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Trials

Economics

Properties

Spectra

Taxonomy

Midodrine

Targets (3)Enzymes (1)Transporters (1)Biointeractions (4)

Identification

Name

Midodrine

Accession Number

DB00211 (APRD01116)

Type

Small Molecule

Groups

Approved

Description

An ethanolamine derivative that is an adrenergic alpha agonist. It is used as a vasoconstrictor agent in the treatment of hypotension.

Structure

Similar Structures

Synonyms

(±)-2-amino-N-(β-hydroxy-2,5-dimethoxyphenethyl)acetamide
1-(2',5'-Dimethoxyphenyl)-2-glycinamidoethanol
2-Amino-N-(2,5-dimethoxy-beta-hydroxyphenethyl)acetamide
DL-N1-(beta-Hydroxy-2,5-dimethoxyphenethyl)glycinamid
Midodrin
Midodrina
Midodrine
Midodrinum

External IDs

ST 1085 / ST-1085

Product Ingredients

Ingredient	UNII	CAS	InChI Key
Midodrine hydrochloride	59JV96YTXV	43218-56-0	MGCQZNBCJBRZDT-UHFFFAOYSA-N

Product Images

Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Amatine	Tablet	5 mg	Oral	Shire Pharma Canada Ulc	1992-12-31	2010-10-04
Amatine	Tablet	2.5 mg	Oral	Shire Pharma Canada Ulc	1992-12-31	2010-09-30
Midodrine	Tablet	5.0 mg	Oral	Aa Pharma Inc	2006-06-13	Not applicable
Midodrine	Tablet	2.5 mg	Oral	Aa Pharma Inc	2006-06-13	Not applicable
ProAmatine	Tablet	10 mg/1	Oral	Shire	1996-09-06	2010-12-31
ProAmatine	Tablet	5 mg/1	Oral	Shire	1996-09-06	2010-12-31
ProAmatine	Tablet	2.5 mg/1	Oral	Shire	1996-09-06	2010-12-31
ProAmatine	Tablet	5 mg/1	Oral	Physicians Total Care, Inc.	2005-09-30	Not applicable

Generic Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Mar-midodrine	Tablet	5 mg	Oral	Marcan Pharmaceuticals Inc	Not applicable	Not applicable
Mar-midodrine	Tablet	2.5 mg	Oral	Marcan Pharmaceuticals Inc	Not applicable	Not applicable
Midodrine HCl	Tablet	5 mg/1	Oral	Eon Labs, Inc.	2003-09-11	Not applicable
Midodrine HCl	Tablet	5 mg/1	Oral	Amerincan Health Packaging	2010-05-06	2019-08-31
Midodrine HCl	Tablet	5 mg/1	Oral	Cardinal Health	2004-11-03	2015-11-30
Midodrine HCl	Tablet	10 mg/1	Oral	Rebel Distributors	2002-07-02	Not applicable
Midodrine HCl	Tablet	2.5 mg/1	Oral	Eon Labs, Inc.	2003-09-11	Not applicable
Midodrine HCl	Tablet	5 mg/1	Oral	Cardinal Health	2012-11-26	Not applicable
Midodrine HCl	Tablet	2.5 mg/1	Oral	Amerincan Health Packaging	2010-09-14	2019-03-31
Midodrine HCl	Tablet	2.5 mg/1	Oral	Cardinal Health	2010-05-11	2019-05-31

Categories

UNII

6YE7PBM15H

CAS number

42794-76-3

Weight

Average: 254.2823
Monoisotopic: 254.126657074

Chemical Formula

C₁₂H₁₈N₂O₄

InChI Key

PTKSEFOSCHHMPD-UHFFFAOYSA-N

InChI

InChI=1S/C12H18N2O4/c1-17-8-3-4-11(18-2)9(5-8)10(15)7-14-12(16)6-13/h3-5,10,15H,6-7,13H2,1-2H3,(H,14,16)

IUPAC Name

2-amino-N-[2-(2,5-dimethoxyphenyl)-2-hydroxyethyl]acetamide

SMILES

COC1=CC(C(O)CNC(=O)CN)=C(OC)C=C1

Pharmacology

Indication

For the treatment of symptomatic orthostatic hypotension (OH).

Associated Conditions

Symptomatic Orthostatic Hypotension

Pharmacodynamics

Midodrine is a prodrug, i.e., the therapeutic effect of orally administered midodrine is due to the major metabolite desglymidodrine formed by deglycination of midodrine. Desglymidodrine diffuses poorly across the blood-brain barrier, and is therefore not associated with effects on the central nervous system. Administration of midodrine results in a rise in standing, sitting, and supine systolic and diastolic blood pressure in patients with orthostatic hypotension of various etiologies. Standing systolic blood pressure is elevated by approximately 15 to 30 mmHg at 1 hour after a 10-mg dose of midodrine, with some effect persisting for 2 to 3 hours. Midodrine has no clinically significant effect on standing or supine pulse rates in patients with autonomic failure.

Mechanism of action

Midodrine forms an active metabolite, desglymidodrine, that is an alpha₁-agonist, and exerts its actions via activation of the alpha-adrenergic receptors of the arteriolar and venous vasculature, producing an increase in vascular tone and elevation of blood pressure. Desglymidodrine does not stimulate cardiac beta-adrenergic receptors.

Target	Actions	Organism
AAlpha-1A adrenergic receptor	agonist	Humans
AAlpha-1B adrenergic receptor	agonist	Humans
UAlpha-1D adrenergic receptor	agonist	Humans

Absorption

Rapidly absorbed following oral administration. The absolute bioavailability of midodrine (measured as desglymidodrine) is 93% and is not affected by food.

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism

Thorough metabolic studies have not been conducted, but it appears that deglycination of midodrine to desglymidodrine takes place in many tissues, and both compounds are metabolized in part by the liver.

Midodrine
desglymidodrine

Route of elimination

Not Available

Half life

The plasma levels of the prodrug peak after about half an hour, and decline with a half-life of approximately 25 minutes, while the metabolite reaches peak blood concentrations about 1 to 2 hours after a dose of midodrine and has a half-life of about 3 to 4 hours.

Clearance

Renal cl=385 mL/minute

Toxicity

Symptoms of overdose could include hypertension, piloerection (goosebumps), a sensation of coldness and urinary retention. The single doses that would be associated with symptoms of overdosage or would be potentially life- threatening are unknown. The oral LD₅₀ is approximately 30 to 50 mg/kg in rats, 675 mg/kg in mice, and 125 to 160 mg/kg in dogs. Desglymidodrine is dialyzable.

Affected organisms

Humans and other mammals

Pathways

Not Available

Pharmacogenomic Effects/ADRs

Not Available

Interactions

Drug Interactions

Drug	Interaction
1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic Acid	The risk or severity of hypertension can be increased when Midodrine is combined with 1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic Acid.
1-benzylimidazole	The risk or severity of hypertension can be increased when Midodrine is combined with 1-benzylimidazole.
2,5-Dimethoxy-4-ethylamphetamine	The risk or severity of adverse effects can be increased when Midodrine is combined with 2,5-Dimethoxy-4-ethylamphetamine.
2,5-Dimethoxy-4-ethylthioamphetamine	The risk or severity of adverse effects can be increased when Midodrine is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
3-isobutyl-1-methyl-7H-xanthine	The risk or severity of adverse effects can be increased when Midodrine is combined with 3-isobutyl-1-methyl-7H-xanthine.
3,4-Methylenedioxyamphetamine	The risk or severity of adverse effects can be increased when Midodrine is combined with 3,4-Methylenedioxyamphetamine.
3,5-diiodothyropropionic acid	The therapeutic efficacy of Midodrine can be increased when used in combination with 3,5-diiodothyropropionic acid.
4-Bromo-2,5-dimethoxyamphetamine	The risk or severity of adverse effects can be increased when Midodrine is combined with 4-Bromo-2,5-dimethoxyamphetamine.
4-Methoxyamphetamine	The metabolism of 4-Methoxyamphetamine can be decreased when combined with Midodrine.
5-methoxy-N,N-dimethyltryptamine	The risk or severity of hypertension can be increased when Midodrine is combined with 5-methoxy-N,N-dimethyltryptamine.

Food Interactions

Take without regard to meals.

References

Synthesis Reference

Anup K. Ray, Hiren Patel, Mahendra R. Patel, "Synthesis of midodrine HCI from a novel intermediate 1-(2',5'-dimethoxyphenyl)-2-azidoethanone." U.S. Patent US6201153, issued July, 1965.

US6201153

General References

Hebenstreit G: [Treatment of hypotension caused by psychopharmacological drugs (author's transl)]. Wien Med Wochenschr. 1981 Feb 28;131(4):109-12. [PubMed:6165144]
Tsuda M, Terada T, Irie M, Katsura T, Niida A, Tomita K, Fujii N, Inui K: Transport characteristics of a novel peptide transporter 1 substrate, antihypotensive drug midodrine, and its amino acid derivatives. J Pharmacol Exp Ther. 2006 Jul;318(1):455-60. Epub 2006 Apr 5. [PubMed:16597710]

External Links

Human Metabolome Database: HMDB0014356
KEGG Drug: D08220
KEGG Compound: C07890
PubChem Compound: 4195
PubChem Substance: 46507373
ChemSpider: 4050
ChEBI: 6933
ChEMBL: CHEMBL1201212
Therapeutic Targets Database: DAP000229
PharmGKB: PA164749381
RxList: RxList Drug Page
Drugs.com: Drugs.com Drug Page
Wikipedia: Midodrine

ATC Codes

C01CA17 — Midodrine

AHFS Codes

12:12.04 — Alpha-adrenergic Agonists

Clinical Trials

Clinical Trials

Phase	Status	Purpose	Conditions	Count
1	Completed	Not Available	Autonomic Failure / Idiopathic orthostatic hypotension	1
1	Completed	Not Available	Healthy Volunteers	3
1	Not Yet Recruiting	Treatment	Hepatopulmonary Syndrome (HPS)	1
1	Recruiting	Basic Science	Autonomic Failure / Idiopathic orthostatic hypotension / Multiple System Atrophy (MSA) / Parkinson's Disease (PD) / Progressive autonomic failure	1
1	Recruiting	Other	Autonomic Failure / Idiopathic orthostatic hypotension / Multiple System Atrophy (MSA) / Progressive autonomic failure	1
1	Recruiting	Treatment	Blood Pressures / Sepsis	1
1, 2	Active Not Recruiting	Treatment	Chronic Orthostatic Intolerance / Tachycardia	1
2	Completed	Treatment	Acute Ischemic Stroke (AIS)	1
2	Completed	Treatment	Liver Cirrhosis / Renal Failure	1
2	Completed	Treatment	Idiopathic orthostatic hypotension / Spinal Cord Injuries (SCI)	2
2	Completed	Treatment	Idiopathic orthostatic hypotension	1
2	Recruiting	Treatment	Autonomic Dysreflexia / Autonomic Integrity / Baroreceptor Integrity / Blood Pressures / Cerebral Blood Flow / Cognitive Function / Hypotensive / Spinal Cord Injuries (SCI) / Sympathetic Integrity / Vagal Integrity	1
2	Recruiting	Treatment	Fibrosis / Hepatorenal Syndrome / Renal Failure	1
2, 3	Active Not Recruiting	Treatment	Liver Cirrhosis / Refractory/Recurrent Ascites	1
2, 3	Completed	Treatment	Refractory Ascites / Type 2 Hepatorenal Syndrome	1
2, 3	Recruiting	Treatment	Arterial Hypotension / Autonomic Dysreflexia / Baroreceptor Integrity / Blood Pressures / Cerebral Blood Flow / Idiopathic orthostatic hypotension / Spinal Cord Injuries (SCI) / Sympathetic Integrity / Vagal Integrity / Venous Occlusion Plethysmography	1
3	Completed	Prevention	Postoperative Orthostatic Hypotension / Postoperative Orthostatic Intolerance	1
3	Recruiting	Treatment	Arterial Hypotension / Critical Illness	1
3	Recruiting	Treatment	Shock, Septic	1
3	Recruiting	Treatment	Spinal Cord Injuries (SCI)	1
3	Terminated	Treatment	Shock, Septic	1
4	Completed	Not Available	Hypothermia / Mild Cognitive Impairment (MCI) / Quadriplegia	1
4	Completed	Prevention	Gastrointestinal Bleedings / Hepatic Encephalopathy / Hyponatremias / Renal Failure / Sepsis	1
4	Completed	Treatment	Ascites / Liver Cirrhosis	1
4	Completed	Treatment	Symptomatic Orthostatic Hypotension	1
4	Completed	Treatment	Idiopathic orthostatic hypotension	3
4	Enrolling by Invitation	Treatment	Intradialytic Hypotension	1
4	Recruiting	Supportive Care	Hypothermia / Mild Cognitive Impairment (MCI) / Quadriplegia	1
4	Recruiting	Treatment	Neurogenic Orthostatic Hypotension	1
4	Recruiting	Treatment	Orthostatic; Hypotension, Neurogenic	1
4	Recruiting	Treatment	Syncope, Vasovagal	1
4	Terminated	Treatment	Idiopathic orthostatic hypotension	1
4	Withdrawn	Supportive Care	Arterial Hypotension / Sepsis / Shock, Septic	1
Not Available	Completed	Not Available	Orthostatic Intolerance	1
Not Available	Completed	Treatment	Acute Kidney Injury (AKI)	1
Not Available	Completed	Treatment	Liver Cirrhosis	1
Not Available	Completed	Treatment	Syncope	1
Not Available	Not Yet Recruiting	Treatment	Hepatic Hydrothorax	1
Not Available	Recruiting	Treatment	Orthostatic Intolerance / Parkinson's Disease (PD)	1
Not Available	Terminated	Treatment	Idiopathic orthostatic hypotension	1
Not Available	Withdrawn	Not Available	Strokes	1
Not Available	Withdrawn	Treatment	Arterial Hypotension / Ascites / End Stage Liver Diseases / Liver Cirrhosis	1

Pharmacoeconomics

Manufacturers

Apotex inc etobicoke site
Impax pharmaceuticals
Mylan pharmaceuticals inc
Sandoz inc
Upsher smith laboratories inc
Shire development inc

Packagers

Actavis Group
Amerisource Health Services Corp.
Apotex Inc.
Eon Labs
Global Pharmaceuticals
Heartland Repack Services LLC
Impax Laboratories Inc.
Kaiser Foundation Hospital
Murfreesboro Pharmaceutical Nursing Supply
Mylan
Nycomed Inc.
Physicians Total Care Inc.
Rebel Distributors Corp.
Resource Optimization and Innovation LLC
Shire Inc.
UDL Laboratories
Upsher Smith Laboratories
Vangard Labs Inc.

Dosage forms

Form	Route	Strength
Tablet	Oral	5 mg
Tablet	Oral	2.5 mg
Tablet	Oral	5.0 mg
Tablet	Oral	10 mg/1
Tablet	Oral	2.5 mg/1
Tablet	Oral	5 mg/1

Prices

Unit description	Cost	Unit
Proamatine 10 mg tablet	5.91USD	tablet
Midodrine hcl 10 mg tablet	4.93USD	tablet
Proamatine 5 mg tablet	3.08USD	tablet
Midodrine hcl 5 mg tablet	2.47USD	tablet
Proamatine 2.5 mg tablet	1.53USD	tablet
Midodrine hcl 2.5 mg tablet	1.23USD	tablet
Apo-Midodrine 5 mg Tablet	0.59USD	tablet
Apo-Midodrine 2.5 mg Tablet	0.35USD	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)	200 to 203°C	Not Available
water solubility	Soluble	Not Available
logP	-0.5	Not Available
pKa	7.8	Not Available

Predicted Properties

Property	Value	Source
Water Solubility	4.45 mg/mL	ALOGPS
logP	-0.49	ALOGPS
logP	-0.95	ChemAxon
logS	-1.8	ALOGPS
pKa (Strongest Acidic)	13.77	ChemAxon
pKa (Strongest Basic)	8.14	ChemAxon
Physiological Charge	1	ChemAxon
Hydrogen Acceptor Count	5	ChemAxon
Hydrogen Donor Count	3	ChemAxon
Polar Surface Area	93.81 Å²	ChemAxon
Rotatable Bond Count	6	ChemAxon
Refractivity	66.22 m³·mol^-1	ChemAxon
Polarizability	26.65 Å³	ChemAxon
Number of Rings	1	ChemAxon
Bioavailability	1	ChemAxon
Rule of Five	Yes	ChemAxon
Ghose Filter	No	ChemAxon
Veber's Rule	No	ChemAxon
MDDR-like Rule	No	ChemAxon

Predicted ADMET features

Property	Value	Probability
Human Intestinal Absorption	+	0.7686
Blood Brain Barrier	-	0.856
Caco-2 permeable	-	0.7382
P-glycoprotein substrate	Substrate	0.784
P-glycoprotein inhibitor I	Non-inhibitor	0.9781
P-glycoprotein inhibitor II	Non-inhibitor	0.9866
Renal organic cation transporter	Non-inhibitor	0.8896
CYP450 2C9 substrate	Non-substrate	0.8519
CYP450 2D6 substrate	Non-substrate	0.7593
CYP450 3A4 substrate	Non-substrate	0.5595
CYP450 1A2 substrate	Inhibitor	0.8848
CYP450 2C9 inhibitor	Non-inhibitor	0.9385
CYP450 2D6 inhibitor	Non-inhibitor	0.9231
CYP450 2C19 inhibitor	Inhibitor	0.8993
CYP450 3A4 inhibitor	Non-inhibitor	0.867
CYP450 inhibitory promiscuity	Low CYP Inhibitory Promiscuity	0.9316
Ames test	Non AMES toxic	0.774
Carcinogenicity	Non-carcinogens	0.8613
Biodegradation	Not ready biodegradable	0.9595
Rat acute toxicity	2.3137 LD50, mol/kg	Not applicable
hERG inhibition (predictor I)	Weak inhibitor	0.9772
hERG inhibition (predictor II)	Non-inhibitor	0.8604

ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)

Not Available

Spectra

Spectrum	Spectrum Type	Splash Key
Predicted GC-MS Spectrum - GC-MS	Predicted GC-MS	Not Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)	Predicted LC-MS/MS	Not Available

Taxonomy

Description: This compound belongs to the class of organic compounds known as dimethoxybenzenes. These are organic aromatic compounds containing a monocyclic benzene moiety carrying exactly two methoxy groups.
Kingdom: Organic compounds
Super Class: Benzenoids
Class: Benzene and substituted derivatives
Sub Class: Methoxybenzenes
Direct Parent: Dimethoxybenzenes
Alternative Parents: Phenoxy compounds / Anisoles / Alkyl aryl ethers / Secondary alcohols / Propargyl-type 1,3-dipolar organic compounds / Carboximidic acids / Organopnictogen compounds / Monoalkylamines / Hydrocarbon derivatives / Aromatic alcohols
Substituents: P-dimethoxybenzene / Dimethoxybenzene / Phenoxy compound / Anisole / Phenol ether / Alkyl aryl ether / Secondary alcohol / Carboximidic acid / Carboximidic acid derivative / Ether
Molecular Framework: Aromatic homomonocyclic compounds
External Descriptors: aromatic ether, amino acid amide, secondary alcohol (CHEBI:6933)

Targets

Details1. Alpha-1A adrenergic receptor

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Agonist

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

Buckner SA, Milicic I, Daza AV, Meyer MD, Altenbach RJ, Williams M, Sullivan JP, Brioni JD: ABT-866, a novel alpha(1A)-adrenoceptor agonist with antagonist properties at the alpha(1B)- and alpha(1D)-adrenoceptor subtypes. Eur J Pharmacol. 2002 Aug 2;449(1-2):159-65. [PubMed:12163120]
Taniguchi N, Hamada K, Ogasawara T, Ukai Y, Yoshikuni Y, Kimura K: NS-49, an alpha 1A-adrenoceptor agonist, selectively increases intraurethral pressure in dogs. Eur J Pharmacol. 1996 Dec 27;318(1):117-22. [PubMed:9007522]
Altenbach RJ, Khilevich A, Kolasa T, Rohde JJ, Bhatia PA, Patel MV, Searle XB, Yang F, Bunnelle WH, Tietje K, Bayburt EK, Carroll WA, Meyer MD, Henry R, Buckner SA, Kuk J, Daza AV, Milicic IV, Cain JC, Kang CH, Ireland LM, Carr TL, Miller TR, Hancock AA, Nakane M, Esbenshade TA, Brune ME, O'Neill AB, Gauvin DM, Katwala SP, Holladay MW, Brioni JD, Sullivan JP: Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist. J Med Chem. 2004 Jun 3;47(12):3220-35. [PubMed:15163201]

Details2. Alpha-1B adrenergic receptor

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Agonist

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

Altenbach RJ, Khilevich A, Kolasa T, Rohde JJ, Bhatia PA, Patel MV, Searle XB, Yang F, Bunnelle WH, Tietje K, Bayburt EK, Carroll WA, Meyer MD, Henry R, Buckner SA, Kuk J, Daza AV, Milicic IV, Cain JC, Kang CH, Ireland LM, Carr TL, Miller TR, Hancock AA, Nakane M, Esbenshade TA, Brune ME, O'Neill AB, Gauvin DM, Katwala SP, Holladay MW, Brioni JD, Sullivan JP: Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist. J Med Chem. 2004 Jun 3;47(12):3220-35. [PubMed:15163201]

Details3. Alpha-1D adrenergic receptor

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Agonist

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

Altenbach RJ, Khilevich A, Meyer MD, Buckner SA, Milicic I, Daza AV, Brune ME, O'Neill AB, Gauvin DM, Cain JC, Nakane M, Holladay MW, Williams M, Brioni JD, Sullivan JP: N-[3-(1H-imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),(1) a novel alpha(1)-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine. J Med Chem. 2002 Sep 26;45(20):4395-7. [PubMed:12238918]

Enzymes

Details1. Cytochrome P450 2D6

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Inhibitor

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]
Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]

Transporters

Details1. Solute carrier family 15 member 1

Kind: Protein
Organism: Humans
Pharmacological action: Unknown

General Function: Proton-dependent oligopeptide secondary active transmembrane transporter activity
Specific Function: Proton-coupled intake of oligopeptides of 2 to 4 amino acids with a preference for dipeptides. May constitute a major route for the absorption of protein digestion end-products.
Gene Name: SLC15A1
Uniprot ID: P46059
Uniprot Name: Solute carrier family 15 member 1
Molecular Weight: 78805.265 Da

References

Tsuda M, Terada T, Irie M, Katsura T, Niida A, Tomita K, Fujii N, Inui K: Transport characteristics of a novel peptide transporter 1 substrate, antihypotensive drug midodrine, and its amino acid derivatives. J Pharmacol Exp Ther. 2006 Jul;318(1):455-60. Epub 2006 Apr 5. [PubMed:16597710]

Drug created on June 13, 2005 07:24 / Updated on February 17, 2019 16:46

Midodrine

Identification

Structure for Midodrine (DB00211)

Pharmacology

Interactions

References

Clinical Trials

Pharmacoeconomics

Properties

Spectra

Taxonomy

Targets

References

References

References

Enzymes

References

Transporters

References