Nebicard

Nebicard is a selective blocker of β-adrenergic receptor activity.

Indications Nebicardium

It is used for increased blood pressure values.

[ 1 ]

Release form

The drug is released in tablets, in the amount of 10 pieces inside a blister pack. The box contains 2 or 5 such packages.

Pharmacodynamics

The component nebivolol is a racemate, which includes 2 enantiomers: SRRR (nebivolol type D) and RSSS (nebivolol type L). It combines the following therapeutic properties:

• D-enantiomer activity promotes selective and competitive blockade of β1-adrenergic receptor activity;
• The L-enantiomer promotes the development of a mild vasodilatory effect through metabolic binding to L-arginine/NO.

After a single or repeated use of the drug, heart rate indicators during exercise and at rest decrease in both people with normal blood pressure and in patients with elevated blood pressure.

Hypotensive activity is maintained during prolonged therapy. Use of the drug in optimal medicinal dosages does not lead to the development of α-adrenergic antagonism.

The drug does not have VSA. When used in therapeutic doses, it does not cause the development of a membrane-stabilizing effect. Also, the drug does not have a noticeable effect on tolerance to physical activity.

[ 2 ], [ 3 ]

Pharmacokinetics

The drug taken is quickly absorbed in the gastrointestinal tract; food intake does not affect the degree of absorption of the drug, which allows it to be taken without reference to food intake.

Nebivolol is involved in liver metabolism processes during which active hydroxymetabolic products are formed. The metabolic process of the substance is associated with oxidative polymorphism of a genetic nature, depending on the CYP2D6 component.

When taking nebivolol orally, its average bioavailability is 12% in people with fast metabolism, and is almost complete in people with slow metabolism. Given the difference in the rate of metabolic processes, it is necessary to select a dose of Nebicard, taking into account the individual characteristics of the patient. People with slow metabolic processes need to use lower doses of the drug.

In individuals with a high metabolic rate, the plasma half-life of nebivolol enantiomers averages 10 hours, while in individuals with a low metabolic rate, these values are three to five times higher. In individuals with a fast metabolic rate, the RSSS values for nebivolol in blood plasma are slightly higher than the SRRR levels for nebivolol.

After 7 days of drug administration, approximately 38% of the drug portion is excreted in the urine, and another 48% in the feces. A maximum of 0.5% of the substance is excreted unchanged in the urine.

[ 4 ], [ 5 ], [ 6 ]

Dosing and administration

The medicine should be used without reference to food intake, washing down the tablets with plain water. It is recommended to take the medicine at the same time of day.

In case of elevated blood pressure, it is necessary to take 1 tablet per day (at the same time of day); it is allowed to take it with food. The development of hypotensive effect is noted after 1-2 weeks of therapy, but sometimes the desired effect can be achieved only after 1 month.

Agents blocking the activity of β-adrenoreceptors may be used as monotherapy or in combination with other antihypertensive drugs. Additional hypotensive effect can be achieved with the combined use of 5 mg of Nebicard and 12.5-25 mg of hydrochlorothiazide.

People with renal insufficiency should initially take 2.5 mg per day. If necessary, the dosage can be increased to 5 mg.

People with liver failure should not use the medication, because experience with taking the drug is limited for this category of patients.

Elderly people (65 years and older) should take 2.5 mg of the drug per day. If necessary, the daily dose is increased to 5 mg. There is only limited data on the use of the drug in people over 75 years of age, which is why when prescribing it to such patients, you need to act very carefully and carefully monitor their condition.

[ 12 ], [ 13 ]

Use Nebicardium during pregnancy

Nebicard is not used during pregnancy or lactation.

Contraindications

Among the contraindications:

• the presence of severe sensitivity to the active ingredient or any auxiliary components of the drug;
• liver failure or problems with liver function;
• acute heart failure, cardiogenic shock, and also decompensated heart failure, which requires the use of inotropic drugs;
• untreated pheochromocytoma;
• SSSU;
• sinoauricular block and 2nd or 3rd degree block (with or without a pacemaker);
• history of bronchospasms or bronchial asthma;
• acidosis of metabolic nature;
• bradycardia (heart rate values are less than 60 beats/minute);
• reduced blood pressure (systolic pressure is less than 90 mm Hg);
• severe peripheral blood flow problems;
• combination with sultopride or floctafenine.

[ 7 ], [ 8 ], [ 9 ], [ 10 ]

Side effects Nebicardium

The use of the medication may provoke the development of certain side effects:

• immune disorders: manifestations of hypersensitivity or Quincke's edema;
• mental problems: nightmares and depression;
• disorders affecting the functioning of the nervous system: paresthesia, headaches, syncope and dizziness;
• visual impairment: visual disturbances;
• disorders in the cardiovascular system: prolongation of AV conduction, bradycardia, decreased blood pressure, AV block, heart failure and potentiation of intermittent claudication;
• problems with the respiratory system: bronchial spasms and dyspnea;
• digestive disorders: bloating, abdominal pain, constipation, vomiting, as well as dyspepsia, diarrhea, nausea and the development of a hepatotoxic effect;
• lesions of the epidermis: itching, manifestations of allergies, skin symptoms similar to erythema, as well as exacerbation of psoriasis;
• symptoms affecting reproductive function: impotence and erectile dysfunction;
• systemic disorders: swelling and feeling of fatigue;
• problems with the functioning of the musculoskeletal system: muscle pain or weakness, as well as cramps.

The following disorders have occasionally occurred with the use of β-blockers: psychosis, dry eye mucosa, confusion, hallucinations, Raynaud's phenomenon, cold extremities, and ocular mucosal intoxication.

[ 11 ]

Overdose

Signs of poisoning: development of acute heart failure or bradycardia, the appearance of bronchial spasms and a decrease in blood pressure.

In case of intoxication or the appearance of a hyperergic reaction, it is necessary to establish constant medical supervision of the patient, as well as provide him with intensive therapeutic care.

Blood sugar levels need to be monitored. Absorption of the active element remaining in the gastrointestinal tract can be prevented by washing the patient's stomach and, in addition, prescribing laxatives with activated carbon. Along with this, it may be necessary to perform artificial pulmonary ventilation.

To prevent the development of bradycardia, methylatropine or atropine is administered.

To treat shock and increase low blood pressure values, it is necessary to use plasma or plasma substitutes, and along with this, if necessary, catecholamines.

The development of the β-blocking effect can be stopped by intravenous injection (at a low rate) of isoprenaline hydrochloride (start with a dose of 2.5 mcg/minute and continue until the desired effect is achieved). If the patient has intolerance, isoprenaline should be combined with dopamine. If the desired result is not achieved and after taking this measure, glucagon should be administered to the victim at a dosage of 50-100 mcg/kg. If necessary, the injection can be repeated within 1 hour, and then, if necessary, intravenous infusion of glucagon through a dropper (the dose is calculated according to the scheme 70 mcg/kg/hour).

In extreme situations, for example, in the case of bradycardia that is resistant to treatment, the use of a pacemaker is permitted.

[ 14 ]

Interactions with other drugs

Calcium antagonists.

The combination of β-adrenergic receptor blocking agents with calcium antagonists (such as diltiazem and verapamil) requires great caution because they have a negative inotropic effect and affect AV conduction. People using Nebicard should not receive verapamil intravenously.

Antiarrhythmic drugs.

The combination of beta-adrenergic receptor blockers and class 1 and 3 antiarrhythmic drugs, as well as amiodarone, requires extreme caution, since this may result in potentiation of their negative inotropic effect and influence on AV and intra-atrial conduction.

Clonidine.

In case of sudden discontinuation of long-term therapy with clonidine, drugs that block α-adrenergic receptors increase the likelihood of withdrawal syndrome, in which blood pressure values increase. In this regard, clonidine should be discontinued gradually.

Digitalis medicines.

Digitalis glycosides, used together with drugs that block the activity of β-adrenergic receptors, are capable of prolonging the period of AV conduction.

Oral hypoglycemic drugs and insulin.

Although Nebicard does not affect sugar levels, it is able to mask signs of hypoglycemia (such as tachycardia).

Anesthetic drugs.

The use of β-blockers together with anesthetic drugs can lead to the suppression of reflex tachycardia, and also increase the likelihood of a decrease in blood pressure. It is necessary to inform the anesthesiologist in advance about the use of Nebicard.

Combination with cimetidine increases plasma levels of nebivolol, but its medicinal activity does not change.

If Nebicard is taken with food and the antacid is taken between meals, both medications can be used together.

Combination with nicardipine increases plasma levels of both substances without changing their therapeutic activity.

Sympathomimetics can interfere with the activity of β-blockers.

Agents that block the activity of β-adrenergic receptors are capable of provoking unimpeded α-adrenergic activity of sympathicotonic drugs that have both α-adrenergic and β-adrenergic effects (there is a risk of developing AV block or severe bradycardia and increased blood pressure).

Combination with barbiturates, tricyclics and phenothiazine derivatives may provoke potentiation of the antihypertensive activity of the drug.

Since the isoenzyme CYP2D6 is involved in the metabolism of nebivolol, concomitant therapy with SSRIs (eg, dextromethorphan or other compounds) that are primarily metabolized by this same pathway may result in a response to treatment in individuals with a high metabolic rate similar to that seen in individuals with a low metabolic rate.

[ 15 ]

Storage conditions

Nebicard should be kept in a place protected from sunlight, moisture and small children. Temperature indicators are within the 25°C mark.

[ 16 ]

Shelf life

Nebicard can be used within 36 months from the date of manufacture of the medicinal product.

[ 17 ]

Application for children

It is prohibited to prescribe the medication in pediatrics.

Analogues

Analogues of the drug are Nebilet, Nebival, Nebitrend with Nebivolol, Nebilong, Nebivolol Sandoz and Nebitenz with Nebivolol-Teva.

[ 18 ], [ 19 ], [ 20 ], [ 21 ], [ 22 ], [ 23 ], [ 24 ]

Reviews

Nebicard helps well with high blood pressure, stabilizing the pressure, which is reflected in the comments of users who have used this medicine. The reviews also note that the medication should be taken at the same time, and at the same time do not expect a very quick result. Usually the effect begins to appear after several weeks, and sometimes a month - you need to be prepared for this. Therefore, this remedy is completely unsuitable as emergency first aid - this should be remembered.