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Identification
NameMidodrine
Accession NumberDB00211  (APRD01116)
TypeSmall Molecule
GroupsApproved
Description

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

Structure
Thumb
Synonyms
(+-)-2-amino-N-(beta-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
Midodrinum
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Amatinetablet2.5 mgoralShire Pharma Canada Ulc1992-12-312010-09-30Canada
Amatinetablet5 mgoralShire Pharma Canada Ulc1992-12-312010-10-04Canada
Midodrinetablet5.0 mgoralAa Pharma Inc2006-06-13Not applicableCanada
Midodrinetablet2.5 mgoralAa Pharma Inc2006-06-13Not applicableCanada
Proamatinetablet2.5 mg/1oralShire US Manufacturing Inc.1996-09-06Not applicableUs
Proamatinetablet5 mg/1oralPhysicians Total Care, Inc.2005-09-30Not applicableUs
Proamatinetablet10 mg/1oralShire US Manufacturing Inc.2002-03-20Not applicableUs
Proamatinetablet5 mg/1oralShire US Manufacturing Inc.1996-09-06Not applicableUs
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Midodrine HCltablet2.5 mg/1oralAmerican Health Packaging2010-05-11Not applicableUs
Midodrine HCltablet2.5 mg/1oralEon Labs, Inc.2003-09-11Not applicableUs
Midodrine HCltablet5 mg/1oralCardinal Health2004-11-03Not applicableUs
Midodrine HCltablet5 mg/1oralMc Kesson Packaging Services A Business Unit Of Mc Kesson Corporation2012-11-26Not applicableUs
Midodrine HCltablet10 mg/1oralRebel Distributors Corp2002-07-02Not applicableUs
Midodrine HCltablet2.5 mg/1oralCardinal Health2010-05-11Not applicableUs
Midodrine HCltablet10 mg/1oralEon Labs, Inc.2002-07-02Not applicableUs
Midodrine HCltablet5 mg/1oralAmerican Health Packaging2010-05-11Not applicableUs
Midodrine HCltablet5 mg/1oralEon Labs, Inc.2003-09-11Not applicableUs
Midodrine HCltablet5 mg/1oralCardinal Health2004-11-03Not applicableUs
Midodrine Hydrochloridetablet5 mg/1oralAv Kare, Inc.2004-05-27Not applicableUs
Midodrine Hydrochloridetablet10 mg/1oralAmerican Health Packaging2015-09-01Not applicableUs
Midodrine Hydrochloridetablet5 mg/1oralAv Pak2011-08-17Not applicableUs
Midodrine Hydrochloridetablet2.5 mg/1oralMylan Pharmaceuticals Inc.2003-09-11Not applicableUs
Midodrine Hydrochloridetablet10 mg/1oralImpax Generics2005-12-16Not applicableUs
Midodrine Hydrochloridetablet10 mg/1oralUpsher Smith Laboratories Inc.2004-11-03Not applicableUs
Midodrine Hydrochloridetablet10 mg/1oralApotex Corp2006-09-12Not applicableUs
Midodrine Hydrochloridetablet2.5 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs2003-09-10Not applicableUs
Midodrine Hydrochloridetablet5 mg/1oralImpax Generics2004-05-27Not applicableUs
Midodrine Hydrochloridetablet2.5 mg/1oralPhysicians Total Care, Inc.2008-08-19Not applicableUs
Midodrine Hydrochloridetablet5 mg/1oralUpsher Smith Laboratories Inc.2004-11-03Not applicableUs
Midodrine Hydrochloridetablet5 mg/1oralApotex Corp2006-09-12Not applicableUs
Midodrine Hydrochloridetablet10 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs2003-09-10Not applicableUs
Midodrine Hydrochloridetablet2.5 mg/1oralImpax Generics2004-05-27Not applicableUs
Midodrine Hydrochloridetablet5 mg/1oralPhysicians Total Care, Inc.2006-01-01Not applicableUs
Midodrine Hydrochloridetablet2.5 mg/1oralUpsher Smith Laboratories Inc.2004-11-03Not applicableUs
Midodrine Hydrochloridetablet2.5 mg/1oralApotex Corp2006-09-12Not applicableUs
Midodrine Hydrochloridetablet5 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs2003-09-10Not applicableUs
Midodrine Hydrochloridetablet2.5 mg/1oralAvera Mc Kennan Hospital2015-03-01Not applicableUs
Midodrine Hydrochloridetablet5 mg/1oralMylan Institutional Inc.2006-09-11Not applicableUs
Midodrine Hydrochloridetablet5 mg/1oralCardinal Health2011-01-14Not applicableUs
Midodrine Hydrochloridetablet10 mg/1oralMylan Pharmaceuticals Inc.2003-09-11Not applicableUs
Midodrine Hydrochloridetablet2.5 mg/1oralAv Pak2011-08-17Not applicableUs
Midodrine Hydrochloridetablet5 mg/1oralCarilion Materials Management2004-05-27Not applicableUs
Midodrine Hydrochloridetablet10 mg/1oralAv Pak2011-08-17Not applicableUs
Midodrine Hydrochloridetablet5 mg/1oralMylan Pharmaceuticals Inc.2003-09-11Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Midodrine hydrochloride
43218-56-0
Thumb
  • InChI Key: MGCQZNBCJBRZDT-UHFFFAOYNA-N
  • Monoisotopic Mass: 290.103334813
  • Average Mass: 290.743
DBSALT000250
Categories
UNII6YE7PBM15H
CAS number42794-76-3
WeightAverage: 254.2823
Monoisotopic: 254.126657074
Chemical FormulaC12H18N2O4
InChI KeyInChIKey=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
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as alpha amino acid amides. These are amide derivatives of alpha amino acids.
KingdomOrganic compounds
Super ClassOrganic acids and derivatives
ClassCarboxylic acids and derivatives
Sub ClassAmino acids, peptides, and analogues
Direct ParentAlpha amino acid amides
Alternative Parents
Substituents
  • Alpha-amino acid amide
  • P-dimethoxybenzene
  • Dimethoxybenzene
  • Methoxybenzene
  • Phenol ether
  • Anisole
  • Alkyl aryl ether
  • Benzenoid
  • Monocyclic benzene moiety
  • Secondary carboxylic acid amide
  • Secondary alcohol
  • Carboxamide group
  • Ether
  • Carboxylic acid amide
  • Hydrocarbon derivative
  • Aromatic alcohol
  • Primary amine
  • Organooxygen compound
  • Organonitrogen compound
  • Primary aliphatic amine
  • Carbonyl group
  • Amine
  • Alcohol
  • Aromatic homomonocyclic compound
Molecular FrameworkAromatic homomonocyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor the treatment of symptomatic orthostatic hypotension (OH).
PharmacodynamicsMidodrine 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 actionMidodrine 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.
Related Articles
AbsorptionRapidly absorbed following oral administration. The absolute bioavailability of midodrine (measured as desglymidodrine) is 93% and is not affected by food.
Volume of distributionNot Available
Protein bindingNot 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.

SubstrateEnzymesProduct
Midodrine
Not Available
desglymidodrineDetails
Route of eliminationNot Available
Half lifeThe 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
ToxicitySymptoms 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
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.7686
Blood Brain Barrier-0.856
Caco-2 permeable-0.7382
P-glycoprotein substrateSubstrate0.784
P-glycoprotein inhibitor INon-inhibitor0.9781
P-glycoprotein inhibitor IINon-inhibitor0.9866
Renal organic cation transporterNon-inhibitor0.8896
CYP450 2C9 substrateNon-substrate0.8519
CYP450 2D6 substrateNon-substrate0.7593
CYP450 3A4 substrateNon-substrate0.5595
CYP450 1A2 substrateInhibitor0.8848
CYP450 2C9 inhibitorNon-inhibitor0.9385
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorInhibitor0.8993
CYP450 3A4 inhibitorNon-inhibitor0.867
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9316
Ames testNon AMES toxic0.774
CarcinogenicityNon-carcinogens0.8613
BiodegradationNot ready biodegradable0.9595
Rat acute toxicity2.3137 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9772
hERG inhibition (predictor II)Non-inhibitor0.8604
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Apotex inc etobicoke site
  • Impax pharmaceuticals
  • Mylan pharmaceuticals inc
  • Sandoz inc
  • Upsher smith laboratories inc
  • Shire development inc
Packagers
Dosage forms
FormRouteStrength
Tabletoral5 mg
Tabletoral2.5 mg
Tabletoral5.0 mg
Tabletoral10 mg/1
Tabletoral2.5 mg/1
Tabletoral5 mg/1
Prices
Unit descriptionCostUnit
Proamatine 10 mg tablet5.91USD tablet
Midodrine hcl 10 mg tablet4.93USD tablet
Proamatine 5 mg tablet3.08USD tablet
Midodrine hcl 5 mg tablet2.47USD tablet
Proamatine 2.5 mg tablet1.53USD tablet
Midodrine hcl 2.5 mg tablet1.23USD tablet
Apo-Midodrine 5 mg Tablet0.59USD tablet
Apo-Midodrine 2.5 mg Tablet0.35USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point200 to 203°CNot Available
water solubilitySolubleNot Available
logP-0.5Not Available
pKa7.8Not Available
Predicted Properties
PropertyValueSource
Water Solubility4.45 mg/mLALOGPS
logP-0.49ALOGPS
logP-0.95ChemAxon
logS-1.8ALOGPS
pKa (Strongest Acidic)13.77ChemAxon
pKa (Strongest Basic)8.14ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area93.81 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity66.22 m3·mol-1ChemAxon
Polarizability26.65 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
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
  1. Hebenstreit G: [Treatment of hypotension caused by psychopharmacological drugs (author's transl)]. Wien Med Wochenschr. 1981 Feb 28;131(4):109-12. [PubMed:6165144 ]
  2. 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
ATC CodesC01CA17
AHFS Codes
  • 12:12.00
  • 12:12.04
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
AcebutololAcebutolol may increase the bradycardic activities of Midodrine.
AcetaminophenThe risk or severity of adverse effects can be increased when Midodrine is combined with Acetaminophen.
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Midodrine is combined with Acetylsalicylic acid.
AlfuzosinAlfuzosin may decrease the vasoconstricting activities of Midodrine.
AminophyllineThe risk or severity of adverse effects can be increased when Midodrine is combined with Aminophylline.
AmitriptylineAmitriptyline may increase the activities of Midodrine.
AmoxapineAmoxapine may increase the activities of Midodrine.
AmphetamineThe risk or severity of adverse effects can be increased when Midodrine is combined with Amphetamine.
ArformoterolThe risk or severity of adverse effects can be increased when Midodrine is combined with Arformoterol.
ArmodafinilThe risk or severity of adverse effects can be increased when Midodrine is combined with Armodafinil.
ArticaineThe risk or severity of adverse effects can be increased when Midodrine is combined with Articaine.
AtenololAtenolol may increase the bradycardic activities of Midodrine.
AtomoxetineAtomoxetine may increase the hypertensive activities of Midodrine.
BendroflumethiazideBendroflumethiazide may increase the activities of Midodrine.
BenzphetamineThe risk or severity of adverse effects can be increased when Benzphetamine is combined with Midodrine.
Benzylpenicilloyl PolylysineMidodrine may decrease effectiveness of Benzylpenicilloyl Polylysine as a diagnostic agent.
BepridilBepridil may increase the bradycardic activities of Midodrine.
BetaxololBetaxolol may increase the bradycardic activities of Midodrine.
BisoprololBisoprolol may increase the bradycardic activities of Midodrine.
BromocriptineBromocriptine may increase the hypertensive activities of Midodrine.
ButalbitalThe risk or severity of adverse effects can be increased when Midodrine is combined with Butalbital.
CabergolineCabergoline may increase the hypertensive activities of Midodrine.
CaffeineThe risk or severity of adverse effects can be increased when Midodrine is combined with Caffeine.
CarteololCarteolol may increase the bradycardic activities of Midodrine.
CarvedilolCarvedilol may increase the bradycardic activities of Midodrine.
ChlorphentermineThe risk or severity of adverse effects can be increased when Chlorphentermine is combined with Midodrine.
ClenbuterolThe risk or severity of adverse effects can be increased when Clenbuterol is combined with Midodrine.
ClomipramineClomipramine may increase the activities of Midodrine.
CocaineThe risk or severity of adverse effects can be increased when Midodrine is combined with Cocaine.
DesipramineDesipramine may increase the activities of Midodrine.
DexmethylphenidateThe risk or severity of adverse effects can be increased when Midodrine is combined with Dexmethylphenidate.
DextroamphetamineThe risk or severity of adverse effects can be increased when Midodrine is combined with Dextroamphetamine.
DiethylpropionThe risk or severity of adverse effects can be increased when Midodrine is combined with Diethylpropion.
DigoxinDigoxin may increase the bradycardic activities of Midodrine.
DihydrocodeineThe risk or severity of adverse effects can be increased when Midodrine is combined with Dihydrocodeine.
DihydroergotamineDihydroergotamine may increase the hypertensive activities of Midodrine.
DiltiazemDiltiazem may increase the bradycardic activities of Midodrine.
DipivefrinThe risk or severity of adverse effects can be increased when Midodrine is combined with Dipivefrin.
DobutamineThe risk or severity of adverse effects can be increased when Dobutamine is combined with Midodrine.
DopamineThe risk or severity of adverse effects can be increased when Dopamine is combined with Midodrine.
DoxapramThe risk or severity of adverse effects can be increased when Midodrine is combined with Doxapram.
DoxazosinDoxazosin may decrease the vasoconstricting activities of Midodrine.
DoxepinDoxepin may increase the activities of Midodrine.
DoxofyllineThe risk or severity of adverse effects can be increased when Midodrine is combined with Doxofylline.
DronabinolDronabinol may increase the tachycardic activities of Midodrine.
DroxidopaMidodrine may increase the hypertensive activities of Droxidopa.
DyphyllineThe risk or severity of adverse effects can be increased when Midodrine is combined with Dyphylline.
EphedrineThe risk or severity of adverse effects can be increased when Midodrine is combined with Ephedrine.
EpinephrineThe risk or severity of adverse effects can be increased when Epinephrine is combined with Midodrine.
ErgonovineErgonovine may increase the hypertensive activities of Midodrine.
ErgotamineErgotamine may increase the hypertensive activities of Midodrine.
EsmololEsmolol may increase the bradycardic activities of Midodrine.
FenoterolThe risk or severity of adverse effects can be increased when Fenoterol is combined with Midodrine.
Fluticasone PropionateThe risk or severity of adverse effects can be increased when Midodrine is combined with Fluticasone Propionate.
FormoterolThe risk or severity of adverse effects can be increased when Formoterol is combined with Midodrine.
ImipramineImipramine may increase the activities of Midodrine.
IndacaterolThe risk or severity of adverse effects can be increased when Midodrine is combined with Indacaterol.
IobenguaneThe therapeutic efficacy of Iobenguane can be decreased when used in combination with Midodrine.
Ipratropium bromideThe risk or severity of adverse effects can be increased when Midodrine is combined with Ipratropium bromide.
IsocarboxazidIsocarboxazid may increase the hypertensive activities of Midodrine.
IsomethepteneThe risk or severity of adverse effects can be increased when Midodrine is combined with Isometheptene.
IsoprenalineThe risk or severity of adverse effects can be increased when Isoprenaline is combined with Midodrine.
LabetalolLabetalol may increase the bradycardic activities of Midodrine.
LevobunololLevobunolol may increase the bradycardic activities of Midodrine.
LevonordefrinThe risk or severity of adverse effects can be increased when Midodrine is combined with Levonordefrin.
LinezolidLinezolid may increase the hypertensive activities of Midodrine.
LisdexamfetamineThe risk or severity of adverse effects can be increased when Midodrine is combined with Lisdexamfetamine.
MephentermineThe risk or severity of adverse effects can be increased when Mephentermine is combined with Midodrine.
MepivacaineThe risk or severity of adverse effects can be increased when Midodrine is combined with Mepivacaine.
MetaraminolThe risk or severity of adverse effects can be increased when Metaraminol is combined with Midodrine.
MethamphetamineThe risk or severity of adverse effects can be increased when Methamphetamine is combined with Midodrine.
MethoxamineThe risk or severity of adverse effects can be increased when Methoxamine is combined with Midodrine.
MethylphenidateThe risk or severity of adverse effects can be increased when Midodrine is combined with Methylphenidate.
MetipranololMetipranolol may increase the bradycardic activities of Midodrine.
MetoprololMetoprolol may increase the bradycardic activities of Midodrine.
MoclobemideMoclobemide may increase the hypertensive activities of Midodrine.
ModafinilThe risk or severity of adverse effects can be increased when Midodrine is combined with Modafinil.
NabiloneNabilone may increase the tachycardic activities of Midodrine.
NadololNadolol may increase the bradycardic activities of Midodrine.
NaphazolineThe risk or severity of adverse effects can be increased when Naphazoline is combined with Midodrine.
NebivololNebivolol may increase the bradycardic activities of Midodrine.
NorepinephrineThe risk or severity of adverse effects can be increased when Norepinephrine is combined with Midodrine.
NortriptylineNortriptyline may increase the activities of Midodrine.
OlodaterolThe risk or severity of adverse effects can be increased when Midodrine is combined with Olodaterol.
OrciprenalineThe risk or severity of adverse effects can be increased when Orciprenaline is combined with Midodrine.
OxymetazolineThe risk or severity of adverse effects can be increased when Oxymetazoline is combined with Midodrine.
PenbutololPenbutolol may increase the bradycardic activities of Midodrine.
PhendimetrazineThe risk or severity of adverse effects can be increased when Midodrine is combined with Phendimetrazine.
PhenelzinePhenelzine may increase the hypertensive activities of Midodrine.
PheniramineThe risk or severity of adverse effects can be increased when Midodrine is combined with Pheniramine.
PhenmetrazineThe risk or severity of adverse effects can be increased when Phenmetrazine is combined with Midodrine.
PhenoxybenzaminePhenoxybenzamine may decrease the vasoconstricting activities of Midodrine.
PhentermineThe risk or severity of adverse effects can be increased when Midodrine is combined with Phentermine.
PhentolaminePhentolamine may decrease the vasoconstricting activities of Midodrine.
PhenylephrineThe risk or severity of adverse effects can be increased when Phenylephrine is combined with Midodrine.
PhenylpropanolamineThe risk or severity of adverse effects can be increased when Phenylpropanolamine is combined with Midodrine.
PindololPindolol may increase the bradycardic activities of Midodrine.
PirbuterolThe risk or severity of adverse effects can be increased when Midodrine is combined with Pirbuterol.
PrazosinPrazosin may decrease the vasoconstricting activities of Midodrine.
ProcarbazineProcarbazine may increase the hypertensive activities of Midodrine.
PropranololPropranolol may increase the bradycardic activities of Midodrine.
PropylhexedrineThe risk or severity of adverse effects can be increased when Midodrine is combined with Propylhexedrine.
ProtriptylineProtriptyline may increase the activities of Midodrine.
PseudoephedrineThe risk or severity of adverse effects can be increased when Midodrine is combined with Pseudoephedrine.
RacepinephrineThe risk or severity of adverse effects can be increased when Midodrine is combined with Racepinephrine.
RasagilineRasagiline may increase the hypertensive activities of Midodrine.
RitodrineThe risk or severity of adverse effects can be increased when Ritodrine is combined with Midodrine.
SalbutamolThe risk or severity of adverse effects can be increased when Midodrine is combined with Salbutamol.
SalmeterolThe risk or severity of adverse effects can be increased when Salmeterol is combined with Midodrine.
SelegilineSelegiline may increase the hypertensive activities of Midodrine.
SilodosinSilodosin may decrease the vasoconstricting activities of Midodrine.
SotalolSotalol may increase the bradycardic activities of Midodrine.
TamsulosinTamsulosin may decrease the vasoconstricting activities of Midodrine.
Tedizolid PhosphateTedizolid Phosphate may increase the hypertensive activities of Midodrine.
TerazosinTerazosin may decrease the vasoconstricting activities of Midodrine.
TerbutalineThe risk or severity of adverse effects can be increased when Terbutaline is combined with Midodrine.
TheophyllineThe risk or severity of adverse effects can be increased when Midodrine is combined with Theophylline.
TimololTimolol may increase the bradycardic activities of Midodrine.
TranylcypromineTranylcypromine may increase the hypertensive activities of Midodrine.
TrimipramineTrimipramine may increase the activities of Midodrine.
TriprolidineThe risk or severity of adverse effects can be increased when Midodrine is combined with Triprolidine.
VerapamilVerapamil may increase the bradycardic activities of Midodrine.
VilanterolThe risk or severity of adverse effects can be increased when Midodrine is combined with Vilanterol.
Food Interactions
  • Take without regard to meals.

Targets

Kind
Protein
Organism
Human
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) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine(PE)-stimulated ERK signaling in cardiac myocytes.
Gene Name:
ADRA1A
Uniprot ID:
P35348
Molecular Weight:
51486.005 Da
References
  1. 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 ]
  2. 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 ]
  3. 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 ]
Kind
Protein
Organism
Human
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) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine (PE)-stimulated ERK signaling in cardiac myocytes.
Gene Name:
ADRA1B
Uniprot ID:
P35368
Molecular Weight:
56835.375 Da
References
  1. 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 ]
Kind
Protein
Organism
Human
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
Molecular Weight:
60462.205 Da
References
  1. 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

Kind
Protein
Organism
Human
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 antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
References
  1. 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 ]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]

Transporters

Kind
Protein
Organism
Human
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
Molecular Weight:
78805.265 Da
References
  1. 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 ]
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Drug created on June 13, 2005 07:24 / Updated on May 01, 2016 13:38