Instructions Spironolactone-Darnitsa tablets 100 mg No. 30
Composition
active ingredient: spironolactone;
1 tablet contains: spironolactone 100 mg;
Excipients: potato starch, lactose monohydrate, povidone, calcium stearate.
Dosage form
Pills.
Main physicochemical properties: flat-cylindrical tablets with a bevel and a score, white or white with a creamy tint.
Pharmacotherapeutic group
Potassium-sparing diuretics. ATX code C03D A01.
Pharmacological properties
Pharmacodynamics.
The active substance of the drug - spironolactone - is a competitive antagonist of aldosterone, which acts on the distal tubules of the kidneys. Due to the blockade of aldosterone, it suppresses the retention of water and Na+ ions and promotes the retention of K+ ions, which not only increases the excretion of Na+ and Cl− ions and reduces the excretion of K+ ions with urine, but also reduces the excretion of H+ ions. As a result, the diuretic effect also has a hypotensive effect.
Pharmacokinetics.
Absorption of spironolactone from the gastrointestinal tract is rapid and complete. It is highly bound to plasma proteins (approximately 90%). Spironolactone is rapidly metabolized. Its active metabolites are 7α-thiomethylspironolactone and canrenone. Although the half-life of spironolactone itself is short (1.3 hours), the half-lives of its active metabolites are longer (2.8 to 11.2 hours). The metabolites are excreted mainly in the urine; a small portion is excreted in the feces. Spironolactone and its metabolites cross the placenta and enter breast milk.
After administration of 100 mg of spironolactone daily for 15 days to healthy volunteers, the time to peak plasma concentration (tmax), peak plasma concentration (Cmax) and half-life (t1/2) of spironolactone were: 2.6 hours, 80 ng/ml and approximately 1.4 hours, respectively. For 7α-thiomethylspironolactone and canrenone, these values were 3.2 and 4.3 hours, 391 ng/ml and 181 ng/ml, 13.8 and 16.5 hours, respectively.
The renal effects of a single dose of spironolactone peak after 7 hours and persist for at least 24 hours.
Indication
– Primary hyperaldosteronism.
– Congestive heart failure – when other diuretics are ineffective or intolerable or when their effectiveness needs to be increased.
– Essential hypertension, mainly with hypokalemia – usually in combination with other antihypertensive drugs.
– Cirrhosis of the liver accompanied by edema and/or ascites.
– Edema caused by nephrotic syndrome.
– Hypokalemia – if other therapy is not possible.
– Prevention of hypokalemia in patients receiving cardiac glycosides – in cases where other therapies are considered inappropriate or inappropriate.
Contraindication
– Hypersensitivity to the active substance or to other components of the drug.
– Acute renal failure, severe impairment of nitrogen-excreting renal function (glomerular filtration rate <10 ml/min), anuria.
– Hyperkalemia, hyponatremia.
– Addison's disease.
– Simultaneous use with potassium-sparing diuretics and potassium preparations – due to the possibility of developing hyperkalemia.
– Pregnancy and breastfeeding.
Interaction with other medicinal products and other types of interactions
Simultaneous use of the drug with other medications may cause:
with antihypertensive agents (especially ganglioblockers, nicardipine, nimodipine) - excessive decrease in blood pressure; with simultaneous use, the dose of antihypertensive agents should be reduced with subsequent correction if necessary;
with ammonium chloride, cholestyramine - increased risk of developing hyperkalemia and hyperchloremic metabolic acidosis;
with potassium-sparing diuretics, potassium preparations, angiotensin-converting enzyme (ACE) inhibitors, angiotensin II receptor blockers, aldosterone receptor blockers, anticholinesterase agents, tacrolimus, cyclosporine - increased risk of hyperkalemia; simultaneous use with potassium-sparing diuretics and potassium preparations is contraindicated due to the possibility of hyperkalemia;
with other diuretics – increased diuretic effect;
with nonsteroidal anti-inflammatory drugs - increased risk of hyperkalemia and renal failure with a concomitant decrease in the diuretic, natriuretic and antihypertensive effects of spironolactone; with simultaneous use with acetylsalicylic acid, prostaglandin synthesis is also inhibited, with antipyrine - its metabolism in the liver is enhanced;
with glucocorticosteroids, adrenocorticotropic hormone (ACTH) – increased diuretic, natriuretic effects of spironolactone and paradoxical increased potassium excretion;
with α- and β-adrenomimetics, carbenoxolone – weakening of the effect of spironolactone;
with antipsychotics, tricyclic antidepressants – increased effect of spironolactone;
with barbiturates, narcotic drugs, ethanol – orthostatic hypotension;
with carbamazepine – increased risk of hyponatremia;
with digoxin – increased risk of glycoside intoxication due to prolongation of its half-life;
with lithium preparations – increased risk of intoxication due to decreased renal clearance of lithium; these preparations should not be used simultaneously;
with indirect anticoagulants (coumarin derivatives), mitotane, pressor amines (epinephrine), cardiac glycosides - weakening of the action of the latter;
with triptorelin, buserelin, gonadorelin - increased action of the latter.
Application features
The use of the drug, especially in patients with impaired renal function, may cause a transient increase in blood urea nitrogen and hyperkalemia, which may lead to the development of cardiac arrhythmias and reversible hyperchloremic metabolic acidosis. The drug should be used with caution in patients with impaired renal function, liver function and elderly patients. Plasma electrolyte levels and renal function should be periodically determined. In the event of hyperkalemia, treatment with the drug should be discontinued.
The drug should be used with caution in patients whose pre-existing diseases may predispose to the development of acidosis and/or hyperkalemia.
The drug should be used with caution in patients with diabetes, especially in the presence of diabetic nephropathy.
Spironolactone therapy may interfere with the determination of cortisol, epinephrine, and digoxin concentrations (by radioimmunoassays).
Prolonged, unjustified use of the drug should be avoided, since, according to studies, prolonged use of spironolactone in animals at maximum doses contributed to the development of carcinoma and myeloid leukemia.
You should not drink alcoholic beverages while using the drug.
The drug contains lactose, therefore patients with rare hereditary forms of galactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome should not take the drug.
Use during pregnancy or breastfeeding
The drug is contraindicated during pregnancy or breastfeeding. If necessary, use of the drug should be discontinued.
Ability to influence reaction speed when driving vehicles or other mechanisms
During the initial period of treatment, the duration of which is individual, driving or operating machinery is contraindicated.
Method of administration and doses
The drug is used internally for adults and children.
The daily dose of the drug is taken in 1 or 2 doses after meals. The daily dose in 1 dose or the first dose of the drug in the case of twice-daily use is recommended in the morning.
The duration of the treatment course is individual, in some cases it can reach several years, while it is necessary to use the drug in the lowest effective daily dose, subject to constant monitoring of the electrolyte composition of the blood serum and kidney function indicators.
Adults.
Primary hyperaldosteronism.
When preparing for surgery, the drug should be used in a dose of 100–400 mg per day.
If surgical treatment is not possible, the drug can be used long-term as maintenance therapy in the lowest effective dose, which is determined individually.
In this case, the initial dose can be reduced every 14 days until the minimum effective dose is reached. If it is necessary to use lower doses of the drug, Spironolactone-Darnitsa tablets should be used in the appropriate dosage. For long-term treatment, it is recommended to use the drug in combination with other diuretics to reduce side effects.
Congestive heart failure, edema due to nephrotic syndrome.
The drug should be used in an initial dose of 100 mg per day in 1 or 2 doses. The daily dose can also vary from 25 to 200 mg.
When higher doses are prescribed, the drug can be used in combination with other diuretics that act in more proximal parts of the renal tubules. In this case, the dose of spironolactone should be adjusted.
Essential hypertension.
The drug should be used in an initial dose of 50-100 mg per day in 1 or 2 doses in combination with other antihypertensive drugs. Treatment should be continued for at least 2 weeks, since by the end of this period the maximum antihypertensive effect is achieved. Further dose adjustment is individual, depending on the achieved effect.
Cirrhosis of the liver accompanied by ascites or edema.
If the ratio of Na+/K+ in the urine is greater than 1, the drug should be used at an initial dose of 100 mg per day. The maximum daily dose is 100 mg/day. If this ratio is less than 1, the drug should be used at a dose of 200 mg per day, with a maximum daily dose of 400 mg/day.
Hypokalemia.
The drug should be used at a dose of 25-100 mg per day in patients who do not receive enough potassium supplements or other methods of potassium replacement therapy.
For children.
The drug should be used at a dose of 1-3 mg/kg of body weight per day in 1 or 2 doses. In the case of maintenance therapy in combination with other diuretics, the daily dose is 1-2 mg/kg of body weight.
The drug is recommended to be used in lower doses with subsequent gradual increase until the maximum effect is achieved. It should be taken into account that this category of patients has hepatic and renal disorders, which may affect the metabolism of the drug and its excretion.
Children
The drug is used in pediatric practice as prescribed by a doctor.
Overdose
Symptoms: drowsiness/lethargy, confusion, electrolyte disturbances.
Treatment: symptomatic therapy. Water-electrolyte and acid-base balance should be maintained: by using potassium-sparing diuretics, parenteral administration of glucose with insulin, and in difficult cases, hemodialysis. There is no specific antidote.
Adverse reactions
From the cardiovascular system: arterial hypotension, arrhythmia (in patients with renal failure and those receiving potassium preparations), 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, inhibition, confusion.
Respiratory, thoracic and mediastinal disorders: change in voice timbre.
On the part of the digestive tract: nausea, vomiting, decreased appetite, abdominal and stomach pain, diarrhea, constipation, intestinal colic, gastritis, gastric and duodenal ulcers, gastric bleeding.
From the hepatobiliary system: hepatitis, liver dysfunction.
From the urinary system: acute renal failure.
Musculoskeletal and connective tissue disorders: osteomalacia, muscle spasm, muscle cramps of the lower extremities.
Metabolism and metabolism: hyperkalemia, hyponatremia, hypercreatinemia, increased blood urea level, hyperuricemia, porphyria, metabolic hyperchloremic acidosis or alkalosis, dehydration.
From the endocrine system: hirsutism.
From the reproductive system and mammary glands: decreased libido, erectile dysfunction, gynecomastia, menstrual irregularities, dysmenorrhea, amenorrhea, metrorrhagia during menopause, swelling and pain of the mammary glands in women, infertility (in case of using high doses - 450 mg per day), benign tumors of the mammary glands.
Immune system, skin and subcutaneous tissue disorders: hypersensitivity reactions, including: rash, itching, urticaria, drug fever; hypertrichosis, alopecia, lupus-like syndrome, hyperemia, erythema multiforme, eczema, Stevens-Johnson syndrome.
General: asthenia, fatigue.
Expiration date
2 years.
Storage conditions
Store in the original packaging at a temperature not exceeding 25 °C.
Keep out of reach of children.
Packaging
10 tablets in a blister pack; 3 blister packs in a pack.
Vacation category
According to the recipe.
Producer
PrJSC "Pharmaceutical Company "Darnitsa".
Location of the manufacturer and its business address
Ukraine, 02093, Kyiv, Boryspilska St., 13.
