betaxolol betaxolol betaxolol is a selective beta1 receptor blocker used in the treatment of hypertension and angina. 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. betaxololclinical datatrade nameskerloneahfs/drugs.commonographmedlineplusa609023pregnancycategory au: c routes ofadministrationby mouth, ocularatc codec07ab05 (who) s01ed02 (who)legal statuslegal status in general: ℞ (prescription only) pharmacokinetic databioavailability89%metabolismliverelimination half-life14–22 hoursexcretionkidney (20%)identifiers iupac name (rs)-1--3-(isopropylamino)propan-2-ol cas number63659-18-7 ypubchem cid2369iuphar/bps549drugbankdb00195 ychemspider2279 yuniio0zr1r6rz2keggd07526 ychebichebi:3082 ychemblchembl423 ycomptox dashboard (epa)dtxsid2022674 echa infocard100.113.058 chemical and physical dataformulac18h29no3molar mass307.434 g·mol−13d model (jsmol)interactive imagechiralityracemic mixture smiles o(ccc1ccc(occ(o)cnc(c)c)cc1)cc2cc2 inchi inchi=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 ykey:nwiutzdmdhavtp-uhfffaoysa-n y (verify) it was patented in 1975 and approved for medical use in 1983. medical uses hypertension betaxolol is most commonly ingested orally alone or with other medications for the management of essential hypertension. it is a cardioselective beta blocker, targeting beta-1 adrenergic receptors found in the cardiac muscle. blood pressure is decreased by the mechanism of blood vessels relaxing and improving the flow of blood. glaucoma ophthalmic betaxolol is an available treatment for primary open angle glaucoma (poag) and optical hypertension. betaxolol effectively prevents the increase of intracellular calcium, which leads to increased production of the aqueous humor. in the context of open angle glaucoma, increased aqueous humor produced by ciliary bodies increases intraocular pressure, causing degeneration of retinal ganglion cells and the optic nerve. furthermore, betaxolol is additionally able to protect retinal neurones following topical application from excitotoxicity or ischemia-reperfusion, providing a neuroprotective effect. this is thought to be attributed to its capacity to attenuate neuronal calcium and sodium influx. contraindications hypersensitivity to the drug patients with sinus bradycardia, heart block greater than first degree, cardiogenic shock, and overt cardiac failure side effects the adverse side-effects of betaxolol can be categorized into local and systemic effects. the local effects include: transient irritation (20-40% of patients) burning pruritus, or general itching punctate keratitis blurry vision systemically, patients taking betaxolol might experience: bradycardia hypotension fatigue sexual impotence hair loss confusion headache dizziness bronchospasm at higher doses cardiac problems such as arrhythmia, bundle branch block, myocardial infarction, sinus arrest, and congestive heart failure mental effects such as depression, disorientation, vertigo, sleepwalking, rhinitis dysuria metabolic side effects such as an increase in ldl cholesterol levels can mask the symptoms of hypoglycemia diabetic patients