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Nebivolol Power Pharmaceutical Intermediates In Stock CAS NO 99200-09-6

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Nebivolol Power Pharmaceutical Intermediates In Stock CAS NO 99200-09-6

Large Image :  Nebivolol Power Pharmaceutical Intermediates In Stock CAS NO 99200-09-6

Product Details:

Place of Origin: China
Brand Name: R&M
Certification: ISO 9001, USP, GMP
Model Number: 01

Payment & Shipping Terms:

Minimum Order Quantity: 1g
Price: negotiation
Packaging Details: vaccum packing of aluminum foil bag
Detailed Product Description
CasNo: 99200-09-6 Appearance: Detailed See Specifications
Molecular Formula: C22H25F2NO4 PackAge: According To The Clients Requirement
Storage: Store In Dry, Dark And Ventilated Plac...

 

 

Nebivolol

Clinical data
Trade names Nebilet, Bystolic
AHFS/Drugs.com Monograph
MedlinePlus a608029
License data
  • US FDA: Nebivolol

Pregnancy
category
  • US: C (Risk not ruled out)

Routes of
administration
Oral
ATC code
  • C07AB12 (WHO)

Legal status
Legal status
  • UK: POM (Prescription only)
    US: ℞-only

Pharmacokinetic data
Protein binding 98%
Metabolism Hepatic (CYP2D6-mediated)
Eliminationhalf-life 10 hours
Excretion Renal and fecal
Identifiers
IUPAC name[hide]
  • (1RS,1' RS)-1,1'-[(2RS,2' SR)-bis(6-fluoro-3,4-dihydro-2H-1-benzopyran-2-yl)]-2,2'-iminodiethanol
    OR
    1-(6-Fluorochroman-2-yl)-{[2-(6-fluorochroman-2-yl)-2-hydroxy-ethyl]amino}ethanol
    OR
    2,2'-Azanediylbis(1-(6-fluorochroman-2-yl)ethanol)
    OR
    1-(6-Fluoro-3,4-dihydro-2H-1-benzopyran-2-yl)-2-{[2-(6-fluoro-3,4-dihydro-2H-1-benzopyran-2-yl)-2-hydroxyethyl]amino}ethan-1-ol
CAS Number
  • 118457-14-0 [No]

PubChem CID
  • 71301

IUPHAR/BPS
  • 7246

DrugBank
  • DB04861 [Yes]

ChemSpider
  • 64421 [Yes]

UNII
  • 030Y90569U

KEGG
  • D05127 [Yes]

ChEMBL
  • CHEMBL434394 [Yes]

Chemical and physical data
Formula C22H25F2NO4
Molar mass 405.435 g/mol
3D model (JSmol)
  • Interactive image

SMILES[hide]
  • Fc4cc1c(OC(CC1)C(O)CNCC(O)C3Oc2ccc(F)cc2CC3)cc4
InChI[hide]
  • InChI=1S/C22H25F2NO4/c23-15-3-7-19-13(9-15)1-5-21(28-19)17(26)11-25-12-18(27)22-6-2-14-10-16(24)4-8-20(14)29-22/h3-4,7-10,17-18,21-22,25-27H,1-2,5-6,11-12H2
  • Key:KOHIRBRYDXPAMZ-UHFFFAOYSA-N

 

β1-selectivity[

 

 

Beta blockers help patients with cardiovascular disease by blocking β receptors, while many of the side-effects of these medications are caused by their blockade of β2 receptors.[2] For this reason, beta blockers that selectively block β1 adrenergic receptors (termed cardioselective or β1-selective beta blockers) produce fewer adverse effects (for instance, bronchoconstriction) than those drugs that non-selectively block both β1 and β2 receptors.

 

In a laboratory experiment conducted on biopsied heart tissue, nebivolol proved to be the most β1-selective of the β-blockers tested, being approximately 3.5 times more β1-selective thanbisoprolol.[3] However, the drug's receptor selectivity in humans is more complex and depends on the drug dose and the genetic profile of the patient taking the medication.[4] The drug is highly cardioselective at 5 mg.[5] In addition, at doses above 10 mg, nebivolol loses its cardioselectivity and blocks both β1 and β2 receptors.[4] (While the recommended starting dose of nebivolol is 5 mg, sufficient control of blood pressure may require doses up to 40 mg).[4] Furthermore, 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.[4] As many as 1 in 10 whites and even more blacks are poor CYP2D6 metabolizers and therefore might benefit less from nebivolol's cardioselectivity although currently there are no directly comparable studies.[citation needed]

Vasodilator action[

 

Nebivolol is unique as a beta-blocker.[6] Unlike carvedilol, it has a nitric oxide (NO)-potentiating, vasodilatory effect via stimulation of β3 receptors.[7][8][9] Along with labetalol, celiprololand carvedilol, it is one of four beta blockers to cause 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 preservation of cardiac output.[10] The net hemodynamic effect of nebivolol is the result of a balance between the depressant effects of beta-blockade and an action that maintains cardiac output.[11] Antihypertensive responses were significantly higher with nebivolol than with placebo in trials enrolling patient groups considered representative of the U.S. hypertensive population, in Black patients, and in those receiving concurrent treatment with other antihypertensive drugs.

 

Pharmacology of side-effects

 

Several studies have suggested that nebivolol has reduced typical beta-blocker-related side effects, such as fatigue, clinical depression, bradycardia, or impotence.[13][14][15] However, according to the FDA[16]

“ Bystolic is associated with a number of serious risks. Bystolic is contraindicated in patients with severe bradycardia, heart block greater than first degree, cardiogenic shock, decompensated cardiac failure, sick sinus syndrome (unless a permanent pacemaker is in place), severe hepatic impairment (Child-Pugh > B) and in patients who are hypersensitive to any component of the product. Bystolic therapy is also associated with warnings regarding abrupt cessation of therapy, cardiac failure, angina and acute myocardial infarction, bronchospastic diseases, anesthesia and major surgery, diabetes and hypoglycemia, thyrotoxicosis, peripheral vascular disease, non-dihydropyridine calcium channel blockers use, as well as precautions regarding use with CYP2D6 inhibitors, impaired renal and hepatic function, and anaphylactic reactions. Finally, Bystolic is associated with other risks as described in the Adverse Reactions section of its PI. For example, a number of treatment-emergent adverse events with an incidence greater than or equal to 1 percent in Bystolic-treated patients and at a higher frequency than placebo-treated patients were identified in clinical studies, including headache, fatigue, and dizziness. ”

 

FDA warning letter about advertising claims

 

In late August 2008, the FDA issued a Warning Letter to Forest Laboratories citing exaggerated and misleading claims in their launch journal ad, in particular over claims of superiority and novelty of action.

 

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