Nebicor

Nebicor is an α- and β-adrenergic blocker.

Indications Nebicora

It is used to lower excessively high blood pressure (as monotherapy or in combination with other antihypertensive medications), and also to treat angina pectoris and coronary heart disease.

Release form

The substance is released in tablets with a volume of 5 mg. Inside the blister pack there are 10 such tablets. In the box there are 3 plates.

Pharmacodynamics

The drug selectively blocks the activity of β1-adrenoreceptors, and also modulates the binding of the endothelium-derived relaxing factor (NO). The decrease in blood pressure occurs due to a decrease in the values of OPSS and CBV, as well as cardiac output, and in addition, due to a slowdown in the formation of renin and a partial loss of sensitivity by baroreceptors. The antihypertensive effect often manifests itself after 7-14 days, with complete stabilization over the course of 1 month.

The drug reduces the heart rate during exercise and at rest, as well as left ventricular diastolic blood pressure. It also improves the state of diastolic cardiac filling, reduces the myocardium's need for oxygen (antianginal effect) and reduces myocardial weight (by 9.7%) along with its mass index (by 5.1%). Information obtained during daily monitoring shows that Nebikor has a positive effect on the values of the daily blood pressure rhythm (both in individuals with healthy indicators and in those who have its disorders).

Does not have a negative impact on lipid metabolism processes.

Pharmacokinetics

After oral administration, it is absorbed at a high rate. Bioavailability values in people with a high rate of metabolic processes (with the effect of the first liver pass) are 12%. At the same time, in people with a low metabolic rate, this indicator is almost complete.

Protein synthesis within plasma is 98%. Equilibrium values in people with a fast metabolism are observed after 24 hours, and the half-life is approximately 10 hours; with a slow metabolism, the half-life is 3-5 times longer.

The transformation occurs through aromatic and alicyclic hydroxylation processes; part of the substance undergoes N-dealkylation. The resulting amino and hydroxy derivatives enter into conjugation with glucuronic acid, after which they are secreted in the form of N- and O-glucuronides.

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

The excretion of the drug is carried out through the kidneys (40%) and the intestines (60%). The substance passes through the BBB and is excreted with breast milk.

Dosing and administration

The medicine should be taken orally, at the same time of day; the tablet is not chewed, but swallowed with plain water. It is taken with or after food. The dosage is 5 mg once a day.

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

It is permissible to take no more than 10 mg of Nebicor per day.

Use Nebicora during pregnancy

The use of the medicine during pregnancy is permitted only if there are strict medical indications.

During the period of therapy, you should refrain from breastfeeding.

Contraindications

Main contraindications:

• the presence of intolerance to the components of the medication;
• sinus bradycardia (values below 45-50 beats/minute);
• SSSU;
• decreased blood pressure;
• cardiogenic shock;
• AV block 2-3 degree;
• severe heart failure refractory to therapy;
• disorder of peripheral blood flow processes;
• sinoatrial block;
• problems with liver function;
• bronchospasms or bronchial asthma.

Side effects Nebicora

The use of the drug can cause the appearance of various side effects:

• disorders affecting the functioning of the nervous system and sensory organs: dizziness, paresthesia, a feeling of weakness and fatigue, as well as headaches often appear. Occasionally, nightmares occur or depression develops. Temporary visual impairment is possible;
• gastrointestinal disorders: sometimes constipation, diarrhea, vomiting, bloating or nausea appear;
• problems with the function of the cardiovascular system and hemostasis processes with hematopoiesis: AV block, symptomatic form of bradycardia, heart failure, decreased blood pressure and exacerbation of intermittent claudication;
• other signs: manifestations on the epidermis and bronchial spasms.

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Overdose

Signs of poisoning: decreased blood pressure, bradycardia, severe heart failure, and bronchial spasms.

To eliminate disorders, gastric lavage is performed, laxatives and activated carbon are prescribed. Artificial ventilation and atropine can also be administered (in case of increased vagotonia or bradycardia), as well as plasma or plasma substitutes; if necessary, catecholamines are used.

To counteract the β-adrenergic blocking effect, isoprenaline hydrochloride is administered (intravenously, at a low rate, with an initial dosage of 5 mcg/minute until the desired result is achieved) and dobutamine (initial dose of 2.5 mcg/minute). If improvement does not occur, glucagon is used (intravenous injection of 50-100 mcg/kg, and then repeated after 60 minutes - infusion of 70 mcg/kg/hour).

When AV block develops, transvenous cardiac stimulation is used.

Interactions with other drugs

Drugs that block the activity of Ca channels potentiate the blockade of AV conduction processes.

Class 1 antiarrhythmic drugs, as well as amiodarone, prolong the period of conduction of excitation impulses within the atria.

Anesthetic agents (such as cyclopropane, ethoxyethane and trichloroethylene), barbiturates with tricyclics, and phenothiazine derivatives enhance the antihypertensive effect.

Nicardipine with cimetidine increases plasma levels of the drug.

Sympathomimetics equalize therapeutic activity.

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Storage conditions

Nebikor must be kept at temperatures of no more than 30°C.

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Shelf life

Nebikor can be used within 36 months from the date of manufacture of the drug.

Application for children

Nebicor is not used in pediatrics.

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Analogues

Analogues of the drug are the medications Binelol, Nebilet with Nevotens, and also Nebivator and Nebilong.