Details of the Drug

General Information of Drug (ID: DMVO0UB)

• Drug Name: Alfentanil
• Synonyms: Alfenta; Alfentanilum; Alfentanyl; Alfenta (TN); Alfentanil (INN); Alfentanil [INN:BAN]; Alfentanilum [INN-Latin]; Rapifen (TN); N-[1-[2-(4-Ethyl-5-oxo-2-tetrazolin-1-yl)ethyl]-4-(methoxymethyl)-4-piperidyl]propionanilide; N-[1-[2-(4-ethyl-5-oxotetrazol-1-yl)ethyl]-4-(methoxymethyl)piperidin-4-yl]-N-phenylpropanamide; N-(1-(2-(4-Ethyl-4,5-dihydro-5-oxotetrazolyl)ethyl)-4-(methoxymethyl)-4-piperidyl)propionanilid; N-(1-(2-(4-Ethyl-5-oxo-2-tetrazolin-1-yl)ethyl)-4-(methoxymethyl)-4-piperidyl)propionanilide; N-(1-(2-(4-Ethyl-4,5-dihydro-5-oxotetrazolyl)ethyl)-4-(methoxymethyl)-4-piperidyl)-N-phenylpropionamid; N-{1-[2-(4-ethyl-5-oxo-4,5-dihydro-1H-tetrazol-1-yl)ethyl]-4-(methoxymethyl)piperidin-4-yl}-N-phenylpropanamide; N-{1-[2-(4-ethyl-5-oxo-4,5-dihydro-1H-tetrazol-1-yl)ethyl]-4-[(methyloxy)methyl]piperidin-4-yl}-N-phenylpropanamide

Indication

Disease Entry	ICD 11	Status	REF
Anaesthesia	9A78.6	Approved	[1]

• Therapeutic Class: Anesthetics
• Affected Organisms: Humans and other mammals
• ATC Code:
  N01AH02: Alfentanil
  N01AH: Opioid anesthetics
  N01A: ANESTHETICS, GENERAL
  N01: ANESTHETICS
  N: NERVOUS SYSTEM
• Drug Type: Small molecular drug
• #Ro5 Violations (Lipinski): 0:
  Molecular Weight (mw); 416.5
  Logarithm of the Partition Coefficient (xlogp); 2.2
  Rotatable Bond Count (rotbonds); 9
  Hydrogen Bond Donor Count (hbonddonor); 0
  Hydrogen Bond Acceptor Count (hbondacc); 6
• ADMET Property:
  Absorption: The drug is only absorbed by intravenous injection or infusion []
  BDDCS Class: Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 1: high solubility and high permeability [2]
  Clearance: The clearance of drug is 5 mL/min/kg []
  Elimination: 0.5% 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 90 - 111 minutes [3]
  Metabolism: The drug is metabolized via the liver []
  MRTD: The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 0.5882 micromolar/kg/day [4]
  Unbound Fraction: The unbound fraction of drug in plasma is 0.086% [3]
  Vd: The volume of distribution (Vd) of drug is 0.4-1 L/kg []
• Chemical Identifiers:
  Formula: C21H32N6O3
  IUPAC Name: N-[1-[2-(4-ethyl-5-oxotetrazol-1-yl)ethyl]-4-(methoxymethyl)piperidin-4-yl]-N-phenylpropanamide
  Canonical SMILES: CCC(=O)N(C1=CC=CC=C1)C2(CCN(CC2)CCN3C(=O)N(N=N3)CC)COC
  InChI: InChI=1S/C21H32N6O3/c1-4-19(28)27(18-9-7-6-8-10-18)21(17-30-3)11-13-24(14-12-21)15-16-26-20(29)25(5-2)22-23-26/h6-10H,4-5,11-17H2,1-3H3
  InChIKey: IDBPHNDTYPBSNI-UHFFFAOYSA-N
• Cross-matching ID:
  PubChem CID: 51263
  ChEBI ID: CHEBI:2569
  CAS Number: 71195-58-9
  UNII: 1N74HM2BS7
  DrugBank ID: DB00802
  TTD ID: D0G5QB
  VARIDT ID: DR00617
  INTEDE ID: DR0061

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Opioid receptor mu (MOP)	TTKWM86	OPRM_HUMAN	Agonist	[5]

Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
Cytochrome P450 3A4 (CYP3A4)	DE4LYSA	CP3A4_HUMAN	Substrate	[6]
Cytochrome P450 3A5 (CYP3A5)	DEIBDNY	CP3A5_HUMAN	Substrate	[7]
Cytochrome P450 3A7 (CYP3A7)	DERD86B	CP3A7_HUMAN	Substrate	[8]

Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
5-hydroxytryptamine receptor 3A (HTR3A)	OTAIV1AK	5HT3A_HUMAN	Gene/Protein Processing	[9]

Molecular Expression Atlas of This Drug

• The Studied Disease: Anaesthesia
• ICD Disease Classification: 9A78.6

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Opioid receptor mu (MOP)	DTT	OPRM1	5.94E-01	-0.02	-0.17
Cytochrome P450 3A5 (CYP3A5)	DME	CYP3A5	5.09E-02	-5.62E-02	-5.19E-01
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	6.06E-01	-2.42E-02	-1.64E-01

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Same Disease as Alfentanil

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Disease	REF
Atracurium	DM42HXN	Moderate	Increased risk of bradycardia by the combination of Alfentanil and Atracurium.	Corneal disease [9A76-9A78]	[10]
Mivacurium	DM473VD	Moderate	Additive hypotensive effects by the combination of Alfentanil and Mivacurium.	Corneal disease [9A76-9A78]	[10]
Levobupivacaine	DM783CH	Minor	Decreased metabolism of Alfentanil caused by Levobupivacaine mediated inhibition of CYP450 enzyme.	Corneal disease [9A76-9A78]	[11]
Pancuronium	DMB0VY8	Moderate	Additive hypotensive effects by the combination of Alfentanil and Pancuronium.	Corneal disease [9A76-9A78]	[10]
Propofol	DMB4OLE	Moderate	Additive cardiorespiratory depression effects by the combination of Alfentanil and Propofol.	Corneal disease [9A76-9A78]	[12]
Tubocurarine	DMBZIVP	Moderate	Increased risk of bradycardia by the combination of Alfentanil and Tubocurarine.	Corneal disease [9A76-9A78]	[10]

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

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Metreleptin	DM1NOEK	Moderate	Increased metabolism of Alfentanil caused by Metreleptin mediated induction of CYP450 enzyme.	Acute diabete complication [5A2Y]	[11]
Ivosidenib	DM8S6T7	Moderate	Increased metabolism of Alfentanil caused by Ivosidenib mediated induction of CYP450 enzyme.	Acute myeloid leukaemia [2A60]	[11]
Arn-509	DMT81LZ	Moderate	Increased metabolism of Alfentanil caused by Arn-509 mediated induction of CYP450 enzyme.	Acute myeloid leukaemia [2A60]	[11]
Dronedarone	DMA8FS5	Major	Decreased metabolism of Alfentanil caused by Dronedarone mediated inhibition of CYP450 enzyme.	Angina pectoris [BA40]	[13]
Methylphenobarbital	DMDSWAG	Major	Additive CNS depression effects by the combination of Alfentanil and Methylphenobarbital.	Anxiety disorder [6B00-6B0Z]	[14]
Chlormezanone	DMTWUXR	Major	Additive CNS depression effects by the combination of Alfentanil and Chlormezanone.	Anxiety disorder [6B00-6B0Z]	[15]
Oxazepam	DMXNZM4	Major	Additive CNS depression effects by the combination of Alfentanil and Oxazepam.	Anxiety disorder [6B00-6B0Z]	[15]
Posaconazole	DMUL5EW	Major	Decreased metabolism of Alfentanil caused by Posaconazole mediated inhibition of CYP450 enzyme.	Aspergillosis [1F20]	[13]
Desipramine	DMT2FDC	Moderate	Additive CNS depression effects by the combination of Alfentanil and Desipramine.	Attention deficit hyperactivity disorder [6A05]	[16]
Dalfopristin	DM4LTKV	Major	Decreased metabolism of Alfentanil caused by Dalfopristin mediated inhibition of CYP450 enzyme.	Bacterial infection [1A00-1C4Z]	[10]
Troleandomycin	DMUZNIG	Major	Decreased metabolism of Alfentanil caused by Troleandomycin mediated inhibition of CYP450 enzyme.	Bacterial infection [1A00-1C4Z]	[13]
Telithromycin	DMZ4P3A	Major	Decreased metabolism of Alfentanil caused by Telithromycin mediated inhibition of CYP450 enzyme.	Bacterial infection [1A00-1C4Z]	[13]
Cariprazine	DMJYDVK	Major	Additive CNS depression effects by the combination of Alfentanil and Cariprazine.	Bipolar disorder [6A60]	[15]
Erdafitinib	DMI782S	Moderate	Increased metabolism of Alfentanil caused by Erdafitinib mediated induction of CYP450 enzyme.	Bladder cancer [2C94]	[17]
Lapatinib	DM3BH1Y	Moderate	Decreased metabolism of Alfentanil caused by Lapatinib mediated inhibition of CYP450 enzyme.	Breast cancer [2C60-2C6Y]	[13]
Tucatinib	DMBESUA	Major	Decreased metabolism of Alfentanil caused by Tucatinib mediated inhibition of CYP450 enzyme.	Breast cancer [2C60-2C6Y]	[13]
Palbociclib	DMD7L94	Moderate	Decreased metabolism of Alfentanil caused by Palbociclib mediated inhibition of CYP450 enzyme.	Breast cancer [2C60-2C6Y]	[13]
Phenylbutazone	DMAYL0T	Moderate	Increased metabolism of Alfentanil caused by Phenylbutazone mediated induction of CYP450 enzyme.	Chronic pain [MG30]	[11]
Levomilnacipran	DMV26S8	Major	Additive serotonergic effects by the combination of Alfentanil and Levomilnacipran.	Chronic pain [MG30]	[18]
Mifepristone	DMGZQEF	Major	Decreased metabolism of Alfentanil caused by Mifepristone mediated inhibition of CYP450 enzyme.	Cushing syndrome [5A70]	[13]
Osilodrostat	DMIJC9X	Moderate	Decreased metabolism of Alfentanil caused by Osilodrostat mediated inhibition of CYP450 enzyme.	Cushing syndrome [5A70]	[13]
Ivacaftor	DMZC1HS	Moderate	Decreased metabolism of Alfentanil caused by Ivacaftor mediated inhibition of CYP450 enzyme.	Cystic fibrosis [CA25]	[13]
Ethanol	DMDRQZU	Moderate	Additive CNS depression effects by the combination of Alfentanil and Ethanol.	Cystitis [GC00]	[19]
MK-8228	DMOB58Q	Major	Decreased metabolism of Alfentanil caused by MK-8228 mediated inhibition of CYP450 enzyme.	Cytomegaloviral disease [1D82]	[13]
Sertraline	DM0FB1J	Major	Additive serotonergic effects by the combination of Alfentanil and Sertraline.	Depression [6A70-6A7Z]	[18]
Cyclobenzaprine	DM1YBRM	Major	Additive CNS depression effects by the combination of Alfentanil and Cyclobenzaprine.	Depression [6A70-6A7Z]	[20]
Vilazodone	DM4LECQ	Major	Additive serotonergic effects by the combination of Alfentanil and Vilazodone.	Depression [6A70-6A7Z]	[18]
Nefazodone	DM4ZS8M	Major	Decreased metabolism of Alfentanil caused by Nefazodone mediated inhibition of CYP450 enzyme.	Depression [6A70-6A7Z]	[13]
Vortioxetine	DM6F1PU	Major	Additive serotonergic effects by the combination of Alfentanil and Vortioxetine.	Depression [6A70-6A7Z]	[18]
Milnacipran	DMBFE74	Major	Additive serotonergic effects by the combination of Alfentanil and Milnacipran.	Depression [6A70-6A7Z]	[18]
Desvenlafaxine	DMHD4PE	Major	Additive serotonergic effects by the combination of Alfentanil and Desvenlafaxine.	Depression [6A70-6A7Z]	[18]
OPC-34712	DMHG57U	Major	Additive CNS depression effects by the combination of Alfentanil and OPC-34712.	Depression [6A70-6A7Z]	[15]
Clomipramine	DMINRKW	Moderate	Additive CNS depression effects by the combination of Alfentanil and Clomipramine.	Depression [6A70-6A7Z]	[16]
Doxepin	DMPI98T	Moderate	Additive serotonergic effects by the combination of Alfentanil and Doxepin.	Depression [6A70-6A7Z]	[16]
Maprotiline	DMPWB7T	Moderate	Additive CNS depression effects by the combination of Alfentanil and Maprotiline.	Depression [6A70-6A7Z]	[16]
Esketamine	DMVU687	Moderate	Additive CNS depression effects by the combination of Alfentanil and Esketamine.	Depression [6A70-6A7Z]	[21]
Mepenzolate	DM8YU2F	Moderate	Additive antimotility effects by the combination of Alfentanil and Mepenzolate.	Digestive system disease [DE2Z]	[22]
Oxybutynine	DMJPBAX	Moderate	Additive antimotility effects by the combination of Alfentanil and Oxybutynine.	Discovery agent [N.A.]	[22]
Diazepam	DM08E9O	Major	Additive CNS depression effects by the combination of Alfentanil and Diazepam.	Epilepsy/seizure [8A61-8A6Z]	[20]
Gabapentin	DM6T924	Major	Additive CNS depression effects by the combination of Alfentanil and Gabapentin.	Epilepsy/seizure [8A61-8A6Z]	[23]
Cenobamate	DM8KLU9	Moderate	Increased metabolism of Alfentanil caused by Cenobamate mediated induction of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[11]
Stiripentol	DMMSDOY	Major	Decreased metabolism of Alfentanil caused by Stiripentol mediated inhibition of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[13]
Fosphenytoin	DMOX3LB	Moderate	Increased metabolism of Alfentanil caused by Fosphenytoin mediated induction of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[11]
Clonazepam	DMTO13J	Major	Additive CNS depression effects by the combination of Alfentanil and Clonazepam.	Epilepsy/seizure [8A61-8A6Z]	[15]
Rufinamide	DMWE60C	Moderate	Increased metabolism of Alfentanil caused by Rufinamide mediated induction of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[11]
Phenobarbital	DMXZOCG	Major	Additive CNS depression effects by the combination of Alfentanil and Phenobarbital.	Epilepsy/seizure [8A61-8A6Z]	[15]
Eslicarbazepine	DMZREFQ	Moderate	Increased metabolism of Alfentanil caused by Eslicarbazepine mediated induction of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[11]
Dantrolene	DM1D8XY	Major	Additive CNS depression effects by the combination of Alfentanil and Dantrolene.	Fever [MG26]	[15]
Tazemetostat	DMWP1BH	Moderate	Increased metabolism of Alfentanil caused by Tazemetostat mediated induction of CYP450 enzyme.	Follicular lymphoma [2A80]	[11]
Solifenacin	DMG592Q	Moderate	Additive antimotility effects by the combination of Alfentanil and Solifenacin.	Functional bladder disorder [GC50]	[22]
Tolterodine	DMSHPW8	Moderate	Additive antimotility effects by the combination of Alfentanil and Tolterodine.	Functional bladder disorder [GC50]	[22]
Itraconazole	DMCR1MV	Major	Decreased metabolism of Alfentanil caused by Itraconazole mediated inhibition of CYP450 enzyme.	Fungal infection [1F29-1F2F]	[13]
Ketoconazole	DMPZI3Q	Major	Decreased metabolism of Alfentanil caused by Ketoconazole mediated inhibition of CYP450 enzyme.	Fungal infection [1F29-1F2F]	[13]
Sulfinpyrazone	DMEV954	Moderate	Increased metabolism of Alfentanil caused by Sulfinpyrazone mediated induction of CYP450 enzyme.	Gout [FA25]	[11]
Boceprevir	DMBSHMF	Major	Decreased metabolism of Alfentanil caused by Boceprevir mediated inhibition of CYP450 enzyme.	Hepatitis virus infection [1E50-1E51]	[13]
Telaprevir	DMMRV29	Major	Decreased metabolism of Alfentanil caused by Telaprevir mediated inhibition of CYP450 enzyme.	Hepatitis virus infection [1E50-1E51]	[13]
Isoniazid	DM5JVS3	Moderate	Decreased metabolism of Alfentanil caused by Isoniazid mediated inhibition of CYP450 enzyme.	HIV-infected patients with tuberculosis [1B10-1B14]	[13]
Rifampin	DMA8J1G	Moderate	Increased metabolism of Alfentanil caused by Rifampin mediated induction of CYP450 enzyme.	HIV-infected patients with tuberculosis [1B10-1B14]	[11]
Fosamprenavir	DM4W9B3	Major	Decreased metabolism of Alfentanil caused by Fosamprenavir mediated inhibition of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[13]
Cobicistat	DM6L4H2	Major	Decreased metabolism of Alfentanil caused by Cobicistat mediated inhibition of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[13]
Saquinavir	DMG814N	Major	Decreased metabolism of Alfentanil caused by Saquinavir mediated inhibition of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[13]
Etravirine	DMGV8QU	Moderate	Increased metabolism of Alfentanil caused by Etravirine mediated induction of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[11]
Darunavir	DMN3GCH	Major	Decreased metabolism of Alfentanil caused by Darunavir mediated inhibition of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[13]
Atazanavir	DMSYRBX	Major	Decreased metabolism of Alfentanil caused by Atazanavir mediated inhibition of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[13]
BMS-201038	DMQTAGO	Moderate	Decreased metabolism of Alfentanil caused by BMS-201038 mediated inhibition of CYP450 enzyme.	Hyper-lipoproteinaemia [5C80]	[13]
Conivaptan	DM1V329	Major	Decreased metabolism of Alfentanil caused by Conivaptan mediated inhibition of CYP450 enzyme.	Hypo-osmolality/hyponatraemia [5C72]	[13]
Lesinurad	DMUR64T	Moderate	Increased metabolism of Alfentanil caused by Lesinurad mediated induction of CYP450 enzyme.	Inborn purine/pyrimidine/nucleotide metabolism error [5C55]	[24]
Belladonna	DM2RBWK	Moderate	Additive CNS depression effects by the combination of Alfentanil and Belladonna.	Infectious gastroenteritis/colitis [1A40]	[22]
Suvorexant	DM0E6S3	Major	Additive CNS depression effects by the combination of Alfentanil and Suvorexant.	Insomnia [7A00-7A0Z]	[15]
Amobarbital	DM0GQ8N	Major	Additive CNS depression effects by the combination of Alfentanil and Amobarbital.	Insomnia [7A00-7A0Z]	[15]
Zaleplon	DMGFWSM	Major	Additive CNS depression effects by the combination of Alfentanil and Zaleplon.	Insomnia [7A00-7A0Z]	[15]
Tasimelteon	DMLOQ1V	Major	Additive CNS depression effects by the combination of Alfentanil and Tasimelteon.	Insomnia [7A00-7A0Z]	[15]
Paraldehyde	DMOC1BX	Major	Additive CNS depression effects by the combination of Alfentanil and Paraldehyde.	Insomnia [7A00-7A0Z]	[15]
ITI-007	DMUQ1DO	Major	Additive CNS depression effects by the combination of Alfentanil and ITI-007.	Insomnia [7A00-7A0Z]	[15]
Quazepam	DMY4D87	Major	Additive CNS depression effects by the combination of Alfentanil and Quazepam.	Insomnia [7A00-7A0Z]	[15]
Estazolam	DMZGXUM	Major	Additive CNS depression effects by the combination of Alfentanil and Estazolam.	Insomnia [7A00-7A0Z]	[15]
Polyethylene glycol	DM4I1JP	Moderate	Increased risk of lowers seizure threshold by the combination of Alfentanil and Polyethylene glycol.	Irritable bowel syndrome [DD91]	[25]
Dicyclomine	DMZSDGX	Moderate	Additive CNS depression effects by the combination of Alfentanil and Dicyclomine.	Irritable bowel syndrome [DD91]	[22]
Remimazolam	DMLVSYX	Major	Additive CNS depression effects by the combination of Alfentanil and Remimazolam.	Labour/delivery anaesthesia complication [JB0C]	[15]
Glycerol phenylbutyrate	DMDGRQO	Moderate	Increased metabolism of Alfentanil caused by Glycerol phenylbutyrate mediated induction of CYP450 enzyme.	Liver disease [DB90-DB9Z]	[26]
Crizotinib	DM4F29C	Major	Decreased metabolism of Alfentanil caused by Crizotinib mediated inhibition of CYP450 enzyme.	Lung cancer [2C25]	[13]
Brigatinib	DM7W94S	Moderate	Increased metabolism of Alfentanil caused by Brigatinib mediated induction of CYP450 enzyme.	Lung cancer [2C25]	[11]
Ceritinib	DMB920Z	Major	Decreased metabolism of Alfentanil caused by Ceritinib mediated inhibition of CYP450 enzyme.	Lung cancer [2C25]	[13]
PF-06463922	DMKM7EW	Moderate	Increased metabolism of Alfentanil caused by PF-06463922 mediated induction of CYP450 enzyme.	Lung cancer [2C25]	[27]
Osimertinib	DMRJLAT	Moderate	Decreased metabolism of Alfentanil caused by Osimertinib mediated inhibition of CYP450 enzyme.	Lung cancer [2C25]	[26]
Selpercatinib	DMZR15V	Moderate	Decreased metabolism of Alfentanil caused by Selpercatinib mediated inhibition of CYP450 enzyme.	Lung cancer [2C25]	[13]
Idelalisib	DM602WT	Major	Decreased metabolism of Alfentanil caused by Idelalisib mediated inhibition of CYP450 enzyme.	Mature B-cell leukaemia [2A82]	[13]
IPI-145	DMWA24P	Major	Decreased metabolism of Alfentanil caused by IPI-145 mediated inhibition of CYP450 enzyme.	Mature B-cell leukaemia [2A82]	[13]
Blinatumomab	DMGECIJ	Moderate	Decreased metabolism of Alfentanil caused by Blinatumomab mediated inhibition of CYP450 enzyme.	Mature B-cell lymphoma [2A85]	[28]
Vemurafenib	DM62UG5	Moderate	Increased metabolism of Alfentanil caused by Vemurafenib mediated induction of CYP450 enzyme.	Melanoma [2C30]	[11]
LGX818	DMNQXV8	Moderate	Increased metabolism of Alfentanil caused by LGX818 mediated induction of CYP450 enzyme.	Melanoma [2C30]	[29]
Dabrafenib	DMX6OE3	Moderate	Increased metabolism of Alfentanil caused by Dabrafenib mediated induction of CYP450 enzyme.	Melanoma [2C30]	[26]
Danazol	DML8KTN	Moderate	Decreased metabolism of Alfentanil caused by Danazol mediated inhibition of CYP450 enzyme.	Menstrual cycle bleeding disorder [GA20]	[13]
Allopregnanolone	DMNLHAC	Moderate	Additive CNS depression effects by the combination of Alfentanil and Allopregnanolone.	Mental/behavioural/neurodevelopmental disorder [6E20-6E8Z]	[30]
Exjade	DMHPRWG	Moderate	Increased metabolism of Alfentanil caused by Exjade mediated induction of CYP450 enzyme.	Mineral absorption/transport disorder [5C64]	[11]
Flibanserin	DM70DTN	Moderate	Additive CNS depression effects by the combination of Alfentanil and Flibanserin.	Mood disorder [6A60-6E23]	[31]
Thalidomide	DM70BU5	Moderate	Additive CNS depression effects by the combination of Alfentanil and Thalidomide.	Multiple myeloma [2A83]	[32]
Fedratinib	DM4ZBK6	Major	Decreased metabolism of Alfentanil caused by Fedratinib mediated inhibition of CYP450 enzyme.	Myeloproliferative neoplasm [2A20]	[13]
Nilotinib	DM7HXWT	Moderate	Decreased metabolism of Alfentanil caused by Nilotinib mediated inhibition of CYP450 enzyme.	Myeloproliferative neoplasm [2A20]	[13]
Dasatinib	DMJV2EK	Moderate	Decreased metabolism of Alfentanil caused by Dasatinib mediated inhibition of CYP450 enzyme.	Myeloproliferative neoplasm [2A20]	[13]
Prasugrel	DM7MT6E	Moderate	Altered absorption of Alfentanil due to GI dynamics variation caused by Prasugrel.	Myocardial infarction [BA41-BA43]	[33]
Metoclopramide	DMFA5MY	Moderate	Additive antimotility effects by the combination of Alfentanil and Metoclopramide.	Nausea/vomiting [MD90]	[34]
Ondansetron	DMOTQ1I	Major	Additive serotonergic effects by the combination of Alfentanil and Ondansetron.	Nausea/vomiting [MD90]	[35]
Bupropion	DM5PCS7	Major	Increased risk of lowers seizure threshold by the combination of Alfentanil and Bupropion.	Nicotine use disorder [6C4A]	[36]
Entrectinib	DMMPTLH	Moderate	Decreased metabolism of Alfentanil 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 Alfentanil and Sibutramine.	Obesity [5B80-5B81]	[37]
Lorcaserin	DMG6OYJ	Major	Additive serotonergic effects by the combination of Alfentanil and Lorcaserin.	Obesity [5B80-5B81]	[38]
Dexfenfluramine	DMJ7YDS	Major	Additive serotonergic effects by the combination of Alfentanil and Dexfenfluramine.	Obesity [5B80-5B81]	[18]
Apraclonidine	DMO4PVE	Moderate	Additive CNS depression effects by the combination of Alfentanil and Apraclonidine.	Optic nerve disorder [9C40]	[39]
Olaparib	DM8QB1D	Moderate	Decreased metabolism of Alfentanil caused by Olaparib mediated inhibition of CYP450 enzyme.	Ovarian cancer [2C73]	[21]
Rucaparib	DM9PVX8	Moderate	Decreased metabolism of Alfentanil caused by Rucaparib mediated inhibition of CYP450 enzyme.	Ovarian cancer [2C73]	[13]
Flavoxate	DMKV4NL	Moderate	Additive antimotility effects by the combination of Alfentanil and Flavoxate.	Pain [MG30-MG3Z]	[22]
Biperiden	DME78OA	Moderate	Additive CNS depression effects by the combination of Alfentanil and Biperiden.	Parkinsonism [8A00]	[40]
Pimavanserin	DMR7IVC	Major	Additive CNS depression effects by the combination of Alfentanil and Pimavanserin.	Parkinsonism [8A00]	[15]
Orphenadrine	DMW542E	Major	Additive CNS depression effects by the combination of Alfentanil and Orphenadrine.	Parkinsonism [8A00]	[15]
Abametapir	DM2RX0I	Moderate	Decreased metabolism of Alfentanil caused by Abametapir mediated inhibition of CYP450 enzyme.	Pediculosis [1G00]	[41]
Methylscopolamine	DM5VWOB	Moderate	Additive antimotility effects by the combination of Alfentanil and Methylscopolamine.	Peptic ulcer [DA61]	[22]
Lefamulin	DME6G97	Moderate	Decreased metabolism of Alfentanil caused by Lefamulin mediated inhibition of CYP450 enzyme.	Pneumonia [CA40]	[42]
Lonafarnib	DMGM2Z6	Major	Decreased metabolism of Alfentanil caused by Lonafarnib mediated inhibition of CYP450 enzyme.	Premature ageing appearance [LD2B]	[13]
Enzalutamide	DMGL19D	Moderate	Increased metabolism of Alfentanil caused by Enzalutamide mediated induction of CYP450 enzyme.	Prostate cancer [2C82]	[11]
Bicalutamide	DMZMSPF	Moderate	Decreased metabolism of Alfentanil caused by Bicalutamide mediated inhibition of CYP450 enzyme.	Prostate cancer [2C82]	[13]
Temsirolimus	DMS104F	Moderate	Increased plasma concentrations of Alfentanil and Temsirolimus due to competitive inhibition of the same metabolic pathway.	Renal cell carcinoma [2C90]	[43]
Dexamethasone	DMMWZET	Moderate	Increased metabolism of Alfentanil caused by Dexamethasone mediated induction of CYP450 enzyme.	Rheumatoid arthritis [FA20]	[11]
Quetiapine	DM1N62C	Major	Additive CNS depression effects by the combination of Alfentanil and Quetiapine.	Schizophrenia [6A20]	[44]
Mesoridazine	DM2ZGAN	Major	Additive CNS depression effects by the combination of Alfentanil and Mesoridazine.	Schizophrenia [6A20]	[44]
Aripiprazole	DM3NUMH	Major	Additive CNS depression effects by the combination of Alfentanil and Aripiprazole.	Schizophrenia [6A20]	[15]
Iloperidone	DM6AUFY	Major	Additive CNS depression effects by the combination of Alfentanil and Iloperidone.	Schizophrenia [6A20]	[15]
Paliperidone	DM7NPJS	Major	Additive CNS depression effects by the combination of Alfentanil and Paliperidone.	Schizophrenia [6A20]	[15]
Perphenazine	DMA4MRX	Major	Additive CNS depression effects by the combination of Alfentanil and Perphenazine.	Schizophrenia [6A20]	[15]
Molindone	DMAH70G	Major	Additive CNS depression effects by the combination of Alfentanil and Molindone.	Schizophrenia [6A20]	[15]
Thiothixene	DMDINC4	Major	Additive CNS depression effects by the combination of Alfentanil and Thiothixene.	Schizophrenia [6A20]	[44]
Trifluoperazine	DMKBYWI	Major	Additive CNS depression effects by the combination of Alfentanil and Trifluoperazine.	Schizophrenia [6A20]	[15]
Pimozide	DMW83TP	Major	Additive CNS depression effects by the combination of Alfentanil and Pimozide.	Schizophrenia [6A20]	[15]
Mepivacaine	DMH2NMY	Minor	Decreased metabolism of Alfentanil caused by Mepivacaine mediated inhibition of CYP450 enzyme.	Sensation disturbance [MB40]	[11]
Voxelotor	DMCS6M5	Moderate	Decreased metabolism of Alfentanil caused by Voxelotor mediated inhibition of CYP450 enzyme.	Sickle-cell disorder [3A51]	[13]
Telotristat ethyl	DMDIYFZ	Moderate	Increased metabolism of Alfentanil caused by Telotristat ethyl mediated induction of CYP450 enzyme.	Small intestine developmental anomaly [DA90]	[26]
Larotrectinib	DM26CQR	Moderate	Decreased metabolism of Alfentanil caused by Larotrectinib mediated inhibition of CYP450 enzyme.	Solid tumour/cancer [2A00-2F9Z]	[13]
Armodafinil	DMGB035	Minor	Increased metabolism of Alfentanil caused by Armodafinil mediated induction of CYP450 enzyme.	Solid tumour/cancer [2A00-2F9Z]	[45]
LEE011	DMMX75K	Moderate	Decreased metabolism of Alfentanil caused by LEE011 mediated inhibition of CYP450 enzyme.	Solid tumour/cancer [2A00-2F9Z]	[13]
Fostamatinib	DM6AUHV	Moderate	Decreased metabolism of Alfentanil caused by Fostamatinib mediated inhibition of CYP450 enzyme.	Thrombocytopenia [3B64]	[46]
Brilinta	DMBR01X	Moderate	Decreased metabolism of Alfentanil caused by Brilinta mediated inhibition of CYP450 enzyme.	Thrombosis [DB61-GB90]	[26]
Pipecuronium	DM5F84A	Moderate	Additive hypotensive effects by the combination of Alfentanil and Pipecuronium.	Tonus and reflex abnormality [MB47]	[10]
Vecuronium	DMP0UK2	Moderate	Increased risk of bradycardia by the combination of Alfentanil and Vecuronium.	Tonus and reflex abnormality [MB47]	[10]
Sirolimus	DMGW1ID	Moderate	Increased plasma concentrations of Alfentanil and Sirolimus due to competitive inhibition of the same metabolic pathway.	Transplant rejection [NE84]	[43]
Elagolix	DMB2C0E	Moderate	Increased metabolism of Alfentanil caused by Elagolix mediated induction of CYP450 enzyme.	Uterine fibroid [2E86]	[11]
Amiodarone	DMUTEX3	Moderate	Decreased metabolism of Alfentanil caused by Amiodarone mediated inhibition of CYP450 enzyme.	Ventricular tachyarrhythmia [BC71]	[13]

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: 7108).
• [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] Concentration-effect relationship of intravenous alfentanil and ketamine on peripheral neurosensory thresholds, allodynia and hyperalgesia of neuropathic pain. Pain. 2001 Mar;91(1-2):177-87.
• [6] Pharmacogenetic determinants of human liver microsomal alfentanil metabolism and the role of cytochrome P450 3A5. Anesthesiology. 2005 Mar;102(3):550-6.
• [7] Influence of CYP3A5 genotype on the pharmacokinetics and pharmacodynamics of the cytochrome P4503A probes alfentanil and midazolam. Clin Pharmacol Ther. 2007 Oct;82(4):410-26.
• [8] Drug Interactions Flockhart Table
• [9] The effects of fentanyl-like opioids and hydromorphone on human 5-HT3A receptors. Anesth Analg. 2008 Jul;107(1):107-12. doi: 10.1213/ane.0b013e31817342c2.
• [10] Product Information. Alfenta (alfentanil). Janssen Pharmaceutica, Titusville, NJ.
• [11] Kharasch ED, Thummel KE "Human alfentanil metabolism by cytochrome P450 3A3/4. An explanation for the interindividual variability in alfentanil clearance?" Anesth Analg 76 (1993): 1033-9. [PMID: 8484504]
• [12] Gill SS, Wright EM, Reilly CS "Pharmacokinetic interaction of propofol and fentanyl: single bolus injection study." Br J Anaesth 65 (1990): 760-5. [PMID: 2265045]
• [13] Bartkowski RR, Goldberg ME, Larijani GE, Boerner T "Inhibition of alfentanil metabolism by erythromycin." Clin Pharmacol Ther 46 (1989): 99-102. [PMID: 2501060]
• [14] US Food and Drug Administration "FDA warns about serious risks and death when combining opioid pain or cough medicines with benzodiazepines requires its strongest warning.".
• [15] US Food and Drug Administration "FDA warns about serious risks and death when combining opioid pain or cough medicines with benzodiazepines requires its strongest warning.".
• [16] Vizcaychipi MP, Walker S, Palazzo M "Serotonin syndrome triggered by tramadol." Br J Anaesth 99 (2007): 919. [PMID: 18006535]
• [17] Product Information. Balversa (erdafitinib). Janssen Products, LP, Horsham, PA.
• [18] Achamallah NS "Visual hallucinations after combining fluoxetine and dextromethorphan ." Am J Psychiatry 149 (1992): 1406. [PMID: 1530079]
• [19] Sturner WQ, Garriott JC "Deaths involving propoxyphene: a study of 41 cases over a two-year period." JAMA 223 (1973): 1125-30. [PMID: 4739371]
• [20] Gilman AG, Rall TW, Nies AS, Taylor P, eds. "Goodman and Gilman's the Pharmacological Basis of Therapeutics. 8th ed." New York, NY: Pergamon Press Inc. (1990):.
• [21] Cerner Multum, Inc. "Australian Product Information.".
• [22] Product Information. Apadaz (acetaminophen-benzhydrocodone). KemPharm, Inc, Coralville, IA.
• [23] Eckhardt K, Ammon S, Hofmann U, Riebe A, Gugeler N, Mikus G "Gabapentin enhances the analgesic effect of morphine in healthy volunteers." Anesth Analg 91 (2000): 185-91. [PMID: 10866910]
• [24] Product Information. Zurampic (lesinurad). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
• [25] Product Information. Suprep Bowel Prep Kit (magnesium/potassium/sodium sulfates). Braintree Laboratories, Braintree, MA.
• [26] Cerner Multum, Inc. "UK Summary of Product Characteristics.".
• [27] Product Information. Lorbrena (lorlatinib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
• [28] Product Information. Blincyto (blinatumomab). Amgen USA, Thousand Oaks, CA.
• [29] Product Information. Braftovi (encorafenib). Array BioPharma Inc., Boulder, CO.
• [30] Product Information. Zulresso (brexanolone). Sage Therapeutics, Inc., Cambridge, MA.
• [31] Product Information. Addyi (flibanserin). Sprout Pharmaceuticals, Raleigh, NC.
• [32] Product Information. Thalomid (thalidomide). Celgene Corporation, Warren, NJ.
• [33] Agencia Espaola de Medicamentos y Productos Sanitarios Healthcare "Centro de informacion online de medicamentos de la AEMPS - CIMA.".
• [34] Product Information. Reglan (metoclopramide). Wyeth-Ayerst Laboratories, Philadelphia, PA.
• [35] Canadian Pharmacists Association.
• [36] Product Information. Wellbutrin XL (buPROPion). GlaxoSmithKline, Philadelphia, PA.
• [37] 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]
• [38] Product Information. Belviq (lorcaserin). Eisai Inc, Teaneck, NJ.
• [39] Product Information. Alphagan (brimonidine ophthalmic). Allergan Inc, Irvine, CA.
• [40] Product Information. Artane (trihexyphenidyl). Lederle Laboratories, Wayne, NJ.
• [41] Product Information. Xeglyze (abametapir topical). Dr. Reddy's Laboratories Inc, Upper Saddle River, NJ.
• [42] Product Information. Xenleta (lefamulin). Nabriva Therapeutics US, Inc., King of Prussia, PA.
• [43] Product Information. Prograf (tacrolimus). Fujisawa, Deerfield, IL.
• [44] Cerner Multum, Inc. "Canadian Product Information.".
• [45] 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]
• [46] Product Information. Tavalisse (fostamatinib). Rigel Pharmaceuticals, South San Francisco, CA.