Spironolactone - an assistant to the cardiovascular system. Spironolactone: instructions for use, analogs and reviews, prices in Russian pharmacies Application for violations of liver function

Instruction

Spironolactone 25 mg is a potassium-sparing diuretic that is prescribed to improve urine flow in various diseases.

Name

Tradename

Spironolactone.

International non-proprietary name

Spironolactone.

Latin name

Pharmacological group

Potassium-sparing diuretic.

Forms of release and composition

Available in the form of tablets, each of which contains 25 mg of spironolactone. Additionally, the composition includes lactose, starch, calcium stearate.

Sold in cardboard packs of 30 tablets in contour cells.

Mechanism of action of Spironolactone 25

Pharmacodynamics

Spironolactone is a diuretic. When stimulating urination, it retains potassium in the body. It has a long-term effect, the basis of which is competitive antagonism to aldosterone.

This hormone promotes fluid retention in the body, prevents the excretion of sodium, stimulates the release of potassium from the body. Spironolactone makes the collecting ducts of nephrons less sensitive to the effects of aldosterone.

By blocking the receptors for this hormone, it ensures the excretion of sodium and chlorine. Under its action, the pH of urine also changes.

The removal of excess fluid from the tissues provides a temporary reduction blood pressure.

The hypotensive effect of the drug allows it to be used for edema and other conditions that require rapid elimination. a large number liquids.

Spironolactone maintains the stability of the electrolyte balance. The potassium-sparing effect prevents the occurrence of muscle dyskinesias, neuralgia, and cardiac arrhythmias.

Pharmacokinetics

Absorbed by the walls when taken orally small intestine within 1-2 hours. The maximum effective concentration of the drug in the bloodstream is observed 2.5-3 hours after administration.

The bioavailability of the drug ranges from 90 to 99%. Approximately 90% of the active substance, when ingested, binds to plasma transport peptides.

The metabolism of the drug is under the influence of liver enzymes. In the liver, several active metabolites of spironolactone are formed, which step into competitive antagonism with aldosterone. The maximum concentration of active metabolites in the bloodstream is observed 4.5 hours after taking the drug.

Spironolactone can cross biological barriers. Its excretion occurs through the kidneys, a small amount of metabolites is excreted in the feces.

With prolonged use of the drug, cumulation phenomena may occur. The accumulation of spironolactone metabolites is due to the fact that some of them are excreted before 96 hours. Daily intake of the drug over time leads to an increase in its concentration in the blood.

What is Spironolactone 25 used for?

The tool can be prescribed in the following cases:

  • edema resulting from congestion in heart failure;
  • essential arterial hypertension;
  • lack of potassium, magnesium in the body;
  • Conn's syndrome elevated level secretion of aldosterone;
  • cirrhosis of the liver with ascites.

Contraindications

Spironolactone is not prescribed for the following conditions:

  • chronic kidney failure in the stage of decompensation;
  • acute renal failure;
  • hypersensitivity to any of the components included in the composition;
  • chronic renal failure;
  • Addison's disease;
  • hyperkalemia;
  • hypercalcemia;
  • hyponatremia;
  • menstrual disorders in women;
  • fermentopathy with lactose intolerance;
  • anuria.

With caution, the drug can be taken by patients with diabetic nephropathy, atrioventricular blockade, recently undergone surgery.

Method of application and dosage of Spironolactone 25

Before prescribing Spironolactone 25 mg, the physician should monitor the patient's fluid and electrolyte balance. It is also necessary to determine the level of certain hormones in the bloodstream.

After delivery laboratory tests the correct dose is selected, which depends on the disease and the condition of the patient's body.

With edematous syndrome resulting from cardiac disorders, 100-200 mg of the drug is prescribed per day. It is possible to increase the dose depending on the degree of edema. It is allowed to combine spironolactone with other diuretics to potentiate the action. The duration of the course of therapy in this case is from 2 to 3 weeks.

With a lack of potassium in the body daily dose funds is up to 300 mg. The drug is taken 2 or 3 times a day during meals. During the course of therapy, the electrolyte composition of the blood is monitored. If after 2 weeks of taking the potassium level has not returned to normal, it is possible to repeat the course of therapy after a while.

The drug can be used for the treatment and diagnosis of primary hyperaldosteronism. For the test, 400 mg of spironolactone is prescribed for 4 days. The level of potassium in the blood is monitored. If, after discontinuation of the drug, it decreases, we can talk about the presence of hyperaldosteronism in the patient.

Side effects

Undesirable effects that may occur during the course of therapy include:

  1. Gastrointestinal tract: nausea, vomiting, ulcerative defects of the mucous membranes of the stomach and intestines, inflammation of the gastrointestinal mucosa, colic, pain in the epigastrium, a change in the nature of the stool, a change in the activity of liver enzymes.
  2. Nervous system: impaired coordination, motor retardation, headaches, sleep disturbances, muscle spasms, impaired consciousness, dizziness, lethargic sleep.
  3. Endocrine system: an increase in the volume of the mammary gland in men with long-term use, erectile dysfunction, hirsutism in women, disorders menstrual cycle, coarsening of the voice, soreness of the mammary glands, uterine bleeding in the climax.
  4. Urinary system: acute impairment of renal function.
  5. Blood: megaloblastosis, decreased platelet count, agranulocytosis.
  6. Immune system: allergic manifestations, rashes, erythema, epidermal necrolysis.
  7. Others: alopecia, hypercreatininemia, calf cramps, hyperuricemia, hesitation water-salt metabolism, alkalosis or acidosis.

Overdose

With an overdose of this drug, nausea and vomiting occur. Blood pressure drops, diarrhea, dehydration phenomena may occur.

When taking large doses of spironolactone, gastric lavage should be performed. Must be accepted Activated carbon and see a doctor for symptomatic therapy. With a strong drop in blood pressure, the appointment of caffeine and other stimulant drugs is recommended.

The resulting hyperkalemia requires the normalization of water and electrolyte balance. For this, potassium-releasing diuretics, dextrose with insulin are prescribed. In severe overdose, hemodialysis may be prescribed.

Application features

Patients with diabetes should be cautious about taking this drug, as there is a risk of hyperkalemia.

With the simultaneous appointment of non-steroidal anti-inflammatory drugs, it is necessary to monitor renal function and electrolyte balance.

During pregnancy and lactation

The use of the drug for the treatment of pregnant and lactating women is not allowed. If there is a need to use spironolactone during breastfeeding, it is necessary to transfer the child to artificial feeding.

In old age

When prescribing a remedy for the elderly, the doctor must make sure that they do not have contraindications for use indicated in the instructions. A laboratory examination of the patient should be ordered if there is a suspicion of impaired renal or hepatic function. During the course of therapy, it is desirable to control the indicators of water and electrolyte balance.

drug interaction

With other drugs

Antihypertensive drugs may potentiate the effect of spironolactone. The same effect can be observed when it is combined with angiotensin-converting enzyme inhibitors. Such combinations lead to an increase in the level of potassium in the blood.

The concentration of digoxin in the bloodstream increases under the influence of spironolactone. The substance increases the concentration of lithium in plasma when taking products containing this trace element.

Glucocorticoids increase the effectiveness of the drug.

Alcohol compatibility

Terms and conditions of storage

It must be stored at a temperature not exceeding +30°C in a dark, dry place. Care should be taken to ensure that children do not have access to tablets.

The shelf life of the drug is 5 years. Application after the expiration date indicated on the package is not recommended due to a decrease in therapeutic properties.

Terms of dispensing from pharmacies

Released by prescription.

Are they sold without a prescription?

What is the price

The price depends on the place of purchase of the funds.

Analogues

Spironolactone analogues include:

  • Veroshpiron;
  • Spilacton;
  • Veroshpilakton;
  • Aldactone.

Description

Spironolactone 25mg

Violet round, biconvex film-coated tablets.

Spironolactone 100mg

Round, biconvex, film-coated tablets of dark purple color with a notch on one side.

Compound

Spironolactone 25mg

Spironolactone 25mg contains:

active substance - spironolactone - 25 mg;

Excipients: lactose monohydrate, corn starch, povidone K 25, magnesium stearate, talc, croscarmellose sodium,

shell: Opadry II 85 F 20086 Violet (Purified Talc, FD&C Blue No. 2 (Indigo Carmine, E132), Carmine (E120), Polyethylene Glycol, Titanium Dioxide, Polyvinyl Alcohol). Spironolactone 100mg

Each coated tablet Spironolactone 100mg contains: current substance - spironolactone -100 mg;

Excipients: lactose monohydrate, corn starch, povidone K 25, magnesium stearate, talc, croscarmellose sodium;

shell: opadri I 85 F 20084 purple (purified talc, FD&C Blue No. 2 (indigo carmine, E132), carmine (E120), polyethylene glycol, titanium dioxide, polyvinyl alcohol).

Pharmacotherapeutic group

Potassium-sparing diuretics. Aldosterone antagonists. Code ATX-C03DA01.

Pharmacological properties

Pharmacodynamics

Spironolactone is a potassium-sparing diuretic, a specific long-acting aldosterone antagonist (mineralocorticosteroid hormone of the adrenal cortex). In the distal nephron, spironolactone prevents aldosterone from retaining sodium and water and inhibits the potassium excretion effect of aldosterone. By binding to aldosterone receptors, it increases the excretion of sodium, chlorine and water ions in the urine, reduces the excretion of potassium and urea ions, and reduces the acidity of the urine.

The maximum effect is observed 7 hours after ingestion and lasts at least 24 hours. The hypotensive effect of the drug is due to the presence of a diuretic effect, which is unstable: the diuretic effect appears on the 2nd-5th day of treatment.

Pharmacokinetics

Spironolactone is well absorbed after oral administration and is mainly metabolized into active metabolites: sulfur-containing metabolites (80%) and partly canrenone (20%). The plasma half-life of Spironolactone is short (1.3 hours), the half-life of active metabolites is longer (from 2.8 to 11.2 hours). Excretion of metabolites occurs mainly through the urine, a small part is excreted in the feces. Spironolactone and its metabolites cross the placenta and are excreted in breast milk.

Following administration of 100 mg Spironolactone per day for 15 days to non-fasted healthy volunteers, Tmax was reached in 2.6 hours, Cmax was approximately 80 ng/mL, and Ti/2 was approximately 1.4 hours. For 7-alpha-(thiomethyl)spironolactone and canrenone - Tmax 3.2 hours and 4.3 hours, Cmax was 391ng/ml and 181ng/ml and T1/213.8 hours and 16.5 hours, respectively.

The action on the kidneys of a single dose of Spironolactone reaches its peak after 7 hours, and activity is maintained for at least 24 hours.

Indications for use

Congestive heart failure. Cirrhosis of the liver with ascites and edema. Malignant ascites. nephrotic syndrome. Diagnosis and treatment of primary aldosteronism.

Method of application and dosage

adults

Congestive heart failure with edema

The initial daily dose is 100 mg Spironolactone, administered as a single dose or divided into 2 doses, which can be adjusted in the range from 25 to 200 mg / day, depending on the response of the patient.

The maintenance dose must be determined individually.

Atpatients with severe heart failure ( NYHA Class III - IV )

Based on a randomized evaluation study (RALES), treatment in combination with standard therapy should be initiated at a dose of Spironolactone 25 mg once daily if potassium levels are ≤ 5 mEq/mL and serum creatinine ≤ 2.5 mg/dL. For patients who tolerate 25 mg once daily, the dose may be increased to 50 mg once daily according to clinical indications. For patients who cannot tolerate 25 mg once daily, the dose is reduced to 25 mg every other day.

Cirrhosis of the liver with ascites and edema

If the Na+/K+ ratio in the urine is greater than 1.0, the dose is 100 mg/day. If the ratio is less than 1.0, then 200-400 mg/day. In each individual case, the dose must be determined individually.

Malignant ascites

The initial dose is usually 100-200 mg/day. In severe cases, the dose may be gradually increased to 400 mg/day. Based on the dynamics of the development of edematous syndrome, the maintenance dose should be determined individually.

nephrotic syndrome

The usual dose is 100-200 mg/day. Spironolactone has not been shown to affect basal pathological process. Its use is only recommended if glucocorticoids alone are not effective enough.

Diagnosis and treatment of primary aldosteronism

Spironolactone can be used as an initial diagnostic test to identify primary hyperaldosteronism while patients are on a normal diet.

Long test: Spironolactone is administered at a daily dose of 400 mg for 3-4 weeks. Correction of hypokalemia and hypertension provides putative evidence for the diagnosis of primary hyperaldosteronism.

Quick test: Spironolactone is administered at a daily dose of 400 mg for four days. If serum potassium rises with spironolactone and falls when spironolactone is discontinued, a presumptive diagnosis of primary hyperaldosteronism should be considered. Once the diagnosis of hyperaldosteronism has been made following the final testing procedures, Spironolactone can be administered at doses of 100 mg to 400 mg per day in preparation for surgery. For patients who cannot be operated on, Spironolactone may be used for long-term therapy at a low effective dose determined for the individual patient.

Elderly patients

The recommended treatment should be started at a low dose and titrated to achieve desired effect. Caution should be exercised in patients with severe hepatic and renal insufficiency, which may alter drug metabolism and elimination.

Children

The initial daily dose should provide 3 mg Spironolactone per kilogram of body weight. Dosage should be adjusted based on response and tolerability. If necessary, the suspension can be obtained by grinding the tablets of Spironolactone.

Side effect

Gynecomastia may develop in connection with the use of Spironolactone. The development of gynecomastia depends on the dose and duration of spironolactone and is usually reversible after discontinuation of the drug. In rare cases, gynecomastia may persist.

The following side reactions are also possible:

General violations: general weakness.

Neoplasms benign, malignant and unspecified (including cysts and polyps): benign breast tumors.

Gastrointestinal Disorders: gastrointestinal disorders, nausea.

Naru blood and lymphatic system: leukopenia (including agranulocytosis), thrombocytopenia.

Hepatobiliary system disorders: liver dysfunction.

Metabolism and eating disorders: electrolyte imbalance, hyperkalemia.

From the musculoskeletal system: spasms of the calf muscles.

Violations by nervous system: dizziness.

Mental disorders: change in libido, confusion.

Violations from the side of the reproductive system and mammary gland: menstrual disorders, chest pain.

Skin disorders and subcutaneous tissue : Stevens-Johnson syndrome, toxic epidermal necrolysis, rash accompanied by eosinophilia and systemic symptoms (DRESS syndrome), alopecia, hypertrichosis, pruritus, rash, urticaria.

Renal and urinary disorders : acute renal failure. In case of occurrence adverse reactions, including those not listed in this leaflet, you should consult a doctor.

Contraindications

Hyperkalemia. Acute renal failure. Severe renal failure (creatinine clearance [CC] less than 10 ml / min). Anuria. Addison's disease. Hyponatremia. Pregnancy. Breast-feeding. Hypersensitivity to any of the components of the drug. Concomitant use of eplerenone or other potassium-sparing diuretics.

Spironolactone should not be taken concomitantly with other diuretics, slowing down the excretion of potassium, potassium supplements, since the development of hyperkalemia is possible.

With caution, the drug should be prescribed for hypercalcemia, metabolic acidosis, AV blockade (hyperkalemia contributes to its enhancement), diabetes mellitus (with confirmed or suspected chronic renal failure), diabetic nephropathy, surgical interventions, taking medications that cause gynecomastia, conducting local and general anesthesia, menstrual irregularities, breast enlargement, liver failure, cirrhosis of the liver, as well as elderly patients.

Overdose

Symptoms: nausea, vomiting, dizziness, diarrhea, skin rash, hyperkalemia (paresthesia, muscle weakness, arrhythmias), hyponatremia (dry mouth, thirst, drowsiness), hypercalcemia, dehydration, increased urea concentration.

Treatment: gastric lavage, symptomatic treatment of dehydration and arterial hypotension. In case of hyperkalemia, it is necessary to normalize the water-electrolyte metabolism with the help of potassium-releasing diuretics, rapid parenteral administration of a dextrose solution (5-20% solutions) with insulin at the rate of 0.25-0.5 IU per 1 g of dextrose; if necessary, repeated administration of dextrose is possible.

Precautionary measures

When using Spironolactone, a temporary increase in the level of urea nitrogen in the blood serum is possible, especially with reduced kidney function and hyperkalemia. It is also possible to develop hyperchloremic metabolic acidosis. When prescribing Spironolactone to patients with impaired renal and hepatic function, elderly patients need regular monitoring of blood serum electrolytes and kidney function.

Hyperkalemia can develop in patients with impaired renal function or in patients with excessive potassium intake and lead to the development of fatal arrhythmias. In the event of hyperkalemia, spironolactone should be discontinued and vigorous measures taken to reduce serum potassium to normal level. Simultaneous use of Spironolactone with other potassium-sparing diuretics, angiotensin-converting enzyme (ACE) inhibitors, non-steroidal anti-inflammatory drugs, angiotensin II antagonists, aldosterone blockers, heparin, low molecular weight heparins or other drugs that contribute to the development of hyperkalemia, as well as in conditions where hyperkalemia may occur (potassium supplements, a diet rich in potassium or salt substitutes containing potassium) can lead to the development of severe hyperkalemia.

Guyperkalemia in patients with severe heart failure

Hyperkalemia can be fatal. Careful monitoring and regulation of the level of potassium in the blood is necessary in the case of the appointment of Spironolactone in patients with severe heart failure. Other potassium-sparing diuretics should be avoided. Potassium supplementation should be avoided in patients with serum potassium > 3.5 mEq/L. It is recommended to monitor potassium and creatinine levels for one week after starting or increasing the dose of Spironolactone, then monthly for the first 3 months, then quarterly for a year, then every 6 months. If the serum potassium level is more than 5 mEq / l or the serum creatinine level is more than 4 mg / dl, treatment should be discontinued.

Despite the absence of a direct effect on carbohydrate metabolism, the presence of diabetes, especially with diabetic nephropathy, requires special care when prescribing Spironolactone because of the possibility of developing hyperkalemia.

During treatment with Spironolactone, drinking alcohol is contraindicated, and food rich in potassium should be avoided.

Use in children

Influence on the ability to drive vehiclessports and machine control

In the initial period of treatment, it is forbidden to drive a car and engage in activities that require increased concentration of attention and speed of psychomotor reactions. The duration of the restrictions is set individually.

Application forliver dysfunction

With caution, the drug should be prescribed for liver failure, cirrhosis of the liver.

When Spironolactone is prescribed to patients with liver disorders, regular monitoring of blood serum electrolytes and kidney function is necessary.

Application for violations of kidney function

The drug is contraindicated in severe renal failure (CC less than 10 ml / min). With caution, the drug should be prescribed for diabetic nephropathy.

When prescribing Spironolactone to patients with impaired renal function, regular monitoring of blood serum electrolytes and kidney function is necessary.

Use during pregnancy and lactation

The use of Spironolactone is contraindicated during pregnancy and during breastfeeding.

Interactionwith other medicines

Simultaneous administration of drugs that promote the development of hyperkalemia with Spironolactone can lead to the development of severe hyperkalemia.

Spironolactone may increase the serum concentration of digoxin and interfere with the assessment of the level of digoxin concentration in the blood serum. In patients receiving digoxin and spironolactone, careful monitoring is necessary to assess for an increased or decreased effect of digoxin.

When Spironolactone is added, the effect of antihypertensive drugs is enhanced, which may require a reduction in their dosages, further dose adjustment is necessary.

Since ACE inhibitors reduce aldosterone production, they should not be given routinely with spironolactone, especially in patients with severe renal insufficiency.

Taking carbenoxolone can lead to sodium retention, and thus reduce the effectiveness of Spironolactone, their simultaneous use should be avoided.

Non-steroidal anti-inflammatory drugs such as aspirin, indomethacin and mefenamic acid can weaken the natriuretic effect of diuretics by inhibiting intrarenal prostaglandin synthesis and reduce the diuretic effect of Spironolactone.

Spironolactone reduces the vascular response to norepinephrine. Caution must be exercised in the case of local or general anesthesia in patients taking Spironolactone.

In fluorometric assays, Spironolactone may interfere with the evaluation of compounds with similar fluorescence characteristics.

Package

Cardboard box containing 100 tablets (10 blisters of 10 tablets).

Manufacturer

Pharmaceutical company "Iran Hormone"

PharmaceuticalCompany " IranHormone"

Address: 11 KMKaraj Special Road, 13185-1767 Tehran, Islamic Republic of Iran. Tel.:

98 21 44905513-9. Fax: +98 21 44905512 address: . Email mail: [email protected].com

In the pharmacy market, you can find many drugs that are used as diuretics. AT medical practice The drug Spironolactone is widely used. Often it is prescribed for pathologies that are accompanied by ascites and edema, to remove excess fluid from the body.

In this article we will tell you what the drug is intended for, what indications, contraindications and side effects. We will also consider the main schemes, the features of taking the medicine for various diseases and its analogues.

What is medicine Spironolactone? This is a drug used to treat various diseases and pathological conditions, which are accompanied or provoked by the accumulation of excess fluid in the body. Let's consider it in more detail.

Drug group, INN, scope

Spironolactone is classified as a special drug group- potassium-sparing diuretics, aldosterone antagonists. Diuretics are diuretics that increase diuresis. Their disadvantage is that they are able to flush out useful substances and trace elements from the body.

Aldosterone antagonists - a group of drugs that block aldosterone receptors, while increasing the excretion of sodium, chlorine and fluid, and potassium and urea in the kidneys remain unchanged. That is, such drugs have a diuretic, antihypertensive and at the same time potassium-sparing effect.

International generic name- This is the unique name of the active ingredient that is contained in the medicine. It determines its action. In this case, the INN is the same as trade name- Spironolactone.

used medication in different areas. Most often, it is prescribed to eliminate edema and ascites in kidney disease or cardiovascular pathologies. Also, such a diuretic is used to reduce weight by removing excess fluid, to eliminate acne, acne and other skin imperfections.

Release forms

Spironolactone is available in several pharmacological forms(Table 1).

Table 1 - Forms of release of the drug

View Characteristic
Capsules or tablets The tablets are white. Gelatin capsules are also white and cylindrical in shape. Inside they contain a white powder with granules. Both forms are for internal use. Depending on the amount of the active ingredient, they are divided into the following types:
  • Spironolactone 25 mg;
  • Spironolactone 50 mg;
  • Spironolactone 100 mg. Pack the medicine in blisters of 10 pieces. There may be 2 or 3 blisters (20 or 30 tablets) in a carton box.
Ampoules They are sold under the name Aldactone (Spironolactone). One ampoule contains 0.2 g of the active ingredient per 10 ml. The drug is administered intravenously. This form is used only under the supervision of a doctor in a hospital.
Cream There is a special form of medicine that is used exclusively externally. This is spironolactone cream. This drug is used to treat problematic facial skin (acne, acne).

Any form of the drug is used if there are appropriate indications. It is also important to follow the rules of use, the recommended dosage.

Average prices in Moscow

The price of the drug depends on several factors, primarily on the concentration of the active substance that is part of the product, the number of tablets or capsules in the package. Also, the pricing policy of a particular pharmacy affects the pricing policy. Average prices for the city of Moscow are presented in the table (Table 2).

Table 2 - Cost of Spironolactone

Name and amount of active substance Manufacturer Average price in Moscow pharmacies, rub.
Spironolactone 25 mg (20 tablets) Sintez JSC, Russia from 34 to 40
Spironolactone 25 mg (30 pieces) Minskintercaps, Belarus 60
Spironolactone 50 mg (30 pieces) Minskintercaps, Belarus 160-170
Spironolactone Sandoz 50 mg (30 tablets) Salutas Pharma, Germany 180
Spironolactone Sandoz 100 mg (30 tablets) Salutas Pharma, Germany 250
Spironolactone Maxogen-S night cream (60 ml) Minoxidil Max about 2800
Spironolactone Maxogen-S day cream (60 ml) Minoxidil Max around 2700

Slightly prices may vary in different cities, different pharmacies. As a rule, medicines are cheaper in online pharmacies. Also, their advantage is fast (often free in the city) delivery.

Composition and useful properties

The preparation contains active substance- spironolactone. it Chemical substance treat potassium-sparing diuretics. It is also an antagonist of aldosterone and other mineralocorticoids (corticosteroid hormones of the adrenal cortex).

This component provides:

  • diuretic effect (removes sodium, chlorine and excess water);
  • maintaining the level of potassium and urea;
  • decreased acidity of urine;
  • a slight decrease in blood pressure (the effect is not permanent).

in different dosage forms contains unequal amounts of spironolactone. This should be considered before prescribing the drug. The tablets also have auxiliary components - corn starch, lactose, magnesium stearate, sodium lauryl sulfate and others. The capsule shell consists of glycerin, gelatin and food additive E 218.

Indications for use

The medicine should be taken only if indicated. Most often, the drug is prescribed for such pathologies:


In some diseases, the drug is prescribed as monotherapy. But in most cases it is used in the composition complex treatment(for example, in chronic heart failure, which is accompanied by edema).

Main contraindications

It is also strictly forbidden to take the medicine simultaneously with potassium-sparing diuretics, as well as drugs that contain potassium. This can lead to the development of hyperkalemia.

Pharmacodynamics and pharmacokinetics

The mechanism of action of the drug is based on the activity of spironolactone - its active component. Pharmacokinetics is the ability of this substance to affect the distal tubules of the kidneys. By blocking special aldosterone receptors, spironolactone provides:

  • potassium retention;
  • retention of urea in the kidneys;
  • excretion of sodium, chlorine and water;
  • increased diuresis;
  • decrease in urine acidity.

Due to the increased excretion of urine from the body, there is also a non-permanent situational effect of lowering blood pressure. The maximum effect of the drug is observed 6 hours after its internal administration and lasts about a day. The diuretic effect appears after 3-5 days of daily medication.

Pharmacokinetics consists in the totality of the processes of absorption, distribution and excretion of the drug. When taking tablets orally, the active substance is quickly and completely (bioavailability 100%) absorbed into gastrointestinal tract. Its maximum concentration in the blood occurs after 6 hours.

Spironolactone binds to blood proteins by 96%. At the same time, it is practically not absorbed into tissues and organs, but it is able to easily penetrate the placental barrier and into breast milk.

The process of metabolism (transformation and processing) of the drug occurs in the liver. The elimination half-life occurs 12-24 hours after ingestion. The drug is excreted in the form of metabolites and partially unchanged along with urine and feces. With pathologies of the liver and kidneys, the half-life increases without signs of accumulation (cumulation).

Instructions for use

Before starting treatment with Spironolactone, you should read the instructions for its use. Depending on the indications and special conditions of the patient, different forms drug, and its dosage is also determined.

Tablet form

Tablets are prescribed most often. As a rule, they are taken once a day with food. There are several dosing regimens that depend on the pathology:

  1. Children are first prescribed a dosage based on their body weight - 3 mg of the active substance per kilogram of the child's weight. Further, the dose is adjusted depending on the response and tolerability of the drug.
  2. Elderly patients are prescribed the minimum dose first. Then it is gradually increased until the maximum therapeutic effect is reached.

The drug in ampoules

Remedy for intravenous administration available in glass ampoules. One ampoule contains 200 mg of the active ingredient. The medicine is injected into a vein. Such treatment is possible only in a hospital setting if it is impossible to take the drug orally.

Cream

Cream for external application is available in a volume of 60 ml. The content of spironolactone is 5%. This remedy is used to reduce the androgenic effect. It is used for:

  • thinning hair;
  • their loss;
  • as a prevention of baldness.

Spironolactone blocks the effect of male hormones on the scalp, which prevents hair loss. At the same time, the cream does not stimulate hair growth.

To achieve the effect, it is enough to apply a small amount of cream on the scalp with rubbing movements 2 times a day - in the morning rub the day cream, which also contains caffeine and vitamin E, use the night cream in the evening.

Possible side effects

The drug is not completely safe. It is a diuretic, so it can provoke a number of side effects:


Also, in some cases, taking the drug causes negative effects in women, which are manifested by a decrease in sexual desire and a number of gynecological pathologies (gynecomastia, menstrual irregularities, early menopause, infertility).

Some features of therapy

In addition to the main indications, the drug is often used for skin diseases, as well as for the purpose of weight loss. What are the features of taking the drug in such conditions? Let's consider them in more detail.

acne treatment

Such a drug is effective only when acne has arisen due to hormonal failure. Spironolactone does not treat ordinary blackheads and subcutaneous whiteheads. This remedy has an antiandrogenic property, that is, the ability to influence hormonal fluctuations. In addition, the drug reduces the production of sebum. These properties help to reduce skin rashes.

To reduce the number of hormonal rashes, you should take Spironolactone tablets every day until the acne disappears. The daily dose is from 100 to 200 mg, depending on the condition of the skin and the age of the patient.

For safe therapy, you should also adhere to the following rules:

  1. Do not take the drug for women under 30 years of age.
  2. Do not continue therapy for more than 6 months.
  3. Stop taking the drug in case of menstrual irregularities and consult a mammologist, as there is an opinion that this remedy increases the risk of developing breast tumors.

For weight loss

Since the drug is classified as a diuretic, it is often used to reduce body weight. This effect is achieved by removing excess fluid from the body and eliminating both external and internal edema. However, this method has its pros and cons, which you should definitely familiarize yourself with.


Cons of this method of losing weight:

  1. Sodium and calcium are actively washed out of the body, which negatively affects the health of losing weight.
  2. After stopping the drug, the weight returns very quickly again, which provokes impaired renal function, loss of skin elasticity. Kilograms go away not due to a decrease in fat mass, but only due to getting rid of the fluid that is essential for the normal functioning of the body.

The dosage of the drug used for weight loss should be minimal - 25-100 mg during the day.

The course should not last more than two weeks. The diuretic effect is observed not immediately, but after 2-3 days. Therefore, you should not increase the dose, otherwise you can provoke an overdose.

Talk to your doctor before using Spironolactone to treat conditions such as acne prone skin or obesity. Self-medication can harm the health of the whole organism.

Analogues

There are many drugs that have similar action on the body, as Spironolactone.

Structural

The best drug substitutes are its structural analogues. These are drugs that have the same active ingredient. Therefore, they are prescribed for the same pathologies, have the same contraindications and side effects. Among them, the most popular and inexpensive:


Preparations based on other components

In case of intolerance to the active substance, drugs of other groups are often prescribed that have a similar effect. The most effective of them:


Any diuretic should be taken only if indicated and under the supervision of a physician. You should not replace the agent with an analogue yourself. This can lead to negative reactions and bad consequences.

Spironolactone is a potassium-sparing diuretic. Instructions for use reports that 25 mg tablets have diuretic properties. Doctors - cardiologists indicate that the drug helps in the treatment of hypertension, edema and hyperaldosteronism.

Release form and composition

Spironolactone is available in the form of white tablets for oral administration in blisters of 10 pieces, 2 blisters in a cardboard box with instructions.

Each tablet of the drug contains 25 mg of the active ingredient - Spironolactone, as well as a number of excipients including lactose monohydrate.

pharmachologic effect

Spironolactone is a potassium-, magnesium-sparing diuretic, a competitive aldosterone antagonist influencing the distal nephron, increases the excretion of Na +, Cl- and water and reduces the excretion of K + and urea, reduces the titratable acidity of urine.

Increased diuresis leads to a hypotensive effect, which is unstable. The hypotensive effect does not depend on the content of renin in the blood plasma and is not manifested in normal blood pressure. diuretic effect usually manifests itself on days 2-5 of therapy.

Indications for use

What helps Spironolactone? Tablets have the following indications for use:

  • cirrhosis of the liver;
  • polycystic ovary syndrome;
  • aldosterone-producing adrenal adenoma;
  • premenstrual syndrome;
  • swelling in the second and third trimester of pregnancy;
  • edema on the background of chronic heart failure;
  • nephrotic syndrome;
  • arterial hypertension;
  • primary hyperaldosteronism.

Instructions for use

Spironolactone is prescribed in an individual dosage, depending on the severity of disturbances in water and electrolyte metabolism and hormonal status.

With edematous syndrome - 100-200 mg per day (less often - 300 mg per day) in 2-3 doses (usually in combination with a "loop" or / and thiazide diuretic) daily for 14-21 days. Dose adjustment should be carried out taking into account the values ​​of the concentration of potassium in the plasma. If necessary, courses are repeated every 10-14 days.

With severe hyperaldosteronism and reduced plasma potassium - 300 mg per day in 2-3 doses. Cirrhosis of the liver: if the Na / K ratio is more than 1.0, the daily dose is 100 mg, if the ratio is less than 1.0 - 200-400 mg per day.

See also: how to relieve swelling and reduce pressure with an analogue.

Contraindications

  • Addison's disease;
  • lactation period;
  • anuria;
  • hypersensitivity to the components of Spironolactone;
  • pregnancy;
  • hyponatremia;
  • hyperkalemia;
  • lactase intolerance, lactose deficiency, glucose-galactose malabsorption syndrome;
  • children's age up to 3 years;
  • severe chronic renal failure (creatinine clearance less than 10 ml/minute).

Carefully:

  • liver failure;
  • elderly age;
  • hypercalcemia;
  • diabetes mellitus with confirmed or suspected chronic renal failure;
  • diabetic nephropathy;
  • atrioventricular block;
  • local and general anesthesia;
  • surgical interventions;
  • dysmenorrhea;
  • gynecomastia or concomitant use of drugs that cause gynecomastia;
  • metabolic acidosis.

Side effects

  • Muscle spasms, decreased potency;
  • Endocrine system: with prolonged use - gynecomastia; in men - erectile dysfunction; in women - coarsening of the voice, amenorrhea, hirsutism, metrorrhagia during menopause, dysmenorrhea, soreness and carcinoma of the breast;
  • Hematopoietic system: thrombocytopenia, agranulocytosis, megaloblastosis;
  • Digestive system: abdominal pain, nausea, vomiting, intestinal colic, gastritis, ulcers and bleeding in the gastrointestinal tract, constipation, diarrhea;
  • Allergic reactions: drug fever, itching, urticaria, maculopapular and erythematous rash;
  • Central nervous system: headache, ataxia, lethargy, drowsiness, dizziness, lethargy;
  • Metabolism: hypercreatininemia, hyperuricemia, increased urea concentration, disturbances in water-salt metabolism and acid-base balance (alkalosis or hypochloremic metabolic acidosis).

During pregnancy and lactation

There are no data on the negative impact of spironolactone on the course of pregnancy and fetal development. However, in the 1st trimester of pregnancy, the use is contraindicated, in the 2nd and 3rd trimesters, it can be used according to indications.

If it is necessary to use during lactation, it should be borne in mind that the metabolite of spironolactone canrenone is excreted in breast milk in small quantities.

special instructions

During the period of treatment with Spironolactone, patients should be careful in driving a car or operating complex machinery, since dizziness and drowsiness may occur during therapy.

Tablets with particular caution should be used in patients with atrioventricular blockade due to the risk of hyperkalemia. For the same reason, treatment with the drug is carried out with caution in patients with cirrhosis of the liver and people who are awaiting surgery.

When prescribing Spironolactone tablets to a patient in combination with other diuretics or drugs for the treatment arterial hypertension it is important to adjust the dose of the latter so as not to cause the patient to develop severe side effects.

During treatment with the drug, the patient must periodically take tests to monitor the level of electrolytes in the body and the level of urea in the blood.

The composition of the tablets includes lactose monohydrate, so patients with congenital intolerance to this component, the drug is contraindicated.

drug interaction

Simultaneous administration with drugs containing potassium, as well as potassium-sparing diuretics, dietary supplements for food and table salt substitutes that contain potassium, leads to the development of hyperkalemia.

Simultaneous reception enhances the action of Gonadorelin, Buserelin and Triptorelin. Simultaneous administration with lithium carbonate increases the concentration of lithium in the blood plasma, with cholestyramine - causes hypochloremic alkalosis, with eprosartan, losartan and candesartan - increases the risk of hyperkalemia.

Analogues of the drug Spironolactone

According to the structure, analogues are determined:

  1. Veroshpilakton;
  2. Spironolactone micronized;
  3. Veroshpiron;
  4. Spironol;
  5. Uracton;
  6. Spironaxane;
  7. Spironolactone Darnitsa;
  8. Spirix;
  9. Aldactone.

To pharmacological group diuretics include analogues:

  1. Adelfan Ezidrex;
  2. Indapamide;
  3. Aquaphor;
  4. Indapamide Sandoz;
  5. Diacarb;
  6. Torasemide;
  7. Uroflux;
  8. Mannitol;
  9. Bufenox;
  10. Acripamide;
  11. Indapsan;
  12. Hygroton;
  13. Ionic;
  14. Triamtel;
  15. Christepin;
  16. Retapress;
  17. Britomar;
  18. Edarbi Clo;
  19. Furosemide;
  20. Isobar;
  21. Tenzar;
  22. Pamid;
  23. Indapres;
  24. Hydrochlorothiazide;
  25. Urea;
  26. Urological (diuretic) collection;
  27. Hypothiazide;
  28. Hydrochlorothiazide;
  29. Arifon;
  30. Inspra;
  31. Lorvas;
  32. Brinerdin;
  33. Lasix;
  34. Nebilong N;
  35. Indap;
  36. Trigrim;
  37. Diuver;
  38. Indapamide retard;
  39. Arifon retard;
  40. Kanefron H;
  41. Ipres long;
  42. Fursemide;
  43. Synepres;
  44. Cymalon;
  45. Clopamid;
  46. Mannitol;
  47. Brusniver;
  48. Acetazolamide;
  49. Zokardis plus;
  50. Eplerenone.

Holiday conditions and price

The average cost of Spironolactone (tablets 25mg No. 20) in Moscow is 40 rubles. The drug is dispensed from pharmacies by prescription.

The shelf life of tablets is 5 years from the date of production, which is indicated on the package. At the end of the shelf life, the tablets should not be taken orally.

Store Spironolactone tablets instructions for use out of the reach of children, avoiding contact with sun rays for the drug.

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Spironolactone is a magnesium-sparing and potassium-sparing diuretic.

It is a competitive aldosterone antagonist, reduces the titratable acidity of urine, increases the excretion of chloride ions, sodium ions, water, and also reduces the excretion of potassium and urea ions.

Each tablet contains 25 mg of the active ingredient - Spironolactone, as well as a number of excipients, including lactose monohydrate.

The diuretic effect develops 2-5 days after the start of the drug.

After oral administration, the active substance is rapidly absorbed in the digestive tract and about 90% binds to plasma proteins. Bioavailability is 92-99% and increases when taken with food.

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Price in pharmacies

Information about the price of Spironolactone in Russian pharmacies is taken from the data of online pharmacies and may differ slightly from the price in your region.

You can buy the drug in pharmacies in Moscow at a price: Spironolactone 25mg tablets 20 pieces - from 40 to 63 rubles.

Conditions for dispensing from pharmacies - by prescription.

Store at temperatures up to 25 ° C in a dry, dark place and out of the reach of children. Shelf life - 5 years.

The list of analogues is presented below.

What is Spironolactone for?

The drug is prescribed in the following cases:

  • edema of various origins - caused by preeclampsia in pregnant women, associated with heart failure;
  • edema in cirrhosis of the liver;
  • nephrotic syndrome, accompanied by edema;
  • arterial hypertension caused by adrenal adenoma;
  • primary hyperaldosteronism;
  • hypokalemia;
  • premenstrual syndrome;
  • polycystic ovaries in women.

Instructions for use Spironolactone 25 mg, doses and rules

The dose of the drug is set individually, depending on the severity of violations of water and electrolyte metabolism and hormonal status.

With edema of various origins, the standard dosage of Spironolactone is from 100 to 200 mg of the drug per day, in severe cases the daily dose can be increased to 300 mg for 5 days in combination with thiazide or loop diuretics. The dose of the drug is usually divided into 2-3 doses at regular intervals. According to the instructions for use, the maintenance daily dose is selected individually: the minimum is 1 tablet Spironolactone 25 mg, the maximum is 200 mg.

Essential hypertension - from 50 to 100 mg once a day, if necessary, the dose is gradually (1 time in 2 weeks) increased to 200 mg. An adequate response to therapy is usually observed after 2 weeks.

Hypokalemia and hypomagnesemia caused by the use of diuretics: 25-100 mg per day in one or more divided doses. If oral potassium preparations or other methods of replenishing its deficiency are ineffective, the daily dose may be increased to the maximum allowable - 400 mg.

Edema due to nephrotic syndrome (in case of failure of other types of therapy) - from 100 to 200 mg.

With severe hyperaldosteronism and a reduced level of potassium in the plasma, 300 mg per day is prescribed in 2-3 doses.

Dose adjustment is carried out taking into account the content of potassium in the plasma. If necessary, courses of therapy are repeated every 10-14 days.

For children with edema, Spironolactone is prescribed at 1–3.3 mg/kg of body weight (30–90 mg/m2) per day for 1–4 doses. Dose adjustments are made after 5 days. If necessary, it can be increased by 3 times compared to the initial one.

Important information

Tablets with particular caution should be used in patients with atrioventricular blockade due to the risk of hyperkalemia. For the same reason, treatment with the drug is carried out with caution in patients with cirrhosis of the liver and people who are awaiting surgery.

During treatment with the drug, it is necessary to periodically take tests - to control the level of electrolytes in the body and the level of urea in the blood.

When prescribing Spironolactone in combination with other diuretics or drugs for the treatment of arterial hypertension, it is important to adjust the dose of the latter so as not to cause the development of severe side effects.

Use during pregnancy and lactation

Animal studies have found negative effects of spironolactone on the fetus. Clinical trials involving pregnant women have not been conducted. Spironolactone should not be taken during the 1st trimester of pregnancy. In the 2nd and 3rd trimesters - only with serious illnesses, as prescribed by a physician who evaluates the possible benefits and risks.

The active metabolite of spironolactone, caneron, passes into breast milk. Breastfeeding should be discontinued if therapy during lactation is clinically justified.

Application features

Before using the drug, read the sections of the instructions for use on contraindications, possible side effects and other important information.

Side effects of Spironolactone

Instructions for use warns of the possibility of side effects of the drug Spironolactone 25 mg:

  • From the side of cardio-vascular system: arterial hypotension, arrhythmia (in patients with renal insufficiency and those receiving potassium supplements), vasculitis.
  • From the blood and lymphatic system: leukopenia (including agranulocytosis), thrombocytopenia, megaloblastic or aplastic anemia, eosinophilia.
  • From the nervous system and psyche: headache, drowsiness, dizziness, ataxia, paralysis, paraplegia, lethargy, lethargy, confusion.
  • From the side respiratory system, bodies chest and mediastinum: change in the timbre of the voice.
  • From the digestive tract: nausea, vomiting, loss of appetite, pain in the abdomen and stomach, diarrhea, constipation, intestinal colic, gastritis, stomach ulcer and duodenum, stomach bleeding.
  • From the side digestive system: hepatitis, liver dysfunction.
  • From the urinary system: acute renal failure.
  • From the musculoskeletal system and connective tissue: osteomalacia, muscle spasm, muscle cramps of the lower extremities.
  • On the part of metabolism and metabolism: hyperkalemia, hyponatremia, hypercreatininemia, increased plasma urea levels, hyperuricemia, porphyria, metabolic hyperchloremic acidosis or alkalosis, dehydration.
  • From the endocrine system: hirsutism.
  • On the part of the reproductive system and mammary glands: decreased libido, erectile dysfunction, gynecomastia, menstrual disorders, dysmenorrhea, amenorrhea, metrorrhagia during menopause, swelling and pain in the mammary glands in women, infertility (when used in high doses- 450 mg / day), a benign breast tumor.
  • From the side immune system, skin and subcutaneous tissue: hypersensitivity reactions, including: rash, itching, urticaria, drug fever; hypertrichosis, alopecia, lupus-like syndrome, hyperemia, erythema annulare, eczema, Stevens-Johnson syndrome.
  • General: asthenia, fatigue.

Contraindications

Spironolactone is contraindicated in the following diseases or conditions:

  • Hypersensitivity to spironolactone;
  • Addison's disease;
  • Hyperkalemia;
  • Hyponatremia;
  • Severe renal failure (Cl creatinine<10 мл/мин);
  • Anuria;
  • Simultaneous use of eplerenone and other potassium-sparing diuretics, potassium preparations (risk of hyperkalemia);
  • Pregnancy and breastfeeding;
  • Children's age (up to 3 years).

Use with extreme caution:

  • AV blockade (possibility of amplification due to the development of hyperkalemia);
  • Diabetes mellitus (with confirmed or suspected chronic renal failure);
  • diabetic nephropathy;
  • Dysmenorrhea;
  • hypercalcemia;
  • metabolic acidosis;
  • Liver failure, cirrhosis of the liver;
  • Surgical interventions;
  • Gynecomastia and simultaneous use of drugs that cause gynecomastia;
  • Carrying out local and general anesthesia;
  • Elderly age.

Overdose

Overdose symptoms - diarrhea, nausea, vomiting, dehydration, hypercalcemia, hyponatremia (thirst, dry mouth, drowsiness), hyperkalemia (weakness, myasthenia gravis, paresthesia, arrhythmias), increased urea concentration, decreased blood pressure, dizziness, skin rash.

Recommended gastric lavage. Therapy of arterial hypotension and dehydration is symptomatic. In the case of hyperkalemia, normalization of water-electrolyte metabolism with potassium-releasing diuretics, rapid parenteral administration of a 5–20% dextrose solution (glucose) with insulin at the rate of 0.25–0.5 units per 1 g of dextrose (glucose) is shown.

If the need arises, dextrose (glucose) is administered repeatedly. In cases of severe intoxication, hemodialysis is performed.

List of analogs Spironolactone

If necessary, replace the drug, there are two options - choosing another drug with the same active ingredient or a drug with a similar effect, but with a different active substance. Drugs with a similar effect are united by the coincidence of the ATX code.

Spironolactone analogues, list of drugs:

  1. Aldactone;
  2. Vero-Spironolactone;
  3. Veroshpilakton.

ATX code matches:

  • aldactone,
  • Veroshpiron,
  • spirix,
  • Spirinol,
  • Uracton.

When choosing a replacement, it is important to understand that the price, instructions for use and reviews of Spironolactone 25 mg do not apply to analogues. Before replacing, you must obtain the approval of the attending physician and do not replace the drug yourself.

According to people who took the drug, Spironolactone is an effective and inexpensive diuretic drug. However, it has many contraindications and can cause side effects, so it should only be used as prescribed by a doctor and under his close supervision.

Special Information for Healthcare Professionals

Interactions

Reduces the effect of anticoagulants, incl. indirect (heparin, coumarin derivatives, indandione) and the toxicity of cardiac glycosides (since the normalization of the potassium content in the blood prevents the development of toxicity).

Enhances the metabolism of phenazone.

Reduces the sensitivity of blood vessels to norepinephrine (requires caution when conducting anesthesia).

Increases T1 / 2 of digoxin - digoxin intoxication is possible.

Enhances the toxic effect of lithium due to a decrease in its clearance.

Accelerates the metabolism and excretion of carbenoxolone. Carbenoxolone promotes sodium retention by spironolactone.

GCS and diuretics (benzothiazine derivatives, furosemide, ethacrynic acid) enhance and accelerate the diuretic and natriuretic effect.

Enhances the effect of antihypertensive drugs.

NSAIDs reduce the diuretic and natriuretic effect, increasing the risk of developing hyperkalemia.

The risk of developing hyperkalemia increases when taken with potassium supplements, potassium supplements and potassium-sparing diuretics, ACE inhibitors (acidosis), ARA II, aldosterone blockers, indomethacin, cyclosporine.

Salicylates, indomethacin reduce the diuretic effect.

Ammonium chloride, cholestyramine contribute to the development of hyperkalemic metabolic acidosis.

Fludrocortisone causes a paradoxical increase in tubular potassium secretion.

Reduces the effect of mitotane.

Enhances the effect of triptorelin, buserelin, gonadorelin.

Ethanol, barbiturates, narcotic analgesics increase orthostatic hypotension.

special instructions

With caution, the drug should be used for AV blockade, decompensated liver cirrhosis, surgical interventions, taking drugs that cause gynecomastia, local and general anesthetics.

When using Spironolactone, it is impossible to prescribe drugs containing potassium, as well as other diuretic drugs that cause potassium retention in the body. Use with carbenoxolone, which causes sodium retention, should be avoided.

During therapy, the content of electrolytes and urea in the blood should be periodically determined.

When used in combination with other diuretic or antihypertensive drugs, the dose of the latter should be reduced. When using Spironolactone with digoxin, it may be necessary to reduce the loading and maintenance dose of the latter.


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