Hypertension: monotherapy or in combination with other antihypertensive drugs. Mild to moderate, chronic, stable heart failure (NYHA II or III). Edema of specific origin: as a consequence of circulatory failure; ascites due to cirrhosis in patients stable under strict control; edema in the course of nephrotic syndrome. Renal diabetes insipidus.
Composition:
1 tabl contains 50 mg chlorthalidone.
Action:
Thiazyscent diuretic with a long duration of action. It mainly affects the distal renal tubule (ascending the nephron loop), inhibiting NaCl reabsorption (by inhibiting the Na+ and Cl–) and promoting Ca-reabsorption2+ (unknown mechanism). Increased transport+ and water to the cortical portion of the coil and (or) increased flow rate lead to increased secretion and excretion of K ions+ and H+. Diurease induced by thiazide diuretics initially leads to a reduction in plasma volume, cardiac output and blood pressure. It is possible to activate the renin-angiotensin-aldosterone system (RAA). The bioavailability of the drug after oral administration is about 64%. Cmax occurs after about 8-12 h. Only a small fraction of chlorthalidone in the blood remains free, which results from the extensive accumulation of the drug in erythrocytes and the binding of the drug to plasma proteins. Chlalidalidone has a high affinity for erythrocyte carbonic anhydrase. About 76% is bound to plasma proteins. It penetrates the placenta barrier and is excreted into breast milk. Metabolism and hepatic biliary excretion represent a small degree of elimination. Chlorthalidone is usually excreted unchanged. T0,5 is 50 hours on average.
Contraindications:
Hypersensitivity to chlorthalidone and other sulfonamide derivatives or to any of the excipients. Anuria, severe renal failure (CCr <30 ml / min). Severe hepatic failure. Treatment-resistant hypokalemia or conditions leading to worsening of potassium loss; hyponatremia and hypercalcemia. Symptomatic hyperuricaemia (gout or presence of uric acid deposits). Hypertension in pregnant women. Simultaneous use of lithium preparations. Untreated Adison's disease.
Precautions:
Use with caution in patients with impaired liver function or progressive liver disease, as even small changes in fluid and electrolyte balance may accelerate the onset of hepatic coma, especially in patients with cirrhosis. Elderly, chlorthalidone excretion is slower - patients should be closely monitored. During treatment, blood electrolytes should be determined regularly (there is a risk of hypokalemia, hyponatremia, hypomagnesaemia and hypercalcaemia). During long-term treatment with chlorthalidone, blood potassium should be measured at the beginning of treatment, then 3-4 weeks later, then (if the potassium balance is not disturbed by additional factors, such as vomiting, diarrhea, change in kidney function, etc.) 4-6 months. Blood electrolyte monitoring is particularly indicated in patients with nephrotic edema (use only under close monitoring and in normal blood potassium and without dehydration), in patients with ascites associated with cirrhosis, in elderly patients. If necessary, the preparation can be administered simultaneously with oral supplements containing potassium or potassium-sparing diuretics (eg thiamteren). In the case of combination therapy, the level of potassium in the blood should be monitored. If hypokalemia is accompanied by clinical symptoms (eg muscle weakness, paresis and changes in the ECG), chlorthalidone should be discontinued. The combination of chlorthalidone and potassium-active diuretic or potassium-sparing diuretics should be avoided in patients receiving concurrent ACE inhibitors or angiotensin II receptor antagonists. In addition, the antihypertensive effect of ACE inhibitors or AT receptor antagonists1 intensify factors that increase plasma renin activity (diuretics) - it is recommended to reduce the dose of diuretics or their discontinuation for 2 to 3 days and (or) to start treatment with ACE inhibitors or AT receptor antagonists1 angiotensin II from low initial doses. The use of chlorthalidone may affect Glucose tolerance (in patients with diabetes, dosage adjustment of oral antidiabetic agents and insulin may be necessary). In addition, increases in cholesterol and triglycerides and hyperuricemia may be associated with the use of thiazide and thiazide diuretics. Do not use chlorthalidone as the first-line treatment in long-term treatment in patients with diabetes or in people treated for hypercholesterolemia (diet or combination therapy).
Pregnancy and lactation:
Chlalidalidone is contraindicated in the treatment of gestational hypertension. The drug may adversely affect fetal-placental perfusion and may cause such effects in the fetus and newborn, such as jaundice, electrolyte imbalance, bone marrow suppression and thrombocytopenia. Chlorthalidone is excreted in breast milk - avoid use during breastfeeding.
Side effects:
Very common: hypokalemia, hyperuricemia and increase in total cholesterol, triglycerides and low density lipoproteins - LDL (mainly when using high doses). Common: hyponatremia (occasionally associated with neurological symptoms such as: nausea, weakness, progressive confusion, apathy), hypomagnesemia, hyperglycemia, urticaria and other forms of rash, orthostatic hypotension, dizziness, mild discomfort in the abdomen, erectile dysfunction. Rarely: hypercalcemia, glucosuria, inadequate diabetes control, gout, photosensitivity reaction, intrahepatic cholestasis, jaundice, arrhythmia, paresthesia, headache, nausea, vomiting, abdominal pain, constipation, diarrhea, thrombocytopenia, leukopenia, agranulocytosis, eosinophilia, view. Very rare: hypochloremic alkalosis, pancreatitis, non-cardiac pulmonary edema, allergic interstitial nephritis, vasculitis.
Dosage:
Orally. Treatment should be started with the lowest possible dose, determined based on the patient's individual response.Hypertension: starting dose of 25 mg daily. The full therapeutic effect occurs after 3-4 weeks. If the reduction in blood pressure is insufficient when using 25 mg or 50 mg daily, it is recommended to use combination therapy with other antihypertensives.Heart failure (NYHA grade II or III): the starting dose is 25-50 mg per day; in severe cases, the dose may be increased to 100-200 mg per day. The average maintenance dose is the lowest effective dose, e.g. a dose of 25-50 mg given on a daily basis as well as every other day. If the patient's response to therapy is insufficient, additional cardiac glycosides or ACE inhibitors or both can be used.Edema of specific originThe lowest effective dose should be determined based on the patient's individual response to the medicine and used only for a limited time. Do not exceed the 50 mg dose per day.Renal diabetes insipidus - adults: initially 100 mg twice daily, maintenance dose 50 mg per day.Special groups of patients. Elderly patients are prescribed a standard, lowest effective dose. In patients with mild renal impairment, the lowest effective dose is recommended; chlorthalidone loses its diuretic properties at CCr <30 ml / min.Children. Use the lowest effective dose. For example, 0.5-1 mg / kg / 48 h was used as the starting dose and 1.7 mg / kg / 48 h as the maximum dose.Way of giving. The recommended single dose, given every day or every other day, should be taken in the morning with a meal. The tablet can be divided into halves.