PharmGKB: The Pharmacogenomics Knowledge Base

Drug/Small Molecule:
lisinopril

2D structure

Overview

Generic Names: lisinopril
Trade Names: Acercomp; Inhibril; Linopril; Lisinopril Dihydrate; Lisipril; Lysinopril; Noperten; Presiten; Prinivil; Prinzide; Renacor; Sinopril; Zestoretic; Zestril
Brand Mixtures: Prinzide (Hydrochlorothiazide + Lisinopril); Zestoretic Tab 10/12.5mg (Hydrochlorothiazide + Lisinopril); Zestoretic Tab 20/12.5mg (Hydrochlorothiazide + Lisinopril); Zestoretic Tab 20/25mg (Hydrochlorothiazide + Lisinopril)
PharmGKB Accession Id: PA450242

Description

One of the angiotensin-converting enzyme inhibitors (ACE inhibitors), orally active, that has been used in the treatment of hypertension and congestive heart failure. PubChem (source: Drug Bank)

Indication

For the treatment of hypertension, heart failure and acute myocardial infarction. It may be used alone or in combination with thiazide diuretics (source: Drug Bank)

ATC Therapeutic Category

  • C09AA:ACE inhibitors, plain

Pharmacology, Interactions, and Contraindications

Mechanism Of Action

Lisinopril competes with angiotensin I for its binding site on the angiotensin-converting enzyme (ACE), an enzyme which converts angiotensin I to angiotensin II. As angiotensin II is a vasoconstrictor and a negative feedback mediator for renin activity, lower angiotensin II plasma levels result in decreased blood pressure and increased plasma renin activity. Baroreceptor reflex mechanisms, stimulated by the fall in blood pressure, release kininase II, an enzyme identical to ACE that degrades bradykinin, a vasodilator. (source: Drug Bank)

Pharmacology

Lisinopril, an angiotensin-converting enzyme (ACE) inhibitor, is used to treat hypertension, congestive heart failure (CHF), postmyocardial infarction, and diabetic nephropathy or retinopathy. Although it is the lysine ester of enalaprilat, the active form of the prodrug enalapril, lisinopril is active unchanged. (source: Drug Bank)

Food Interactions

Avoid alcohol.
Avoid excess salt/sodium unless otherwise instructed by your physician.
Avoid natural licorice.
Avoid salt substitutes containing potassium.
Take without regard to meals. (source: Drug Bank)

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Lisinopril does not undergo metabolism and is excreted unchanged entirely in the urine (source: Drug Bank)

Protein Binding

Lisinopril does not appear to be bound to other serum proteins (source: Drug Bank)

Absorption

Approximately 25%, but widely variable between individuals (6 to 60%) (source: Drug Bank)

Toxicity

hypotension, LD<sub>50</sub>= 2000 mg/kg(orally in rat) (source: Drug Bank)

Isomeric SMILES Code:

c1ccc(cc1)CC[C@@H](C(=O)O)N[C@@H](CCCCN)C(=O)N2CCC[C@H]2C(=O)O (source: Drug Bank)

Curated Annotations (Curated Annotation)

  1. rs5065 at chr1:11828655 in CLCN6, NPPA
    This variant has been associated with modification of antihypertensive medication effects on blood pressure and cardiovascular disease.
    Variant Name:
    NPPA:T2238C
    Related Drugs:
    amlodipine, chlorthalidone, doxazosin, lisinopril
    Related Diseases:
    Cardiovascular Diseases, Coronary Disease, Stroke
    Evidence:
    PMID:18212314
  2. rs699 at chr1:228912417 in AGT
    The AGT:Met235Thr variant was not associated with response to antihypertensives in a study of 97 hypertensive British individuals.
    Variant Name:
    AGT M235T, AGT:Met235Thr
    Related Drugs:
    atenolol, lisinopril, nifedipine
    Related Diseases:
    Hypertension
    Evidence:
    PMID:8728305
  3. rs5182 at chr3:149942085 in AGTR1
    The C allele carriers tend to have reduced risk of myocardial infarction in patients taking ACE inhibitors.
    Variant Name:
    AGTR1: 573C/T; 573C>T
    Related Drugs:
    Ace Inhibitors, Plain, captopril, enalapril, fosinopril, imidapril, lisinopril
    Related Diseases:
    Hypertension, Myocardial Infarction, Stroke
    Evidence:
    PMID:18347611
Variant names are different names that have been used in the literature and other resources to refer to the same variant.

The following genes are in curated knowledge about this drug.

  Gene Relationship Evidence
Phenotype data available Genotype Data Available Literature annotations available Has annotations
ACE
  •   
  • PD
  •   
  • FA
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
ADD1
  • CO
  •   
  •   
  •   
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
AGT
  •   
  • PD
  •   
  •   
  • GN
Publications, Variants
Phenotype data available Genotype Data Available Literature annotations available Not annotated
AGTR1
  • CO
  • PD
  •   
  •   
  • GN
Publications, Variants
No phenotype data Genotype Data Available No literature annotations Not annotated
CLCN6
  •   
  •   
  •   
  •   
  •   
Variants
No phenotype data No genotype data Literature annotations available Not annotated
NPPA
  • CO
  •   
  •   
  •   
  • GN
Publications, Variants

A list of non-curated publications that mention this drug along with other genes is available.

Drug Targets

Gene Description
ACE Uncurated Annotation (source: Drug Bank)
AGT Uncurated Annotation (source: Drug Bank)

A list of non-curated publications that mention this drug along with other drugs is available.

Drug Interactions

Drug Description
amiloride Uncurated Annotation Increased risk of hyperkaliemia (source: Drug Bank)
clozapine Uncurated Annotation Increases the effect and toxicity of clozapine (source: Drug Bank)
lithium Uncurated Annotation The ACE inhibitor increases serum levels of lithium (source: Drug Bank)
potassium Uncurated Annotation Increased risk of hyperkaliemia (source: Drug Bank)
spironolactone Uncurated Annotation Increased risk of hyperkaliemia (source: Drug Bank)
tizanidine Uncurated Annotation Tizanidine increases the risk of hypotension with the ACE inhibitor (source: Drug Bank)
triamterene Uncurated Annotation Increased risk of hyperkaliemia (source: Drug Bank)

Curated Information

The following diseases are in curated knowledge about this drug.

  Disease Relationship Evidence
No phenotype data No genotype data Literature annotations available Not annotated
Angioedema
  •   
  •   
  •   
  •   
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
Cardiovascular Diseases
  • CO
  •   
  •   
  •   
  • GN
Publications, Variants
No phenotype data No genotype data Literature annotations available Not annotated
Coronary Disease
  • CO
  •   
  •   
  •   
  • GN
Publications, Variants
No phenotype data No genotype data Literature annotations available Not annotated
Cough
  •   
  •   
  •   
  •   
  • GN
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Death
  • CO
  •   
  •   
  •   
  • GN
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Diabetes Mellitus, Type 1
  •   
  • PD
  •   
  •   
  • GN
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Heart Failure
  • CO
  •   
  •   
  •   
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
Hypertension
  • CO
  • PD
  •   
  •   
  • GN
Publications, Variants
Phenotype data available Genotype Data Available Literature annotations available Not annotated
Myocardial Infarction
  • CO
  • PD
  •   
  •   
  • GN
Publications, Variants
Phenotype data available No genotype data Literature annotations available Not annotated
Stroke
  • CO
  • PD
  •   
  •   
  • GN
Publications, Variants

Non-Curated Information

A list of non-curated publications that mention this drug along with other diseases is available.

LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB00722
KEGG Drug ID:
D00362
PubChem Compound ID:
5362119
PubChem Substance ID:
205105

Common Searches

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Non-Curated Publications

A list of non-curated publications that mention this drug is available.

PharmGKB integrates drug information from different sources: DrugBank, Open Eye Scientific Software.
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