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Nebilet contains the active ingredient Nebivolol hydrochloride, belongs to a group of cardiovascular drugs indicated in the treatment of hypertension, chronic heart failure from mild to moderate... Let's learn about the uses and usage of Nebilet through the article. down here.1. What does Nebilet do?
1.1. Indications for use of the drug Nebilet 5mg Nebilet drug contains the active ingredient Nebivolol 5mg (exists in two forms, d - nebivolol and l - nebivolol). The drug is indicated in the treatment of the following diseases:
Treatment of hypertension; Treatment of mild to moderate chronic heart failure in patients 70 years of age and older. 1.2. Pharmacodynamics Nebivolol belongs to the group of cardiovascular drugs that selectively block beta receptors (selective cardiovascular effects). The drug has the effect of controlling the pumping ability of the heart, preventing increased heart rate, dilating blood vessels and contributing to lowering blood pressure. Nebivolol exists in a mixture of 2 isomers (d - nebivolol and l - nebivolol) with specific pharmacological effects as follows:
The d - nebivolol isomer is a selective and competitive beta-receptor antagonist; Both isomers have mild vasodilator properties due to interactions with the L-arginine/nitric oxide NO pathway. Nebivolol used in single or repeated doses has been shown to reduce heart rate and blood pressure at rest and during exercise (both in normal subjects and in hypertensive patients). The effectiveness of maintaining stable blood pressure is increased with long-term drug treatment.
Nebivolol short-term treatment of hypertension reduces systemic resistance. In which, heart rate decreases but cardiac output at rest and exercise remains unchanged due to increase in stroke volume. The drug increases the NO-mediated vasodilator response to acetylcholine (this parameter is reduced in patients with endovascular dysfunction).
Nebivolol was shown to prolong time to hospital admission or time to cardiovascular death (relative risk reduction ratio 14%, absolute risk 4.2%). Efficacy of the drug was independent of gender, age or degree of reduced left ventricular ejection fraction (LVEF) in study subjects. The benefit in reducing the risk of all-cause mortality was not different when compared with placebo (absolute ratio 2.3%).
In vitro and in vivo studies in animals have shown that the drug does not have endogenous sympathomimetic effects, and at pharmacological doses, there is no membrane stabilizing effect.
In healthy volunteers, Nebivolol did not affect maximal exercise capacity or endurance.
1.3. The pharmacokinetics of the two isomers of Nebivolol are rapidly absorbed from the gastrointestinal tract after oral administration. Absorption is not affected by food, so the drug can be taken with or without food. The majority of Nebivolol is metabolised via aromatic and saturated ring hydroxylation, glucuronidation and alkyl reduction. In addition, the glucuronide of the hydroxyl metabolite is also formed. Bioavailability after oral administration is about 12% with the rapid metabolite and almost completely with the poor metabolite. At a given dose and at steady state, peak plasma concentrations of nebivolol are unchanged, the poorly metabolised form is 2 to 3 times higher than that of the rapidly metabolized form. Comparing the metabolized and unmetabolized forms, the difference in plasma concentrations is about 1.3 to 1.4 times. Because of the different changes in the rate of metabolism, the dose of Nebilet is always adjusted appropriately for each patient (lower metabolizers use lower doses).
2. Dosage and how to use Nebilet
2.1. Dosage of Nebilet The use of Nebilet 5mg in the treatment of hypertension, mild to moderate heart failure with dosage depends on the specific condition of the patient. Dosage should always be exactly as prescribed by your doctor. The drug can be taken before, during or after a meal and should be taken with plenty of water. The specific dosage of the drug is as follows:
- Treatment of hypertension:
The usual dose is 1 tablet/day, taken at the same time of day; Elderly patients or patients with renal dysfunction should take the usual starting dose of 1⁄2 tablets/day; Effective blood pressure control after 1-2 weeks of treatment, in some cases can last after 4 weeks of treatment. - Treatment of chronic heart failure:
Treatment of heart failure with Nebilet must be supervised by an experienced treating physician; The starting dose of treatment is 1⁄4 tablets/day, can be increased to 1⁄2 tablets/day after 1-2 weeks of treatment, then increase to 1 tablet/day and 2 tablets/day until adequate dose is reached. suitable for the patient; The maximum dose of Nebilet is 2 tablets/day; Patients should not stop taking the drug suddenly because it can aggravate heart failure; Do not treat heart failure with Nebilet in patients with severe underlying renal failure; Take the medicine every day, preferably at the same time. 2.2. Treatment of overdose In case the patient accidentally takes an overdose, it is necessary to notify the treating doctor immediately. Some common overdose symptoms are low blood pressure which can cause fainting, very slow heart rate, shortness of breath as in an asthma attack (caused by bronchospasm), acute heart failure.
3. Contraindications
Treatment with Nebilet 5mg is contraindicated in the following cases:
The patient is allergic to any component of Nebilet; People with medical conditions including low blood pressure, severe circulatory disorders in the legs and arms, slow heart rate (less than 60 beats/min); People with serious cardiac arrhythmias such as cardiac conduction disturbances, second- and third-degree atrioventricular block; Heart failure gets worse; The patient is being treated for circulatory shock due to acute heart failure; Bronchial asthma or wheezing difficulty; People with adrenal gland tumor , mesophilic cell tumor are not treated; People with liver dysfunction; People with metabolic disorders such as diabetic ketoacidosis.
4. Undesirable effects
Nebilet 5mg drug may cause some side effects as follows:
Common side effects (Frequency > 1/100 and < 1/10 in patients taking the drug): Constipation, headache, dizziness, shortness of breath, fatigue, unusual itching, diarrhea, swelling of the hands and feet, dizziness; Uncommon side effects (Frequency > 1/1000 and <1/100): Slow heart rate or cardiovascular problems such as indigestion, vomiting, bloating in the stomach, rash, low blood pressure, itching, pain in the legs like cramps when walking, shortness of breath, impotence, visual disturbances, feelings of depression, nightmares; Very rare side effects (Frequency < 1/10000): Exacerbation of psoriasis, syncope; Side effects reported in a few isolated cases with Nebilet such as generalized red skin rash, systemic allergic reactions, rapidly spreading edema especially in the eyes, around the lips or tongue can cause sudden difficulty breathing. suddenly.
5. Drug interactions
Patients need to inform the treating doctor when taking any of the following medicines when treating with Nebilet 5mg:
Heart disease drugs and blood pressure control drugs: Clonidine, Amiodarone, Amlodipine, Digoxin, Cibenzodin, Disopyramid, Diltiazem, Hydroquinidin, Felodipine, Lacidipine, Guanfacin, Flecainide, Methyldopa, Moxonidin, Nifedipine, Nitrendipin, Nimodipine, Quinidin, Verapamil, Rilmenidin, Propafenon; Medicines to treat neurological diseases, sedatives such as Barbiturates, Phenothiazines, Thioridazines; Medicines to treat depression such as Paroxetin, Amitriptylin, Fluoxetin; Anesthesia and anesthesia in surgery; Medicines for stuffy noses, asthma and eye disorders such as glaucoma (increased pressure in the eye), dilated pupils; Amifostin (a protective drug used in cancer patients), Baclofen (an antispasmodic); Medicines to treat stomach ulcers or increase gastric acid secretion, such as cimetidine. In this case, the patient should take antacids before meals, Nebilet during or after meals.
6. Effects of drugs on special subjects
Pregnant women and lactating women: Do not use Nebilet in pregnant or lactating women, unless absolutely necessary and prescribed by a doctor. Driving and operating machines: Nebilet may cause dizziness, lightheadedness, dizziness and fatigue. Therefore, patients should not drive or operate machinery while taking the drug. The article has provided information on dosage, contraindications and notes during the use of Nebilet. Note, this is a prescription drug, patients do not arbitrarily use to ensure safety for health.
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