active ingredient: spironolactone;
1 tablet contains 50 mg or 100 mg of spironolactone;
excipients: corn starch, calcium hydrogen phosphate dihydrate, povidone K 25, sodium lauryl sulphate, silica colloidal anhydrous, magnesium stearate.
The main physical and chemical properties: round, two-plane tablets with smooth edges, white with a notch on one side.
ATC code C03D A01.
Spironolactone is a competitive antagonist of aldosterone. It affects the distal tubules of the kidneys.
Due to the blockade of aldosterone suppresses water retention and Na + and promotes retention of K+, which not only increases the excretion of Na + and Cl -, and reduces the excretion of K + in the urine, but also reduces the excretion of H+. As a result, the diuretic effect also has a hypotensive effect.
Spironolactone is rapidly absorbed after oral administration by 73%. The absorption of spironolactone increases when taken with food. As a result, the concentration of the main substance in the serum increases by 50-100%
Binding of spironolactone and canrenone with plasma proteins is depending on the method of determining 90% (equilibrium dialysis method) or 98% (ultrafiltration method).
After oral administration, spironolactone has a pronounced effect of the first pass and is metabolized in the liver and kidneys. Its main metabolites are 7-?-thiospironolactone, canrenone or canrenoate, 7-?-thiomethylspironolactone or 6-?-hydroxy-7-?-thiomethylspironolactone. Compared to the original substance, the three metabolites mentioned above have a relatively low antimineralocorticoid effect of 26.68 and 33%, respectively.
After oral administration, the maximum concentration of spironolactone in blood plasma is reached in 1-2 hours, and the maximum concentration of metabolites - in 2-3 hours.
At low doses (50-200 mg), the area under the concentration-time curve of the canrenone increases linearly with the dose, whereas high doses lead to lower concentrations, probably due to enzymatic conversion into metabolites.
The equilibrium concentration of the canrenone is within 50-188 ng/ml and is achieved 3-8 days after daily application of spironolactone. In patients with liver cirrhosis and ascites, it is achieved only after 14 days.
Spironolactone is excreted mainly in the urine and to a lesser extent with bile. The ratio of spironolactone in unchanged form is insignificant. With urine, only metabolites are excreted, mainly canrenone and its glucuronide ether and 6-?-hydroxide-sulfoxide. After receiving a single dose of spironolactone with a radioactive label 47-57% excreted in the urine and 35-41% - with feces for 6 days.
After oral administration of spironolactone the elimination half-life is 1-2 hours, whereas metabolites are excreted more slowly. Terminal half-life canrenone is approximately 20 hours, approximately 3 to 7-?-dimethylaminoethanol and about 10:00 for 6-?-hydroxy-7-?-dimetilaminoetanol.
Spironolactone and its metabolites pass through the placental barrier. Kanrenon is excreted with breast milk.
Congestive heart failure in patients who are not responsible for the treatment of other diuretics, or if necessary, potentiating their effects.
Essential hypertension, mainly in the case of hypokalemia (usually in combination with other antihypertensive drugs).
Cirrhosis of the liver accompanied by edema and/or ascites.
Edema due to nephrotic syndrome.
Hypokalemia, in case of impossibility of receiving other therapy.
The drug is used for prevention of hypokalemia in patients receiving cardiac glycosides, if other approaches are seen as impractical or inappropriate.
Hypersensitivity to the active substance or any other auxiliary substances.
Anuria, acute renal insufficiency, severe violation of azotovydelitelnoy renal function (glomerular filtration rate
Severe renal failure accompanied by oliguria or anuria (creatinine clearance below 30 ml/min at 1.73 m2 of body surface and/or serum creatinine above 1.8 mg/DL).
Hypovolemia or dehydration.
You cannot apply at the same time with kalisberegatmi dioretikami drugs and potassium to prevent hyperkalemia.
Interaction with other medicinal products and other forms of interaction
Avoid concurrent use of spironolactone and potassium-containing solutions (e.g. potassium chloride), ACE inhibitors (e.g. captopril, enalapril), antagonists of angiotensin II receptors blockers, aldosterone blockers, or potassium-sparing diuretics (triamterene, amiloride) may lead to increased levels of potassium in the blood serum and the development of severe and probably life-threatening hyperkalemia.
The simultaneous use of ACE inhibitors, furosemide and spironolactone can lead to the development of acute renal failure.
In the case of additional administration of drugs to reduce blood pressure, there may be a significant decrease in blood pressure.
Other diuretics: increased diuresis and a significant decrease in blood pressure.
Cholesterol, ammonium chloride: increased risk of hyperkalemia and hyperchloremic metabolic acidosis).
Immunosuppressants (tacrolimus and cyclosporine): increased risk of hyperkalemia.
Tricyclic antidepressants and antipsychotic drugs can enhance the antihypertensive effect of spironolactone Sandoz .
Antihypertensive drugs (especially ganglioblockers): excessive hypotension may develop. Thus, the dose of antihypertensive drugs can be reduced by adding to the therapeutic scheme spironolactone Sandoz with subsequent adjustment if necessary.
Alcohol, barbiturates or narcotic drugs may enhance orthostatic hypotension caused by spironolactone.
Pressor amines (norepinephrine): spironolactone reduces their effect. This should be taken into account when conducting local or General anesthesia with the use of these drugs.
Nonsteroidal anti-inflammatory drugs (NSAIDs), in particular acetylsalicylic acid, indomethacin and mefenamic acid increase the risk of hyperkalemia with a concomitant decrease in diuretic, natriuretic and antihypertensive action of spironolactone. In patients who develop hypovolemia or dehydration during spironolactone therapy, the combined use of nonsteroidal anti-inflammatory drugs (NSAIDs) can cause acute renal failure.
Corticosteroids, ACTH (ACTH): a paradoxical increase in excretion of potassium).
Digoxin: spironolactone may increase the half-life of digoxin, which may lead to an increase in its serum content and the development of glycoside intoxication.
Lithium drugs should not be administered concurrently with diuretics because they reduce lithium renal clearance and can increase the risk of intoxication.
Carbenoxolone can cause sodium retention and thus reduce the effectiveness of spironolactone, possibly a mutual decrease in the effectiveness of drugs. The use of a large number of licorice has the effect similar to the action carbenoxolone.
Carbamazepine while taking spironolactone can cause the development of clinically significant hyponatremia.
Terfenadin in the case of simultaneous use with spironolactone increases the risk of ventricular arrhythmia through hypokalemia and imbalance of other electrolytes.
Coumarin derivatives : their effect is weakened.
Triptorelin, buserelin, gonadorelin: their effects are increasing.
Neomycin may delay the absorption of spironolactone.
Influence on the results of laboratory tests: influence on the process of determining the concentration of digoxin by radioimmunological methods may be expected.
The simultaneous use of spironolactone and ACE inhibitors (such as captopril, enalapril) is associated with the risk of a significant decrease in blood pressure, can progress to a state of shock, and with the risk of exacerbation of renal dysfunction, in some cases, can lead to acute renal failure. In order to avoid the possible development of hypotension at the beginning of treatment, the use of diuretics should be discontinued 2-3 days before the start of therapy with ACE inhibitors.
You need to establish a thorough monitoring of the state:
patients with impaired renal function average degree (creatinine clearance 30-60 ml/min and/or creatinine in blood serum in the range of 1.2-1.8 mg/DL)
patients with diathesis, acidosis and/or hyperkalemia caused by a major disease (e.g. diabetes mellitus).
patients with arterial hypotension.
Spironolactone may increase the risk of hyperkalemia in patients with diabetic nephropathy.
Spironolactone therapy can cause a transient increase in serum urea nitrogen, especially in patients with pre-existing renal impairment and hyperkalemia. Spironolactone can cause the development of circulating hyperchloremic metabolic acidosis. Thus, in patients with impaired renal and liver function, as well as in elderly patients should be regularly investigated biochemical parameters of kidney function, as well as electrolyte balance.
During the treatment of spironolactone alcohol is prohibited.
It is necessary to avoid prolonged unreasonable use of the drug, because, according to published data, prolonged use of spironolactone in animals at maximum doses contributed to the development of carcinoma, myeloid leukemia.
Concurrent use of spironolactone and potassium-sparing diuretics (e.g. triamterene, amiloride), potassium-containing solutions or ACE inhibitors may cause hyperkalemia, life-threatening. In this regard, the use of the above-mentioned drugs is not recommended.
In in the case of severe renal failure (glomerular filtration rate below 30 ml/min and/or serum creatinine above 1.8 ml/DL), spironolactone is not only ineffective, but even harmful, since glomerular filtration rate will continue to decrease.
In case of impaired renal function (serum creatinine level is between 1.2-1.8 mg/DL and creatinine clearance - within 60-30 ml/min.) and the simultaneous use of drugs that can increase the level of potassium in the blood, spironolactone therapy should be carried out subject to regular monitoring of potassium levels in the blood.
During treatment with spironolactone and electrolyte balance of the serum (mainly potassium, sodium, calcium, bicarbonate), creatinine serum urea and uric acid which are usually excreted in the urine, and acid-base status should be regularly monitored.
Loss of body weight caused by increased urination should not exceed 1 kg/day, regardless of the volume of urination.
Due to chronic abuse of diuretics can appear pseudorandom of Barter with edema. Edema is an expression of renin increase, the consequence of which is secondary hyperaldosteronism.
Spironolactone may affect the results of certain diagnostic tests (e.g. determination of serum digoxin concentration by radioimmune analysis (RIA), plasma cortisol, and epinephrine).
During the treatment of spironolactone, patients should take a sufficient amount of fluid.
The use of spironolactone Sandoz ? can provoke a false positive result of doping control.
Improper use of the drug Spironolactone Sandoz ? how doping can damage your health.
Information for patients with diabetes
One tablet contains less than 0.01 HE.
Use during pregnancy or breast-feeding.
Spironolactone should not be used during pregnancy and lactation.
There is no sufficient data on the use of spironolactone in pregnant women. In animal experiments was observed the feminization of the genital organs of the offspring and the male sex hormonal disorders in offspring, male and female. People had anti-androgen effects. In this regard, spironolactone is contraindicated during pregnancy.
Unknown, spironolactone is excreted with breast milk. Pharmacologically active metabolite canrenoate is excreted in breast milk (concentrations in breast milk plasma is 0.7). In this regard, spironolactone is contraindicated during breast-feeding. If necessary, in the treatment of breast-feeding should be discontinued.
The ability to influence the reaction rate when driving motor transport or operating other mechanisms.
In the initial period of application of spironolactone which duration individual, it is forbidden to operate the car and working mechanisms on which work is connected with the increased risk of traumatism.
Method of application and doses
The dose is determined individually, depending on the severity and degree of hyperaldosteronism.
In the case of diagnosed primary hyperaldosteronism the drug can be administered in preparation for surgery in a daily dose of 100-400 mg. Patients who surgery is not planned, the drug can be used as long-term maintenance therapy at the lowest effective dose which is determined individually. In this situation, the initial dose can be reduced every 14 days until the minimum effective dose. In case of prolonged use it is recommended to use in combination with diuretics of other groups to reduce side effects.
Edema (congestive heart failure, nephrotic syndrome)
Adults: the initial daily dose is 100 mg (25-200 mg) and is used in 1 or 2 doses. In the case of appointment of higher doses spironolactone Sandoz can be taken in combination with other groups of diuretics, acting in more proximal renal tubules. In this case, the dosage of spironolactone Sandoz should be adjusted.
Cirrhosis of the liver, accompanied by ascites or edema
If the ratio Na +/K + in the urine of more than 1, the initial daily and maximum daily doses up to 100 mg. If this ratio is less than 1, the initial daily dose is 200 mg, maximum 400 mg/day.
The maintenance dose should be determined individually.
Essential arterial hypertension
The initial daily dose is assigned to 1 or 2 admission is 50-100 mg, it should be taken in combination with other antihypertensive drugs. Therapy is continued for at least two weeks, since by the end of this period the maximum antihypertensive effect is achieved. Then the dose should be adjusted individually, depending on the effect achieved.
Patients who do not have enough food additives with K + or other methods of potassium-amisnoic therapy, the drug is taken in a daily dose of 25-100 mg.
The recommended initial dose for children is 1 to 3 mg of spironolactone per 1 kg of body weight for 1 or 2 doses daily for 5 days. If it is necessary to use the drug for children under 3 years, the tablet must be crushed, dissolved and allowed to drink a child in the form of a suspension.
If the treatment continues, the dose should be reduced, keeping the achieved effect of the drug.
It is recommended to start treatment with low doses, followed by a gradual increase until maximum effect. It is necessary to take into account the existing hepatic and renal disorders, as they affect the metabolism of the drug and its excretion.
Spironolactone Sandoz 100 mg ?
Due to the high content of the active substance, spironolactone Sandoz (100 mg) is not suitable for the treatment of children.
Method and duration of application.
The tablets should be swallowed without chewing, with a sufficient quantity of liquid (e.g. glass of water).
The duration of treatment depends on the type and severity of the disease. The duration of treatment should be as short as possible. The need for long-term treatment of spironolactone should be checked from time to time.
? Sandoz spironolactone tablets, 50 mg use in Pediatrics.
Due to the high content of the active substance, spironolactone Sandoz , 100 mg tablets are not suitable for the treatment of children.
Drowsiness/lethargy, confusion and electrolyte disorders.
Symptomatic, specific antidote does not exist. It is necessary to maintain the water-electrolyte and acid-alkaline balances by assigning diuretics that remove potassium; parenteral administration of glucose with insulin, in difficult cases - hemodialysis.
Adverse reactions are the result of competitive aldosterone antagonism, increases the excretion of potassium and antiandrogens spironolactone.
Adverse reactions are listed according to the classes of organ systems according to the Medical dictionary for regulatory activities MedDRA using the definition of frequency MedDRA:
very often (1/10)
frequently (1/100 to <1/10)
infrequently (1/1,000 to <1/100)
rare (1/10,000 to
very rarely (
unknown frequency (cannot be set according to available data).
Adverse reactions by organ system, according to MedDRAочень cytocentrifugation reconaissance frequency
The blood and lymphatic system Thrombocytopenia, agranulocytosis, eosinophil-Leah
The immune system Hypercall-news
endocrine disorders of hirsutism
From the metabolism and petnieciskie-MIA 1Гипер-kalemia 2 Hyponatremia, dehydration, porphyria Hyperglobe - cal acidosis
From the psyche of Splut ness of consciousness
From the nervous system Drowsiness 3, headache, vertigo Paralysis, paraplegia
From the cardiovascular sistemarti 4
From the respiratory System change the tone of the voice
From the digestive system Nausea, bluwan niya
Dry mouth, intestinal colic.Gastritis, ulcer, gastric bleeding, stomach pain, diarrhea
From hepatobiliar Noah system Hepatitis, hepato - toxicity nestinarstvo liver function
The skin and its derivatives Rash, itching, nettle-ka, exanthema, urticaria, erythemally, eczema, ring-shaped erythema, wauchope similar skin lesions, hirsutism have gensinger host, redness, Stevens-Johnson syndrome 6
From the side of musculoskeletal system and connective tissue muscle Spasms of the lower extremities osteomalacia
From the urinary system Acute renal failure ness
From reproductiv Noah system and dairy zheleznenie libido, erectile dysfunction, giacomos-ment (in men), increased sensitivity of the nipples and breast tenderness, breast augmentation, Earl-realini disorders in germinativum-Ah 5Нарушение sexual potency Dobraja-no mammary tumors, amenorrhea 7
Systemic disorders of Asthenia, fatigue
Changes in laboratory parameters Of increased blood serum urea content
1 in patients with renal insufficiency and those who receive potassium preparations.
2 in elderly patients, diabetics and those who receive ACE inhibitors.
3 in patients with liver cirrhosis.
4 in patients with renal insufficiency and those who receive potassium preparations.
5, With the use of high doses (450 mg per day).
6 in individual cases.
Metabolism and digestive disorders
When use of spironolactone hyperkalemia, life-threatening, may occur mainly in patients with impaired renal function. This can cause symptoms such as muscle paralysis (hyperkalemic paralysis) and arrhythmia. In this regard, additional administration of potassium, other potassium-saving diuretics or a diet enriched with potassium should be avoided.
In case of renal dysfunction, violation of water-electrolyte balance (hyponatremia, hypomagnesemia, hyperchloremia, hypercalcemia, etc.) may occur due to increased excretion of water and electrolytes.
As a result of excessive diuresis, hypovolemia and hyponatremia can develop in patients. Hyponatremia may occur, especially after the excessive consumption of water while taking spironolactone. Due to the imbalance of electrolytes in the blood, there may be loss of appetite, dry mouth, thirst, vomiting, headache or blood flow to the head, asthenia, vertigo, drowsiness, fatigue, visual impairment, apathy, confusion, General myasthenia gravis, myospasm (convulsions in the back of the Shin), as well as arrhythmia and circulatory disorders (see para. adverse reactions "from the heart"). In this regard, it is necessary to balance the undesirable loss of fluid (for example, due to vomiting, diarrhea, hyperhidrosis).
In the case of irregular heart rate, fatigue or myasthenia gravis (for example, in the legs) should consider the possibility of hyperkalemia. After taking high doses, lethargy and confusion were observed.
The electrolyte balance of serum (especially potassium, sodium and calcium) should be checked regularly.
At the beginning of therapy and for long-term use of spironolactone, it is necessary to monitor the level of potassium in the serum at regular intervals in order to prevent the occurrence of excess potassium in the blood.
Acid-base balance disorders are possible. Spironolactone can cause or exacerbate hyperchloremic metabolic acidosis.
Of cases reverse the increase in concentration of nitrogen compounds usually excreted in the urine (urea, creatinine) has been reported infrequently.
We observed frequent cases giperurikemii during spironolactone therapy. This can lead to the development of acute gout in predisposed patients.
Concentrations of urea, creatinine and uric acid in serum, as well as acid-alkaline balance and water-electrolyte balance during therapy spironolactone should be regularly checked.
From the heart
As a result of excessive diuresis through hypovolemia can occur headache, vertigo, visual impairment, dry mouth and thirst, as well as orthostatic dysregulation or sudden decrease in blood pressure, progresses in vascular insufficiency.
In the case of excessive diuresis, dehydration and as a result of hypovolemia, the volume of plasma may decrease, resulting in an increased risk of thrombosis and embolism in elderly patients.
When applying spironolactone may increase the concentration of serum creatinine and urea. Increased urine production can lead to deterioration or exacerbation of existing disorders in patients with urinary tract obstruction.
Special storage conditions are not required.
Keep out of reach of children.
There are 10 tablets in blister, 2 or 3 or 6 blisters in a cardboard box.
Category home away from home
Salutas Pharma GmbH/
Salutas Pharma GmbH.
Manufacturer's location and address of the place of business
Otto-Von-Guericke-Allee 1, 39179, Barleben, Germany/
Otto-Von-Guericke-Allee 1, 39179 Barleben, Germany.
TABLETS DIACARB 250MG
Diakarb tablets 250 mg №30 are in pharmacology protivoglaucomny and miotic drugs. Means biconvex round shape, white.
The medicine diuretic and anti-epileptic actions. Inhibits carbonic anhydrase, reduces formation of aqueous humor, due to these effects the intraocular pressure is reduced. Antiepileptic activity is associated with a decrease in the brain carbonic anhydrase. Distribution:
in plasma, the highest concentration is observed after 1-3 hours;
reaction with proteins – up to 90%;
the half-life time equal to 4-9 hours;
per day is excreted in the urine 90% dose.
A means for therapy is used:
edema in heart failure and medication;
of glaucoma chronic open-angle, secondary, and in the pre-period short-term;
epilepsy in children with small seizures, in adults with large seizures, with a mixed manifestation of forms.
Mandatory consultation with a doctor, as there are contraindications and ambiguous interaction with some drugs.
The medicine is intended for internal reception. With edema, the daily rate is prescribed from one tablet. When glaucoma dose is used depending on the intraocular pressure. You can take 1-4 times a day with an open-angle form, on a tablet after 4 hours with a secondary. Also use 4 times a day for one tablet in attacks of closed-angle form of the disease.
In epilepsy the dose depending on the weight of 8-30 mg/kg, the optimum is 1 to 4 tablets.