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Scott Med J. 1986 Oct;31(4):234-8.
Use of nifedipine as the drug of third choice in management of hypertension.

Roulston JE, Wathen CG, Muir AL.

Nifedipine has been used in the management of hypertension in 36 consecutive patients who could not tolerate, or were not controlled by, atenolol and thiazide diuretics. Mean supine blood pressure was reduced from 193/110 +/- 5/2 (SEM) mmHg to 162/91 +/- 5/2 mmHg at eight weeks and remained at that level for the six months of follow-up. Blood pressure reduction at four weeks was not always a predictor of final BP level. Eight patients could not tolerate atenolol, nine patients could not tolerate thiazide diuretics and four patients could not tolerate nifedipine. No significant changes in plasma urea, creatinine, sodium, potassium urate, 'total CO2' or glucose were observed. We conclude that nifedipine is a well-tolerated drug and may be useful after beta-blockers and thiazide have been tried in the management of hypertension.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=3563462&dopt=Abstract




S Afr Med J. 1983 Oct 1;64(15):572-3.
Beta-adrenergic blocking drugs and renal function.

Walters L, Dormehl I, Goosen DJ, Avenant JC, Du Plessis M, Jacobs N, Schoeman HS.

A baboon model was used to investigate the effects of atenolol, nadolol, sotalol and labetalol on renal function. The glomerular filtration rate (GFR) and renal blood flow (RBF) were measured, using radionuclides and a gamma camera, before and after 1 week's oral administration of these drugs. All the drugs caused an increase in the GFR, but this reached statistical significance only in the cases of sotalol (P less than 0,025) and labetalol (0,05 less than P less than 0,10). The RBF was not significantly changed, although it decreased in all cases.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=6137878&dopt=Abstract




J Drug Target. 1993;1(1):29-39.
Segmental differences in drug permeability, esterase activity and ketone reductase activity in the albino rabbit intestine.

Narawane M, Podder SK, Bundgaard H, Lee VH.

University of Southern California, School of Pharmacy, Department of Pharmaceutical Sciences, Los Angeles 90033.

Possible segmental differences in drug permeability as well as esterase and ketone reductase activities in the albino rabbit intestine were investigated. Beta adrenergic antagonists and timolol prodrugs spanning four orders of magnitude in distribution coefficient were used as model drugs. Drug penetration was evaluated in Ussing chambers using isolated segments of the duodenum, jejunum, ileum, ascending colon, descending colon, and rectum. Esterase and ketone reductase activities were determined in homogenates of the above segments using timolol ester prodrugs and levobunolol as substrates, respectively. The results indicate that the hydrophilic beta adrenergic antagonists atenolol and sotalol and moderately lipophilic metoprolol penetrated all intestinal segments equally well, whereas moderately lipophilic timolol and lipophilic propranolol, levobunolol and betaxolol were better absorbed from the large than from the small intestinal segments. Changes in lipophilicity exerted a more pronounced effect on the penetration of beta adrenergic antagonists in the large than the small intestinal segments. A similar pattern existed for timolol prodrugs. In addition to segmental differences in drug permeability, segmental differences in esterase and ketone reductase activities also existed. The level of esterase and ketone reductase activities in the small intestinal segments was, on average, 12 times and 5 times higher, respectively, than in the large intestinal segments. The implication of the above findings is that segmental differences in drug permeability and metabolism must be considered in the design of oral drug delivery systems.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=7915178&dopt=Abstract













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