Atenolol-Darnitsa
Producer: CJSC Pharmaceutical Firm Darnitsa Ukraine
Code of automatic telephone exchange: C07AB03
Release form: Firm dosage forms. Tablets.
General characteristics. Structure:
Active ingredient: atenolol; 1 tablet contains an atenolol (in terms of 100% dry matter) 100 mg;
excipients: lactoses monohydrate, cellulose microcrystallic, talc, кросповидон, gipromelloza, magnesium stearate, titanium dioxide (E 171), macrogoal of 1500.
Pharmacological properties:
Pharmacodynamics. Anti-hypertensive, anti-anginal, antiarrhytmic means. Cardioselective β1-адреноблокатор without internal sympathomimetic and membrane stabilizing activity. Reduces the stimulating influence on heart of a sympathetic nervous system and the catecholamines circulating in blood. Reduces contractility of a myocardium, cordial emission and arterial pressure, reduces the need of a myocardium for oxygen. Reduces automatism of a sinus node, increases duration of the refractory period, slows down AV conductivity, reduces heart rate.
Pharmacokinetics. After intake about 50% are soaked up, elderly people – have slightly more. Cmax is reached in 2–4 h, linkng with proteins of plasma — 6–16%. Badly gets through a blood-brain barrier, passes through a placental barrier and in breast milk. Practically it is not metabolized in a liver, removed by kidneys by glomerular filtering (85%). T1/2 is 6–7 h, increases at patients of advanced age. The renal failure is followed by lengthening of T1/2 and cumulation: ability to cumulation is shown at clearance of creatinine lower than 35 ml/min. (reduction of doses is necessary).
Pharmaceutical characteristics.
Main physical and chemical properties: tablets, coated, white color, with a biconvex surface and risky.
Indications to use:
- functional disturbances from cardiovascular system (a hyperkinetic cardial syndrome, functional disturbances of regulation of arterial pressure as monotherapy or in a combination with other hypotensive drugs, especially thiazide diuretics);
- treatment and prevention of attacks of stenocardia (chronic stable and unstable stenocardia, especially in the presence of tachycardia and arterial hypertension);
- disturbance of a cordial rhythm (sinus tachycardia; prevention of supraventricular tachycardia, Bouveret's supraventricular disease; blinking and atrial flutter; the ventrikulyarny (ventricular) arrhythmias including caused by the raised exercise stress, reception of sympathomimetic means; prevention of ventricular tachycardia and ventricular fibrillation;
- a myocardial infarction (treatment and prevention for decrease in a lethality and reduction of risk of a repeated heart attack).
Route of administration and doses:
Apply Atenolol-Darnits's adult inside, without chewing, washing down with water, before meal, it is desirable at the same time.
Doses of drug and duration of treatment are established by the doctor individually depending on the gained therapeutic effect.
It is impossible to change dosing or to stop treatment atenololy without doctor's advice. At sudden drug withdrawal development of a withdrawal is possible. Therefore drug withdrawal and a dose decline have to happen slowly and gradually.
Arterial hypertension: treatment, as a rule, begin from single application 50 mg of an atenolol (1/2 tablets) of 1 times a day. If necessary the daily dose in a week is increased to 100 mg (1 tablet) which take for 1–2 times.
Functional disturbances of cardiovascular system: usually apply 25 mg of an atenolol a day (drugs of an atenolol with a possibility of such dosing are used).
Chronic stable and unstable stenocardia: usually appoint 50–100 mg of an atenolol a day (1/2–1 tablet) which take for 1–2 times.
Supraventricular (supraventricular) and ventrikulyarny (ventricular) arrhythmias: Atenolol-Darnits is appointed by 1–2 times a day on 50–100 mg (1/2–1 tablet).
The maximum daily dose makes 200 mg.
In patients with considerable renal failures: the scheme of a drug dosing changes depending on degree of a renal failure. At clearance of creatinine of 10-30 ml/min. appoint 50 mg every other day or 25 mg/days (drugs of an atenolol with a possibility of such dosing); at clearance of creatinine it is less than 10 ml/min. – 25 mg every other day, or at treatment by a hemodialysis on 25 mg after each dialysis.
The maximum daily dose for such patients makes 100 mg.
Features of use:
Treatment is carried out at regular medical control. Before therapy it is necessary to compensate heart failure. During treatment monitoring of heart rate, arterial pressure, glucose level in blood (dose adjustment of antidiabetic drugs is possible) and control of emergence of symptoms of heart failure is necessary.
Patients with coronary heart disease during drug withdrawal have to be under careful observation. Atenolol it is necessary to cancel for 48 h before performing surgery with use of the general anesthesia (chloroform or ether) or to choose anesthetic with the smallest negative inotropic effect. The anesthesiologist should be warned about performing treatment atenololy.
At patients with a diabetes mellitus and hyperfunction of a thyroid gland can mask the tachycardia caused by a hypoglycemia or a thyrotoxicosis. At a pheochromocytoma it is necessary to apply α-adrenolytic drugs at the same time.......... Strengthening of expressiveness of reaction of hypersensitivity and lack of effect of usual doses of Epinephrinum against the background of the burdened allergological anamnesis is possible.
For the period of therapy it is recommended to exclude alcohol intake.
Features of use. With care and under medical supervision it is necessary to appoint Atenolol-Darnits at: to an atrioventricular block of the I degree, at abnormal liver functions and/or kidneys, at a diabetes mellitus with fluctuations of level of sugar in blood, the patient with disturbance of peripheric circulation (including Reynaud's syndrome), to patients who are on the desensibilizing therapy or with heavy allergic reactions in the anamnesis.
Ability to influence the speed of reactions at control of motor transport or work with other mechanisms. During Atenololom-Darnits's treatment it is necessary to refrain from control of motor transport and the work connected with the increased concentration of attention.
Side effects:
Allergic reactions: itch, rash, erythema, small tortoiseshell, psoriazopodobny and dystrophic changes of skin.
From cardiovascular system and blood (a hemopoiesis, a hemostasis): occasionally AV conductivity disturbances, bradycardia, hypotension, symptoms of heart failure, asthma attacks, a hypoglycemia can be observed.
From a nervous system and sense bodys: increased fatigue, weakness, dizziness, headache, drowsiness or sleeplessness, nightmares, depression, concern, confusion of consciousness or short-term loss of memory, hallucination, reduction in the rate of reaction, paresthesia, spasms; vision disorder, reduction of secretion of saliva and the lacrimal liquid, conjunctivitis.
From bodies of digestive tract: dryness in an oral cavity, nausea, vomiting, an abdominal pain, diarrhea, a lock, abnormal liver functions.
Others: reversible allopecia, hyperhidrosis, cold snap of extremities, myasthenia, easing libido, impotence, Peyroni's disease, change of activity of enzymes, bilirubin level, withdrawal, hypothyroid state, hypoglycemia.
Interaction with other medicines:
Prolongs action of the anti-depolarizing muscle relaxants, anti-coagulative effect of coumarins.
Three/tetracyclic antidepressants, neuroleptics, sedative, hypnagogues and alcohol exponentiate oppression of TsNS.
Antiarrhytmic and narcotic means strengthen cardiodepressive action (the risk of development of bradycardia, arrhythmia, hypotension, heart failure increases). Reserpinum, Methyldopum, a clonidine, гуанфацин, cardiac glycosides potentiate negative hrono-, dromo-and bathmotropic effect, insulin and other antidiabetic means – a hypoglycemia. Non-steroidal anti-inflammatory drugs, estrogen, sympathomimetics, xanthines weaken hypotensive effect, absorption, increase – sympatholytics, nitroglycerine, гидралазин and other hypotensive medicines, antacids slow down absorption. Cimetidinum slows down metabolism.
It is incompatible with MAO inhibitors (furasolidone, Procarbazinum, селегелин).
Contraindications:
- Hypersensitivity to components of drug and other β-adrenoblockers;;;;;;;;;;
- atrioventricular block of II and III degrees;
- sick sinus syndrome;
- sinuatrial blockade;
- a sinus bradycardia (heart rate is less than 50 blows in 1 minute);
- arterial hypotension (systolic pressure is less than 90 mm Hg);
- late stages of disturbance of peripheric circulation;
- a concomitant use of MAO inhibitors (except for MAO-B inhibitors);
- feeding period breast.
Use during pregnancy or feeding by a breast. During pregnancy drug can be used only if the expected effect of therapy exceeds potential risk for a fruit. For the period of treatment it is necessary to stop feeding by a breast.
Children. Atenolol-Darnits is not appointed to children owing to lack of data on efficiency and safety of use.
Overdose:
Symptoms: bradycardia, AV blockade of the II-III degree, heart failure, breath disturbance, arterial hypotension, bronchospasm, hypoglycemia.
Treatment: a gastric lavage and purpose of the adsorbing means; symptomatic therapy: atropine, изопреналин, орципреналин, cardiac glycosides or glucagon, diuretics, angiotonic means (dopamine, Dobutaminum or Norepinephrinum), the selection β-adrenomimetik, glucose solution (intravenously), installation of an artificial pacemaker. Atenolol is brought at a hemodialysis.
Storage conditions:
Period of validity. 2 years. To store in the place, unavailable to children, in original packaging, at a temperature not above 25 °C.
Issue conditions:
According to the recipe
Packaging:
On 10 tablets in a blister strip packaging, on two blister strip packagings in a pack.
