Spironolakton-Darnitsa

General characteristics. Structure:

Active ingredient: spironolactone; 1 tablet contains Spironolactonum (in terms of 100% substance) 25 mg;

excipients: potato starch; lactose, monohydrate; povidone (polyvinylpirrolidone low-molecular medical); calcium stearate.

Pharmacological properties:

Pharmacodynamics. Spironolakton-Darnitsa is kaliysberigayushchy diuretic with moderate natriuretic effect. The diuretic effect of Spironolaktona-Darnitsa is connected with its antagonism concerning an adrenal hormone – Aldosteronum. Action of Spironolaktona-Darnitsa happens in distal renal tubules: drug reduces removal of potassium ions and strengthens removal of ions of sodium and water without considerable disturbance of electrolytic balance; reduces titrable acidity of urine and reduces urea removal. Due to strengthening of removal of ions of Spironolakton-Darnitsa sodium shows non-constant moderate anti-hypertensive action. Spironolakton-Darnitsa interferes with linkng of Aldosteronum with proteinaceous receptors of cells of target organs.

Pharmacokinetics. After intake of Spironolakton-Darnitsa it is quickly soaked up in the digestive channel and for 90% contacts proteins of plasma. Spironolakton-Darnitsa it is quickly metabolized in a liver. The main pharmacological active metabolites are 7-α-тиоспиронолактон, 7-α-тиометилспиронолактон and канренон. Antialdosteronovy action defines канренон what makes about 50% of all metabolites of Spironolaktona-Darnitsa. Time of achievement of the maximum concentration (Tmax) of a kanrenon makes 2-4 hours, and the period of its semi-removal of T1/2 makes in average 12,5 h. Bioavailability of drug is in limits of 92-99%, and it can increase a little at its reception with food. Spironolaktonu-Darnitsa inherent cumulative effect. Its diuretic action develops gradually and reaches the maximum value for 2-5 days of treatment. Gets through a placenta and into breast milk. It is brought out of an organism with urine and a stake. The main way of elimination – kidneys.

Pharmaceutical characteristics.

Main physical and chemical properties: tablets of color, white or white with a creamy shade, with a flat surface and a facet.

Indications to use:

Primary hyper aldosteronism:

- for a short, preoperative course of treatment;

- for long use in case of not operability or at refusal of the patient of operation.

Hypostases which are connected with a secondary hyper aldosteronism.

Edematous syndrome:

- the hypostasis caused by chronic insufficiency at inefficiency or intolerance of other treatment or in need of increase in efficiency of other diuretics;

- a nephrotic syndrome in case of inefficiency of treatment of a basic disease, use of diuretics and restriction of consumption of salt with food;

- hypostases and/or ascites in patients with cirrhosis.

Essential hypertensia, mainly, at a hypopotassemia, combining with other antihypertensives.

Hypopotassemia when it is impossible to apply other treatment.

Prevention of a hypopotassemia, during treatment by digitalis drugs when other ways of treatment are unacceptable.

Route of administration and doses:

Apply inside. The usual daily dose of Spironolakton-Darnitsa is accepted in 1-2 receptions. Use of a daily dose in 1 reception or the first administration of drug at double use is recommended in the morning.

Primary hyper aldosteronism: after installation of the diagnosis by the adult appoint    100-400 mg/days as preparation for operational intervention.

In case of not operability it is possible to carry out long treatment by the smaller effective dose which is picked up individually. In such cases each 14 days the initial dose is subject to decrease until the smallest effective dose is reached. At long treatment it is reasonable to combine drug with other diuretics, in order to avoid development of side reactions.

Edematous syndrome (heart failure, cirrhosis, nephrotic syndrome): the usual initial dose for adults makes 100 mg/days (the daily dose can fluctuate from 25 to 200 mg), distributed on 2 receptions. At purpose of higher doses reasonable use in a combination with diuretics which affect proximal departments of renal tubules at the same time the dose of Spironolaktona-Darnitsa remains invariable.

To children appoint at the rate of 3 mg/kg of body weight a day once or having distributed on 2 receptions.

Essential hypertensia: it is appointed in a combination with other diuretics, the usual initial dose for adults makes 50-100 mg/days and is distributed on 2 receptions. It is necessary to continue treatment not less than 2 weeks as the maximum hypotensive effect occurs after the termination of this term. Further dosing individual.

Hypopotassemia: adult appoint 25-100 mg/days if the peroral way of replenishment of potassium or other kaliysokhranyayushchy way is insufficiently effective.

Duration of a course of treatment at children and adults individual, in certain cases can reach several years, but at the same time there is always necessary a use of drug in the smallest effective daily dose, on condition of constant control of electrolytic composition of blood serum and indicators of function of kidneys.

Features of use:

Use during pregnancy or feeding by a breast. The drug "Spironolakton-Darnitsa" is contraindicated during pregnancy or feeding by a breast.

Children. Spironolakton-Darnitsa apply to children at an edematous syndrome.

Route of administration and doses: drug is appointed at the rate of 3 mg/kg of body weight a day, once or having distributed on 2 receptions.

 In drug use cases by patients with reduced function of kidneys, temporary increase in level of an urea nitrogen in blood serum, and also a hyperpotassemia can be observed that in turn can lead to development of disturbances of a cordial rhythm and reversible giperkhloremichesky metabolic acidosis. If the hyperpotassemia, drug Spironolactonum use develops in the patient - Darnitsa it is necessary to stop immediately.

In this regard at a disease of kidneys, a liver and in old age, not обходимо to carry out systematic control of electrolytes of blood serum and indicators of function of kidneys.

Spironolakton-Darnitsa complicates definition of digoxin in serum, cortisol and adrenaline in a blood plasma.

In spite of the fact that drug directly does not influence carbohydrate metabolism, its use by patients with a diabetes mellitus, especially in the presence of a diabetic nephropathy, demands extra care in connection with danger of emergence of a hyperpotassemia. Spironolactonum - Darnits should not be applied together with other drugs which cause potassium detention.

During reception of Spironolactonum - Darnits it is forbidden to take alcoholic drinks.

At simultaneous use of the drug Spironolactonum - Darnitsa in a complex with other diuretics, possible development of a hyponatremia.

At hypostases it is reasonable to apply Spironolactonum - Darnitsa in a complex with other diuretics, to limit the use of kitchen salt and liquid, if necessary - to adhere to a bed rest.

Ability to influence the speed of reactions at control of motor transport or works with other mechanisms. In an initial stage of use of drug which time is defined individually it is forbidden to direct the car and to perform other complex dangerous works with mechanisms which demand the speed of physical and mental reactions. Further the possibility of their implementation is defined individually.

Side effects:

From TsNS and peripheral nervous system: headache, block, dizziness, drowsiness, lethargy, confusion of consciousness, ataxy, muscular spasm, spasms of gastrocnemius muscles.

From a GIT: nausea, loss of appetite, abdominal pains, vomiting, diarrhea, lock, intestinal gripes, disturbance of functions of a liver, gastritis, gastric bleeding, stomach ulcer and duodenum.

From system of bodies of a hemopoiesis: leukopenia (including agranulocytosis), thrombocytopenia, megaloblastny or aplastic anemia.

From endocrine system: a gynecomastia and decrease in an erection at men, disturbance of a menstrual cycle, a dysmenorrhea, an amenorrhea, a metrorrhagia at climacteric age, a hirsutism, swelling and mammary gland pain at women; possible change of a timbre of a voice both at men, and at women.

From skin: hypertrichosis, alopecia, hyperemia, lupoid syndrome.

Allergic reactions: urticaria, papular and erythematic rash, itch, fever.

From a metabolism: hyperpotassemia, hyponatremia, hypercreatinemia, hyperuricemia, increase in level of urea, metabolic giperkhloremichesky acidosis or alkalosis.

From a liver: hepatitis (separate case).

From an urinary system: acute renal failure.

From cardiovascular system: arterial hypotension.

From a musculoskeletal system: osteomalacy (separate case).

Interaction with other medicines:

-  salicylates - reduction of diuretichny effect;

-  diuretics - are exponentiated by effect of diuretics;

-  kaliysoderzhashchy diuretics, antagonists to angiotensin ІІ, inhibitors of an angiotensin-converting enzyme and Aldosteronum - increase in risk of emergence of a hyperpotassemia, especially at patients with diseases of kidneys;

-  anti-hypertensive means - strengthening of hypotensive effect;

-  non-steroidal anti-inflammatory drugs - strengthening of a natriuretic effect, increase in risk of developing of acidosis;

-  ammonium chloride - increase in risk of developing of acidosis;

-  флудрокортизон - there is a paradoxical increase in canalicular secretion of potassium;

-  Mitotanum - reduction of effect of Mitotanum;

-  нимодипин - a dangerous lowering of arterial pressure;

-  anticoagulants of indirect action (coumarin derivatives) - their effect decreases;

-  трипторелин, бузерелин, гонадорелин - their effect increases;

-  Triamterenum, amiloride - a dangerous delay of potassium, risk of developing of arrhythmia;

-  digoxin - increases digoxin semi-removal time, possible strengthening of intoxication digoxin;

-  antipyrine - amplifies metabolism of drug in a liver.

Contraindications:

Addison's disease, hyperpotassemia, hyponatremia, acute renal failure, essential depression of function of kidneys (glomerular filtering <10 ml/min.), an anury, pregnancy, the breastfeeding period, hypersensitivity to drug components.

Overdose:

Symptoms: from TsNS and a peripheral nervous system: general weakness, dizziness, drowsiness, confusion of consciousness, paresthesia, muscular weakness.

From a GIT: dryness in a mouth, thirst, nausea, vomiting, diarrhea.

From cardiovascular system: arrhythmia.

Allergic reactions: skin rashes.

From a metabolism: hypercalcemia, hyponatremia, hypercreatinemia, hyperuricemia, increase in level of urea.

Treatment: there is no special antidote. It is necessary to provide balance of water and electrolytic exchange by purpose of diuretics that render assistance to release of potassium, to provide parenteral administration of solution of glucose with insulin. In hard cases carry out a hemodialysis.

Storage conditions:

Period of validity. 3 years. To store in the place, unavailable to children, in original packaging at a temperature not above 25 °C.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in blister strip packagings, on the 3rd blister strip packagings in a pack.