Veroshpiron

Active material: Spironolactone
When ATH: C03DA01
CCF: Kaliйsberegaющiй diuretic
ICD-10 codes (testimony): E26, E61.2, E87.6, I10, I50.0, K74, N04
When CSF: 01.08.03
Manufacturer: GEDEON RICHTER Ltd. (Hungary)

DOSAGE FORM, COMPOSITION AND PACKAGING

Pills white or nearly white, round, flat, chamfered, with a characteristic odor of mercaptan, labeled “VEROSPIRON” on one side.

1 tab.
spironolactone25 mg

Excipients: colloidal silicon dioxide, magnesium stearate, talc, corn starch, lactose monohydrate.

20 PC. – blisters (1) – packs cardboard.

Capsules hard gelatin, size №3, with opaque yellow cap and opaque white body.

1 caps.
spironolactone50 mg

Excipients: sodium lauryl, magnesium stearate, corn starch, lactose monohydrate.

Composition of a gelatin capsule: quinoline yellow (E104) C.I.47005, Titanium dioxide (E171) C.I.77891, gelatin.

10 PC. – blisters (3) – packs cardboard.

Capsules hard gelatin, size №0, with an opaque orange cap and opaque yellow body.

1 caps.
spironolactone100 mg

Excipients: sodium lauryl, magnesium stearate, corn starch, lactose monohydrate.

Composition of a gelatin capsule: orange dye (E110) C.I.15985, Titanium dioxide (E171) C.I.77891, quinoline yellow (E104) C.I.47005, gelatin.

10 PC. – blisters (3) – packs cardboard.

 

Pharmacological action

Kaliйsberegaющiй diuretic, competitive antagonist of aldosterone.

In the distal nephron spironolactone prevents aldosterone delay of sodium and water and inhibits the effect of aldosterone kaliyvyvodyaschy, It reduces the synthesis of aldosterone in permeases-sensitive area of ​​the collecting ducts and distal tubules. Svyazыvayas with aldosterone receptors, increases the excretion of sodium ions, chlorine and water excretion, reduces the excretion of potassium and urea, reduces the acidity of urine.

The maximum effect is observed after 7 hours after ingestion of capsules inside and lasts at least 24 no. The hypotensive effect is caused by diuretic effect, kotorыy mutable. The diuretic effect is seen on 2-5 day treatment.

 

Pharmacokinetics

Absorption

Once inside quickly and completely absorbed from the gastrointestinal tract. Bioavailability is 100%. After daily administration 100 mg spironolactone for 15 With daysmax is 80 ng / ml, From time to reachmax after a morning reception – 2-6 no.

Distribution

Associated with the plasma protein on 98%.

Spironolactone badly into the organs and tissues, while he spironolactone and its metabolites cross the placental barrier, and canrenone – in breast milk. Vd – 0.05 l / kg.

Metabolism

In the process of biotransformation in the liver metabolites formed active sulfur-7 alpha tiometilspironolakton and canrenone. Canrenone reaches its Cmax through 2-4 no, its relation to plasma proteins is 90%.

Deduction

T1/2 – 13-24 ch.Vyvoditsya mostly in the urine (50% – as metabolites, 10% – unchanged) and partially – with feces. Withdrawal canrenone (mainly, urine) two-phase, T1/2 in the first phase – 2-3 no, in the second – 12-96 no.

Pharmacokinetics in special clinical situations

In cirrhosis of the liver and heart failure duration T1/2 increasing with no signs of accumulation, the probability is higher in patients with chronic renal failure and hyperkalemia.

 

INDICATIONS

- Essential hypertension (in a combination therapy);

- Edema syndrome in patients with chronic heart failure (It can be used as monotherapy and in combination with standard therapy);

- State, which can be detected when secondary hyperaldosteronism, incl. cirrhosis of the liver, accompanied by ascites and / or swelling, nephrotic syndrome, and other conditions, accompanied by edema;

- Gipokaliemiya / gipomagniemiya (as an aid to prevent it during treatment with diuretics and if you can not use other methods of correcting the level of potassium);

- Primary hyperaldosteronism (Horse Syndrome) – for a short pre-operative treatment;

- To establish the diagnosis of primary hyperaldosteronism.

 

DOSAGE

At essential hypertension daily dose for Adult generally 50-100 mg once daily and may be increased to 200 mg, while increasing the dose should be gradually, 1 once every 2 of the week. In order to achieve an adequate response to therapy, the drug should be taken at least 2 weeks. If necessary to adjust the dose.

At idiopathic hyperaldosteronism the drug is prescribed in a dose 100-400 mg / day.

At expressed hypokalemia and hyperaldosteronism daily dose is 300 mg (maximally 400 mg) for 2-3 admission, while improving the dose gradually reduced to 25 mg / day.

At hypokalemia and / or hypomagnesemia, caused by diuretic therapy, Veroshpiron prescribe a dose 25-100 mg / day, single or divided doses. The maximum daily dose is 400 mg, If oral potassium supplements or other methods to fill its deficit ineffective.

At diagnosis and treatment of primary hyperaldosteronism as diagnostic means for short diagnostic test Veroshpiron appointed within 4 days 400 mg / day, distributing the daily dose into several doses per day. When the concentration of potassium in the blood during treatment and decrease after cancellation it can suggest the presence of primary hyperaldosteronism. At prolonged diagnostic test drug administered in the same dose during the 3-4 weeks. Upon reaching the correction of hypokalemia and hypertension can suggest the presence of primary hyperaldosteronism.

After diagnosis hyperaldosteronism set with more accurate diagnostic methods, as a short course of preoperative treatment of primary hyperaldosteronism Veroshpiron should take a daily dose 100-400 mg, dividing it by the 1-4 reception over the entire period of preparation for surgery. If the operation is not shown, the Veroshpiron used for long-term maintenance therapy, it uses the lowest effective dose, which is chosen individually for each patient.

When treating swelling in the background of nephrotic syndrome daily dose for Adult generally 100-200 mg. There was no effect of spironolactone on the main pathological process and therefore the use of this drug is recommended only in cases, when other therapies are ineffective.

At Edema syndrome with chronic heart failure drug prescribed daily for 5 days 100-200 mg / day 2-3 admission, in combination with “loop” or a thiazide diuretic. Depending on the effect to reduce the daily dose 25 mg. The maintenance dose is adjusted individually. The maximum daily dose is 200 mg.

At swelling in the background of liver cirrhosis the daily dose for veroshpiron Adult generally 100 mg, if the ratio of sodium ions and potassium (On+/K+) in urine is greater than 1.0. If the ratio is less than 1.0, the daily dose is typically 200-400 mg. The maintenance dose is adjusted individually.

At edema in children starting dose is 1-3.3 mg / kg body weight or 30-90 mg / m2/sut 1-4 admission. Through 5 day dose correction is performed if necessary to increase its 3 times compared to original.

 

SIDE EFFECT

From the digestive system: nausea, vomiting, diarrhea, ulceration and bleeding from the gastrointestinal tract, gastritis, kišečnaâ how, abdominal pain, constipation, abnormal liver function.

From the central and peripheral nervous system: ataxia, lethargy, dizziness, headache, drowsiness, lethargy, confusion, muscle spasm, leg cramps.

On the part of the blood system: agranulocytosis, thrombocytopenia, megaloblastoz.

Metabolism: hyperuricemia, giperkreatininemiя, increasing concentrations of urea, hyperkalemia, giponatriemiya, metabolic acidosis or alkalosis hyperchloraemic.

On the part of the endocrine system: brutalization vote, males – gynecomastia (probability of dose-dependent, the duration of treatment and usually is reversible), reduced potency and erection; female – menstrual irregularities, dysmenorrhoea, amenorrhea, metrorrhagia, menopause, girsutizm, pain in the breast, breast carcinoma (a connection with the drug intake is not installed).

Allergic reactions: hives, rarely – maculo-papular and erythematous rash, drug fever, itch.

Dermatological reactions: alopecia, hypertryhoz.

From the urinary system: acute renal failure.

 

CONTRAINDICATIONS

- Addison's disease;

- Hyperkalemia;

- Giponatriemiya;

- Severe renal insufficiency (CC less than 10 ml / min);

- Anurija;

- Pregnancy;

- Lactation;

- Hypersensitivity to any component of the drug.

FROM caution should be prescribed the drug for hypercalcemia, metabolic acidosis, AV-blockade (hyperkalemia contributes to its enhancement), diabetes (if confirmed or suspected renal insufficiency), diabetic nephropathy, surgery, taking drugs, causing gynecomastia, the holding of local and general anesthesia, menstrual irregularities, breast enlargement, hepatic insufficiency, cirrhosis, and elderly patients.

 

Pregnancy and lactation

Application veroshpiron contraindicated in pregnancy and lactation.

 

Cautions

When applying veroshpironom may temporarily increased BUN serum, especially with reduced kidney function and hyperkalemia. It is also possible the development of metabolic acidosis hyperchloraemic. In appointing veroshpiron patients with impaired renal and hepatic function, elderly patients requires regular monitoring of serum electrolytes and renal function.

Admission veroshpiron difficult to determine the concentration of digoxin, cortisol and adrenaline.

Despite the lack of direct effect on carbohydrate metabolism, the presence of diabetes, especially with diabetic nephropathy, It requires special care when assigning veroshpiron because of the possibility of hyperkalemia.

In the treatment of NSAIDs in patients receiving veroshpiron should monitor kidney function and blood electrolyte levels.

During treatment veroshpiron alcohol is contraindicated, Avoid consumption of food, rich in potassium.

Effects on ability to drive vehicles and management mechanisms

In the initial period of treatment is prohibited to drive and engage in activities, require high concentration and speed of psychomotor reactions. Length restrictions set individually.

 

OVERDOSE

Symptoms: nausea, vomiting, dizziness, diarrhea, skin rash, hyperkalemia (paresthesia, muscular weakness, Arrhythmia), giponatriemiya (dry mouth, thirst, drowsiness), hypercalcemia, degidratatsiya, increasing the concentration of urea.

Treatment: gastric lavage, symptomatic treatment of dehydration and hypotension. When hyperkalemia is necessary to normalize the water-electrolyte metabolism using diuretics kaliyvyvodyaschih, Fast parenteral administration dextrose (5-20% solutions) insulin based 0.25-0.5 ED 1 g dextrose; if necessary, may re-introduction of dextrose. In severe cases, hemodialysis.

 

Drug Interactions

Veroshpiron while the application reduces the effect of anticoagulants (geparina, coumarin derivatives, indandiona) and mitotane; It enhances the effect of diuretics and antihypertensive drugs, enhances the effect of triptorelin, buserelyna, gonadorelina.

When taken concurrently with drugs veroshpiron potassium, potassium supplements and potassium-sparing diuretics, ACE inhibitors, angiotensin II antagonists increases the risk of hyperkalemia.

Against the background of veroshpiron decreases the toxicity of cardiac glycosides (tk. normal levels of potassium in the blood interferes with the development of toxicity).

Veroshpiron reduces the sensitivity of vessels to norepinephrine (It requires compliance with caution during anesthesia).

“Loop” and thiazide diuretics increase and accelerate the diuretic and natriuretic effects veroshpiron.

GCS also enhance the diuretic and natriuretic effect veroshpiron with hypoalbuminemia and / or hyponatremia.

Salicilaty, indomethacin reduce diuretic effect veroshpiron.

Ammonium chloride, kolestiramin while the use of veroshpiron giperkaliemicheskogo contribute to the development of metabolic acidosis, and fludrocortisone is paradoxical strengthening of tubular secretion of potassium.

In an application Veroshpiron enhances the toxic effect of lithium because of the decrease in its clearance.

Veroshpiron while the application increases the metabolism of phenazone (antipirina), increases the half-life of digoxin (vozmozhna intoxication digoksinom), It speeds up the metabolism and excretion of carbenoxolone. Karbenoksolon promotes sodium retention spironolactone.

 

Conditions of supply of pharmacies

The drug is released under the prescription.

 

TERMS AND CONDITIONS OF STORAGE

The drug should be stored out of reach of children at temperature from 15 ° to 30 ° C. Shelf life – 5 years.

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