Torasemide Injection
Torasemide Injection

[Indications] For patients with congestive heart failure, cirrhosis, ascites, and kidney diseases requiring rapid diuresis or oral diuretics.

[Name of drug]
Torasemide Injection

Trade name:Li Quan

Chinese Name: 托拉塞米注射液

Chinese Pinyin: Tuolasaimi zhusheye

 

[Ingredients] Torasemide

Chemical name: 1- isopropyl -3-[(4-, toluene, amino, -3- pyridyl) sulfonyl] urea

Chemical formula:

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Molecular formula: C16H20N4O3S

Molecular weight: 348.43

All auxiliary components: Polyethylene glycol 400, sodium hydroxide.

 

[Character] This product is colorless or nearly colorless transparent liquid.

[Indications] For patients with congestive heart failure, cirrhosis, ascites, and kidney diseases requiring rapid diuresis or oral diuretics.

[Specification] 2ml:10mg

[Usage and Dosage]

Edema, ascites of cirrhosis of the liver caused by congestive heart failure: the initial dose of 5mg (half) or l0mg (1), once a day, intravenous injection, can also use 5% glucose solution or saline diluted intravenous infusion; if the satisfied effect can increase the dose to 20mg (2). Once a day, the maximum daily dose of 40mg (4), the course is not more than a week. Edema caused by kidney disease, the initial dose of 20mg (2), once a day, according to the needs of the gradual increase in dosage to the maximum dose of 100mg (10 per day), the course of treatment is not more than a week.

 

[Adverse Effects]

The common adverse reactions were headache, dizziness, fatigue, anorexia, muscle cramps, nausea and vomiting, high blood glucose, hyperuricemia, constipation and diarrhea; a large number of long-term use of water and electrolyte imbalance may occur. Polyuria occurs early and treatment of older patients, individual patients due to blood concentration caused by low blood pressure, mental disorder, thrombotic complications and cardiac or cerebral ischemia induced arrhythmia, angina, acute myocardial infarction or fainting, hypokalemia can occur in low potassium diet, vomiting, diarrhea, excessive use of laxatives and patients with abnormal liver functions. Individual patients may have skin allergies, occasionally itching, rash, photosensitive reactions, rare dry mouth, limb abnormalities, visual impairment.

[Contraindicated]

No urine in patients with renal failure, hepatic precoma or hepatic coma patients, for this product or sulfonylurea allergic patients, low blood pressure, low blood volume, low potassium or hyponatremia, severe dysuria (such as hypertrophy of the prostate) patients to disable this product.

 

[Matters Needing Attention]

1, The use of this product should be regularly checked electrolytes (especially blood potassium), blood sugar, uric acid, creatinine, blood lipids and so on.
2, Before the beginning of this treatment, voiding disorders must be corrected, especially in elderly patients or at the beginning of treatment, to carefully monitor the inadequacy of electrolytes and blood volume and related symptoms of blood concentration.
3, Patients with ascites due to cirrhosis should be treated in the hospital when they are treated with diuresis. These patients, such as excessive diuresis, can cause severe electrolyte disturbances and hepatic coma.
4, This product may be used with aldosterone antagonists or with potassium sparing drugs to prevent hypokalemia and metabolic alkalosis.
5, Prostate hypertrophy patients dysuria, the use of this product increased urine volume can lead to urinary retention and bladder dilatation.

6, When the initial treatment with this product or other drugs into the use of this product treatment or start a new adjuvant drug treatment, individual patients alert state is affected (such as in the driving vehicle or operate the machine).
7, This product must be slowly intravenous injection, this product should not be mixed with other drugs after intravenous injection, but may need to use physiological saline or 5% glucose solution dilution.
8, If you need long-term medication advice as soon as possible from intravenous to oral medication, intravenous medication history is limited to a week.
 

 

[Medication for pregnant women and lactating women]  Women who are pregnant and lactating are not recommended for use.

[Child Medication] Whether the patient is safe or effective remains unclear.

[Senile Medication] The efficacy and safety of this product in elderly patients are no different from those in young adults, but older patients should pay attention to monitoring blood pressure, electrolytes and dysuria.

 

[Drug Interactions]

1, The low potassium caused by this product can aggravate the adverse reactions of cardiac glycosides.
2, This product can strengthen salt and sugar corticosteroid and laxative potassium consumption.
3, Non steroidal anti-inflammatory drugs (such as indomethacin) and probenecid can reduce the product of the diuretic and antihypertensive effect.
4, This product can strengthen the role of antihypertensive drugs.
5, The continuous use of this drug or the initiation of a combination of an angiotensin-converting enzyme inhibitor may lead to an excessive drop in blood pressure.
6, This product can reduce the role of antidiabetic drugs.
7, When used in high doses may aggravate the aminoglycoside antibiotics (such as kanamycin, gentamicin, tobramycin), preparation of cephalosporin and cisplatin ototoxicity and renal toxicity.
8, This product can strengthen curaremimetic muscle relaxant and theophylline drugs.
9, This product can reduce the role of norepinephrine and epinephrine.
10, When patients use large doses of salicylic acid, this product can increase the toxicity of salicylate.

[Overdose]

Loss of fluid and electrolytes may result in drowsiness, electrolyte disturbances, and gastrointestinal symptoms when the drug is too large. Treatment: symptomatic and supportive treatment, timely replenishment of body fluids and electrolytes, and dynamic monitoring of electrolytes.

 

[Pharmacology and Toxicology]

The mechanism of this product is sulfonylurea pyridine diuretics, its role in "mtal, inhibition of Na+/K+/2Cl- vector system, the urinary Na+, K+, Cl- and water excretion increased, but the glomerular filtration rate, no significant effect of renal plasma flow or acid-base balance. The pharmacodynamics of this product has a strong diuretic effect on rats and dogs. In these two animals, the urine volume and urinary electrolyte excretion are linearly related to the logarithm of the dose. The minimum effective dose was 0.2mg/kg, the dog was less than 0.1mg/kg, and the maximum dose was 10mg/kg. The pharmacological weight on the rat diuresis as furosemide 9 ~ 40 times, the dog 10 times, diuresis rats lasted about 2 hours, and the dog has lasted more than 8 hours of rats oral daily 10mg/kg of this product for 15 days the diuretic effect does not diminish. The dog intravenous injection of 1, 3, 10mg/kg of torasemide, systolic blood pressure, diastolic pressure and mean pressure, had no effect on heart rate, respiratory rate, respiratory pressure and electrocardiogram. Carcinogenicity studies of carcinogenic rats and mice for lifetime carcinogenicity showed that the products were 9mg/kg/ and 32mg/kg/, with no increase in tumor incidence. Based on weight, the dose was 27~96 times the dose of 20mg; based on the surface area of 5~8 times. The mutagenicity of torasemide and its metabolites by bacterial Ames test, chromosome aberration and human lymphocyte sister chromatid exchange experiment, bone marrow cell, abnormal experimental hamsters and rats, mice and rats of non conventional DNA synthesis experiments, in vitro and in vivo test showed no mutagenicity. The reproductive toxicity of female rats and male rats was 25mg/kg/ days, which had no adverse effects on reproductive performance. The dose of 5mg/kg/ on rat or rabbit dose of 1.6mg/kg/ day without toxic or teratogenic. When the doses of rats and rabbits were greater than 5 and 4 times respectively, the average weight of fetus and maternal body decreased, and the absorption and ossification of the fetus increased. The long-term toxicity in rats after oral administration of torasemide 0.2, 5 and 25mg/kg, 1, the 12 consecutive month. In the above dose group, the weight gain of 5mg/kg was inhibited, the total protein and Cl- decreased, and the BUN increased. The pathological examination showed that the surface of the kidney was granular, the renal tubular dilated and infiltrated and fibrosis, and the 25mg/kg in group K+ decreased. The dog 0.0l, and 0.08 0.4mg/kg/ of torasemide oral day, for 12 consecutive months, 0.4mg/kg group, male dogs all have nasal dryness. Pathological examination of male dog more than 0.4mg/kg group and 0.08mg/kg group showed renal tubular bitch, degeneration, expansion, cell infiltration, fibrosis and calcinosis. The changes of hearing, ophthalmology, physiology and kidney function were not related to this product.
 

[Pharmacokinetics]

After 1 hours intravenous infusion of 20mg, the serum concentration of the healthy volunteers was 3.18mg/L. The peak time of metabolite M1 and M5 was 1~2 hours, and the amounts were 3.5% and 27.4% respectively. Its elimination half-life is 3.5 hours. The distribution volume of this product in healthy adults, mild to moderate renal failure and congestive heart failure is 12 to 15L, and the distribution volume of cirrhosis patients is about doubled. Study on the tissue distribution of radioactive marker showed that rats after single administration of this product is 0.5 ~ l hours each tissue radioactivity reached maximum, the highest in liver and kidney, but lower than the plasma, 72 hours after the radioactive tissue below the detection volume, administered 14 times and 1 times administration organizations in comparison without radioactive significant difference in pregnant rats after administration can enter the fetus, 6 hours after administration of the highest concentration, decreased slowly after. Plasma protein binding rate, >99%. This product, 80%, is metabolized in the liver and the major metabolite is inactive carboxylic acid derivatives. 20% renal excretion. Special population: in addition to the decline of renal function and the decrease of renal clearance in the elderly, the pharmacokinetic process is similar to that of young subjects. Decompensated congestive heart failure patients in the use of torasemide after liver and renal clearance rate were reduced, may be due to a decrease in hepatic congestion and renal blood flow, the total removal rate of torasemide is roughly equivalent to 50% healthy volunteers. The plasma half-life and AUC value increase. Since the renal clearance rate is reduced, only a small amount of this product can enter the site of action in the spinal cord, so the effect of this product on sodium excretion in patients with congestive heart failure is lower than that in healthy volunteers. When the renal function is impaired, this product can be compensated by the metabolic pathway of the liver. Therefore, the total clearance rate and the elimination half-life of the patients with impaired renal function remain within the normal range. The volume of distribution, the half-life of plasma and the rate of renal clearance increased in cirrhotic patients, but there was no change in the total clearance rate.

[Storage] Keep out of the light, sealed and kept in the shade (no more than 20 degrees Celsius).

[Packing] Ampoule packing, 10 pcs /  boxes

[Validity]  Tentative 24 months

[Implementation Criteria] YBH18992005

[Approval Number] SFDA approval number H20051396

[Production Enterprise]

Name of enterprise: Zhejiang Chengyi Pharmaceutical Co., Ltd

Production address: No. 118, Chemical Road, Dongtou District, Wenzhou city,Zhejiang province,China

Phone number: 86-577-6348-3979

Fax number: 86-577-6348-5135

URL:http://en.chengyipharma.com

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