Details of the Drug

General Information of Drug (ID: DMW649X)

• Drug Name: Eletriptan
• Synonyms: Eletriptanum; Relpax; UK 116044; UK116044; Eletriptan (INN); Eletriptan [INN:BAN]; Relpax (TN); UK-116044; UK-116044-04; (R)-3-[(1-Methyl-2-pyrrolidinyl)methyl]-5-[2-(phenylsulfonyl)ethyl]-1H-Indole; (R)-5-[2-(Benzenesulfonyl)ethyl]-3-[(N-methylpyrrolidin-2-yl)methyl]-1H-indole; 3-(((R)-1-Methyl-2-pyrrolidinyl)methyl)-5-(2-(phenylsulfonyl)ethyl)indole; 3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-5-[2-(phenylsulfonyl)ethyl]-1H-indole; 5-[2-(benzenesulfonyl)ethyl]-3-[[(2R)-1-methylpyrrolidin-2-yl]methyl]-1H-indole

Indication

Disease Entry	ICD 11	Status	REF
Migraine	8A80	Approved	[1]

• Therapeutic Class: Antimigraine Agents
• Affected Organisms: Humans and other mammals
• ATC Code:
  N02CC06: Eletriptan
  N02CC: Selective serotonin (5HT1) agonists
  N02C: ANTIMIGRAINE PREPARATIONS
  N02: ANALGESICS
  N: NERVOUS SYSTEM
• Drug Type: Small molecular drug
• #Ro5 Violations (Lipinski): 0:
  Molecular Weight (mw); 382.5
  Logarithm of the Partition Coefficient (xlogp); 4.1
  Rotatable Bond Count (rotbonds); 6
  Hydrogen Bond Donor Count (hbonddonor); 1
  Hydrogen Bond Acceptor Count (hbondacc); 3
• ADMET Property:
  BDDCS Class: Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 1: high solubility and high permeability [2]
  Bioavailability: The bioavailability of drug is 50% []
  Clearance: The renal clearance of drug is 3.9 L/h []
  Elimination: 5% of drug is excreted from urine in the unchanged form [2]
  Half-life: The concentration or amount of drug in body reduced by one-half in 4 hours [3]
  Metabolism: The drug is metabolized via the cytochrome P-450 enzyme CYP3A4 []
  MRTD: The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 1.494 micromolar/kg/day [4]
  Unbound Fraction: The unbound fraction of drug in plasma is 0.15% [3]
  Vd: The volume of distribution (Vd) of drug is 138 L []
  Water Solubility: The ability of drug to dissolve in water is measured as 4 mg/mL [2]
• Chemical Identifiers:
  Formula: C22H26N2O2S
  IUPAC Name: 5-[2-(benzenesulfonyl)ethyl]-3-[[(2R)-1-methylpyrrolidin-2-yl]methyl]-1H-indole
  Canonical SMILES: CN1CCC[C@@H]1CC2=CNC3=C2C=C(C=C3)CCS(=O)(=O)C4=CC=CC=C4
  InChI: InChI=1S/C22H26N2O2S/c1-24-12-5-6-19(24)15-18-16-23-22-10-9-17(14-21(18)22)11-13-27(25,26)20-7-3-2-4-8-20/h2-4,7-10,14,16,19,23H,5-6,11-13,15H2,1H3/t19-/m1/s1
  InChIKey: PWVXXGRKLHYWKM-LJQANCHMSA-N
• Cross-matching ID:
  PubChem CID: 77993
  ChEBI ID: CHEBI:50922
  CAS Number: 143322-58-1
  UNII: 22QOO9B8KI
  DrugBank ID: DB00216
  TTD ID: D02DMQ
  VARIDT ID: DR00981
  INTEDE ID: DR0564
  ACDINA ID: D00223

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
5-HT 1B receptor (HTR1B)	TTK8CXU	5HT1B_HUMAN	Modulator	[5]
5-HT 1D receptor (HTR1D)	TT6MSOK	5HT1D_HUMAN	Modulator	[5]

Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	MOA	REF
P-glycoprotein 1 (ABCB1)	DTUGYRD	MDR1_HUMAN	Substrate	[6]

Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
Cytochrome P450 3A4 (CYP3A4) Main DME	DE4LYSA	CP3A4_HUMAN	Substrate	[7]
Cytochrome P450 2D6 (CYP2D6)	DECB0K3	CP2D6_HUMAN	Substrate	[8]
Cytochrome P450 2C9 (CYP2C9)	DE5IED8	CP2C9_HUMAN	Substrate	[9]
Prostaglandin G/H synthase 1 (COX-1)	DE073H6	PGH1_HUMAN	Substrate	[7]

Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-3 (GNB3)	OTA6HYBA	GBB3_HUMAN	Drug Response	[10]

Drug-Drug Interaction (DDI) Information of This Drug

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

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Methylene blue	DMJAPE7	Major	Additive serotonergic effects by the combination of Eletriptan and Methylene blue.	Acquired methaemoglobinaemia [3A93]	[11]
Oliceridine	DM6MDCF	Moderate	Additive CNS depression effects by the combination of Eletriptan and Oliceridine.	Acute pain [MG31]	[12]
Dronedarone	DMA8FS5	Moderate	Decreased metabolism of Eletriptan caused by Dronedarone mediated inhibition of CYP450 enzyme.	Angina pectoris [BA40]	[13]
Nifedipine	DMSVOZT	Moderate	Decreased metabolism of Eletriptan caused by Nifedipine mediated inhibition of CYP450 enzyme.	Angina pectoris [BA40]	[13]
Posaconazole	DMUL5EW	Major	Decreased metabolism of Eletriptan caused by Posaconazole mediated inhibition of CYP450 enzyme.	Aspergillosis [1F20]	[13]
Zafirlukast	DMHNQOG	Moderate	Decreased metabolism of Eletriptan caused by Zafirlukast mediated inhibition of CYP450 enzyme.	Asthma [CA23]	[13]
Desipramine	DMT2FDC	Major	Additive serotonergic effects by the combination of Eletriptan and Desipramine.	Attention deficit hyperactivity disorder [6A05]	[14]
Droxidopa	DM5YF4M	Moderate	Additive hypertensive effects by the combination of Eletriptan and Droxidopa.	Autonomic nervous system disorder [8D87]	[15]
Ciprofloxacin XR	DM2NLS9	Moderate	Decreased metabolism of Eletriptan caused by Ciprofloxacin XR mediated inhibition of CYP450 enzyme.	Bacterial infection [1A00-1C4Z]	[13]
Dalfopristin	DM4LTKV	Moderate	Decreased metabolism of Eletriptan caused by Dalfopristin mediated inhibition of CYP450 enzyme.	Bacterial infection [1A00-1C4Z]	[13]
Clarithromycin	DM4M1SG	Major	Decreased metabolism of Eletriptan caused by Clarithromycin mediated inhibition of CYP450 enzyme.	Bacterial infection [1A00-1C4Z]	[13]
Chloramphenicol	DMFXEWT	Moderate	Decreased metabolism of Eletriptan caused by Chloramphenicol mediated inhibition of CYP450 enzyme.	Bacterial infection [1A00-1C4Z]	[13]
Linezolid	DMGFPU2	Major	Additive serotonergic effects by the combination of Eletriptan and Linezolid.	Bacterial infection [1A00-1C4Z]	[16]
Troleandomycin	DMUZNIG	Major	Decreased metabolism of Eletriptan caused by Troleandomycin mediated inhibition of CYP450 enzyme.	Bacterial infection [1A00-1C4Z]	[13]
Telithromycin	DMZ4P3A	Major	Decreased metabolism of Eletriptan caused by Telithromycin mediated inhibition of CYP450 enzyme.	Bacterial infection [1A00-1C4Z]	[13]
Lapatinib	DM3BH1Y	Moderate	Decreased metabolism of Eletriptan caused by Lapatinib mediated inhibition of CYP450 enzyme.	Breast cancer [2C60-2C6Y]	[13]
Tucatinib	DMBESUA	Major	Decreased metabolism of Eletriptan caused by Tucatinib mediated inhibition of CYP450 enzyme.	Breast cancer [2C60-2C6Y]	[13]
Grepafloxacin	DMGLX0T	Moderate	Decreased metabolism of Eletriptan caused by Grepafloxacin mediated inhibition of CYP450 enzyme.	Bronchitis [CA20]	[13]
Morphine	DMRMS0L	Moderate	Additive CNS depression effects by the combination of Eletriptan and Morphine.	Chronic pain [MG30]	[12]
Levomilnacipran	DMV26S8	Major	Additive serotonergic effects by the combination of Eletriptan and Levomilnacipran.	Chronic pain [MG30]	[14]
Methadone	DMTW6IU	Moderate	Additive serotonergic effects by the combination of Eletriptan and Methadone.	Cough [MD12]	[12]
Mifepristone	DMGZQEF	Major	Decreased metabolism of Eletriptan caused by Mifepristone mediated inhibition of CYP450 enzyme.	Cushing syndrome [5A70]	[17]
Osilodrostat	DMIJC9X	Moderate	Decreased metabolism of Eletriptan caused by Osilodrostat mediated inhibition of CYP450 enzyme.	Cushing syndrome [5A70]	[13]
Ivacaftor	DMZC1HS	Moderate	Decreased metabolism of Eletriptan caused by Ivacaftor mediated inhibition of CYP450 enzyme.	Cystic fibrosis [CA25]	[13]
MK-8228	DMOB58Q	Moderate	Decreased metabolism of Eletriptan caused by MK-8228 mediated inhibition of CYP450 enzyme.	Cytomegaloviral disease [1D82]	[13]
Aprepitant	DM053KT	Moderate	Decreased metabolism of Eletriptan caused by Aprepitant mediated inhibition of CYP450 enzyme.	Depression [6A70-6A7Z]	[13]
Sertraline	DM0FB1J	Major	Additive serotonergic effects by the combination of Eletriptan and Sertraline.	Depression [6A70-6A7Z]	[14]
Fluoxetine	DM3PD2C	Major	Additive serotonergic effects by the combination of Eletriptan and Fluoxetine.	Depression [6A70-6A7Z]	[14]
Vilazodone	DM4LECQ	Major	Additive serotonergic effects by the combination of Eletriptan and Vilazodone.	Depression [6A70-6A7Z]	[14]
Nefazodone	DM4ZS8M	Major	Decreased metabolism of Eletriptan caused by Nefazodone mediated inhibition of CYP450 enzyme.	Depression [6A70-6A7Z]	[13]
Paroxetine	DM5PVQE	Major	Additive serotonergic effects by the combination of Eletriptan and Paroxetine.	Depression [6A70-6A7Z]	[14]
Vortioxetine	DM6F1PU	Major	Additive serotonergic effects by the combination of Eletriptan and Vortioxetine.	Depression [6A70-6A7Z]	[14]
Duloxetine	DM9BI7M	Major	Additive serotonergic effects by the combination of Eletriptan and Duloxetine.	Depression [6A70-6A7Z]	[14]
Isocarboxazid	DMAF1NB	Major	Additive serotonergic effects by the combination of Eletriptan and Isocarboxazid.	Depression [6A70-6A7Z]	[11]
Milnacipran	DMBFE74	Major	Additive serotonergic effects by the combination of Eletriptan and Milnacipran.	Depression [6A70-6A7Z]	[14]
Escitalopram	DMFK9HG	Major	Additive serotonergic effects by the combination of Eletriptan and Escitalopram.	Depression [6A70-6A7Z]	[14]
Tranylcypromine	DMGB5RE	Major	Additive serotonergic effects by the combination of Eletriptan and Tranylcypromine.	Depression [6A70-6A7Z]	[11]
Desvenlafaxine	DMHD4PE	Major	Additive serotonergic effects by the combination of Eletriptan and Desvenlafaxine.	Depression [6A70-6A7Z]	[14]
Phenelzine	DMHIDUE	Major	Additive serotonergic effects by the combination of Eletriptan and Phenelzine.	Depression [6A70-6A7Z]	[11]
Trazodone	DMK1GBJ	Major	Additive serotonergic effects by the combination of Eletriptan and Trazodone.	Depression [6A70-6A7Z]	[14]
Venlafaxine	DMR6QH0	Major	Additive serotonergic effects by the combination of Eletriptan and Venlafaxine.	Depression [6A70-6A7Z]	[14]
5-hydroxy-L-tryptophan	DMDWZGJ	Major	Additive serotonergic effects by the combination of Eletriptan and 5-hydroxy-L-tryptophan.	Discovery agent [N.A.]	[18]
Fenfluramine	DM0762O	Major	Additive serotonergic effects by the combination of Eletriptan and Fenfluramine.	Epilepsy/seizure [8A61-8A6Z]	[14]
Stiripentol	DMMSDOY	Moderate	Decreased metabolism of Eletriptan caused by Stiripentol mediated inhibition of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[13]
Rufinamide	DMWE60C	Moderate	Increased metabolism of Eletriptan caused by Rufinamide mediated induction of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[19]
Itraconazole	DMCR1MV	Major	Decreased metabolism of Eletriptan caused by Itraconazole mediated inhibition of CYP450 enzyme.	Fungal infection [1F29-1F2F]	[13]
Clotrimazole	DMMFCIH	Moderate	Decreased metabolism of Eletriptan caused by Clotrimazole mediated inhibition of CYP450 enzyme.	Fungal infection [1F29-1F2F]	[13]
Ketoconazole	DMPZI3Q	Major	Decreased metabolism of Eletriptan caused by Ketoconazole mediated inhibition of CYP450 enzyme.	Fungal infection [1F29-1F2F]	[13]
Cimetidine	DMH61ZB	Moderate	Decreased metabolism of Eletriptan caused by Cimetidine mediated inhibition of CYP450 enzyme.	Gastro-oesophageal reflux disease [DA22]	[13]
Boceprevir	DMBSHMF	Major	Decreased metabolism of Eletriptan caused by Boceprevir mediated inhibition of CYP450 enzyme.	Hepatitis virus infection [1E50-1E51]	[13]
Telaprevir	DMMRV29	Major	Decreased metabolism of Eletriptan caused by Telaprevir mediated inhibition of CYP450 enzyme.	Hepatitis virus infection [1E50-1E51]	[13]
Isoniazid	DM5JVS3	Moderate	Decreased metabolism of Eletriptan caused by Isoniazid mediated inhibition of CYP450 enzyme.	HIV-infected patients with tuberculosis [1B10-1B14]	[13]
Rifapentine	DMCHV4I	Moderate	Increased metabolism of Eletriptan caused by Rifapentine mediated induction of CYP450 enzyme.	HIV-infected patients with tuberculosis [1B10-1B14]	[20]
Procarbazine	DMIK367	Major	Additive serotonergic effects by the combination of Eletriptan and Procarbazine.	Hodgkin lymphoma [2B30]	[11]
Indinavir	DM0T3YH	Major	Decreased metabolism of Eletriptan caused by Indinavir mediated inhibition of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[13]
Delavirdine	DM3NF5G	Major	Decreased metabolism of Eletriptan caused by Delavirdine mediated inhibition of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[13]
Fosamprenavir	DM4W9B3	Major	Decreased metabolism of Eletriptan caused by Fosamprenavir mediated inhibition of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[13]
Nevirapine	DM6HX9B	Moderate	Increased metabolism of Eletriptan caused by Nevirapine mediated induction of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[21]
Cobicistat	DM6L4H2	Major	Decreased metabolism of Eletriptan caused by Cobicistat mediated inhibition of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[13]
Efavirenz	DMC0GSJ	Moderate	Increased metabolism of Eletriptan caused by Efavirenz mediated induction of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[22]
Saquinavir	DMG814N	Major	Decreased metabolism of Eletriptan caused by Saquinavir mediated inhibition of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[13]
Amprenavir	DMLMXE0	Major	Decreased metabolism of Eletriptan caused by Amprenavir mediated inhibition of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[13]
Darunavir	DMN3GCH	Moderate	Decreased metabolism of Eletriptan caused by Darunavir mediated inhibition of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[13]
Atazanavir	DMSYRBX	Major	Decreased metabolism of Eletriptan caused by Atazanavir mediated inhibition of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[13]
Ritonavir	DMU764S	Major	Decreased metabolism of Eletriptan caused by Ritonavir mediated inhibition of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[13]
BMS-201038	DMQTAGO	Moderate	Decreased metabolism of Eletriptan caused by BMS-201038 mediated inhibition of CYP450 enzyme.	Hyper-lipoproteinaemia [5C80]	[13]
Verapamil	DMA7PEW	Moderate	Decreased metabolism of Eletriptan caused by Verapamil mediated inhibition of CYP450 enzyme.	Hypertension [BA00-BA04]	[13]
Diltiazem	DMAI7ZV	Moderate	Decreased metabolism of Eletriptan caused by Diltiazem mediated inhibition of CYP450 enzyme.	Hypertension [BA00-BA04]	[13]
Berotralstat	DMWA2DZ	Moderate	Decreased metabolism of Eletriptan caused by Berotralstat mediated inhibition of CYP450 enzyme.	Innate/adaptive immunodeficiency [4A00]	[13]
Suvorexant	DM0E6S3	Moderate	Decreased metabolism of Eletriptan caused by Suvorexant mediated inhibition of CYP450 enzyme.	Insomnia [7A00-7A0Z]	[13]
Crizotinib	DM4F29C	Moderate	Decreased metabolism of Eletriptan caused by Crizotinib mediated inhibition of CYP450 enzyme.	Lung cancer [2C25]	[13]
Ceritinib	DMB920Z	Major	Decreased metabolism of Eletriptan caused by Ceritinib mediated inhibition of CYP450 enzyme.	Lung cancer [2C25]	[13]
PF-06463922	DMKM7EW	Moderate	Increased metabolism of Eletriptan caused by PF-06463922 mediated induction of CYP450 enzyme.	Lung cancer [2C25]	[23]
Selpercatinib	DMZR15V	Moderate	Decreased metabolism of Eletriptan caused by Selpercatinib mediated inhibition of CYP450 enzyme.	Lung cancer [2C25]	[13]
Idelalisib	DM602WT	Major	Decreased metabolism of Eletriptan caused by Idelalisib mediated inhibition of CYP450 enzyme.	Mature B-cell leukaemia [2A82]	[13]
IPI-145	DMWA24P	Moderate	Decreased metabolism of Eletriptan caused by IPI-145 mediated inhibition of CYP450 enzyme.	Mature B-cell leukaemia [2A82]	[13]
Danazol	DML8KTN	Moderate	Decreased metabolism of Eletriptan caused by Danazol mediated inhibition of CYP450 enzyme.	Menstrual cycle bleeding disorder [GA20]	[13]
Exjade	DMHPRWG	Moderate	Decreased metabolism of Eletriptan caused by Exjade mediated inhibition of CYP450 enzyme.	Mineral absorption/transport disorder [5C64]	[24]
Ozanimod	DMT6AM2	Major	Additive serotonergic effects by the combination of Eletriptan and Ozanimod.	Multiple sclerosis [8A40]	[25]
Fedratinib	DM4ZBK6	Moderate	Decreased metabolism of Eletriptan caused by Fedratinib mediated inhibition of CYP450 enzyme.	Myeloproliferative neoplasm [2A20]	[13]
Nilotinib	DM7HXWT	Moderate	Decreased metabolism of Eletriptan caused by Nilotinib mediated inhibition of CYP450 enzyme.	Myeloproliferative neoplasm [2A20]	[13]
Imatinib	DM7RJXL	Moderate	Decreased metabolism of Eletriptan caused by Imatinib mediated inhibition of CYP450 enzyme.	Myeloproliferative neoplasm [2A20]	[13]
Dasatinib	DMJV2EK	Moderate	Decreased metabolism of Eletriptan caused by Dasatinib mediated inhibition of CYP450 enzyme.	Myeloproliferative neoplasm [2A20]	[13]
Modafinil	DMYILBE	Minor	Increased metabolism of Eletriptan caused by Modafinil mediated induction of CYP450 enzyme.	Narcolepsy [7A20]	[26]
Palonosetron	DMBHMOX	Major	Additive serotonergic effects by the combination of Eletriptan and Palonosetron.	Nausea/vomiting [MD90]	[27]
Granisetron	DMIUW25	Major	Additive serotonergic effects by the combination of Eletriptan and Granisetron.	Nausea/vomiting [MD90]	[27]
Dolasetron	DMMG26Z	Major	Additive serotonergic effects by the combination of Eletriptan and Dolasetron.	Nausea/vomiting [MD90]	[27]
Ondansetron	DMOTQ1I	Major	Additive serotonergic effects by the combination of Eletriptan and Ondansetron.	Nausea/vomiting [MD90]	[27]
Entrectinib	DMMPTLH	Moderate	Decreased metabolism of Eletriptan caused by Entrectinib mediated inhibition of CYP450 enzyme.	Non-small cell lung cancer [2C25]	[13]
Sibutramine	DMFJTDI	Major	Additive serotonergic effects by the combination of Eletriptan and Sibutramine.	Obesity [5B80-5B81]	[11]
Lorcaserin	DMG6OYJ	Major	Additive serotonergic effects by the combination of Eletriptan and Lorcaserin.	Obesity [5B80-5B81]	[28]
Dexfenfluramine	DMJ7YDS	Major	Additive serotonergic effects by the combination of Eletriptan and Dexfenfluramine.	Obesity [5B80-5B81]	[14]
Levomethadyl Acetate	DM06HG5	Moderate	Additive CNS depression effects by the combination of Eletriptan and Levomethadyl Acetate.	Opioid use disorder [6C43]	[12]
Rucaparib	DM9PVX8	Moderate	Decreased metabolism of Eletriptan caused by Rucaparib mediated inhibition of CYP450 enzyme.	Ovarian cancer [2C73]	[13]
Oxymorphone	DM65AGJ	Moderate	Additive CNS depression effects by the combination of Eletriptan and Oxymorphone.	Pain [MG30-MG3Z]	[12]
Levorphanol	DMGS80V	Moderate	Additive CNS depression effects by the combination of Eletriptan and Levorphanol.	Pain [MG30-MG3Z]	[12]
Hydromorphone	DMHP21E	Moderate	Additive CNS depression effects by the combination of Eletriptan and Hydromorphone.	Pain [MG30-MG3Z]	[12]
Dezocine	DMJDB0Y	Moderate	Additive CNS depression effects by the combination of Eletriptan and Dezocine.	Pain [MG30-MG3Z]	[12]
Nalbuphine	DMOSQGU	Moderate	Additive CNS depression effects by the combination of Eletriptan and Nalbuphine.	Pain [MG30-MG3Z]	[12]
Buprenorphine	DMPRI8G	Moderate	Additive CNS depression effects by the combination of Eletriptan and Buprenorphine.	Pain [MG30-MG3Z]	[12]
Hydrocodone	DMQ2JO5	Moderate	Additive CNS depression effects by the combination of Eletriptan and Hydrocodone.	Pain [MG30-MG3Z]	[12]
Oxycodone	DMXLKHV	Moderate	Additive CNS depression effects by the combination of Eletriptan and Oxycodone.	Pain [MG30-MG3Z]	[12]
Abametapir	DM2RX0I	Moderate	Decreased metabolism of Eletriptan caused by Abametapir mediated inhibition of CYP450 enzyme.	Pediculosis [1G00]	[29]
Lefamulin	DME6G97	Moderate	Decreased metabolism of Eletriptan caused by Lefamulin mediated inhibition of CYP450 enzyme.	Pneumonia [CA40]	[30]
Lonafarnib	DMGM2Z6	Major	Decreased metabolism of Eletriptan caused by Lonafarnib mediated inhibition of CYP450 enzyme.	Premature ageing appearance [LD2B]	[13]
Bicalutamide	DMZMSPF	Moderate	Decreased metabolism of Eletriptan caused by Bicalutamide mediated inhibition of CYP450 enzyme.	Prostate cancer [2C82]	[13]
Temsirolimus	DMS104F	Moderate	Increased plasma concentrations of Eletriptan and Temsirolimus due to competitive inhibition of the same metabolic pathway.	Renal cell carcinoma [2C90]	[31]
Fentanyl	DM8WAHT	Major	Additive serotonergic effects by the combination of Eletriptan and Fentanyl.	Sensation disturbance [MB40]	[14]
Voxelotor	DMCS6M5	Moderate	Decreased metabolism of Eletriptan caused by Voxelotor mediated inhibition of CYP450 enzyme.	Sickle-cell disorder [3A51]	[13]
Telotristat ethyl	DMDIYFZ	Moderate	Increased metabolism of Eletriptan caused by Telotristat ethyl mediated induction of CYP450 enzyme.	Small intestine developmental anomaly [DA90]	[19]
Larotrectinib	DM26CQR	Moderate	Decreased metabolism of Eletriptan caused by Larotrectinib mediated inhibition of CYP450 enzyme.	Solid tumour/cancer [2A00-2F9Z]	[13]
Armodafinil	DMGB035	Minor	Increased metabolism of Eletriptan caused by Armodafinil mediated induction of CYP450 enzyme.	Solid tumour/cancer [2A00-2F9Z]	[26]
LEE011	DMMX75K	Moderate	Decreased metabolism of Eletriptan caused by LEE011 mediated inhibition of CYP450 enzyme.	Solid tumour/cancer [2A00-2F9Z]	[13]
Pitolisant	DM8RFNJ	Moderate	Increased metabolism of Eletriptan caused by Pitolisant mediated induction of CYP450 enzyme.	Somnolence [MG42]	[19]
Fostamatinib	DM6AUHV	Moderate	Decreased metabolism of Eletriptan caused by Fostamatinib mediated inhibition of CYP450 enzyme.	Thrombocytopenia [3B64]	[32]
Brilinta	DMBR01X	Moderate	Decreased metabolism of Eletriptan caused by Brilinta mediated inhibition of CYP450 enzyme.	Thrombosis [DB61-GB90]	[13]
Tizanidine	DMR2IQ4	Moderate	Additive CNS depression effects by the combination of Eletriptan and Tizanidine.	Tonus and reflex abnormality [MB47]	[33]
Sirolimus	DMGW1ID	Moderate	Increased plasma concentrations of Eletriptan and Sirolimus due to competitive inhibition of the same metabolic pathway.	Transplant rejection [NE84]	[31]
Tacrolimus	DMZ7XNQ	Moderate	Increased plasma concentrations of Eletriptan and Tacrolimus due to competitive inhibition of the same metabolic pathway.	Transplant rejection [NE84]	[31]
Amiodarone	DMUTEX3	Moderate	Decreased metabolism of Eletriptan caused by Amiodarone mediated inhibition of CYP450 enzyme.	Ventricular tachyarrhythmia [BC71]	[13]

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
Quinoline yellow WS	E00309	24671	Colorant
Sunset yellow FCF	E00255	17730	Colorant
Beta-D-lactose	E00099	6134	Diluent; Dry powder inhaler carrier; Lyophilization aid
Carmellose sodium	E00625	Not Available	Disintegrant
Eisenoxyd	E00585	56841934	Colorant
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
Silicon dioxide	E00670	Not Available	Anticaking agent; Opacifying agent; Viscosity-controlling agent
Soybean lecithin	E00637	Not Available	Other agent
Talc	E00520	16211421	Anticaking agent; Diluent; Glidant; lubricant
Titanium dioxide	E00322	26042	Coating agent; Colorant; Opacifying agent
Triacetin	E00080	5541	Humectant; Plasticizing agent; Solvent
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
Eletriptan 20 mg tablet	20 mg	Oral Tablet	Oral
Eletriptan 40 mg tablet	40 mg	Oral 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: 40).
• [2] BDDCS applied to over 900 drugs
• [3] Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
• [4] 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
• [5] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [6] Improving the prediction of the brain disposition for orally administered drugs using BDDCS. Adv Drug Deliv Rev. 2012 Jan;64(1):95-109.
• [7] Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
• [8] Eletriptan metabolism by human hepatic CYP450 enzymes and transport by human P-glycoprotein. Drug Metab Dispos. 2003 Jul;31(7):861-9.
• [9] Eletriptan in the management of acute migraine: an update on the evidence for efficacy, safety, and consistent response. Ther Adv Neurol Disord. 2016 Sep;9(5):414-23.
• [10] G protein beta3 polymorphism and triptan response in cluster headache. Clin Pharmacol Ther. 2007 Oct;82(4):396-401. doi: 10.1038/sj.clpt.6100159. Epub 2007 Mar 14.
• [11] Chan BSH, Graudins A, Whyte IM, Dawson AH, Braitberg G, Duggin GG "Serotonin syndrome resulting from drug interactions." Med J Aust 169 (1998): 523-5. [PMID: 9861909]
• [12] Vizcaychipi MP, Walker S, Palazzo M "Serotonin syndrome triggered by tramadol." Br J Anaesth 99 (2007): 919. [PMID: 18006535]
• [13] Product Information. Relpax (eletriptan). Pfizer U.S. Pharmaceuticals, New York, NY.
• [14] Achamallah NS "Visual hallucinations after combining fluoxetine and dextromethorphan ." Am J Psychiatry 149 (1992): 1406. [PMID: 1530079]
• [15] Product Information. Northera (droxidopa). Chelsea Therapeutics Inc, Charlotte, NC.
• [16] Bergeron L, Boule M, Perreault S "Serotonin toxicity associated with concomitant use of linezolid." Ann Pharmacother 39 (2005): 956-61. [PMID: 15827071]
• [17] He K, Woolf TF, Hollenberg PF "Mechanism-based inactivation of cytochrome P-450-3A4 by mifepristone (RU486)." J Pharmacol Exp Ther 288 (1999): 791-7. [PMID: 9918590]
• [18] Ciraulo DA, Shader RI "Fluoxetine drug-drug interactions: I. Antidepressants and antipsychotics." J Clin Psychopharmacol 10 (1990): 48-50. [PMID: 1968472]
• [19] Cerner Multum, Inc. "UK Summary of Product Characteristics.".
• [20] Product Information. Priftin (rifapentine). Hoechst Marion-Roussel Inc, Kansas City, MO.
• [21] Cerner Multum, Inc. "Australian Product Information.".
• [22] Product Information. Sustiva (efavirenz). DuPont Pharmaceuticals, Wilmington, DE.
• [23] Product Information. Lorbrena (lorlatinib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
• [24] Product Information. Exjade (deferasirox). Novartis Pharmaceuticals, East Hanover, NJ.
• [25] Alvine G, Black DW, Tsuang D "Case of delirium secondary to phenelzine/L-tryptophan combination." J Clin Psychiatry 51 (1990): 311. [PMID: 2365671]
• [26] Doherty MM, Charman WN "The mucosa of the small intestine: how clinically relevant as an organ of drug metabolism?" Clin Pharmacokinet 41 (2002): 235-53. [PMID: 11978143]
• [27] Canadian Pharmacists Association.
• [28] Product Information. Belviq (lorcaserin). Eisai Inc, Teaneck, NJ.
• [29] Product Information. Xeglyze (abametapir topical). Dr. Reddy's Laboratories Inc, Upper Saddle River, NJ.
• [30] Product Information. Xenleta (lefamulin). Nabriva Therapeutics US, Inc., King of Prussia, PA.
• [31] Product Information. Prograf (tacrolimus). Fujisawa, Deerfield, IL.
• [32] Product Information. Tavalisse (fostamatinib). Rigel Pharmaceuticals, South San Francisco, CA.
• [33] Product Information. Zanaflex (tizanidine). Acorda Therapeutics, Hawthorne, NY.