Ivolol 2.5

Indications:

• Heart Failure
• Hypertension (High Blood Pressure)

Administration:

• Can be taken with or without food for convenience.

Adult Dosage:

For Hypertension:

• Starting Dose: 5 mg once daily.
• Maintenance Dose: Can increase to a maximum of 40 mg daily, depending on the patient’s needs, with dose adjustments made at 2-week intervals.

For Elderly Patients (over 65 years):

• Starting Dose: 2.5 mg once daily, increasing to 5 mg once daily if needed.

For Heart Failure:

• Starting Dose: 1.25 mg once daily.
• Maintenance: Can double the dose every 1-2 weeks if well tolerated. The maximum dose is 10 mg once daily.

In Case of Hepatic Impairment:

• Start with 2.5 mg per day, and increase cautiously under medical supervision.

Renal Impairment Dosage:

• For Creatinine Clearance (CrCl) < 30 mL/min: Start with 2.5 mg once daily. The dose may be increased to 5 mg daily if required.

Contraindications:

• Hepatic Impairment
• Sick Sinus Syndrome
• Second and Third-Degree Heart Block (unless using a pacemaker)
• History of Asthma
• Metabolic Acidosis
• Severe Peripheral Arterial Disease
• Severe Bradycardia
• Cardiogenic Shock or Decompensated Heart Failure
• Untreated Pheochromocytoma
• Pregnancy and Lactation (not recommended)

Mode of Action:

• Nebivolol selectively blocks beta-1 adrenergic receptors and promotes vasodilation through nitric oxide release from the endothelium. Unlike other beta-blockers, it does not have intrinsic sympathomimetic activity or membrane-stabilizing effects.

Precautions:

• Caution in patients with:
  • Inadequate cardiac function
  • Well-compensated heart failure
  • Myasthenia Gravis
  • Major surgery with general anesthesia
• Potential risks:
  • May mask symptoms of hypoglycemia and hyperthyroidism.
  • Abrupt discontinuation can worsen angina, and may precipitate myocardial infarction (MI) and ventricular arrhythmias, especially in patients with coronary artery disease.
• Monitoring:
  • Regularly monitor ECG, blood pressure, and blood glucose in diabetic patients.
• Pregnancy & Lactation:
  • Not recommended during pregnancy and lactation as safety is not established.

Side Effects:

• Common (1-10%):
  • Headache (6-9%), Fatigue (2-5%), Dizziness (2-4%), Diarrhea (2-3%), Nausea (1-3%), Increased triglyceride levels and insulin resistance, Decreased HDL levels (1%), Insomnia (1%), Peripheral edema (1%), Weakness (1%)
• Less Common (<1%):
  • Bradycardia, Chest pain, Dyspnea, Anaphylaxis (potentially fatal)

Drug Interactions:

• Increased plasma concentration with potent CYP2D6 inhibitors (e.g., paroxetine, fluoxetine, propafenone, thioridazine, quinidine).
• Concomitant use with antiarrhythmic drugs (e.g., amiodarone, disopyramide) or nondihydropyridine calcium channel blockers (e.g., diltiazem, verapamil) may cause conduction disturbances.
• Additive effects on AV conduction and heart rate when used with other beta-blockers or digoxin.
• Hypotension or bradycardia may occur when used with catecholamine-depleting agents (e.g., reserpine).
• Abrupt clonidine withdrawal may increase the risk of rebound hypertension.