Drug/Small Molecule:
propranolol

PharmGKB contains no dosing guidelines for this drug/small molecule. To report known genotype-based dosing guidelines, or if you are interested in developing guidelines, click here.

PharmGKB annotates drug labels containing pharmacogenetic information approved by the US Food and Drug Administration (FDA), European Medicines Agency (EMA) and the Pharmaceuticals and Medical Devices Agency, Japan (PMDA). PharmGKB annotations provide a brief summary of the PGx in the label, an excerpt from the label and a downloadable highlighted label PDF file. A list of genes and phenotypes found within the label is mapped to label section headers and listed at the end of each annotation. PharmGKB also attempts to interpret the level of action implied in each label with the "PGx Level" tag.

Sources:

  • FDA Information is gathered from the FDA's "Table of Pharmacogenomic Biomarkers in Drug Labels" and from FDA-approved labels brought to our attention. Please note that drugs may be removed from or added to the FDA's Table without our knowledge. We periodically check the Table for changes and update PharmGKB accordingly. Drugs listed on the Table to our knowledge are tagged with the Biomarker icon. A drug label that has been removed from the Table will not have the Biomarker icon but will continue to have an annotation on PharmGKB stating the label has been removed from the FDA's Table. We acquire label PDF files from DailyMed.
  • EMA European Public Assessment Reports (EPARs) that contain PGx information were identified from [Article:24433361] and also by searching for drugs for which we have PGx-containing FDA drug labels.

We welcome any information regarding drug labels containing PGx information approved by the FDA, EMA, PMDA or other Medicine Agencies around the world - please contact feedback.



last updated 10/25/2013

FDA Label for propranolol and CYP2D6

Informative PGx

Summary

Propranolol is metabolized primarily by CYP2D6. CYP1A2 and CYP2C19 may also play a role in propranolol metabolism. The drug label states that proranolol should be used with caution when co-administered with drugs that have an affect on CYP2D6, 1A2, or 2C19 metabolic pathways. Co-administration of such drugs with propranolol may lead to clinically relevant drug interactions and changes on its efficacy and/or toxicity.

Annotation

Propanolol is a beta-blocker which is used for treatment of various conditions including hypertension, angina pectoris and migraine.

Excerpts from the propanolol drug label:

In-vitro studies have indicated that the aromatic hydroxylation of propranolol is catalyzed mainly by polymorphic CYP2D6. Side-chain oxidation is mediated mainly by CYP1A2 and to some extent by CYP2D6. 4-hydroxy propranolol is a weak inhibitor of CYP2D6.
Propranolol is also a substrate of CYP2C19 and a substrate for the intestinal efflux transporter, p-glycoprotein (p-gp). Studies suggest however that p-gp is not dose-limiting for intestinal absorption of propranolol in the usual therapeutic dose range.

In healthy subjects, no difference was observed between CYP2D6 extensive metabolizers (EMs) and poor metabolizers (PMs) with respect to oral clearance or elimination half-life. Partial clearance of 4-hydroxy propranolol was significantly higher and naphthyloxyactic acid was significantly lower in EMs than PMs.

Blood levels and/or toxicity of propranolol may be increased by co-administration with substrates or inhibitors of CYP2D6, such as amiodarone, cimetidine, delavudin, fluoxetine, paroxetine, quinidine, and ritonavir. No interactions were observed with either ranitidine or lansoprazole.

Caution should be exercised when Inderal LA is administered with drugs that have an affect on CYP2D6, 1A2, or 2C19 metabolic pathways. Co-administration of such drugs with propranolol may lead to clinically relevant drug interactions and changes on its efficacy and/or toxicity.

For the complete drug label text with sections containing pharmacogenetic information highlighted, see the Propanolol drug label.

*Disclaimer: The contents of this page have not been endorsed by the FDA and are the sole responsibility of PharmGKB.

Full label available at DailyMed

Genes and/or phenotypes found in this label

  • Cardiomyopathy, Dilated
    • Indications & usage section, Precautions section
    • source: PHONT
  • Cardiomyopathy, Hypertrophic
    • Precautions section
    • source: PHONT
  • Heart Failure
    • Warnings section, Adverse reactions section
    • source: PHONT
  • CYP1A2
    • Drug interactions section, Clinical pharmacology section, Precautions section, metabolism/PK
    • source: FDA Label
  • CYP2C19
    • Drug interactions section, Clinical pharmacology section, Precautions section, metabolism/PK
    • source: FDA Label
  • CYP2D6
    • Drug interactions section, Clinical pharmacology section, Precautions section, metabolism/PK
    • source: FDA Label

last updated 06/26/2014

European Medicines Agency (EMA) Label for propranolol and CYP2D6

Informative PGx

Summary

The EMA European Public Assessment Report (EPAR) for propranolol hydrochloride (Hemangiol) gives information regarding the metabolism of the drug by three different routes which varies between individuals, but that no difference in oral clearance or elimination is observed between CYP2D6 extensive and poor metabolizers.

Annotation

The enzymes CYP2D6, CYP1A2 and CYP2C19 enzymes are involved in metabolism of propanolol. No difference in oral clearance or elimination is observed between CYP2D6 extensive and poor metabolizers.

Excerpt from the propranolol hydrochloride (Hemangiol) EPAR:

Propranolol is metabolized through three primary routes: aromatic hydroxylation (mainly 4-hydroxylation), N-dealkylation followed by further side-chain oxidation, and direct glucuronidation. The percentage contributions of these routes to total metabolism are 42%, 41% and 17%, respectively, but with considerable variability between individuals. The four major final metabolites are propranolol glucuronide, naphthyloxylactic acid and glucuronic acid, and sulfate conjugates of 4-hydroxypropranolol. In vitro studies indicated that CYP2D6 (aromatic hydroxylation), CYP1A2 (chain oxidation) and to a less extent CYP2C19 were involved in propranolol metabolism. In healthy subjects, no difference was observed between CYP2D6 extensive metabolizers and poor metabolizers with respect to oral clearance or elimination half-life.

For the complete drug label text with sections containing pharmacogenetic information highlighted, see the propranolol EMA drug label.

*Disclaimer: The contents of this page have not been endorsed by the EMA and are the sole responsibility of PharmGKB.

Genes and/or phenotypes found in this label

  • CYP1A2
    • Pharmacokinetics section, metabolism/PK
    • source: European Medicines Agency (EMA) Label
  • CYP2C19
    • Pharmacokinetics section, metabolism/PK
    • source: European Medicines Agency (EMA) Label
  • CYP2D6
    • Pharmacokinetics section, metabolism/PK
    • source: European Medicines Agency (EMA) Label

PharmGKB contains no Clinical Variants that meet the highest level of criteria.

To see more Clinical Variants with lower levels of criteria, click the button at the bottom of the page.

Disclaimer: The PharmGKB's clinical annotations reflect expert consensus based on clinical evidence and peer-reviewed literature available at the time they are written and are intended only to assist clinicians in decision-making and to identify questions for further research. New evidence may have emerged since the time an annotation was submitted to the PharmGKB. The annotations are limited in scope and are not applicable to interventions or diseases that are not specifically identified.

The annotations do not account for individual variations among patients, and cannot be considered inclusive of all proper methods of care or exclusive of other treatments. It remains the responsibility of the health-care provider to determine the best course of treatment for a patient. Adherence to any guideline is voluntary, with the ultimate determination regarding its application to be made solely by the clinician and the patient. PharmGKB assumes no responsibility for any injury or damage to persons or property arising out of or related to any use of the PharmGKB clinical annotations, or for any errors or omissions.

? = Mouse-over for quick help

This is a non-comprehensive list of genetic tests with pharmacogenetics relevance, typically submitted by the manufacturer and manually curated by PharmGKB. The information listed is provided for educational purposes only and does not constitute an endorsement of any listed test or manufacturer.

A more complete listing of genetic tests is found at the Genetic Testing Registry (GTR).

PGx Test Variants Assayed Gene?
Spartan RX CYP2C19 System CYP2C19*17, CYP2C19*2, CYP2C19*3 , rs12248560 , rs4986893 , rs4244285

The table below contains information about pharmacogenomic variants on PharmGKB. Please follow the link in the "Variant" column for more information about a particular variant. Each link in the "Variant" column leads to the corresponding PharmGKB Variant Page. The Variant Page contains summary data, including PharmGKB manually curated information about variant-drug pairs based on individual PubMed publications. The PMIDs for these PubMed publications can be found on the Variant Page.

The tags in the first column of the table indicate what type of information can be found on the corresponding Variant Page.

Links in the "Gene" column lead to PharmGKB Gene Pages.

List of all propranolol variant annotations

Gene ? Variant?
(142)
Alternate Names ? Drugs ? Alleles ?
(+ chr strand)
Function ? Amino Acid?
Translation
VIP No VIP available No VIP available CYP2C19 *2A N/A N/A N/A
VIP No VIP available No VIP available CYP2C19 *3A N/A N/A N/A
No VIP available CA VA CYP2D6 *1 N/A N/A N/A
No VIP available CA VA CYP2D6 *10 N/A N/A N/A
No VIP available No Clinical Annotations available VA
CYP2D6 poor metabolizer N/A N/A N/A
No VIP available No Clinical Annotations available VA
rs1065852 100C>T, 21917263G>A, 42526694G>A, 5190C>T, CYP2D6:100C>T, Pro34Ser, part of CYP2D6*4 and CYP2D6*10
G > A
Missense
Pro34Ser
rs4244285 24154G>A, 24154G>C, 47346080G>A, 47346080G>C, 681G>A, 681G>C, 96541616G>A, 96541616G>C, CYP2C19*2, CYP2C19:681G>A, CYP2C19:G681A, Pro227=
G > A
G > C
Synonymous
Pro227Pro
rs4986893 22948G>A, 47344874G>A, 636G>A, 96540410G>A, CYP2C19*3, CYP2C19:636G>A, CYP2C19:G636A, Trp212Ter
G > A
Stop Codon
Trp212null
VIP No Clinical Annotations available No Variant Annotations available
rs776746 12083G>A, 219-237G>A, 321-1G>A, 37303382C>T, 581-237G>A, 689-1G>A, 99270539C>T, CYP3A5*1, CYP3A5*3, CYP3A5*3C, CYP3A5:6986A>G, g.6986A>G, intron 3 splicing defect, rs776746 A>G
C > T
Acceptor
Alleles, Functions, and Amino Acid Translations are all sourced from dbSNP 142
2D structure from PubChem
provided by PubChem

Overview

Generic Names
  • Dl-Propranolol Hydrochloride
  • Propanalol
  • Propanolol
  • Propranalol
  • Propranolol Hcl
  • Propranolol Hydrochloride
  • R,S-Propranolol Hydrochloride
  • propranolol
Trade Names
  • Angilol
  • Apsolol
  • Avlocardyl
  • Bedranol
  • Beprane
  • Berkolol
  • Beta-Neg
  • Beta-Propranolol
  • Beta-Tablinen
  • Beta-Timelets
  • Betachron
  • Betalong
  • Cardinol
  • Caridolol
  • Corpendol
  • Deralin
  • Dociton
  • Duranol
  • Efektolol
  • Elbrol
  • Etalong
  • Euprovasin
  • Frekven
  • Inderal
  • Inderal La
  • Inderide
  • Indobloc
  • Innopran XL
  • Intermigran
  • Kemi S
  • Migrastat
  • Obsidan
  • Oposim
  • Prano-Puren
  • Propanix
  • Prophylux
  • Propranolol Hcl Intensol
  • Propranur
  • Proprasylyt
  • Pylapron
  • Rapynogen
  • Reducor
  • Reducor Line
  • Sagittol
  • Servanolol
  • Sloprolol
  • Sumial
  • Tesnol
Brand Mixture Names

PharmGKB Accession Id:
PA451145

Description

A widely used non-cardioselective beta-adrenergic antagonist. Propranolol is used in the treatment or prevention of many disorders including acute myocardial infarction, arrhythmias, angina pectoris, hypertension, hypertensive emergencies, hyperthyroidism, migraine, pheochromocytoma, menopause, and anxiety.

Source: Drug Bank

Indication

For the prophylaxis of migraine.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

Propranolol competes with sympathomimetic neurotransmitters such as catecholamines for binding at beta(1)-adrenergic receptors in the heart, inhibiting sympathetic stimulation. This results in a reduction in resting heart rate, cardiac output, systolic and diastolic blood pressure, and reflex orthostatic hypotension.

Source: Drug Bank

Pharmacology

Propranolol, the prototype of the beta-adrenergic receptor antagonists, is a competitive, nonselective beta-blocker similar to nadolol without intrinsic sympathomimetic activity. Propanolol is a racemic compound; the l-isomer is responsible for adrenergic blocking activity.

Source: Drug Bank

Food Interaction

Avoid alcohol.|Avoid natural licorice.|Take with food.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatic

Source: Drug Bank

Protein Binding

More than 90%

Source: Drug Bank

Absorption

Propranolol is almost completely absorbed from the GI tract; however, plasma concentrations attained are quite variable among individuals.

Source: Drug Bank

Half-Life

4 hours

Source: Drug Bank

Toxicity

Symptoms of overdose include bradycardia, cardiac failure, hypotension, and brochospasm. LD 50=565 mg/kg (orally in mice).

Source: Drug Bank

Route of Elimination

Propranolol is extensively metabolized with most metabolites appearing in the urine.

Source: Drug Bank

Volume of Distribution

  • 4 L

Source: Drug Bank

Chemical Properties

Chemical Formula

C16H21NO2

Source: Drug Bank

Isomeric SMILES

CC(C)NCC(COc1cccc2c1cccc2)O

Source: OpenEye

Canonical SMILES

CC(C)NCC(O)COC1=CC=CC2=CC=CC=C12

Source: Drug Bank

Average Molecular Weight

259.3434

Source: Drug Bank

Monoisotopic Molecular Weight

259.157228921

Source: Drug Bank

PharmGKB Curated Pathways

Pathways created internally by PharmGKB based primarily on literature evidence.

  1. Beta-agonist/Beta-blocker Pathway, Pharmacodynamics
    Simplified pharmacodynamic pathway of drug action on beta 2 adrenergic receptor in a stylized airway cell.

External Pathways

Links to non-PharmGKB pathways.

PharmGKB contains no links to external pathways for this drug. To report a pathway, click here.

Genes that are associated with this drug in PharmGKB's database based on (1) variant annotations, (2) literature review, (3) pathways or (4) information automatically retrieved from DrugBank, depending on the "evidence" and "source" listed below.

Curated Information ?

Drug Targets

Gene Description
ADRB1 (source: Drug Bank)
ADRB2 (source: Drug Bank)
ADRB3 (source: Drug Bank)
HTR1A (source: Drug Bank)
HTR1B (source: Drug Bank)

Drug Interactions

Drug Description
propranolol The beta-blocker, propranolol, may decrease symptoms of hypoglycemia. (source: Drug Bank)
propranolol Antagonism of action and increased effect of theophylline (source: Drug Bank)
propranolol Increased effect of both drugs (source: Drug Bank)
propranolol Increased effect of both drugs (source: Drug Bank)
propranolol The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
propranolol The beta-blocker, propranolol, may decrease symptoms of hypoglycemia. (source: Drug Bank)
propranolol Increases the effect of the beta-blocker (source: Drug Bank)
propranolol Cimetidine may increase the serum concentration of propranolol by decreasing its metabolism. (source: Drug Bank)
propranolol This SSRI increases the effect of the beta-blocker (source: Drug Bank)
propranolol The SSRI, citalopram, may increase the bradycardic effect of the beta-blocker, propranolol. (source: Drug Bank)
propranolol Increased hypertension when clonidine stopped (source: Drug Bank)
propranolol Increased hypertension when clonidine stopped (source: Drug Bank)
propranolol Ischemia with risk of gangrene (source: Drug Bank)
propranolol Ischemia with risk of gangrene (source: Drug Bank)
propranolol Increased risk of bradycardia (source: Drug Bank)
propranolol Increased risk of bradycardia (source: Drug Bank)
propranolol The beta-blocker increases toxicity of disopyramide (source: Drug Bank)
propranolol The beta-blocker, propranolol, may increase the toxicity of disopyramide. (source: Drug Bank)
propranolol Hypertension, then bradycardia (source: Drug Bank)
propranolol Hypertension, then bradycardia (source: Drug Bank)
propranolol Ischemia with risk of gangrene (source: Drug Bank)
propranolol Ischemia with risk of gangrene (source: Drug Bank)
propranolol The SSRI increases the effect of the beta-blocker (source: Drug Bank)
propranolol The SSRI, escitalopram, may increase the bradycardic effect of the beta-blocker, propranolol. (source: Drug Bank)
propranolol Antagonism (source: Drug Bank)
propranolol Antagonism (source: Drug Bank)
propranolol The SSRI increases the effect of the beta-blocker (source: Drug Bank)
propranolol The SSRI, fluoxetine, may increase the bradycardic effect of the beta-blocker, propranolol. (source: Drug Bank)
propranolol Antagonism (source: Drug Bank)
propranolol Antagonism (source: Drug Bank)
propranolol The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
propranolol The beta-blocker, propranolol, may decrease symptoms of hypoglycemia. (source: Drug Bank)
propranolol The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
propranolol The beta-blocker, propranolol, may decrease symptoms of hypoglycemia. (source: Drug Bank)
propranolol Increased effect of both drugs (source: Drug Bank)
propranolol Increased effect of both drugs (source: Drug Bank)
propranolol Risk of inhibition of renal prostaglandins (source: Drug Bank)
propranolol Risk of inhibition of renal prostaglandins (source: Drug Bank)
propranolol Risk of inhibition of renal prostaglandins (source: Drug Bank)
propranolol Risk of inhibition of renal prostaglandins (source: Drug Bank)
propranolol The beta-blocker, propranolol, may decrease symptoms of hypoglycemia. (source: Drug Bank)
propranolol The beta-blocker, propranolol, may decrease symptoms of hypoglycemia. (source: Drug Bank)
propranolol Possible hypertensive crisis (source: Drug Bank)
propranolol Possible hypertensive crisis (source: Drug Bank)
propranolol Propranolol increases the serum levels of cisapride (source: Drug Bank)
propranolol Propranolol increases the serum levels of cisapride (source: Drug Bank)
propranolol Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
propranolol Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
propranolol Ischemia with risk of gangrene (source: Drug Bank)
propranolol Ischemia with risk of gangrene (source: Drug Bank)
propranolol Antagonism (source: Drug Bank)
propranolol Antagonism (source: Drug Bank)
propranolol Antagonism of action and increased effect of theophylline (source: Drug Bank)
propranolol The SSRI increases the effect of the beta-blocker (source: Drug Bank)
propranolol The SSRI increases the effect of the beta-blocker (source: Drug Bank)
propranolol The barbiturate decreases the effect of the metabolized beta-blocker (source: Drug Bank)
propranolol The barbiturate decreases the effect of the metabolized beta-blocker (source: Drug Bank)
propranolol Antagonism (source: Drug Bank)
propranolol Risk of inhibition of renal prostaglandins (source: Drug Bank)
propranolol Risk of inhibition of renal prostaglandins (source: Drug Bank)
propranolol Risk of hypotension at the beginning of therapy (source: Drug Bank)
propranolol Risk of hypotension at the beginning of therapy (source: Drug Bank)
propranolol The barbiturate decreases the effect of metabolized beta-blocker (source: Drug Bank)
propranolol The barbiturate decreases the effect of metabolized beta-blocker (source: Drug Bank)
propranolol Propafenone increases the effect of the beta-blocker (source: Drug Bank)
propranolol Propafenone increases the effect of the beta-blocker (source: Drug Bank)
acetohexamide The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
acetohexamide The beta-blocker, propranolol, may decrease symptoms of hypoglycemia. (source: Drug Bank)
aminophylline Antagonism of action and increased effect of theophylline (source: Drug Bank)
aminophylline Antagonism of action and increased effect of theophylline (source: Drug Bank)
amobarbital The barbiturate decreases the effect of metabolized beta-blocker (source: Drug Bank)
amobarbital The barbiturate decreases the effect of metabolized beta-blocker (source: Drug Bank)
aprobarbital The barbiturate decreases the effect of metabolized beta-blocker (source: Drug Bank)
aprobarbital The barbiturate decreases the effect of metabolized beta-blocker (source: Drug Bank)
butabarbital The barbiturate decreases the effect of metabolized beta-blocker (source: Drug Bank)
butabarbital The barbiturate decreases the effect of metabolized beta-blocker (source: Drug Bank)
butalbital The barbiturate decreases the effect of metabolized beta-blocker (source: Drug Bank)
butalbital The barbiturate decreases the effect of metabolized beta-blocker (source: Drug Bank)
butethal The barbiturate decreases the effect of metabolized beta-blocker (source: Drug Bank)
butethal The barbiturate decreases the effect of metabolized beta-blocker (source: Drug Bank)
chlorpromazine Increased effect of both drugs (source: Drug Bank)
chlorpromazine Increased effect of both drugs (source: Drug Bank)
chlorpropamide The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
chlorpropamide The beta-blocker, propranolol, may decrease symptoms of hypoglycemia. (source: Drug Bank)
cimetidine Cimetidine increases the effect of the beta-blocker (source: Drug Bank)
cimetidine Cimetidine increases the effect of the beta-blocker (source: Drug Bank)
citalopram The SSRI increases the effect of the beta-blocker (source: Drug Bank)
citalopram The SSRI, citalopram, may increase the bradycardic effect of the beta-blocker, propranolol. (source: Drug Bank)
clonidine Increased hypertension when clonidine stopped (source: Drug Bank)
clonidine Increased hypertension when clonidine stopped (source: Drug Bank)
dihydroergotamine Ischemia with risk of gangrene (source: Drug Bank)
dihydroergotamine Ischemia with risk of gangrene (source: Drug Bank)
dihydroergotoxine Ischemia with risk of gangrene (source: Drug Bank)
dihydroergotoxine Ischemia with risk of gangrene (source: Drug Bank)
diltiazem Increased risk of bradycardia (source: Drug Bank)
diltiazem Increased risk of bradycardia (source: Drug Bank)
disopyramide The beta-blocker increases toxicity of disopyramide (source: Drug Bank)
disopyramide The beta-blocker increases toxicity of disopyramide (source: Drug Bank)
dyphylline Antagonism of action and increased effect of theophylline (source: Drug Bank)
dyphylline Antagonism of action and increased effect of theophylline (source: Drug Bank)
epinephrine Hypertension, then bradycardia (source: Drug Bank)
epinephrine Hypertension, then bradycardia (source: Drug Bank)
ergonovine Ischemia with risk of gangrene (source: Drug Bank)
ergonovine Ischemia with risk of gangrene (source: Drug Bank)
ergotamine Ischemia with risk of gangrene (source: Drug Bank)
ergotamine Ischemia with risk of gangrene (source: Drug Bank)
escitalopram The SSRI increases the effect of the beta-blocker (source: Drug Bank)
escitalopram The SSRI, escitalopram, may increase the bradycardic effect of the beta-blocker, propranolol. (source: Drug Bank)
fenoterol Antagonism (source: Drug Bank)
fenoterol Antagonism (source: Drug Bank)
fluoxetine The SSRI increases the effect of the beta-blocker (source: Drug Bank)
fluoxetine The SSRI, fluoxetine, may increase the bradycardic effect of the beta-blocker, propranolol. (source: Drug Bank)
formoterol Antagonism (source: Drug Bank)
formoterol Antagonism (source: Drug Bank)
glibenclamide The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
glibenclamide The beta-blocker, propranolol, may decrease symptoms of hypoglycemia. (source: Drug Bank)
gliclazide The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
gliclazide The beta-blocker, propranolol, may decrease symptoms of hypoglycemia. (source: Drug Bank)
glipizide The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
glipizide The beta-blocker, propranolol, may decrease symptoms of hypoglycemia. (source: Drug Bank)
glisoxepide The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
glisoxepide The beta-blocker, propranolol, may decrease symptoms of hypoglycemia. (source: Drug Bank)
glycodiazine The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
glycodiazine The beta-blocker, propranolol, may decrease symptoms of hypoglycemia. (source: Drug Bank)
haloperidol Increased effect of both drugs (source: Drug Bank)
haloperidol Increased effect of both drugs (source: Drug Bank)
heptabarbital The barbiturate decreases the effect of metabolized beta-blocker (source: Drug Bank)
heptabarbital The barbiturate decreases the effect of metabolized beta-blocker (source: Drug Bank)
hexobarbital The barbiturate decreases the effect of metabolized beta-blocker (source: Drug Bank)
hexobarbital The barbiturate decreases the effect of metabolized beta-blocker (source: Drug Bank)
hydralazine Increased effect of both drugs (source: Drug Bank)
hydralazine Increased effect of both drugs (source: Drug Bank)
ibuprofen Risk of inhibition of renal prostaglandins (source: Drug Bank)
ibuprofen Risk of inhibition of renal prostaglandins (source: Drug Bank)
indomethacin Risk of inhibition of renal prostaglandins (source: Drug Bank)
indomethacin Risk of inhibition of renal prostaglandins (source: Drug Bank)
isoproterenol Antagonism (source: Drug Bank)
isoproterenol Antagonism (source: Drug Bank)
l-methyldopa Possible hypertensive crisis (source: Drug Bank)
lidocaine The beta-blocker increases the effect and toxicity of lidocaine (source: Drug Bank)
lidocaine The beta-blocker, propranolol, may increase the effect and toxicity of lidocaine. (source: Drug Bank)
maprotiline Propranolol increases the serum levels of cisapride (source: Drug Bank)
maprotiline Propranolol increases the serum levels of cisapride (source: Drug Bank)
mesoridazine Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
mesoridazine Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
methohexital The barbiturate decreases the effect of metabolized beta-blocker (source: Drug Bank)
methohexital The barbiturate decreases the effect of metabolized beta-blocker (source: Drug Bank)
Methyldopa Possible hypertensive crisis (source: Drug Bank)
Methyldopa Possible hypertensive crisis (source: Drug Bank)
methylphenobarbital The barbiturate decreases the effect of metabolized beta-blocker (source: Drug Bank)
methylphenobarbital The barbiturate decreases the effect of metabolized beta-blocker (source: Drug Bank)
methysergide Ischemia with risk of gangrene (source: Drug Bank)
methysergide Ischemia with risk of gangrene (source: Drug Bank)
orciprenaline Antagonism (source: Drug Bank)
orciprenaline Antagonism (source: Drug Bank)
oxtriphylline Antagonism of action and increased effect of theophylline (source: Drug Bank)
oxtriphylline Antagonism of action and increased effect of theophylline (source: Drug Bank)
paroxetine The SSRI increases the effect of the beta-blocker (source: Drug Bank)
paroxetine The SSRI, paroxetine, may increase the bradycardic effect of the beta-blocker, propranolol. (source: Drug Bank)
pentobarbital The barbiturate decreases the effect of metabolized beta-blocker (source: Drug Bank)
pentobarbital The barbiturate decreases the effect of metabolized beta-blocker (source: Drug Bank)
phenobarbital The barbiturate decreases the effect of metabolized beta-blocker (source: Drug Bank)
phenobarbital The barbiturate decreases the effect of metabolized beta-blocker (source: Drug Bank)
pirbuterol Antagonism (source: Drug Bank)
pirbuterol Antagonism (source: Drug Bank)
piroxicam Risk of inhibition of renal prostaglandins (source: Drug Bank)
piroxicam Risk of inhibition of renal prostaglandins (source: Drug Bank)
prazosin Risk of hypotension at the beginning of therapy (source: Drug Bank)
prazosin Risk of hypotension at the beginning of therapy (source: Drug Bank)
primidone The barbiturate decreases the effect of metabolized beta-blocker (source: Drug Bank)
primidone The barbiturate decreases the effect of metabolized beta-blocker (source: Drug Bank)
procaterol Antagonism (source: Drug Bank)
procaterol Antagonism (source: Drug Bank)
propafenone Propafenone increases the effect of the beta-blocker (source: Drug Bank)
propafenone Propafenone may increase the effect of the beta-blocker, propranolol. (source: Drug Bank)
quinidine The barbiturate decreases the effect of metabolized beta-blocker (source: Drug Bank)
quinidine The barbiturate decreases the effect of metabolized beta-blocker (source: Drug Bank)
repaglinide The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
repaglinide The beta-blocker, propranolol, may decrease symptoms of hypoglycemia. (source: Drug Bank)
rifampin Rifampin decreases the effect of the metabolized beta-blocker (source: Drug Bank)
rifampin Rifampin may decrease the serum concentration of propranolol by increasing its metabolism. (source: Drug Bank)
rizatriptan Propranolol increases the effect and toxicity of rizatriptan (source: Drug Bank)
rizatriptan Propranolol increases the effect and toxicity of rizatriptan (source: Drug Bank)
salbutamol Antagonism (source: Drug Bank)
salbutamol Antagonism (source: Drug Bank)
salmeterol Antagonism (source: Drug Bank)
salmeterol Antagonism (source: Drug Bank)
secobarbital The barbiturate decreases the effect of metabolized beta-blocker (source: Drug Bank)
secobarbital The barbiturate decreases the effect of metabolized beta-blocker (source: Drug Bank)
sertraline The SSRI increases the effect of the beta-blocker (source: Drug Bank)
sertraline The SSRI, sertraline, may increase the bradycardic effect of the beta-blocker, propranolol. (source: Drug Bank)
talbutal The barbiturate decreases the effect of metabolized beta-blocker (source: Drug Bank)
talbutal The barbiturate decreases the effect of metabolized beta-blocker (source: Drug Bank)
terbutaline Antagonism (source: Drug Bank)
terbutaline Antagonism (source: Drug Bank)
theophylline Antagonism of action and increased effect of theophylline (source: Drug Bank)
theophylline Antagonism of action and increased effect of theophylline (source: Drug Bank)
thioridazine Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
thioridazine Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
tolazamide The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
tolazamide The beta-blocker, propranolol, may decrease symptoms of hypoglycemia. (source: Drug Bank)
tolbutamide The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
tolbutamide The beta-blocker, propranolol, may decrease symptoms of hypoglycemia. (source: Drug Bank)
verapamil Increased effect of both drugs (source: Drug Bank)
verapamil Increased effect of both drugs (source: Drug Bank)
propranolol The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
propranolol The beta-blocker, propranolol, may decrease symptoms of hypoglycemia. (source: Drug Bank)
propranolol Rifampin decreases the effect of the metabolized beta-blocker (source: Drug Bank)
propranolol Rifampin may decrease the serum concentration of propranolol by increasing its metabolism. (source: Drug Bank)
propranolol Increased risk of hypotension. Initiate concomitant therapy cautiously. (source: Drug Bank)
propranolol Terbinafine may reduce the metabolism and clearance of Propranolol. Consider alternate therapy or monitor for therapeutic/adverse effects of Propranolol if Terbinafine is initiated, discontinued or dose changed. (source: Drug Bank)
propranolol Antagonism (source: Drug Bank)
propranolol Antagonism (source: Drug Bank)
propranolol Antagonism of action and increased effect of theophylline (source: Drug Bank)
propranolol Antagonism of action and increased effect of theophylline (source: Drug Bank)
propranolol Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
propranolol Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
propranolol The p-glycoprotein inhibitor, Propranolol, may increase the bioavailability of oral Topotecan. A clinically significant effect is also expected with IV Topotecan. Concomitant therapy should be avoided. (source: Drug Bank)

Curated Information ?

Relationships from National Drug File - Reference Terminology (NDF-RT)

May Treat
Contraindicated With

Publications related to propranolol: 42

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Challenges in pharmacogenetics. European journal of clinical pharmacology. 2013. Cascorbi Ingolf, et al. PubMed
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PharmGKB summary: very important pharmacogene information for CYP3A5. Pharmacogenetics and genomics. 2012. Lamba Jatinder, et al. PubMed
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PharmGKB summary: very important pharmacogene information for cytochrome P450, family 2, subfamily C, polypeptide 19. Pharmacogenetics and genomics. 2011. Scott Stuart A, et al. PubMed
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Nodular regenerative liver hyperplasia as a complication of azathioprine-containing immunosuppressive treatment for Crohn's disease. Immunopharmacology and immunotoxicology. 2011. Błogowski Wojciech, et al. PubMed
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Very important pharmacogene summary: ABCB1 (MDR1, P-glycoprotein). Pharmacogenetics and genomics. 2011. Hodges Laura M, et al. PubMed
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Systematic review of pharmacoeconomic studies of pharmacogenomic tests. Pharmacogenomics. 2010. Beaulieu Mathieu, et al. PubMed
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beta-blocker therapy and heart rate control during exercise testing in the general population: role of a common G-protein beta-3 subunit variant. Pharmacogenomics. 2010. Dörr Marcus, et al. PubMed
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Effect of catechol-O-methyltransferase polymorphism on response to propranolol therapy in chronic musculoskeletal pain: a randomized, double-blind, placebo-controlled, crossover pilot study. Pharmacogenetics and genomics. 2010. Tchivileva Inna E, et al. PubMed
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Very important pharmacogene summary ADRB2. Pharmacogenetics and genomics. 2010. Litonjua Augusto A, et al. PubMed
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Warfarin interactions with substances listed in drug information compendia and in the FDA-approved label for warfarin sodium. Clinical pharmacology and therapeutics. 2009. Anthony M, et al. PubMed
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Histone deacetylase inhibitors induce a very broad, pleiotropic anticancer drug resistance phenotype in acute myeloid leukemia cells by modulation of multiple ABC transporter genes. Clinical cancer research : an official journal of the American Association for Cancer Research. 2009. Hauswald Stefanie, et al. PubMed
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Genetic determinants of response to clopidogrel and cardiovascular events. The New England journal of medicine. 2009. Simon Tabassome, et al. PubMed
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Redox regulation of multidrug resistance in cancer chemotherapy: molecular mechanisms and therapeutic opportunities. Antioxidants & redox signaling. 2009. Kuo Macus Tien. PubMed
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Genetic variation in the CYP2D6 gene is associated with a lower heart rate and blood pressure in beta-blocker users. Clinical pharmacology and therapeutics. 2009. Bijl M J, et al. PubMed
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Several major antiepileptic drugs are substrates for human P-glycoprotein. Neuropharmacology. 2008. Luna-Tortós Carlos, et al. PubMed
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Functional pharmacogenetics/genomics of human cytochromes P450 involved in drug biotransformation. Analytical and bioanalytical chemistry. 2008. Zanger Ulrich M, et al. PubMed
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Structure, function and regulation of P-glycoprotein and its clinical relevance in drug disposition. Xenobiotica; the fate of foreign compounds in biological systems. 2008. Zhou S-F. PubMed
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A GRK5 polymorphism that inhibits beta-adrenergic receptor signaling is protective in heart failure. Nature medicine. 2008. Liggett Stephen B, et al. PubMed
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Polymorphisms in the drug transporter gene ABCB1 predict antidepressant treatment response in depression. Neuron. 2008. Uhr Manfred, et al. PubMed
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Citalopram enantiomers in plasma and cerebrospinal fluid of ABCB1 genotyped depressive patients and clinical response: a pilot study. Pharmacological research : the official journal of the Italian Pharmacological Society. 2008. Nikisch Georg, et al. PubMed
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Cobalamin potentiates vinblastine cytotoxicity through downregulation of mdr-1 gene expression in HepG2 cells. Cellular physiology and biochemistry : international journal of experimental cellular physiology, biochemistry, and pharmacology. 2007. Marguerite Véronique, et al. PubMed
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Mechanism of inhibition of P-glycoprotein mediated efflux by vitamin E TPGS: influence on ATPase activity and membrane fluidity. Molecular pharmaceutics. 2007. Collnot Eva-Maria, et al. PubMed
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Gefitinib modulates the function of multiple ATP-binding cassette transporters in vivo. Cancer research. 2006. Leggas Markos, et al. PubMed
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Impact of P-glycoprotein on clopidogrel absorption. Clinical pharmacology and therapeutics. 2006. Taubert Dirk, et al. PubMed
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Single nucleotide polymorphisms in human P-glycoprotein: its impact on drug delivery and disposition. Expert opinion on drug delivery. 2006. Dey Surajit. PubMed
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Influence of lipid lowering fibrates on P-glycoprotein activity in vitro. Biochemical pharmacology. 2004. Ehrhardt Manuela, et al. PubMed
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Interactions of human P-glycoprotein with simvastatin, simvastatin acid, and atorvastatin. Pharmaceutical research. 2004. Hochman Jerome H, et al. PubMed
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Polymorphisms in human MDR1 (P-glycoprotein): recent advances and clinical relevance. Clinical pharmacology and therapeutics. 2004. Marzolini Catia, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Dose-response relationships of propranolol in Chinese subjects with different CYP2D6 genotypes. Journal of the Chinese Medical Association : JCMA. 2003. Huang Chin-Wei, et al. PubMed
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Genetic polymorphisms of the human MDR1 drug transporter. Annual review of pharmacology and toxicology. 2003. Schwab Matthias, et al. PubMed
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Med-psych drug-drug interactions update. Psychosomatics. 2002. Armstrong Scott C, et al. PubMed
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Interaction of omeprazole, lansoprazole and pantoprazole with P-glycoprotein. Naunyn-Schmiedeberg's archives of pharmacology. 2001. Pauli-Magnus C, et al. PubMed
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CYP1A2 and CYP2D6 4-hydroxylate propranolol and both reactions exhibit racial differences. The Journal of pharmacology and experimental therapeutics. 2000. Johnson J A, et al. PubMed
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The role of intestinal P-glycoprotein in the interaction of digoxin and rifampin. The Journal of clinical investigation. 1999. Greiner B, et al. PubMed
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Biochemical, cellular, and pharmacological aspects of the multidrug transporter. Annual review of pharmacology and toxicology. 1999. Ambudkar S V, et al. PubMed
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The glucuronidation of opioids, other xenobiotics, and androgens by human UGT2B7Y(268) and UGT2B7H(268). Drug metabolism and disposition: the biological fate of chemicals. 1998. Coffman B L, et al. PubMed
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Competitive, non-competitive and cooperative interactions between substrates of P-glycoprotein as measured by its ATPase activity. Biochimica et biophysica acta. 1997. Litman T, et al. PubMed
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Impact of CYP2D6 poor metabolizer phenotype on propranolol pharmacokinetics and response. Pharmacotherapy. 1997. Sowinski K M, et al. PubMed
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Propranolol disposition in Chinese subjects of different CYP2D6 genotypes. Clinical pharmacology and therapeutics. 1995. Lai M L, et al. PubMed
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Cytochrome P450 isozymes involved in propranolol metabolism in human liver microsomes. The role of CYP2D6 as ring-hydroxylase and CYP1A2 as N-desisopropylase. Drug metabolism and disposition: the biological fate of chemicals. 1994. Masubuchi Y, et al. PubMed
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P-glycoprotein structure and evolutionary homologies. Cytotechnology. 1993. Croop J M. PubMed
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Selective induction of propranolol metabolism by smoking: additional effects on renal clearance of metabolites. The Journal of pharmacology and experimental therapeutics. 1987. Walle T, et al. PubMed

LinkOuts

Web Resource:
Wikipedia
National Drug Code Directory:
65726-251-10
DrugBank:
DB00571
ChEBI:
8499
KEGG Compound:
C07407
PubChem Compound:
4946
PubChem Substance:
153977
46505387
IUPHAR Ligand:
564
63
Drugs Product Database (DPD):
663719
BindingDB:
25761
ChemSpider:
4777
Therapeutic Targets Database:
DAP000089

Clinical Trials

These are trials that mention propranolol and are related to either pharmacogenetics or pharmacogenomics.

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Sources for PharmGKB drug information: DrugBank, Open Eye Scientific Software.