Nebivolol Tablets

Mechanism

Nebivolol selectively blocks β1-adrenergic receptors, reducing heart rate and cardiac output. It also stimulates nitric oxide release from vascular endothelium, leading to vasodilation and improved arterial compliance.

Pharmacokinetics

• Absorption: Rapidly absorbed after oral administration; peak plasma concentration in 1.5–4 hours.
• Bioavailability: ~12% due to extensive first-pass metabolism; higher in poor CYP2D6 metabolizers.
• Distribution: Highly lipophilic; plasma protein binding ~98%; volume of distribution ~10 L/kg.
• Metabolism: Extensively metabolized in liver via CYP2D6; genetic polymorphism affects plasma levels.
• Excretion: ~38% via urine, ~48% via feces; metabolites inactive.
• Half-life: ~12 hours in extensive metabolizers; up to 20 hours in poor metabolizers.
• Special Populations: Clearance reduced in hepatic and renal impairment; dose adjustment required.

Side Effects

• Headache
• Dizziness
• Fatigue
• Diarrhea
• Bradycardia (serious)

Contraindication

• Severe bradycardia or AV block
• Cardiogenic shock
• Severe hepatic impairment
• Hypersensitivity to Nebivolol

Interaction

• CYP2D6 inhibitors (fluoxetine, paroxetine – increase Nebivolol levels)
• Other antihypertensives (clonidine, verapamil – additive hypotension)
• Insulin/antidiabetics (mask hypoglycemia symptoms)
• NSAIDs (may reduce antihypertensive effect)

Warning and Precautions

• Monitor heart rate and blood pressure regularly
• Use under medical supervision only
• Caution in elderly patients

Dosage

As directed by the Physician.