Drugs online research references









Int J Clin Pharmacol Ther. 2000 Nov;38(11):532-9.
Similarity in the linear and non-linear oral absorption of drugs between human and rat.

Chiou WL, Ma C, Chung SM, Wu TC, Jeong HY.

Department of Pharmaceutics and Pharmacodynamics, College of Pharmacy, University of Illinois at Chicago, 60612, USA.

OBJECTIVE: The main aim of this study was to provide a simple, pharmacokinetic rationale for great similarity in the extent (Fab) of gastrointestinal absorption of about 100 different, diverse compounds between human and the rat in linear dosing range, and to test the general applicability of a novel empirical method to correlate the non-linear Fab between the human and the rat by normalizing doses by body surface area (BSA) or body weight 0.67. METHOD: The mean small intestinal transit time (t) of 36 rats was estimated from the reported study, and this was used to compare with that in humans. The reported great similarity in apparent first-order absorption rate constants (k) of seven structurally diverse compounds between the two species were obtained. Extensive computer search was made and non-linear Fab data for the two species were obtained for chlorothiazide, acyclovir, miglitol and pafenolol. RESULTS: The mean t for rats was estimated to be 3.32 h which is almost identical to that reported in humans. The great similarity in Fab between human and rat in linear absorption range can be rationalized by similar t and k between the two species. The markedly different Fab vs dose/kg of body weight profiles between human and rat for the four drugs showing dose-dependent Fab were found to collapse when doses were normalized by BW0.67. CONCLUSION: For Fab not limited by the solubility problem, the great similarity in Fab between human and rat in linear absorption range can be rationalized by the similar t and k. For non-linear Fab drugs, great similarity in Fab can also be obtained between human and rat when doses are normalized by BSA or BW0.67. Regardless of absorption properties (active, passive or facilitated), similar Fab between the two species may be generally obtained when doses used in humans are about 5 to 7 times lower than that in rats. The above findings may be valuable in drug development.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=11097145&dopt=Abstract




Rev Laryngol Otol Rhinol (Bord). 2000;121(3):199-202.
[Facial paralysis: treatment with an acyclovir-methylprednisolone combination, preliminary results]

[Article in French]

Darrouzet V, Lacher-Fougere S, Duclos JY, Chambrin A, Bebear JP.

C.H.U. Pellegrin, Clinique Universitaire O.R.L., Bordeaux, France.

RATIONAL: Many actual data suspect a viral etiology to Bell's palsy. Herpes viridae are more and more incriminated. On these basis, we have studied the efficacity of parenteral association of 30 mg/Kg/j of Aciclovir and 1 mg/Kg/j of Methylprednisolone in the treatment of Bell's palsy with less than 12 days of evolution. METHOD: The evaluation concern 53 patients. We also evaluated the functional motor result (using House and Brackmann staging) and search prognostic factors in clinic and paraclinic data. A viral investigation have been made in most of the cases. RESULTS: Only one of our patients treated with Aciclovir keeps some sequeles (stage III of House and Brackmann classification). We didn't found any deleterious effect. Statistically, the electromyography is the only one test with a prognostic value. But we feel that delay between the starting and the treatment of the palsy is important. Viral tests show sometime abnormal Ig against the Herpes viridae group. CONCLUSIONS: These promising results are lightened with a review of the literature. A multicentric investigation is already in place for a stronger statistic effect.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=11109888&dopt=Abstract




Clin Exp Obstet Gynecol. 2000;27(3-4):227-30.
Hepatic and renal effects of azidothymidine and acyclovir on pregnant rats.

Mamede JA, Oliveira-Filho RM, Simo s MJ, Mora OA, Espiridiao SKulay L Jr.

Universidade de Mogi das Cruzes School of Medicine, Brazil.

The antiviral effect of azidothymidine (AZT) can be potentiated by acyclovir (ACV), and this drug association has been used in the management of HIV-infected patients. In the present study we examined the effects of this association on the livers and kidneys of both pregnant rats and their concepts. Previous data from this laboratory suggested that the deleterious effects of ACV on rat pregnancy are due to its extraplacental actions and these are, at least in part, counteracted by concomitant treatment with AZT. Kidneys and livers of pregnant rats were noticed to be much more sensitive to the toxic action of the drugs than those of their concepts, ACV eliciting much more evident morphological alterations than did AZT. Contrary to what was expected, in the group of rats treated with both drugs AZT was not able to diminish the severity of the alterations evoked by ACV. The proposed "protective" action of AZT against the abortive effect of ACV on rat pregnancy does not seem to be exerted through a renal or hepatic pathway.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=11214960&dopt=Abstract













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