Aldaron 25 mg (20 tablets)

The instruction for medical use of Aldaron® medicine the Trade name of Aldaron® the International unlicensed name Spironolactonum Dosage Form of the Tablet, 25 mg Structure One tablet contains active agent - Spironolactonum of 25.0 mg, excipients: lactoses monohydrate, talc, silicon dioxide colloidal anhydrous, magnesium or calcium stearate, potato starch. Description of the Tablet of white color, round, biconvex. Pharmacotherapeutic group Diuretics. Kaliysberegayushchy diuretics. Aldosteronum antagonists. Spironolactonum the ATX C03DA01 Code the Pharmacological Pharmacokinetics At properties intake active agent of drug – Spironolactonum is well soaked up from digestive tract (bioavailability more than 90%), absorption increases at a concomitant use with food (bioavailability of nearly 100%). It biotransformirutsya quickly and extensively in a liver with formation of several sulfur-containing metabolites, including 7 - alpha thiomethylspirolactonum, 6-бета-гидрокси−7-альфа-тиометилспиролактона and the main active metabolite — a kanrenon. Linking of Spironolactonum and a kanrenon with proteins of blood plasma — more than 90%. Spironolactonum and its metabolites pass through a placental barrier, kanrenon gets into breast milk. The maximum concentration (Cmax) of Spironolactonum is reached in 2.6 h and makes 80 ng/ml, the maximum concentration (Cmax) of a kanrenon – in 4.3 h and makes 181 ng/ml, 7 - alpha thiomethylspirolactonum in 3.2 h and makes 391 ng/ml, 6-бета-гидрокси−7-альфа-тиометилспиролактона – in 5.1 h and makes 125 ng/ml. 10% are removed, mainly, with urine in the form of metabolites — in not changed look and also in the form of metabolites with bile/excrements. Elimination half-life (T1/2) of Spironolactonum — 10 min., elimination half-life (T1/2) of a kanrenon makes 13–24 h (on average 19 h) at reception 1–2 times a day, 9–16 h (on average 12.5 h) at reception 4 times a day. A pharmacodynamics Spironolactonum – kaliysberegayushchy diuretic. Competes with Aldosteronum for places of binding on cytoplasmatic mineralokortikoidny receptors. Inhibits Aldosteronum - adjustable exchange of ions of sodium for potassium ions in collective tubules and distal tubules. Brakes a reabsorption of ions of sodium through an apical cell membrane of a renal epithelium, increases excretion with urine of ions of sodium, chlorine and water, lowers secretion and removal of potassium (kaliysberegayushchy effect), magnesium, urea and increases their concentration in blood. Has moderate long-term diuretic effect and weak antihypertensive action. The diuretic effect is shown for the 2-5th day and remains within 2–3 days after the reception termination. Hypotensive action is shown on the 2-3rd week of treatment. The antihypertensive activity is caused by increase in excretion of ions of sodium and reduction of volume of the circulating blood and extracellular liquid. As diuretic is most effective in the hypostases connected with the raised products of Aldosteronum, especially when kaliysberegayushchy diuretic action, century of t is desirable. h in stagnant heart failure, cirrhosis and a nephrotic syndrome. Indications - swell in chronic heart failure when at the patient the response to treatment is not observed by other diuretics or there is a need for potentiation of their effects - cirrhosis with ascites and hypostases - a nephrotic syndrome, especially at simultaneous existence of a hypopotassemia and hyper aldosteronism (as a part of combination therapy) - malignant ascites - primary hyper aldosteronism the Route of administration and doses Inside once a day at meal time. Adults Stagnant heart failure with hypostasis the Initial daily dose of 100 mg (can be in the range from 25 to 200 mg a day), is recommended to apply in one or several receptions. The maintenance dose has to be established individually. Cirrhosis with ascites and hypostases If Na+/K relation + in urine more than 1.0, initial daily and maximum daily doses make 100 mg. If this ratio less than 1.0, an initial daily dose makes 200 mg, maximum – 400 mg/days. The dosage can be established individually. Malignant ascites the Initial dose usually 100-200 mg a day. In hard cases the dose can be gradually increased up to 400 mg a day. The maintenance dose has to be established individually. A nephrotic syndrome Usual doses – 100-200 mg a day. Альдарон® it is recommended only in case of inefficiency of monotherapy by glucocorticosteroids. Primary hyper aldosteronism After establishment of the diagnosis of 100-400 mg a day in quality of training to surgery. In case of impossibility of operational treatment it is possible to carry out long therapy by the smallest effective dose which is picked up individually. In such cases each 14 days the initial dose is subject to decrease until the smallest effective dose is reached. At long-term treatment it is reasonable to combine drug with other diuretics in order to avoid development of side reactions. Duration of treatment is established by the attending physician individually. Children to Children from 12 years are also more senior appoint at the rate of 3 mg/kg/days, once or in 2 receptions, the dose is selected individually. Elderly patients It is recommended to begin treatment with lower doses with the subsequent gradual increase up to achievement of the maximum effect. It is necessary to take into account the hepatic and renal disturbances taking place as they influence metabolism of drug and its excretion. Side effects Very often (˃1/10) - a hyperpotassemia (at patients with a renal failure and those who receive potassium drugs) - arrhythmia (at patients with a renal failure and those who receive potassium drugs) - decrease a libido erectile dysfunction, a gynecomastia (at men), morbidity of a mammary gland, increase in a mammary gland, menstrual disturbances (at women) it is frequent (˃1/100, & lt, 1/10) - a hyperpotassemia (at elderly patients, diabetics and receiving APF inhibitors) - nausea, vomiting - infertility (in case of use of high doses (450 mg a day)) Infrequently (˃1/1000, & lt, 1/100) - a headache, confusion of consciousness, drowsiness, an asthenia, fatigue, dizziness, muscular spasms, an ataxy, spasms of gastrocnemius muscles Seldom (˃1/10000, & lt, 1/1000) - hypersensitivity - a hyponatremia, dehydration, a porphyria - gastritis, an ulcer, gastric bleeding, a stomach ache, diarrhea, a constipation - rash, urticaria, hyperaemia Very seldom (& lt, 1/10000) - thrombocytopenia, an agranulocytosis, an eosinophilia, megaloblastoz - a hirsutism - paralysis, a paraplegia - a vasculitis - change of a timbre of a voice - hepatitis - an alopecia, eczema, a ring-shaped erythema, lupoid and similar damages of skin - osteomalacy - an acute renal failure - increase in content of urea of blood serum, a giperkreatininemiya Unknown frequency - giperkhloremichesky acidosis or an alkalosis - undesirable hypotension Undesirable effects are usually stopped after drug withdrawal. Contraindications - hypersensitivity, hypersensitivity to active ingredient or to any of excipients - Addison's disease - the acute or quickly progressing renal failure, chronic kidney disease with considerable decrease in secretory function (clearance of creatinine less than 10 ml/min.) - an anury - a hyperpotassemia - a hyponatremia - a hypercalcemia - a concomitant use of other kaliysberegayushchy diuretics and potassium additives - pregnancy and the period of a lactation - children's age up to 12 years Medicinal interactions At combined use with: - other diuretics (the raised diuresis) - holestiraminy, ammonium chloride (increase in risk of a hyperpotassemia and a giperkhloremichesky metabolic acidosis) - immunodepressants (takrolimus and cyclosporine) - increase in risk of a hyperpotassemia - antihypertensive drugs (especially ganglioblokator) – can develop excessive hypotension, thus, the dose of antihypertensive drugs can be subject to reduction at addition to the therapeutic scheme Aldarona® with the subsequent adjustment as required - alcohol, barbiturates or narcotic drugs - can exponentiate the orthostatic hypotension caused by Spironolactonum - pressor amines (Norepinephrinum): Альдарон® reduces their action, it should be considered when carrying out local or general anesthesia using these drugs - non-steroidal anti-inflammatory drugs (NPVS), in particular, acetylsalicylic acid, indometacin and mefenamovy acid - increase in risk of a hyperpotassemia with the accompanying decrease in diuretic, natriuretic and antihypertensive effect of Aldarona® - glucocorticosteroids, AKTG - paradoxical increase in excretion of potassium - digoxin - Spironolactonum is capable to increase elimination half-life of digoxin that can lead to increase in its content in blood serum and development of glikozidny intoxication - lithium - it is not necessary to appoint drugs of lithium along with diuretics as they reduce renal clearance of lithium and can increase risk of intoxication - karbenoksolony - can cause a delay of sodium and thus, to reduce efficiency of Spironolactonum - carbamazepine - at a concomitant use with Spironolactonum can cause development of clinically significant hyponatremia - coumarin derivatives - their effect is weakened - triptoreliny, busereliny, gonadoreliny - their effects amplify Influence on results of laboratory researches - can be expected influence on process of definition of concentration of digoxin by radio immunological methods. The special instructions Aldaron® should be applied with extra care at the patients having diseases which can cause development of acidosis and/or a hyperpotassemia. Drug can increase risk of development of a hyperpotassemia at patients with a diabetic nephropathy. With care appoint at surgical intervention against the background of local and general anesthetics, to elderly patients (risk of development of a hyperpotassemia is increased). It is not necessary to appoint Spironolactonum together with the medicines causing a gynecomastia. At doses over 100 mg/days develop endocrine/anti-androgenic effects more often, action on the central nervous system and irritation of a mucous membrane of digestive tract is shown. During therapy it is necessary to control carefully the content of electrolytes, level of ureal nitrogen, urea and creatinine in blood (especially at elderly patients and at patients with a renal failure and/or a liver), regularly to watch indicators of arterial blood pressure. Hyperpotassemia: at patients with a renal failure or at the excessive use of potassium the condition of a hyperpotassemia leading to disturbances of warm activity can develop. At development of a hyperpotassemia the use of Aldarona® has to be stopped, and, if necessary, active measures are taken for decrease in level of potassium in blood serum. At some patients with dekompensirovanny cirrhosis, even at normal function of kidneys, the reversible giperkhloremichesky metabolic acidosis, as a rule, in combination with a hyperpotassemia can develop. Simultaneous use of Aldarona® with other kaliysberegayushchy diuretics, APF inhibitors, antagonists of angiotensin II, Aldosteronum blockers, heparin, low-molecular heparins or other drugs causing a hyperpotassemia or with the diet rich with potassium, or the salt substitutes containing potassium can lead to a serious hyperpotassemia. Patients with heavy heart failure can have a deadly hyperpotassemia. It is very important to control potassium level in blood serum at the patients with heavy heart failure receiving Aldaron®. It is necessary to avoid use of two kaliysberegayushchy diuretics, nutritional supplements of potassium for patients with potassium content in blood serum higher than 3.5 mg-ekv/l. It is recommended to carry out monitoring of level of potassium and creatinine in one week after the beginning of use or increase in a dose of Aldarona®, then monthly within the first 3 months, quarterly within a year, then each 6 months. It is necessary to stop treatment if potassium level in serum exceeds 5 mg-ekv/l or the level of creatinine exceeds 4 mg/dl. At test for tolerance to glucose at patients with a diabetic nephropathy Spironolactonum should be cancelled, at least, in 3 days prior to test (in connection with risk of a heavy hyperpotassemia). During treatment of Aldaronom® the alcohol intake is forbidden. Pregnancy and the period of a lactation pass Spironolactonum and its metabolites through a placental barrier. In experiments on rats it is established that Spironolactonum causes feminization of male fruits. It is necessary to stop breastfeeding during use of Aldarona®. Drug contains lactose therefore it is contraindicated in a congenital lactose intolerance, deficiency of Lappa lactase, glucose galactose malabsorption. The feature of influence of medicine on ability to run the vehicle or potentially dangerous mechanisms Needs care to drivers of vehicles and people whose profession is connected with the increased concentration of attention. Overdose Symptoms: drowsiness, dizziness, confusion of consciousness, spasm of gastrocnemius muscles, nausea, vomiting, diarrhea, organism dehydration, disturbance of water and electrolytic balance, skin rash. Treatment: the termination of administration of drug, induction of vomiting, gastric lavage, symptomatic therapy of dehydration and disturbances of water and electrolytic balance, arterial hypotension, maintenance of the vital functions, in case of a hyperpotassemia — 20–50% of solution of glucose, fast in/in introduction, and insulin — 0.25-0.5 PIECES/g of glucose, are used kaliyvyvodyashchy diuretics and ion-exchange resins, carrying out a hemodialysis is possible, there is no specific antidote. Form of release and packing of the Tablet, 25 mg. On 10 tablets in blister strip packaging from a film of the polyvinylchloride and printing aluminum foil varnished. On the 2nd blister strip packagings together with the instruction for medical use in the state and Russian languages in a cardboard pack. To Store storage conditions in the dry, protected from light place, at a temperature not higher than 25 wasps. To store out of children's reach! A period of storage of 5 years not to use drug after the expiration date specified on packing. Prescription status According to the prescription Republic of Kazakhstan Abdi Ibrahim Global Pharm LLP Producer, the Almaty Region, the Iliysky area, Industrial zone 282 ph.: +7 (727) 356-11-00, 8-800-070-11-00 The owner of the registration certificate of Abdi Ibrahim Global Pharm LLP the Republic of Kazakhstan the Address of the organization accepting in the territory of the Republic of Kazakhstan claims from consumers on quality of products (goods) of Abdi Ibrahim Global Pharm LLP, the Republic of Kazakhstan, the Almaty Region, the Iliysky area, Industrial zone 282, ph.: +7 (727) 356-11-00, 8-800-070-11-00, the e-mail address: info@aigp.kz the Address of the organization responsible for post-registration observation of safety of medicine in the territory of the Republic of Kazakhstan Abdi Ibrahim Global Pharm LLP, the Republic of Kazakhstan, the Almaty Region, Iliysky area, Industrial zone 282, ph.: +7 (727) 356-11-00, 8-800-070-11-00, the e-mail address:
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