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Bumetanide injection

Function and Efficacy

The effect on water and electrolyte excretion is basically the same as furosemide, and its diuretic effect is 20 to 60 times that of furosemide. It mainly inhibits the active reabsorption of NaCl by the thick wall segment of the ascending limb of the renal tubular loop of Henle, and also inhibits the reabsorption of Na+ in the proximal tubule, but has no effect on the distal tubule, so the potassium excretion effect is less than furosemide. It can inhibit the activity of prostaglandin degrading enzymes, increase the content of prostaglandin E2, and thus have a vasodilatory effect. Dilation of renal blood vessels, reduction of renal vascular resistance, and increase of renal blood flow, especially deep renal cortical blood flow, are of great significance in the diuretic effect of bumetanide, and are also the theoretical basis for its use in the prevention of acute renal failure. In addition, unlike other diuretics, loop diuretics increase the flow of renal tubular fluid while the glomerular filtration rate does not decrease, which may be related to the reduction of chloride flowing through the macula densa, thereby weakening or blocking the glomerular-tubular balance. Bumetanide can dilate the pulmonary capacitance veins and reduce the permeability of pulmonary capillaries. Its diuretic effect can reduce the amount of blood returning to the heart and the left ventricular end-diastolic pressure, which is helpful for the treatment of acute left heart failure. Since bumetanide can reduce the permeability of pulmonary capillaries, it provides a theoretical basis for its treatment of adult respiratory distress syndrome.

Ingredients

The main ingredient of this product is bumetanide. Its chemical name is 5-n-butylamino-4-phenoxy-3-aminosulfonylbenzoic acid. Molecular formula: C17H20N2O5S Molecular weight: 364.42

Name Description Content CAS NO. Manufacturer
BumetanideIngredients

The effect on water and electrolyte excretion is basically the same as furosemide, and its diuretic effect is 20 to 60 times that of furosemide. It mainly inhibits the active reabsorption of NaCl by the thick wall segment of the ascending limb of the renal tubular loop of Henle, and also inhibits the reabsorption of Na+ in the proximal tubule, but has no effect on the distal tubule, so the potassium excretion effect is less than furosemide. It can inhibit the activity of prostaglandin degrading enzymes, increase the content of prostaglandin E2, and thus have a vasodilatory effect. Dilation of renal blood vessels, reduction of renal vascular resistance, and increase of renal blood flow, especially deep renal cortical blood flow, are of great significance in the diuretic effect of bumetanide, and are also the theoretical basis for its use in the prevention of acute renal failure. In addition, unlike other diuretics, loop diuretics increase the flow of renal tubular fluid while the glomerular filtration rate does not decrease, which may be related to the reduction of chloride flowing through the macula densa, thereby weakening or blocking the glomerular-tubular balance. Bumetanide can dilate the pulmonary capacitance veins and reduce the permeability of pulmonary capillaries. Its diuretic effect can reduce the amount of blood returning to the heart and the left ventricular end-diastolic pressure, which is helpful for the treatment of acute left heart failure. Since bumetanide can reduce the permeability of pulmonary capillaries, it provides a theoretical basis for its treatment of adult respiratory distress syndrome.

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Appearance

This product is a colorless clear liquid.

Indication

1. Edema diseases include congestive heart failure, cirrhosis, kidney disease (nephritis, nephropathy and acute and chronic renal failure caused by various reasons), especially when other diuretics are ineffective, this type of drug may still be effective. Used in combination with other drugs to treat acute pulmonary edema and acute cerebral edema. 2. Hypertension In the step therapy of hypertension, it is not the first choice for the treatment of primary hypertension, but when thiazide drugs are ineffective, especially when accompanied by renal insufficiency or hypertensive crisis, this type of drug is particularly suitable. 3. Prevention of acute renal failure It is used for insufficient renal blood perfusion caused by various reasons, such as dehydration, shock, poisoning, anesthesia accidents and circulatory insufficiency. Timely application while correcting insufficient blood volume can reduce the mechanism of acute tubular necrosis.

Usage and Dosage

1. For adults to treat edema or hypertension, the initial dose is 0.5-1 mg intravenously or intramuscularly, and if necessary, repeat every 2-3 hours. The maximum dose is 10 mg per day. For acute pulmonary edema, the initial dose is 1-2 mg intravenously, and if necessary, repeat every 20 minutes. It can also be diluted to 2-5 mg and slowly dripped (not less than 30-60 minutes). 2. For children, the initial dose is 0.01-0.02 mg/kg per body weight intramuscularly or intravenously, and if necessary, once every 4-6 hours.

Adverse Reactions

Common symptoms are related to water and electrolyte disorders, especially when used in large doses or for a long time, such as postural hypotension, shock, hypokalemia, hypochloremia, hypochloremic alkalosis, hyponatremia, hypocalcemia, and related thirst, fatigue, muscle aches, arrhythmias, etc. Rare symptoms include allergic reactions (including rashes and even cardiac arrest), dizziness, headache, anorexia, nausea, vomiting, abdominal pain, diarrhea, pancreatitis, muscle rigidity, bone marrow suppression leading to granulocytopenia, thrombocytopenic purpura and aplastic anemia, liver damage, paresthesia of fingers (toes), hyperglycemia, positive urine sugar, aggravation of existing diabetes, and hyperuricemia. Tinnitus and hearing impairment are more common when large doses are injected intravenously rapidly (doses greater than 4-15 mg per minute), and are mostly temporary, and a few are irreversible, especially when used simultaneously with other ototoxic drugs. In the case of hypercalcemia, kidney stones may be caused. There are also reports that this drug can aggravate idiopathic edema. Occasionally, unmarried men may experience spermatorrhea and difficulty in penile erection. Large doses may cause muscle aches and chest pains. The effect on glucose metabolism may be less than that of furosemide.

Precautions

1. Patients who are allergic to this product, sulfonamides, and thiazide diuretics are contraindicated. 2. Pregnant women within three months of pregnancy are contraindicated.

Special Population Medication

Precautions for children: The half-life of this drug is significantly prolonged in newborns, so the interval between doses for newborns should be extended. Precautions for pregnancy and lactation: 1. This drug can pass through the placental barrier, so pregnant women, especially those in the first 3 months of pregnancy, should avoid using it as much as possible. It has no preventive effect on pregnancy-induced hypertension syndrome. Animal experiments have shown that this product can cause fetal hydronephrosis, delay fetal growth and ossification, and increase miscarriage and fetal mortality. 2. This drug can be secreted through breast milk, so lactating women should use it with caution. Precautions for the elderly: When the elderly use this drug, they are more likely to experience hypotension, electrolyte imbalance, thrombosis and renal damage.

Drug Interactions

1. Adrenal glucose, mineralocorticoids, adrenocorticotropic hormone and estrogen can reduce the diuretic effect of this drug and increase the chance of electrolyte disorders, especially hypokalemia; 2. Non-steroidal anti-inflammatory analgesics can reduce the diuretic effect of this drug and increase the chance of renal damage, which is related to the former inhibiting prostaglandin synthesis and reducing renal blood flow; 3. When used in combination with sympathomimetic drugs and anticonvulsant drugs, the diuretic effect is weakened; 4. When used in combination with clofibrate (clofibrate), the effects of both drugs are enhanced, and muscle soreness and stiffness may occur; 5. When used in combination with dopamine, the diuretic effect is enhanced; 6. Drinking alcohol, alcohol-containing preparations and drugs that can cause a drop in blood pressure can enhance the diuretic and antihypertensive effects of this drug; when used in combination with barbiturates and anesthetics, it is easy to cause orthostatic hypotension; 7. This drug can reduce uric acid excretion and increase blood uric acid, so when used in combination with drugs for the treatment of gout, the latter's dose should be appropriately adjusted. Adjustment; 8 Reduce the efficacy of hypoglycemic drugs; 9 Reduce the effects of anticoagulants and antifibrinolytic drugs, mainly due to the decrease in blood volume after diuresis, which leads to an increase in the concentration of coagulation factors in the blood, and diuresis improves the blood supply to the liver and increases the synthesis of coagulation factors in the liver; 10 This drug enhances the effect of non-depolarizing muscle relaxants, which is related to the decrease in blood potassium; 11 When used in combination with antibiotics such as amphotericin, cephalosporin, and aminoglycosides, nephrotoxicity and ototoxicity increase, especially when there is original renal damage; 12 When used in combination with antihistamines, ototoxicity increases, and tinnitus, dizziness, and vertigo are prone to occur; 13 When used in combination with lithium, nephrotoxicity is significantly increased and should be avoided as much as possible; 14 After taking chloral hydrate, intravenous injection of this drug can cause sweating, facial flushing and increased blood pressure, which is related to the increase in the conversion of thyroid hormone from a bound state to a free state, leading to enhanced catabolism; 15 When used in combination with sodium bicarbonate, the chance of hypochloremic alkalosis increases.

Storage

Keep away from light and store in sealed container.

Packaging Specification

2ml:1.0mg

Validity Period

24 months

Manufacturer

Liaoning Yuhuang Pharmaceutical Co., Ltd.

  • Founded in:

    2005-01-26
  • Address:

    No. 5-5, Jialin Road, Sujiatun District, Shenyang City, Liaoning Province
  • Tax NO.:

    912101117695668202
  • Registered Funds:

    14 million yuan
  • Email:

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