Nebilet 5mg tablet Menarini treats hypertension and chronic heart failure (1 blister x 14 tablets)

Dosage form Box of 1 blister x 14 tablets
Specifications Nebivolol

Ingredient

Composition information	Content
Nebivolol	5mg

Uses

Indications

Treatment Hypertension :

Treatment of idiopathic hypertension

Chronic heart failure (CHF):

Coordinate with standard treatment to treat chronic heart failure to stabilize mild to medium level in patients aged 70 and over.

Pharmacological

Nebivolol is a mixture of two types of optical isomers, SRRR - Nebivolol (D - Nebivolol) and RSSS - Nebivolol (L - Nebivolol). The drug combines two pharmacological effects:

Selective antagonism and receptor competion β: The effect of SRRR-Enantiomer isomers (D-Enantiomer).

There is a mild vascular stretching due to interaction with the L - Arginine/Nitric Oxid NO road.

Use nebivolol single dose or repeat dose to reduce heart rate and lower blood pressure when resting and when physical exercise, both normal people and hypertension patients. Hypotension effect is maintained when long -term treatment.

In the treatment dose, Nebivolol has no antagonistic effect α - adrenergic.

Short and long -term treatment with nebivolol for patients with hypertension, body resistance decreases. Although the heart rate decreases, the cardiac amount when resting and when physical activity does not change due to increasing the volume of the squeeze.

Nebivolol increases the vascular stretching of NO intermediaries for acetylcholine whose parameters usually decrease in patients with endothelial dysfunction.

In vitro and in vivo tests show that Nebivolol does not have the same effect as endogenous sympathetic (Intrinsic Sympathomimetic Activity) and use Nebivolol at non -membrane pharmacological doses.

Pharmacokinetics

absorption

Both Nebivolol's optical isomers are absorbed quickly after drinking. The absorption of the drug is not affected by food. The average bioavailability of Nebivolol after drinking is 12% with fast metabolites and almost entirely with poor metabolites.

In plasma, both isomers are mainly associated with albumin. The cohesion with plasma protein is 98.1% with SRRR isomers and 97.9% with RSSS isomers.

Metabolism

Nebivolol is widely metabolized, largely into active hydroxy metabolites. Nebivolol is metabolized through the saturated and aromatic hydroxylation (due to the enzyme CYP2D6), reducing Alkyl and glucuronide; Glucuronide of hydroxyl metabolites is also formed.

Elimination

The sale time of the average rapid metabolites is 10 hours and will last 3-5 times in slow metabolites. When rapid metabolism, the plasma concentration of the RSSS isomer is a little higher than the SRRR isomer. When rapid metabolism, the sale time of hydroxyl metabolites of the two types of isomer average is 24 hours, and lasts 2 times when the metabolism is slow. Nebivolol concentration in plasma is stable within 24 hours and a few days for hydroxyl metabolites.

Before taking Nebilet 5mg tablet Menarini treats hypertension and chronic heart failure (1 blister x 14 tablets)

How to use

oral medication. Can be taken at meals.

Dosage

Hypertension

Adults: 1 tablet/day (5 mg), preferably taken at the same time every day.

Hypotension effect will be clear after 1-2 weeks of treatment. Sometimes, the maximum efficiency is only achieved after 4 weeks.

Coordinate with other anti -hypertension drugs:

β blockers may be used or combined with other blood pressure drugs. Hypotension effect is enhanced when coordinated with hydrochlorothiazide 12.5 - 25 mg.

Patient kidney failure : The starting dose is 2.5 mg/day. If necessary, the dose can be increased to 5 mg/day.

Patients with liver failure: data is limited. Therefore, contraindicated use of Nebilet for this object.

Elderly: In patients over 65 years old, the starting dose is 2.5 mg/day. If necessary, the dose can be increased to 5 mg. However, there is little experience in treating patients over 75 years old, cautious and tightly controlled when taking the drug for this object.

Children: There is no data on the safety and effectiveness of Nebilet in children and teenagers under 18 years old. Do not recommend using medicine for this object.

chronic heart failure

To treat chronic heart failure stable, the dose should be increased slowly until the optimal dose for each patient.

Patients with stable chronic heart failure are patients who do not suffer from acute heart failure occurred within 6 weeks. The treatment doctor must be experienced in the treatment of chronic heart failure.

For patients who are taking cardiovascular drugs (diuretics, digoxin, ACE inhibitors, Angiotensin II antagonists), should maintain stable dose of these drugs for 2 weeks before starting treatment with Nebilet.

Adjusting the dose increasing should be conducted in step by step, with the gap between the dose increases is 1-2 weeks depending on the response of the patient: 1.25 mg of Nebivolol, up to 2.5 mg x 1 time/day, then 5 mg x 1 time/day, then 10 mg x 1 time/day. The maximum dose is 10 mg x 1 time/day.

When starting to treat and every time the dose increases should be monitored by the doctor with experience for at least 2 hours to ensure the clinical states are still stable (blood pressure, heart rate, conduction disorders, signs of more severe heart failure).

ADR's appearance can cause patients to not be treated at maximum doses. If necessary, the maximum dose can also be reduced step by step and re -use the appropriate dose.

During the dose adjustment, if the disease

heart failure is more serious or the patient is intolerant to the drug, the dose reduced or stopped immediately if needed (when lowered with severe blood pressure, the more severe heart failure is accompanied by acute pulmonary edema, cardiovaol, symptomatic heart rate, atrial block).

Treatment of chronic heart failure with Nebivolol is often long -term treatment.

Do not stop nebivolol suddenly because it can make the heart failure more seriously. If stopping the drug is necessary, it is necessary to reduce the dose slowly every week.

Patients with renal impairment: No dose adjustment for patients with mild to moderate renal impairment because the maximum increase is adjusted to each patient. There is no experience in treating patients with severe renal impairment (serum creatinine ≥ 250 μmol/l). Nebivolol should not be used for these patients.

Patients with liver failure: data is limited. Contraindicated Nebilet for these patients.

Elderly: No need to adjust the dose because the maximum tolerance has been adjusted for each patient.

Children: There is no data on the safety and effectiveness of Nebilet in children and teenagers under 18 years old. Do not recommend using medicine for this object.

Note: The above dose is for reference only. Specific dosage depends on the condition and level of progression of the disease. For a suitable dose, you need to consult a doctor or medical specialist.What to do when overdose?

Treatment: In case of overdose or hypersensitivity, the patient must be closely monitored and treated at the Department of Active Care. Should check blood sugar levels. Prevent the remaining drug absorption in the stomach by lavely and take active carbon or laxative. Artificial respiration can sometimes be required. Bradycardia or vagus reaction can be treated by using atropine or methylatropine. Hypotension and shock can be treated by plasma infusion or plasma alternative solutions and if can use catecholamine. The effect of β blockers can be opposed by slow venous infusion isoprenaline hydrochloride at the starting dose of about 5 μg/min, or dobutamine with the starting dose of about 2.5 μg/minute, until the requirements are reached. If still not achieved, it is possible to use isoprenaline with dopamine . If it is still not effective, it is possible to consider glucagon intravenously 50 - 100 μg/kg. If necessary, the injection is repeated within 1 hour, then, if necessary, Glucagon 70 μg/kg/h can be transmitted. In some rare cases of anti -treatment heart rate, the pacemaker can be used.

What to do when you forget a dose? However, if close to the next dose, skip the forgotten dose and take the next dose at the time as planned. Do not drink twice as prescribed.

Side Effects

Common, ADR> 1/100

Nervous system: headache , dizziness, paresthesia.

Digestive system: constipation , nausea, diarrhea.

Respiratory system: Difficulty.

Other: fatigue, edema.

Uncommon, 1/1000

Mental: nightmares, depression .

vision: Reduction of vision. Cardiovascular system: Slow heart rate, heart failure, atrial block - ventricular, slowly conductive - ventricular, lower blood pressure.

Automatic system: Bronchospasm.

Digestive system: indigestion, flatulence, vomiting.

Skin and subcutaneous tissue: itching, rash.

Reproductive system: impotence.

Instructions on how to handle ADR

When experiencing side effects of the drug, it is necessary to stop using and notify the doctor or go to the nearest medical facility for timely treatment.

Warnings

Before using the drug you need to read the instructions carefully and refer to the information below.

Contraindicated

contraindicated drugs used in the following cases:

Hypersensitivity to any ingredients of the drug.

Hepatic failure or liver dysfunction. Acute heart failure, heart shock, loss of heart failure to use drugs to use medications that cause intravenous heart muscle contraction.

Sinus impairment syndrome, including sinus - atrial block.

Block heart level 2 and degree 3 (without pacemaker).

History of bronchospasm or bronchial asthma .

Patients with colored cell tumors have not been treated.

Metabolic acidosis.

Slow heart rate (heart rate

Hypotension (systolic blood pressure

Severe peripheral vascular disease.

Be cautious when used

Continue to be treated with β blockers reduces the risk of arrhythmia during anesthesia and intubation. If you stop taking β blockers before surgery, it is stopped at least 24 h earlier. Be cautious when using some anesthetic because it can reduce myocardial strength. Atropin intravenous injection can help patients avoid vagus reactions.

Do not use β blockers for patients with congestive heart failure, unless it is stable when heart failure is stable.

Stop slowly (through 1-2 weeks) β blockers in patients with ischemia. If necessary, should start treating with other drugs at the time of stopping the drug to avoid overeating angina.

Need to control regularly when the beginning of the treatment of chronic heart failure with Nebivolol. Do not suddenly stop pesticides when indicated clearly.

β blockers may slow down the heart rate. If the heart rate is below 50 - 55 BPM when resting and/or with symptoms of slow heart rate, the dose should be reduced.

Caution in patients with peripheral circulatory disorders (Raynaud's syndrome, limp) because these disorders may be more serious.

Caution in patients with cardiac block 1, because of the effect of slowing the transmission time of the β blockers.

Precautions in patients with prinzmetal angina due to the effect of alpha receptor antagonism causing coronary spasms, β blockers can increase the frequency and time of angina.

It is not recommended to combine Nebivolol with calcium blockers in Verapamil and Diltiazem, anti -arrhythmia group I, antihypertensive drugs acting on the central.

Nebilet does not affect blood sugar in diabetes patients. However, it is necessary to be cautious because Nebivolol can cover some signs of hypoglycemia (fast heartbeat, chest drum).

β blockers can cover heart symptoms quickly in hyperthyroidism patients. Sudden stopping of the drug may increase symptoms.

In patients with COPD, can use β blockers but must be cautious because it can increase respiratory spasms.

Patients with a history of psoriasis are only used for blocking pills when carefully considered.

β blockers can cause increased sensitivity to allergens and worsen hypersensitivity reactions.

The ability to drive and operate machinery

There has been no research on the effect of the drug on the ability to drive and operate machinery. The drug does not affect the mental function. When driving and operating machinery, should pay attention that dizziness and fatigue can sometimes occur

pregnancy

nebivolol can be harmful to pregnancy, fetus/infant. In general, the β blockers reduce the circulatory flow through the placenta, make the fetus underdeveloped, the fetal death, miscarriage or early labor. Other unwanted side effects (hypotension, slow heart rate) may occur for fetus/infant.

Do not use nebivolol during pregnancy unless really necessary. If you need treatment with β blockers, you should use selective inhibitors on the receptor β1 and closely monitor the blood flow to the uterus - each other and the development of the fetus. If it is harmful to the mother and the fetus, it is advisable to consider using other drugs. Symptoms of hypotension and slow heart rate often occur in the first 3 days.

Lactation period

In vivo studies show that Nebivolol is excreted through milk. No data in humans. Most β blockers (especially fat -soluble preparations such as Nebivolol and its active metabolites) excrete on breast milk, although different levels. Do not breastfeed when using nebivolol.

Drug interaction

Antihyodfight drugs Group I (Quinidine, hydroquinidine, cibenzoline, flecainide, disopyramide, lidocaine, Mexiletine , Propafenone): Slow the atrial -ventilated time and reduce heart muscle contractions.

Verapamil/diltiazem calcium blockers: reduce myocardial contraction and inhibit the atrial - ventricular conduction.

Coordinate with hypotension effectively acting on the central level (Clonidine, guanfacin , moxonidine, methyldopa , rilmenidine ) can seriously cause heart failure due to reducing the force of central sympathetic nerves (reducing heart rate and heart vascular arc). Sudden stopping the drug, especially if it has previously stopped using β blockers, which may increase the risk of "hypertension backwards".

Anti -arrhythmia group III (Amiodarone): Affects the time of the atrial - ventricular.

Simultaneous use of β blockers and Halogen anesthetics can reduce reflected tachycardia and increase the risk of hypotension.

cardiac glycosides: simultaneous use may increase the time of atrial - ventricular.

Simultaneously used with calcium blockers dihydropyridine group (amlodipine, felodipine, lacidipine, nifedipine , nicardipine, nimodipine , nitrendipine) can increase the risk of lowering blood pressure, reduced pump function of heart failure in the patient.

Mental medications, antidepressants (three rounds, barbiturate, phenothiazine): simultaneous use may increase the lowering effects of β blockers.

Sympathetic drugs: simultaneous use may cause loss of the effect of β blockers. The β blockers can stimulate the effect of alpha adrenergic of sympathetic drugs with both α and β - adrenergic systems (risk of hypertension, heart rate and cardiac block).

The metabolism of Nebivolol is related to CYP2D6, so the simultaneous use of these enzyme inhibitors, (especially paroxetine, fluoxetine, thioridazine, quinidine) can increase the concentration of nebivolol in plasma, increase the risk of excessive slow heart rate and other ADRs.

Nebivolol combination with cimetidine increases the concentration of Nebivolol in plasma but does not change the clinical effect. Collaborate with Ranitidine does not affect the pharmacokinetics of Nebivolol. As long as taking Nebilet during meals, or using antacids between meals, these two drugs can be used together.

Nebivolol combination with nicardipine increases the concentration of both drugs in plasma but does not change the clinical effect. Using drugs with alcohol, Furosemide or hydrochlorothiazide does not affect the pharmacokinetics of Nebivolol. Nebivolol does not affect the pharmacokinetics and pharmacology of Warfarin.

Storage

Storage below 30 ° C.

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