Identification
- Summary
Dronedarone is an antiarrhythmic agent used in the reduce the risk of hospitalization in patients with paroxysmal or persistent atrial fibrillation.
- Brand Names
- Multaq
- Generic Name
- Dronedarone
- DrugBank Accession Number
- DB04855
- Background
Dronedarone is a Class III antiarrhythmic drug that works to restore the normal sinus rhythm in patients with paroxysmal or persistent atrial fibrillation. Atrial fibrillation is a common sustained arrhythmia where the treatment primarily focuses on stroke prevention and symptom management. It is managed by rate control, rhythm control, prevention of thromboembolic events, and treatment of the underlying disease.1 Similar to amiodarone, dronedarone is a multichannel blocker that works to control rhythm and rate in atrial fibrillation.2 It meets criteria of all four Vaughan Williams antiarrhythmic drug classes by blocking sodium, potassium, and calcium ion channels and inhibiting β-adrenergic receptors.1,13
Dronedarone is a related benzofuran compound to amiodarone but its chemical structure lacks iodine moieties which are associated with amiodarone-induced thyroid problems.1,8 Additionally, the methyl sulfonyl group in its structure renders dronedarone to be more lipophilic with a shorter half-life than amiodarone.1 This ultimately leads to reduced tissue accumulation of the drug and decreased risk for organ toxicities, such as thyroid and pulmonary toxicities.8 Commonly marketed as Multaq®, dronedarone was approved by the FDA in July 2009 and Health Canada in August 2009. A safety concern for the risk of drug-induced hepatocellular injury has been issued following marketing of dronedarone.11
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Dronedarone (DB04855)
- Weight
- Average: 556.756
Monoisotopic: 556.297093218 - Chemical Formula
- C31H44N2O5S
- Synonyms
- Dronedarona
- Dronedarone
- N-(2-butyl-3-(4-(3-(dibutylamino)propoxy)benzoyl)-5-benzofuranyl)-methanesulfonamide
- N-(2-butyl-3-(p-(3-(dibutylamino)propoxy)benzoyl)-5-benzofuranyl)methanesulfonamide
- External IDs
- SR 33589
- SR-33589
- SR33589
Pharmacology
- Indication
Dronedarone is indicated for the management of atrial fibrillation (AF) in patients in sinus rhythm with a history of paroxysmal or persistent AF to reduce the risk of hospitalization.13
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Management of Atrial fibrillation •••••••••••• •••••••••• •••••• •••••••••••• •••••• Management of Atrial fibrillation •••••••••••• •••••••••• •••••• •••••••••••• •••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
Dronedarone is an antiarrhythmic agent that restores normal sinus rhythm and reduces heart rate in atrial fibrillation. In another model, it prevents ventricular tachycardia and ventricular fibrillation.9 Dronedarone moderately prolongs the QTc interval by about 10 ms on average.13 Dronedarone decreases arterial blood pressure and reduces oxygen consumption. It reduces myocardial contractility with no change in left ventricular ejection fraction. Dronedarone vasodilates coronary arteries through activation of the nitric oxide pathway.9 In clinical studies, dronedarone reduced incidence of hospitalizations for acute coronary syndromes and reduced incidence of stroke.3 Dronedarone exhibits antiadrenergic effects by reducing alpha-adrenergic blood pressure response to epinephrine and beta 1 and beta 2 responses to isoproterenol.9
Dronedarone was shown to inhibit triiodothyronine (T3) signalling by binding to TRα1 but much less so to TRβ1.7 The treatment of dronedarone in patients with severe heart failure and left ventricular systolic dysfunction was associated with increased early mortality related to the worsening of heart failure.4 In animal studies, the use of dronedarone at doses equivalent to the recommended human doses was associated with fetal harm. In clinical studies and postmarketing reports, dronedarone was shown to cause hepatocellular liver injury and pulmonary toxicities, such as interstitial lung disease, pneumonitis, and pulmonary fibrosis.13 Compared to its related compound amiodarone, dronedarone has a faster onset and offset of actions with a shorter elimination half-life and low tissue accumulation.1,8
- Mechanism of action
Atrial fibrillation is the most common type of arrhythmia that is caused by abnormal electrical activity in the atria. In atrial fibrillation, tachyarrhythmia, or fast heart rate, can either be paroxysmal (less than 7 days) or persistent (more than 7 days). Atrial fibrillation causes turbulent and abnormal blood flow through the heart chambers, leading to decreased the effectiveness of the heart to pump blood and an increased likelihood of thrombus formation within the atria which can ultimately dislodge and cause a stroke.12
Dronedarone achieves heart rate and rhythm control in atrial fibrillation. In vitro, dronedarone decreased the maximum rate of the rise of an action potential in a concentration- and frequency-dependent manner.2 Cardiac action potentials are generated by ionic currents of multiple voltage-gated ion channels, including potassium, sodium, and calcium channels.6 Dronedarone is a multichannel blocker that meets the criteria of all four Vaughan Williams antiarrhythmic drug classes1 but the contribution of each of these activities to the drug's antiarrhythmic effect is unknown.13 Dronedarone inhibits rapid Na+ currents rate-dependently (class Ib), non-competitively antagonizes α– and β-adrenergic receptors (class II), blocks K+ outward currents (class III) and blocks slow Ca2+ inward currents (class IV).1 More specifically, it decreases delayed-rectifier K+ current (IKr), slowly activating delayed-rectifier K+ current (IKs), inward rectifier potassium current (IK1), peak Na+ current (INa) and L-type Ca2+ current (ICa (L)).2,3 Dronedarone ultimately increases refractory periods, decelerates cardiac conduction, and prolongs cardiac action potential and refractory periods.1,9
- Absorption
Dronedarone is well absorbed after oral administration (>70%).1 It displays low systemic bioavailability due to extensive first-pass metabolism. The absolute bioavailability of dronedarone without and with a high-fat meal is 4% and 15%, respectively. The peak plasma concentrations of dronedarone and its main circulating N-debutyl metabolite are reached within 3 to 6 hours after administration with food.
Following repeated administration of 400 mg dronedarone twice daily, the steady-state was reached within 4 to 8 days of initial treatment. The steady-state Cmax and systemic exposure to the N-debutyl metabolite are similar to that of the parent compound.13
- Volume of distribution
The volume of distribution at steady-state ranges from 1200 to 1400 L following intravenous administration.13
- Protein binding
The in vitro plasma protein binding of dronedarone and its N-debutyl metabolite is 99.7% and 98.5%, respectively. Both mainly bind to albumin and are not capable of saturation.1
- Metabolism
Dronedarone predominantly undergoes CYP3A-mediated hepatic metabolism. Initial metabolism of dronedarone involves N-debutylation to form the N-debutyl-dronedarone, which retains 1/10 to 1/3 of pharmacological activity of the parent compound.13 N-debutyl-dronedarone can be further metabolized to phenol-dronedarone via O-dealkylation and propanoic acid-dronedarone via oxidative deamination. Dronedarone can also be metabolized by CYP2D6 to form benzofuran-hydroxyl-dronedarone. Other detectable metabolites include C-dealkyl-dronedarone and dibutylamine-hydroxyl-dronedarone, along with other minor downstream metabolites with undetermined chemical structures.5
Hover over products below to view reaction partners
- Route of elimination
Following oral administration, about 84% of the labeled dose is excreted in feces and 6% is excreted in urine, mainly as metabolites. Unchanged parent compound and the N-debutyl metabolite accounted for less than 15% of the total radioactivity in the plasma.13
- Half-life
The elimination half life ranges from 13 to 19 hours.13
- Clearance
Following intravenous administration, the clearance ranged from 130 to 150 L/h.13
- Adverse Effects
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In an acute toxicity study, the oral LD50 in rat was >2,000 mg/kg.10
In oral studies, dronedarone showed a limited potential for toxicity in humans in acute overdose situations.9 However, it is recommended that the patient's cardiac rhythm and blood pressure is monitored in the event of overdose. Symptomatic and supportive treatments should be initiated.13
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your software1,2-Benzodiazepine The metabolism of 1,2-Benzodiazepine can be decreased when combined with Dronedarone. Abametapir The serum concentration of Dronedarone can be increased when it is combined with Abametapir. Abatacept The metabolism of Dronedarone can be increased when combined with Abatacept. Abemaciclib The serum concentration of Abemaciclib can be increased when it is combined with Dronedarone. Abiraterone The metabolism of Abiraterone can be decreased when combined with Dronedarone. - Food Interactions
- Avoid grapefruit products. Co-administration with grapefruit may increase drug concentrations by 3-fold.
- Avoid St. John's Wort. This herb induces CYP3A4 and may increase the serum concentration of dronedarone.
- Take with food. Food, especially high-fat food, increases drug absorption.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Dronedarone hydrochloride FA36DV299Q 141625-93-6 DWKVCQXJYURSIQ-UHFFFAOYSA-N - Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Asn-dronedarone Tablet 400 mg Oral Ascend Laboratories Ltd Not applicable Not applicable Canada 
Multaq Tablet 400 mg Oral Sanofi Aventis 2009-09-28 Not applicable Canada Multaq Tablet, film coated 400 mg/1 Oral Cardinal Health 107, LLC 2009-07-01 Not applicable US 
Multaq Tablet, film coated 400 mg Oral SANOFI WINTHROP INDUSTRIE 2016-09-08 Not applicable EU 
Multaq Tablet, film coated 400 mg Oral SANOFI WINTHROP INDUSTRIE 2016-09-08 Not applicable EU
Categories
- ATC Codes
- C01BD07 — Dronedarone
- Drug Categories
- Adrenergic alpha-1 Receptor Antagonists
- Adrenergic alpha-Antagonists
- Adrenergic Antagonists
- Agents that produce hypertension
- Antiarrhythmic agents
- Antiarrhythmics, Class III
- Benzofurans
- Bradycardia-Causing Agents
- Cardiac Therapy
- Cardiovascular Agents
- Cytochrome P-450 CYP2D6 Inhibitors
- Cytochrome P-450 CYP2D6 Inhibitors (moderate)
- Cytochrome P-450 CYP2D6 Substrates
- Cytochrome P-450 CYP2D6 Substrates with a Narrow Therapeutic Index
- Cytochrome P-450 CYP3A Inhibitors
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Inhibitors
- Cytochrome P-450 CYP3A4 Inhibitors (moderate)
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A4 Substrates with a Narrow Therapeutic Index
- Cytochrome P-450 CYP3A5 Inhibitors
- Cytochrome P-450 CYP3A5 Inhibitors (strength unknown)
- Cytochrome P-450 CYP3A5 Substrates
- Cytochrome P-450 CYP3A5 Substrates with a Narrow Therapeutic Index
- Cytochrome P-450 Enzyme Inhibitors
- Cytochrome P-450 Substrates
- Drugs causing inadvertant photosensitivity
- Heterocyclic Compounds, Fused-Ring
- Highest Risk QTc-Prolonging Agents
- Narrow Therapeutic Index Drugs
- OAT3/SLC22A8 Inhibitors
- OATP1B1/SLCO1B1 Inhibitors
- OATP1B3 inhibitors
- OCT1 inhibitors
- OCT2 Inhibitors
- P-glycoprotein inhibitors
- Photosensitizing Agents
- QTc Prolonging Agents
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as aryl-phenylketones. These are aromatic compounds containing a ketone substituted by one aryl group, and a phenyl group.
- Kingdom
- Organic compounds
- Super Class
- Organic oxygen compounds
- Class
- Organooxygen compounds
- Sub Class
- Carbonyl compounds
- Direct Parent
- Aryl-phenylketones
- Alternative Parents
- Sulfanilides / Benzofurans / 3-aroylfurans / Benzoyl derivatives / Phenol ethers / Phenoxy compounds / Alkyl aryl ethers / Organic sulfonamides / Organosulfonamides / Heteroaromatic compounds show 6 more
- Substituents
- 3-aroylfuran / Alkyl aryl ether / Amine / Aminosulfonyl compound / Aromatic heteropolycyclic compound / Aryl-phenylketone / Benzenoid / Benzofuran / Benzoyl / Ether show 21 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- tertiary amino compound, aromatic ether, sulfonamide, 1-benzofurans, aromatic ketone (CHEBI:50659)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- JQZ1L091Y2
- CAS number
- 141626-36-0
- InChI Key
- ZQTNQVWKHCQYLQ-UHFFFAOYSA-N
- InChI
- InChI=1S/C31H44N2O5S/c1-5-8-12-29-30(27-23-25(32-39(4,35)36)15-18-28(27)38-29)31(34)24-13-16-26(17-14-24)37-22-11-21-33(19-9-6-2)20-10-7-3/h13-18,23,32H,5-12,19-22H2,1-4H3
- IUPAC Name
- N-(2-butyl-3-{4-[3-(dibutylamino)propoxy]benzoyl}-1-benzofuran-5-yl)methanesulfonamide
- SMILES
- CCCCN(CCCC)CCCOC1=CC=C(C=C1)C(=O)C1=C(CCCC)OC2=C1C=C(NS(C)(=O)=O)C=C2
References
- Synthesis Reference
Arie Gutman, Gennadi Nisnevich, Lev Yudovitch, "Process for the preparation of dronedarone." U.S. Patent US20050049302, issued March 03, 2005.
US20050049302- General References
- Schweizer PA, Becker R, Katus HA, Thomas D: Dronedarone: current evidence for its safety and efficacy in the management of atrial fibrillation. Drug Des Devel Ther. 2011 Jan 6;5:27-39. doi: 10.2147/DDDT.S10315. [Article]
- Patel PD, Bhuriya R, Patel DD, Arora BL, Singh PP, Arora RR: Dronedarone for atrial fibrillation: a new therapeutic agent. Vasc Health Risk Manag. 2009;5:635-42. doi: 10.2147/vhrm.s6185. Epub 2009 Aug 6. [Article]
- Heijman J, Heusch G, Dobrev D: Pleiotropic effects of antiarrhythmic agents: dronedarone in the treatment of atrial fibrillation. Clin Med Insights Cardiol. 2013 Aug 11;7:127-40. doi: 10.4137/CMC.S8445. eCollection 2013. [Article]
- Kober L, Torp-Pedersen C, McMurray JJ, Gotzsche O, Levy S, Crijns H, Amlie J, Carlsen J: Increased mortality after dronedarone therapy for severe heart failure. N Engl J Med. 2008 Jun 19;358(25):2678-87. doi: 10.1056/NEJMoa0800456. [Article]
- Klieber S, Arabeyre-Fabre C, Moliner P, Marti E, Mandray M, Ngo R, Ollier C, Brun P, Fabre G: Identification of metabolic pathways and enzyme systems involved in the in vitro human hepatic metabolism of dronedarone, a potent new oral antiarrhythmic drug. Pharmacol Res Perspect. 2014 Jun;2(3):e00044. doi: 10.1002/prp2.44. Epub 2014 Apr 22. [Article]
- Rahm AK, Lugenbiel P, Schweizer PA, Katus HA, Thomas D: Role of ion channels in heart failure and channelopathies. Biophys Rev. 2018 Aug;10(4):1097-1106. doi: 10.1007/s12551-018-0442-3. Epub 2018 Jul 17. [Article]
- Van Beeren HC, Jong WM, Kaptein E, Visser TJ, Bakker O, Wiersinga WM: Dronerarone acts as a selective inhibitor of 3,5,3'-triiodothyronine binding to thyroid hormone receptor-alpha1: in vitro and in vivo evidence. Endocrinology. 2003 Feb;144(2):552-8. doi: 10.1210/en.2002-220604. [Article]
- 21. (2012). In Rang and Dale's Pharmacology (7th ed., pp. 257). Edinburgh: Elsevier/Churchill Livingstone. [ISBN:978-0-7020-3471-8]
- MULTAQ® (dronedarone hydrochloride) Product Monograph [Link]
- MULTAQ® (dronedarone) Safety Data Sheet - Van Wert Health [Link]
- Health Canada Endorsed Important Safety Information on Multaq [Link]
- Atrial Fibrillation (A Fib) - StatPearls - NCBI Bookshelf [Link]
- FDA Approved Drug Products: Multaq (dronedarone) oral tablets [Link]
- FDA Approved Drug Products: Multaq (dronedarone) tablets for oral use (October 2023) [Link]
- External Links
- Human Metabolome Database
- HMDB0251621
- KEGG Drug
- D02537
- PubChem Compound
- 208898
- PubChem Substance
- 175426865
- ChemSpider
- 180996
- BindingDB
- 50151864
- 233698
- ChEBI
- 50659
- ChEMBL
- CHEMBL184412
- ZINC
- ZINC000049933061
- PharmGKB
- PA153619853
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Dronedarone
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Active Not Recruiting Treatment Atrial Fibrillation 1 4 Completed Treatment Atrial Fibrillation 3 4 Recruiting Treatment Atrial Fibrillation 1 4 Terminated Prevention Atrial Fibrillation / Recurrent Atrial Fibrillation 1 4 Terminated Treatment Atrial Fibrillation 3
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet Oral 400 mg Tablet, film coated Oral 400 mg/1 Tablet, coated Oral 400 mg Tablet, film coated Oral 400 mg Tablet Oral 426.000 mg - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region CA2294812 No 2009-09-29 2018-06-19 Canada CA2047773 No 2000-09-12 2011-07-24 Canada US5223510 No 1993-06-29 2016-07-26 US US8410167 No 2013-04-02 2029-04-16 US US8602215 No 2013-12-10 2031-06-30 US US9107900 No 2015-08-18 2029-04-16 US US8318800 No 2012-11-27 2018-06-19 US US7323493 No 2008-01-29 2018-06-19 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 137-145 MULTAQ® (dronedarone) Safety Data Sheet - Van Wert Health water solubility 0.64 g/l MULTAQ® (dronedarone) Safety Data Sheet - Van Wert Health logP 4.63 MULTAQ® (dronedarone) Safety Data Sheet - Van Wert Health - Predicted Properties
Property Value Source Water Solubility 0.00201 mg/mL ALOGPS logP 6.46 ALOGPS logP 5.18 Chemaxon logS -5.4 ALOGPS pKa (Strongest Acidic) 9.18 Chemaxon pKa (Strongest Basic) 10.31 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 5 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 88.85 Å2 Chemaxon Rotatable Bond Count 17 Chemaxon Refractivity 158.13 m3·mol-1 Chemaxon Polarizability 66.05 Å3 Chemaxon Number of Rings 3 Chemaxon Bioavailability 0 Chemaxon Rule of Five No Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule Yes Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 1.0 Blood Brain Barrier + 0.9156 Caco-2 permeable - 0.6057 P-glycoprotein substrate Substrate 0.6265 P-glycoprotein inhibitor I Inhibitor 0.7879 P-glycoprotein inhibitor II Non-inhibitor 0.5218 Renal organic cation transporter Non-inhibitor 0.7334 CYP450 2C9 substrate Non-substrate 0.7339 CYP450 2D6 substrate Non-substrate 0.7682 CYP450 3A4 substrate Substrate 0.6963 CYP450 1A2 substrate Non-inhibitor 0.5487 CYP450 2C9 inhibitor Inhibitor 0.6209 CYP450 2D6 inhibitor Non-inhibitor 0.8299 CYP450 2C19 inhibitor Non-inhibitor 0.5319 CYP450 3A4 inhibitor Non-inhibitor 0.5198 CYP450 inhibitory promiscuity High CYP Inhibitory Promiscuity 0.8288 Ames test Non AMES toxic 0.5248 Carcinogenicity Non-carcinogens 0.6132 Biodegradation Not ready biodegradable 1.0 Rat acute toxicity 2.6273 LD50, mol/kg Not applicable hERG inhibition (predictor I) Strong inhibitor 0.8036 hERG inhibition (predictor II) Inhibitor 0.8051
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 245.1934713 predictedDarkChem Lite v0.1.0 [M-H]- 228.9139 predictedDeepCCS 1.0 (2019) [M+H]+ 244.7341713 predictedDarkChem Lite v0.1.0 [M+H]+ 231.30943 predictedDeepCCS 1.0 (2019) [M+Na]+ 245.2514713 predictedDarkChem Lite v0.1.0 [M+Na]+ 237.22197 predictedDeepCCS 1.0 (2019)
Targets
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Protein heterodimerization activity
- Specific Function
- This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) prot...
- Gene Name
- ADRA1A
- Uniprot ID
- P35348
- Uniprot Name
- Alpha-1A adrenergic receptor
- Molecular Weight
- 51486.005 Da
References
- Dale KM, White CM: Dronedarone: an amiodarone analog for the treatment of atrial fibrillation and atrial flutter. Ann Pharmacother. 2007 Apr;41(4):599-605. Epub 2007 Mar 27. [Article]
- Heijman J, Heusch G, Dobrev D: Pleiotropic effects of antiarrhythmic agents: dronedarone in the treatment of atrial fibrillation. Clin Med Insights Cardiol. 2013 Aug 11;7:127-40. doi: 10.4137/CMC.S8445. eCollection 2013. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Protein heterodimerization activity
- Specific Function
- This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) prot...
- Gene Name
- ADRA1B
- Uniprot ID
- P35368
- Uniprot Name
- Alpha-1B adrenergic receptor
- Molecular Weight
- 56835.375 Da
References
- Dale KM, White CM: Dronedarone: an amiodarone analog for the treatment of atrial fibrillation and atrial flutter. Ann Pharmacother. 2007 Apr;41(4):599-605. Epub 2007 Mar 27. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Alpha1-adrenergic receptor activity
- Specific Function
- This alpha-adrenergic receptor mediates its effect through the influx of extracellular calcium.
- Gene Name
- ADRA1D
- Uniprot ID
- P25100
- Uniprot Name
- Alpha-1D adrenergic receptor
- Molecular Weight
- 60462.205 Da
References
- Dale KM, White CM: Dronedarone: an amiodarone analog for the treatment of atrial fibrillation and atrial flutter. Ann Pharmacother. 2007 Apr;41(4):599-605. Epub 2007 Mar 27. [Article]
- Heijman J, Heusch G, Dobrev D: Pleiotropic effects of antiarrhythmic agents: dronedarone in the treatment of atrial fibrillation. Clin Med Insights Cardiol. 2013 Aug 11;7:127-40. doi: 10.4137/CMC.S8445. eCollection 2013. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Thioesterase binding
- Specific Function
- Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazo...
- Gene Name
- ADRA2A
- Uniprot ID
- P08913
- Uniprot Name
- Alpha-2A adrenergic receptor
- Molecular Weight
- 48956.275 Da
References
- Dale KM, White CM: Dronedarone: an amiodarone analog for the treatment of atrial fibrillation and atrial flutter. Ann Pharmacother. 2007 Apr;41(4):599-605. Epub 2007 Mar 27. [Article]
- Heijman J, Heusch G, Dobrev D: Pleiotropic effects of antiarrhythmic agents: dronedarone in the treatment of atrial fibrillation. Clin Med Insights Cardiol. 2013 Aug 11;7:127-40. doi: 10.4137/CMC.S8445. eCollection 2013. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Epinephrine binding
- Specific Function
- Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is clonidine...
- Gene Name
- ADRA2B
- Uniprot ID
- P18089
- Uniprot Name
- Alpha-2B adrenergic receptor
- Molecular Weight
- 49565.8 Da
References
- Dale KM, White CM: Dronedarone: an amiodarone analog for the treatment of atrial fibrillation and atrial flutter. Ann Pharmacother. 2007 Apr;41(4):599-605. Epub 2007 Mar 27. [Article]
- Heijman J, Heusch G, Dobrev D: Pleiotropic effects of antiarrhythmic agents: dronedarone in the treatment of atrial fibrillation. Clin Med Insights Cardiol. 2013 Aug 11;7:127-40. doi: 10.4137/CMC.S8445. eCollection 2013. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Protein homodimerization activity
- Specific Function
- Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins.
- Gene Name
- ADRA2C
- Uniprot ID
- P18825
- Uniprot Name
- Alpha-2C adrenergic receptor
- Molecular Weight
- 49521.585 Da
References
- Dale KM, White CM: Dronedarone: an amiodarone analog for the treatment of atrial fibrillation and atrial flutter. Ann Pharmacother. 2007 Apr;41(4):599-605. Epub 2007 Mar 27. [Article]
- Heijman J, Heusch G, Dobrev D: Pleiotropic effects of antiarrhythmic agents: dronedarone in the treatment of atrial fibrillation. Clin Med Insights Cardiol. 2013 Aug 11;7:127-40. doi: 10.4137/CMC.S8445. eCollection 2013. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarization
- Specific Function
- Pore-forming (alpha) subunit of voltage-gated inwardly rectifying potassium channel. Channel properties are modulated by cAMP and subunit assembly. Mediates the rapidly activating component of the ...
- Gene Name
- KCNH2
- Uniprot ID
- Q12809
- Uniprot Name
- Potassium voltage-gated channel subfamily H member 2
- Molecular Weight
- 126653.52 Da
References
- Iwamoto T, Watanabe Y, Kita S, Blaustein MP: Na+/Ca2+ exchange inhibitors: a new class of calcium regulators. Cardiovasc Hematol Disord Drug Targets. 2007 Sep;7(3):188-98. [Article]
- Heijman J, Heusch G, Dobrev D: Pleiotropic effects of antiarrhythmic agents: dronedarone in the treatment of atrial fibrillation. Clin Med Insights Cardiol. 2013 Aug 11;7:127-40. doi: 10.4137/CMC.S8445. eCollection 2013. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Voltage-gated calcium channel activity
- Specific Function
- Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...
- Gene Name
- CACNA1C
- Uniprot ID
- Q13936
- Uniprot Name
- Voltage-dependent L-type calcium channel subunit alpha-1C
- Molecular Weight
- 248974.1 Da
References
- Heijman J, Heusch G, Dobrev D: Pleiotropic effects of antiarrhythmic agents: dronedarone in the treatment of atrial fibrillation. Clin Med Insights Cardiol. 2013 Aug 11;7:127-40. doi: 10.4137/CMC.S8445. eCollection 2013. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Voltage-gated calcium channel activity involved sa node cell action potential
- Specific Function
- Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...
- Gene Name
- CACNA1D
- Uniprot ID
- Q01668
- Uniprot Name
- Voltage-dependent L-type calcium channel subunit alpha-1D
- Molecular Weight
- 245138.75 Da
References
- Heijman J, Heusch G, Dobrev D: Pleiotropic effects of antiarrhythmic agents: dronedarone in the treatment of atrial fibrillation. Clin Med Insights Cardiol. 2013 Aug 11;7:127-40. doi: 10.4137/CMC.S8445. eCollection 2013. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Voltage-gated calcium channel activity
- Specific Function
- Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...
- Gene Name
- CACNA1F
- Uniprot ID
- O60840
- Uniprot Name
- Voltage-dependent L-type calcium channel subunit alpha-1F
- Molecular Weight
- 220675.9 Da
References
- Heijman J, Heusch G, Dobrev D: Pleiotropic effects of antiarrhythmic agents: dronedarone in the treatment of atrial fibrillation. Clin Med Insights Cardiol. 2013 Aug 11;7:127-40. doi: 10.4137/CMC.S8445. eCollection 2013. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Voltage-gated calcium channel activity
- Specific Function
- Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...
- Gene Name
- CACNA1S
- Uniprot ID
- Q13698
- Uniprot Name
- Voltage-dependent L-type calcium channel subunit alpha-1S
- Molecular Weight
- 212348.1 Da
References
- Heijman J, Heusch G, Dobrev D: Pleiotropic effects of antiarrhythmic agents: dronedarone in the treatment of atrial fibrillation. Clin Med Insights Cardiol. 2013 Aug 11;7:127-40. doi: 10.4137/CMC.S8445. eCollection 2013. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Voltage-gated calcium channel activity
- Specific Function
- The beta subunit of voltage-dependent calcium channels contributes to the function of the calcium channel by increasing peak calcium current, shifting the voltage dependencies of activation and ina...
- Gene Name
- CACNB1
- Uniprot ID
- Q02641
- Uniprot Name
- Voltage-dependent L-type calcium channel subunit beta-1
- Molecular Weight
- 65712.995 Da
References
- Heijman J, Heusch G, Dobrev D: Pleiotropic effects of antiarrhythmic agents: dronedarone in the treatment of atrial fibrillation. Clin Med Insights Cardiol. 2013 Aug 11;7:127-40. doi: 10.4137/CMC.S8445. eCollection 2013. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Voltage-gated calcium channel activity
- Specific Function
- The beta subunit of voltage-dependent calcium channels contributes to the function of the calcium channel by increasing peak calcium current, shifting the voltage dependencies of activation and ina...
- Gene Name
- CACNB2
- Uniprot ID
- Q08289
- Uniprot Name
- Voltage-dependent L-type calcium channel subunit beta-2
- Molecular Weight
- 73579.925 Da
References
- Heijman J, Heusch G, Dobrev D: Pleiotropic effects of antiarrhythmic agents: dronedarone in the treatment of atrial fibrillation. Clin Med Insights Cardiol. 2013 Aug 11;7:127-40. doi: 10.4137/CMC.S8445. eCollection 2013. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Voltage-gated calcium channel activity
- Specific Function
- The beta subunit of voltage-dependent calcium channels contributes to the function of the calcium channel by increasing peak calcium current, shifting the voltage dependencies of activation and ina...
- Gene Name
- CACNB3
- Uniprot ID
- P54284
- Uniprot Name
- Voltage-dependent L-type calcium channel subunit beta-3
- Molecular Weight
- 54531.425 Da
References
- Heijman J, Heusch G, Dobrev D: Pleiotropic effects of antiarrhythmic agents: dronedarone in the treatment of atrial fibrillation. Clin Med Insights Cardiol. 2013 Aug 11;7:127-40. doi: 10.4137/CMC.S8445. eCollection 2013. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Voltage-gated calcium channel activity
- Specific Function
- The beta subunit of voltage-dependent calcium channels contributes to the function of the calcium channel by increasing peak calcium current, shifting the voltage dependencies of activation and ina...
- Gene Name
- CACNB4
- Uniprot ID
- O00305
- Uniprot Name
- Voltage-dependent L-type calcium channel subunit beta-4
- Molecular Weight
- 58168.625 Da
References
- Heijman J, Heusch G, Dobrev D: Pleiotropic effects of antiarrhythmic agents: dronedarone in the treatment of atrial fibrillation. Clin Med Insights Cardiol. 2013 Aug 11;7:127-40. doi: 10.4137/CMC.S8445. eCollection 2013. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Potassium ion leak channel activity
- Specific Function
- Ion channel that contributes to passive transmembrane potassium transport (PubMed:23169818). Reversibly converts between a voltage-insensitive potassium leak channel and a voltage-dependent outward...
- Gene Name
- KCNK2
- Uniprot ID
- O95069
- Uniprot Name
- Potassium channel subfamily K member 2
- Molecular Weight
- 47092.215 Da
References
- Schmidt C, Wiedmann F, Schweizer PA, Becker R, Katus HA, Thomas D: Novel electrophysiological properties of dronedarone: inhibition of human cardiac two-pore-domain potassium (K2P) channels. Naunyn Schmiedebergs Arch Pharmacol. 2012 Oct;385(10):1003-16. doi: 10.1007/s00210-012-0780-9. Epub 2012 Jul 13. [Article]
- Heijman J, Heusch G, Dobrev D: Pleiotropic effects of antiarrhythmic agents: dronedarone in the treatment of atrial fibrillation. Clin Med Insights Cardiol. 2013 Aug 11;7:127-40. doi: 10.4137/CMC.S8445. eCollection 2013. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Voltage-gated sodium channel activity involved in sa node cell action potential
- Specific Function
- This protein mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the pr...
- Gene Name
- SCN5A
- Uniprot ID
- Q14524
- Uniprot Name
- Sodium channel protein type 5 subunit alpha
- Molecular Weight
- 226937.475 Da
References
- Heijman J, Heusch G, Dobrev D: Pleiotropic effects of antiarrhythmic agents: dronedarone in the treatment of atrial fibrillation. Clin Med Insights Cardiol. 2013 Aug 11;7:127-40. doi: 10.4137/CMC.S8445. eCollection 2013. [Article]
- Lalevee N, Nargeot J, Barrere-Lemaire S, Gautier P, Richard S: Effects of amiodarone and dronedarone on voltage-dependent sodium current in human cardiomyocytes. J Cardiovasc Electrophysiol. 2003 Aug;14(8):885-90. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- G-protein activated inward rectifier potassium channel activity
- Specific Function
- This potassium channel is controlled by G proteins. Inward rectifier potassium channels are characterized by a greater tendency to allow potassium to flow into the cell rather than out of it. Their...
- Gene Name
- KCNJ3
- Uniprot ID
- P48549
- Uniprot Name
- G protein-activated inward rectifier potassium channel 1
- Molecular Weight
- 56602.84 Da
References
- Heijman J, Heusch G, Dobrev D: Pleiotropic effects of antiarrhythmic agents: dronedarone in the treatment of atrial fibrillation. Clin Med Insights Cardiol. 2013 Aug 11;7:127-40. doi: 10.4137/CMC.S8445. eCollection 2013. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarization
- Specific Function
- Potassium channel that plays an important role in a number of tissues, including heart, inner ear, stomach and colon (By similarity) (PubMed:10646604). Associates with KCNE beta subunits that modul...
- Gene Name
- KCNQ1
- Uniprot ID
- P51787
- Uniprot Name
- Potassium voltage-gated channel subfamily KQT member 1
- Molecular Weight
- 74697.925 Da
References
- Heijman J, Heusch G, Dobrev D: Pleiotropic effects of antiarrhythmic agents: dronedarone in the treatment of atrial fibrillation. Clin Med Insights Cardiol. 2013 Aug 11;7:127-40. doi: 10.4137/CMC.S8445. eCollection 2013. [Article]
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Inward rectifier potassium channel activity
- Specific Function
- Inward rectifying potassium channel that is activated by phosphatidylinositol 4,5-bisphosphate and that probably participates in controlling the resting membrane potential in electrically excitable...
Components:
References
- Heijman J, Heusch G, Dobrev D: Pleiotropic effects of antiarrhythmic agents: dronedarone in the treatment of atrial fibrillation. Clin Med Insights Cardiol. 2013 Aug 11;7:127-40. doi: 10.4137/CMC.S8445. eCollection 2013. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Ion channel binding
- Specific Function
- Mediates the exchange of one Ca(2+) ion against three to four Na(+) ions across the cell membrane, and thereby contributes to the regulation of cytoplasmic Ca(2+) levels and Ca(2+)-dependent cellul...
- Gene Name
- SLC8A1
- Uniprot ID
- P32418
- Uniprot Name
- Sodium/calcium exchanger 1
- Molecular Weight
- 108546.06 Da
References
- Heijman J, Heusch G, Dobrev D: Pleiotropic effects of antiarrhythmic agents: dronedarone in the treatment of atrial fibrillation. Clin Med Insights Cardiol. 2013 Aug 11;7:127-40. doi: 10.4137/CMC.S8445. eCollection 2013. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Metal ion binding
- Specific Function
- Pore-forming (alpha) subunit of voltage-gated rapidly inactivating A-type potassium channels. May contribute to I(To) current in heart and I(Sa) current in neurons. Channel properties are modulated...
- Gene Name
- KCND3
- Uniprot ID
- Q9UK17
- Uniprot Name
- Potassium voltage-gated channel subfamily D member 3
- Molecular Weight
- 73450.53 Da
References
- Heijman J, Heusch G, Dobrev D: Pleiotropic effects of antiarrhythmic agents: dronedarone in the treatment of atrial fibrillation. Clin Med Insights Cardiol. 2013 Aug 11;7:127-40. doi: 10.4137/CMC.S8445. eCollection 2013. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Receptor signaling protein activity
- Specific Function
- Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. This receptor binds epinephrine and norepinephrine with approximately e...
- Gene Name
- ADRB1
- Uniprot ID
- P08588
- Uniprot Name
- Beta-1 adrenergic receptor
- Molecular Weight
- 51322.1 Da
References
- Dale KM, White CM: Dronedarone: an amiodarone analog for the treatment of atrial fibrillation and atrial flutter. Ann Pharmacother. 2007 Apr;41(4):599-605. Epub 2007 Mar 27. [Article]
- Heijman J, Heusch G, Dobrev D: Pleiotropic effects of antiarrhythmic agents: dronedarone in the treatment of atrial fibrillation. Clin Med Insights Cardiol. 2013 Aug 11;7:127-40. doi: 10.4137/CMC.S8445. eCollection 2013. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Zinc ion binding
- Specific Function
- Isoform Alpha-1: Nuclear hormone receptor that can act as a repressor or activator of transcription. High affinity receptor for thyroid hormones, including triiodothyronine and thyroxine.Isoform Al...
- Gene Name
- THRA
- Uniprot ID
- P10827
- Uniprot Name
- Thyroid hormone receptor alpha
- Molecular Weight
- 54815.055 Da
References
- Van Beeren HC, Jong WM, Kaptein E, Visser TJ, Bakker O, Wiersinga WM: Dronerarone acts as a selective inhibitor of 3,5,3'-triiodothyronine binding to thyroid hormone receptor-alpha1: in vitro and in vivo evidence. Endocrinology. 2003 Feb;144(2):552-8. doi: 10.1210/en.2002-220604. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- General Function
- Oxygen binding
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP3A5
- Uniprot ID
- P20815
- Uniprot Name
- Cytochrome P450 3A5
- Molecular Weight
- 57108.065 Da
References
- Klieber S, Arabeyre-Fabre C, Moliner P, Marti E, Mandray M, Ngo R, Ollier C, Brun P, Fabre G: Identification of metabolic pathways and enzyme systems involved in the in vitro human hepatic metabolism of dronedarone, a potent new oral antiarrhythmic drug. Pharmacol Res Perspect. 2014 Jun;2(3):e00044. doi: 10.1002/prp2.44. Epub 2014 Apr 22. [Article]
- Hong Y, Chia YM, Yeo RH, Venkatesan G, Koh SK, Chai CL, Zhou L, Kojodjojo P, Chan EC: Inactivation of Human Cytochrome P450 3A4 and 3A5 by Dronedarone and N-Desbutyl Dronedarone. Mol Pharmacol. 2016 Jan;89(1):1-13. doi: 10.1124/mol.115.100891. Epub 2015 Oct 21. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Steroid hydroxylase activity
- Specific Function
- This enzyme metabolizes arachidonic acid predominantly via a NADPH-dependent olefin epoxidation to all four regioisomeric cis-epoxyeicosatrienoic acids. One of the predominant enzymes responsible f...
- Gene Name
- CYP2J2
- Uniprot ID
- P51589
- Uniprot Name
- Cytochrome P450 2J2
- Molecular Weight
- 57610.165 Da
References
- Karkhanis A, Lam HY, Venkatesan G, Koh SK, Chai CL, Zhou L, Hong Y, Kojodjojo P, Chan EC: Multiple modes of inhibition of human cytochrome P450 2J2 by dronedarone, amiodarone and their active metabolites. Biochem Pharmacol. 2016 May 1;107:67-80. doi: 10.1016/j.bcp.2016.03.005. Epub 2016 Mar 10. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- General Function
- Steroid hydroxylase activity
- Specific Function
- Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
- Gene Name
- CYP2D6
- Uniprot ID
- P10635
- Uniprot Name
- Cytochrome P450 2D6
- Molecular Weight
- 55768.94 Da
References
- Schafer JA, Kjesbo NK, Gleason PP: Dronedarone: current evidence and future questions. Cardiovasc Ther. 2010 Spring;28(1):38-47. doi: 10.1111/j.1755-5922.2009.00112.x. [Article]
- De Ferrari GM, Dusi V: Drug safety evaluation of dronedarone in atrial fibrillation. Expert Opin Drug Saf. 2012 Nov;11(6):1023-45. doi: 10.1517/14740338.2012.722994. Epub 2012 Sep 13. [Article]
- Kim MS, Baek IH: Effect of dronedarone on the pharmacokinetics of carvedilol following oral administration to rats. Eur J Pharm Sci. 2018 Jan 1;111:13-19. doi: 10.1016/j.ejps.2017.09.029. Epub 2017 Sep 20. [Article]
- Klieber S, Arabeyre-Fabre C, Moliner P, Marti E, Mandray M, Ngo R, Ollier C, Brun P, Fabre G: Identification of metabolic pathways and enzyme systems involved in the in vitro human hepatic metabolism of dronedarone, a potent new oral antiarrhythmic drug. Pharmacol Res Perspect. 2014 Jun;2(3):e00044. doi: 10.1002/prp2.44. Epub 2014 Apr 22. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- General Function
- Vitamin d3 25-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- Dorian P: Clinical pharmacology of dronedarone: implications for the therapy of atrial fibrillation. J Cardiovasc Pharmacol Ther. 2010 Dec;15(4 Suppl):15S-8S. doi: 10.1177/1074248410367792. Epub 2010 May 14. [Article]
- Schafer JA, Kjesbo NK, Gleason PP: Dronedarone: current evidence and future questions. Cardiovasc Ther. 2010 Spring;28(1):38-47. doi: 10.1111/j.1755-5922.2009.00112.x. [Article]
- De Ferrari GM, Dusi V: Drug safety evaluation of dronedarone in atrial fibrillation. Expert Opin Drug Saf. 2012 Nov;11(6):1023-45. doi: 10.1517/14740338.2012.722994. Epub 2012 Sep 13. [Article]
- FDA Drug Development and Drug Interactions: Table of Substrates, Inhibitors and Inducers [Link]
- Dronedarone FDA Label [Link]
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Binder
- General Function
- Toxic substance binding
- Specific Function
- Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
- Gene Name
- ALB
- Uniprot ID
- P02768
- Uniprot Name
- Serum albumin
- Molecular Weight
- 69365.94 Da
References
- MULTAQ® (dronedarone hydrochloride) Product Monograph [Link]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Xenobiotic-transporting atpase activity
- Specific Function
- Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
- Gene Name
- ABCB1
- Uniprot ID
- P08183
- Uniprot Name
- Multidrug resistance protein 1
- Molecular Weight
- 141477.255 Da
References
- De Ferrari GM, Dusi V: Drug safety evaluation of dronedarone in atrial fibrillation. Expert Opin Drug Saf. 2012 Nov;11(6):1023-45. doi: 10.1517/14740338.2012.722994. Epub 2012 Sep 13. [Article]
- Schafer JA, Kjesbo NK, Gleason PP: Dronedarone: current evidence and future questions. Cardiovasc Ther. 2010 Spring;28(1):38-47. doi: 10.1111/j.1755-5922.2009.00112.x. [Article]
- FDA Drug Development and Drug Interactions: Table of Substrates, Inhibitors and Inducers [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Quaternary ammonium group transmembrane transporter activity
- Specific Function
- Mediates tubular uptake of organic compounds from circulation. Mediates the influx of agmatine, dopamine, noradrenaline (norepinephrine), serotonin, choline, famotidine, ranitidine, histamin, creat...
- Gene Name
- SLC22A2
- Uniprot ID
- O15244
- Uniprot Name
- Solute carrier family 22 member 2
- Molecular Weight
- 62579.99 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Secondary active organic cation transmembrane transporter activity
- Specific Function
- Translocates a broad array of organic cations with various structures and molecular weights including the model compounds 1-methyl-4-phenylpyridinium (MPP), tetraethylammonium (TEA), N-1-methylnico...
- Gene Name
- SLC22A1
- Uniprot ID
- O15245
- Uniprot Name
- Solute carrier family 22 member 1
- Molecular Weight
- 61153.345 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostagland...
- Gene Name
- SLCO1B1
- Uniprot ID
- Q9Y6L6
- Uniprot Name
- Solute carrier organic anion transporter family member 1B1
- Molecular Weight
- 76447.99 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Mediates the Na(+)-independent uptake of organic anions such as 17-beta-glucuronosyl estradiol, taurocholate, triiodothyronine (T3), leukotriene C4, dehydroepiandrosterone sulfate (DHEAS), methotre...
- Gene Name
- SLCO1B3
- Uniprot ID
- Q9NPD5
- Uniprot Name
- Solute carrier organic anion transporter family member 1B3
- Molecular Weight
- 77402.175 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Plays an important role in the excretion/detoxification of endogenous and exogenous organic anions, especially from the brain and kidney. Involved in the transport basolateral of steviol, fexofenad...
- Gene Name
- SLC22A8
- Uniprot ID
- Q8TCC7
- Uniprot Name
- Solute carrier family 22 member 8
- Molecular Weight
- 59855.585 Da
Drug created at October 18, 2007 23:47 / Updated at February 20, 2024 23:54