Bisoprolol-Vertex, 10 mg 60 pcs

Bisoprolol is a selective beta1-adrenoblocker without sympathomimetic activity of its own; it has antihypertensive, antiarrhythmic and antianginal effects. By blocking in low doses beta1-adrenoreceptors of the heart, it reduces catecholamine-stimulated formation of cyclic adenosine monophosphate (cAMP) from adenosine triphosphate (ATP), decreases intracellular calcium ions (Ca2+) flow, has negative chrono-, dromo-, batmo- and inotropic effects (decreases heart rate, inhibits conduction and excitability, decreases myocardial contractility).

With increasing dose has beta2-adrenoblocking effect.

Total peripheral vascular resistance at the beginning of administration of beta-adrenoblockers, in the first 24 hours, increases (as a result of reciprocal increase of activity of alpha-adrenoreceptors and elimination of stimulation of beta2-adrenoreceptors) which in 1-3 days returns to baseline, and with long-term prescription decreases.

The antihypertensive effect is connected with decrease of the minute blood volume, sympathetic stimulation of peripheral vessels, decrease of renin-angiotensin-aldosteron system activity (it is more important for patients with initial renin hypersecretion), restoration of aortic arch baroreceptors sensitivity (their activity in response to arterial pressure (AP) decrease is not increased) and the influence on the central nervous system. In case of arterial hypertension the effect comes in 2-5 days, stable effect – in 1-2 months.

Antianginal effect is caused by decrease of myocardial oxygen demand as the result of heart rate reduction and contractility decrease, prolongation of diastole, improvement of myocardial perfusion. By increasing left ventricular end-diastolic pressure and increasing ventricular muscle fiber stretch may increase myocardial oxygen demand, especially in patients with chronic heart failure (CHF).

. In contrast to non-selective beta-adrenoblockers when administered in medium therapeutic doses, it has less pronounced effect on the organs containing beta2-adrenoreceptors (pancreas, skeletal muscles, smooth muscle of peripheral arteries, bronchi and uterus) and on carbohydrate metabolism, does not cause delay of sodium ions (Na+) in the body. When used in high doses has a blocking effect on both subtypes of beta-adrenoreceptors.

Pharmacokinetics.

Bisoprolol is almost completely absorbed from the gastrointestinal tract (80-90%). Food intake does not affect the absorption of the drug. Maximum plasma concentration is reached after 2-3 hours. Binding with plasma proteins is approximately 35%. Hematoencephalic barrier and placental barrier permeability is low, secretion with breast milk is low.

Metabolized in the liver. Period of half-life (T1/2) is 9-12 hours; it is prolonged in patients with kidney function disorders (in creatinine clearance less than
40 ml/min – 3 times), in elderly age and in case of liver diseases (in cirrhosis it is prolonged up to 21.7 hours). Excreted by the kidneys – 50% unchanged, less than 2% through the intestine.

Indications

Active ingredient

Composition

1 tablet contains:

Active substance:

bisoprolol fumarate 10 mg.

Associates:

Lactose monohydrate,

Microcrystalline cellulose,

/p>

colloidal silicon dioxide,

crospovidone,

magnesium stearate.

How to take, the dosage

In the morning on an empty stomach, without chewing, 5 mg once.

If necessary, the dose is increased to 10 mg once daily. The maximum daily dose is 20 mg/day.

In patients with impaired renal function and creatine clearance less than 20 ml/min or with significant hepatic impairment the maximum daily dose is 10 mg. No dose adjustment is required in elderly patients.

Interaction

When concomitant use of antacids and antidiarrheals may decrease the absorption of beta-adrenoblockers.

Concomitant use of antiarrhythmic agents may cause a sharp decrease in BP, lower HR, development of arrhythmias and/or heart failure.

The simultaneous use of antihypertensive agents may increase the antihypertensive effect.

Concomitant use of cardiac glycosides may cause conduction disorders.

The concomitant use of sympathomimetics (including those contained in cough products, nasal drops, eye drops) decreases the effectiveness of bisoprolol.

Concomitant use of verapamil, diltiazem may cause a sharp decrease in BP, lower HR, development of arrhythmia and/or heart failure.

Concomitant use of guanfacine may cause marked bradycardia and conduction disturbances.

In concomitant use of insulin, hypoglycemic agents for oral administration, the effect of insulin or other hypoglycemic agents increases (regular monitoring of plasma glucose levels is necessary).

When clonidine is used concomitantly there may be severe bradycardia, arterial hypotension and conduction disorders.

In case of abrupt clonidine withdrawal, patients receiving bisoprolol may experience a sharp increase in BP.

The simultaneous use of nifedipine, other calcium channel blockers, dihydropyridine derivatives increases the antihypertensive effect of bisoprolol.

The simultaneous use of reserpine, alpha-methyldopa may cause marked bradycardia.

Concomitant use of rifampicin may slightly decrease T1/2 of bisoprolol.

Concomitant use of ergotamine derivatives (including migraine medications containing ergotamine) increases symptoms of peripheral circulatory disorders.

Special Instructions

Nervous system disorders:weakness, fatigue, dizziness, headache, sleep disorders, mental disorders (depression, rarely – hallucinations), cold sensation and paresthesias in the extremities.

Cardiovascular system disorders: Orthostatic hypotension, bradycardia, AV conduction disorders, appearance of symptoms of heart failure, worsening of intermittent claudication and basic clinical symptoms in Raynaud’s syndrome.

Visual side: decreased lacrimal fluid secretion, conjunctivitis.

Digestive system disorders:diarrhea, constipation, nausea, abdominal pain.

Muscular system:muscular weakness, muscle cramps.

Skin and subcutaneous tissues:cutaneous itching; in some cases – aggravation of psoriasis, the appearance of psoriasis-like rashes.

In the respiratory system:in predisposed patients there may be symptoms of bronchial obstruction.

Others:Sweating, hot flashes, impaired potency, decreased glucose tolerance in diabetic patients, allergic reactions.

Contraindications

Side effects

Nervous system disorders:weakness, fatigue, dizziness, headache, sleep disorders, mental disorders (depression, rarely – hallucinations), cold sensation and paresthesias in the extremities.

Cardiovascular system disorders: Orthostatic hypotension, bradycardia, AV conduction disorders, appearance of symptoms of heart failure, worsening of intermittent claudication and basic clinical symptoms in Raynaud’s syndrome.

Outlooking organ: decreased lacrimal fluid secretion, conjunctivitis.

Digestive system disorders:diarrhea, constipation, nausea, abdominal pain.

From the musculoskeletal system: muscle weakness, muscle cramps.

Skin and subcutaneous tissues: skin itching; in some cases – aggravation of psoriasis, the appearance of psoriasis-like rashes.

Respiratory system disorders: in susceptible patients there may be symptoms of bronchial obstruction.

Others:Sweating, hot flashes, impaired potency, decreased glucose tolerance in diabetic patients, allergic reactions.

Overdose

Symptoms:

Arrhythmia, ventricular extrasystoles, marked bradycardia, AV blockade, marked BP decrease, chronic heart failure, cyanosis of finger nails or palms, difficulty breathing, bronchospasm, dizziness, fainting, seizures.
Treatment: gastric lavage and administration of adsorptive medications;

Symptomatic therapy:

In case of developed AV blockade – intravenous injection of 1-2 mg of atropine, epinephrine or placement of a temporary pacemaker; in ventricular extrasystole – lidocaine (class IA drugs are not used ); if BP decreases – the patient should be in Trendelenburg position; if there are no signs of pulmonary edema – intravenous plasma exchange solutions, if ineffective – administration of epinephrine, dopamine, dobutamine (to maintain chronotropic and inotropic action and to eliminate marked BP decrease); in heart failure – cardiac glycosides, diuretics, glucagon; in convulsions – intravenous diazepam; in bronchospasm – inhaled beta2-adrenergic stimulants

Similarities