PubMed · 15366196
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Joaquim Ferreira, Cristina Sampaio. 2003. Essential tremor.. https://pubmed.ncbi.nlm.nih.gov/15366196/
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This study aimed to determine the transport characteristics of chiral drug enantiomers across Caco-2 cell monolayers as a model of human intestinal epithelial membrane. Esmolol was chosen as a model drug, and the study focused on the transepithelial transport of esmolol enantiomers in this in vitro model system. Separation and quantitation of (S)- and (R)-esmolol were performed by RP-HPLC with the use of GITC as a precolumn derivatizing agent. Bidirectional transport studies of 5.0-400.0 micromol/l esmolol demonstrated that the two enantiomers were transported mainly by a passive, transcellular mechanism. At concentrations of 5.0-100.0 micromol/l, enantioselective permeability of esmolol was observed. In the absorptive transport, Papp of (S)-esmolol was smaller than (R)-esmolol and vice versa for secretory transport. The enantioselectivity disappeared when the drug concentration was increased to 200.0 micromol/l. In conclusion, the transport characteristics of (S)- and (R)-esmolol were distinctly different. An enantioselective carrier-mediated mechanism in addition to passive diffusion was involved in the transport process of esmolol across Caco-2 cell monolayers.
PURPOSE: To compare pattern of antihypertensive drug utilization in 1998 with 2000 following the: (a) publication of 1999 World Health Organization/International Society of Hypertension (WHO/ISH) guidelines for drug management of hypertension; and (b) introducing new antihypertensives to the essential drug list, in primary care, Bahrain. METHODS: Retrospective prescription-based survey carried out in seven out of 20 primary care health centers in Bahrain. A total of 9272 patients comprising 6543 with uncomplicated hypertension and 2729 with diabetic hypertension were studied. RESULTS: Between 1998 and 2000, the prescription rate of beta-blockers and methyldopa significantly declined (p < 0.0001) while the rate of angiotensin converting enzyme (ACE) inhibitors and calcium channel blockers (CCBs) increased (p < 0.0001) in uncomplicated hypertension. However, in diabetic hypertension there was a non-significant decline in utilization of beta-blockers, CCBs, methyldopa, and diuretics whereas a significant increase in prescribing of ACE inhibitors (p < 0.0001). Inclusion of Perindopril into the essential drug list resulted in an overall increase in utilization of ACE inhibitors: use of captopril and enalapril declined while lisinopril and perindopril increased. Substitution of immediate-release (IR) indapamide by sustained-release (SR) formulation did not change the overall utilization of diuretics; however, intra-class changes were evident with a significant decline in use of thiazide diuretics and concomitant increase in use of SR indapamide by 2000. CONCLUSIONS: The antihypertensive prescribing pattern is influenced by WHO/ISH guidelines as well as by introduction of new antihypertensives to primary care essential drug list in primary care. The choice of a drug is also influenced by presence of co-morbidity with diabetes mellitus.