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At least 73 records · Page 4Linked to original sources
PubMed1994

Effect of topical administration of L-arginine on formalin-induced nociception in the mouse: a dual role of peripherally formed NO in pain modulation.

1. We investigated the effects of intraplantar (i.pl.) administration of L-arginine and NG-nitro-L-arginine methyl ester (L-NAME) on formalin-induced behavioural nociception in the mouse. 2. L- but not D-arginine, at 0.1-1 microgram per paw, coadministered with i.pl. formalin, enhanced the second-but not the first-phase nociceptive responses, whereas it was without significant effects at 3 micrograms per paw, and conversely, produced antinociception at 10 micrograms per paw, resulting in a bell-shaped dose-response curve. 3. L-NAME at 0.1-1 microgram per paw, when administered i.pl., exhibited antinociceptive activity in the second phase in a dose-dependent manner, although its D-enantiomer produced no effect. 4. An antinociceptive dose (1 microgram per paw) of L-NAME (i.pl.) considerably reduced the increase in second-phase nociception elicited by low doses (1 microgram per paw) of i.pl. L-arginine. The second-phase nociception decrease induced by a large dose (10 micrograms per paw) of i.pl. L-arginine was markedly reversed by i.pl. L-NAME at 0.1 micrograms per paw, raising it to a level above that of the control (formalin only). 5. These results suggest that peripheral NO plays a dual role in nociceptive modulation, depending on the tissue level, inducing either nociceptive or antinociceptive responses.

Administration, Topical↗
PubMed1980

Effects of systemic and topical administration of metoprolol on intraocular pressure in healthy subjects.

The effect of a single dose metoprolol tablets or eye drops on intraocular pressure (IOP), blood pressure and heart rate was determined in healthy volunteers. The ocular tolerance of 6 weeks treatment with 1% eye drops was also studied. A 100 mg tablet reduced IOP for least 10 h with a maximum effect after 4 h corresponding to 32% of the pre-treatment pressure. The effects of 25 and 50 mg tablets were less pronounced and of a shorter duration. No consistent effect on blood-pressure was obtained, but doses that reduced IOP also reduced heart rate. A short-lasting reduction in IOP was obtained with 0.5% eye drops, while 1, 3 and 5% all caused significant reductions lasting at least 10-12 h. IOP was reduced by 13, 20 and 27% 4 h after administration of 1, 3 and 5% eye drops, respectively. No effect was observed in the contralateral, untreated eye, and no cardiovascular effects were obtained after administration of the eye drops. 1% eye drops administered twice daily for 6 weeks caused no clinically significant side effect.

Administration, Oral↗
PubMed1985

Topical administration of 5-aminosalicylic acid enemas in patients with ulcerative colitis. Studies on rectal absorption and excretion.

5-aminosalicylic acid (5-ASA) is a new treatment for patients suffering from ulcerative colitis but only limited information is available about its rectal absorption. We therefore studied seven patients with ulcerative colitis in remission, and five with active disease to determine acetylated and free 5-ASA plasma concentrations and urinary acetyl 5-ASA after the administration of three different types of enemas: (2 g 5-ASA/100 ml, 4 g/100 ml, and 200 ml). In patients in remission urinary acetyl 5-ASA excretion was dose and volume dependent (p less than 0.01; p less than 0.05) but this correlation was absent in active disease. Because aminosalicylates are usually eliminated through the kidney, these low values (10% in active disease and 19% in those in remission) suggest that the beneficial action may be local. Urinary recovery was significantly lower in patients with active disease (p less than 0.01; p less than 0.02). No accumulation of 5-ASA was found in plasma after repeated daily administration.

Administration, Topical↗
PubMedDate not supplied

Ocular perfusion pressure and visual field indice modifications induced by alpha-agonist compound (clonidine 0.125%, apraclonidine 1.0% and brimonidine 0.2%) topical administration. An acute study on primary open-angle glaucoma patients.

OBJECTIVE: The aim of this study was to verify the acute effects of alpha-adrenoreceptor agonist eyedrop administration on visual field parameters and ocular perfusion pressure (OPP) in patients affected by primary open-angle glaucoma. METHODS: A prospective, randomized double-blind study was carried out. Sixty-four glaucomatous subjects were enrolled in the clinical trial and subsequently separated into four study groups, of 16 patients each, to compare the systemic and ocular effects of placebo, clonidine 0.125%, apraclonidine 1.0% and brimonidine 0.2%. RESULTS: No significant variations in the ocular or systemic parameters were observed after placebo administration. All the alpha-adrenoreceptor agonist compounds induced a significant reduction of the intraocular pressure. Clonidine induced significant modifications of mean blood pressure, OPP and visual field indices. The acute administration of apraclonidine did not affect both mean blood pressure and OPP, but a worsening of the visual field was nevertheless recorded. The analyzed parameters did not significantly vary after brimonidine instillation. CONCLUSIONS: The present findings demonstrate that the lack of effects on the blood flow and the absence of vasomotor activity at the level of the posterior pole exhibited by brimonidine is related to its alpha-2 selectivity, as appears by comparing this compound with the other alpha-agonists available for the management of glaucoma.

Administration, Topical↗
PubMed1991

Topical administration of leukotriene antagonists in immunogenic keratitis.

Antagonists of leukotriene D4 (LTD4), 3-[7-(2-n-propyl-3-hydroxy-4-acetyl- phenoxy)-propoxy-2-methyl-3,4-dihydro-4-8-n-propyl-2H-1-benzopyran- 2-yl]-propionic acid (SC-39070) and 7-[3-(4-acetyl-3-hydroxy-2-propylphenoxy)-2-hydroxy- propoxy]-4-methyl- 2-oxo-2H-1-benzopyran-3-acetic acid (FPL-60319) were locally administered to eyes of rabbits with immunogenic keratitis. The period of circular leukocyte infiltration (Wessely's ring) in the cornea was markedly decreased. Edema and neovascularization of the cornea were not influenced.

Administration, Topical↗
PubMedDate not supplied

[Topical administration of hydralazine hydrochloride on the viability of randon skin flaps in rats].

PURPOSE: Assess the effect of hydralazine hydrochloride, for iontophoresis, on the viability of random skin flaps in rats. METHODS: Sixty Wistar rats was randonly destributed in 4 groups (n=15), these animals was submited as randon dorsal skin flaps as cranial base with measure 10 x 4 cm. The animals from group 1 was utilized as control, in group 2 was submitted to direct current o 4mA-20' immediately after the surgery and on the two subsequent days. In group 3 the stimulation eletric simulation with hydralazine hydrochloride. In group 4 iontophorese with hydralazine hydrochloride 4mA-20'. The analysis of the results was made on the seventh day post operative and interpreted with test non parametric of Kruskal-Wallis. RESULTS: and the necrotic area stayed fixed in: group 1=45%; group 2=39%; group 3=46% and group 4=41%, being the statistical analysis did not evidenced any significant. CONCLUSION: The hydralazine hydrochloride when taken for iontophorese was not efficacious in reduce the necrotic area.

Administration, Topical↗
PubMed1986

Distribution of a steroid antagonist in the eye following topical administration.

The distribution of a steroid antagonist, RU486, that is known to reduce rabbit intraocular pressure has been examined in the eye. On an equal tissue weight basis, the corneal epithelium is the site of maximal absorption followed by conjunctival tissues (bulbar and palpebral) and the rest of the cornea. Aqueous humor concentrations of drug vary between 5 X 10(-6) and 5 X 10(-8) at 1 and 24 hours, respectively: these concentrations have been shown by others to inhibit dexamethasone binding to rat thymocytes, and are sufficient to act as an antagonist at steroid receptors in the eye. Multiple drop administration for 10 days (3 drops per day) revealed no accumulation in the treated eye, but did show the presence of drug in the untreated contralateral eye that could explain the contralateral pharmacological effect seen on intraocular pressure after several days of treatment.

Administration, Topical↗