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Cardiovascular Drugs during Pregnancy
Published in “Bert” Bertis Britt Little, Drugs and Pregnancy, 2022
No human teratology or reproduction studies with betaxolol, carteolol, nadolol, penbutolol, or timolol have been published. No increase in congenital malformations was noted in the offspring of pregnant mice who received up to 150 mg/kg/day of carteolol (Tanaka et al., 1979). Only six infants were exposed to betaxolol during the first trimester in the Swedish Birth Defects Registry (Kallen, 2019). Also, no increase in the frequency of malformations was found among the offspring of rats, rabbits, and hamsters that had received nadolol in doses several times higher than the usual human dose (Sibley et al., 1978; Stevens et al., 1984). No increased frequency of adverse fetal effects was found in the offspring of mice treated with penbutolol (Sugisaki et al., 1981).
Betaxolol
Published in Anton C. de Groot, Monographs in Contact Allergy, 2021
Betaxolol is a racemic mixture and selective β1-adrenergic receptor antagonist with antihypertensive and anti- glaucoma activities, which is devoid of intrinsic sympathomimetic activity. The drug is used to treat hypertension, arrhythmias, coronary heart disease, glaucoma, and is also used to reduce non-fatal cardiac events in patients with heart failure. In pharmaceutical products, betaxolol is employed as betaxolol hydrochloride (CAS number 63659-19- 8, EC number 264-384-3, molecular formula C18H30ClNO3) (1).
Medical Therapy for Glaucoma
Published in Neil T. Choplin, Carlo E. Traverso, Atlas of Glaucoma, 2014
Jennifer E. Williamson, Janet B. Serle
Betaxolol (Figure 14.8) is the only commercially available topical β1 selective intraocular pressure-lowering medication. It is available as a 0.25% suspension (Betoptic-S) and a 0.5% solution. The suspension is more comfortable than the solution for most patients, but the two are equally efficacious. Both formulations lower intraocular pressure between 20% and 25% from baseline. This agent can be considered in patients with mild to moderate pulmonary disease without other contraindications to this class of compounds. All β-adrenoreceptor antagonists must be used with caution in any patient with a history of reactive airway disease. It is advisable to consult with a patient’s internist or pulmonologist prior to prescribing these agents in patients with pulmonary disease. Betaxolol has intrinsic calcium channel blocking activity, which may increase ocular blood flow. Additional investigations of this property and the potential clinical benefit need to be conducted.
Emerging drugs for the treatment of glaucoma: a review of phase II & III trials
Published in Expert Opinion on Emerging Drugs, 2022
Tyler M. Kaplan, Arthur J. Sit
Beta blockers reduce aqueous humor production by 20–50% through the reduction of intracellular cAMP in the ciliary epithelium [53,54]. Members of this class of medication include timolol, carteolol, levobunolol, and betaxolol, which reduce IOP by 20–25% except betaxolol which reduces IOP by 15–20% [11,55,56]. While beta blockers can cause conjunctival injection and blepharitis [3], they are generally very well tolerated in terms of local side effects. However, beta blockers are less effective at night [57], likely because aqueous production is reduced by approximately 50% at night [58,59]. They may also reduce outflow facility [60] and decrease ocular perfusion pressure [61] which can potentially worsen disease status. Further, they can cause systemic side effects including decreased cardiac output, decompensated heart failure, heart block, and bradycardia. Patients with asthma or chronic obstructive pulmonary disease (COPD) can develop respiratory side effects [3,6]. These systemic side effects are most frequently seen in nonselective beta blocker due to inhibition of beta-1 and beta-2 receptors, while betaxolol has a lower risk of pulmonary complications since it is more beta-1 selective [62].
Adrenergic agonists and antagonists as antiglaucoma agents: a literature and patent review (2013–2019)
Published in Expert Opinion on Therapeutic Patents, 2019
Alessio Nocentini, Claudiu T. Supuran
Betaxolol is a β1-selective adrenoceptor antagonist. It exerts the effect on IOP by inhibiting aqueous humor flow [28]. As the ciliary body hardly contains β1-adrenoceptors, it is likely that betaxolol lower IOP by its weak β2-blocking properties. As a result, the effect betaxolol 0.5% (Betoptic®) on IOP is smaller than timolol (18 to 26%) [29]. Nonetheless, betaxolol better preserves the visual field than timolol over the long term. Burning and stinging are frequently observed after topical administration. Clinical evidence showed that betaxolol has less effect on cardiac and pulmonary function than nonselective β-blockers. Unexpectedly, cardiovascular adverse effects such as bradycardia, arrhythmias, and congestive heart failure occur less frequently with betaxolol than with nonselective β-blockers probably because it strongly binds to plasma proteins reducing free plasma concentration [30].
Age-dependent sympathetic neural responses to ß1 selective beta-blockade in untreated hypertension-related tachycardia
Published in Blood Pressure, 2018
Dagmara Hering, Wiesława Kucharska, Marzena Chrostowska, Krzysztof Narkiewicz
Strengths of our study include the first clinical and pathophysiological evaluations of the effects of β1 highly cardioselective beta-blocker in untreated essential hypertension and tachycardia. The steady-state effects of betaxolol on sympathetic CV profile were determined in newly diagnosed younger and older males with essential hypertension and tachycardia confirmed by ambulatory BP and HR monitoring, none of whom had ever been treated with antihypertensive medication, thereby eliminating potential confounding effects on HR, BP, MSNA and HRV. The specific pharmacokinetics properties of betaxolol and findings derived from this study appear to be of clinical relevance. However, the long-term CV outcomes associated with betaxolol warrants further studies.