Details of the Drug

General Information of Drug (ID: DMA2Z4F)

Drug Name
Minoxidil
Synonyms
Alopexil; Alostil; Loniten; Lonolox; Minodyl; Minossidile; Minoxidilum; Minoxigaine; Minoximen; Neoxidil; Normoxidil; Pierminox; Prexidil; Regaine; RiUP; Rogaine; Theroxidil; Tricoxidil; Trocoxidil; MINOXIDIL EXTRA STRENGTH FOR MEN; Men s Rogaine Foam; Mens Rogaine Foam; Minossidile [Italian]; Minoxidil Pfizer Brand; PfizerBrand of Minoxidil; Rogaine Extra Strength for Men; Rogaine for Men; Rogaine for Women; M 4145; M1389; U 10858; Apo-Gain; Gen-Minoxidil; Loniten (TN); MINOXIDIL (FOR MEN); MINOXIDIL (FOR WOMEN); MINOXIDIL EXTRA STRENGTH (FOR MEN); Men's Rogaine; Minoxidilum [INN-Latin]; ROGAINE (FOR MEN); ROGAINE (FOR WOMEN); ROGAINE EXTRA STRENGTH (FOR MEN); Regaine (TN); Riup (TN); Rogaine (TN); TM-160; U-10858; Minoxidil (USP/INN); Minoxidil [USAN:BAN:INN]; U-10,858; Rogaine, Regaine, Avacor and Mintop, Minoxidil; Pyrimidine, 2,4-diamino-6-piperidino-, 3-oxide; 2,3-Dihydro-3-hydroxy-2-imino-6-(1-piperidinyl)-4-pyrimidinamine; 2,4-Diamino-6-piperidinilpirimidina-3-ossido; 2,4-Diamino-6-piperidinilpirimidina-3-ossido [Italian]; 2,4-Diamino-6-piperidino-pyrimidine-3-oxide; 2,4-Diamino-6-piperidinopyrimidine 3-N-oxide; 2,4-Diamino-6-piperidinopyrimidine 3-oxide; 2,4-Pyrimidinediamine, 6-(1-piperidinyl)-, 3-oxide; 2,6-Diamino-4-piperidinopyrimidin-1-oxid; 3-hydroxy-2-imino-6-(1-piperidyl)pyrimidin-4-amine; 3-hydroxy-2-imino-6-piperidin-1-ylpyrimidin-4-amine; 6-(1-Piperidinyl)-2,4-pyrimidinediamine 3-oxide; 6-(piperidin-1-yl)pyrimidine-2,4-diamine 3-oxide; 6-Amino-1,2-dihydro-1-hydroxy-2-imino-4-piperidinopyrimidine; 6-Piperidino-2,4-diaminopyrimidine 3-oxide; 6-[1-Piperidinyl]pyrimidine-2,4-diamine 3 oxide
Indication
Disease Entry ICD 11 Status REF
Alopecia ED70 Approved [1]
Hypertension BA00-BA04 Approved [2]
Malignant essential hypertension BA00 Approved [1]
Therapeutic Class
Antihypertensive Agents
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 209.25
Logarithm of the Partition Coefficient (xlogp) 1.2
Rotatable Bond Count (rotbonds) 1
Hydrogen Bond Donor Count (hbonddonor) 3
Hydrogen Bond Acceptor Count (hbondacc) 3
ADMET Property
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 1: high solubility and high permeability [3]
Bioavailability
95% of drug becomes completely available to its intended biological destination(s) [4]
Clearance
The drug present in the plasma can be removed from the body at the rate of 11.5 mL/min/kg [5]
Elimination
10% of drug is excreted from urine in the unchanged form [3]
Half-life
The concentration or amount of drug in body reduced by one-half in 4.2 hours [5]
Metabolism
The drug is metabolized via the conjugation with glucuronic acid at the N-oxide position in the pyrimidine ring []
MRTD
The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 6.8271 micromolar/kg/day [6]
Unbound Fraction
The unbound fraction of drug in plasma is 1% [5]
Vd
Fluid volume that would be required to contain the amount of drug present in the body at the same concentration as in the plasma 0.9 L/kg [5]
Water Solubility
The ability of drug to dissolve in water is measured as 2.2 mg/mL [3]
Chemical Identifiers
Formula
C9H15N5O
IUPAC Name
3-hydroxy-2-imino-6-piperidin-1-ylpyrimidin-4-amine
Canonical SMILES
C1CCN(CC1)C2=NC(=N)N(C(=C2)N)O
InChI
InChI=1S/C9H15N5O/c10-7-6-8(12-9(11)14(7)15)13-4-2-1-3-5-13/h6,11,15H,1-5,10H2
InChIKey
ZIMGGGWCDYVHOY-UHFFFAOYSA-N
Cross-matching ID
PubChem CID
4201
ChEBI ID
CHEBI:6942
CAS Number
38304-91-5
DrugBank ID
DB00350
TTD ID
D0Y2CJ
INTEDE ID
DR1095
ACDINA ID
D00438
Combinatorial Drugs (CBD) Click to Jump to the Detailed CBD Information of This Drug
Repurposed Drugs (RPD) Click to Jump to the Detailed RPD Information of This Drug

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Potassium channel unspecific (KC) TT1VOHK NOUNIPROTAC Modulator [7]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
UDP-glucuronosyltransferase 1A1 (UGT1A1) DEYGVN4 UD11_HUMAN Substrate [8]
Sulfotransferase 1A1 (SULT1A1) DEYWLRK ST1A1_HUMAN Substrate [9]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Antileukoproteinase (SLPI) OTUNFUU8 SLPI_HUMAN Gene/Protein Processing [10]
Hepatocyte growth factor receptor (MET) OT7K55MU MET_HUMAN Gene/Protein Processing [10]
Interleukin-24 (IL24) OT4VUWH1 IL24_HUMAN Gene/Protein Processing [10]
Proepiregulin (EREG) OTRM4NQY EREG_HUMAN Gene/Protein Processing [10]
Renin (REN) OT52GZR2 RENI_HUMAN Gene/Protein Processing [11]
Sulfotransferase 1A1 (SULT1A1) OT0K7JIE ST1A1_HUMAN Biotransformations [12]
Sulfotransferase 1A3 (SULT1A4) OTHJ8WWV ST1A3_HUMAN Biotransformations [12]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Minoxidil (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Promazine DMZAL7W Moderate Additive hypotensive effects by the combination of Minoxidil and Promazine. Appearance/behaviour symptom [MB23] [13]
Linezolid DMGFPU2 Moderate Additive hypotensive effects by the combination of Minoxidil and Linezolid. Bacterial infection [1A00-1C4Z] [14]
Cariprazine DMJYDVK Moderate Additive hypotensive effects by the combination of Minoxidil and Cariprazine. Bipolar disorder [6A60] [13]
Olopatadine DMKMWQG Moderate Additive CNS depression effects by the combination of Minoxidil and Olopatadine. Conjunctiva disorder [9A60] [15]
Selegiline DM6034S Moderate Additive hypotensive effects by the combination of Minoxidil and Selegiline. Depression [6A70-6A7Z] [14]
Isocarboxazid DMAF1NB Moderate Additive hypotensive effects by the combination of Minoxidil and Isocarboxazid. Depression [6A70-6A7Z] [14]
Tranylcypromine DMGB5RE Moderate Additive hypotensive effects by the combination of Minoxidil and Tranylcypromine. Depression [6A70-6A7Z] [14]
OPC-34712 DMHG57U Moderate Additive hypotensive effects by the combination of Minoxidil and OPC-34712. Depression [6A70-6A7Z] [13]
Phenelzine DMHIDUE Moderate Additive hypotensive effects by the combination of Minoxidil and Phenelzine. Depression [6A70-6A7Z] [14]
Procarbazine DMIK367 Moderate Additive hypotensive effects by the combination of Minoxidil and Procarbazine. Hodgkin lymphoma [2B30] [14]
Propiomazine DMKY8V1 Moderate Additive hypotensive effects by the combination of Minoxidil and Propiomazine. Insomnia [7A00-7A0Z] [13]
ITI-007 DMUQ1DO Moderate Additive hypotensive effects by the combination of Minoxidil and ITI-007. Insomnia [7A00-7A0Z] [13]
Ozanimod DMT6AM2 Moderate Additive hypotensive effects by the combination of Minoxidil and Ozanimod. Multiple sclerosis [8A40] [14]
Prochlorperazine DM53SRA Moderate Additive hypotensive effects by the combination of Minoxidil and Prochlorperazine. Nausea/vomiting [MD90] [13]
Promethazine DM6I5GR Moderate Additive hypotensive effects by the combination of Minoxidil and Promethazine. Nausea/vomiting [MD90] [13]
Thiethylperazine DMU3IET Moderate Additive hypotensive effects by the combination of Minoxidil and Thiethylperazine. Nausea/vomiting [MD90] [13]
Safinamide DM0YWJC Moderate Additive hypotensive effects by the combination of Minoxidil and Safinamide. Parkinsonism [8A00] [14]
Rasagiline DM3WKQ4 Moderate Additive hypotensive effects by the combination of Minoxidil and Rasagiline. Parkinsonism [8A00] [14]
Levomepromazine DMIKFEL Moderate Additive hypotensive effects by the combination of Minoxidil and Levomepromazine. Psychotic disorder [6A20-6A25] [13]
Fluphenazine DMIT8LX Moderate Additive hypotensive effects by the combination of Minoxidil and Fluphenazine. Psychotic disorder [6A20-6A25] [13]
Triflupromazine DMKFQJP Moderate Additive hypotensive effects by the combination of Minoxidil and Triflupromazine. Psychotic disorder [6A20-6A25] [13]
Quetiapine DM1N62C Moderate Additive hypotensive effects by the combination of Minoxidil and Quetiapine. Schizophrenia [6A20] [13]
Mesoridazine DM2ZGAN Moderate Additive hypotensive effects by the combination of Minoxidil and Mesoridazine. Schizophrenia [6A20] [13]
Thioridazine DM35M8J Moderate Additive hypotensive effects by the combination of Minoxidil and Thioridazine. Schizophrenia [6A20] [13]
Aripiprazole DM3NUMH Moderate Additive hypotensive effects by the combination of Minoxidil and Aripiprazole. Schizophrenia [6A20] [13]
Iloperidone DM6AUFY Moderate Additive hypotensive effects by the combination of Minoxidil and Iloperidone. Schizophrenia [6A20] [13]
Paliperidone DM7NPJS Moderate Additive hypotensive effects by the combination of Minoxidil and Paliperidone. Schizophrenia [6A20] [13]
Loxapine DM8AI9U Moderate Additive hypotensive effects by the combination of Minoxidil and Loxapine. Schizophrenia [6A20] [13]
Haloperidol DM96SE0 Moderate Additive hypotensive effects by the combination of Minoxidil and Haloperidol. Schizophrenia [6A20] [13]
Perphenazine DMA4MRX Moderate Additive hypotensive effects by the combination of Minoxidil and Perphenazine. Schizophrenia [6A20] [13]
Molindone DMAH70G Moderate Additive hypotensive effects by the combination of Minoxidil and Molindone. Schizophrenia [6A20] [13]
Chlorpromazine DMBGZI3 Moderate Additive hypotensive effects by the combination of Minoxidil and Chlorpromazine. Schizophrenia [6A20] [13]
Thiothixene DMDINC4 Moderate Additive hypotensive effects by the combination of Minoxidil and Thiothixene. Schizophrenia [6A20] [13]
Clozapine DMFC71L Moderate Additive hypotensive effects by the combination of Minoxidil and Clozapine. Schizophrenia [6A20] [13]
Trifluoperazine DMKBYWI Moderate Additive hypotensive effects by the combination of Minoxidil and Trifluoperazine. Schizophrenia [6A20] [13]
Risperidone DMN6DXL Moderate Additive hypotensive effects by the combination of Minoxidil and Risperidone. Schizophrenia [6A20] [13]
Amisulpride DMSJVAM Moderate Additive hypotensive effects by the combination of Minoxidil and Amisulpride. Schizophrenia [6A20] [13]
Methdilazine DMAUHQX Moderate Additive hypotensive effects by the combination of Minoxidil and Methdilazine. Vasomotor/allergic rhinitis [CA08] [13]
Trimeprazine DMEMV9D Moderate Additive hypotensive effects by the combination of Minoxidil and Trimeprazine. Vasomotor/allergic rhinitis [CA08] [16]
⏷ Show the Full List of 39 DDI Information of This Drug

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG
DIG Name DIG ID PubChem CID Functional Classification
Docusate sodium E00563 23673837 Surfactant
Sodium benzoate E00432 517055 Antimicrobial preservative; lubricant
Beta-D-lactose E00099 6134 Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate E00208 11177 lubricant
Silicon dioxide E00670 Not Available Anticaking agent; Opacifying agent; Viscosity-controlling agent
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Minoxidil 10 mg tablet 10 mg Oral Tablet Oral
Minoxidil 2.5 mg tablet 2.5 mg Oral Tablet Oral
Jump to Detail Pharmaceutical Formulation Page of This Drug

References

1 Minoxidil FDA Label
2 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4254).
3 BDDCS applied to over 900 drugs
4 Critical Evaluation of Human Oral Bioavailability for Pharmaceutical Drugs by Using Various Cheminformatics Approaches
5 Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
6 Estimating the safe starting dose in phase I clinical trials and no observed effect level based on QSAR modeling of the human maximum recommended daily dose
7 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
8 Human udp-glucuronosyltransferases: isoform selectivity and kinetics of 4-methylumbelliferone and 1-naphthol glucuronidation, effects of organic solvents, and inhibition by diclofenac and probenecid. Drug Metab Dispos. 2004 Apr;32(4):413-23.
9 Sulfation of minoxidil by multiple human cytosolic sulfotransferases. Chem Biol Interact. 1998 Feb 20;109(1-3):53-67.
10 An in vitro coculture system of human peripheral blood mononuclear cells with hepatocellular carcinoma-derived cells for predicting drug-induced liver injury. Arch Toxicol. 2021 Jan;95(1):149-168. doi: 10.1007/s00204-020-02882-4. Epub 2020 Aug 20.
11 Need for beta-blockade in hypertension reduced with long-term minoxidil. Br Med J. 1978 Aug 5;2(6134):385-8. doi: 10.1136/bmj.2.6134.385.
12 Enzymatic characterization and interspecies difference of phenol sulfotransferases, ST1A forms. Drug Metab Dispos. 2001 Mar;29(3):274-81.
13 Aronowitz JS, Chakos MH, Safferman AZ, Lieberman JA "Syncope associated with the combination of clozapine and enalapril." J Clin Psychopharmacol 14 (1994): 429-30. [PMID: 7884028]
14 Ban TA "Drug interactions with psychoactive drugs." Dis Nerv Syst 36 (1975): 164-6. [PMID: 1116424]
15 Warrington SJ, Ankier SI, Turner P "Evaluation of possible interactions between ethanol and trazodone or amitriptyline." Neuropsychobiology 15 (1986): 31-7. [PMID: 3725002]
16 Product Information. Clozaril (clozapine). Novartis Pharmaceuticals, East Hanover, NJ.