Details of the Drug

General Information of Drug (ID: DMU8JGH)

• Drug Name: Hydralazine
• Synonyms: Apresolin; Apresoline; Apressin; Apressoline; Aprezolin; HLZ; Hidral; Hidralazin; Hidralazina; Hipoftalin; Hydralazin; Hydralazinum; Hydrallazin; Hydrallazine; Hydrazinophthalazine; Hypophthalin; Idralazina; Hidralazina [Spanish]; Idralazina [DCIT]; Idralazina [Italian]; BA 5968; C 5968; Ciba 5968; Praparat 5968; Apresoline (TN); Apressin (pharmaceutical); C-5068; C-5968; Hidral (TN); Hidralazina [INN-Spanish]; Hydralazine (INN); Hydralazine [INN:BAN]; Hydralazinum [INN-Latin]; Hydrazone 1(2H)-phthalazinone; Phthalazin-1-ylhydrazine; [2H-Phthalazin-(1Z)-Ylidene]-Hydrazine Hydrochloride; (1Z)-1(2H)-Phthalazinone hydrazone; (2H)-Phthalazinone hydrazone; 1(2H)-Phthalazinone hydrazone; 1(2H)-Phthalazinone, hydrazone; 1-Hydrazinophthalazine; 1-Phthalazinylhydrazine; 6-Hydralazine

Indication

Disease Entry	ICD 11	Status	REF
Hypertension	BA00-BA04	Approved	[1], [2]

• Therapeutic Class: Antihypertensive Agents
• Drug Type: Small molecular drug
• #Ro5 Violations (Lipinski): 0:
  Molecular Weight (mw); 160.18
  Topological Polar Surface Area (xlogp); 0.7
  Rotatable Bond Count (rotbonds); 1
  Hydrogen Bond Donor Count (hbonddonor); 2
  Hydrogen Bond Acceptor Count (hbondacc); 4
• ADMET Property:
  BDDCS Class: Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 1: high solubility and high permeability [3]
  Clearance: The clearance of drug is 1.77 +/- 0.48 L/h/kg [4]
  Elimination: Less than 10% of drug is recovered in the feces and 65-90% is recovered in the urine [4]
  Half-life: The concentration or amount of drug in body reduced by one-half in 57 - 241 minutes (in heart failure patients), and 200 minutes (in hypertensive patients) [4]
  Metabolism: The drug is metabolized via the glucuronidation [5]
  MRTD: The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 20.78914 micromolar/kg/day [6]
  Unbound Fraction: The unbound fraction of drug in plasma is 0.12% [7]
  Vd: The volume of distribution (Vd) of drug is 1.34 +/- 0.79 L/kg [4]
  Water Solubility: The ability of drug to dissolve in water is measured as 44.2 mg/mL [3]
• Chemical Identifiers:
  Formula: C8H8N4
  IUPAC Name: phthalazin-1-ylhydrazine
  Canonical SMILES: C1=CC=C2C(=C1)C=NN=C2NN
  InChI: InChI=1S/C8H8N4/c9-11-8-7-4-2-1-3-6(7)5-10-12-8/h1-5H,9H2,(H,11,12)
  InChIKey: RPTUSVTUFVMDQK-UHFFFAOYSA-N
• Cross-matching ID:
  PubChem CID: 3637
  ChEBI ID: CHEBI:5775
  CAS Number: 86-54-4
  DrugBank ID: DB01275
  TTD ID: D0K1XK
  VARIDT ID: DR00942
  INTEDE ID: DR0813
  ACDINA ID: D00311

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Membrane copper amine oxidase (AOC3)	TT7HC21	AOC3_HUMAN	Modulator	[8]

Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
N-acetyltransferase 1 (NAT1)	DE7OAB3	ARY1_HUMAN	Substrate	[9]
RNA cytidine acetyltransferase (hALP)	DEZV4AP	NAT10_HUMAN	Substrate	[10]
N-acetyltransferase 2 (NAT2)	DER7TA0	ARY2_HUMAN	Substrate	[9]

Molecular Expression Atlas of This Drug

• The Studied Disease: Hypertension
• ICD Disease Classification: BA00-BA04

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Membrane copper amine oxidase (AOC3)	DTT	AOC3	8.36E-22	-1.03	-1.54
RNA cytidine acetyltransferase (hALP)	DME	NAT10	1.53E-02	1.17E-01	4.09E-01
N-acetyltransferase 2 (NAT2)	DME	NAT2	7.77E-14	-2.86E-01	-6.87E-01
N-acetyltransferase 1 (NAT1)	DME	NAT1	1.17E-06	2.81E-01	4.42E-01

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Same Disease as Hydralazine

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Disease	REF
Penbutolol	DM4ES8F	Minor	Decreased metabolism of Hydralazine caused by Penbutolol mediated interference with first-pass metabolism.	Hypertension [BA00-BA04]	[34]

Coadministration of a Drug Treating the Disease Different from Hydralazine (Comorbidity)

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Cariprazine	DMJYDVK	Moderate	Additive hypotensive effects by the combination of Hydralazine and Cariprazine.	Bipolar disorder [6A60]	[35]
OPC-34712	DMHG57U	Moderate	Additive hypotensive effects by the combination of Hydralazine and OPC-34712.	Depression [6A70-6A7Z]	[35]
Brentuximab vedotin	DMWLC57	Moderate	Increased risk of peripheral neuropathy by the combination of Hydralazine and Brentuximab vedotin.	Hodgkin lymphoma [2B30]	[36]
ITI-007	DMUQ1DO	Moderate	Additive hypotensive effects by the combination of Hydralazine and ITI-007.	Insomnia [7A00-7A0Z]	[35]
Ozanimod	DMT6AM2	Moderate	Additive hypotensive effects by the combination of Hydralazine and Ozanimod.	Multiple sclerosis [8A40]	[37]
Rasagiline	DM3WKQ4	Moderate	Additive hypotensive effects by the combination of Hydralazine and Rasagiline.	Parkinsonism [8A00]	[37]
Levomepromazine	DMIKFEL	Moderate	Additive hypotensive effects by the combination of Hydralazine and Levomepromazine.	Psychotic disorder [6A20-6A25]	[35]
Iloperidone	DM6AUFY	Moderate	Additive hypotensive effects by the combination of Hydralazine and Iloperidone.	Schizophrenia [6A20]	[35]
Molindone	DMAH70G	Moderate	Additive hypotensive effects by the combination of Hydralazine and Molindone.	Schizophrenia [6A20]	[35]
Thiothixene	DMDINC4	Moderate	Additive hypotensive effects by the combination of Hydralazine and Thiothixene.	Schizophrenia [6A20]	[35]
Asenapine	DMSQZE2	Moderate	Additive hypotensive effects by the combination of Hydralazine and Asenapine.	Schizophrenia [6A20]	[35]

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

DIG

DIG Name	DIG ID	PubChem CID	Functional Classification
Allura red AC dye	E00338	33258	Colorant
Mannitol	E00103	6251	Diluent; Flavoring agent; Lyophilization aid; Plasticizing agent; Tonicity agent
Sodium lauryl sulfate	E00464	3423265	Emulsifying agent; Modified-release agent; Penetration agent; Solubilizing agent; Surfactant; lubricant
Stearic acid	E00079	5281	Emulsifying agent; Solubilizing agent; Viscosity-controlling agent; lubricant
Sunset yellow FCF	E00255	17730	Colorant
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
Sodium stearoyl lactylate	E00558	23671849	Emulsifying agent
Titanium dioxide	E00322	26042	Coating agent; Colorant; Opacifying agent
Vinylpyrrolidone	E00668	Not Available	Binding agent; Coating agent; Disintegrant; Film/membrane-forming agent; Solubilizing agent; Suspending agent

Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Hydralazine 10 mg tablet	10 mg	Oral Tablet	Oral
Hydralazine 100 mg tablet	100 mg	Oral Tablet	Oral
Hydralazine 25 mg tablet	25 mg	Oral Tablet	Oral
Hydralazine 50 mg tablet	50 mg	Oral Tablet	Oral

Jump to Detail Pharmaceutical Formulation Page of This Drug

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