Trigrim

General characteristics. Structure:

Active agent: торасемид 2,5 mg

Active agent: торасемид 5 mg

Active agent: торасемид 10 mg.

Pharmacological properties:

Pharmacodynamics. Torasemid — loopback diuretic. At use oppresses a reabsorption of ions of sodium and chlorine in the ascending part of a Henle's loop. Anti-hypertensive action of a torasemid is caused by decrease in OPSS due to normalization of the broken electrolytic balance and mainly decrease of the activity of free calcium in cells of a muscular layer of arteries.

Pharmacokinetics. After oral administration торасемид quickly and almost it is completely absorbed, Cmax in a blood plasma is reached in 1–2 h. More than 90% of a torasemid contact proteins of a blood plasma.
Distribution. Linkng of a torasemid with blood proteins — more than 99%. The volume of distribution of a torasemid makes 12–15 l. At patients with cirrhosis the volume of distribution increases almost twice.
Removal. Т½ the torasemida makes about 4 h. Process of removal is provided with metabolism in a liver (about 80% of the general clearance) and allocation by kidneys (patients have about 20% with normal function of kidneys) due to removal of connection through proximal tubules with urine.
At patients with dekompensirovanny heart failure hepatic and renal clearance decrease, T½ and AUC are extended.
At patients with a renal failure the renal clearance of a torasemid is considerably reduced, the indicator of the general clearance significantly does not change. The necessary diuretic effect at this group of patients is provided with increase in dosing.

Indications to use:

The hypostases caused by congestive heart failure, diseases of kidneys or a liver.
Essential AG (as monotherapy or in a combination with other anti-hypertensive drugs).

Route of administration and doses:

Pill should be taken, without chewing and without crushing, irrespective of the use of food and of time of day, washing down with a small amount of liquid.
Congestive heart failure. The general initial dose makes 10–20 mg of 1 times a day.
In the absence of necessary diuretic action it is necessary to double a dose (20–40 mg/days) before achievement of necessary effect.
Chronic renal failure. The general initial dose makes 20 mg of 1 times a day.
In the absence of necessary diuretic action it is necessary to double a dose (40 mg/days) before achievement of necessary effect.
Cirrhosis. The general initial dose makes 5–10 mg of 1 times a day at the combined use with the drugs antagonists of Aldosteronum or diuretics promoting a potassium delay in an organism. In the absence of necessary diuretic action it is necessary to raise a dose twice (10–20 mg/days) to achievement of necessary effect.
There are no data on a single dose in doses> 40 mg/days.
Essential hypertensia. The recommended initial dose makes 2,5 mg of a torasemid of 1 times a day. Maximum efficiency is reached after 12 weeks of continuous treatment.
If it is necessary, the dose can be raised to 5 mg/days. It is known that increase in a dose of more than 5 mg/days does not lead to decrease in the ABP.
In case of need it is necessary to apply complex therapy with other anti-hypertensive means.
Patients of advanced age do not need special selection of a dose.
Increase in dosing for achievement of necessary diuretic effect in connection with reduced clearance of a torasemid can be required by patients with a renal failure.
Patients with a heavy abnormal liver function need to consider that the increased renal clearance of a torasemid can be followed by decrease in removal of ions of sodium.

Features of use:

In an initiation of treatment control at the patient of electrolytic exchange — hypopotassemias is necessary, for a hyponatremia, hypovolemia and disturbances of an urination.
At long treatment torasemidy regular monitoring of electrolytic balance, level of glucose, uric acid, creatinine and lipids of blood is recommended.
Careful monitoring of patients with a tendency to a hyperuricemia and gout is recommended.
It is necessary to control carbohydrate metabolism at patients with a latent and severe form of a diabetes mellitus.
Drug Trigrim should be used with extra care to patients with liver diseases which are followed by cirrhosis and ascites as sudden changes of water and electrolytic balance can lead to a hepatic coma. Patients of this group need to carry out therapy using Trigrim (as well as other diuretics) in the conditions of a hospital. For the prevention of a hypopotassemia and a metabolic acidosis it is necessary to appoint drug with the drugs antagonists of Aldosteronum or drugs promoting a potassium delay in an organism.
After reception of a torasemid noted the ototoxicity phenomena (a sonitus and hearing losses) having reversible character, but a feedforward using drug it is not established.
At purpose of diuretics it is necessary to control carefully clinical symptoms of disturbance of electrolytic balance, a hypovolemia, an extrarenal azotemia and other disturbances which can be shown in the form of dryness in a mouth, thirst, weakness, slackness, drowsiness, excitement, muscular pain or spasms, a myasthenia, hypotonia, an oliguria, tachycardia, nausea, vomiting. The excessive diuresis can become the organism dehydration reason, lead to decrease to OTsK, a thrombogenesis and an embolism of blood vessels, especially at patients of advanced age.
Patients with disturbance of water and electrolytic balance need to stop use of drug and after elimination of side effects to recover therapy by Trigrim, since lower doses.
At patients with cardiovascular diseases, especially in case of reception of cardiac glycosides, the hypopotassemia arising at reception of diuretics can increase risk of development of arrhythmia.
At purpose of drug it is necessary to carry out regular laboratory control of indicators of level of potassium and other electrolytes in a blood plasma.
Use during pregnancy and feeding by a breast. There are no data on action of a torasemid on an embryo and a fruit of the person, and also about penetration into breast milk therefore it is not recommended to accept торасемид during pregnancy and feeding by a breast.
Children. The safety given relatively and efficiency of use of a torasemid for children are absent therefore this age category of patients should not appoint drug Trigry.
Ability to influence speed of response at control of vehicles or work with other mechanisms. Drug can change the speed of response of the person, reducing it during control of vehicles or work with other mechanisms, especially at simultaneous use with alcohol. Therefore it is necessary to avoid control of vehicles or work with potentially dangerous mechanisms during treatment as drug.

Side effects:

Side effects on the frequency of emergence classify by such categories: very often (> 1/10), it is frequent (> 1/100, <1/10), sometimes (> 1/1000, <1/100), is rare (> 1/10 000,> 1/1000), is very rare (1/10 000), including separate messages.
From a metabolism: sometimes — a hypercholesterolemia, a lipidemia, a polydipsia.
From a nervous system: often — dizziness, a headache, drowsiness; sometimes — spasms of the lower extremities.
From cardiovascular system: sometimes — premature ventricular contraction, the accelerated heartbeat, tachycardia, a hyperemia of the person.
From respiratory system: sometimes — nasal bleedings.
From a GIT: often — diarrhea; sometimes — an abdominal pain, a meteorism.
From an urinary system: often — increase in frequency of urination, a polyuria, a night polyuria; sometimes — desires to an urination.
General disturbances: sometimes — thirst, weakness, fatigue, hyperactivity, nervousness.
Changes of laboratory indicators: sometimes — decrease in level of thrombocytes.
Other side reactions can be shown in the form of nausea, vomiting, a hyperglycemia, a hyperuricemia, a hypovolemia, arterial hypotension, impotence, thromboses, skin reactions, a syncope.

Interaction with other medicines:

At simultaneous use of Trigrim with blockers of β-adrenoceptors, blockers of calcium channels, APF inhibitors, foxglove drugs, organic nitrates did not reveal new or unforeseen by-effects.
Trigrim's reception does not influence ability of linkng of Glibenclamidum or warfarin with proteins of a blood plasma, does not change also anticoagulative properties of a fenprokumon, does not influence pharmacokinetic characteristics of digoxin or a karvedilol. In case of the combined use of a torasemid with Spironolactonum the renal clearance of the last decreases, however there is no need for correction of doses of drugs.
At the combined use with salicylates in high doses toxic effect of salicylates increases. NPVP (including acetylsalicylic acid) at the combined use with drug and other diuretics which action point — a Henle's loop, can break function of kidneys.
At the combined use with indometacin diuretic action of a torasemid (only on condition of limited intake of sodium in an organism partially is suppressed — 50 мэкв / days), in the conditions of normal intake of sodium (150 мэкв / days) the similar phenomena are noted.
Cimetidinum, Spironolactonum do not change efficiency of a torasemid.
Digoxin can increase AUC of a torasemid by 50%, however in dose adjustment there is no need.
The combined therapy with Colestyraminum is recommended to be carried out to different periods.
At a concomitant use with probenetsidy diuretic action of a torasemid decreases.
Diuretics reduce renal clearance of lithium, increasing its toxic action, and can increase expressiveness of ototoksichesky effect of aminoglycosides and Acidum etacrynicum, especially at patients with a renal failure. The research of these interactions with Trigrim was not conducted.

Contraindications:

Hypersensitivity to a torasemid or excipients of drug, sulphonylurea derivatives. A renal failure with an anury, a hepatic coma, precoma, arterial hypotension, arrhythmia, a lactose intolerance or disturbance of absorption of glucose galactose. Period of pregnancy and feeding by a breast.

Overdose:

There is no typical picture of intoxication.
Symptoms: strengthening of a diuresis with threat of dehydration and loss of electrolytes that can result in drowsiness and confusion of consciousness, arterial hypotension, cardiovascular insufficiency.
Treatment. There is no special antidote. It is necessary to lower a dose or to stop use of a torasemid and at the same time to carry out completion of volume of liquid and correction of electrolytes.

Storage conditions:

To store in the dry, protected from light place at a temperature not above 25 °C.

Issue conditions:

According to the recipe

Packaging:

Tab. of 2,5 mg, No. 10, No. 30.
Tab. of 5 mg, No. 10, No. 30.
Tab. of 10 mg, No. 10, No. 30.