Nebivolol

BRAND NAME:

Bystolic  - It is an oral tablet that contains Nebivolol as the active ingredient, which helps in decreasing blood pressure and it is marketed as Bystolic Nebivolol 2.5mg,5mg,10mg, and 20mg.

MECHANISM OF ACTION:

A β-1 adrenergic receptor antagonist, nibivolol functions by obstructing beta-1 receptors.  Normally, hormones referred to as catecholamines bind to these receptors. Nitric oxide synthase, which is involved in NO-mediated vasodilation, is stimulated by this medication, which also affects the vascular endothelium. By stimulating the synthesis of NO synthase from the endothelium through β-agonism, nevivolol reduces systemic vascular resistance. Additionally, beta blockers like carvedilol and labetalol have vasodilatory effects. Slowing down the heartbeat is achieved by blocking these receptors. It also relaxes the blood vessels in your body. These effects have the potential to decrease blood pressure and lower the risk of stroke and heart attack.

PHARMACOKINETICS:

Absorption: Nebivolol takes 1.5 to 4 hours to reach its peak plasma concentration. The bioavailability can range from 12  - 96%. Food does not affect any absorption levels.

Distribution: It mainly binds with albumin and its protein bound is 98%.

Metabolism: The liver is where nebivolol is mostly metabolized. It is metabolized via hydroxylation mediated by CYP2D6 and glucuronidation. The half-life of the active isomer is approximately 12 hours in CYP2D6 fast metabolizers and 19 hours in slow metabolizers.

Excretion: Nebivolol is eliminated as oxidative metabolites or glucuronide conjugates. 35% of nebivolol is eliminated through urine and 44% through feces. Patients with slow metabolizers excrete 67% in urine and 3% in feces.

PHARMACODYNAMICS:

Nebivolol is a selective beta -1 androgenic receptor antagonist that reduces vascular resistance, increases stroke volume and cardiac output, and has no negative effect on left ventricular function.

DOSAGE AND ADMINISTRATION:

Nebivolol is available in the form of oral tablets with strengths of 2.5, 5, 10, and 20mg.

The dosing of nebivolol in patients with hypertension is based on their needs. The recommended dose for patients is 5mg once daily, which can be taken independently of meals. The dose depends on the patient's health condition. The maximum dose is 40mg once daily. It should not be discontinued without doctors' advice.

DRUG INTERACTIONS:

Some medications when interacting with nebivolol may change the way a drug works and can be harmful. Before taking nebivolol it is important to discuss with the doctor the drugs taken previously for the treatment of other health conditions, based on this the doctor may decrease the dosage of the drugs. Below are the drugs that interact with nebivolol.

• Depression drugs - Fluoxetine, Paroxetine

• Heart drugs - Digoxin, Verapamil, Diltiazem, Disopyramide

• Alpha blockers – Doxazosin, Prazosin and Terazosin

• Catecholamine-depleting drugs – Reserpine, Guanethidine

• High blood pressure drugs – Nadolol, carvedilol, atenolol, acebutolol, metoprolol, betaxolol, bisoprolol, penbutolol, propranolol, timolol

• Irregular heartbeat drugs – Quinidine, propafenone.

• Sildenafil

• Clonidine

FOOD INTERACTION:

Avoid alcohol, salted food, and high cholesterol-related foods.

CONTRAINDICATIONS: 

Nebivolol is contraindicated in patients with cardiogenic shock, decompensated heart failure, hepatic impairment, sinus, and bradycardia, and also be cautious with patients having a history of severe anaphylaxis to various allergens.

ADVERSE EFFECTS:

• Headache

• Fatigue

• Paresthesias

• Asthenia

• Insomnia

• Hyperuricemia

• Rhinitis

• Dizziness

• Diarrhea

• Abdominal pain

• Nausea

• Kidney injury

• Edema

• Angioedema

• Bronchospasm

• Atrioventricular blocking

• Liver injuries

• Thrombocytes

• Psoriasis

TOXICITY:

Overdosage of Nebivolol can lead to some toxic effects as mentioned below

• Vomiting

• Heart failure

• Bronchospasm

• AV Block