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Nebicard belongs to the group of cardiovascular treatment, often indicated in patients with chronic heart failure and hypertensive disease. The drug helps to stabilize heart failure in elderly patients and is effective when treating other classes of cardiovascular drugs.
1. What is Nebicard?
Nebicard belongs to the group of cardiovascular drugs produced in the form of tablets. The main ingredient is Nebivolol Hydrochoride with a strength of 2.5 mg. Usually indicated for the treatment of conditions such as essential hypertension and mild to moderate heart failure in patients over 70, in combination with other therapies.
2. Composition of the drug Nebicard
Nebivolol is a mixture of two isomers SRRR-nebivolol and RSSS-nebivolol giving the drug two synergistic effects. A selective and competitive beta-blocker for the action of SRRR-nebivolol and has mild vasodilator properties due to interaction with L-arginin/nitric oxide.
3. How is Nebicard metabolized?
Both isomers of nebivolol are rapidly absorbed after oral administration. The absorption of nebivolol is unaffected by food, therefore nebivolol can be taken without regard to meals.
The drug is easily reduced in effectiveness in people with malnutrition. Peak concentrations are reached within 24 hours and within a few days thereafter for the hydroxyl metabolites. In the blood, the drug is mostly conjugated with plasma albumin.
Nebivolol is metabolised in the liver and partially metabolized to the active hydroxyl radicals. The metabolism of aromatic ring hydrolysis is dependent on CYP2D6. The oral drug effect of nebivolol averaged 12% in rapidly metabolizing patients and almost completely in slow metabolisers.
Because of differences in the extent of metabolism, the dose of nebivolol is recommended according to individual patient response. Patients with low metabolism require a lower dose. In rapid metabolizers, the mean half-life of nebivolol is 10 hours. In slow metabolizers, the half-life is 3 to 5 times longer. After one week of use, Nebivolol was eliminated 38% in the urine and 48% in the feces.
4. Dosage and usage
4.1 Treatment of hypertension For hypertension indications in adults, the dose is 5mg/day, preferably at the same time of day. The effect to help lower blood pressure begins to be effective after 1-2 weeks of treatment. Sometimes, some patients will achieve optimal effects after 4 weeks.
Beta blockers such as nebivolol can be used alone or in combination with other antihypertensive agents. According to current research, nebivolol 5mg is effective only when combined with hydrochlorothiazide 12.5-25mg.
In patients with severe renal impairment, the recommended starting dose is 2.5 mg/day and the dose can be increased to 5 mg/day.
Data on patients with hepatic impairment or impaired liver function are limited, so caution should be exercised and nebivolol is not indicated in patients with serious liver disease.
For patients over 65 years of age, a starting dose of 2.5 mg/day is recommended. If necessary, the dose may be increased to 5 mg/day. However, for patients over 75 years of age, caution should be exercised and the patient should be closely monitored for adverse events.
There are no reliable data on the efficacy and safety of nebivolol in children and adolescents under 18 years of age. Therefore, nebivolol is not indicated for use in children under 18 years of age due to the lack of data on safety and efficacy.
4.2 Treatment of Chronic Heart Failure: Treatment of stable chronic heart failure should be initiated by gradual titration until the optimal individual maintenance dose is reached.
Patient must have stable heart failure with no symptoms of acute heart failure within the past 6 weeks.
For patients being treated with cardiovascular drugs including diuretics and ACE inhibitors or angiotensin II receptor antagonists, the dosage of these drugs should be stabilized for the previous 2 weeks before when initiating treatment with nebivolol.
Initiating dose escalation is done in increments of approximately 1-2 weeks based on patient tolerability: 1.25mg nebivolol, increased to 2.5mg nebivolol once daily, then increased to 5mg x 1 times/day and 10mg x 1 time/day.
The maximum recommended dose is 10mg x 1 time/day.
Initiation and each dose escalation should be carried out under the supervision of an experienced physician over a period of at least 2 hours to ensure clinical status (especially for blood pressure, heart rate, conduction disturbances, signs of worsening heart failure) remained stable.
The occurrence of adverse events may preclude all patients from being treated with the maximum recommended dose. If necessary, the dose can be gradually reduced to be achieved in increments and re-administered to the appropriate dose.
During the titration phase, in the event of worsening of heart failure or intolerance, a reduction in the dose of nebivolol is recommended first, or immediate discontinuation if necessary (in case of severe hypotension, severe heart failure with edema). acute pulmonary disease, cardiogenic shock, symptomatic bradycardia or atrioventricular block).
Treatment of stable chronic heart failure with nebivolol requires long-term therapy. Treatment with nebivolol must not be stopped abruptly as this may lead to worsening heart failure. If discontinuation is necessary, the dose should be gradually reduced to half a weekly dose.
No dose adjustment is required in mild to moderate renal impairment as dose escalation to maximally tolerated dose is individualized. There is no therapeutic experience in patients with severe renal impairment (serum creatinine ≥ 250 μmol/L). Therefore, nebivolol should not be used in these patients.
Data on patients with hepatic impairment or impaired liver function are limited. Therefore, nebivolol should not be used in these patients.
No dose adjustment is required as the maximum tolerated dose is individually adjusted for each patient.
Nebivolol is not recommended for use in children under 18 years of age due to lack of data on safety and efficacy.
Drink at a certain time of the day, can be taken with meals.
5. Contraindications:
Hypersensitivity to nebivolol or any of the ingredients. Liver failure or impaired liver function. Acute heart failure, cardiogenic shock, or episodes of decompensated heart failure require intravenous inotropes. Sinus node conduction dysfunction syndrome, including sinoatrial block. 2nd or 3rd degree heart block (without pacemaker). History of bronchospasm or bronchial asthma. Untreated adrenal myeloma. Metabolic acidosis. Bradycardia (heart rate < 60 beats/min before starting treatment) Hypotension (systolic blood pressure < 90 mmHg). Severe peripheral circulatory disorders.
6. Side effects
Adverse effects are reported separately for hypertension and chronic heart failure because of differences in comorbidities. In most cases mild to moderate adverse reactions were reported, presented in the following table, classified by body system and in order of frequency. Common (1/100 ≤ ADR < 1/10): + Nervous system disorders: Headache, dizziness, paresthesia. + Disorders of the respiratory system, chest and mediastinum: Shortness of breath. + Digestive disorders: Constipation, nausea, diarrhea. + General disorders: Fatigue, edema. + Psychiatric disorders: Nightmares, depression. Visual disturbances: Decreased visual acuity. + Cardiac arrhythmias: bradycardia, heart failure, atrioventricular conduction bradycardia/ atrioventricular block. + Vascular disorders: hypotension (increased) intermittent claudication. + Disorders of the respiratory system, chest and mediastinum: Bronchospasm. + Digestive disorders: Indigestion, flatulence, vomiting. Skin and subcutaneous tissue disorders: Pruritus, rash, erythema. + Disorders of the mammary gland and reproductive system: Impotence. Very rare (ADR <1/10, 000): + Nervous system disorders: Syncope. Skin and subcutaneous tissue disorders: Exacerbation of psoriasis. Not known: + Immune system disorders: Angioedema, hypersensitivity reactions.
7. Drug recommendations for pregnant and lactating women
Nebivolol has pharmacological effects that may cause harm to a pregnant woman and/or the fetus/newborn child. In general, beta-blockers reduce the amount of blood that crosses the placenta; has been associated with growth retardation, intrauterine death, miscarriage, or preterm birth. Adverse effects (eg, hypoglycemia, bradycardia) may occur in the fetus and neonate. If treatment with a beta-blocker is necessary, it is preferable to use a selective beta-1 inhibitor. Nebivolol should not be used during pregnancy unless clearly needed. If treatment with nebivolol is considered essential, blood flow to the uterus and placenta and fetal growth should be monitored. In case of adverse effects on the pregnant woman or the fetus, alternative treatment should be considered. Newborns must be closely monitored. Symptoms of hypoglycemia and bradycardia usually occur during the first 3 days. It is not known whether nebivolol is excreted in human milk. Animal studies have shown that nebivolol is excreted in human milk. Most beta-blockers, especially lipophilic compounds such as nebivolol and its metabolites, pass into breast milk to varying degrees. Nebivolol should not be used during breastfeeding.
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