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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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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, Sérgio 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.

Read more at Wikipedia.org

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Are you making the healthiest choices?
From Shape, 10/1/04

Every day, you make choices about your health and well--being. But are you making the right ones? Take another look at some of the decisions you face each day, and see if your choices are the best ones for you and your body.

The Breakfast Club

It's been called "the most important meal of the day"--but chances are your breakfast is overlooked, or skipped altogether. Some food for thought: missing meals can lead to overeating later in the day and weight gain. So eat up and choose wisely--go for whole grains and proteins for energy and sharpened focus.

Work It Out

Can't find time to exercise? You've got choices. Opt for a morning workout--you'll fit in fitness and gain energy for the day. If you still can't swing it, make the choice to exercise whenever you can--take the stairs instead of the elevator, or get off the bus a few stops early and walk the rest of the way to work.

Be Choosy ... in Love and in Birth Control

Whether you're choosing the right guy or looking for a pill that works best for you, your needs are unique. Not all birth control pills are the same, either--and, with more than 40 pills to choose from, it's important to make the choice that is best for you.

Yasmin[R] is a low-dose birth control pill that is more than 99% effective at preventing pregnancy. Yasmin can help:

* Give you shorter, lighter periods

* Reduce cramps

* Regulate your cycle

Know your body, know your mind and know your choices!

Talk to your healthcare provider about Yasmin and see the important safety information on the opposite page.

Learn more at www.yasmin.com

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Important safety information about Yasmin:

What makes Yasmin[R] different from other birth control pills?

It contains a different kind of progestin which may increase potassium. For healthy women this is not a problem.

How can you be sure Yasmin is safe for you?

Consult your doctor. You should not take Yasmin if you have kidney, liver or adrenal disease because this could cause serious heart and health problems.

What drugs could interfere with Yasmin?

Potassium-increasing drugs. Tell your doctor if you are on daily, long-term treatment for a chronic condition with any of the following: NSAIDs-ibuprofen (Motrin[R], Advil[R]), naproxen (Naprosyn[R], Aleve[R], and others) when taken long-term and daily for arthritis or other diseases or conditions, potassium-sparing diuretics (spironolactone and others), potassium supplementation, ACE inhibitors (Capoten[R], Vasotec[R], Zestril[R], and others). Angiotensin-II receptor antagonists (Cozaar[R], Diovan[R], Avapro[R], and others), and Heparin. Women who take any of the preceding drugs every day should have their potassium level checked in the first month of taking Yasmin.

What are the risks involved with taking any oral contraceptive (OC)?

OCs can be associated with increased risks of several serious side effects, and do not protect against HIV infection or other STDs. Women, particularly those 35 and over, are strongly advised not to smoke due to the risk of serious cardiovascular side effects.

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