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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
Metipranolol is a β- adrenergic antagonist effective for both β1- and β2- receptors that has antiarrhythmic, antihypertensive, and antiglaucoma properties. Metipranolol is indicated in the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma. According to some sources, it is also used as an antihypertensive and anti-arrhythmia drug. Metipranolol is used in eye drops as metipranolol hydrochloride (CAS number 36592-77-5, EC number not available, molecular formula C17H28C1NO4) (1).
Drug Combinations
Published in Josef Hladovec, Antithrombotic Drugs in Thrombosis Models, 2020
Prenylamine combinations (minus the interactions with heparin, ASA, dipyridamole, and sulfinpyrazone which were mentioned previously) showed no marked interaction with troxerutin, at least with lower doses (Figure 36) in the arterial model and some synergism in the venous model. No interaction was recorded in the arterial model and a marked synergism in the venous model with pentoxifylline (Figure 37). A tendency to an antagonistic interaction was seen with metipranolol in both the arterial and venous models (Figure 38). An antagonism predominated with ketanserin, particularly with high doses, in the arterial model and a pronounced synergism in the venous model (Figure 39).
Immunomodulatory properties of antihypertensive drugs and digitalis glycosides
Published in Expert Review of Cardiovascular Therapy, 2022
Paweł Bryniarski, Katarzyna Nazimek, Janusz Marcinkiewicz
Indications for the use of beta blockers are as follows: hypertension, ischemic heart disease, supraventricular arrhythmias associated with increased excitability, ventricular arrhythmias, sinus tachycardia, hyperthyroidism (propranolol), glaucoma (reduce intraocular pressure: carteolol, metipranolol, timolol), headache including migraines, alcohol abstinence (relief of psychosomatic symptoms), anxiety neurosis. Contraindications for beta-blockers are sinus bradycardia, second degree atrioventricular block and third degree atrioventricular block, cardiogenic shock, severe peripheral circulatory disorders, decompensated bronchial asthma, chronic obstructive pulmonary disease or other chronic lung diseases, and Prinzmetal’s angina. Beta-blockers have many side effects, the most common of which are as follows: bradycardia, circulatory failure, atrioventricular block, hypotension, cold hands and feet, blurred vision, hallucinations, unusual dreams, memory problems, nausea, vomiting, abdominal pain, diarrhea or constipation, exacerbation or provocation of a bronchial asthma attack, and transient impotence.
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].
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
Metipranolol is a nonselective β-blocker without ISA [35]. It has been reported to exert some corneal anesthetic effect. Metipranolol is available in 0.1, 0.3 and 0.6% solutions (OptiPranolol®, Beta-ophtiole®) and should be administered twice daily. The IOP drop ranges between 25 and 33% after metipranolol 0.3%-0.6% administration [36]. Metipranolol causes more stinging and burning than timolol for a short period of time. It can induce mild conjunctival hyperemia, similar to levobunolol. As some studies found a slight reduction in pulse rate and systolic blood pressure, metipranolol should be avoided in patients with cardiovascular or pulmonary diseases [36].