Nebivolol

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Nebivolol is a receptor blocker? ₁ with a potent nitric oxide-vasodilation effect used in the treatment of hypertension and, in Europe, as well as for left ventricular failure. It's very cardioselective in certain circumstances. Nebivolol has also been paired with other blood pressure-lowering drugs, angiotensin receptor blockers valsartan.

Video Nebivolol

Pharmacology and biochemistry

? 1-selectivity

Beta blockers help patients with cardiovascular disease by blocking? receptors, while many of the side effects of these drugs are caused by their receptor blockade 2. For this reason, blocking beta blockers? 1 adrenergic receptor (called a cardioselective or 1-selective beta blocker) produces fewer side effects (eg, bronchoconstriction) than drugs that non-selectively block both 1 and 2 receptors.

In laboratory experiments performed on biopsied heart tissue, nebivolol proved to be the most-1-selective of the tested-blockers, being about 3.5 times as much? 1-selective than bisoprolol. However, the selectivity of drug receptors in humans is more complex and depends on the drug dose and the genetic profile of patients taking the drug. The drug is highly cardioselective at 5 mg. In addition, at doses above 10 mg, nebivolol loses cardioselectivity and blocks both receptors 1 and 2. (While the recommended initial dose of nebivolol is 5 mg, adequate blood pressure control may require doses up to 40 mg). In addition, nebivolol is also not cardioselective when taken by patients with a genetic makeup that makes them "poor metabolizers" of nebivolol (and other drugs) or with CYP2D6 inhibitors. As many as 1 in 10 white and even black are poor CYP2D6 metabolites and therefore may benefit less from nebivolol cardioselectivity although no direct comparative study is currently available.

Action vasodilator

Nebivolol is unique as a beta-blocker. Unlike carvedilol, it has nitric oxide (NO) - potentiation, vasodilation effects through stimulation of receptors 3. Along with labetalol, celiprolol and carvedilol, this is one of four beta blockers that causes dilation of blood vessels in addition to effects on the heart.

Antihypertensive effect

Nebivolol lowers blood pressure (BP) by reducing peripheral vascular resistance, and significantly increases stroke volume with cardiac output preservation. The net hemodynamic effect of nebivolol is the result of a balance between the effects of beta-blockade depressants and actions that maintain cardiac output. The antihypertensive response was significantly higher with nebivolol compared with placebo in trials that enrolled a group of patients considered to represent the US hypertensive population, in Black patients, and in those who received treatment alongside other antihypertensive drugs.

Pharmacological side effects

Several studies have shown that nebivolol has reduced the side effects of a typical beta-blocker, such as fatigue, clinical depression, bradycardia, or impotence. However, according to the FDA

FDA warning letter about ad claims

At the end of August 2008, the FDA issued a Warning Letter to the Forest Laboratory citing exaggerated and misleading statements in their launch journal ads, in particular on claims of superiority and novelty of action.

Maps Nebivolol

Contraindications

• Heavy brains
• The heart block is bigger than the first level
• Patients with cardiogenic shock
• Decompensated heart failure
• Sinus syndrome pain (except permanent pacemaker)
• Patients with severe liver disorders (Child-Pugh class B)
• Patients who are hypersensitive to any component of this product.

src: dailymed.nlm.nih.gov

Adverse drug reactions

• Headache
• Paresthesia
• Dizzy

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History

Mylan Laboratories grants licenses to US and Canada rights to nebivolol from Janssen Pharmaceutica N.V. in 2001. Nebivolol has been registered and successfully marketed in more than 50 countries, including the United States where it is marketed under the Bystolic brand name of Mylan Laboratories and Forest Laboratories. Nebivolol is produced by Forest Laboratories.

In India, nebivolol is available as Nebizok (Eris life-sciences), Nebicip (Cipla ltd), Nebilong (Micro Labs), Nebistar (Lupine ltd), Nebicard (Torrent), Nubeta (Abbott Healthcare Pvt Ltd - India), and Nodon ( Cadila Pharmaceuticals). In Greece and Italy, nebivolol is marketed by Menarini as Lobivon. In the Middle East, Russia and in Australia, it is marketed under the name Nebilet and in Pakistan marketed by The Searle Company Limited as Byscard.

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References

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External links

• Prescription Information for BYSTOLIC

Source of the article : Wikipedia