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Monographs of Topical Drugs that Have Caused Contact Allergy/Allergic Contact Dermatitis
Published in Anton C. de Groot, Monographs in Contact Allergy, 2021
Levobunolol, the L-isomer of bunolol, is a naphthalenone and non-cardioselective β-adrenergic receptor antagonist with anti-glaucoma activity. Upon administration in the eye, this agent blocks β-adrenergic receptors, thereby causing vasoconstriction. Levobunolol also decreases the ciliary body’s production of aqueous humor, which, in turn, results in a lower intraocular pressure. Levobunolol is indicated for lowering intraocular pressure in patients with chronic open-angle glaucoma or ocular hypertension. In pharmaceutical products, levobunolol is employed as levobunolol hydrochloride (CAS number 27912-14-7, EC number 248-725-3, molecular formula C17H26C1NO3) (1).
Adrenergic Antagonists
Published in Sahab Uddin, Rashid Mamunur, Advances in Neuropharmacology, 2020
Levobunolol is an adrenergic β receptor non-selective antagonist. After administration it changes to a metabolite, dihydrobunolol (DHB) with same potency as levobunolol (Di et al., 1977; Mayama et al., 2013). In the retina and choroid, the diffusion of DHB is less because of its polarity and possesses a decreased risk for vasoconstriction (Acheampong et al., 1995; Dong et al., 2007; Mayama et al., 2013). There is no major variation in the blood flow parameters following an administration of a single dose of levobunolol. The rate of blood flow in the retinal vein increase slightly and in retrobulbar arteries, blood flow was unchanged (Altan-Yaycioglu et al., 2001; Bloom et al., 1997; Leung et al., 1997; Mayama et al., 2013; Schmetterer et al., 1997). Several studies report an increase in pulsatile ocular blood flow following a single drop of levobunolol 0.5% or with levobunolol treatment daily twice for a week (Bosem et al., 1992; Mayama et al., 2013; Morsman et al., 1995).
Local Anesthetics and Anesthetic Solutions: Classification, Mode of Action and Dosages
Published in Marwali Harahap, Adel R. Abadir, Anesthesia and Analgesia in Dermatologic Surgery, 2019
A large number of drugs may interfere with local anesthetics, although to a variable degree. In these cases, the physician may have to change the dose, or other precautions may be necessary. A drug history is therefore mandatory. β-Adrenergic blocking agents [carteolol, e.g., Cartrol; carvedilol, e.g., Coreg; labetolol, e.g., Normodyne; nadolol, e.g., Corgard; oxprenolol, e.g., Trasicor; penbutolol, e.g., Levatol; pindolol, e.g., Visken; propranolol, e.g., Inderal; sotalol, e.g., Sotacor; timolol, e.g., Blocadren; or Carteolol (ophthalmic), e.g., Ocupress; Levobunolol (ophthalmic), e.g., Betagan; Metipranolol (ophthalmic), e.g., OptiPranolol; or Timolol (ophthalmic), e.g., Timoptic.]
The prophylactic effect of betaxolol 0.5% versus brimonidine 0.2% on IOP elevation after Nd:YAG laser posterior capsulotomy
Published in Clinical and Experimental Optometry, 2022
Navid Elmi Sadr, Elnaz Saber, Fatemeh Paknazar
Studies have shown that IOP begins to increase just after laser application and reaches a peak after 3–4 hours.3–6,12,15,20 However, this acute rise of IOP is transient but can be vision-threatening in some patients. Brimonidine 0.2% and apraclonidine 0.5% have become the drugs of choice for prophylaxis of IOP elevation after laser application.8,9 Brimonidine tartrate is a selective α2-adrenergic agonist which lowers IOP by decreasing aqueous production and increasing uveoscleral outflow.23 Ocular allergic reactions, central nervous system depression, dry mouth, and granulomatous anterior uveitis are the reported side effects of brimonidine.12,13,24 So, as there are limitations to the use of brimonidine in all patients, numerous studies have been performed to compare the effectiveness of other anti-glaucoma medications with brimonidine 0.2% and with each other to prevent acute IOP rise following Nd:YAG laser posterior capsulotomy. Brimonidine purite 0.15%, bimatoprost 0.03%, levobunolol 0.5%, timolol 0.5%, pilocarpin, dorzolamide 2% and oral acetazolamide have been studied.12–20
Common systemic medications that every optometrist should know
Published in Clinical and Experimental Optometry, 2022
Analgesics are generally well tolerated and may be used for chronic pain relief without adverse effects to the eyes. On rare occasion, use of ibuprofen has shown ocular toxicity with blurred vision,81,82 visual field defects,82–84 diplopia,85 and toxic amblyopia.86 Most cases reported improvement in visual symptoms after discontinuation of ibuprofen. Among the rare reported side effects of ibuprofen use is glaucoma progression, although the evidence has not shown a definitive causal link. In fact, ibuprofen may have beneficial IOP lowering effects. A pilot clinical study compared the IOP lowering effects of oral paracetamol with topical levobunolol over two weeks, concluding that the oral analgesic taken every six hours has a similar IOP reduction to that of the topical beta blocker.87 Additional studies are needed to determine the effects analgesics have on glaucoma progression. Furthermore, IOP should be monitored regularly in patients with glaucoma, and optometrists should be made aware of any changes to the patient’s medical and medication history.
Advances in the discovery of novel agents for the treatment of glaucoma
Published in Expert Opinion on Drug Discovery, 2021
Francesco Mincione, Alessio Nocentini, Claudiu T. Supuran
The nonselective β-blockers inhibit both β1- and β2-ARs, and they include timolol 6, levobunolol 8, carteolol 9 and metipranolol 10, whereas betaxolol 7 is a β1-selective antagonist [13]. Timolol is available in 0.1, 0.25 and 0.5% eye drops solutions which must be applied twice daily for effectively reducing IOP or once daily in gel formulation [27]. It shows relatively few ocular adverse effects (e.g. hyperemia, stinging and burning sensation of the eye, as well as superficial punctate keratitis), but as all β-blockers, severe systemic cardiac adverse effects may occur [27]. Betaxolol 7 is less effective than timolol as an IOP lowering agent, probably due to its selective binding to the β1- adrenoceptors, but it also has some effects on the β2 receptors which probably explain its pharmacologic effects as anti-glaucoma agent, and the fact that it better preserves visual field after long-term use [27,29]. Levobunolol 8 has similar ocular hypotensive effects as timolol (IOP reduction up to 27%), and a similar side effects profile to 6 [27]. Carteolol 9 is used as 1 and 2% eye drops solutions, being applied twice daily. Its side effects are quite similar to those of the other drugs belonging to this class [27]. Metipranolol 10, apart of being a nonselective β-blocker, has also been reported to exert some corneal anesthetic effects [32]. Its efficacy as well as ocular and systemic side effects are rather similar to those of timolol [27].