What are the effects of Nebilet?

Nebilet contains the active ingredient Nebivolol hydrochloride, belonging to the cardiovascular drug group, indicated for the treatment of hypertension, mild to moderate chronic heart failure... Let's find out about the uses and how to use Nebilet through this article.

1. What are the effects of Nebilet?

1.1. Indications for the use of Nebilet 5mg

Nebilet contains the active ingredient Nebivolol 5mg (existing in 2 forms: d-nebivolol and l-nebivolol). The drug is indicated for the treatment of the following conditions:

• Treatment of hypertension;
• Treatment of mild to moderate chronic heart failure in patients aged 70 years and over.

1.2. Pharmacodynamics

Nebivolol belongs to the group of cardiovascular drugs that selectively inhibit beta-blocker(selective effect on the cardiovascular system). The drug is used to control the heart's ability to pump blood, prevent increased heart rate, dilate blood vessels and contribute to lowering blood pressure.  Nebivolol exists in the form of a mixture of 2 enantiomers (d-nebivolol and l-nebivolol) with specific pharmacological effects as follows:

• The d-nebivolol enantiomer is a selective and competitive beta-receptor antagonist;
• Both enantiomers have mild vasodilating properties due to interaction with the L-arginine/nitric oxide pathway.

Nebivolol, when used in single or repeated doses, reduces heart rate and blood pressure at rest and during exercise (in both normal individuals and hypertensive patients). The effect of maintaining stable blood pressure increases with long-term drug treatment.
Nebivolol treatment of hypertension in the short term reduces total peripheral resistance. In which, heart rate decreases but cardiac output at rest and during exercise remains unchanged due to increased stroke volume. The drug increases NO-mediated vasodilator response to acetylcholine (this parameter is reduced in patients with endothelial dysfunction).
Nebivolol has been demonstrated to prolong the time to rehospitalization or death from cardiovascular causes (relative risk reduction of 14%, absolute 4.2%). The efficacy of the drug is independent of gender, age, or the degree of left ventricular ejection fraction (LVEF) reduction in the study population. The benefit of reducing the risk of death from all causes did not differ when compared to placebo (absolute rate 2.3%).
In vitro and in vivo studies in animals have shown that the drug has no intrinsic sympathomimetic activity, and the pharmacological dose of the drug does not have membrane stabilizing properties
In healthy volunteers, Nebivolol did not affect peak exercise capacity or endurance.

1.3. Pharmacokinetics

Both enantiomers of Nebivolol are rapidly absorbed from the gastrointestinal tract after oral administration. The absorption process is not affected by food, so the drug can be taken with or without food.
Most of Nebivolol is metabolized via aromatic and alicyclic hydroxylation, glucuronidation, and alkyl reduction. In addition, glucuronides of the hydroxyl metabolite are also formed. The bioavailability of the drug after oral administration is about 12% with rapid metabolizers and almost complete with poor metabolizers. At a fixed dose and at steady state, the peak plasma concentration of nebivolol is unchanged, and the poor metabolizer has a 2-3 times higher concentration than the rapid metabolizer. Comparing the metabolite and the unchanged form, the difference in plasma concentration is about 1.3-1.4 times. Due to the different changes in the rate of metabolism, the dosage of Nebilet is always adjusted appropriately for each patient (poor metabolism requires a lower dose.

2. Dosage and administration of Nebilet

2.1. Dosage of Nebilet

The effectiveness of Nebilet 5mg in treating hypertension and mild to moderate heart failure depends on the specific condition of the patient. Patients must always take the medication as prescribed. The drug can be taken before, during, or after meals and should be taken with plenty of water. Specific dosage of the drug is as follows:

- Treatment of hypertension:

• The usual dosage is 1 tablet/day, taken at the same time each day;
• Elderly patients or those with impaired renal function should start with a usual dose of 1/2 tablet/day;
• The effect of blood pressure control is seen after 1-2 weeks of treatment, in some cases it may take up to 4 weeks to see the effect.

- Treatment of chronic heart failure:

• Treatment of heart failure with Nebilet must be supervised by an experienced doctor;
• The starting dose is 1/4 tablet/day, which can be increased to 1/2 tablet/day after 1-2 weeks of treatment, then increased to 1 tablet/day and 2 tablets/day until the appropriate dose for the patient is reached;
• The maximum dose of Nebilet is 2 tablets/day;
• Patients should not stop taking the drug suddenly as this may worsen heart failure;
• Nebilet should not be used to treat heart failure in patients with severe underlying kidney disease;
• Take the medicine every day, preferably at the same time.

2.2. Management of overdose

In case a patient accidentally takes an overdose of the drug, they should immediately notify their doctor. Some common symptoms of overdose include low blood pressure which can cause fainting, very slow heart rate, difficulty breathing as in an asthma attack (due to bronchoconstriction), and acute heart failure.

3. Contraindications

Nebilet 5mg is contraindicated in the following cases:

• Patients who are hypersensitive to any component of Nebilet;
• Patients with conditions such as low blood pressure, severe peripheral circulatory disorders, and slow heart rate (below 60 beats per minute);
• Patients with serious heart rhythm disorders such as heart conduction disorders, second and third-degree atrioventricular block;
• Worsening heart failure;
• Patients being treated for circulatory shock due to acute heart failure;
• Asthma or wheezing;
• Patients with pheochromocytoma, untreated pheochromocytoma;
• Patients with impaired liver function;
• Patients with metabolic disorders such as ketoacidosis due to diabetes.

4. Undesirable effects

Nebilet 5mg may cause some side effects as follows:

• Common side effects (Frequency > 1/100 and < 1/10 in patients): Constipation, headache, dizziness, difficulty breathing, fatigue, abnormal itching sensation, diarrhea, swelling of hands and feet, blurred vision;
• Uncommon side effects (Frequency > 1/1000 and < 1/100): Slow heart rate or other cardiovascular problems such as indigestion, vomiting, bloating, rash, low blood pressure, itching, leg pain like cramps when walking, difficulty breathing, impotence, visual disturbances, feeling of depression, nightmares;
• Very rare side effects (Frequency < 1/10000): Worsening of psoriasis, fainting;
• Side effects have been reported in some individual cases when using Nebilet such as generalized red rash, systemic allergic reactions, rapid spreading edema, especially around the eyes, mouth or tongue, which may cause sudden difficulty breathing.

5. Drug interactions

Patients should inform their doctor about any of the following medications when taking Nebilet 5mg:

• Medications for heart disease and blood pressure control: Clonidine, Amiodaron, Amlodipine, Digoxin, Cibenzodin, Disopyramide, Diltiazem, Hydroquinidine, Felodipin, Lacidipin, Guanfacin, Flecainid, Methyldopa, Moxonidin, Nifedipin, Nitrendipin, Nimodipin, Quinidin, Verapamil, Rilmenidin, Propafenon;
• Medications for neurological disorders and sedatives such as Barbiturates, Phenothiazin, Thioridazin;
• Antidepressants such as Paroxetin, Amitriptylin, Fluoxetine;
• Anesthetics during surgery;
• Medications for nasal congestion, asthma and eye disorders such as glaucoma (increased eye pressure), mydriasis;
• Amifostine (a protective drug used for cancer patients), Baclofen (antispasmodic);
• Medications for treating stomach ulcers or increased stomach acid secretion such as Cimetidine. In this case, patients should take antacids before meals, and Nebilet during or after meals.

6. Effects of the drug on special populations

• Pregnant and lactating women: Nebilet should not be used in pregnant women or women who are breastfeeding, unless absolutely necessary and prescribed by a doctor.
• Drivers and machinery operators: Nebilet can cause blurred vision, dizziness, vertigo, and fatigue. Therefore, patients should not drive or operate machinery while taking the medication.

This article has provided information on dosage, contraindications, and precautions when using Nebilet. Please note that this is a prescription drug, and patients should not self-medicate to ensure safety.

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