Details of the Drug

General Information of Drug (ID: DMW6GVL)

Drug Name

Nadolol

Synonyms

Anabet; Corgard; Corgaretic; Nadic; Nadololum; Solgol; SQ 11725; SQ11725; Anabet (TN); Corgard (TN); Corzide (TN); Nadololum [INN-Latin]; SQ-11725; Solgol (TN); Alti-Nadolol (TN); Apo-Nadol (TN); Novo-Nadolol (TN); Nadolol (JP15/USP/INN); Nadolol [USAN:BAN:INN:JAN]; (2R,3S)-5-(3-(tert-Butylamino)-2-hydroxypropoxy)-1,2,3,4-tetrahydronaphthalene-2,3-diol; (2R,3S)-5-({3-[(1,1-dimethylethyl)amino]-2-hydroxypropyl}oxy)-1,2,3,4-tetrahydronaphthalene-2,3-diol; (2R,3S)-5-[3-(tert-butylamino)-2-hydroxypropoxy]-1,2,3,4-tetrahydronaphthalene-2,3-diol; 2,3-cis-1,2,3,4-Tetrahydro-5-((2-hydroxy-3-tert-butylamino)propoxy)-2,3-naphthalenediol; 5-(3-((1,1-Dimethylethyl)amino)-2-hydroxypropoxy)-1,2,3,4-tetrahydro-2,3-naphthalenediol

Indication

Disease Entry	ICD 11	Status	REF
Angina pectoris	BA40	Approved	[1]
High blood pressure	BA00	Approved	[2]
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Therapeutic Class

Antihypertensive Agents

Drug Type

Small molecular drug

Structure

3D MOL

2D MOL

#Ro5 Violations (Lipinski): 0

Molecular Weight (mw)

309.4

Logarithm of the Partition Coefficient (xlogp)

0.7

Rotatable Bond Count (rotbonds)

Hydrogen Bond Donor Count (hbonddonor)

Hydrogen Bond Acceptor Count (hbondacc)

ADMET Property

Absorption AUC: The area under the plot of plasma concentration (AUC) of drug is 1021 mcgh/L [3]
Absorption Cmax: The maximum plasma concentration (Cmax) of drug is 69 +/- 15 mcg/L [3]
Absorption Tmax: The time to maximum plasma concentration (Tmax) is 2.7 h [3]
BDDCS Class: Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 3: high solubility and low permeability [4]
Clearance: The renal clearance of drug is 131-150 mL/min [5]
Elimination: In healthy subjects, following intravenous dosing, 60% of a dose is eliminated in the urine and 15% in the feces after 72 hours [5]
Half-life: The concentration or amount of drug in body reduced by one-half in 20 - 24 hours [6]
Metabolism: The drug is not metabolised [5]
MRTD: The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 34.58205 micromolar/kg/day [7]
Unbound Fraction: The unbound fraction of drug in plasma is 0.14% [8]
Vd: The volume of distribution (Vd) of drug is 147-157 L [5]
Water Solubility: The ability of drug to dissolve in water is measured as 30.4 mg/mL [4]

Adverse Drug Reaction (ADR)

ADR Term	Variation	Related DOT	DOT ID	REF
Adverse drug reaction	Not Available	CYP2D6	OTZJC802	[9]
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Chemical Identifiers

Formula: C17H27NO4
IUPAC Name: (2R,3S)-5-[3-(tert-butylamino)-2-hydroxypropoxy]-1,2,3,4-tetrahydronaphthalene-2,3-diol
Canonical SMILES: CC(C)(C)NCC(COC1=CC=CC2=C1C[C@@H]([C@@H](C2)O)O)O
InChI: InChI=1S/C17H27NO4/c1-17(2,3)18-9-12(19)10-22-16-6-4-5-11-7-14(20)15(21)8-13(11)16/h4-6,12,14-15,18-21H,7-10H2,1-3H3/t12?,14-,15+/m1/s1
InChIKey: VWPOSFSPZNDTMJ-UCWKZMIHSA-N

Cross-matching ID

PubChem CID: 39147
CAS Number: 220045-89-6
DrugBank ID: DB01203
TTD ID: D05SHK
VARIDT ID: DR01261
ACDINA ID: D00452

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
Adrenergic receptor beta-1 (ADRB1)	TTR6W5O	ADRB1_HUMAN	Modulator	[10]

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Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	MOA	REF
Organic anion transporting polypeptide 1A2 (SLCO1A2)	DTE2B1D	SO1A2_HUMAN	Substrate	[11]
P-glycoprotein 1 (ABCB1)	DTUGYRD	MDR1_HUMAN	Substrate	[12]

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Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
Cytochrome P450 2D6 (CYP2D6)	OTZJC802	CP2D6_HUMAN	Drug Response	[9]

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Molecular Interaction Atlas (MIA)

MIA Detail

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Drug-Drug Interaction (DDI) Information of This Drug

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

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Bepridil	DM0RKS4	Moderate	Increased risk of cardiac depression by the combination of Nadolol and Bepridil.	Angina pectoris [BA40]	[13]
Dronedarone	DMA8FS5	Moderate	Decreased metabolism of Nadolol caused by Dronedarone mediated inhibition of CYP450 enzyme.	Angina pectoris [BA40]	[14]
Cariprazine	DMJYDVK	Moderate	Additive hypotensive effects by the combination of Nadolol and Cariprazine.	Bipolar disorder [6A60]	[15]
Atracurium	DM42HXN	Moderate	Additive cardiorespiratory depression effects by the combination of Nadolol and Atracurium.	Corneal disease [9A76-9A78]	[16]
Mivacurium	DM473VD	Moderate	Additive neuromuscular blocking effects by the combination of Nadolol and Mivacurium.	Corneal disease [9A76-9A78]	[16]
Pasireotide	DMHM7JS	Moderate	Increased risk of atrioventricular block by the combination of Nadolol and Pasireotide.	Cushing syndrome [5A70]	[17]
OPC-34712	DMHG57U	Moderate	Additive hypotensive effects by the combination of Nadolol and OPC-34712.	Depression [6A70-6A7Z]	[15]
Mepenzolate	DM8YU2F	Moderate	Antagonize the effect of Nadolol when combined with Mepenzolate.	Digestive system disease [DE2Z]	[18]
Levamlodipine	DM92S6N	Moderate	Increased risk of cardiac depression by the combination of Nadolol and Levamlodipine.	Hypertension [BA00-BA04]	[13]
Clevidipine butyrate	DMW4M97	Moderate	Increased risk of cardiac depression by the combination of Nadolol and Clevidipine butyrate.	Hypertension [BA00-BA04]	[13]
Belladonna	DM2RBWK	Moderate	Antagonize the effect of Nadolol when combined with Belladonna.	Infectious gastroenteritis/colitis [1A40]	[18]
ITI-007	DMUQ1DO	Moderate	Additive hypotensive effects by the combination of Nadolol and ITI-007.	Insomnia [7A00-7A0Z]	[15]
Lanthanum carbonate	DMMJQSH	Moderate	Decreased absorption of Nadolol due to formation of complexes caused by Lanthanum carbonate.	Mineral absorption/transport disorder [5C64]	[17]
Siponimod	DM2R86O	Major	Increased risk of bradycardia by the combination of Nadolol and Siponimod.	Multiple sclerosis [8A40]	[19]
Fingolimod	DM5JVAN	Major	Increased risk of bradycardia by the combination of Nadolol and Fingolimod.	Multiple sclerosis [8A40]	[20]
Ozanimod	DMT6AM2	Moderate	Increased risk of bradycardia by the combination of Nadolol and Ozanimod.	Multiple sclerosis [8A40]	[21]
Polythiazide	DMCH80F	Moderate	Increased risk of ventricular arrhythmias by the combination of Nadolol and Polythiazide.	Oedema [MG29]	[22]
Methylscopolamine	DM5VWOB	Moderate	Antagonize the effect of Nadolol when combined with Methylscopolamine.	Peptic ulcer [DA61]	[18]
Silodosin	DMJSBT6	Moderate	Additive hypotensive effects by the combination of Nadolol and Silodosin.	Prostate hyperplasia [GA90]	[23]
Levomepromazine	DMIKFEL	Moderate	Additive hypotensive effects by the combination of Nadolol and Levomepromazine.	Psychotic disorder [6A20-6A25]	[15]
Quetiapine	DM1N62C	Moderate	Additive hypotensive effects by the combination of Nadolol and Quetiapine.	Schizophrenia [6A20]	[15]
Aripiprazole	DM3NUMH	Moderate	Additive hypotensive effects by the combination of Nadolol and Aripiprazole.	Schizophrenia [6A20]	[15]
Iloperidone	DM6AUFY	Moderate	Additive hypotensive effects by the combination of Nadolol and Iloperidone.	Schizophrenia [6A20]	[15]
Paliperidone	DM7NPJS	Moderate	Additive hypotensive effects by the combination of Nadolol and Paliperidone.	Schizophrenia [6A20]	[15]
Molindone	DMAH70G	Moderate	Additive hypotensive effects by the combination of Nadolol and Molindone.	Schizophrenia [6A20]	[15]
Thiothixene	DMDINC4	Moderate	Additive hypotensive effects by the combination of Nadolol and Thiothixene.	Schizophrenia [6A20]	[15]
Asenapine	DMSQZE2	Moderate	Additive hypotensive effects by the combination of Nadolol and Asenapine.	Schizophrenia [6A20]	[15]
Pipecuronium	DM5F84A	Moderate	Additive cardiorespiratory depression effects by the combination of Nadolol and Pipecuronium.	Tonus and reflex abnormality [MB47]	[16]
Vecuronium	DMP0UK2	Moderate	Additive neuromuscular blocking effects by the combination of Nadolol and Vecuronium.	Tonus and reflex abnormality [MB47]	[16]
Trimeprazine	DMEMV9D	Moderate	Additive hypotensive effects by the combination of Nadolol and Trimeprazine.	Vasomotor/allergic rhinitis [CA08]	[24]
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⏷ Show the Full List of 30 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
FD&C blue no. 2	E00446	2723854	Colorant
Kyselina citronova	E00014	311	Acidulant; Antioxidant; Buffering agent; Complexing agent; Flavoring agent
Quinoline yellow WS	E00309	24671	Colorant
Sodium lauryl sulfate	E00464	3423265	Emulsifying agent; Modified-release agent; Penetration agent; Solubilizing agent; Surfactant; lubricant
Beta-D-lactose	E00099	6134	Diluent; Dry powder inhaler carrier; Lyophilization aid
Carmellose sodium	E00625	Not Available	Disintegrant
Citric acid monohydrate	E00271	22230	Acidulant; Antioxidant; Buffering agent; Complexing agent; Flavoring agent
Ferric hydroxide oxide yellow	E00539	23320441	Colorant
Lactose monohydrate	E00393	104938	Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate	E00208	11177	lubricant
Povidone	E00667	Not Available	Binding agent; Coating agent; Disintegrant; Film/membrane-forming agent; Solubilizing agent; Suspending agent
Silicon dioxide	E00670	Not Available	Anticaking agent; Opacifying agent; Viscosity-controlling agent
Vinylpyrrolidone	E00668	Not Available	Binding agent; Coating agent; Disintegrant; Film/membrane-forming agent; Solubilizing agent; Suspending agent
Water	E00035	962	Solvent
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Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Nadolol 80 mg tablet	80 mg	Oral Tablet	Oral
Nadolol 20 mg tablet	20 mg	Oral Tablet	Oral
Nadolol 40 mg tablet	40 mg	Oral Tablet	Oral

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References

1	Nadolol 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: 554).
3	Schafer-Korting M, Bach N, Knauf H, Mutschler E: Pharmacokinetics of nadolol in healthy subjects. Eur J Clin Pharmacol. 1984;26(1):125-7.
4	BDDCS applied to over 900 drugs
5	Kohne CH, Peters GJ: UFT: mechanism of drug action. Oncology (Williston Park). 2000 Oct;14(10 Suppl 9):13-8.
6	FDA Approved Drug Products: Nadolol Oral Tablets
7	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
8	Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
9	ADReCS-Target: target profiles for aiding drug safety research and application. Nucleic Acids Res. 2018 Jan 4;46(D1):D911-D917. doi: 10.1093/nar/gkx899.
10	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
11	Involvement of influx and efflux transport systems in gastrointestinal absorption of celiprolol. J Pharm Sci. 2009 Jul;98(7):2529-39.
12	Tarascon Pocket Pharmacopoeia 2018 Classic Shirt-Pocket Edition.
13	Anastassiades CJ "Nifedipine and beta-blocker drugs." Br Med J 281 (1980): 1251-2. [PMID: 6107167]
14	Product Information. Multaq (dronedarone). sanofi-aventis , Bridgewater, NJ.
15	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]
16	Chapple DJ, Clark JS, Hughes R "Interaction between atracurium and drugs used in anaesthesia." Br J Anaesth 55 Suppl 1 (1983): s17-22. [PMID: 6688011]
17	Canadian Pharmacists Association.
18	Cerner Multum, Inc. "UK Summary of Product Characteristics.".
19	Cerner Multum, Inc. "Australian Product Information.".
20	Product Information. Gilenya (fingolimod). Novartis Pharmaceuticals, East Hanover, NJ.
21	Product Information. Zeposia (ozanimod). Celgene Corporation, Summit, NJ.
22	Dean S, Kendall MJ, Potter S, Thompson MH, Jackson DA "Nadolol in combination with indapamide and xipamide in resistant hypertensives." Eur J Clin Pharmacol 28 (1985): 29-33. [PMID: 3987783]
23	Chrysant SG "Experience with terazosin administered in combination with other antihypertensive agents." Am J Med 80 (1986): 55-61. [PMID: 2872808]
24	Product Information. Clozaril (clozapine). Novartis Pharmaceuticals, East Hanover, NJ.