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Zestril

Lisinopril (lye-SIH-no-pril, ATC code C09AA is a drug of the angiotensin converting enzyme (ACE) inhibitor class that is primarily used in treatment of hypertension, congestive heart failure and heart attacks.
Historically, lisinopril was the third ACE inhibitor, after captopril and enalapril that was introduced into therapy in early 1990s . Lisinopril has a number of properties that distinguish it from other ACE inhibitors: it is hydrophilic, has long half life and tissue penetration and is not metabolized by the liver. more...

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Pharmacology

Chemistry

Lisinopril is chemically described as (S)-1--L-proline dihydrate. Its empirical formula is C21H31N3O5•2H2O. Lisinopril is the lysine-analog of enalapril. Unlike other ACE inhibitors lisinopril is not a prodrug and tablets contain pharamacologically active substance.

Absorption

After oral dosing peak blood levels are reached within ca. 7 hours. The oral bioavailability is approximately 25% according to measurements of the unchanged drug in urine. The interindividual variability is 6 to 60% within the full dose range of 5 to 80 mg. Emptiness of stomach does obviously not influence the extent of gastrointestinal resorption.

Half life

The halflife of Lisinopril under steady-state conditions is 12.6 hours. The terminal phase shows a prolonged terminal phase, but no cumulation of the drug is seen under normal circumstances.

Metabolism

Lisinopril is not metabolized.

Elimination

Lisinopril is solely excreted in urine in the unchanged form. Elimination of the drug depends on glomerular filtration and tubular excretion. Rate of lisinopril elimination decreases with old age and kindney or heart failure. There is a relation between creatinine and lisinopril clearance. With prolonged therapy dose reduction can be necessary to avoid cumulation.

Lisinopril can be removed from circulation by dialysis.

Mode of action

Lisinopril acts by competitive inhibition of Angiotensin Converting Enzyme (ACE), a key enzyme in the renin-angiotensin system (RAS) which plays a crucial role in controlling of blood pressure. Diminished formation of a potent vasocontrictor - Angiotensin II from Angiotensin I leads to lowering of hypertension. Besides it limits degradation of a vasodilator - bradykinin by ACE. Angiotensin II also increases blood pressure by stimulation the production of aldosterone, which promotes sodium and water retention in the body. So the complete action consists of

  • diminished production of angiotensin II
  • diminished degradation of bradykinin
  • diminished production of aldosterone

Indications

  • hypertension
  • congestive heart failure alone or with diuretics
  • acute myocardial infarction
  • renal and retinal complications of diabetes.

Contraindications and Precautions

As with all angiotensin converting enzyme (ACE) inhibitors

Pregnancy

Category D

When lisinopril therapy in women of child-bearing age is started pregnancy must be excluded and effective contraceptive methods used.

Read more at Wikipedia.org


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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

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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

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* 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.

COPYRIGHT 2004 Weider Publications
COPYRIGHT 2004 Gale Group

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