Disease relevance of Thymoxamine

• Time course of thymoxamine reversal of phenylephrine-induced mydriasis [1].
• Thymoxamine test. Differentiating angle-closure glaucoma form open-angle glaucoma with narrow angles [2].
• Thymoxamine does not contract the ciliary muscle and does not alter the IOP or facility of outflow in open-angle glaucoma, but it can relieve angle-closure glaucoma [2].
• Thymoxamine resulted in a full in systemic resistance together with a rise in cardiac index without reflex tachycardia [3].
• Intraocular thymoxamine for miosis during surgery [4].

Psychiatry related information on Thymoxamine

• We assessed the efficiency and tolerance of the alpha-blocking agent moxisylyte in 2 double-blind studies versus placebo performed in 12 neurogenic patients with spinal cord lesions and in 61 patients presenting with either psychogenic impotence (30) or erectile dysfunction that was predominantly neither psychogenic, hormonal nor neurogenic (31) [5].
• To explore the role of alpha-1-adrenoreceptor-mediated pathways on human upper gut motor function in vivo, we studied the effects of the alpha-1-agonist phenylephrine and the alpha-1-antagonist thymoxamine on oro-caecal transit and antroduodenal motor activity [6].
• 1 An alpha-adrenergic receptor blocking agent, thymoxamine (150 mg i.v.) in the early night sleep of young adults increased REM sleep duration and also brief awakenings in the early night, while slow wave sleep, stage 3+4, was diminished [7].
• Thymoxamine HCl (10 mg/kg IP), a specific alpha-adrenergic receptor blocker, depressed self-stimulation at all sites, but significantly more severely at DA sites [8].

High impact information on Thymoxamine

• The plasma gastrin response to a meal was moderately enhanced by thymoxamine and markedly enhanced by atropine [9].
• Dose-related effect of moxisylyte on maximal urethral closing pressure in patients with spinal cord injuries [10].
• To examine this possibility we measured serum LH, FSH, and PRL concentrations at 10-min intervals and total testosterone and 17 beta-estradiol at 60-min intervals for 8 h basally and during the infusion of the alpha 1-adrenoceptor antagonist thymoxamine (10 micrograms/kg X min) in 10 young women with PCO [11].
• A significant inhibition of postexercise bronchoconstriction was observed in 12 of 13 patients following thymoxamine or cromolyn sodium inhalation [12].
• No statistically significant difference was found in the rate of aqueous humor formation, intraocular pressure, anterior chamber volume, or premeability of the blood-aqueous barrier between thymoxamine-treated and placebo-treated eyes [13].

Chemical compound and disease context of Thymoxamine

• PURPOSE: We compared the efficacy and safety of alprostadil alpha-cyclodextrin and moxisylyte chlorhydrate to induce erections adequate for sexual intercourse in a prospective, randomized, parallel double-blind study in patients with erectile dysfunction [14].
• Evaluation of the effect of thymoxamine solution 0.5% on mydriasis induced by ibopamine solution 1% [15].
• Reversal of tropicamide-induced mydriasis by thymoxamine eye drops [16].
• The effects of thymoxamine 0.5% solution and of a placebo solution (mannitol) on the mydriasis induced by ibopamine 1% solution were evaluated in 8 healthy volunteers and 12 patients with eye diseases [15].
• Intraocular thymoxamine or acetylcholine for the reversal of mydriasis [17].

Biological context of Thymoxamine

• Investigators assessed erections after alprostadil alpha-cyclodextrin to be adequate for sexual intercourse in 61 patients (81%) compared to 37 patients (46%) after moxisylyte chlorhydrate [14].
• Pharmacokinetics of moxisylyte in healthy volunteers after intravenous and intracavernous administration [18].
• Plasma levels of moxisylyte and its biotransformation products were assayed by a specific high-performance liquid chromatography method with fluorescence detection [18].
• METHODS: The hydrolytic activity of HSA and its inhibition by physostigmine were measured fluorimetrically by monitoring the hydrolysis of the ester substrate moxisylyte [19].
• Control experiments demonstrated that thymoxamine (i.v.) was without effect on blood pressure [7].

Anatomical context of Thymoxamine

• Thymoxamine-treated eyes had 12% greater aqueous humor flow than placebo-treated eyes, but this difference was not statistically significant [13].
• The lack of an effect on the aqueous system could be interpreted as being a result of too low a concentration of thymoxamine in the ciliary body, lack of blockable receptors in the ciliary body, lack of physiologic tone in a blockable receptor system, or lack of a role of such a receptor system in the formation of aqueous humor [13].
• The alpha adrenoceptor antagonists, thymoxamine, piperoxan and yohimbine, antagonized the inhibitory effects of alpha-MNA in spontaneously-active preganglionic neurones and neurones activated by visceral afferents [20].
• Seven drugs that are known to relax smooth muscle (phenoxybenzamine, phentolamine, thymoxamine, imipramine, verapamil, papaverine, naftidrofuryl) caused erection when injected intracavernosally [21].
• The purpose of this study was to investigate whether the alpha 1-adrenoceptor antagonist thymoxamine possesses antihistaminic activity in clinical doses in man, as has been reported on the guinea pig ileum in vitro [22].

Associations of Thymoxamine with other chemical compounds

• The non-selective alpha adrenoceptor antagonists phentolamine (10(-5) M) and thymoxamine (10(-5) M) and the alpha 1 adrenoceptor antagonist prazosin (10(-5) M) partially blocked the response to noradrenaline, while the alpha 2 adrenoceptor antagonist idazoxan (10(-5) M) and timolol (10(-5) M) had no effect [23].
• Post-micturition residual volumes and clinical symptoms of 49 patients with MSA were evaluated at trial entry and after 4 weeks (prazosin; n=21 and moxisylyte; n=28) [24].
• Five normal subjects were given on three separate occasions intravenous infusions of thymoxamine (0.15 mg kg-1 loading dose followed by 0.15 mg kg-1 h-1), chlorpheniramine (1.5 mg loading dose followed by 1.5 mg h-1) and normal saline (placebo) [22].
• 6. alpha-Adrenoceptor blockade with thymoxamine (0.3 mg kg-1 bolus + 0.3 mg kg-1 h-1 infusion), singly and combined with intravenous propranolol (10 mg i.v. over 10 min), did not alter the pressor or tachycardic effects of 500 micrograms TRH [25].
• Six normal males were given continuous 3 h i.v. infusions of normal saline, methoxamine (alpha-1 adrenoceptor agonist) and thymoxamine (alpha-1 adrenoceptor antagonist) [26].

Gene context of Thymoxamine

• In in vitro studies with human and rabbit corpus cavernosum strips in organ chambers, the alpha-adrenergic receptor antagonists (alpha-ARAs) moxisylyte and yohimbine and their corresponding nitrosylated compounds, SNO-moxisylyte (NMI-221) and SNO-yohimbine (NMI-187), concentration-dependently relaxed endothelin-induced contraction [27].
• Normal values were those of the International Continence Society. Alpha blocker test was done by intravenous injection of thymoxamine (0.5 mg/kg) and was considered as positive if urethral closure pressure (UCP) decrease was greater than 30% after 10 minutes [28].
• Thymoxamine, a prodrug, is rapidly deacetylated in the plasma to give two phase I metabolites, DMAT and DAT, which are further sulpho- and glucuro-conjugated and then excreted mainly in the urine [29].

Analytical, diagnostic and therapeutic context of Thymoxamine

• Determination of metabolites of thymoxamine in plasma by high performance liquid chromatography [30].
• Effect of thymoxamine on aqueous humor formation in the normal human eye as measured by fluorophotometry [13].
• Intra-ocular pressure was measured before and after the topical administration of an alpha-receptor blocking agent, thymoxamine [31].
• Multiple-dose pharmacokinetics of moxisylyte after oral administration to healthy volunteers [32].
• Moxisylyte was assayed in plasma and urine by a specific HPLC method with fluorimetric detection [32].

References