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Lisinopril - Article


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Lisinopril

Prinivil; Zestril


Article: Lisinopril

Image:Lisinopril.png
Lisinopril
Systematic (IUPAC) name
1-[6-amino-2- (1-carboxy-3-phenyl-propyl) amino-hexanoyl]pyrrolidine- 2-carboxylic acid dihydrate
Identifiers
CAS number 83915-83-7
ATC code C09AA03
PubChem 5362119
DrugBank APRD00560
Chemical data
Formula C21H31N3O5
Mol. weight 405.488 g/mol
Pharmacokinetic data
Bioavailability approx. 25%, but wide range between individuals (6 to 60%)
Protein binding 0
Metabolism none - eliminated unchanged in urine
Half life 12 hours
Excretion  ?
Therapeutic considerations
Pregnancy cat.

D - teratogenic

Legal status

Prescription only

Routes  ?

Lisinopril (lye-SIH-no-pril, is a drug of the angiotensin converting enzyme (ACE) inhibitor class that is primarily used in treatment of hypertension, congestive heart failure, heart attacks and also in preventing renal and retinal complications of diabetes.

Historically, lisinopril was the third ACE inhibitor, after captopril and enalapril that was introduced into therapy in early 1990s.[1] 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.

Pharmacology

Lisinopril is the lysine-analog of enalapril. Unlike other ACE inhibitors lisinopril is not a prodrug and excreted unchanged in the urine. In cases of overdosage, it can be removed from circulation by dialysis.

Clinical use

Its indications, contraindications and side effects are as those for all ACE inhibitors.

Its long half-life allows for once a day dosing which aids patient compliance. The usual daily dose in all indications ranges from 2.5mg in sensitive patients to 40mg. Some patients have been treated with 80mg daily and have tolerated this high dose well.

Lower dosages must be used in patients with higher grade renal impairment (glomerular filtration rate (GFR) lower than 30ml/min).

History/Brand Names

Lisinopril was developed by Merck & Co. and is marketed worldwide as Prinivil® and by AstraZeneca as Zestril®. In Australia it is marketed by AlphaPharm as Lisodur®.



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July 25, 2008



Page Updated: July 22, 2006
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