabetes, gout, lactating women, and children. It has cross-allergic reactions with sulfonamide drugs. People who are allergic to sulfonamide drugs should use it with caution or should not use it.

2. If there is an increase in serum urea nitrogen and oliguria during treatment, the drug should be discontinued.

3. Patients with refractory edema who take furosemide are prone to hypokalemia and should be given potassium salts at the same time.

4. Since furosemide can reduce the excretion of uric acid, it can cause hyperuricemia and induce acute gout attacks, so patients with gout should use it with caution. 6.11 Adverse reactions of furosemide

Long-term medication can lead to a sharp decrease in extracellular fluid, and hemoconcentration can lead to electrolyte disorders, mainly including hyponatremia, hypokalemia, hypomagnesemia and hypochloride poisoning. . High-dose intravenous injection can cause tinnitus, hearing loss or temporary deafness. Permanent deafness is rare. It can lead to hyperuricemia and induce gout. Combination with triamterene can reduce the incidence of this reaction. Symptoms such as nausea, vomiting, abdominal pain, diarrhea, and even gastric bleeding may occur. Ulcers may occur after prolonged use. Occasionally, granulocytopenia, thrombocytopenia, erythema multiforme, hearing impairment, orthostatic hypotension, hemolytic anemia, allergic interstitial nephritis, etc. may occur. Intravenous injection may also cause arrhythmia. In rare cases, pancreatitis may occur after use, and liver dysfunction may cause jaundice. Long-term use may cause gastric and duodenal ulcers. 6.12 Usage and dosage of furosemide

1. Initially, 20 to 40 mg once a day or 40 mg once every other day, then 20 mg each time, 2 to 3 times a day, and the maximum dose is 120 mg per day. . The initial dose for children is 1 to 2 mg/kg per day. For long-term users (7 to 10 days), the diuretic effect of the drug disappears, and intermittent therapy should be used, with administration for 1 to 3 days and drug withdrawal for 2 to 4 days.

2. Intramuscular injection or intravenous injection: 20 to 40 mg each time, diluted with sodium chloride injection and then infused slowly, once every other day.

3. Acute pulmonary edema: The starting dose for intravenous injection in adults is 40 mg, and then give it after 60 to 90 minutes.

4. Acute renal failure: Adults can start with 40 to 80 mg and gradually increase to achieve the required diuretic effect, but the total amount required in 24 hours rarely exceeds 500 mg. When injecting large doses intravenously, the injection rate should not exceed 4 mg per minute to avoid damage to the auditory nerve. The intensity of furosemide's effect is dose-related. The general dosage range is 40 to 200 mg per day. Plasma volume depletion must be ruled out before use in patients with oliguria. Oral administration: Adults can start with 20 to 80 mg, preferably once in the morning. If no diuretic effect occurs, the dose can be increased every 6 to 8 hours. The effective maintenance dose varies greatly, and a clear upper limit has not yet been proposed. Some reports suggest that the maximum dose is 600 mg. One or two large doses are more effective than multiple small doses, especially for patients with reduced renal function. Furosemide can be administered every day, every other day, or 2 to 4 days a week. Some patients with refractory edema may benefit best from intermittent medication. 6.13 Drug interactions

It can cause hyperuricemia and induce gout. Combination with triamterene can reduce the incidence of this reaction. Concomitant use with nephrotoxic antibiotics (cefotaxime, polymyxin, kanamycin, gentamicin, etc.) can aggravate the risk of nephrotoxicity and ototoxicity, and reduce the clearance rate of cefotaxime. Sometimes it can cause acute renal failure. When combined with amiodarone, benzyl bromide, quinidines, and sotalol, it may cause torsade de pointes arrhythmia, and hypokalemia should be prevented. Combined use with glucose, mineralocorticoids, and amphotericin B may cause hypokalemia, and serum potassium should be monitored. Concomitant use with phenytoin may reduce the diuretic effect by up to 50%. Combined use with aspirin can increase uric acid and cause acute gout. Probenecid can prolong the half-life of furosemide and increase its diuretic effect, but it has the risk of increasing serum uric acid, so its combined use should be avoided in patients with gout. Barbiturates and pethidine (Meperidine) can significantly weaken the diuretic effect of furosemide. Combined use with drugs such as clofibrate (clofibrate) and tealin can extend the half-life of the latter, increase blood concentration, and increase toxic effects. Respiratory muscle paralysis can easily occur when combined with muscle relaxants. Injections precipitate when exposed to acid. Furosemide is incompatible with calcium gluconate, vitamin C, tetracyclines, urea, and epinephrine. Furosemide should not be used in combination with aminoglycoside antibiotics. Furosemide can increase the effect of antihypertensive drugs, and the dosage of antihypertensive drugs should be reduced when used together. 6.14 Expert Comments

According to domestic reports, 11 cases of anterior chamber failure were treated with glaucoma filtering surgery after ineffective treatment with mydriatics, acetate, mannitol and other drugs and follicle compression bandages. Add 20 to 40 mg of furosemide to 60 ml of 50% glucose injection for intravenous injection once a day. The anterior chamber will form and return to normal 2 to 5 days after administration. Another report showed that for neonatal transient hyperglycemia, when the diuretic effect is poor, good curative effects can be achieved by increasing the dosage daily until 160 mg per day is intravenously injected or taken orally. Intramuscular injection of furosemide combined with antibiotics was used to treat 50 cases of severe pneumonia in children, and the hospitalization time of the sick children was shortened by 3 days. 13 cases of leptospirosis complicated with acute renal failure were treated with high-dose furosemide 60 to 100 mg intravenously every 1 to 2 hours and doubled until diuretic reaction occurred. The total dosage in 24 hours was (1.5±0.2) g. 10 cases were cured without any adverse effects. reaction.

A large dose of 2.5 to 3.5 mg/kg is injected intravenously into 40 ml of 10% glucose injection each time to rescue acute cerebral edema and acute pulmonary edema. Repeat every 2 to 4 hours for 2 to 4 times. Approximately after the first dose The patient will urinate a lot in 15 to 20 minutes, and the symptoms will begin to improve in 5 ± 1 minutes. It is characterized by fast action, significant curative effect, few adverse reactions, and will not cause hypokalemia. Concomitant diuretics are the most powerful diuretics currently in clinical use. They act quickly and reliably. They are suitable for edema caused by various causes. They are the first choice drug for acute pulmonary edema. Among loop diuretics, furosemide has relatively mild adverse reactions, is relatively safe, and is favored by most clinicians. The biggest adverse reaction of this drug is water and electrolyte imbalance, especially hypokalemia, which should be avoided as much as possible, because hypokalemia can often cause severe ventricular arrhythmia, which is particularly dangerous in patients with organic heart disease. 7 Furosemide poisoning

Furosemide (furosemide) mainly inhibits the reabsorption of Cl and Na+ in the medullary part of the ascending medullary loop and cortex of the kidney, and promotes the large amount of Cl, Na+, K+ and water. Excretion and diuresis. It is clinically used to treat cardiac edema, renal edema, liver cirrhosis ascites, pulmonary edema, cerebral edema, acute renal failure or peripheral edema caused by blood vessel wall disorders. In case of drug poisoning, it can be used to accelerate the excretion of poison. This drug is rapidly absorbed after oral administration, with a plasma half-life of 30 to 70 minutes. About 10% of the drug is metabolized in the body and is mainly excreted unchanged through the kidneys. Excretion is rapid, and there is no obvious retention in tissues after 24 hours. The oral LD50 is 2g/kg for dogs, 0.8g/kg for rabbits, and 4.6g/kg for rats. The usual dosage is 20mg each time, intramuscular injection or intravenous injection. Orally administered 40 mg/d. It mainly affects water and salt metabolism, leading to disorders of water and electrolyte balance and acid and salt balance. [1] Human body surface area calculator BMI index calculation and evaluation Female safe period calculator Pregnancy date calculator Normal weight gain during pregnancy Safety classification of medications during pregnancy (FDA) Five elements and eight characters Adult blood pressure evaluation Body temperature level evaluation Diabetes diet recommendations Clinical biochemistry common unit conversion Basal metabolic rate calculation, sodium supplementation calculator, iron supplementation calculator, prescription commonly used Latin abbreviations, quick check of common pharmacokinetic symbols, quick check of effective plasma osmolality calculator, ethanol intake calculator

Medical Encyclopedia, now calculate! 7.1 Clinical manifestations

Adverse reactions are as follows [2]:

1. Metabolic abnormalities

This drug has a rapid and powerful diuretic effect and can easily cause water and electrolyte balance. Disorders may lead to dehydration, hyponatremia, hypokalemia, hypochloremia, hypomagnesemia and hypochloremia.

2. Digestive system

Nausea, vomiting, burning sensation in the mouth and stomach, anorexia, abdominal pain, diarrhea, constipation, large doses can cause gastric and duodenal ulcers and bleeding , acute pancreatitis, jaundice, and can induce hepatic encephalopathy in patients with liver cirrhosis.

3. Circulatory system

*** Hypotension, syncope, arrhythmia (individual reports causing atrioventricular block), embolic vasculitis, etc.

4. Urinary system

Low back pain, frequent urination, hematuria, oliguria, elevated blood urea nitrogen, urine sugar, hyperuricemia, acute renal failure, etc.

5. Central nervous system and ototoxicity

May cause headache, dizziness, vertigo, abnormal sensation, tinnitus, hearing loss or temporary deafness or hearing loss.

6. Allergic reactions

Skin itching, urticaria, erythema multiforme, purpura, photosensitivity, exfoliative dermatitis, occasionally bullous hemorrhagic dermatitis and allergic asthma , anaphylactic shock, etc.

7. Others

Fatigue, tiredness, thirst, muscle spasm, hyperglycemia, acute gout, lupus erythematosus activity, etc. Occasionally a man *** feminizes. 7.2 Treatment

The key points in the treatment of furosemide poisoning are [3]:

1. Those poisoned by oral administration of large doses should induce vomiting and gastric lavage immediately.

2. Replenish fluids and potassium salts to correct water and electrolyte imbalances.