Nichicard

Non-bicardi is an selective blocker of β-adrenergic receptor activity.

Indications In Nebraska

It is used with increased blood pressure.

[1]

Release form

The preparation is sold in tablets, in the amount of 10 pieces inside the blister pack. The box contains 2 or 5 of these packages.

Pharmacodynamics

The nebivolol component is a racemate containing 2 enantomers: SRRR (Nebivolol type D), and RSSS (Nebivolol type L). It combines such therapeutic properties:

• the activity of the D enantomer promotes selective and competitive blocking of the activity of β1-adrenergic receptors;
• The L enantomer helps to develop a mild vasodilating effect by metabolic binding to L-arginine / NO.

After a 1-time or repeated use of drugs, the HR values under load and in a calm state decrease in people with normal blood pressure and in patients with elevated blood pressure.

Hypotensive activity persists with prolonged therapy. The use of the drug in optimal dosage does not lead to the development of α-adrenergic antagonism.

The drug does not have an ICA. When used in therapeutic portions, the membrane-stabilizing effect does not develop. Also, the medicine does not have a noticeable effect on tolerance with respect to physical exertion.

[2], [3]

Pharmacokinetics

The drug absorbed quickly absorbed inside the gastrointestinal tract; the intake of food does not affect the degree of absorption of the drug, which allows you to take it without binding to eating.

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

When nebivolol is administered orally, the average bioavailability is 12% in people with fast metabolism, and is also almost complete in people with slow metabolism. Given the difference in the rate of metabolic processes, it is necessary to select a portion of Nebikard, taking into account the individual characteristics of the patient. People with slow metabolic processes need to use lower dosages of drugs.

In people with a high metabolic rate, the plasma half-life of nebivolol enantomers is about 10 hours on average, and in persons with a low rate these rates are three times five times higher. In fast metabolism users, the values of RSSS-nebivolol within the blood plasma are slightly higher than the level of SRRR-nebivolol.

After a lapse of 7 days after applying the drug, approximately 38% of the drug is excreted in the urine, and another 48% - with feces. In the unchanged state, together with the urine, a maximum of 0.5% of the substance is excreted.

[4], [5], [6],

Dosing and administration

Use the medicine should not be tied to eating, squeezed pills with plain water. It is recommended to take drugs at the same time of day.

With elevated blood pressure, it is necessary to take 1 tablet a day (at the same time of day); admittance with food is allowed. Development of hypotensive effect is observed after 1-2 weeks of therapy, but sometimes the required effect can be achieved only after 1 month.

Means that block the activity of β-adrenoreceptors, can be used as monotherapy or in combination with other antihypertensive drugs. An additional hypotensive effect can be achieved with the combined use of 5 mg of Nebikard, as well as 12.5-25 mg of hydrochlorothiazide.

People with a deficiency of kidney function first need to consume 2.5 mg per day. If necessary, the dosage can be increased to 5 mg.

People with liver failure are not allowed to use the medication, because for this category of patients, the experience of taking drugs is limited.

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

[12], [13]

Use In Nebraska during pregnancy

Nebikard is not used in pregnancy or lactation.

Contraindications

Among the contraindications:

• presence of strong sensitivity with respect to the active element or any auxiliary components of drugs;
• insufficiency of hepatic activity or problems with liver function;
• heart failure in the acute stage, cardiogenic shock, and in addition, decompensated heart failure, in which it is necessary to use inotropic drugs;
• untreated pheochromocytoma;
• SSSU;
• a blockade of a sinouauric character and a blockade of the 2nd or 3rd degree (with or without an electrocardiostimulator);
• bronchial spasms or asthma, available in history;
• acidosis, which has a metabolic character;
• bradycardia (HR values are less than 60 beats / minute);
• reduced blood pressure (systolic pressure is less than 90 mm Hg);
• problems with peripheral blood flow in severe degree;
• combination with sultopride or floktaphenin.

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

Side effects In Nebraska

The use of medication can trigger the development of certain side-effects:

• Immune disorders: manifestations of hypersensitivity or edema Quincke;
• mental problems: nightmares and depression;
• disorders affecting the work of the National Assembly: paresthesia, headaches, syncope and dizziness;
• lesions of the visual organs: visual disorders;
• violations in the CCC area: prolongation of AV-conduction, bradycardia, lowering of blood pressure, AV blockade, heart failure and potentiation of intermittent claudication;
• problems in the work of respiratory organs: spasms of bronchi and dyspnoea;
• disorders of digestive activity: bloating, abdominal pain, constipation, vomiting, and besides dyspepsia, diarrhea, nausea and the development of hepatotoxic effect;
• damage to the epidermis: itching, allergy, skin symptoms similar to erythema, and exacerbation of psoriasis;
• signs affecting the reproductive function: impotence and erectile dysfunction;
• systemic disorders: swelling and fatigue;
• problems with the work of the ODA: muscle pain or weakness, as well as convulsions.

With the use of β-blockers, there were sometimes such disorders: psychosis, dry eye mucous membranes, confusion, hallucinations, Raynaud's disease, cold extremities and intoxication of the eye mucosa.

[11]

Overdose

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

When intoxication or the appearance of hyperergic reaction, it is necessary to establish constant medical control over the patient, as well as to provide him with intensive therapeutic assistance.

It is required to track blood sugar values. Absorption of the active element remaining inside the gastrointestinal tract can be prevented by rinsing the stomach to the patient, and in addition appointing a laxative with activated charcoal. Along with this, it may be necessary to perform the procedure of artificial pulmonary ventilation.

To prevent the development of bradycardia, enter methylatropine or atropine.

To treat shock and increase the reduced values of blood pressure, it is required to use plasma or plasma substitutes, and with this, when the need arises, catecholamines.

The development of the β-blocking effect can be stopped by iv injection (at low speed) of isoprenaline hydrochloride (start with 2.5 μg / minute, and continue until the desired effect is achieved). If the patient is intolerant, it is necessary to combine isoprenaline with dopamine. In the absence of the required result and after taking such a measure, it is necessary to inject glucagon in the dose of 50-100 mcg / kg. If necessary, the injection can be repeated for 1 hour, and then, if necessary, perform IV infusion of glucagon through a dropper (the portion is calculated according to the scheme of 70 μg / kg / hour).

In extreme situations, for example, in the case of a bradycardia that is stable with respect to treatment, it is allowed to apply a pacemaker.

[14]

Interactions with other drugs

Calcium antagonists.

The combination of β-adrenoreceptor blocking substances with calcium antagonists (such as diltiazem and verapamil) requires great care, because they have a negative inotropic effect and influence on AV conductivity. People who use Nebikard should not be injected with verapamil intravenously.

Antiarrhythmic drugs.

Combination of β-adrenoreceptor blocking agents and antiarrhythmic medicines of the 1 st and 3 rd classes, as well as of amiodarone, requires use with extreme caution, because in this case, potentiation of their negative inotropic action and influence with respect to the AV and intracardiac conductivity can be noted.

Klonidin.

In the case of sudden cancellation of long-term therapy with clonidine, drugs blocking α-adrenergic receptors increase the likelihood of withdrawal syndrome, in which the values of blood pressure increase. In this regard, the abolition of the use of clonidine should be done gradually.

Digitalis medications.

Niphenenchic glycosides, used together with drugs that block the activity of β-adrenergic receptors, are able to prolong the period of AB-conduction.

Ingestable hypoglycemic drugs and insulin.

While Nebikard has no effect on sugar, it can mask signs of hypoglycemia (such as tachycardia).

Anesthetic preparations.

The use of β-blockers together with anesthetic drugs can lead to inhibition of reflex tachycardia, as well as increase the likelihood of a decrease in pressure. It is necessary to inform the anesthesiologist in advance about the use of Nebikard.

Combination with cimetidine increases the plasma values of nebivolol, but its drug activity does not change.

If you take Nebikard with food, and the antacid drug - between meals, both of these medicines can be used together.

The combination with nicardipine increases the plasma indices of both these substances without changing their therapeutic activity.

Sympathomimetics can interfere with the activity of β-blockers.

The agents blocking the activity of β-adrenergic receptors are able to provoke unhindered α-adrenergic activity of sympathicotonic drugs possessing both α-adrenergic and β-adrenergic effects (there is a risk of AV blockade or severe bradycardia and increased blood pressure values).

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

Since the isoenzyme CYP2D6 participates in the metabolic processes of nebivolol and is carried out against the backdrop of SSRI therapy (eg, dextromethorphan or other compounds) metabolized mainly by the same metabolic pathway, it can lead to the fact that the response to treatment in people with a high metabolic rate will become is similar to the response observed in people with a low rate of this process.

[15]

Storage conditions

Non-bacardi must be kept in a place that is closed from sunlight, moisture and small children. Temperatures are within 25 ° C.

[16]

Shelf life

The non-bicardium can be used within 36 months from the date of manufacture of the medicinal product.

[17]

Application for children

It is forbidden to prescribe a medication in pediatrics.

Analogues

The analogues of the drug are Nebilet, Nebival, Nebitrend with Nebivolol, Nebilong, Nebivolol Sandoz and Nebitens from Nebivolol Teva.

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

Reviews

The non-bicarde helps well with increased blood pressure, stabilizing the pressure, which is reflected in the comments of users who used this medicine. Also in the reviews it is noted that you should take the medicine at the same time, and at the same time do not expect a very quick result. Usually the effect begins to appear after a few weeks, and sometimes a month - to this you need to be ready. Therefore, as an emergency emergency aid, this remedy is completely inappropriate - this should be remembered.