Drug General Information (ID: D0043)
  Drug Name
Alosetron
  Drug Type Small molecule
  Drug Synonymous
Lotronex; Lotrpnex; ALOSETRON HYDROCHLORIDE; Alosetron HCl; Alosetron hydrochloride [USAN]; Alosetron monohydrochloride; GR 68755; GR 68755X; GR 68755c; GR68755; Alosetron (INN); Alosetron [INN:BAN]; Alosetron hydrochloride (USAN); GR-68755C; Lotronex (TN); Lotrpnex (TN); 1H-Pyrido(4,3-b)indol-1-one, 2,3,4,5-tetrahydro-5-methyl-2((5-methyl-1H-imidazol-4-yl)methyl)-, monohydrochloride; 1H-Pyrido(4,3-b)indol-1-one, 2,3,4,5-tetrahydro-5-methyl-2-((5-methyl-1H-imidazol-4-yl)methyl)-, monohydrochloride; 1H-Pyrido[4,3-b]indol-1-one, 2,3,4,5-tetrahydro-5-methyl-2-[(4-methyl-1H-imidazol-5-yl)methyl]-, hydrochloride (1:1); 1H-Pyrido[4,3-b]indol-1-one, 2,3,4,5-tetrahydro-5-methyl-2-[(5-methyl-1H-imidazol; 1H-Pyrido[4,3-b]indol-1-one, 2,3,4,5-tetrahydro-5-methyl-2-[(5-methyl-1H-imidazol-4-yl)methyl]-(9CI); 2,3,4,5-Tetrahydro-5-methyl-2-((5-methyl-1H-imidazol-4-yl)methyl)-1H-pyrido(4,3-b)indol-1-one; 2,3,4,5-Tetrahydro-5-methyl-2-((5-methylimidazol-4-yl)methyl)-1H-pyrido(4,3-b)indol-1-one monohydrochloride; 2,3,4,5-tetrahydro-5-methyl-2-((5-methylimidazol-4-yl)methyl)-1H-pyridol(4,3-b)indol-1-one monohydrochloride; 2,3,4,5-tetrahydro-5-methyl-2-[(5-methyl-1H-imidazol-4-yl)methyl]-1H-pyrido[4,3-b]indol-1-one, monohydrochloride; 5-methyl-2-[(5-methyl-1H-imidazol-4-yl)methyl]-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indol-1-one; 5-methyl-2-[(5-methyl-1H-imidazol-4-yl)methyl]-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indol-1-one hydrochloride; 5-methyl-2-[(5-methyl-1H-imidazol-4-yl)methyl]-3,4-dihydropyrido[4,3-b]indol-1-one; 5-methyl-2-[(5-methyl-1H-imidazol-4-yl)methyl]-3,4-dihydropyrido[4,3-b]indol-1-one hydrochloride
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  Disease Class DD91: Irritable bowel syndrome
  Therapeutic Class Gastrointestinal Agents
  Structure Could Not Find 2D Structure
3D Structure 2D Structure
  Formula C17H18N4O
  InChI 1S/C17H18N4O/c1-11-13(19-10-18-11)9-21-8-7-15-16(17(21)22)12-5-3-4-6-14(12)20(15)2/h3-6,10H,7-9H2,1-2H3,(H,18,19)
  InChIKey JSWZEAMFRNKZNL-UHFFFAOYSA-N
  Canonical SMILES CC1=C(N=CN1)CN2CCC3=C(C2=O)C4=CC=CC=C4N3C
  External Link
Pubchem ID 2099
CAS Number 122852-42-0
CHEBI ID 253342
TTD ID D06GKN

Drug-Drug Interaction Network
  Sunburst Graph
AM004  Affected intra/extra-hepatic metabolism
AM006  Pharmacodynamic additive effects
BM017  CYP450 enzyme inhibition
BM018  Non-CYP450 enzyme inhibition
BM022  CYP450 enzyme induction
BM076  Increased risk of prolong QT interval
BM109  Increased risk of other adverse reactions (Unspecific)
  Relation Graph
 Full list of drugs interacting with Alosetron
      Affected intra/extra-hepatic metabolism
   CYP450 enzyme inhibition Drug Num:  46
Drug ID
 
Drug Name
Formula Pubchem ID Severity Level Interaction Detail REF
D0687
 
Fluvoxamine
 
C15H21F3N2O2
 
5324346 
Major    Inter Info   
[4], [5]
D0002
 
Abametapir (topical)
 
C12H12N2
 
15664 
Moderate    Inter Info   
[6]
D0116
 
Atazanavir
 
C38H52N6O7
 
148192 
Moderate    Inter Info   
[5]
D0251
 
Capmatinib
 
C23H17FN6O
 
25145656 
Moderate    Inter Info   
[5]
D0349
 
Clarithromycin
 
C38H69NO13
 
84029 
Moderate    Inter Info   
[5]
D0432
 
Deferasirox
 
C21H15N3O4
 
214348 
Moderate    Inter Info   
[5]
D0545
 
Echinacea
 
NA
 
NA
Moderate    Inter Info   
[5]
D0692
 
Fosamprenavir
 
C25H36N3O9PS
 
131536 
Moderate    Inter Info   
[5]
D0699
 
Fostamatinib
 
C23H26FN6O9P
 
11671467 
Moderate    Inter Info   
[15]
D0724
 
Givosiran
 
C78H139N11O30
 
119058042 
Moderate    Inter Info   
[5]
D0867
 
Itraconazole
 
C35H38Cl2N8O4
 
55283 
Moderate    Inter Info   
[5]
D0880
 
Ketoconazole
 
C26H28Cl2N4O4
 
456201 
Moderate    Inter Info   
[5]
D1057
 
Miconazole
 
C18H14Cl4N2O
 
4189 
Moderate    Inter Info   
[5]
D1117
 
Nefazodone
 
C25H32ClN5O2
 
4449 
Moderate    Inter Info   
[5]
D1131
 
Niclosamide
 
C13H8Cl2N2O4
 
4477 
Moderate    Inter Info   
[5]
D1160
 
Obeticholic acid
 
C26H44O4
 
447715 
Moderate    Inter Info   
[5]
D1189
 
Osilodrostat
 
C13H10FN3
 
44139752 
Moderate    Inter Info   
[5]
D1339
 
Primaquine
 
C15H21N3O
 
4908 
Moderate    Inter Info   
[5]
D1353
 
Propafenone
 
C21H27NO3
 
4932 
Moderate    Inter Info   
[5]
D1398
 
Ribociclib
 
C23H30N8O
 
44631912 
Moderate    Inter Info   
[19], [20], [21], [22], [23], [24], [25], [26], [27]
D1432
 
Rucaparib
 
C19H18FN3O
 
9931954 
Moderate    Inter Info   
[5]
D1544
 
Telithromycin
 
C43H65N5O10
 
3002190 
Moderate    Inter Info   
[5]
D1653
 
Troleandomycin
 
C41H67NO15
 
202225 
Moderate    Inter Info   
[5]
D1687
 
Vemurafenib
 
C23H18ClF2N3O3S
 
42611257 
Moderate    Inter Info   
[5]
D0080
 
Amprenavir
 
C25H35N3O6S
 
65016 
Moderate    Inter Info   
[5]
D0084
 
Anagrelide
 
C10H7Cl2N3O
 
135409400 
Moderate    Inter Info   
[5]
D0231
 
Caffeine
 
C8H10N4O2
 
2519 
Moderate    Inter Info   
[5]
D0337
 
Cimetidine
 
C10H16N6S
 
2756 
Moderate    Inter Info   
[5]
D0341
 
Ciprofloxacin
 
C17H18FN3O3
 
2764 
Moderate    Inter Info   
[5]
D0439
 
Delavirdine
 
C22H28N6O3S
 
5625 
Moderate    Inter Info   
[5]
D0573
 
Enoxacin
 
C15H17FN4O3
 
3229 
Moderate    Inter Info   
[5]
D0597
 
Erythromycin
 
C37H67NO13
 
12560 
Moderate    Inter Info   
[5]
D0740
 
Grepafloxacin
 
C19H22FN3O3
 
72474 
Moderate    Inter Info   
[5]
D0799
 
Indinavir
 
C36H47N5O4
 
5362440 
Moderate    Inter Info   
[5]
D0858
 
Isoniazid
 
C6H7N3O
 
3767 
Moderate    Inter Info   
[5]
D1028
 
Methoxsalen
 
C12H8O4
 
4114 
Moderate    Inter Info   
[5]
D1054
 
Mexiletine
 
C11H17NO
 
4178 
Moderate    Inter Info   
[5]
D1102
 
Nalidixic acid
 
C12H12N2O3
 
4421 
Moderate    Inter Info   
[5]
D1119
 
Nelfinavir
 
C32H45N3O4S
 
64143 
Moderate    Inter Info   
[5]
D1415
 
Ritonavir
 
C37H48N6O5S2
 
392622 
Moderate    Inter Info   
[5]
D1421
 
Rofecoxib
 
C17H14O4S
 
5090 
Moderate    Inter Info   
[5]
D1525
 
Tacrine
 
C13H14N2
 
1935 
Moderate    Inter Info   
[5]
D1571
 
Thiabendazole
 
C10H7N3S
 
5430 
Moderate    Inter Info   
[5]
D1581
 
Ticlopidine
 
C14H14ClNS
 
5472 
Moderate    Inter Info   
[5]
D1706
 
Voriconazole
 
C16H14F3N5O
 
71616 
Moderate    Inter Info   
[5]
D1721
 
Zileuton
 
C11H12N2O2S
 
60490 
Moderate    Inter Info   
[5]
   Non-CYP450 enzyme inhibition Drug Num:  2
Drug ID
 
Drug Name
Formula Pubchem ID Severity Level Interaction Detail REF
D0770
 
Hydralazine
 
C8H8N4
 
3637 
Minor    Inter Info   
[5]
D1343
 
Procainamide
 
C13H21N3O
 
4913 
Minor    Inter Info   
[5]
   CYP450 enzyme induction Drug Num:  9
Drug ID
 
Drug Name
Formula Pubchem ID Severity Level Interaction Detail REF
D0044
 
Alpelisib
 
C19H22F3N5O2S
 
56649450 
Moderate    Inter Info   
[7]
D0095
 
Apalutamide
 
C21H15F4N5O2S
 
24872560 
Moderate    Inter Info   
[8], [9]
D0578
 
Enzalutamide
 
C21H16F4N4O2S
 
15951529 
Moderate    Inter Info   
[11], [12], [8], [13]
D0693
 
Fosaprepitant
 
C23H22F7N4O6P
 
135413538 
Moderate    Inter Info   
[14]
D0953
 
Lorlatinib
 
C21H19FN6O2
 
71731823 
Moderate    Inter Info   
[12], [8], [16]
D1167
 
Olaparib
 
C24H23FN4O3
 
23725625 
Moderate    Inter Info   
[12], [8], [17]
D1190
 
Osimertinib
 
C28H33N7O2
 
71496458 
Moderate    Inter Info   
[18]
D1556
 
Teriflunomide
 
C12H9F3N2O2
 
54684141 
Moderate    Inter Info   
[12], [8], [28]
D0100
 
Aprepitant
 
C23H21F7N4O3
 
135413536 
Moderate    Inter Info   
[14]
      Pharmacodynamic additive effects
   Increased risk of prolong QT interval Drug Num:  1
Drug ID
 
Drug Name
Formula Pubchem ID Severity Level Interaction Detail REF
D0097
 
Apomorphine
 
C17H17NO2
 
6005 
Major    Inter Info   
[1], [2], [3]
   Increased risk of other adverse reactions (Unspecific) Drug Num:  1
Drug ID
 
Drug Name
Formula Pubchem ID Severity Level Interaction Detail REF
D0562
 
Eluxadoline
 
C32H35N5O5
 
11250029 
Moderate    Inter Info   
[8], [10]
References
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2 Product Information. Anzemet (dolasetron). Hoechst Marion-Roussel Inc, Kansas City, MO.
3 Product Information. Apokyn (apomorphine). Mylan Pharmaceuticals Inc, Morgantown, WV.
4 Brosen K, Skjelbo E, Rasmussen BB, Poulsen HE, Loft S "Fluvoxamine is a potent inhibitor of cytochrome P4501A2." Biochem Pharmacol 45 (1993): 1211-4. [PMID: 8466541]
5 Product Information. Lotronex (alosetron). Glaxo Wellcome, Research Triangle Park, NC.
6 Product Information. Xeglyze (abametapir topical). Dr. Reddy's Laboratories Inc, Upper Saddle River, NJ.
7 Product Information. Piqray (alpelisib). Novartis Pharmaceuticals, East Hanover, NJ.
8 Cerner Multum, Inc. "UK Summary of Product Characteristics.".
9 Product Information. Erleada (apalutamide). Janssen Biotech, Inc., Horsham, PA, PA.
10 Product Information. Viberzi (eluxadoline). Actavis Pharma, Inc., Parsippany, NJ.
11 Benoist G, van Oort I, et al "Drug-drug interaction potential in men treated with enzalutamide: Mind the gap." Br J Clin Pharmacol 0 (2017): epub. [PMID: 28881501]
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13 Product Information. Xtandi (enzalutamide). Astellas Pharma US, Inc, Deerfield, IL.
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15 Product Information. Tavalisse (fostamatinib). Rigel Pharmaceuticals, South San Francisco, CA.
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17 EMA. European Medicines Agency. European Union "EMA - List of medicines under additional monitoring.".
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19 DSouza DL, Levasseur LM, Nezamis J, Robbins DK, Simms L, Koch KM "Effect of alosetron on the pharmacokinetics of alprazolam." J Clin Pharmacol 41 (2001): 452-4. [PMID: 11304902]
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