Pharmacodynamics and pharmacokinetics
The main substance is spironaloctone . In the distal parts of the nephron, it prevents the retention of water and sodium by aldosterone, reduces the potassium-removing effect of aldosterone, and reduces the synthesis of permeases. The maximum effect of taking the drug is observed 7 hours after taking the capsule and lasts for 24 hours. A decrease in blood pressure is achieved by a diuretic effect, which manifests itself after 2-5 weeks of use. The active substance becomes active metabolites. The medicine is excreted by the kidneys.
Description of the dosage form
Tablets are white or white with a creamy tint, round, flat-cylindrical, with a score on one side and a bevel, almost odorless or with a weak specific odor.
pharmachologic effect
Spironolactone is a potassium-sparing diuretic, a specific antagonist of aldosterone (mineralocorticosteroid hormone of the adrenal cortex) with prolonged action. In the distal parts of the nephron, spironolactone prevents the retention of sodium and water by aldosterone and suppresses the potassium-removing effect of aldosterone, reduces the synthesis of permeases in the aldosterone-dependent area of the collecting ducts and distal tubules. 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 urine.
The maximum effect is observed 7 hours after oral administration and lasts for at least 24 hours. The hypotensive effect of the drug is due to the presence of a diuretic effect, which is not constant: the diuretic effect appears on days 2-5 of treatment.
Pharmacokinetics
Suction and distribution
When taken orally, it is quickly and completely absorbed from the gastrointestinal tract. The maximum concentration of Cmax canrenone in the blood plasma is achieved 2-4 hours after administration. Binds to plasma proteins by approximately 98% (canrenone - 90%). Volume of distribution (Vd) - 0.05 l/kg.
After daily administration of spironolactone at a dose of 100 mg for 15 days, Cmax is 80 ng/ml, the time to reach Cmax after the next morning dose is 2-6 hours.
Spironolactone penetrates poorly into organs and tissues, while itself and its metabolites penetrate the placental barrier, and canrenone passes into breast milk.
Metabolism
Spironolactone is converted into active metabolites: a metabolite containing sulfur (80%) and partly canrenone (20%).
Removal
Excreted by the kidneys: 50% - in the form of metabolites, 10% - unchanged and partially through the intestines. The half-life (T1/2) of spironolactone is 13-24 hours, of active metabolites - up to 15 hours. The elimination of canrenone (mainly by the kidneys) is two-phase, T1/2 in the first phase is 2-3 hours, in the second - 12-96 hours.
Pharmacokinetics in selected patient groups
In liver cirrhosis and heart failure, the duration of T1/2 increases without signs of cumulation, the likelihood of which is higher in chronic renal failure and hyperkalemia.
Indications for use of Veroshpiron
What is the medicine for? Let's look at why Veroshpiron is prescribed.
Tablets and capsules are used as part of combination therapy for essential hypertension . Indications for the use of Veroshpiron also include: edema syndrome in CHF, nephrotic syndrome, ascites , liver cirrhosis .
The drug is also used as an auxiliary substance in the prevention of hypomagnesemia and hypokalemia during treatment with diuretics. The medicine is successfully used for Conn's syndrome during a short preoperative course of treatment, as well as for the purpose of establishing a diagnosis of primary hyperaldosteronism .
What does Veroshpiron help with?
The drug is taken as an additional remedy for the treatment of such pathologies:
- essential hypertension (high blood pressure);
- swelling due to CHF;
- ascites;
- nephrotic syndrome;
- cirrhosis of the liver;
- prevention of potassium and magnesium deficiency;
- Conn's syndrome (treatment on the eve of surgery);
- diagnostic tool (to confirm the disease “Primary hyperaldosteronism”).
Contraindications
Contraindications for Veroshpiron are:
- hypersensitivity to the components of the drug;
- hyperkalemia;
- hyponatremia;
- Addison's disease;
- anuria;
- severe renal failure (creatinine clearance less than 10 ml/min);
- pregnancy and lactation period.
The drug is prescribed with extreme caution when
- metabolic acidosis ;
- hypercalcemia;
- AV block;
- diabetes mellitus;
- diabetic nephropathy;
- menstrual irregularities;
- carrying out general and local anesthesia;
- diseases of the liver, kidneys;
- in elderly people.
Contraindications for use
Taking the drug is prohibited in the presence of the following violations:
- anuria;
- severe renal failure;
- sodium deficiency;
- excess potassium;
- Addison's pathology.
During pregnancy and during breastfeeding (any period), Veroshpiron is also not taken. The drug should be used with caution in elderly people and patients with the following diseases:
- diabetes mellitus of both types;
- acidosis;
- excess calcium;
- installation of AV block;
- disturbances of the monthly cycle;
- chronic kidney and liver diseases;
- local or general anesthesia;
- diabetic nephropathy.
Side effects
Gastrointestinal tract: diarrhea , nausea, vomiting, gastritis , constipation , intestinal colic , liver dysfunction.
Central nervous system: lethargy, ataxia , headaches, dizziness, lethargy, drowsiness, muscle spasms, confusion, calf muscle cramps.
Side effects from the hematopoietic organs: thrombocytopenia , agranulocytosis , megaloblastosis .
Metabolism: hypercreatininemia , hyperuricemia , hyperkalemia , increased urea levels, hyponatremia , hyperchloremic metabolic alkalosis and acidosis .
Endocrine system: men may develop gynecomastia, erectile dysfunction , and decreased potency. In women amenorrhea , dysmenorrhea , hirsutism , terorrhagia , and breast carcinoma .
Allergic reaction: itching, drug fever, urticaria, erythematous, maculopapular rash.
Dermatological reaction: hypertrichosis , alopecia .
Urinary system: acute renal failure .
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 balance with the help of potassium-removing diuretics, rapid parenteral administration of a 5-20% dextrose (glucose) solution with insulin at the rate of 0.25-0.5 units per 1 g of dextrose (glucose); can be re-entered if necessary. In severe cases, hemodialysis is performed.
Instructions for use of Veroshpiron (Method and dosage)
Veroshpiron capsules and tablets have the same instructions for use. It all depends on the amount of active substance taken.
Essential hypertension: adults: 50-100 mg once. The dose can be gradually increased to 200 mg, the amount of the drug is increased once every 2 weeks.
Idiopathic hyperaldosteronism: 100-400 mg per day.
Severe hyperaldosteronism, hypokalemia: 300 mg per day in 2-3 doses. Gradually, the dose of the drug is reduced to 25 mg per day.
Hypomagnesemia, nipokalemia, provoked by the action of diuretics: 25-100 mg per day, once or in several doses.
Diagnosis and treatment of primary hyperaldosteronism: 400 mg per day for 4 days. The daily dose of the medicine is divided into several doses.
How to take for swelling?
Edema in nephrotic syndrome: adults 100-200 mg per day. Veroshpiron is used only if other treatment methods have been ineffective.
Edema syndrome in CHF: 100-200 mg per day (several doses) for 5 days in combination with thiazide and loop diuretics. The daily dose can be reduced to 25 mg.
Edema in cirrhosis: if the Na+/K+ ratio in the urine is above 1.0, then 100 mg is prescribed. If less than 1.0, then the daily dose is 200-400 mg.
Edema in children: initially 1-3.3 mg per 1 kg of body weight, or 30-90 mg/m2 per day for 1-4 doses. After 5 days, the dose is adjusted.
How long can I take it?
The usual course is 20 days, followed by a break of at least six months. The longest possible use is for a couple of months. Long-term use can lead to acute renal failure.
How to take - before or after meals?
It is recommended to take the medicine after meals.
Interaction
The drug reduces the effectiveness of mitotane , anticoagulants , and increases the effect of antihypertensive and diuretic drugs.
Stimulates the effect of Buserelin , Triptorelin , Gonadorelin .
When taken simultaneously with potassium supplements, the risk of developing hyperkalemia increases.
Reduces the toxicity of cardiac glycosides.
Indomethacin , salicylates - reduce the diuretic effect of the drug.
Veroshpiron increases the metabolism of Antipyrin and increases the half-life of Digoxin .
Drug interactions
Reduces the effect of anticoagulants, indirect anticoagulants (heparin, coumarin derivatives, indanedione) and the toxicity of cardiac glycosides (since normalization of potassium content in the blood prevents the development of toxicity).
Enhances the metabolism of phenazone (antipyrine).
Reduces the sensitivity of blood vessels to norepinephrine (care is required when performing anesthesia), increases T1/2 of digoxin - digoxin intoxication is possible.
Increases the toxic effect of lithium due to decreased clearance.
Possibly enhances the effect of non-depolarizing muscle relaxants (for example, tubocurarine).
Accelerates the metabolism and excretion of carbenoxolone.
Carbenoxolone promotes sodium retention by spironolactone.
GCS and diuretics (thiazides and thiazide-like, furosemide, ethacrynic acid) enhance and accelerate the diuretic and natriuretic effects.
Enhances the effect of diuretic and antihypertensive drugs.
NSAIDs reduce the diuretic and natriuretic effects, increasing the risk of hyperkalemia.
Alcohol (ethanol), barbiturates, and narcotic substances increase orthostatic hypotension.
GCS enhance the diuretic and natriuretic effect in hypoalbuminemia and/or hyponatremia.
The risk of developing hyperkalemia increases when taken with potassium preparations, potassium supplements and potassium-sparing diuretics, ACE inhibitors (acidosis), angiotensin II receptor antagonists, aldosterone blockers, indomethacin, cyclosporine.
Salicylates and indomethacin reduce the diuretic effect of spironolactone.
Ammonium chloride and cholestyramine contribute to the development of hyperkalemic metabolic acidosis.
Fludrocortisone causes a paradoxical increase in tubular secretion of potassium.
Spironolactone reduces the effect of mitotane.
Enhances the effects of triptorelin, buserelin, gonadorelin.
special instructions
Veroshpiron is prescribed in gynecology to reduce androgen levels in women with PCOS ( polycystic ovary syndrome ). The drug can cause bleeding and disrupt the menstrual cycle.
Veroshpiron is often recommended to be taken together with contraceptives in order to normalize the menstrual cycle and reduce hirsutism .
Recipe in Latin:
Rp.: Verospironi 0.025 D. td N 20 in tabul. S.
Reviews about Veroshpiron
Reviews about Veroshpiron on forums testify in favor of this drug. The medicine is effective, but it is advised to use it in moderation and as prescribed by a doctor, since the drug has side effects and contraindications.
Diuretic tablets fully cope with their assigned function, and also effectively help against edema. In gynecology, the drug is successfully used for PCOS.
Veroshpiron also helps for weight loss, as it has a diuretic property.
Those who have used the medication claim that it does not help with hirsutism.
Veroshpiron price, where to buy
The price of Veroshpiron in tablets is about 100 rubles for 20 pieces.
50 mg capsules can be purchased for an average of 180 rubles per 30 pieces. Capsules 100 mg - 300 rubles for 30 pieces.
- Online pharmacies in RussiaRussia
- Online pharmacies in UkraineUkraine
- Online pharmacies in KazakhstanKazakhstan
ZdravCity
- Veroshpiron tab.
25 mg 20 pcs. JSC "Gedeon Richter-RUS" RU 88 rub. order - Veroshpiron capsules 50 mg 30 pcs. JSC "Gedeon Richter-RUS"
RUB 176 order
- Veroshpiron capsules 100 mg 30 pcs. JSC "Gedeon Richter-RUS"
RUB 259 order
Pharmacy Dialogue
- Veroshpiron (caps. 100 mg No. 30) Gedeon-Richter-RUS ZAO
RUB 317 order
- Veroshpiron capsules 50 mg No. 30 Gedeon-Richter
RUB 187 order
- Veroshpiron tablets 25 mg No. 20Gedeon-Richter
89 rub. order
- Veroshpiron (tab. 25 mg No. 20) Gedeon-Richter-RUS ZAO
92 rub. order
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Pharmacy24
- Veroshpiron 50 mg No. 30 capsules VAT "Gedeon Richter", Ugorshchina
97 UAH. order - Veroshpiron 25 mg N20 tablets AT"Gedeon Richter"/TOV "Gedeon Richter Poland", Ugorshchina/Poland
34 UAH order
- Veroshpiron 100 mg No. 30 capsules VAT "Gedeon Richter", Ugorshchina
135 UAH order
PaniPharmacy
- Veroshpiron tablets Veroshpiron tablets 25 mg No. 20 Hungary, Gedeon Richter
34 UAH order
- Veroshpiron capsule Veroshpiron caps. 100 mg No. 30 Hungary, Gedeon Richter
138 UAH order
- Veroshpiron capsule Veroshpiron caps. 50 mg No. 30 Hungary, Gedeon Richter
100 UAH order
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