The development of a solution-phase synthesis of distamycin A and its extension to the preparation of 2640 analogues are described. Thus, solution-phase synthesis techniques with reaction workup an...

Total Synthesis of Distamycin A and 2640 Analogues: A Solution-Phase Combinatorial Approach to the Discovery of New, Bioactive DNA Binding Agents and Development of a Rapid, High-Throughput Screen for Determining Relative DNA Binding Affinity or DNA Binding Sequence Selectivity

Patient education is an essential component in quality management of the anticoagulated patient. Because it is time consuming for clinicians and overwhelming for patients, education of the anticoagulated patient is often neglected. We surveyed the medical literature in order to identify the best patient education strategies. Study Selection: Two reviewers independently searched the MEDLINE and Google Scholar databases (last search March 2007) using the terms "warfarin" or "anticoagulation", and "patient education". The initial search identified 206 citations, A total of 166 citations were excluded because patients were of pediatric age (4), the article was not related to patient education (48), did not contain original data or inadequate program description (141), was focused solely on patient self-testing (1), was a duplicate citation (3), the article was judged otherwise irrelevant (44), or no abstract was available (25). Data Extraction: Clinical setting, study design, group size, content source, time and personnel involved, educational strategy and domains, measures of knowledge retention. Data Synthesis: A total of 32 articles were ultimately used for data extraction. Thirteen articles adequately described features of the educational strategy. Five programs used a nurse or pharmacist, 4 used a physician, and 2 studies used other personnel/vehicles (lay educators (1), videotapes (1)). The duration of the educational intervention ranged from 1 to 10 sessions. Patient group size most often averaged 3 to 5 patients but ranged from as low as 1 patient to as much as 11 patients. Although 12 articles offered information about education content, the wording and lack of detail in the description made it too difficult to accurately assign categories of education topics and to compare articles with one another. For the 17 articles that reported measures of patient knowledge, 5 of the 17 sites where the surveys were administered were located in anticoagulation clinics/centers. The number of questions ranged from as few as 4 to as many as 28, and questions were most often of multiple choice format. Three were self-administered, and 2 were completed over the telephone. Two reports described instruments along with formal testing of the validity and reliability of the instrument. Published reports of patient education related to warfarin anticoagulation vary greatly in strategy, content, and patient testing. Prioritizing the educational domains, standardizing the educational content, and delivering the content more efficiently will be necessary to improve the quality of anticoagulation with warfarin.

/pdf/best-strategies-for-patient-education-about-anticoagulation-327z6unsrc.pdf

Best strategies for patient education about anticoagulation with warfarin: a systematic review

Solubilization by Cosolvents I: Organic Solutes in Propylene Glycol-Water Mixtures

In an eight-subject two-way crossover study, 05-mg oral doses of digoxin were administered as two 025-mg tablets made by two different manufacturers Treatment "B" yielded average peak plasma levels and areas under the curves that were 59% and 55%, respectively, of those attained following treatment "A" Two of the eight subjects also received the same dose in 5% dextrose both orally and by constant rate intravenous infusion during a one-hour period Average peaks were 419, 376, 146, and 070 ng/ml following the intravenous infusion, solution orally, treatment A (tablet) orally, and treatment B (tablet) orally, respectively Relative areas under the curves were 100%, 802%, 567%, and 307% for the treatments in the same order

Equivalence Lack in Digoxin Plasma Levels

Fosphenytoin sodium, a phosphate ester prodrug of phenytoin, was developed as a replacement for parenteral phenytoin sodium. Unlike phenytoin, fosphenytoin is freely soluble in aqueous solutions, including standard i.v. solutions, and is rapidly absorbed by the i.m. route. Fosphenytoin is metabolized (conversion half-life of 8 to 15 min) to phenytoin by endogenous phosphatases. Therapeutic free (unbound) and total plasma phenytoin concentrations are consistently attained after i.m. or i.v. administration of fosphenytoin loading doses. Fosphenytoin has fewer local adverse effects (e.g., pain, burning, and itching at the injection site) after i.m. or i.v. administration than parenteral phenytoin. Systemic effects related to the CNS are similar for both preparations, but transient paresthesias are more common with fosphenytoin.

Pharmacology and pharmacokinetics of fosphenytoin

Glucose esters of 4‐ and 5‐aminosalicylic acid were obtainable by reaction of the benzyloxynitrobenzoic acid chlorides with diacetone glucose, followed by catalytic hydrogenation of the nitro groups. Conversion of the amines to hydrochlorides removed one or both of the acetone groups from the glucose. Complete removal of the acetone groups gave a glucose ester that was unstable on standing, but the protected glucose esters were found to be stable. The free‐amino ester of 4‐amino‐salicylic acid was obtained in excellent yield for tuberculostatic and toxicity determinations.

Edward G. Feldmann

Papers

Glucose ester derivatives of aminosalicylic acids

The β-Nitration of 2-Thenaldehyde

The pharmaceutical sciences in America, 1952-2002.

Drug Product Selection—Freedom With Responsibility*

Brand versus generic drugs.