Lisinopril


Description

Lisinopril is a potent, competitive inhibitor of angiotensin-converting enzyme (ACE), the enzyme responsible for the conversion of angiotensin I (ATI) to angiotensin II (ATII). ATII regulates blood pressure and is a key component of the renin-angiote...

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Pharmacology

Indication

For the treatment of hypertension and symptomatic congestive heart failure. May be used in conjuncti... Read more

Pharmacodynamic

Lisinopril is an orally active ACE inhibitor that antagonizes the effect of the RAAS. The RAAS is a... Read more

Mechanismofaction

There are two isoforms of ACE: the somatic isoform, which exists as a glycoprotein comprised of a si... Read more

Absorption

Approximately 25%, but widely variable between individuals (6 to 60%) in all doses tested (5-80 mg);... Read more

Proteinbinding

Lisinopril does not appear to be bound to serum proteins other than ACE.

Volumeofdistribution

Information currently not available.

Clearance

10 L/h [child weighting 30 kg receiving doses of 0.1 to 0.2 mg/kg]

Halflife

Effective half life of accumulation following multiple dosing is 12 hours.

Routeofelimination

Lisinopril does not undergo metabolism and is excreted unchanged entirely in the urine.

Toxicity

Symptoms of overdose include severe hypotension, electrolyte disturbances, and renal failure. LD Read more


Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Dizziness US
  • Kind: experimental
    • Percent: 12-19%
  • Clinical Trial
    Hypotension US
  • Kind: experimental
    • Percent: 7-11%
  • Clinical Trial
    Creatinine increased US
  • Kind: experimental
    • Percent: 7-10%
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 8%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Syncope US
  • Kind: experimental
    • Percent: 5-7%
  • Clinical Trial
    Hyperkalemia US
  • Kind: experimental
    • Percent: 4-6%
  • Clinical Trial
    Hypotension US
  • Kind: experimental
    • Percent: 5%
  • Clinical Trial
    Headache US
  • Kind: experimental
    • Percent: 5%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 4%
  • Clinical Trial
    Headache US
  • Kind: experimental
    • Percent: 4%
  • Clinical Trial
    Fatigue US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Cough US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Cough US
  • Kind: experimental
    • Percent: 3%
  • Clinical Trial
    Diarrhea US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Orthostatic effects US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Asthenia US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Paresthesia US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Muscle Cramps US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Upper Respiratory Infection US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Pancreatitis US
  • Kind: experimental
    • Percent: ≥1%
  • Clinical Trial
    Constipation US
  • Kind: experimental
    • Percent: ≥1%
  • Clinical Trial
    Orthostatic effects US
  • Kind: experimental
    • Percent: ≥1%
  • Clinical Trial
    Pancreatitis US
  • Kind: experimental
    • Percent: ≥1%
  • Clinical Trial
    Flatulence US
  • Kind: experimental
    • Percent: ≥1%
  • Clinical Trial
    Dry Mouth US
  • Kind: experimental
    • Percent: ≥1%
  • Clinical Trial
    Constipation US
  • Kind: experimental
    • Percent: ≥1%
  • Clinical Trial
    Flatulence US
  • Kind: experimental
    • Percent: ≥1%
  • Clinical Trial
    Renal Dysfunction US
  • Kind: experimental
    • Percent: 1%
  • Clinical Trial
    Fatigue US
  • Kind: experimental
    • Percent: ≥1%
  • Clinical Trial
    Asthenia US
  • Kind: experimental
    • Percent: ≥1%
  • Clinical Trial
    Orthostatic effects US
  • Kind: experimental
    • Percent: ≥1%
  • Clinical Trial
    Fatigue US
  • Kind: experimental
    • Percent: ≥1%
  • Clinical Trial
    Asthenia US
  • Kind: experimental
    • Percent: ≥1%
  • Clinical Trial
    Cutaneous pseudolymphoma US
  • Kind: experimental
    • Percent: 0.3-1%
  • Clinical Trial
    Diaphoresis US
  • Kind: experimental
    • Percent: 0.3-1%
  • Clinical Trial
    Skin Inflammation US
  • Kind: experimental
    • Percent: 0.3-1%
  • Clinical Trial
    Pruritus US
  • Kind: experimental
    • Percent: 0.3-1%
  • Clinical Trial
    Flushing US
  • Kind: experimental
    • Percent: 0.3-1%
  • Clinical Trial
    Angioedema of the face US
  • Kind: experimental
    • Percent: 0.3-1%
  • Clinical Trial
    Urinary Tract Infection US
  • Kind: experimental
    • Percent: 0.3-1%
  • Clinical Trial
    Otalgia US
  • Kind: experimental
    • Percent: 0.3-1%
  • Clinical Trial
    Tinnitus US
  • Kind: experimental
    • Percent: 0.3-1%
  • Clinical Trial
    Blurred vision US
  • Kind: experimental
    • Percent: 0.3-1%
  • Clinical Trial
    Angioedema of larynx US
  • Kind: experimental
    • Percent: 0.3-1%
  • Clinical Trial
    Angioedema of glottis US
  • Kind: experimental
    • Percent: 0.3-1%
  • Clinical Trial
    Angioedema of tongue US
  • Kind: experimental
    • Percent: 0.3-1%
  • Clinical Trial
    Angioedema of extremities US
  • Kind: experimental
    • Percent: 0.3-1%
  • Clinical Trial
    Angioedema of lips US
  • Kind: experimental
    • Percent: 0.3-1%
  • Clinical Trial
    Pulmonary Congestion US
  • Kind: experimental
    • Percent: 0.3-1%
  • Clinical Trial

    Contraindications

    • Regions: US
    • Patient Conditions:
        • Name: Hereditary or idiopathic angioedema
        • Drugbank Id: DBCOND0107806
    • Regions: US
    • Patient Conditions:
        • Name: Angioedema
        • Drugbank Id: DBCOND0013604
    • Hypersensitivity:
      • Angiotensin-Converting Enzyme Inhibitors
    • Regions: US
    • Regions: US
    • Patient Conditions:
        • Name: Diabetes
        • Drugbank Id: DBCOND0022048
    • With Drugs Coadmin:
        • Name: Aliskiren
        • Drugbank Id: DB09026

    Food Interactions

    • Herbs that may attenuate the antihypertensive effect of lisinopril include: bayberry, blue cohash, cayenne, ephedra, ginger, ginseng (American), kola and licorice.
    • High salt intake may attenuate the antihypertensive effect of lisinopril.
    • Lisinopril decreases the excretion of potassium. Salt substitutes containing potassium increase the risk of hyperkalemia.
    • Take without regard to meals.

    Interactions

    Type in a drug name to check for interaction with Lisinopril

    1-benzylimidazole may decrease the antihypertensive activities of Lisinopril.
    2,5-Dimethoxy-4-ethylamphetamine may decrease the antihypertensive activities of Lisinopril.
    2,5-Dimethoxy-4-ethylthioamphetamine may decrease the antihypertensive activities of Lisinopril.
    4-Bromo-2,5-dimethoxyamphetamine may decrease the antihypertensive activities of Lisinopril.
    4-Methoxyamphetamine may decrease the antihypertensive activities of Lisinopril.
    5-methoxy-N,N-dimethyltryptamine may decrease the antihypertensive activities of Lisinopril.
    7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the hypotensive activities of Lisinopril.
    Lisinopril may decrease the excretion rate of Abacavir which could result in a higher serum level.
    Abediterol may decrease the antihypertensive activities of Lisinopril.
    Acarbose may decrease the excretion rate of Lisinopril which could result in a higher serum level.
    The risk or severity of hyperkalemia can be increased when Lisinopril is combined with Acebutolol.
    The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Aceclofenac is combined with Lisinopril.
    The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Acemetacin is combined with Lisinopril.
    Acepromazine may decrease the antihypertensive activities of Lisinopril.
    Acetaminophen may decrease the excretion rate of Lisinopril which could result in a higher serum level.
    Acetazolamide may increase the excretion rate of Lisinopril which could result in a lower serum level and potentially a reduction in efficacy.
    The therapeutic efficacy of Lisinopril can be decreased when used in combination with Acetylsalicylic acid.
    Lisinopril may decrease the excretion rate of Aclidinium which could result in a higher serum level.
    Lisinopril may decrease the excretion rate of Acrivastine which could result in a higher serum level.
    Acyclovir may decrease the excretion rate of Lisinopril which could result in a higher serum level.

    References

    • 1 . Abdelmalek MF, Douglas DD: Lisinopril-induced isolated visceral angioedema: review of ACE-inhibitor-induced small bowel angioedema. Dig Dis Sci. 1997 Apr;42(4):847-50. [PubMed: 9125659]
    • 2 . Hasslacher C: Influence of the ACE inhibitor lisinopril on blood pressure, metabolism, and renal function parameter in hypertensive type II diabetic patients: a postmarketing surveillance study. J Diabetes Complications. 1996 May-Jun;10(3):136-8. [PubMed: 8807458]
    • 3 . Nielsen SE, Sugaya T, Tarnow L, Lajer M, Schjoedt KJ, Astrup AS, Baba T, Parving HH, Rossing P: Tubular and glomerular injury in diabetes and the impact of ACE inhibition. Diabetes Care. 2009 Sep;32(9):1684-8. doi: 10.2337/dc09-0429. Epub 2009 Jun 5. [PubMed: 19502542]
    • 4 . Patchett AA, Harris E, Tristram EW, Wyvratt MJ, Wu MT, Taub D, Peterson ER, Ikeler TJ, ten Broeke J, Payne LG, Ondeyka DL, Thorsett ED, Greenlee WJ, Lohr NS, Hoffsommer RD, Joshua H, Ruyle WV, Rothrock JW, Aster SD, Maycock AL, Robinson FM, Hirschmann R, Sweet CS, Ulm EH, Gross DM, Vassil TC, Stone CA: A new class of angiotensin-converting enzyme inhibitors. Nature. 1980 Nov 20;288(5788):280-3. [PubMed: 6253826]

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