“Betaxolol”的意思、由来-开放百科全书

词条

Betaxolol

释义

Medical uses
Contraindications
Side effects
History
Brand names
See also
References
External links

{{one source|date=August 2017}}{{Drugbox
| verifiedrevid = 459977756
| IUPAC_name = (RS)-14-[2-(cyclopropylmethoxy)ethyl]-
phenoxy3-(isopropylamino)propan-2-ol
| image = Betaxolol structure.svg
| width = 300
| chirality = Racemic mixture
| image2 = Betaxolol ball-and-stick.png
| tradename = Kerlone
| Drugs.com = {{drugs.com|monograph|betaxolol-hydrochloride}}
| MedlinePlus = a609023
| pregnancy_AU = C
| pregnancy_US = C
| pregnancy_category =
| legal_status = Rx-only
| routes_of_administration = oral, ocular
| bioavailability = 89%
| metabolism = Liver
| elimination_half-life = 14–22 hours
| excretion = Kidney (20%)
| CAS_number_Ref = {{cascite|correct|??}}
| CAS_number = 63659-18-7
| ATC_prefix = C07
| ATC_suffix = AB05
| ATC_supplemental = {{ATC|S01|ED02}}
| PubChem = 2369
| IUPHAR_ligand = 549
| DrugBank_Ref = {{drugbankcite|correct|drugbank}}
| DrugBank = DB00195
| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}}
| ChemSpiderID = 2279
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = O0ZR1R6RZ2
| KEGG_Ref = {{keggcite|correct|kegg}}
| KEGG = D07526
| ChEBI_Ref = {{ebicite|correct|EBI}}
| ChEBI = 3082
| ChEMBL_Ref = {{ebicite|correct|EBI}}
| ChEMBL = 423
| C=18 | H=29 | N=1 | O=3
| molecular_weight = 307.428 g/mol
| SMILES = O(CCc1ccc(OCC(O)CNC(C)C)cc1)CC2CC2
| StdInChI_Ref = {{stdinchicite|correct|chemspider}}
| StdInChI = 1S/C18H29NO3/c1-14(2)19-11-17(20)13-22-18-7-5-15(6-8-18)9-10-21-12-16-3-4-16/h5-8,14,16-17,19-20H,3-4,9-13H2,1-2H3
| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}}
| StdInChIKey = NWIUTZDMDHAVTP-UHFFFAOYSA-N
}}

Betaxolol is a selective beta₁ receptor blocker used in the treatment of hypertension and glaucoma.^[1] Being selective for beta₁ receptors, it typically has fewer systemic side effects than non-selective beta-blockers, for example, not causing bronchospasm (mediated by beta₂ receptors) as timolol may. Betaxolol also shows greater affinity for beta₁ receptors than metoprolol. In addition to its effect on the heart, betaxolol reduces the pressure within the eye (intraocular pressure). This effect is thought to be caused by reducing the production of the liquid (which is called the aqueous humor) within the eye. The precise mechanism of this effect is not known. The reduction in intraocular pressure reduces the risk of damage to the optic nerve and loss of vision in patients with elevated intraocular pressure due to glaucoma.

It was patented in 1975 and approved for medical use in 1983.^[2]

Medical uses

Oral: for the management of hypertension
Ophthalmic: for the management of glaucoma
the drug seems to have an effect of neuroprotection in glaucoma treatment

Contraindications

Hypersensitivity to the drug
Patients with sinus bradycardia, heart block greater than first degree, cardiogenic shock, and overt cardiac failure

Side effects

History

Betaxolol was approved by the U.S. Food and Drug Administration (FDA) for ocular use as a 0.5% solution (Betoptic) in 1985 and as a 0.25% solution (Betoptic S) in 1989.

Brand names

Brand names include Betoptic, Betoptic S, Lokren, Kerlone.

References

1. ^{{cite journal|last1=Buckley|first1=MM|last2=Goa|first2=KL|last3=Clissold|first3=SP|title=Ocular betaxolol. A review of its pharmacological properties, and therapeutic efficacy in glaucoma and ocular hypertension.|journal=Drugs|date=July 1990|volume=40|issue=1|pages=75–90|pmid=2202584|doi=10.2165/00003495-199040010-00005}}
2. ^{{cite book |last1=Fischer |first1=Jnos |last2=Ganellin |first2=C. Robin |title=Analogue-based Drug Discovery |date=2006 |publisher=John Wiley & Sons |isbn=9783527607495 |page=461 |url=https://books.google.ca/books?id=FjKfqkaKkAAC&pg=PA461 |language=en}}

External links

[https://web.archive.org/web/20071020131717/http://products.sanofi-aventis.us/kerlone/kerlone.pdf Kerlone prescribing information]

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