Aritel, 10 mg 30 pcs.

Aritel is a beta-adrenoblocking, hypotensive, antianginal.

Pharmacodynamics

A selective β₁-adrenoblocker, without its own sympathomimetic activity, has no membrane stabilizing effect. It has only slight affinity for β₂-adrenoreceptors of bronchial and vascular smooth muscle as well as for β₂-adrenoreceptors involved in metabolic regulation. Consequently, bisoprolol generally has no effect on airway resistance and metabolic processes in which β₂-adrenoreceptors are involved.

In general, maximum BP reduction is achieved 2 weeks after initiation of therapy.

Bisoprolol reduces sympathoadrenal activity by blocking β₁-adrenoceptors in the heart.

On single oral administration in patients with CHD without signs of CHD, bisoprolol decreases HR, reduces blood stroke volume and, consequently, decreases ejection fraction and myocardial oxygen demand. With long-term therapy, initially elevated ROS decreases. Reduction of plasma renin activity is considered to be one of the components of the antihypertensive effect of β-adrenoblockers.

Pharmacokinetics

Extraction

Bisoprolol is almost completely (over 90%) absorbed from the GI tract. Its bioavailability due to minor metabolism during the first passage through the liver (at about 10%) is about 90% after oral administration. Food intake has no effect on bioavailability. Bisoprolol exhibits linear kinetics, with plasma concentrations proportional to the dose taken in the dose range from 5 to 20 mg. T_max is 2-3 h.

Distribution

Bisoprolol is fairly widely distributed. V_d is 3.5 L/kg. The binding to plasma proteins reaches about 30%.

Metabolism

Metabolized by the oxidative pathway without subsequent conjugation. All metabolites are polar (water-soluble) and are excreted by the kidneys. The major metabolites found in blood plasma and urine have no pharmacological activity. The data obtained from experiments with human liver microsomes in vitro show that bisoprolol is metabolized primarily by the CYP3A4 isoenzyme (about 95%) and the CYP2D6 isoenzyme plays only a minor role.

Elimation

The clearance of bisoprololol is determined by a balance between excretion by the kidneys unchanged (about 50%) and metabolism in the liver (about 50%) to metabolites, which are also excreted by the kidneys. Total clearance is 15 l/h. T_1/2 is 10-12 h.

There is no information on the pharmacokinetics of bisoprolol in patients with CHF and concomitant hepatic or renal impairment.

Indications

Arterial hypertension;

Coronary heart disease: prevention of angina attacks.

Active ingredient

Composition

1 tablet contains:

Active ingredients:

Bisoprolol fumarate 10 mg.

Auxiliary substances:

Potato starch;

Povidone (collidone-30);

Lactose;

How to take, the dosage

Interaction

Allergens used for immunotherapy or allergen extracts for skin testing increase the risk of severe systemic allergic reactions or anaphylaxis in patients receiving bisoprolol.
Iodine-containing X-ray contrast agents for intravenous administration increase the risk of anaphylactic reactions.
Phenytoin when administered intravenously, drugs for inhalation general anesthesia (hydrocarbon derivatives) increase the severity of cardiodepressive effects and the likelihood of BP reduction.
Aritel changes the effectiveness of insulin and oral hypoglycemic drugs, masks the symptoms of developing hypoglycemia (tachycardia, increased BP). Reduces clearance of lidocaine and xanthines (except diphylline) and increases their plasma concentrations, especially in patients with initially increased clearance of theophylline under the influence of smoking.
Hypotensive effect is weakened by nonsteroidal anti-inflammatory drugs (Na+ retention and blockade of prostaglandin synthesis by kidneys), glucocorticosteroids and estrogens (Na+ ion retention).
Heart glycosides, methyldopa, reserpine and guanfacine, “slow” calcium channel blockers (verapamil, diltiazem), amiodorone and other antiarrhythmic drugs increase the risk of developing or worsening bradycardia, AV block, heart failure and heart failure.
Nifedipine may lead to significant BP reductions.
Diuretics, clonidine, sympatholytics, hydralazine, and other hypotensive medications may lead to excessive BP reductions.
Extends the effects of non-depolarizing myorelaxants and the anticoagulant effect of coumarins.
Tricyclic and tetracyclic antidepressants, antipsychotic drugs (neuroleptics), ethanol, sedatives and hypnotics increase CNS depression.
Concomitant use with MAO inhibitors is not recommended due to significant increase in hypotensive effect, a break in treatment between MAO inhibitors and bisoprolol should be at least 14 days.
Unhydrogenated ergot alkaloids increase the risk of peripheral circulatory disorders.
Ergotamine increases the risk of peripheral circulation disorders; sulfasalazine increases the plasma concentration of bisoprolol; rifampicin shortens the elimination half-life.

Special Instructions

Contraindications

Hypersensitivity to drug components and other beta-adrenoblockers,

Shock (including cardiogenic);

Collapse;

Pulmonary edema;

Acute heart failure, decompensated chronic heart failure, AV block II-III degree., Sinoatrial block, sinus node weakness syndrome, severe bradycardia, Prinzmetal angina, cardiomegaly (without signs of heart failure), arterial hypotension (systolic BP less than 100 mmHg, especially in myocardial infarction);

Bronchial asthma and chronic obstructive pulmonary disease in the history;

Concurrent use of monoamine oxidase inhibitors (MAOIs) (except MAO-B);

Late stages of peripheral circulatory disorders, Raynaud’s disease);

Pheochromocytoma (without concurrent use of alpha-adrenoblockers);

Metabolic acidosis;

Age

Side effects

Central nervous system disorders:fatigue, weakness, dizziness, headache, sleep disorders, depression, anxiety, confusion or short-term memory loss, hallucinations, asthenia, myasthenia, paresthesias in the extremities (in patients with “intermittent” claudication and Raynaud’s syndrome), tremor.

Sensory organs: vision disorders, decreased tear fluid secretion, dry and painful eyes, conjunctivitis.

Cardiovascular system side: sinus bradycardia, palpitations, myocardial conduction disorders, AV blockade (up to development of complete transverse blockade and cardiac arrest), arrhythmias, weakened myocardial contractility, development (worsening) of chronic heart failure (swelling of ankles, feet; dyspnea), BP decrease, orthostatic hypotension, manifestation of angiospasm (worsening of peripheral circulatory disorders, coldness of the lower extremities, Raynaud’s syndrome), chest pain.

Digestive system disorders: dry mouth, nausea, vomiting, abdominal pain, constipation or diarrhea, liver disorders (dark urine, jaundice of sclerae or skin, cholestasis), changes in taste.

In the respiratory system:nasal congestion, difficulty in breathing when prescribed in high doses (loss of selectivity) and/or in predisposed patients – laryngo- and bronchospasm.

Endocrine system: hyperglycemia (in patients with insulin-independent diabetes mellitus), hypoglycemia (in patients receiving insulin), hypothyroidism.

Allergic reactions: skin itching, rash, urticaria.

Skin reactions:increased sweating, skin hyperemia, exanthema, psoriasis-like skin reactions, exacerbation of psoriasis symptoms.

Laboratory findings: thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, leukopenia, changes in liver enzyme activity (increased ALT, AST), bilirubin levels, triglycerides.

Fetal effects:intrauterine growth retardation, hypoglycemia, bradycardia.

Others:back pain, arthralgia, decreased libido, decreased potency, withdrawal syndrome (increased angina attacks, increased BP).

Overdose

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