Details of the Drug

General Information of Drug (ID: DMB39LO)

• Drug Name: Metolazone
• Synonyms: Diulo; Metalazone; Metalozone; Metenix; Metolazona; Metolazonum; Microx; Mykrox; Oldren; Xuret; Zaroxolyn; Metolazona [INN-Spanish]; Metolazonum [INN-Latin]; Mykrox (TN); SR 720-22; Zaroxolyn (TN); SR-720-22; Metolazone (JAN/USP/INN); Metolazone [USAN:BAN:INN:JAN]; Mykrox, Zaroxolyn, Diulo, Metolazone; 2-Methyl-3-o-tolyl-6-sulfamyl-7-chloro-1,2,3,4-tetrahydro-4-quinazolinone; 7-Chloro-1,2,3,4-tetrahydro-2-methyl-3-(2-methylphenyl)-4-oxo-6-quinazolinesulfonamide; 7-Chloro-1,2,3,4-tetrahydro-2-methyl-4-oxo-3-o-tolyl-6-quinazolinesulfonamide; 7-chloro-2-methyl-3-(2-methylphenyl)-4-oxo-1,2-dihydroquinazoline-6-sulfonamide

Indication

Disease Entry	ICD 11	Status	REF
Edema	MG29	Approved	[1], [2], [3]
Hypertension	BA00-BA04	Approved	[1], [2], [3]

• Therapeutic Class: Antihypertensive Agents
• Drug Type: Small molecular drug
• #Ro5 Violations (Lipinski): 0:
  Molecular Weight (mw); 365.8
  Topological Polar Surface Area (xlogp); 4.1
  Rotatable Bond Count (rotbonds); 2
  Hydrogen Bond Donor Count (hbonddonor); 2
  Hydrogen Bond Acceptor Count (hbondacc); 5
• ADMET Property:
  BDDCS Class: Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 3: high solubility and low permeability [4]
  Bioavailability: 65% of drug becomes completely available to its intended biological destination(s) [5]
  Clearance: The drug present in the plasma can be removed from the body at the rate of 1.4 mL/min/kg [6]
  Half-life: The concentration or amount of drug in body reduced by one-half in 14 hours [6]
  Metabolism: The drug is metabolized via the glomerular filtration and active tubular secretion [7]
  MRTD: The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 0.781 micromolar/kg/day [8]
  Unbound Fraction: The unbound fraction of drug in plasma is 0.05% [6]
  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 1.6 L/kg [6]
• Chemical Identifiers:
  Formula: C16H16ClN3O3S
  IUPAC Name: 7-chloro-2-methyl-3-(2-methylphenyl)-4-oxo-1,2-dihydroquinazoline-6-sulfonamide
  Canonical SMILES: CC1NC2=CC(=C(C=C2C(=O)N1C3=CC=CC=C3C)S(=O)(=O)N)Cl
  InChI: InChI=1S/C16H16ClN3O3S/c1-9-5-3-4-6-14(9)20-10(2)19-13-8-12(17)15(24(18,22)23)7-11(13)16(20)21/h3-8,10,19H,1-2H3,(H2,18,22,23)
  InChIKey: AQCHWTWZEMGIFD-UHFFFAOYSA-N
• Cross-matching ID:
  PubChem CID: 4170
  ChEBI ID: CHEBI:64354
  CAS Number: 17560-51-9
  DrugBank ID: DB00524
  TTD ID: D01WLC
  VARIDT ID: DR01032
  ACDINA ID: D00423

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Solute carrier family 12 member 3 (SLC12A3)	TTP362L	S12A3_HUMAN	Blocker	[9]

Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	MOA	REF
Thiazide-sensitive sodium-chloride cotransporter (SLC12A3)	DT6MDC9	S12A3_HUMAN	Substrate	[10]

Drug-Drug Interaction (DDI) Information of This Drug

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

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Scopolamine	DMOM8AL	Minor	Altered absorption of Metolazone due to GI dynamics variation caused by Scopolamine.	Addictive disorder [6C50-6C5Z]	[13]
Dronedarone	DMA8FS5	Major	Increased risk of ventricular arrhythmias by the combination of Metolazone and Dronedarone.	Angina pectoris [BA40]	[14]
Linezolid	DMGFPU2	Moderate	Additive hypotensive effects by the combination of Metolazone and Linezolid.	Bacterial infection [1A00-1C4Z]	[15]
Rabeprazole	DMMZXIW	Moderate	Increased risk of hypomagnesemia by the combination of Metolazone and Rabeprazole.	Bacterial infection [1A00-1C4Z]	[16]
Cariprazine	DMJYDVK	Moderate	Additive hypotensive effects by the combination of Metolazone and Cariprazine.	Bipolar disorder [6A60]	[17]
Phenylbutazone	DMAYL0T	Moderate	Antagonize the effect of Metolazone when combined with Phenylbutazone.	Chronic pain [MG30]	[18]
Ketoprofen	DMRKXPT	Moderate	Antagonize the effect of Metolazone when combined with Ketoprofen.	Chronic pain [MG30]	[18]
Levomilnacipran	DMV26S8	Moderate	Increased risk of hyponatremia by the combination of Metolazone and Levomilnacipran.	Chronic pain [MG30]	[19]
Olopatadine	DMKMWQG	Moderate	Additive CNS depression effects by the combination of Metolazone and Olopatadine.	Conjunctiva disorder [9A60]	[20]
Sertraline	DM0FB1J	Moderate	Increased risk of hyponatremia by the combination of Metolazone and Sertraline.	Depression [6A70-6A7Z]	[19]
Vilazodone	DM4LECQ	Moderate	Increased risk of hyponatremia by the combination of Metolazone and Vilazodone.	Depression [6A70-6A7Z]	[19]
Paroxetine	DM5PVQE	Moderate	Increased risk of hyponatremia by the combination of Metolazone and Paroxetine.	Depression [6A70-6A7Z]	[19]
Selegiline	DM6034S	Moderate	Additive hypotensive effects by the combination of Metolazone and Selegiline.	Depression [6A70-6A7Z]	[15]
Vortioxetine	DM6F1PU	Moderate	Increased risk of hyponatremia by the combination of Metolazone and Vortioxetine.	Depression [6A70-6A7Z]	[19]
Isocarboxazid	DMAF1NB	Moderate	Additive hypotensive effects by the combination of Metolazone and Isocarboxazid.	Depression [6A70-6A7Z]	[15]
Milnacipran	DMBFE74	Moderate	Increased risk of hyponatremia by the combination of Metolazone and Milnacipran.	Depression [6A70-6A7Z]	[19]
Escitalopram	DMFK9HG	Moderate	Increased risk of hyponatremia by the combination of Metolazone and Escitalopram.	Depression [6A70-6A7Z]	[19]
Tranylcypromine	DMGB5RE	Moderate	Additive hypotensive effects by the combination of Metolazone and Tranylcypromine.	Depression [6A70-6A7Z]	[15]
Desvenlafaxine	DMHD4PE	Moderate	Increased risk of hyponatremia by the combination of Metolazone and Desvenlafaxine.	Depression [6A70-6A7Z]	[19]
OPC-34712	DMHG57U	Moderate	Additive hypotensive effects by the combination of Metolazone and OPC-34712.	Depression [6A70-6A7Z]	[17]
Phenelzine	DMHIDUE	Moderate	Additive hypotensive effects by the combination of Metolazone and Phenelzine.	Depression [6A70-6A7Z]	[15]
Mepenzolate	DM8YU2F	Minor	Altered absorption of Metolazone due to GI dynamics variation caused by Mepenzolate.	Digestive system disease [DE2Z]	[13]
Oxybutynine	DMJPBAX	Minor	Altered absorption of Metolazone due to GI dynamics variation caused by Oxybutynine.	Discovery agent [N.A.]	[13]
Carbamazepine	DMZOLBI	Moderate	Increased risk of hyponatremia by the combination of Metolazone and Carbamazepine.	Epilepsy/seizure [8A61-8A6Z]	[21]
Eslicarbazepine	DMZREFQ	Moderate	Increased risk of hyponatremia by the combination of Metolazone and Eslicarbazepine.	Epilepsy/seizure [8A61-8A6Z]	[22]
Ethacrynic acid	DM60QMR	Moderate	Increased risk of fluid/electrolyte loss by the combination of Metolazone and Ethacrynic acid.	Essential hypertension [BA00]	[23]
Nadolol	DMW6GVL	Moderate	Increased risk of hyperglycemia by the combination of Metolazone and Nadolol.	Essential hypertension [BA00]	[24]
Mefenamic acid	DMK7HFI	Moderate	Antagonize the effect of Metolazone when combined with Mefenamic acid.	Female pelvic pain [GA34]	[18]
Solifenacin	DMG592Q	Minor	Altered absorption of Metolazone due to GI dynamics variation caused by Solifenacin.	Functional bladder disorder [GC50]	[13]
Tolterodine	DMSHPW8	Minor	Altered absorption of Metolazone due to GI dynamics variation caused by Tolterodine.	Functional bladder disorder [GC50]	[13]
Propantheline	DM2EN6G	Minor	Altered absorption of Metolazone due to GI dynamics variation caused by Propantheline.	Gastric ulcer [DA60]	[13]
Dexlansoprazole	DM1DBV5	Moderate	Increased risk of hypomagnesemia by the combination of Metolazone and Dexlansoprazole.	Gastro-oesophageal reflux disease [DA22]	[16]
Cisapride	DMY7PED	Major	Increased risk of ventricular arrhythmias by the combination of Metolazone and Cisapride.	Gastro-oesophageal reflux disease [DA22]	[25]
Metipranolol	DMJMVKI	Moderate	Increased risk of hypertriglyceridemia by the combination of Metolazone and Metipranolol.	Glaucoma [9C61]	[24]
Levobunolol	DMTNFCQ	Moderate	Increased risk of hypertriglyceridemia by the combination of Metolazone and Levobunolol.	Glaucoma [9C61]	[24]
Carvedilol	DMHTEAO	Moderate	Increased risk of hyperglycemia by the combination of Metolazone and Carvedilol.	Heart failure [BD10-BD1Z]	[24]
Furosemide	DMMQ8ZG	Moderate	Increased risk of fluid/electrolyte loss by the combination of Metolazone and Furosemide.	Heart failure [BD10-BD1Z]	[23]
Bumetanide	DMRV7H0	Moderate	Increased risk of fluid/electrolyte loss by the combination of Metolazone and Bumetanide.	Heart failure [BD10-BD1Z]	[23]
Digitoxin	DMWVIGP	Moderate	Increased risk of hypokalemia by the combination of Metolazone and Digitoxin.	Heart failure [BD10-BD1Z]	[26]
Procarbazine	DMIK367	Moderate	Additive hypotensive effects by the combination of Metolazone and Procarbazine.	Hodgkin lymphoma [2B30]	[15]
Acebutolol	DM0TI4U	Moderate	Increased risk of hyperglycemia by the combination of Metolazone and Acebutolol.	Hypertension [BA00-BA04]	[24]
Moexipril	DM26E4B	Moderate	Additive hypotensive effects by the combination of Metolazone and Moexipril.	Hypertension [BA00-BA04]	[27]
Bisoprolol	DM3UZ95	Moderate	Increased risk of ventricular arrhythmias by the combination of Metolazone and Bisoprolol.	Hypertension [BA00-BA04]	[24]
Captopril	DM458UM	Moderate	Additive hypotensive effects by the combination of Metolazone and Captopril.	Hypertension [BA00-BA04]	[27]
Nebivolol	DM7F1PA	Moderate	Increased risk of hyperglycemia by the combination of Metolazone and Nebivolol.	Hypertension [BA00-BA04]	[24]
Pindolol	DMD2NV7	Moderate	Increased risk of ventricular arrhythmias by the combination of Metolazone and Pindolol.	Hypertension [BA00-BA04]	[24]
Benazepril	DMH1M9B	Moderate	Additive hypotensive effects by the combination of Metolazone and Benazepril.	Hypertension [BA00-BA04]	[27]
Labetalol	DMK8U72	Moderate	Increased risk of ventricular arrhythmias by the combination of Metolazone and Labetalol.	Hypertension [BA00-BA04]	[24]
Enalapril	DMNFUZR	Moderate	Additive hypotensive effects by the combination of Metolazone and Enalapril.	Hypertension [BA00-BA04]	[27]
Perindopril	DMOPZDT	Moderate	Additive hypotensive effects by the combination of Metolazone and Perindopril.	Hypertension [BA00-BA04]	[27]
Quinapril	DMR8H31	Moderate	Additive hypotensive effects by the combination of Metolazone and Quinapril.	Hypertension [BA00-BA04]	[27]
Lisinopril	DMUOK4C	Moderate	Additive hypotensive effects by the combination of Metolazone and Lisinopril.	Hypertension [BA00-BA04]	[27]
Belladonna	DM2RBWK	Minor	Altered absorption of Metolazone due to GI dynamics variation caused by Belladonna.	Infectious gastroenteritis/colitis [1A40]	[13]
Meclofenamic acid	DM05FXR	Moderate	Antagonize the effect of Metolazone when combined with Meclofenamic acid.	Inflammatory spondyloarthritis [FA92]	[18]
Propiomazine	DMKY8V1	Moderate	Additive hypotensive effects by the combination of Metolazone and Propiomazine.	Insomnia [7A00-7A0Z]	[17]
ITI-007	DMUQ1DO	Moderate	Additive hypotensive effects by the combination of Metolazone and ITI-007.	Insomnia [7A00-7A0Z]	[17]
Clidinium	DMUMQZ0	Minor	Altered absorption of Metolazone due to GI dynamics variation caused by Clidinium.	Irritable bowel syndrome [DD91]	[13]
Dicyclomine	DMZSDGX	Minor	Altered absorption of Metolazone due to GI dynamics variation caused by Dicyclomine.	Irritable bowel syndrome [DD91]	[13]
Porfimer Sodium	DM7ZWNY	Moderate	Increased risk of photosensitivity reactions by the combination of Metolazone and Porfimer Sodium.	Lung cancer [2C25]	[28]
Arsenic trioxide	DM61TA4	Major	Increased risk of ventricular arrhythmias by the combination of Metolazone and Arsenic trioxide.	Mature B-cell lymphoma [2A85]	[29]
Propranolol	DM79NTF	Moderate	Increased risk of ventricular arrhythmias by the combination of Metolazone and Propranolol.	Migraine [8A80]	[24]
Ozanimod	DMT6AM2	Moderate	Additive hypotensive effects by the combination of Metolazone and Ozanimod.	Multiple sclerosis [8A40]	[15]
Methoxsalen	DME8FZ9	Moderate	Increased risk of photosensitivity reactions by the combination of Metolazone and Methoxsalen.	Mycosis fungoides [2B01]	[30]
Promethazine	DM6I5GR	Moderate	Additive hypotensive effects by the combination of Metolazone and Promethazine.	Nausea/vomiting [MD90]	[17]
Sibutramine	DMFJTDI	Moderate	Increased risk of hyponatremia by the combination of Metolazone and Sibutramine.	Obesity [5B80-5B81]	[19]
Levomethadyl Acetate	DM06HG5	Major	Increased risk of ventricular arrhythmias by the combination of Metolazone and Levomethadyl Acetate.	Opioid use disorder [6C43]	[31]
Rofecoxib	DM3P5DA	Moderate	Antagonize the effect of Metolazone when combined with Rofecoxib.	Osteoarthritis [FA00-FA05]	[18]
Valdecoxib	DMAY7H4	Moderate	Antagonize the effect of Metolazone when combined with Valdecoxib.	Osteoarthritis [FA00-FA05]	[18]
Diclofenac	DMPIHLS	Moderate	Antagonize the effect of Metolazone when combined with Diclofenac.	Osteoarthritis [FA00-FA05]	[18]
Naproxen	DMZ5RGV	Moderate	Antagonize the effect of Metolazone when combined with Naproxen.	Osteoarthritis [FA00-FA05]	[18]
Etodolac	DM6WJO9	Moderate	Antagonize the effect of Metolazone when combined with Etodolac.	Pain [MG30-MG3Z]	[18]
Diflunisal	DM7EN8I	Moderate	Antagonize the effect of Metolazone when combined with Diflunisal.	Pain [MG30-MG3Z]	[18]
Ibuprofen	DM8VCBE	Moderate	Antagonize the effect of Metolazone when combined with Ibuprofen.	Pain [MG30-MG3Z]	[18]
Flavoxate	DMKV4NL	Minor	Altered absorption of Metolazone due to GI dynamics variation caused by Flavoxate.	Pain [MG30-MG3Z]	[13]
Piroxicam	DMTK234	Moderate	Antagonize the effect of Metolazone when combined with Piroxicam.	Pain [MG30-MG3Z]	[18]
Safinamide	DM0YWJC	Moderate	Additive hypotensive effects by the combination of Metolazone and Safinamide.	Parkinsonism [8A00]	[15]
Rasagiline	DM3WKQ4	Moderate	Additive hypotensive effects by the combination of Metolazone and Rasagiline.	Parkinsonism [8A00]	[15]
Biperiden	DME78OA	Minor	Altered absorption of Metolazone due to GI dynamics variation caused by Biperiden.	Parkinsonism [8A00]	[13]
Methylscopolamine	DM5VWOB	Minor	Altered absorption of Metolazone due to GI dynamics variation caused by Methylscopolamine.	Peptic ulcer [DA61]	[13]
Esomeprazole	DM7BN0X	Moderate	Increased risk of hypomagnesemia by the combination of Metolazone and Esomeprazole.	Peptic ulcer [DA61]	[16]
Bromfenac	DMKB79O	Moderate	Antagonize the effect of Metolazone when combined with Bromfenac.	Postoperative inflammation [1A00-CA43]	[18]
Levomepromazine	DMIKFEL	Moderate	Additive hypotensive effects by the combination of Metolazone and Levomepromazine.	Psychotic disorder [6A20-6A25]	[17]
Fluphenazine	DMIT8LX	Moderate	Increased risk of ventricular arrhythmias by the combination of Metolazone and Fluphenazine.	Psychotic disorder [6A20-6A25]	[30]
Meloxicam	DM2AR7L	Moderate	Antagonize the effect of Metolazone when combined with Meloxicam.	Rheumatoid arthritis [FA20]	[18]
Sulindac	DM2QHZU	Moderate	Antagonize the effect of Metolazone when combined with Sulindac.	Rheumatoid arthritis [FA20]	[18]
Oxaprozin	DM9UB0P	Moderate	Antagonize the effect of Metolazone when combined with Oxaprozin.	Rheumatoid arthritis [FA20]	[18]
Flurbiprofen	DMGN4BY	Moderate	Antagonize the effect of Metolazone when combined with Flurbiprofen.	Rheumatoid arthritis [FA20]	[18]
Fenoprofen	DML5VQ0	Moderate	Antagonize the effect of Metolazone when combined with Fenoprofen.	Rheumatoid arthritis [FA20]	[18]
Quetiapine	DM1N62C	Moderate	Additive hypotensive effects by the combination of Metolazone and Quetiapine.	Schizophrenia [6A20]	[17]
Mesoridazine	DM2ZGAN	Moderate	Increased risk of ventricular arrhythmias by the combination of Metolazone and Mesoridazine.	Schizophrenia [6A20]	[30]
Thioridazine	DM35M8J	Moderate	Increased risk of ventricular arrhythmias by the combination of Metolazone and Thioridazine.	Schizophrenia [6A20]	[30]
Aripiprazole	DM3NUMH	Moderate	Additive hypotensive effects by the combination of Metolazone and Aripiprazole.	Schizophrenia [6A20]	[17]
Iloperidone	DM6AUFY	Moderate	Increased risk of ventricular arrhythmias by the combination of Metolazone and Iloperidone.	Schizophrenia [6A20]	[30]
Paliperidone	DM7NPJS	Moderate	Increased risk of ventricular arrhythmias by the combination of Metolazone and Paliperidone.	Schizophrenia [6A20]	[30]
Perphenazine	DMA4MRX	Moderate	Increased risk of ventricular arrhythmias by the combination of Metolazone and Perphenazine.	Schizophrenia [6A20]	[30]
Molindone	DMAH70G	Moderate	Additive hypotensive effects by the combination of Metolazone and Molindone.	Schizophrenia [6A20]	[17]
Thiothixene	DMDINC4	Moderate	Additive hypotensive effects by the combination of Metolazone and Thiothixene.	Schizophrenia [6A20]	[17]
Trifluoperazine	DMKBYWI	Moderate	Increased risk of ventricular arrhythmias by the combination of Metolazone and Trifluoperazine.	Schizophrenia [6A20]	[30]
Risperidone	DMN6DXL	Moderate	Increased risk of ventricular arrhythmias by the combination of Metolazone and Risperidone.	Schizophrenia [6A20]	[30]
Amisulpride	DMSJVAM	Moderate	Increased risk of ventricular arrhythmias by the combination of Metolazone and Amisulpride.	Schizophrenia [6A20]	[30]
Asenapine	DMSQZE2	Moderate	Additive hypotensive effects by the combination of Metolazone and Asenapine.	Schizophrenia [6A20]	[17]
Pimozide	DMW83TP	Major	Increased risk of ventricular arrhythmias by the combination of Metolazone and Pimozide.	Schizophrenia [6A20]	[32]
Atropine	DMEN6X7	Minor	Altered absorption of Metolazone due to GI dynamics variation caused by Atropine.	Unspecific substance harmful effect [NE6Z]	[13]
Methdilazine	DMAUHQX	Moderate	Additive hypotensive effects by the combination of Metolazone and Methdilazine.	Vasomotor/allergic rhinitis [CA08]	[17]
Trimeprazine	DMEMV9D	Moderate	Additive hypotensive effects by the combination of Metolazone and Trimeprazine.	Vasomotor/allergic rhinitis [CA08]	[33]
Amiodarone	DMUTEX3	Major	Increased risk of ventricular arrhythmias by the combination of Metolazone and Amiodarone.	Ventricular tachyarrhythmia [BC71]	[34]

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

DIG

DIG Name	DIG ID	PubChem CID	Functional Classification
D&C red no. 30	E00456	3000709	Colorant
D&C red no. 33	E00261	19116	Colorant
FD&C blue no. 2	E00446	2723854	Colorant
Quinoline yellow WS	E00309	24671	Colorant
Sunset yellow FCF	E00255	17730	Colorant
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
Metolazone 10 mg tablet	10 mg	Oral Tablet	Oral
Metolazone 2.5 mg tablet	2.5 mg	Oral Tablet	Oral
Metolazone 5 mg tablet	5 mg	Oral Tablet	Oral

Jump to Detail Pharmaceutical Formulation Page of This Drug

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