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IdentificationPharmacologyInteractionsReferencesTrialsEconomicsPropertiesSpectraTaxonomyIdentification
- Name
- Doxazosin
- Accession Number
- DB00590 (APRD00474)
- Type
- Small Molecule
- Groups
- Approved
- Description
Doxazosin is a quinazoline-derivative that selectively antagonizes postsynaptic α1-adrenergic receptors. It may be used to mild to moderate hypertension and in the management of symptomatic benign prostatic hyperplasia (BPH). α1-Receptors mediate contraction and hypertrophic growth of smooth muscle cells. Antagonism of these receptors leads to smooth muscle relaxation in the peripheral vasculature and prostate gland.
- Structure
Structure for Doxazosin (DB00590)
- Synonyms
- 1-(4-Amino-6,7-dimethoxy-2-chinazolinyl)-4-(2,3-dihydro-1,4-benzodioxixin-2-ylcarbonyl)piperazin
- 1-(4-Amino-6,7-Dimethoxy-2-quinazolinyl)-4-(1,4-benzodioxan-2-ylcarbonyl)piperazin
- Doxazosin
- Doxazosina
- Doxazosine
- Doxazosinum
- Product Ingredients
Ingredient UNII CAS InChI Key Doxazosin mesylate 86P6PQK0MU 77883-43-3 VJECBOKJABCYMF-UHFFFAOYSA-N - Product Images
- Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Cardura Tablet 1 mg/1 Oral Physicians Total Care, Inc. 1995-10-16 2012-06-30 US 
Cardura Tablet 8 mg/1 Oral Roerig 1990-11-02 Not applicable US Cardura Tablet 8 mg/1 Oral Physicians Total Care, Inc. 1994-12-13 2012-06-30 US Cardura Tablet 4 mg/1 Oral Roerig 1990-11-02 Not applicable US Cardura Tablet 4 mg/1 Oral Physicians Total Care, Inc. 1993-06-22 2012-07-16 US Cardura Tablet 2 mg/1 Oral Roerig 1990-11-02 Not applicable US Cardura Tablet 2 mg/1 Oral Physicians Total Care, Inc. 1999-02-10 2012-06-30 US Cardura Tablet 1 mg/1 Oral Roerig 1990-11-02 Not applicable US Cardura XL Tablet, multilayer, extended release 8 mg/1 Oral Roerig 2005-02-22 Not applicable US Cardura XL Tablet, multilayer, extended release 4 mg/1 Oral Roerig 2005-02-22 Not applicable US - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Apo-doxazosin Tablet 4 mg Oral Apotex Corporation 1999-07-22 Not applicable Canada 
Apo-doxazosin Tablet 2 mg Oral Apotex Corporation 1999-07-22 Not applicable Canada Apo-doxazosin Tablet 1 mg Oral Apotex Corporation 1999-07-22 Not applicable Canada Dom-doxazosin Tablet 4 mg Oral Dominion Pharmacal 2004-05-26 Not applicable Canada Dom-doxazosin Tablet 2 mg Oral Dominion Pharmacal 2004-05-26 Not applicable Canada Dom-doxazosin Tablet 1 mg Oral Dominion Pharmacal 2004-05-26 Not applicable Canada Doxazosin Tablet 4 mg/1 Oral State of Florida DOH Central Pharmacy 2009-07-01 Not applicable US 
Doxazosin Tablet 2 mg/1 Oral A-S Medication Solutions 2015-04-22 Not applicable US 
Doxazosin Tablet 2 mg/1 Oral PD-Rx Pharmaceuticals, Inc. 2011-07-14 Not applicable US Doxazosin Tablet 2 mg/1 Oral Unit Dose Services 2015-04-29 Not applicable US 
- Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Cardura-1,2,and 4 Doxazosin (1 mg) + Doxazosin (2 mg) + Doxazosin (4 mg) Kit; Tablet Oral Astra Zeneca Not applicable Not applicable Canada Cardura-1,2,and 4 Doxazosin (1 mg) + Doxazosin (2 mg) + Doxazosin (4 mg) Kit; Tablet Oral Astra Zeneca Not applicable Not applicable Canada Cardura-1,2,and 4 Doxazosin (1 mg) + Doxazosin (2 mg) + Doxazosin (4 mg) Kit; Tablet Oral Astra Zeneca Not applicable Not applicable Canada - International/Other Brands
- Alfadil (Pfizer (Sweden)) / Cardenalin (Pfizer (Japan; discontinued)) / Cardular (Pfizer (Germany)) / Cardura-1 (Pfizer (Canada)) / Cardura-2 (Pfizer (Canada)) / Cardura-4 (Pfizer (Canada)) / Carduran (Pfizer (Brazil, Denmark, Norway, Spain)) / Diblocin (AstraZeneca (Germany)) / Normothen (Bioindustria (Italy)) / Supressin (Pfizer (Austria))
- Categories
- Adrenergic Agents
- Adrenergic alpha-1 Receptor Antagonists
- Adrenergic alpha-Antagonists
- Adrenergic Antagonists
- Antiadrenergic Agents, Peripherally Acting
- Antihypertensive Agents
- Cardiovascular Agents
- Cytochrome P-450 CYP2D6 Substrates
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Hypotensive Agents
- Neurotransmitter Agents
- P-glycoprotein/ABCB1 Inhibitors
- Prazosin
- Quinazolines
- UNII
- NW1291F1W8
- CAS number
- 74191-85-8
- Weight
- Average: 451.4751
Monoisotopic: 451.185568935 - Chemical Formula
- C23H25N5O5
- InChI Key
- RUZYUOTYCVRMRZ-UHFFFAOYSA-N
- InChI
- InChI=1S/C23H25N5O5/c1-30-18-11-14-15(12-19(18)31-2)25-23(26-21(14)24)28-9-7-27(8-10-28)22(29)20-13-32-16-5-3-4-6-17(16)33-20/h3-6,11-12,20H,7-10,13H2,1-2H3,(H2,24,25,26)
- IUPAC Name
- 2-[4-(2,3-dihydro-1,4-benzodioxine-2-carbonyl)piperazin-1-yl]-6,7-dimethoxyquinazolin-4-amine
- SMILES
- COC1=C(OC)C=C2C(N)=NC(=NC2=C1)N1CCN(CC1)C(=O)C1COC2=CC=CC=C2O1
Pharmacology
- Indication
For treatment and management of mild to moderate hypertension and urinary obstruction symptoms caused by BPH.
- Associated Conditions
- Pharmacodynamics
Doxazosin is an alpha-adrenergic blocking agent used to treat hypertension and benign prostatic hyperplasia. Accordingly, Doxazosin is a selective inhibitor of the alpha1 subtype of alpha adrenergic receptors. In the human prostate, Doxazosin antagonizes phenylephrine (alpha1 agonist)-induced contractions, in vitro, and binds with high affinity to the alpha1a adrenoceptor, which is thought to be the predominant functional type in the prostate. Studies in normal human subjects have shown that Doxazosin competitively antagonized the pressor effects of phenylephrine (an alpha1 agonist) and the systolic pressor effect of norepinephrine. The antihypertensive effect of Doxazosin results from a decrease in systemic vascular resistance and the parent compound Doxazosin is primarily responsible for the antihypertensive activity.
- Mechanism of action
Doxazosin acts by inhibiting the postsynaptic alpha(1)-adrenoceptors on vascular smooth muscle. This inhibits the vasoconstrictor effect of circulating and locally released catecholamines (epinephrine and norepinephrine), resulting in peripheral vasodilation.
Target Actions Organism AAlpha-1A adrenergic receptor antagonistHumans AAlpha-1B adrenergic receptor antagonistHumans AAlpha-1D adrenergic receptor antagonistHumans UPotassium voltage-gated channel subfamily H member 2 inhibitorHumans UPotassium voltage-gated channel subfamily H member 6 inhibitorHumans UPotassium voltage-gated channel subfamily H member 7 inhibitorHumans - Absorption
65%
- Volume of distribution
- Not Available
- Protein binding
98%
- Metabolism
Hepatic.
- Route of elimination
On average only 4.8% of the dose was excreted as unchanged drug in the feces and only a trace of the total radioactivity in the urine was attributed to unchanged drug.
- Half life
22 hours
- Clearance
- Not Available
- Toxicity
Symptoms of overdose include hypotension. Oral LD50 is greater than 1000 mg/kg in mice and rats.
- Affected organisms
- Humans and other mammals
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
Drug Interaction (R)-warfarin The metabolism of (R)-warfarin can be decreased when combined with Doxazosin. (S)-Warfarin The metabolism of (S)-Warfarin can be decreased when combined with Doxazosin. 1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic Acid Doxazosin may increase the hypotensive activities of 1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic Acid. 1-benzylimidazole 1-benzylimidazole may decrease the antihypertensive activities of Doxazosin. 2,5-Dimethoxy-4-ethylamphetamine The therapeutic efficacy of Doxazosin can be decreased when used in combination with 2,5-Dimethoxy-4-ethylamphetamine. 2,5-Dimethoxy-4-ethylthioamphetamine The therapeutic efficacy of Doxazosin can be decreased when used in combination with 2,5-Dimethoxy-4-ethylthioamphetamine. 3,4-Methylenedioxyamphetamine The therapeutic efficacy of Doxazosin can be decreased when used in combination with 3,4-Methylenedioxyamphetamine. 3,5-diiodothyropropionic acid The metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Doxazosin. 4-Bromo-2,5-dimethoxyamphetamine The therapeutic efficacy of Doxazosin can be decreased when used in combination with 4-Bromo-2,5-dimethoxyamphetamine. 4-hydroxycoumarin The metabolism of 4-hydroxycoumarin can be decreased when combined with Doxazosin. - Food Interactions
- Avoid alcohol.
- Avoid natural licorice.
- Take without regard to meals.
References
- Synthesis Reference
K. S. Keshava Murthy, Gamini Weeratunga, Tianhao Zhou, Bhaskar Reddy Guntoori, "Process for the manufacture of intermediates suitable to make doxazosin, terazosin, prazosin, tiodazosin and related antihypertensive medicines." U.S. Patent US5919931, issued September, 1986.
US5919931- General References
- Cushman WC, Ford CE, Cutler JA, Margolis KL, Davis BR, Grimm RH, Black HR, Hamilton BP, Holland J, Nwachuku C, Papademetriou V, Probstfield J, Wright JT Jr, Alderman MH, Weiss RJ, Piller L, Bettencourt J, Walsh SM: Success and predictors of blood pressure control in diverse North American settings: the antihypertensive and lipid-lowering treatment to prevent heart attack trial (ALLHAT). J Clin Hypertens (Greenwich). 2002 Nov-Dec;4(6):393-404. [PubMed:12461301]
- External Links
- Human Metabolome Database
- HMDB0014728
- KEGG Drug
- D07874
- KEGG Compound
- C06970
- PubChem Compound
- 3157
- PubChem Substance
- 46506825
- ChemSpider
- 3045
- BindingDB
- 86731
- ChEBI
- 4708
- ChEMBL
- CHEMBL707
- Therapeutic Targets Database
- DAP000381
- PharmGKB
- PA449407
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- PDRhealth
- PDRhealth Drug Page
- Wikipedia
- Doxazosin
- ATC Codes
- C02CA04 — Doxazosin
- AHFS Codes
- 24:20.00 — Alpha-adrenergic Blocking Agents
- FDA label
- Download (511 KB)
Clinical Trials
- Clinical Trials
Pharmacoeconomics
- Manufacturers
- Pfizer inc
- Pfizer laboratories div pfizer inc
- Actavis elizabeth llc
- Apotex inc
- Dava pharmaceuticals inc
- Genpharm inc
- Ivax pharmaceuticals inc sub teva pharmaceuticals usa
- Kv pharmaceutical co
- Mylan pharmaceuticals inc
- Pliva inc
- Sandoz inc
- Teva pharmaceuticals usa inc
- Watson laboratories inc
- Packagers
- Actavis Group
- Advanced Pharmaceutical Services Inc.
- Amerisource Health Services Corp.
- Apotex Inc.
- A-S Medication Solutions LLC
- Cardinal Health
- DAVA Pharmaceuticals
- Dept Health Central Pharmacy
- Direct Dispensing Inc.
- Dispensing Solutions
- Diversified Healthcare Services Inc.
- General Injectables and Vaccines Inc.
- Golden State Medical Supply Inc.
- Heartland Repack Services LLC
- International Laboratories Inc.
- Ivax Pharmaceuticals
- Legacy Pharmaceuticals Packaging LLC
- Major Pharmaceuticals
- Merrell Pharmaceuticals Inc.
- Murfreesboro Pharmaceutical Nursing Supply
- Mylan
- Novopharm Ltd.
- Nucare Pharmaceuticals Inc.
- Palmetto Pharmaceuticals Inc.
- Par Pharmaceuticals
- Patheon Inc.
- Pfizer Inc.
- Pharmaceutical Utilization Management Program VA Inc.
- Physicians Total Care Inc.
- Pliva Inc.
- Preferred Pharmaceuticals Inc.
- Prepackage Specialists
- Prepak Systems Inc.
- Redpharm Drug
- Remedy Repack
- Sandhills Packaging Inc.
- Southwood Pharmaceuticals
- Stat Rx Usa
- Teva Pharmaceutical Industries Ltd.
- Torpharm Inc.
- Tya Pharmaceuticals
- UDL Laboratories
- US Pharmaceutical Group
- Vangard Labs Inc.
- Dosage forms
Form Route Strength Tablet, multilayer, extended release Oral 4 mg/1 Tablet, multilayer, extended release Oral 8 mg/1 Tablet Oral 1 mg Kit; tablet Oral Tablet Oral 2 mg Tablet Oral 4 mg Tablet Oral 1 mg/1 Tablet Oral 2 mg/1 Tablet Oral 4 mg/1 Tablet Oral 8 mg/1 - Prices
Unit description Cost Unit Cardura XL 4 mg 24 Hour tablet 2.22USD tablet Cardura xl 8 mg tablet 2.04USD tablet Cardura xl 4 mg tablet 1.94USD tablet Cardura 8 mg tablet 1.93USD tablet Cardura 4 mg tablet 1.89USD tablet Cardura 2 mg tablet 1.81USD tablet Cardura 1 mg tablet 1.72USD tablet Doxazosin mesylate 8 mg tablet 1.04USD tablet Cardura 4 mg Tablet 1.0USD tablet Doxazosin mesylate 4 mg tablet 0.99USD tablet Doxazosin mesylate 1 mg tablet 0.94USD tablet Doxazosin mesylate 2 mg tablet 0.94USD tablet Cardura 2 mg Tablet 0.77USD tablet Cardura 1 mg Tablet 0.64USD tablet Apo-Doxazosin 4 mg Tablet 0.56USD tablet Mylan-Doxazosin 4 mg Tablet 0.56USD tablet Novo-Doxazosin 4 mg Tablet 0.56USD tablet Pms-Doxazosin 4 mg Tablet 0.56USD tablet Apo-Doxazosin 2 mg Tablet 0.43USD tablet Mylan-Doxazosin 2 mg Tablet 0.43USD tablet Novo-Doxazosin 2 mg Tablet 0.43USD tablet Pms-Doxazosin 2 mg Tablet 0.43USD tablet Apo-Doxazosin 1 mg Tablet 0.36USD tablet Mylan-Doxazosin 1 mg Tablet 0.36USD tablet Novo-Doxazosin 1 mg Tablet 0.36USD tablet Pms-Doxazosin 1 mg Tablet 0.36USD tablet DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 289-290 °C Not Available water solubility 24 mg/L Not Available logP 2.1 Not Available - Predicted Properties
Property Value Source Water Solubility 0.79 mg/mL ALOGPS logP 2.53 ALOGPS logP 2.14 ChemAxon logS -2.8 ALOGPS pKa (Strongest Acidic) 12.67 ChemAxon pKa (Strongest Basic) 7.24 ChemAxon Physiological Charge 1 ChemAxon Hydrogen Acceptor Count 9 ChemAxon Hydrogen Donor Count 1 ChemAxon Polar Surface Area 112.27 Å2 ChemAxon Rotatable Bond Count 4 ChemAxon Refractivity 121.64 m3·mol-1 ChemAxon Polarizability 46.63 Å3 ChemAxon Number of Rings 5 ChemAxon Bioavailability 1 ChemAxon Rule of Five Yes ChemAxon Ghose Filter Yes ChemAxon Veber's Rule No ChemAxon MDDR-like Rule No ChemAxon - Predicted ADMET features
Property Value Probability Human Intestinal Absorption + 1.0 Blood Brain Barrier + 0.9627 Caco-2 permeable + 0.7863 P-glycoprotein substrate Substrate 0.7303 P-glycoprotein inhibitor I Non-inhibitor 0.7391 P-glycoprotein inhibitor II Non-inhibitor 0.9528 Renal organic cation transporter Non-inhibitor 0.6909 CYP450 2C9 substrate Non-substrate 0.9011 CYP450 2D6 substrate Non-substrate 0.8195 CYP450 3A4 substrate Substrate 0.7228 CYP450 1A2 substrate Non-inhibitor 0.8293 CYP450 2C9 inhibitor Non-inhibitor 0.9161 CYP450 2D6 inhibitor Non-inhibitor 0.9533 CYP450 2C19 inhibitor Non-inhibitor 0.9084 CYP450 3A4 inhibitor Non-inhibitor 0.8002 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9078 Ames test Non AMES toxic 0.5648 Carcinogenicity Non-carcinogens 0.8905 Biodegradation Not ready biodegradable 0.9854 Rat acute toxicity 2.1954 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.8602 hERG inhibition (predictor II) Inhibitor 0.823
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Taxonomy
- Description
- This compound belongs to the class of organic compounds known as n-arylpiperazines. These are organic compounds containing a piperazine ring where the nitrogen ring atom carries an aryl group.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Diazinanes
- Sub Class
- Piperazines
- Direct Parent
- N-arylpiperazines
- Alternative Parents
- Quinazolinamines / Benzo-1,4-dioxanes / Anisoles / Dialkylarylamines / Alkyl aryl ethers / Aminopyrimidines and derivatives / Para dioxins / Imidolactams / Tertiary carboxylic acid amides / Heteroaromatic compounds show 8 more
- Substituents
- N-arylpiperazine / Quinazolinamine / Diazanaphthalene / Benzo-1,4-dioxane / Benzodioxane / Quinazoline / Anisole / Dialkylarylamine / Alkyl aryl ether / Aminopyrimidine show 23 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- N-arylpiperazine, monocarboxylic acid amide, aromatic amine, quinazolines, benzodioxine, N-acylpiperazine (CHEBI:4708)
Targets
- 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
- Yono M, Foster HE Jr, Shin D, Takahashi W, Pouresmail M, Latifpour J: Doxazosin-induced up-regulation of alpha 1A-adrenoceptor mRNA in the rat lower urinary tract. Can J Physiol Pharmacol. 2004 Oct;82(10):872-8. [PubMed:15573147]
- Michel MC, Grubbel B, Taguchi K, Verfurth F, Otto T, Kropfl D: Drugs for treatment of benign prostatic hyperplasia: affinity comparison at cloned alpha 1-adrenoceptor subtypes and in human prostate. J Auton Pharmacol. 1996 Feb;16(1):21-8. [PubMed:8736427]
- Roehrborn CG, Schwinn DA: Alpha1-adrenergic receptors and their inhibitors in lower urinary tract symptoms and benign prostatic hyperplasia. J Urol. 2004 Mar;171(3):1029-35. [PubMed:14767264]
- Ishizuka O, Pandita RK, Mattiasson A, Steers WD, Andersson KE: Stimulation of bladder activity by volume, L-dopa and capsaicin in normal conscious rats--effects of spinal alpha 1-adrenoceptor blockade. Naunyn Schmiedebergs Arch Pharmacol. 1997 Jun;355(6):787-93. [PubMed:9205965]
- Bae JH, Jung PB, Lee JG: The effects of alpha-adrenoceptor antagonists on the urethral perfusion pressure of the female rat. BJU Int. 2005 Nov;96(7):1131-5. [PubMed:16225542]
- Greco KA, McVary KT: The role of combination medical therapy in benign prostatic hyperplasia. Int J Impot Res. 2008 Dec;20 Suppl 3:S33-43. doi: 10.1038/ijir.2008.51. [PubMed:19002123]
- Shannon R, Chaudhry M: Effect of alpha1-adrenergic receptors in cardiac pathophysiology. Am Heart J. 2006 Nov;152(5):842-50. [PubMed:17070143]
- Martin DJ: Preclinical pharmacology of alpha1-adrenoceptor antagonists. Eur Urol. 1999;36 Suppl 1:35-41; discussion 65. [PubMed:10393471]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
- 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
- Lepor H: Alpha blockers for the treatment of benign prostatic hyperplasia. Rev Urol. 2007 Fall;9(4):181-90. [PubMed:18231614]
- Greco KA, McVary KT: The role of combination medical therapy in benign prostatic hyperplasia. Int J Impot Res. 2008 Dec;20 Suppl 3:S33-43. doi: 10.1038/ijir.2008.51. [PubMed:19002123]
- Shannon R, Chaudhry M: Effect of alpha1-adrenergic receptors in cardiac pathophysiology. Am Heart J. 2006 Nov;152(5):842-50. [PubMed:17070143]
- Martin DJ: Preclinical pharmacology of alpha1-adrenoceptor antagonists. Eur Urol. 1999;36 Suppl 1:35-41; discussion 65. [PubMed:10393471]
- 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
- Lepor H: Alpha blockers for the treatment of benign prostatic hyperplasia. Rev Urol. 2007 Fall;9(4):181-90. [PubMed:18231614]
- Greco KA, McVary KT: The role of combination medical therapy in benign prostatic hyperplasia. Int J Impot Res. 2008 Dec;20 Suppl 3:S33-43. doi: 10.1038/ijir.2008.51. [PubMed:19002123]
- Shannon R, Chaudhry M: Effect of alpha1-adrenergic receptors in cardiac pathophysiology. Am Heart J. 2006 Nov;152(5):842-50. [PubMed:17070143]
- Martin DJ: Preclinical pharmacology of alpha1-adrenoceptor antagonists. Eur Urol. 1999;36 Suppl 1:35-41; discussion 65. [PubMed:10393471]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- 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
- Thomas D, Wimmer AB, Wu K, Hammerling BC, Ficker EK, Kuryshev YA, Kiehn J, Katus HA, Schoels W, Karle CA: Inhibition of human ether-a-go-go-related gene potassium channels by alpha 1-adrenoceptor antagonists prazosin, doxazosin, and terazosin. Naunyn Schmiedebergs Arch Pharmacol. 2004 May;369(5):462-72. Epub 2004 Apr 20. [PubMed:15098086]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Voltage-gated potassium channel activity
- Specific Function
- Pore-forming (alpha) subunit of voltage-gated potassium channel. Elicits a slowly activating, rectifying current (By similarity). Channel properties may be modulated by cAMP and subunit assembly.
- Gene Name
- KCNH6
- Uniprot ID
- Q9H252
- Uniprot Name
- Potassium voltage-gated channel subfamily H member 6
- Molecular Weight
- 109923.705 Da
References
- Thomas D, Wimmer AB, Wu K, Hammerling BC, Ficker EK, Kuryshev YA, Kiehn J, Katus HA, Schoels W, Karle CA: Inhibition of human ether-a-go-go-related gene potassium channels by alpha 1-adrenoceptor antagonists prazosin, doxazosin, and terazosin. Naunyn Schmiedebergs Arch Pharmacol. 2004 May;369(5):462-72. Epub 2004 Apr 20. [PubMed:15098086]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Voltage-gated potassium channel activity
- Specific Function
- Pore-forming (alpha) subunit of voltage-gated potassium channel. Channel properties may be modulated by cAMP and subunit assembly.
- Gene Name
- KCNH7
- Uniprot ID
- Q9NS40
- Uniprot Name
- Potassium voltage-gated channel subfamily H member 7
- Molecular Weight
- 134998.525 Da
References
- Thomas D, Wimmer AB, Wu K, Hammerling BC, Ficker EK, Kuryshev YA, Kiehn J, Katus HA, Schoels W, Karle CA: Inhibition of human ether-a-go-go-related gene potassium channels by alpha 1-adrenoceptor antagonists prazosin, doxazosin, and terazosin. Naunyn Schmiedebergs Arch Pharmacol. 2004 May;369(5):462-72. Epub 2004 Apr 20. [PubMed:15098086]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Steroid hydroxylase activity
- Specific Function
- Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
- Gene Name
- CYP2C19
- Uniprot ID
- P33261
- Uniprot Name
- Cytochrome P450 2C19
- Molecular Weight
- 55930.545 Da
References
- Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- 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
- Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- 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
- Dailymed [Link]
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- General Function
- Not Available
- Specific Function
- Functions as transport protein in the blood stream. Binds various ligands in the interior of its beta-barrel domain. Also binds synthetic drugs and influences their distribution and availability in...
- Gene Name
- ORM1
- Uniprot ID
- P02763
- Uniprot Name
- Alpha-1-acid glycoprotein 1
- Molecular Weight
- 23511.38 Da
References
- Ferry DG, Caplan NB, Cubeddu LX: Interaction between antidepressants and alpha 1-adrenergic receptor antagonists on the binding to alpha 1-acid glycoprotein. J Pharm Sci. 1986 Feb;75(2):146-9. [PubMed:2870173]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- 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
- Takara K, Kakumoto M, Tanigawara Y, Funakoshi J, Sakaeda T, Okumura K: Interaction of digoxin with antihypertensive drugs via MDR1. Life Sci. 2002 Feb 15;70(13):1491-500. [PubMed:11895100]
- Takara K, Sakaeda T, Kakumoto M, Tanigawara Y, Kobayashi H, Okumura K, Ohnishi N, Yokoyama T: Effects of alpha-adrenoceptor antagonist doxazosin on MDR1-mediated multidrug resistance and transcellular transport. Oncol Res. 2009;17(11-12):527-33. [PubMed:19806783]
- 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
References
- Stage TB, Brosen K, Christensen MM: A Comprehensive Review of Drug-Drug Interactions with Metformin. Clin Pharmacokinet. 2015 Aug;54(8):811-24. doi: 10.1007/s40262-015-0270-6. [PubMed:25943187]
Drug created on June 13, 2005 07:24 / Updated on February 22, 2019 22:55