General
Preferred name
MIDODRINE
Synonyms
MIDODRINE HYDROCHLORIDE ()
Midodrine (D6 hydrochloride) ()
(¡À)-Midodrine hydrochlorid ()
(¡À)-Midodrin ()
Pro-Amatine ()
(??)-Midodrine hydrochlorid ()
(??)-Midodrin ()
Midodrine (hydrochloride) ()
Pro-Amatine3092-17-9 ()
(±)-Midodrin ()
(±)-Midodrine (hydrochloride) ()
(R)-Midodrine hydrochloride ()
ST-PETER-224 ()
Proamatine ()
NSC-758429 ()
ST1085 HYDROCHLORIDE ()
Bramox ()
ST-1085 ()
ST 1085 [AS THE BASE] ()
Orvaten ()
Hipertan ()
Gutron ()
ST 1085 HYDROCHLORIDE ()
Midodrine hcl ()
ST-1085 HYDROCHLORIDE ()
ST-1085 BASE ()
Amatine ()
St. Peter 224 ()
A-4020 Linz ()
Midodrine monohydrochloride ()
Midon ()
Metligine ()
ST 1085 ()
midodrine ()
Midodrine-d6 (hydrochloride) ()
P&D ID
PD010170
CAS
3092-17-9
42794-76-3
43218-56-0
133163-28-7
1188265-43-1
Tags
prodrug
natural product
drug
available
Approved by
FDA
First approval
1996
Drug Status
approved
Drug indication
Antihypotensive
Orthostatic hypotension
Max Phase
Phase 4
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
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. 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.
MOA
Midodrine undergoes metabolism to form its pharmacologically active metabolite, desglymidodrine. Desglymidodrine acts as an agonist at the alpha1-adrenergic receptors expressed in the arteriolar and venous vasculature. Activation of alpha1-adrenergic receptor signaling pathways lead to an increase in the vascular tone and elevation of blood pressure. Desglymidodrine is reported to have negligible effect on the cardiac beta-adrenergic receptors.
ABSORPTION
Rapidly absorbed following oral administration. The peak plasma concentrations of the prodrug, desglymidodrine, is reached about half an hour following drug administration. The metabolites reach their peak plasma concentrations at about 1 to 2 hours following drug administration. The absolute bioavailability of midodrine (measured as desglymidodrine) is 93% and is not affected by food. As desglymidodrine displays poor diffusibility across the blood-brain barrier, it is expected to have minimal effects on the central nervous system.
HALF-LIFE
The metabolites display a half-life of about 3 to 4 hours.
DESCRIPTION
The active metabolite of midodrine is desglymidodrine (CHEMBL1076).
Marketed formulations may contain midodrine hydrochloride (PubChem CID 18340). (GtoPdb)
Marketed formulations may contain midodrine hydrochloride (PubChem CID 18340). (GtoPdb)
DESCRIPTION
Midodrine is a Alpha adrenergic receptor under the development of Shire for the treatment of dysautonomia and orthostatic hypotension. In August 2010, the FDA proposed withdrawing this approval because Shire has failed to complete required studies after the medicine reached the market. In September 2011, Shire announced that it was continuing the process to work with the FDA towards a final approval of the drug.
(BOC Sciences Bioactive Compounds)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Compound Sets
21
BOC Sciences Bioactive Compounds
ChEMBL Approved Drugs
ChEMBL Drugs
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMAP
DrugMAP Approved Drugs
DrugMatrix
Guide to Pharmacology
NCATS Inxight Approved Drugs
NIH Clinical Collections (NCC)
NPC Screening Collection
Prestwick Chemical Library
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
The Spectrum Collection
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
66
Molecular Weight
254.13
Hydrogen Bond Acceptors
5
Hydrogen Bond Donors
3
Rotatable Bonds
6
Ring Count
1
Aromatic Ring Count
1
cLogP
-0.19
TPSA
93.81
Fraction CSP3
0.42
Chiral centers
1.0
Largest ring
6.0
QED
0.65
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Pathway
GPCR/G protein
Neuronal Signaling
Target
??1-adrenergic receptor
¦Á1-adrenergic receptor
Adrenergic Receptor
Therapeutic Class
Vasoconstrictor Agents
Solubility
Soluble in DMSO
Source data
