Bisoprolol

When ATH:
C07AB07

Characteristic

Cardioselective beta₁-adrenoblokator, It has no intrinsic sympathomimetic activity and membrane stabilizing. Bisoprolol fumarate - a white crystalline powder. It is soluble in water, methanol, ethanol, xloroforme. Molecular weight 766,97.

Pharmacological action

Gipotenzivnoe, antianginalnoe, antiarrhythmic.

Application

Arterial hypertension, angina, post-infarction period, Arrhythmia, congestive heart failure (moderately expressed, stable without peaking during the last 6 Sun).

Contraindications

Hypersensitivity, sinusovaya bradycardia (less than 45-50 beats. / min), sick sinus syndrome, синоатриальная и AV блокада II–III степени, cardiogenic shock, acute and refractory to treatment of severe heart failure, acute myocardial infarction, hypotension (Sad below 90 mm Hg. Art.), severe obstructive respiratory failure, pregnancy, lactation.

Restrictions apply

Chronic obstructive pulmonary disease, severe asthma, variant angina (Princmetala), tendency to bradycardia, AV block I degrees, the peripheral blood circulation (incl. Raynaud's syndrome), diabetes, gipoglikemiâ, thyrotoxicosis, psoriasis, of the liver and kidneys, Acidosis, childhood (safety and effectiveness in children have not identified).

Pregnancy and breast-feeding

Maybe, if the effect of therapy for the mother outweighs the potential risk to the fetus and child (adequate and well-controlled studies of the safety of use in pregnant and lactating women have not performed). Because of the risk of bradycardia, gipotenzii, hypoglycemia and respiratory disorders (neonatal asphyxia) in newborn, bisoprolol fumarate treatment should be discontinued 48-72 hours before delivery. If this is not possible, infant should be kept under close medical observation for 48-72 hours after birth. There was studied the allocation of bisoprolol fumarate breast milk, but because it is secreted into breast milk in rats (less 2%), infants should be under medical supervision.

Category actions result in FDA - C. (The study of reproduction in animals has revealed adverse effects on the fetus, and adequate and well-controlled studies in pregnant women have not held, However, the potential benefits, associated with drugs in pregnant, may justify its use, in spite of the possible risk.)

Side effects

The frequency of side effects listed at doses, not exceeding 40 mg.

From the nervous system and sensory organs: dizziness (3,5%), insomnia (2,5%), asthenia (1,5%), gipestezii (1,5%), depression (0,2%), drowsiness, anxiety, paresthesia (cold feeling in extremities), hallucinations, aphronia, focus, orientation in time and space, balance, emotional lability, noise in ears, conjunctivitis, visual disturbances, reduced secretion of tear fluid, convulsions.

Cardio-vascular system and blood (hematopoiesis, hemostasis): bradycardia (0,5%), arrhythmia, heartbeat, OF блокада, gipotenziya, heart failure, violation of the microcirculation in the myocardium and limbs, intermittent claudication, vasculitis, agranulocytosis, thrombocytopenia, trombotsitopenicheskaya purpura.

From the digestive tract: diarrhea (3,5%), nausea (2,2%), vomiting (1,5%), dry mouth (1,3%), dyspepsia, constipation, ishemicheskiy colitis, mezenteryalnoy artery thrombosis.

From the respiratory system: cough (2,5%), breathlessness (1,5%), ʙronxo- and laryngospasm, pharyngitis (2,2%), rhinitis (4%), sinusitis (2,2%), respiratory tract infections (5%), respiratory distress syndrome.

With the genitourinary system: peripheral edema (3%), decreased libido, impotence, Peyronie's disease, cystitis, počečnaâ how.

For the skin: rash, acne, ekzemopodobnye reaction, prurigo, redness of the skin, hyperhidrosis, dermatitis, alopecia.

Metabolism: increased concentration of liver enzymes (IS, GOLD), hyperglycemia or increased glucose tolerance, hyperuricemia, change in the concentration of potassium in the blood.

Other: pain syndrome (headache - 10,9%, arthralgia - 2,7%, myalgia, abdominal pain, chest - 1,5%, eyes, ears), weight gain.

Cooperation

Chance of violations of automaticity, conduction and cardiac contractility increases (mutually) against the backdrop of amiodarone, diltiazema, verapamil, quinidine medicines, cardiac glycosides, reserpine, alpha metildofy. Co-administration of dihydropyridine calcium antagonists, especially in patients with latent cardiac insufficiency, It increases the risk of hypotension and cardiac decompensation. Effectively lowers xanthines and sympathomimetics, рифампицин уменьшает T_1/2, ergotamine derivatives potentiate the peripheral blood circulation. Incompatible with MAO inhibitors.

Overdose

Symptoms: bradycardia, arrhythmia, gipotenziya, heart failure (difficulty breathing, acrocyanosis, swelling), gipoglikemiâ, in severe cases - collapse.

Treatment: gastric lavage and appointment of absorbent, simptomaticheskaya therapy: atropyn, beta-agonists (Isoprenaline), sedativnыe (diazepam, Lorazepam) and cardiac (doʙutamin, Dopamine, epinephrine, norepinephrine) preparations, cardiac glycosides, Diuretic, glucagon, etc.. With heart block - transvenous pacing, connection pacemaker.

Dosing and Administration

Inside, without chewing, drinking a small amount of liquid, in the morning on an empty stomach or during breakfast 1,25-10 mg 1 once a day. Dosage regimen individual, increase the dose under the control of blood pressure and heart rate. Arterial hypertension and angina: 5-10 Mg; mild hypertension (Dad minder 105 mmHg.): 2,5 mg; congestive heart failure: by 1,25 mg / day (during 1 Sun), then with good endurance dose increase to 2,5 mg / day (1 Sun), 3,75 mg / day (1 Sun), 5 mg / day (4 Sun), 7,5 mg / day (4 Sun), hereinafter 10 mg / day (target dose). The maximum daily dose for adults - 20 mg.

Precautions

Keep in mind the possibility of masking the symptoms of hypoglycemia and hyperthyroidism during treatment. Perhaps the increased severity of hypersensitivity reactions and the lack of effect of conventional doses of epinephrine with aggravated allergic history. In severe hepatic dysfunction, Acute renal failure (Cl creatinine less than 20 ml / min), sick, located on the hemo- or peritoneal dialysis, the dose should be reduced. When pheochromocytoma should not be given without the introduction of alpha-blockers. Bisoprolol reduces the compensatory cardiovascular reactions in response to the use of general anesthetics and iodine-containing contrast agents. It is necessary to stop the drug for 48 hours prior to anesthesia or choose anesthetic with the least negative inotropic effects. Treatment should be stopped gradually, for about 2 Sun (possible withdrawal). Be wary of during the drivers of vehicles and people, skills relate to the high concentration of attention. It is necessary to exclude the use of alcoholic beverages during treatment (the risk of orthostatic hypotension).

Cautions

You can change the results of the tests in the lab.

Cooperation