Mechanism of action
Potassium-sparing diuretic. As an aldosterone antagonist, it is competitively associated with aldosterone receptors in the distal renal tubules. The drug increases the excretion of sodium ions and water, while reducing the excretion of potassium and Magnesium ions.
The diuretic effect develops at 2-5 days of treatment and persists for 2-3 days after discontinuation of the drug.
When ingestion is absorbed from the gastrointestinal tract. Bioavailability is 90%. Food intake enhances the absorption and bioavailability of spironolactone.
Plasma protein binding - 90%.
Spironolactone and its metabolites pass through the placenta, are excreted in breast milk.
Rapidly metabolized in the liver. Subject to the effect of "first pass".
The main metabolites of spironolactone is canrenone and 7-alpha (thiomethyl) -spironolactone.
Spironolactone and metabolites are excreted in the urine, partly in the bile and feces.
Indications and usage
- Edema syndrome in chronic heart failure, liver cirrhosis, nephrotic syndrome;
- Essential arterial hypertension (in adults);
- primary hyperaldosteronism (to clarify the diagnosis and short-term preoperative treatment);
- Prevention of hypokalemia in the treatment of saluretics;
At edema syndrome in chronic heart failure drug is prescribed for adults in the initial daily dose of 25 mg. The maximum dose is 100 mg / day. Maintenance dose is determined individually.
At edema syndrome in liver cirrhosis the drug is prescribed in a dose of 100-400 mg / day (depending on the ratio of potassium and sodium). Maintenance dose is determined individually.
At edema syndrome in nephrotic syndrome the drug is prescribed in a dose of 100-200 mg / day.
At essential hypertension the initial daily dose is 50-100 mg (divided into several doses). If necessary, the daily dose is gradually increased to 200 mg over 2 weeks. Duration of treatment for at least 2 weeks.
For prevention of hypokalemiacaused by taking saluretiki, Verospiron used in a daily dose of 25-100 mg.
Verospiron can be used for initial diagnostics as an indirect indicator. primary aldosteronism in patients on a normal diet. To do this, conduct tests.
Long test: for adults Verospiron prescribed in a daily dose of 400 mg for 3-4 weeks. The elimination of hypokalemia and hypertension indirectly indicates primary hyperaldosteronism.
Short test: Verospiron prescribed in a daily dose of 400 mg for 4 days. If, during the period of taking the drug, the concentration of potassium in the blood serum increases and decreases with the cancellation of Verospiron, the result may indirectly indicate primary hyperaldosteronism.
After the diagnosis of hyperaldosteronism is made using more informative diagnostic tests, Verospiron can be prescribed in preparation for surgery at a dose of 100-400 mg / day.
In patients not subject to surgery, Verospiron can be used as a long-term maintenance therapy in the lowest effective doses, which are set individually.
For children prescribe the drug in a daily dose at the rate of 3 mg / kg. Dose picked individually. The multiplicity of reception - 1-2 times / day.
On the part of the endocrine system: gynecomastia (usually disappears after drug withdrawal, but in rare cases it may persist), pain in the mammary glands, decreased libido, and menstrual disorders.
Gastrointestinal: dyspeptic phenomena (including nausea), abnormal liver function.
From the side of the central nervous system: dizziness, weakness, confusion.
Fluid and electrolyte balance: hyperkalemia, electrolyte imbalance.
Hemic and lymphatic: leukopenia, agranulocytosis, thrombocytopenia
Dermatologic: alopecia, hypertrichosis, urticaria, pruritus, rash.
Other: cramps gastrocnemius muscles.
- Addison's disease;
- acute renal failure;
- chronic renal failure with a significant decrease in excretory function (CC <10 ml / min);
- lactation (breastfeeding);
- hypersensitivity to spironolactone and other components of the drug.
Pregnancy and breastfeeding
Verospiron is contraindicated for use during pregnancy and during breastfeeding.
When taking Veroshpirona, you should exclude or limit the consumption of foods rich in potassium (potatoes, apricots, raisins, tomato juice), as well as other potassium-containing drugs.
In connection with the possibility of the development of hyperkalemia, hyponatremia and transient increase of blood urea nitrogen during the use of the drug, it is necessary to periodically monitor the content of electrolytes in the serum, especially in elderly patients with reduced kidney or liver function.
Patients should be informed that if the next dose was missed, the next dose should be taken as soon as possible. Do not double the missed dose.
Some patients with decompensated cirrhosis have reported the development of reversible hypochloremic metabolic acidosis, usually accompanying hyperkalemia (even with normal kidney function).
During the treatment Veroshpironom should avoid alcohol.
Influence on ability to drive motor transport and control mechanisms
In the initial period of use of the drug Verospiron prohibited driving a car and other activities that require the speed of psychomotor reactions.In the future, the possibility of practicing these types of activities is determined individually.
Symptoms: nausea, vomiting, drowsiness, confusion, skin rash, diarrhea. Possible violation of water and electrolyte balance and dehydration.
Treatment: Immediately stop taking the drug, induce vomiting and flush the stomach. There is no specific antidote. Symptomatic therapy of dehydration, disturbances of water and electrolyte balance, arterial hypotension should be carried out. The elimination of hyperkalemia is achieved by the rapid introduction of glucose (20-50% solutions) and insulin at the rate of 0.25-0.5 IU per 1 g of glucose. Potassium diuretics and ion exchange resins are used. Hemodialysis is possible.
Verospiron reduces the sensitivity of vessels to norepinephrine. This should be considered during general and local anesthesia.
With the simultaneous use of Verospiron with other diuretic or antihypertensive agents, it is possible to enhance the hypotensive effect (if necessary, combination therapy is necessary to reduce the dose of the above drugs).
The combined use of Veroshpirone in high doses with Indomethacin or ACE inhibitors can lead to hyperkalemia.
With simultaneous use Verospiron reduces the effect of indirect anticoagulants (coumarin derivatives).
With simultaneous use of Verospiron with triptorelin, Buserelin, gonadorelin increases the effect of the latter.
With simultaneous use of Verospiron and Digoxin increases T1/2 last one. This can lead to an increase in the concentration of digoxin in the blood up to toxic (if necessary, their joint use should reduce the dose or increase the interval between doses of digoxin).
When applied simultaneously with Verohspiron, Acetylsalicylic acid weakens the diuretic effect of spironolactone by blocking the secretion of canrenone in the renal tubules.
Indomethacin and mefanamic acid have been shown to inhibit canrenone excretion.
The drug should be stored in a dark place at a temperature of from 15 ° to 30 ° C.