Nebesel
Nebesel Uses, Dosage, Side Effects, Food Interaction and all others data.
Nebesel is a β-adrenergic receptor blocking agent. Nebesel is a racemate of two enantiomers, d-Nebesel and l-Nebesel. Nebesel exhibits high selectivity for β1-adrenergic receptors and has vasodilating activity due to a direct action on the endothelium, involving nitric oxide release. It lacks intrinsic sympathomimetic and membrane-stabilising activity.
Nebesel is a selective beta-1 adrenergic receptor antagonist that decreases vascular resistance, increases stroke volume and cardiac output, and does not negatively affect left ventricular function. It has a long duration of action as effects can be seen 48 hours after stopping the medication and a wide therapeutic window as patients generally take 5-40mg daily. Patients should not abruptly stop taking this medication as this may lead to exacerbation of coronary artery disease. Diabetic patients should monitor their blood glucose levels as beta blockers may mask signs of hypoglycemia.
| Trade Name | Nebesel |
| Availability | Prescription only |
| Generic | Nebivolol |
| Nebivolol Other Names | Narbivolol, Nebivolol, Nebivololum |
| Related Drugs | amlodipine, lisinopril, metoprolol, losartan, furosemide, hydrochlorothiazide |
| Type | Tablet |
| Formula | C22H25F2NO4 |
| Weight | Average: 405.435 Monoisotopic: 405.175164703 |
| Protein binding | Nebivolol is 98% bound to plasma proteins, mostly to serum albumin. |
| Groups | Approved, Investigational |
| Therapeutic Class | Beta-adrenoceptor blocking drugs, Beta-blockers |
| Manufacturer | Zuventus Health Care Ltd |
| Available Country | India |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Nebesel is used for the treatment of essential hypertension and adjunct in stable mild to moderate heart failure in patients over 70 years.
Nebesel is also used to associated treatment for these conditions: High Blood Pressure (Hypertension)
How Nebesel works
Nebesel is a highly selective beta-1 adrenergic receptor antagonist with weak beta-2 adrenergic receptor antagonist activity. Blocking beta-1 adrenergic receptors by d-nebivolol leads to decreased resting heart rate, exercise heart rate, myocardial contracility, systolic blood pressure, and diastolic blood pressure. The selectivity of d-nebivolol limits the magnitude of beta blocker adverse effects in the airways or relating to insulin sensitivity. Nebesel also inhibits aldosterone, and beta-1 antagonism in the juxtaglomerular apparatus also inhibits the release of renin. Decreased aldosterone leads to decreased blood volume, and decreased renin leads to reduced vasoconstriction. l-nebivolol is responsible for beta-3 adrenergic receptor agonist activity that stimulates endothelial nitric oxide synthase, increasing nitric oxide levels; leading to vasodilation, decreased peripheral vascular resistance, increased stroke volume, ejection fraction, and cardiac output. The vasodilation, reduced oxidative stress, and reduced platelet volume and aggregation of nebivolol may lead to benefits in heart failure patients.
Dosage
Nebesel dosage
Adults: 5 mg daily, maximum recommended dose 40 mg once daily.
Renal Impairment: In patients with severe renal impairment the recommended initial dose is 2.5 mg once daily; titrate up slowly if needed.
Hepatic Impairment: In patients with moderate hepatic impairment, the recommended initial dose is 2.5 mg once daily; titrate up slowly if needed.
Geriatric Patients: It is not necessary to adjust the dose in the elderly.
Pediatric Use: Safety and effectiveness of Nebesel in pediatric patients have not been established.
Side Effects
The most common side effects are headache, nausea and bradycardia.
Toxicity
Patients experiencing an overdose may present with bradycardia, hypotension, cardiac failure, dizziness, hypoglycemia, fatigue, vomiting, bronchospasm and heart block. Treat overdose with general supportive measures including intravenous atropine for bradycardia, vasopressors and intravenous fluids for hypotension, isoproterenol infusion for heart block, digitalis glycosides and diuretics for congestive heart failure, bronchodilators for bronchospasm, and intravenous glucose for hypoglycemia.
Precaution
Patients with inadequate cardiac function, well-compensated heart failure, myasthenia gravis. Patients undergoing major surgery involving general anaesth. May mask signs and symptoms of hypoglycaemia and hyperthyroidism. Abrupt withdrawal may exacerbate angina symptoms and/or precipitate MI and ventricular arrhythmias in patients with coronary artery disease. Pregnancy and lactation.
Interaction
Use caution when Nebesel is co-administered with CYP2D6 inhibitors (quinidine, propafenone, fluoxetine, paroxetine, etc.), Do not use Nebesel with other β-blockers, both digitalis glycosides and β-blockers slow atrioventricular conduction and decrease heart rate. Concomitant use can increase the risk of bradycardia, Nebesel can exacerbate the effects of myocardial depressants or inhibitors of AV conduction, such as certain calcium antagonists (verapamil and diltiazem), or antiarrhythmic agents, such as disopyramide.
Food Interaction
- Avoid alcohol.
- Take with or without food.
Nebesel Alcohol interaction
[Moderate]
Many psychotherapeutic and CNS-active agents (e.g., anxiolytics, sedatives, hypnotics, antidepressants, antipsychotics, opioids, alcohol, muscle relaxants) exhibit hypotensive effects, especially during initiation of therapy and dose escalation.
Coadministration with antihypertensives and other hypotensive agents, in particular vasodilators and alpha-blockers, may result in additive effects on blood pressure and orthostasis.
Caution and close monitoring for development of hypotension is advised during coadministration of these agents.
Some authorities recommend avoiding alcohol in patients receiving vasodilating antihypertensive drugs.
Patients should be advised to avoid rising abruptly from a sitting or recumbent position and to notify their physician if they experience dizziness, lightheadedness, syncope, orthostasis, or tachycardia.
Nebesel Cholesterol interaction
[Moderate] Beta-adrenergic receptor blocking agents (aka beta-blockers) may alter serum lipid profiles.
Increases in serum VLDL and LDL cholesterol and triglycerides, as well as decreases in HDL cholesterol, have been reported with some beta-blockers.
Patients with preexisting hyperlipidemia may require closer monitoring during beta-blocker therapy, and adjustments made accordingly in their lipid-lowering regimen.
Nebesel multivitamins interaction
[Moderate] ADJUST DOSING INTERVAL: Concurrent administration with calcium salts may decrease the oral bioavailability of atenolol and possibly other beta-blockers.
The exact mechanism of interaction is unknown.
In six healthy subjects, calcium 500 mg (as lactate, carbonate, and gluconate) reduced the mean peak plasma concentration (Cmax) and area under the concentration-time curve (AUC) of atenolol (100 mg) by 51% and 32%, respectively.
The elimination half-life increased by 44%.
Twelve hours after the combination, beta-blocking activity (as indicated by inhibition of exercise tachycardia) was reduced compared to that with atenolol alone.
However, during a 4-week treatment in six hypertensive patients, there was no difference in blood pressure values between treatments.
The investigators suggest that prolongation of the elimination half-life induced by calcium coadministration may have led to atenolol cumulation during long-term dosing, which compensated for the reduced bioavailability.
It may help to separate the administration times of beta-blockers and calcium products by at least 2 hours.
Patients should be monitored for potentially diminished beta-blocking effects following the addition of calcium therapy.
Nebesel Drug Interaction
Moderate: furosemide, amlodipine, alprazolamMinor: aspirin, aspirin, aspirinUnknown: ubiquinone, rosuvastatin, apixaban, omega-3 polyunsaturated fatty acids, atorvastatin, pregabalin, esomeprazole, omega-3 polyunsaturated fatty acids, acetaminophen, clopidogrel, multivitamin, cyanocobalamin, ascorbic acid, cholecalciferol
Nebesel Disease Interaction
Major: bradyarrhythmia/AV block, cardiogenic shock/hypotension, CHF, diabetes, hypersensitivity, ischemic heart disease, PVD, hepatic impairmentModerate: cerebrovascular insufficiency, glaucoma, hyperlipidemia, hyperthyroidism, myasthenia gravis, pheochromocytoma, psoriasis, tachycardia, asthma/COPD, renal impairment
Volume of Distribution
For a 20mg dose, d-nebivolol has an apparent volume of distribution of 10,290.81±3911.72L, l-nebivolol has an apparent volume of distribution of 8,066.66±4,055.50L, and both enantiomers together have a volume of distribution of 10,423.42±6796.50L.
Elimination Route
The absorption of nebivolol is not affected by food. Nebesel has a Tmax of 1.5-4 hours. Bioavailability can range from 12-96% for extensive to poor CYP2D6 metabolizers. For a 20mg dose, d-nebivolol has a Cmax of 2.75±1.55ng/mL, l-nebivolol has a Cmax of 5.29±2.06ng/mL, both enantiomers have a Cmax of 8.02±3.47ng/mL, and nebivolol glucuronides have a Cmax of 68.34±44.68ng/mL. For a 20mg dose, d-nebivolol has an AUC of 13.78±15.27ng*h/mL, l-nebivolol has an AUC of 27.72±15.32ng*h/mL, both enantiomers have an AUC of 41.50±29.76ng*h/mL, and nebivolol glucuronides have an AUC of 396.78±297.94ng*h/mL.
Half Life
d-nebivolol has a half life of 12 hours in CYP2D6 extensive metabolizers and 19 hours in poor metabolizers.
Clearance
For a 20mg dose, the clearance of d-nebivolol is 1241.63±749.77L/h, l-nebivolol is 435.53±180.93L/h, and both enantiomers is 635.31±300.25L/h.
Elimination Route
In extensive CYP2D6 metabolizers, 38% is eliminated in the urine and 44% in the feces. In poor CYP2D6 metabolizers, 67% is eliminated in the urine and 13% in the feces. 5
Pregnancy & Breastfeeding use
Pregnancy category C and not recommended during nursing.
Contraindication
Nebesel is contraindicated in the following conditions: severe bradycardia, heart block greater than first degree, patients with cardiogenic shock, decompensated cardiac failure, sick sinus syndrome, patients with severe hepatic impairment, patients who are hypersensitive to any component of this product.
Acute Overdose
Symptoms: Bradycardia, hypotension, cardiac failure, dizziness, fatigue, hypoglycaemia, vomiting, bronchospasm, heart block.
Management: Symptomatic and supportive treatment. IV atropine may be given for bradycardia, if it persists, admin IV isoproterenol cautiously. For hypotension, admin IV fluids and vasopressors. IV glucagon may also be useful. A β2-agonist and/or aminophylline for bronchospasm. Admin IV glucose for hypoglycaemia and an IV cardiac glycoside and diuretic may be used for CHF.
Storage Condition
Store between 20-25° C. Protect from light. Keep out of the reach of children.
Innovators Monograph
You find simplified version here Nebesel
Nebesel contains Nebivolol see full prescribing information from innovator Nebesel Monograph, Nebesel MSDS, Nebesel FDA label
FAQ
What is Nebesel used for?
Nebesel is a beta blocker used to treat high blood pressure and heart failure. As with other β-blockers, it is generally a less preferred treatment for high blood pressure. It may be used by itself or with other blood pressure medication.
How safe is Nebesel?
Nebesel is well-tolerated in patients with hypertension. In clinical trials, reported adverse events are mostly mild to moderate in nature with an incidence similar to that observed with placebo.
How does Nebesel work?
Nebesel works by affecting the response to nerve impulses in certain parts of the body, like the heart. As a result, the heart beats slower and decreases the blood pressure. When the blood pressure is lowered, the amount of blood and oxygen is increased to the heart.
What are the common side effects of Nebesel?
Common side effects of Nebesel are include:
- Bloating or swelling of the face, arms, hands, lower legs, or feet
- chest pain or discomfort
- difficult or labored breathing
- lightheadedness, dizziness, or fainting
- rapid weight gain
- shortness of breath
- slow or irregular heartbeat
- tightness in the chest
- tingling of the hands or feet
- unusual tiredness or weakness
- unusual weight gain or loss
- wheezing
Is Nebesel safe during pregnancy?
The Nebesel administration produce adverse effects on fetal growth and postnatal development, that limits their therapeutic use in females during pregnancy.
Is Nebesel safe during breastfeeding?
Beta-adrenergic blocking agents, particularly lipophilic agents like this Nebesel, have caused adverse events in breastfed newborns.
Can I drink alcohol with Nebesel?
Alcohol will add to the blood pressure-lowering effect of Nebesel and so may not be advisable for you. If you have diabetes, Nebesel can block the symptoms of low blood sugar.
Can I drive after taking Nebesel?
Nebesel oral tablet may cause tiredness. Avoid driving or using heavy machinery until you know how this drug affects you.
When is the best time to take Nebesel?
Nebesel tablets may be taken before, during or after the meal, but, alternatively, you can take it independently of meals.
How often can I take Nebesel?
Adults, at first, 5 milligrams (mg) once a day. Your doctor may increase your dose if needed. Children, use and dose must be determined by your doctor.
How long does Nebesel take to work?
Nebesel may take 2 weeks before the full benefit of Nebesel is seen in blood pressure readings.
What is the half-life of Nebesel?
The half-life of Nebesel varies as well: 10.3 hours in extensive metabolizers and 31.9 hours in poor metabolizers.
Who should not take Nebesel ?
You should not take Nebesel if you are allergic to it, or if you have: a serious heart condition such as heart failure, "AV block" (2nd or 3rd degree), or sick sinus syndrome (unless you have a pacemaker); very slow heartbeats; severe liver disease.
What happen If I missed Nebesel?
If you miss a dose of Nebesel, take it as soon as you remember. If you remember close to your next dosage time, skip the missed dose and take the next dose. Do not take a double dose to compensate for the missed dose.
What happens if I take too much Nebesel?
If you take too much: Taking too much of this drug may cause severe side effects such as very low blood pressure (hypotension), a dangerously slow heart rate (bradycardia), heart failure, trouble breathing, extreme tiredness, dizziness, or very low blood sugar that could even lead to a coma.
Can I take Nebesel for a long time?
If it continues for a long time, the heart and arteries may not function properly. This can damage the blood vessels of the brain, heart, and kidneys, resulting in a stroke, heart failure, or kidney failure. High blood pressure may also increase the risk of heart attacks.
What happens if I stop taking Nebesel?
Do not stop taking Nebesel without talking to your doctor. If you suddenly stop taking Nebesel it may cause angina (chest pain), heart attack, or irregular heartbeat. Your doctor will probably decrease your dose gradually over 1 to 2 weeks.
Can Nebesel affects my heart ?
Taking Nebesel can worsen heart failure. It can also slow your heart rate down to a rate that is unsafe. For people with circulation problems: This Nebesel can worsen peripheral vascular disease.
Can Nebesel affects my liver?
Drug-induced liver injury is a common cause of acute liver failure. Despite its use in several large clinical trials, nebivolol has not been linked to cases of clinically apparent liver injury. Likelihood score: E (unlikely cause of clinically apparent liver injury).
Can Nebesel affect my kidneys?
Nebesel has beneficial effect on the kidney allograft. Studies in animal transplants have shown that Nebesel could reduce ischemia-induced reperfusion injury, alleviate renal perfusion pressure and increase NO release with associated vasodilation of the renal vasculature.
