Disease relevance of Metipranolol

• Metipranolol is a non-selective beta-adrenoceptor blocking agent used for the topical treatment of elevated intraocular pressure in patients with chronic open angle glaucoma or ocular hypertension [1].
• Ocular metipranolol. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in glaucoma and ocular hypertension [1].
• CONCLUSIONS: The combined data suggest that oxidative injury to RPE cells and photoreceptors may be caused by elevated levels of zinc in diseases such as age-related macular degeneration (AMD) and that metipranolol may act as an efficacious antioxidant to blunt this process [2].
• Cidofovir, pamidronic acid, sulfonamides, rifabutin and topical metipranolol can 'probably' cause uveitis [3].
• The rats treated with metipranolol 1 and 4 hr before hypoxia produced significantly less erythropoietin in response to hypoxia than saline-treated control animals [4].

Psychiatry related information on Metipranolol

• The lack of psychotropic effects for metipranolol and propranolol as compared to bunitrolol cannot be predicted from pharmacokinetic properties or peripheral effects of the three drugs, arguing for the need for systematic screening using psychometric and psychophysiological methods of current and new beta-blocking drugs [5].
• Effects of beta-blocking agent Metipranolol on metabolic variables in patients with ischemic heart disease, hyperkinetic syndrome, hyperthyreosis and in healthy subjects [6].

High impact information on Metipranolol

• Each treatment significantly decreased the intraocular pressure: metipranolol 3.6 +/- 0.4 mm Hg (P less than 0.001), timolol 2.44 +/- 0.4 mm Hg (P less than 0.01), and carteolol 2.38 +/- 0.48 mm Hg (P less than 0.01) compared with placebo [7].
• Immunohistochemistry, immunoblot analysis and the terminal-deoxynucleotidyl transferase dUTP-linked nick-end labeling (TUNEL) procedure determined the effects of zinc with or without trolox or metipranolol on photoreceptor death in situ [2].
• Zinc-induced apoptosis of cultured RPE cells and photoreceptors were attenuated only by metipranolol and trolox [2].
• Thus, ocular metipranolol provides a viable alternative to ocular timolol and levobunolol in the topical treatment of chronic open angle glaucoma or ocular hypertension [1].
• The effect on erythropoietin production: in rats metipranolol or dl-propranolol was injected daily in a single dose of 10 mg/kg b.wt [4].

Chemical compound and disease context of Metipranolol

• Timolol 0.25% significantly reduced exercise tachycardia (P less than 0.05), an effect which was not shown by metipranolol 0.1 or 0.3% [8].
• 4. Topical metipranolol, 0.3% and 0.6%, blocked both the hypotension (beta2-mediated) and the tachycardia (beta1-mediated) elicited in ganglion-blocked, conscious rabbits by isoproterenol, 0.5 microgram/kg, i.v. The Ki for displacement of 3H-dihydroalprenolol binding to rabbit iris + ciliary body homogenates was 34 nM [9].
• The disposition kinetics and heart rate reducing effect of deacetylmetipranolol (DMP), the active form of the beta-adrenoreceptor blocking agent metipranolol (MP), administered as a single 40 mg oral dose have been compared in 6 patients with cirrhosis and 6 healthy volunteers [10].

Biological context of Metipranolol

• Metipranolol blunts nitric oxide-induced lipid peroxidation and death of retinal photoreceptors: a comparison with other anti-glaucoma drugs [11].
• The beta-adrenergic receptor antagonist metipranolol blunts zinc-induced photoreceptor and RPE apoptosis [2].
• The effect on erythrocyte production: in rats treated daily with metipranolol in a single dose of 10 mg/kg b.wt., for a period of 10 days, the rate of erythropoiesis measured by the incorporation of 59Fe into red blood cells was decreased, dl-propranolol (10 mg/kg b.wt.) did not reduce the rate of erythropoiesis [4].
• 2. A significant and equal decrease in blood pressure was achieved both with trimepranol and chlorthalidone, whereas their combination was significantly more effective [12].
• 3. BM 12.434 increased the peripheral resistance less than metipranolol [13].

Anatomical context of Metipranolol

• Determination of metipranolol and desacetylmetipranolol in aqueous humor of rabbit eye by gas chromatography with electron-capture detection [14].
• Administration of Trimepranol to IHA-exposed rats significantly decreased the values of right ventricular systolic and mean pressure, right ventricular hypertrophy as well as the degree of muscularization of pulmonary arteries [15].
• Inhibition of neutrophil chemotaxis and free radical production is a novel mode of action of metipranolol and timolol that may be relevant for beneficial effects in the topical treatment of eye disease [16].
• Investigation of one functional parameter--the ability to produce hematopoietic colonies in the spleen after transplantation of the bone marrow irradiated in vitro by microwaves--indicated the possibility of affecting stimulatory and inhibitory effects of microwaves by using a blocker of cell receptors, Trimepranol [17].
• Cardioprotective effect of metipranolol on ischemic heart muscle [18].

Associations of Metipranolol with other chemical compounds

• Effects of single oral doses of the beta-blocking drugs propranolol (40 mg) and metipranolol (Disorat, Boehringer, Mannheim, FRG, 5 and 20 mg), in comparison with placebo, on mental performance and psychophysiological measures were investigated in a double-blind crossover study comprising 12 healthy volunteers [5].
• Propranolol and metipranolol had no effects on mental performance, in contrast to findings in a previous study for bunitrolol (Stresson, Boehringer, Ingelheim, FRG) [5].
• With the approval of the District Ethics Committee 7 of those patients were rechallenged with metipranolol 0.3% compared to timolol maleate 0.5% in a double blind trial [19].
• In the atenolol subgroup, the blood pressure was reduced by 11 mm Hg, in the metipranolol subgroup by 15 mm Hg, and in the pindolol subgroup by 18 mm Hg [20].
• A HPLC method is presented for the identification and quantification in plasma and urine of beta-adrenergic receptor antagonists (betaxolol, carteolol, metipranolol, and timolol) commonly prescribed in ophthalmology [21].

Gene context of Metipranolol

• In addition, of the tested ophthalmic beta-blockers only metipranolol has powerful antioxidant properties [22].
• Inhibition of neutrophil migration and oxygen free radical release by metipranolol and timolol [16].

Analytical, diagnostic and therapeutic context of Metipranolol

• Determination of ophthalmic therapeutic metipranolol and its degradation product by reversed-phase high-performance liquid chromatography [23].
• CONCLUSIONS: This study shows that systemic as well as topical application of metipranolol leads to increased retinal blood flow velocities [24].
• The perfusion pressure increased after topical application and remained unchanged after systemic application of metipranolol [24].
• On the other hand, an i.v. injection of methypranol (Trimepranol Spofa) given prior to ligation increased the level of ventricular fibrillation threshold 3 to 4 times compared to control value before occlusion in all 10 studied dogs [25].
• Metipranolol (1 mg/kg) was given 30 min prior to inducing the ischemia of left rat kidney followed with a contralateral nephrectomy [26].

References