Details of the Drug

General Information of Drug (ID: DM3JCVS)

Drug Name
Terazosin
Synonyms
Blavin; Flumarc; Fosfomic; Hytracin; Hytrin; Terazosabb; Terazosina; Terazosine; Terazosinum; Vasomet; Trazosin HCl; A 45975; Abbott 45975; A-45975; Hytrin (TN); Terazosabb (TN); Terazosin (INN); Terazosin [INN:BAN]; Terazosina [INN-Spanish]; Terazosine [INN-French]; Terazosinum [INN-Latin]; [4-(4-amino-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl](tetrahydrofuran-2-yl)methanone; [4-(4-amino-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl]-(oxolan-2-yl)methanone; 1-(4-Amino-6,7-dimethoxy-2-quinazolinyl)-4-((tetrahydro-2-furanyl)carbonyl)piperazine; 1-(4-Amino-6,7-dimethoxy-2-quinazolinyl)-4-(tetrahydro-2-furoyl)piperazine; 6,7-bis(methyloxy)-2-[4-(tetrahydrofuran-2-ylcarbonyl)piperazin-1-yl]quinazolin-4-amine; 6,7-dimethoxy-2-[4-(tetrahydrofuran-2-ylcarbonyl)piperazin-1-yl]quinazolin-4-amine
Indication
Disease Entry ICD 11 Status REF
Benign prostatic hyperplasia GA90 Approved [1]
Therapeutic Class
Anticancer Agents
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 387.4
Logarithm of the Partition Coefficient (xlogp) 1.4
Rotatable Bond Count (rotbonds) 4
Hydrogen Bond Donor Count (hbonddonor) 1
Hydrogen Bond Acceptor Count (hbondacc) 8
ADMET Property
Absorption
The absorption of drug is 90% [2]
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 1: high solubility and high permeability [3]
Bioavailability
90% of drug becomes completely available to its intended biological destination(s) [4]
Clearance
The renal clearance of drug is 10 mL/min [2]
Elimination
Approximately 10% of the oral dose is excreted unchanged in the urine and approximately 20% is excreted in the feces [2]
Half-life
The concentration or amount of drug in body reduced by one-half in 12 hours [2]
Metabolism
The drug is metabolized via the hepatic [2]
MRTD
The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 0.85948 micromolar/kg/day [5]
Unbound Fraction
The unbound fraction of drug in plasma is 0.08% [6]
Vd
The volume of distribution (Vd) of drug is 25-30 L [2]
Water Solubility
The ability of drug to dissolve in water is measured as 24.2 mg/mL [3]
Chemical Identifiers
Formula
C19H25N5O4
IUPAC Name
[4-(4-amino-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl]-(oxolan-2-yl)methanone
Canonical SMILES
COC1=C(C=C2C(=C1)C(=NC(=N2)N3CCN(CC3)C(=O)C4CCCO4)N)OC
InChI
InChI=1S/C19H25N5O4/c1-26-15-10-12-13(11-16(15)27-2)21-19(22-17(12)20)24-7-5-23(6-8-24)18(25)14-4-3-9-28-14/h10-11,14H,3-9H2,1-2H3,(H2,20,21,22)
InChIKey
VCKUSRYTPJJLNI-UHFFFAOYSA-N
Cross-matching ID
PubChem CID
5401
ChEBI ID
CHEBI:9445
CAS Number
63590-64-7
DrugBank ID
DB01162
TTD ID
D0P9RF
VARIDT ID
DR00869
ACDINA ID
D00662
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
Adrenergic receptor alpha-1D (ADRA1D) TT34BHT ADA1D_HUMAN Antagonist [7]
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 Same Disease as Terazosin
DDI Drug Name DDI Drug ID Severity Mechanism Disease REF
Silodosin DMJSBT6 Moderate Additive hypotensive effects by the combination of Terazosin and Silodosin. Prostate hyperplasia [GA90] [8]
Coadministration of a Drug Treating the Disease Different from Terazosin (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Cariprazine DMJYDVK Moderate Additive hypotensive effects by the combination of Terazosin and Cariprazine. Bipolar disorder [6A60] [9]
Isocarboxazid DMAF1NB Moderate Additive hypotensive effects by the combination of Terazosin and Isocarboxazid. Depression [6A70-6A7Z] [10]
OPC-34712 DMHG57U Moderate Additive hypotensive effects by the combination of Terazosin and OPC-34712. Depression [6A70-6A7Z] [9]
Nadolol DMW6GVL Moderate Additive hypotensive effects by the combination of Terazosin and Nadolol. Essential hypertension [BA00] [11]
Metipranolol DMJMVKI Moderate Additive hypotensive effects by the combination of Terazosin and Metipranolol. Glaucoma [9C61] [11]
Levobetaxolol DMSREPX Moderate Additive hypotensive effects by the combination of Terazosin and Levobetaxolol. Glaucoma [9C61] [11]
Levobunolol DMTNFCQ Moderate Additive hypotensive effects by the combination of Terazosin and Levobunolol. Glaucoma [9C61] [11]
Procarbazine DMIK367 Moderate Additive hypotensive effects by the combination of Terazosin and Procarbazine. Hodgkin lymphoma [2B30] [10]
Acebutolol DM0TI4U Moderate Additive hypotensive effects by the combination of Terazosin and Acebutolol. Hypertension [BA00-BA04] [11]
Captopril DM458UM Moderate Additive hypotensive effects by the combination of Terazosin and Captopril. Hypertension [BA00-BA04] [12]
Penbutolol DM4ES8F Moderate Additive hypotensive effects by the combination of Terazosin and Penbutolol. Hypertension [BA00-BA04] [11]
Nebivolol DM7F1PA Moderate Additive hypotensive effects by the combination of Terazosin and Nebivolol. Hypertension [BA00-BA04] [11]
ITI-007 DMUQ1DO Moderate Additive hypotensive effects by the combination of Terazosin and ITI-007. Insomnia [7A00-7A0Z] [9]
Allopregnanolone DMNLHAC Moderate Additive CNS depression effects by the combination of Terazosin and Allopregnanolone. Mental/behavioural/neurodevelopmental disorder [6E20-6E8Z] [13]
Lasmiditan DMXLVDT Moderate Additive CNS depression effects by the combination of Terazosin and Lasmiditan. Migraine [8A80] [14]
Ozanimod DMT6AM2 Moderate Additive hypotensive effects by the combination of Terazosin and Ozanimod. Multiple sclerosis [8A40] [10]
Rasagiline DM3WKQ4 Moderate Additive hypotensive effects by the combination of Terazosin and Rasagiline. Parkinsonism [8A00] [10]
Levomepromazine DMIKFEL Moderate Additive hypotensive effects by the combination of Terazosin and Levomepromazine. Psychotic disorder [6A20-6A25] [9]
Quetiapine DM1N62C Moderate Additive hypotensive effects by the combination of Terazosin and Quetiapine. Schizophrenia [6A20] [9]
Aripiprazole DM3NUMH Moderate Additive hypotensive effects by the combination of Terazosin and Aripiprazole. Schizophrenia [6A20] [9]
Iloperidone DM6AUFY Moderate Additive hypotensive effects by the combination of Terazosin and Iloperidone. Schizophrenia [6A20] [9]
Paliperidone DM7NPJS Moderate Additive hypotensive effects by the combination of Terazosin and Paliperidone. Schizophrenia [6A20] [9]
Molindone DMAH70G Moderate Additive hypotensive effects by the combination of Terazosin and Molindone. Schizophrenia [6A20] [9]
Thiothixene DMDINC4 Moderate Additive hypotensive effects by the combination of Terazosin and Thiothixene. Schizophrenia [6A20] [9]
Amisulpride DMSJVAM Moderate Additive hypotensive effects by the combination of Terazosin and Amisulpride. Schizophrenia [6A20] [9]
Asenapine DMSQZE2 Moderate Additive hypotensive effects by the combination of Terazosin and Asenapine. Schizophrenia [6A20] [9]
Trimeprazine DMEMV9D Moderate Additive hypotensive effects by the combination of Terazosin and Trimeprazine. Vasomotor/allergic rhinitis [CA08] [15]
⏷ Show the Full List of 27 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
Allura red AC dye E00338 33258 Colorant
D&C red no. 28 E00491 6097185 Colorant
D&C red no. 33 E00261 19116 Colorant
FD&C blue no. 1 E00263 19700 Colorant
FD&C blue no. 2 E00446 2723854 Colorant
Quinoline yellow WS E00309 24671 Colorant
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
Aluminum chlorohydrex propylene glycol E00594 71587575 Other agent
Ammonia E00007 222 Alkalizing agent
Beta-D-lactose E00099 6134 Diluent; Dry powder inhaler carrier; Lyophilization aid
Crospovidone E00626 Not Available Disintegrant
Ferric hydroxide oxide yellow E00539 23320441 Colorant
Ferrosoferric oxide E00231 14789 Colorant
Gelatin E00630 Not Available Other agent
Lactose monohydrate E00393 104938 Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate E00208 11177 lubricant
Potassium hydroxide E00233 14797 Alkalizing agent
Povidone E00667 Not Available Binding agent; Coating agent; Disintegrant; Film/membrane-forming agent; Solubilizing agent; Suspending agent
Propylene glycol E00040 1030 Antimicrobial preservative; Humectant; Plasticizing agent; Solvent
Silicon dioxide E00670 Not Available Anticaking agent; Opacifying agent; Viscosity-controlling agent
Talc E00520 16211421 Anticaking agent; Diluent; Glidant; lubricant
Titanium dioxide E00322 26042 Coating agent; Colorant; Opacifying agent
Hydrophobic colloidal silica E00285 24261 Anticaking agent; Emulsion stabilizing agent; Glidant; Suspending agent; Viscosity-controlling agent
Pregelatinized starch E00674 Not Available Binding agent; Diluent; Disintegrant
⏷ Show the Full List of 25 Pharmaceutical Excipients of This Drug
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Terazosin 2 mg capsule 2 mg Oral Capsule Oral
Terazosin 10 mg capsule 10 mg Oral Capsule Oral
Terazosin 5 mg capsule 5 mg Oral Capsule Oral
Terazosin 1 mg capsule 1 mg Oral Capsule Oral
Terazosin Hydrochloride eq 10mg base capsule eq 10mg base Capsule Oral
Terazosin Hydrochloride eq 2mg base capsule eq 2mg base Capsule Oral
Terazosin Hydrochloride eq 1mg base tablet eq 1mg base Tablet Oral
Jump to Detail Pharmaceutical Formulation Page of This Drug

References

1 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: 7302).
2 Pharmacokinetics of terazosin. Am J Med. 1986 May 23;80(5B):20-4.
3 BDDCS applied to over 900 drugs
4 Critical Evaluation of Human Oral Bioavailability for Pharmaceutical Drugs by Using Various Cheminformatics Approaches
5 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
6 Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
7 Induction of prostate apoptosis by alpha1-adrenoceptor antagonists: mechanistic significance of the quinazoline component. Prostate Cancer Prostatic Dis. 2002;5(2):88-95.
8 Product Information. Flomax (tamsulosin). Boehringer-Ingelheim, Ridgefield, CT.
9 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]
10 Ban TA "Drug interactions with psychoactive drugs." Dis Nerv Syst 36 (1975): 164-6. [PMID: 1116424]
11 Chrysant SG "Experience with terazosin administered in combination with other antihypertensive agents." Am J Med 80 (1986): 55-61. [PMID: 2872808]
12 Baba T, Tomiyama T, Takebe K "Enhancement by an ACE inhibitor of first-dose hypotension caused by an alpha-blocker." N Engl J Med 322 (1990): 1237. [PMID: 1970122]
13 Product Information. Zulresso (brexanolone). Sage Therapeutics, Inc., Cambridge, MA.
14 Product Information. Reyvow (lasmiditan). Lilly, Eli and Company, Indianapolis, IN.
15 Product Information. Clozaril (clozapine). Novartis Pharmaceuticals, East Hanover, NJ.