Nebikor

Nebikor is α-, as well as β-adrenoblocker.

Indications Nebikor

It is used to lower excessively high values of blood pressure (either monotherapy or in combination with other antihypertensive medications), and in addition for the treatment of angina and coronary artery disease.

Release form

The release of the substance is realized in tablets having a volume of 5 mg. Inside the blister pack - 10 such tablets. In the box there are 3 plates.

Pharmacodynamics

The drug selectively blocks the activity of β1-adrenergic receptors, and also modulates the binding of the relaxing endothelial factor (NO). Reduction in blood pressure is due to a decrease in the values of OPSS and BCC, as well as cardiac output, and in addition to this, due to the slowing down of the formation of renin and a partial loss of sensitivity by baroreceptors. Antihypertensive effect is often manifested after 7-14 days, with complete stabilization during the first month.

The medicine lowers the level of heart rate under stress and in a calm state, and in addition the left ventricular parameters of DAD. It also improves the state of diastolic heart filling, weakens myocardial need for oxygen production (antianginal effect) and reduces myocardial weight (by 9.7%), together with its mass index (by 5.1%). The information obtained with daily monitoring shows that Nebikor positively influences the values of the circadian rhythm of BP (both in individuals with healthy indices and in those who have its disturbances).

Does not have a negative effect on lipid metabolism.

Pharmacokinetics

After oral administration, it is absorbed at high speed. The values of bioavailability in people with a high rate of metabolic processes (with the effect of the 1st hepatic transit) are 12%. In this case, in people with a low metabolic rate, this indicator is almost complete.

Protein synthesis inside the plasma is 98%. Equilibrium indicators in people with metabolic rate are observed after 24 hours, and the half-life is approximately 10 hours; with slow metabolism, the half-life is longer than 3-5 times.

Transformation takes place through the processes of aromatic, as well as alicyclic hydroxylation; part of the substance is N-dealkylated. The forming amino- and hydroxy-derivatives enter into conjugation with glucuronic acid, after which they are secreted in the form of N-, as well as O-glucuronides.

The half-life of hydroxymetabolites in individuals with a high metabolic rate is on average 24 hours, and in people with a low metabolism it is twice as high.

Excretion of the medication is carried out through the kidneys (by 40%), as well as the intestines (by 60%). The substance passes through the BBB and is excreted in the mother's milk.

Dosing and administration

Take the medicine by mouth at the same time of day; The tablet is not chewed, but swallowed, washed down with plain water. Reception is carried out with or after food. Dosage is 5 mg 1-fold per day.

People with kidney failure, as well as people over 65 years of age, need to take 2.5 mg of the drug per day.

Within a day, no more than 10 mg Nebikor can be taken.

Use Nebikor during pregnancy

Use of the drug during pregnancy is allowed only if there are strict medical indications.

For the period of therapy, one should refrain from breastfeeding.

Contraindications

The main contraindications:

• the presence of intolerance relative to the elements of the drug;
• bradycardia of sinus character (values below 45-50 beats / minute);
• SSSU;
• decreased blood pressure;
• cardiogenic shock;
• AV-blockade of the 2-3rd degree;
• heart failure in severe degree, refractory regarding therapy;
• disorder of peripheral blood flow;
• blockade of sinoatrial type;
• problems with hepatic activity;
• spasms of bronchi or asthma.

Side effects Nebikor

The use of medication can cause a variety of adverse symptoms:

• disorders affecting the work of the National Assembly and senses: often there are dizziness, paresthesia, a sense of weakness and fatigue, as well as headaches. Occasionally, nightmares arise or depression develops. Perhaps temporary visual disturbance;
• disorders in the gastrointestinal tract: sometimes there are constipation, diarrhea, vomiting, bloating or nausea;
• problems with the function of CCC and hemostasis processes with hematopoiesis: AV blockade, symptomatic bradycardia, heart failure, lowering blood pressure and exacerbation of intermittent claudication;
• Other signs: manifestations on the epidermis and bronchial spasms.

[1],

Overdose

Signs of poisoning: a decrease in blood pressure, bradycardia, heart failure, which is of a serious nature, and spasms of the bronchi.

To eliminate the disorders perform gastric lavage, prescribe laxatives and activated charcoal. It can also be used for ventilation and atropine (with increased vagotonia or bradycardia), and in addition plasma or plasma substitutes; if necessary - apply catecholamines.

To inhibit β-adrenergic blocking, isoprenaline hydrochloride is administered (intravenously, at low speed, with an initial dosage of 5 μg / min until the desired result is obtained) and dobutamine (the initial dose is 2.5 μg / min). If improvement does not occur, glucagon is used (intravenous injection 50-100 μg / kg, and then repeated procedure 60 minutes later - infusion of 70 μg / kg / hour).

With the development of AV blockade, transvenous cardiac stimulation is used.

Interactions with other drugs

Medicaments that block the activity of Ca channels, potentiate the blockade of AB-conduction processes.

Antiarrhythmic drugs of the 1st class, as well as amiodarone, prolong the period of the excitation pulses inside the atria.

Anesthetics (such as cyclopropane, ethoxyethane and trichlorethylene), barbiturates with tricyclics, and phenothiazine derivatives enhance the antihypertensive effect.

Nicardipine with cimetidine increase plasma values of the drug.

Sympathomimetics equalize the therapeutic activity.

[2]

Storage conditions

Nebicore is required to be kept at temperature values of a maximum of 30 ° C.

[3]

Shelf life

Nebikor can be applied within 36 months from the date of manufacture of the medicinal product.

Application for children

Nebikor is not used in pediatrics.

[4]

Analogues

Analogues of the drug are medicines Binelol, Nebilet with Nevotenzom, and in addition Nebivator and Nebilong.