Molecular structure of captopril
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Capoten

Captopril is an Angiotensin-Converting Enzyme inhibitor (ACE inhibitor) used for the treatment of hypertension and some types of chronic heart failure. Captopril was the first ACE inhibitor developed and was considered a breakthrough both because of its novel mechanism of action and also because of the revolutionary development process. The original innovator drug Bristol-Myers Squibb's Capoten®. more...

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Clinical Use

Development of captopril

Captopril was invented in 1975 by three researchers at the American drug company Squibb (now Bristol-Myers Squibb) , Miguel Ondetti, Bernard Rubin and David Cushman. Squibb filed for American patent protection on the drug in February 1976 and U.S. Patent was 4,046,889 was granted in September 1977.

The development of captopril was amongst the earliest successes of the revolutionary concept of structure-based drug design. The renin-angiontensin-aldosterone system had been extensively studied in the mid-20th century and it had been decided that this system presented several opportune targets in the development of novel treatments for hypertension. The first two targets that were attempted were renin and ACE. Captopril was the culmination of efforts by Squibb's laboratories to develop an ACE inhibitor.

Ondetti, Cushman and colleagues built on work that had been done in the 1960s by the British Nobel laureate Sir John Vane when he was a researcher at the Royal College of Surgeons. Working with a Brazilian colleage, SĂ©rgio Ferreira, Vane discovered a peptide in Brazilian viper venom which was a 'collected-product inhibitor' of angiotensin II. Captopril was developed from this peptide after it was found via QSAR-based modification that the terminal sulfhydryl-moiety of the peptide provided a high potency of ACE inhibition.

Capoten gained FDA approval in June 1981. The drug went generic in the U.S. in February 1996 as a result of the end of market exclusivity for Bristol-Myers Squibb.

Shortcomings

During Phase III/IV trials of captopril, it was found that captopril had some undesirable adverse effects. The most predominant of which included cough, rash and taste disturbances (metallic or loss of taste). Cough is an adverse effect common to all of the ACE inhibitors, but the rash and taste disturbances were attributed to the very sulfhydryl moiety which granted captopril its potency. An additional shortcoming of captopril is the short half-life, necessitating 2-3 times daily dosing.

The development of longer-acting ACE inhibitors lacking the sulfhydryl-moiety such as enalapril proved to be the downfall of captopril and, whilst it is still used, it is no longer amongst the more widely used ACE inhibitors.

Reference

  • Smith CG, Vane JR. The discovery of captopril. FASEB J 2003;17:788-9. Fulltext. PMID 12724335.

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Conjunctivitis: diagnostic usefulness of signs and symptoms unknown
From Journal of Family Practice, 2/1/04 by Eric Rotert

Rietveld RR, van Weert HCPM, ter Riet G, and Bindels PJE. Diagnostic impact of signs and symptoms in acute infectious conjunctivitis: systematic literature search. BMJ 2003; 327:789.

* PRACTICE RECOMMENDATIONS

Despite recommendations in ophthalmologic texts for differentiating bacterial from viral conjunctivitis, no research supports the usefulness of any signs or symptoms to make this distinction. This raises validity questions about treatment studies based on clinically diagnosed bacterial conjunctivitis.

* BACKGROUND

Primary care providers often prescribe antibiotics based on physical findings of papillary conjunctivitis, mucopurulent discharge, and rapid spread between eyes. However, though often recommended in ophthalmologic texts, the evidence supporting these criteria is unknown.

* STUDY DESIGN AND VALIDITY

The researchers searched 4 databases (PubMed, Embase, CINAHL, and Cochrane Controlled Trials Register) and manually searched bibliographies from relevant articles, guidelines, and textbooks to find 2903 articles regarding diagnostic accuracy. They included studies comparing signs, symptoms, or both with bacterial culture.

After they excluded studies of newborns, eye surgery, and Chlamydia trachomatis patients, only 1 article remained. The methodology of this study did not hold up to their qualitative data analysis.

One investigator conducted the search, but 2 reviewed the articles. They do not mention how they resolved disagreements (if they existed) about study inclusion. (Level of evidence: 1a)

* RESULTS

This systematic review did not find any evidence to support or refute the clinical criteria physicians commonly use to distinguish bacterial from viral conjunctivitis.

DRUG BRAND NAMES

Amoxicillin-clavulanate * Augmentin Azithromycin * Zithromax Candesartan * Atacand Captopril * Capoten Fluoxetine * Prozac Nortriptyline * Aventyl, Pamelor Simvastatin * Zocor Valsartan * Diovan

Eric M. Rotert, MD, and Beth Potter, Md, Department of Family Medicine, University of Wisconsin-Madison. E-mail: erotert@wisc.edu.

COPYRIGHT 2004 Dowden Health Media, Inc.
COPYRIGHT 2004 Gale Group

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