Nebita

Approved Indications:

• Hypertension (Essential):
  Indicated for the treatment of primary (essential) hypertension in adults, as monotherapy or in combination with other antihypertensive agents.
• Heart Failure (Chronic, Mild to Moderate):
  Indicated for the treatment of stable, mild to moderate chronic heart failure (NYHA Class II or III) in addition to standard therapies in patients aged 70 years or older.

Clinically Accepted Off-label Uses:

• Migraine Prophylaxis:
  Used off-label in select cases for the prevention of migraine attacks, particularly in patients who cannot tolerate other prophylactic agents.
• Hypertension with Metabolic Syndrome or Diabetes:
  Preferred in these populations due to its neutral or beneficial effect on lipid and glucose metabolism.

রেজিস্টার্ড চিকিৎসকের নির্দেশনা অনুযায়ী ঔষধ সেবন করুন।

Adults (Hypertension):

• Initial Dose: 5 mg once daily.
• Titration: May be increased to 10 mg once daily based on patient response.
• Maximum Dose: 40 mg/day in divided doses (rarely used).
• Administration: Orally, with or without food, at the same time each day.

Adults (Heart Failure):

• Initial Dose: 1.25 mg once daily.
• Titration: Gradually increase at 1-2 week intervals to 2.5 mg, 5 mg, and up to a maximum of 10 mg once daily as tolerated.

Elderly:

• Start at lower doses (e.g., 2.5 mg/day). Titrate slowly with monitoring of heart rate and renal function.

Pediatric Use:

• Not recommended. Safety and efficacy have not been established in patients under 18 years of age.

Renal Impairment:

• Mild to Moderate (CrCl ≥30 mL/min): Start with lower doses (2.5 mg/day).
• Severe (CrCl <30 mL/min): Use with caution; monitor closely.

Hepatic Impairment:

• Mild to Moderate: Start at 2.5 mg/day.
• Severe Hepatic Impairment: Contraindicated.

রেজিস্টার্ড চিকিৎসকের নির্দেশনা অনুযায়ী ঔষধ সেবন করুন।

Nebivolol Hydrochloride is a highly selective β1-adrenergic receptor blocker that decreases heart rate and myocardial contractility, thereby lowering blood pressure and myocardial oxygen demand. It is unique among beta-blockers due to its stimulation of endothelial nitric oxide (NO) release via β3-adrenergic agonism, which results in peripheral vasodilation and improved vascular compliance. This dual action—beta-blockade and NO-mediated vasodilation—contributes to enhanced antihypertensive efficacy and reduced side effects such as fatigue and sexual dysfunction compared to non-selective beta-blockers.

• Absorption: Rapid and complete after oral administration.
• Bioavailability: ~12% in extensive metabolizers; ~96% in poor metabolizers (CYP2D6-dependent).
• Distribution: Highly protein-bound (~98%); volume of distribution: ~10 L/kg.
• Metabolism: Extensively metabolized in the liver via CYP2D6 into active hydroxylated metabolites.
• Elimination:
• Renal: ~38% as metabolites.
• Fecal: Remaining portion via biliary route.
• Half-life:
• Extensive metabolizers: 10–12 hours.
• Poor metabolizers: Up to 30 hours.
• Steady-State: Achieved within 5–7 days of daily dosing.

Pregnancy:

• FDA Classification: Not assigned (previously Category C).
  Beta-blockers may reduce uteroplacental blood flow, leading to fetal bradycardia, growth restriction, and neonatal hypoglycemia. Use only if benefits clearly outweigh risks.

Lactation:

• Excretion into Breast Milk: Yes (small amounts).
  May cause bradycardia, hypoglycemia, or hypotension in breastfed infants.
• Recommendation: Use with caution. Monitor infant for signs of adverse effects if therapy is necessary during lactation.

• Primary Therapeutic Class: Antihypertensive Agent
• Subclass:
• β1-selective Beta-blocker (Cardioselective)
• Third-generation Beta-blocker with Vasodilatory Action

• Known hypersensitivity to Nebivolol or any formulation component
• Severe hepatic impairment
• Second- or third-degree AV block (without pacemaker)
• Sick sinus syndrome
• Symptomatic bradycardia
• Cardiogenic shock
• Decompensated heart failure
• Severe hypotension
• Severe peripheral arterial disorders
• Pregnancy (relative contraindication in 2nd/3rd trimester)

• Bradycardia: Monitor heart rate, especially in elderly or with concomitant digoxin.
• Heart Failure: May be used in stable CHF but contraindicated in decompensated heart failure.
• Abrupt Withdrawal: Should be avoided; may cause rebound hypertension or ischemia.
• Asthma or COPD: Use with caution due to risk of bronchospasm.
• Diabetes Mellitus: May mask hypoglycemic symptoms.
• Renal or Hepatic Impairment: Dose adjustment required; monitor renal and hepatic function periodically.
• Peripheral Vascular Disease: May worsen symptoms.
• Thyrotoxicosis: May mask tachycardia, a key warning sign.

Common Side Effects:

• Cardiovascular: Bradycardia, orthostatic hypotension
• Neurological: Fatigue, dizziness, headache
• Gastrointestinal: Nausea, diarrhea
• General: Edema, cold extremities

Less Common:

• Insomnia
• Depression
• Decreased libido
• Dyspnea (mild)

Serious (Rare):

• Severe bradycardia or AV block
• Exacerbation of heart failure
• Bronchospasm (especially in predisposed individuals)
• Hypotension requiring intervention

Onset: Within the first few days to weeks of therapy
Dose-dependence: More pronounced at higher doses, especially in sensitive populations

Major Interactions:

• CYP2D6 inhibitors (e.g., paroxetine, fluoxetine, quinidine): May increase plasma levels of Nebivolol, enhancing bradycardia or hypotension.
• Calcium channel blockers (e.g., verapamil, diltiazem): Risk of additive negative chronotropic effects; avoid IV use together.
• Other antihypertensives: Additive hypotensive effect.
• Digoxin: Risk of bradycardia.
• Anesthetic agents: Enhanced hypotensive effect; monitor during surgery.
• Insulin or oral antidiabetics: May mask signs of hypoglycemia.

Food Interaction:

• Food slightly delays absorption but does not reduce the extent. Can be taken with or without meals.

Alcohol:

• May enhance hypotensive effects. Use cautiously.

• AHA/ACC 2023 Hypertension Guidelines: Endorse beta-blockers as second-line or add-on therapy in uncomplicated hypertension; preferred in heart failure, post-MI, and high sympathetic drive.
• ESC Guidelines: Favor Nebivolol in elderly patients and those with metabolic comorbidities due to favorable tolerability profile.
• Formulation Enhancements: Extended-release formulations being developed for once-daily convenience.

• Temperature: Store below 25°C (77°F)
• Humidity: Keep in a dry place
• Light: Store in the original container to protect from light
• Handling Instructions:
• Do not crush or chew tablets
• Keep out of reach of children
• Refrigeration: Not required