minoxidil Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
vasodilators 1814 38304-91-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • minoxidil
  • loniten
  • rogaine
A potent direct-acting peripheral vasodilator (VASODILATOR AGENTS) that reduces peripheral resistance and produces a fall in BLOOD PRESSURE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p371)
  • Molecular weight: 209.25
  • Formula: C9H15N5O
  • CLOGP: 0.02
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 2
  • TPSA: 93.63
  • ALOGS: -1.02
  • ROTB: 1

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
20 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 2.20 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 10 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 6.83 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 95 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 0.90 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 11.50 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 1 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 1.50 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Oct. 18, 1979 FDA

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Hypertrichosis 172.71 35.94 23 338 204 2357520
Product formulation issue 113.69 35.94 16 345 218 2357506
Dermatitis contact 97.07 35.94 18 343 1448 2356276
Alopecia 92.52 35.94 29 332 21972 2335752
Drug ineffective 78.22 35.94 39 322 101585 2256139
Hypertension 52.00 35.94 20 341 27341 2330383
Hair growth abnormal 50.34 35.94 9 352 583 2357141
Product use in unapproved indication 47.80 35.94 15 346 11185 2346539
Pruritus 46.29 35.94 21 340 43319 2314405
Hair texture abnormal 44.44 35.94 8 353 538 2357186
Hypotension 38.66 35.94 17 344 32419 2325305
Vanishing bile duct syndrome 38.45 35.94 6 355 168 2357556
Palpitations 38.36 35.94 14 347 16442 2341282
Fluid retention 36.65 35.94 11 350 7035 2350689

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Pericardial effusion 238.85 41.07 48 349 3342 1743042
Hypertrichosis 208.43 41.07 27 370 92 1746292
Product formulation issue 189.37 41.07 26 371 151 1746233
Alopecia 69.46 41.07 18 379 3735 1742649
Dizziness 59.79 41.07 28 369 34333 1712051
Oedema peripheral 58.54 41.07 22 375 15528 1730856
Hypotension 57.28 41.07 26 371 29628 1716756
Palpitations 50.40 41.07 16 381 6798 1739586
Product label on wrong product 49.17 41.07 6 391 10 1746374
Dermatitis contact 44.08 41.07 9 388 644 1745740
Pleural effusion 42.74 41.07 16 381 11094 1735290

Pharmacologic Action:

SourceCodeDescription
ATC C02DC01 CARDIOVASCULAR SYSTEM
ANTIHYPERTENSIVES
ARTERIOLAR SMOOTH MUSCLE, AGENTS ACTING ON
Pyrimidine derivatives
ATC D11AX01 DERMATOLOGICALS
OTHER DERMATOLOGICAL PREPARATIONS
OTHER DERMATOLOGICAL PREPARATIONS
Other dermatologicals
FDA PE N0000175379 Arteriolar Vasodilation
FDA EPC N0000175564 Arteriolar Vasodilator
CHEBI has role CHEBI:35620 vasodilator agent
CHEBI has role CHEBI:35674 antihypertensive agent
MeSH PA D000959 Antihypertensive Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D014665 Vasodilator Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Hypertensive disorder indication 38341003 DOID:10763
Alopecia indication 56317004 DOID:987
Pericarditis contraindication 3238004 DOID:1787
Myocardial infarction contraindication 22298006 DOID:5844
Orthostatic hypotension contraindication 28651003
Cardiac tamponade contraindication 35304003 DOID:115
Chronic heart failure contraindication 48447003
Disorder of cardiovascular system contraindication 49601007 DOID:1287
Cerebrovascular disease contraindication 62914000 DOID:6713
Kidney disease contraindication 90708001 DOID:557
Angina pectoris contraindication 194828000
Cerebrovascular accident contraindication 230690007
Pheochromocytoma contraindication 302835009
Pericardial effusion contraindication 373945007 DOID:118
Dermatosis of scalp contraindication 402694007 DOID:3136

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 4.35 Basic
pKa2 2.62 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Sulfonylurea receptor 2, Kir6.2 Ion channel OPENER CHEMBL SCIENTIFIC LITERATURE
ATP-sensitive inward rectifier potassium channel 1 Ion channel IC50 6.97 WOMBAT-PK

External reference:

IDSource
4018077 VUID
N0000146416 NUI
C0026196 UMLSCUI
D00418 KEGG_DRUG
5965120SH1 UNII
2987 INN_ID
49577002 SNOMEDCT_US
4018077 VANDF
7147 MMSL
6984 RXNORM
387272001 SNOMEDCT_US
5119 MMSL
d00135 MMSL
000637 NDDF
4201 PUBCHEM_CID
CHEBI:6942 CHEBI
CHEMBL802 ChEMBL_ID
DB00350 DRUGBANK_ID
MXD PDB_CHEM_ID
D008914 MESH_DESCRIPTOR_UI
4254 IUPHAR_LIGAND_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Good Sense Hair Regrowth Treatment HUMAN OTC DRUG LABEL 1 0113-0798 SOLUTION 3 g TOPICAL ANDA 10 sections
Good Sense Hair Regrowth Treatment HUMAN OTC DRUG LABEL 1 0113-1129 AEROSOL, FOAM 50 mg TOPICAL ANDA 16 sections
basic care hair regrowth treatment HUMAN OTC DRUG LABEL 1 0113-7129 AEROSOL, FOAM 50 mg TOPICAL ANDA 16 sections
basic care hair regrowth treatment HUMAN OTC DRUG LABEL 1 0113-7202 SOLUTION 2 g TOPICAL ANDA 10 sections
basic care hair regrowth treatment HUMAN OTC DRUG LABEL 1 0113-7294 AEROSOL, FOAM 5 g TOPICAL ANDA 10 sections
Basic Care Hair Regrowth HUMAN OTC DRUG LABEL 1 0113-7798 SOLUTION 3 g TOPICAL ANDA 9 sections
minoxidil HUMAN OTC DRUG LABEL 1 0363-0294 AEROSOL, FOAM 5 g TOPICAL ANDA 10 sections
minoxidil HUMAN OTC DRUG LABEL 1 0363-0798 SOLUTION 3 g TOPICAL ANDA 10 sections
hair regrowth treatment HUMAN OTC DRUG LABEL 1 0363-1129 AEROSOL, FOAM 50 mg TOPICAL ANDA 16 sections
Solution HUMAN OTC DRUG LABEL 1 0363-2173 SOLUTION 0.02 g TOPICAL ANDA 13 sections
hair regrowth treatment HUMAN OTC DRUG LABEL 1 0363-2294 AEROSOL, FOAM 5 g TOPICAL ANDA 10 sections
hair regrowth treatment HUMAN OTC DRUG LABEL 1 0363-2798 SOLUTION 3 g TOPICAL ANDA 9 sections
hair regrowth treatment HUMAN OTC DRUG LABEL 1 0363-7202 SOLUTION 2 g TOPICAL ANDA 10 sections
Minoxidil HUMAN OTC DRUG LABEL 1 0472-0066 SOLUTION 2 g TOPICAL ANDA 9 sections
Minoxidil HUMAN OTC DRUG LABEL 1 0472-0094 SOLUTION 50 mg TOPICAL ANDA 10 sections
minoxidil HUMAN OTC DRUG LABEL 1 0472-1660 AEROSOL, FOAM 5 g TOPICAL ANDA 9 sections
minoxidil HUMAN OTC DRUG LABEL 1 0472-1665 AEROSOL, FOAM 5 g TOPICAL ANDA 15 sections
Minoxidil HUMAN PRESCRIPTION DRUG LABEL 1 0591-5642 TABLET 2.50 mg ORAL ANDA 14 sections
Minoxidil HUMAN PRESCRIPTION DRUG LABEL 1 0591-5643 TABLET 10 mg ORAL ANDA 14 sections
Minoxidil HUMAN PRESCRIPTION DRUG LABEL 1 0615-7593 TABLET 2.50 mg ORAL ANDA 12 sections
just for men minoxidil HUMAN OTC DRUG LABEL 1 11509-0798 SOLUTION 3 g TOPICAL ANDA 9 sections
up and up hair regrowth treatment for women HUMAN OTC DRUG LABEL 1 11673-189 SOLUTION 2 g TOPICAL ANDA 10 sections
up and up hair regrowth treatment for women HUMAN OTC DRUG LABEL 1 11673-431 AEROSOL, FOAM 50 mg TOPICAL ANDA 16 sections
up and up hair regrowth treatment for men HUMAN OTC DRUG LABEL 1 11673-632 SOLUTION 5 g TOPICAL ANDA 10 sections
up and up hair regrowth treatment for men HUMAN OTC DRUG LABEL 1 11673-707 AEROSOL, FOAM 5 g TOPICAL ANDA 10 sections
Minoxidil HUMAN OTC DRUG LABEL 1 11822-0129 AEROSOL, FOAM 50 mg TOPICAL ANDA 16 sections
Minoxidil HUMAN OTC DRUG LABEL 1 11822-0202 SOLUTION 2 g TOPICAL ANDA 10 sections
Daylogic For Men HUMAN OTC DRUG LABEL 1 11822-0606 AEROSOL, FOAM 5 g TOPICAL ANDA 10 sections
minoxidil HUMAN OTC DRUG LABEL 1 11822-0798 SOLUTION 3 g TOPICAL ANDA 9 sections
signature care hair regrowth treatment for women HUMAN OTC DRUG LABEL 1 21130-163 AEROSOL, FOAM 50 mg TOPICAL ANDA 16 sections