Atenolol, Chlortalidone
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Pharmacological properties
combined antihypertensive drug containing atenolol and chlortalidone. atenolol is a cardioselective β1-adrenergic receptor blocker. It has antihypertensive, antianginal and antiarrhythmic effects. does not have internal sympathomimetic activity and membrane stabilizing effect. it mainly blocks β1-adrenergic receptors of the heart, decreasing the adrenergic effect on the heart of the sympathetic nervous system and catecholamines circulating in the blood, as a result of which the automatism of the sinus node, heart rate decreases, slows av conductivity, reduces myocardial contractility and its oxygen demand.
Chlortalidone is a long-acting thiazide-like diuretic. It blocks the reabsorption of sodium ions, chlorine and, accordingly, water in the distal tubules of the nephron. Increases the excretion of potassium, magnesium ions from the body. Delays the excretion of calcium and uric acid ions. It reduces blood pressure by reducing bcc, lowering cardiac output, as well as reducing the overall peripheral vascular resistance with prolonged use.
The antihypertensive effect lasts for 24 hours after taking the drug. The stabilization of the therapeutic effect usually occurs after 2 weeks of using the drug.
Pharmacokinetics
Suction. After oral administration, 50% of the dose of atenolol is absorbed in the digestive tract; ingestion does not significantly affect absorption.
WITHmax in blood plasma is reached after 2–4 hours. After oral administration, chlortalidone is absorbed quite quickly, bioavailability is almost 60%.
Distribution. The binding of atenolol to plasma proteins is about 6-16%. Chlortalidone is 90% bound to plasma proteins and red blood cells.
Metabolism and excretion. Atenolol is practically not metabolized in the liver.
It is allocated mainly by kidneys (90%). T½ is 6–9 hours. Chlortalidone is excreted in feces and urine. T½ is 24–55 hours, in the elderly and with renal failure increases.
Indications
Ag
Application
The drug is not intended for initial therapy ag. the drug is prescribed if monotherapy is ineffective. doses of the drug and the duration of treatment are set individually depending on the therapeutic effect obtained.
Dinoric-Darnitsa tablets are prescribed for adults inside. Accepted without chewing, washed down with water, before eating 1 time per day (in the morning).
The dosage regimen is given in terms of atenolol.
In hypertension, the initial dose is 50 mg (½ tablet) per day. In the absence of a clinical effect, you can increase the dose to 100 mg (1 tablet) per day. A further increase in dose in most cases does not lead to a decrease in blood pressure. If necessary, other antihypertensive agents are used. The greatest therapeutic effect is observed after 1-2 weeks of treatment. The drug should be discontinued gradually, since with a sharp cessation of the drug, the development of the withdrawal syndrome is possible. For elderly patients, a lower dose of the drug (for atenolol) is required, which is determined by the doctor.
Patients with impaired renal function
In patients with impaired renal function, the dosage regimen depends on the degree of decrease in glomerular filtration and creatinine clearance (table).
Creatinine clearance, ml / min | Maximum dose |
---|---|
15–35 | 50 mg daily or 100 mg every other day |
15 | 50 mg every other day |
Hemodialysis | 50 mg daily immediately after dialysis |
Contraindications
Hypersensitivity to active substances or other components of the drug, severe sinus bradycardia, degree II – III av blockade, sinoauricular block, sinus node weakness syndrome, acute heart failure, decompensated chronic heart failure, hypotension, cardiogenic shock, severe peripheral circulation disturbances, metabolic acidosis, hypokalemia, hyponatremia, hypercalcemia, anuria, severe renal and / or