Selection of Drugs

The relative selectivity of drugs such as haloperidol for the higher affinity (+)SKF-10,047 labeled sites allowed the determination of the pharmacological profile of the low affinity sites, which was very similar to that of 3H-TCP labeled sites. PCP and... 

An approach to selection of drugs for the treatment of patients with hypertension should be evidence-based with considerations regarding the individual s co-existing disease states, co-prescribed medications, and practical patient-specific issues including costs. 

Directly observed treatment (DOT) should be used whenever possible to reduce treatment failures and the selection of drug-resistant isolates. 

Chaires JB (2005) Structural Selectivity of Drug-Nucleic Acid Interactions Probed by Competition Dialysis. 253 33-53 Cherkinsky M, see Braverman S (2007) 275 67-101... 

Selection of drug therapy should follow the JNC 7 guidelines, but the treatment approach in some patient populations may be slightly different. In these situations, alternative agents may have unique properties that benefit a coexisting condition, but the data may not be based on evidence from outcome studies in hypertension. 

Patients with diminished renal and/or hepatic function will accumulate certain drugs unless dosage is adjusted. Any concomitant therapy the patient is receiving may influence the selection of drug therapy, the dose,... 

Factors directly related to the drug selection include an inappropriate selection of drug, dosage, or route of administration. Malabsorption of a drug product because of GI disease (e.g., short-bowel syndrome) or a drug interaction (e.g., complexation of fluoroquinolones with multivalent cations resulting in reduced absorption) may lead to potentially subtherapeu-tic serum concentrations. 

The ex vivo methods lend themselves easily for the performance of mechanistic investigations. In order to optimize selection of drug candidates prior to further clinical development, it is important to decipher the contributive roles of permeation, metabolism, efflux, and toxicity. This will then make it possible to properly channel the optimization process, for instance, by permeation enhancement, mucoadhesion, modification of the physicochemical characteristics of the drug, or even change in the route of administration in case the drug and/or formulation turns out to be too toxic. Regarding permeability studies, it is possible not only to quantify passive diffusion but also to identify and characterize (compound)-specific carrier-mediated transport routes. These tools have been used to identify and characterize the relative contribution of... 

The experimental methods for evaluating the BRB transport in vivo and the ocular pharmacokinetics of systemic drug administration are relatively straightforward and have been in use for over two decades. Overall, they are useful as a guide for the selection of drug candidates for the treatment of retinal diseases. With the combined use of conventional in vivo methods and newly developed... 

The expectation that HTS and combinatorial chemistry could by themselves improve the drug discovery process is now clearly erroneous,50 and effort is currently focussed on developing methods to decrease clinical attrition through early selection of drug candidates with the best chances of success. 

Drug development work also includes formulation, stability studies, and selection of drug delivery systems, as discussed in Section 5.6. Once the API has been prepared, excipients are added ... 

Table 6.1. Distribution and selectivity of drugs for 5-HT receptor subtypes 5-HTj receptors...

Using the index it is possible to gain an insight into the selection of drugs covered in such examinations. Check that you know the meaning of the conditions listed in Appendix B and make lists of medicines that are indicated and contraindicated or that may precipitate the condition. 

White NJ, Pongtavompinyo W. (2003) The de-novo selection of drug resistance in malaria parasites. Philos Trans R Soc LondBBiol Sci 270 545-554. 

It is reasonable that data should be required to demonstrate whether the response of patients to a new active substance is likely to change or be changed by concomitant medication. However, there is clearly a huge number of potential drug combinations, and some rational selection is required. To assist with the selection of drug combinations for which data are required, the following seven questions at least should be asked. 

Absolute selectivity of drug action does not exist. Any given effector tissue probably contains more than one receptor subtype, and it is likely that the proportion of receptor subtypes varies within that effector. Nevertheless, the designation of a drug as a selective agent for either a Pi-receptor or a P2-receptor seems both useful and justified if one keeps in mind that the designation represents a shorthand notation for what is only a predominance of activities. 

Selection of Drug-Receptor Binding Forces in Drug Design... 

Capranico G. A rational selection of drug targets needs deeper insights into general regulation mechanisms. CurrMed Chem Anti-Canc Agents 2004 4 393-394. 

---