Drugs online research references
Ann Otol Rhinol Laryngol. 2003 Mar;112(3):197-201.
Outcome of treatment with valacyclovir and prednisone in patients with Bell's palsy.
Axelsson S, Lindberg S, Stjernquist-Desatnik A.
Department of Otorhinolaryngology-Head and Neck Surgery, Hospital of Helsingborg, Helsingborg, Sweden.
Idiopathic facial paralysis, or Bell's palsy, shows a nonepidemic pattern that might indicate reactivation of a latent microorganism such as herpes simplex type I as a causative agent. Thirty percent of patients with Bell's palsy given no treatment will not recover completely, and 5% will have severe sequelae. The aim of this study was to find out whether treatment with an antiviral drug in combination with corticosteroids is more effective than no medical treatment at all in patients with Bell's palsy. Fifty-six consecutive adult patients attending the otorhinolaryngology department of the University Hospital of Lund from 1997 to 1999 were treated with 1 g of valacyclovir hydrochloride 3 times per day for 7 days and 50 mg of prednisone daily for 5 days, with the dose being reduced by 10 mg daily for the next 5 days. Fifty-six adult patients with Bell's palsy attending the same department between 1995 and 1996 who were given no medical treatment were studied retrospectively and used as the control group. Forty-nine patients (87.5%) in the treatment group recovered completely, as compared with 38 patients (68%) in the control group (p < .05). One patient (1.8%) in the treatment group displayed severe sequelae, defined as a House-Brackmann score of IV or worse, as compared with 10 of 56 patients (18%) in the control group (p < .01). Among patients over 60 years old, 10 of 10 in the treatment group had complete recovery, as compared with 5 of 12 patients in the control group (p < .01). The present study showed a significantly better outcome in patients with Bell's palsy treated with valacyclovir and prednisone as compared with patients given no medical treatment. This difference in outcome was especially pronounced among elderly patients.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=12656408&dopt=Abstract
Curr Eye Res. 2002 Oct;25(4):243-52.
Ocular penetration of acyclovir and its peptide prodrugs valacyclovir and val-valacyclovir following systemic administration in rabbits: An evaluation using ocular microdialysis and LC-MS.
Dias C, Nashed Y, Atluri H, Mitra A.
Division of Pharmaceutical Sciences, School of Pharmacy, University of Missouri-Kansas City, Kansas City, MO 64110-2499, USA.
PURPOSE: To investigate the ocular penetration of acyclovir and its prodrugs following systemic administration and to elucidate the mechanism of penetration. METHODS: Hydrophilic peptide prodrugs of acyclovir were infused intravenously in New Zealand albino rabbits over 45 min at a dose equivalent to 30 mmoles/kg acyclovir. Aqueous and vitreous humor samples were obtained utilizing ocular microdialysis and blood samples were obtained from the mid ear vein using a cannula. RESULTS: The plasma bioavailability for acyclovir, valacyclovir and val-valacyclovir were similar with area under curve values being 896.24 (+/-143.58), 776.54 (+/-197.52), 824.69 (+/-217.43) min x micromoles/L respectively. Anterior segment area under curve values were 53.70 (+/-35.58), 139.85 (+/-9.43) and 291.05 (+/-88.13) min x micromoles/L respectively while the mean residence time values were 46.47 (+/-24.94), 76.30 (+/-7.24) and 188.39 (+/-80.73) min respectively. Vitreous levels of the prodrugs were not measurable. CONCLUSIONS: The valine and valine-valine ester prodrugs of ACV penetrated the anterior segment of the eye much better than acyclovir alone, probably via a carrier mediated transport mechanism.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=12658558&dopt=Abstract
J Pharmacol Exp Ther. 2003 Jun;305(3):1087-97. Epub 2003 Mar 26.
Contribution of organic anion transporters to the renal uptake of anionic compounds and nucleoside derivatives in rat.
Hasegawa M, Kusuhara H, Endou H, Sugiyama Y.
Graduate School of Pharmaceutical Sciences, University of Tokyo, 7-3-1, Hongo, Bunkyo-ku, Tokyo 113-0033, Japan.
Our previous kinetic analyses have shown that rat organic anion transporter 1 (rOat1; Slc22a6) and rOat3 (Slc22a8) are responsible for the renal uptake of p-aminohippurate and pravastatin, respectively. In this study, their contribution to the renal uptake of organic anions and nucleoside derivatives was examined by investigating the uptake by rOat1- and rOat3-expressing cells and kidney slices. Transfection of rOat1 resulted in an increase of the uptake of temocaprilat (Km = 0.56 microM), 2,4-dichlorophenoxyacetate (2,4-D; Km = 10 microM), and 3'-azido-3'-deoxythymidine (AZT; Km = 43 microM). rOat3-expressing cells showed significant uptake of temocaprilat (Km = 1.4 microM), estrone sulfate (Km = 5.3 microM), dehydroepiandrosterone sulfate (DHEAS; Km = 12 microM), and benzylpenicillin (PCG; Km = 85 microM). All the test compounds were accumulated in kidney slices in a carrier-mediated manner, although the saturable components of AZT and acyclovir were small. The Km of 2,4-D uptake by kidney slices was comparable with that of rOat1, and the corresponding values of DHEAS and PCG were similar to those of rOat3. The uptake of estrone sulfate and temocaprilat by kidney slices consisted of two saturable components, with the Km values of their high-affinity components being similar to those for rOat3 (estrone sulfate), and rOat1 and rOat3 (temocaprilat), respectively. These results suggest that the renal uptake of 2,4-D is mainly accounted for by rOat1 and the uptake of PCG and DHEAS by rOat3, and rOat3 is partly involved in the renal uptake of temocaprilat and estrone sulfate.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=12660303&dopt=Abstract
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