Lisinopril

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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. mass 405.488 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability approx. 25%, but wide range between individuals (6 to 60%)
Protein binding 0
Metabolism None
Half life 12 hours
Excretion Eliminated unchanged in Urine
Therapeutic considerations
Pregnancy cat.

D - teratogenic
Legal status

℞ Prescription only
Routes  ?

Lisinopril (lye-SIN-o-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. It has been compared with omapatrilat which is of similar function.

Historically, lisinopril was the third ACE inhibitor, after captopril and enalapril, and was introduced into therapy in the 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.

Contents

[edit] Pharmacology

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

[edit] 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 2.5 mg in sensitive patients to 40 mg. Some patients have been treated with 80 mg 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 30 ml/min).

[edit] Adverse effects

Rare, serious side effects that would require immediate medical attention include:

Less severe side effects of moderate concern include:

  • abdominal pain, bloating, vomiting
  • chest pain or tightness, dizziness, lightheadedness, fainting (syncope)
  • fever
  • joint pain
  • rash

The following side effects are common and likely to improve with time:

  • cough
  • diarrhea, loss of taste, nausea
  • drowsiness, headache, tiredness

Lisinopril causes the kidneys to retain potassium, which may lead to hyperkalemia.

[edit] History/brand names

Lisinopril was developed by Merck & Co. and is marketed worldwide as Prinivil or Tensopril and by AstraZeneca as Zestril. In India it is marketed by Micro Labs as Hipril. Like other ACE inhibitors, it is derived from the venom of the jararaca, a Brazilian pit viper (Bothrops jararaca).

[edit] References

  • Bussien JP, Waeber B, Nussberger J, Gomez HJ, Brunner HR. Once-daily lisinopril in hypertensive patients: Effect on blood pressure and the renin-angiotensin system. Curr Therap Res 1985;37:342-51.
  • Lisinopril info - rx-list.com
  • Goodman & Gilman's : The pharmacological basis of therapeutics, 10th. ed., 2001
  • Lisinopril.com - Lisinopril information

[edit] Footnotes

  1. ^ Patchett A, Harris E, Tristram E, Wyvratt M, Wu M, Taub D, Peterson E, Ikeler T, ten Broeke J, Payne L, Ondeyka D, Thorsett E, Greenlee W, Lohr N, Hoffsommer R, Joshua H, Ruyle W, Rothrock J, Aster S, Maycock A, Robinson F, Hirschmann R, Sweet C, Ulm E, Gross D, Vassil T, Stone C (1980). "A new class of angiotensin-converting enzyme inhibitors.". Nature 288 (5788): 280-3. PMID 6253826. 
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[edit] See also

v • d • e
Agents acting on the renin-angiotensin system (C09)
ACE inhibitors
Angiotensin II receptor antagonists (AIIRA)
Renin inhibitors