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Identification
NameAlfentanil
Accession NumberDB00802  (APRD00726)
TypeSmall Molecule
GroupsApproved, Illicit
Description

A short-acting opioid anesthetic and analgesic derivative of fentanyl. It produces an early peak analgesic effect and fast recovery of consciousness. Alfentanil is effective as an anesthetic during surgery, for supplementation of analgesia during surgical procedures, and as an analgesic for critically ill patients. [PubChem]

Structure
Thumb
Synonyms
Alfentanilum
Alfentanyl
N-(1-(2-(4-Ethyl-5-oxo-2-tetrazolin-1-yl)ethyl)-4-(methoxymethyl)-4-piperidyl)propionanilide
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Alfenta Inj 500mcg/mlsolution500 mcgintravenousJanssen Inc1988-12-312008-09-05Canada
Alfentanilinjection500 ug/mLintravenousAkorn, Inc.2013-07-19Not applicableUs
Alfentanil Hydrochlorideinjection500 ug/mLintravenousAkorn, Inc.2010-02-01Not applicableUs
Alfentanil Injection USPsolution500 mcgintravenousSandoz Canada Incorporated2004-11-01Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Alfentanil Hydrochlorideinjection, solution500 ug/mLintravenousHospira, Inc.1999-10-28Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
RapifenJanssen
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Alfentanil hydrochloride
ThumbNot applicableDBSALT001202
Categories
UNII1N74HM2BS7
CAS number71195-58-9
WeightAverage: 416.5172
Monoisotopic: 416.25358892
Chemical FormulaC21H32N6O3
InChI KeyInChIKey=IDBPHNDTYPBSNI-UHFFFAOYSA-N
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
IUPAC Name
N-{1-[2-(4-ethyl-5-oxo-4,5-dihydro-1H-1,2,3,4-tetrazol-1-yl)ethyl]-4-(methoxymethyl)piperidin-4-yl}-N-phenylpropanamide
SMILES
CCN1N=NN(CCN2CCC(COC)(CC2)N(C(=O)CC)C2=CC=CC=C2)C1=O
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as anilides. These are organic heterocyclic compounds derived from oxoacids RkE(=O)l(OH)m (l not 0) by replacing an OH group by the NHPh group or derivative formed by ring substitution.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassAnilides
Direct ParentAnilides
Alternative Parents
Substituents
  • Anilide
  • 4-aminopiperidine
  • Piperidine
  • Heteroaromatic compound
  • Tetrazole
  • Tertiary carboxylic acid amide
  • Azole
  • Tertiary aliphatic amine
  • Tertiary amine
  • Carboxamide group
  • Azacycle
  • Organoheterocyclic compound
  • Ether
  • Dialkyl ether
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External Descriptors
Pharmacology
IndicationFor the management of postoperative pain and the maintenance of general anesthesia.
PharmacodynamicsAlfentanil is a synthetic opioid analgesic. Alfentanil interacts predominately with the opioid mu-receptor. These mu-binding sites are discretely distributed in the human brain, spinal cord, and other tissues. In clinical settings, alfentanil exerts its principal pharmacologic effects on the central nervous system. Its primary actions of therapeutic value are analgesia and sedation. Alfentanil may increase the patient's tolerance for pain and decrease the perception of suffering, although the presence of the pain itself may still be recognized. In addition to analgesia, alterations in mood, euphoria and dysphoria, and drowsiness commonly occur. Alfentanil depresses the respiratory centers, depresses the cough reflex, and constricts the pupils.
Mechanism of actionOpiate receptors are coupled with G-protein receptors and function as both positive and negative regulators of synaptic transmission via G-proteins that activate effector proteins. Binding of the opiate stimulates the exchange of GTP for GDP on the G-protein complex. As the effector system is adenylate cyclase and cAMP located at the inner surface of the plasma membrane, opioids decrease intracellular cAMP by inhibiting adenylate cyclase. Subsequently, the release of nociceptive neurotransmitters such as substance P, GABA, dopamine, acetylcholine and noradrenaline is inhibited. Opioids also inhibit the release of vasopressin, somatostatin, insulin and glucagon. Alfentanil's analgesic activity is, most likely, due to its conversion to morphine. Opioids close N-type voltage-operated calcium channels (OP2-receptor agonist) and open calcium-dependent inwardly rectifying potassium channels (OP3 and OP1 receptor agonist). This results in hyperpolarization and reduced neuronal excitability.
Related Articles
AbsorptionFor intravenous injection or infusion only.
Volume of distribution
  • 0.4 to 1 L/kg
Protein binding92%
Metabolism

The liver is the major site of biotransformation.

SubstrateEnzymesProduct
Alfentanil
AMXDetails
Alfentanil
noralfentanilDetails
Route of eliminationOnly 1.0% of the dose is excreted as unchanged drug; urinary excretion is the major route of elimination of metabolites.
Half life90-111 minutes
Clearance
  • 5 mL/kg/min
ToxicitySymptoms of overexposure include characteristic rigidity of the skeletal muscles, cardiac and respiratory depression, and narrowing of the pupils.
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Alfentanil Action PathwayDrug actionSMP00413
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9957
Blood Brain Barrier+0.9396
Caco-2 permeable-0.5368
P-glycoprotein substrateSubstrate0.7156
P-glycoprotein inhibitor IInhibitor0.8809
P-glycoprotein inhibitor IINon-inhibitor0.8381
Renal organic cation transporterNon-inhibitor0.7077
CYP450 2C9 substrateNon-substrate0.7897
CYP450 2D6 substrateNon-substrate0.9115
CYP450 3A4 substrateSubstrate0.7407
CYP450 1A2 substrateNon-inhibitor0.9067
CYP450 2C9 inhibitorInhibitor0.6051
CYP450 2D6 inhibitorNon-inhibitor0.9003
CYP450 2C19 inhibitorNon-inhibitor0.5591
CYP450 3A4 inhibitorInhibitor0.6691
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.6692
Ames testAMES toxic0.5858
CarcinogenicityNon-carcinogens0.7729
BiodegradationNot ready biodegradable0.9877
Rat acute toxicity2.9997 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Strong inhibitor0.6413
hERG inhibition (predictor II)Inhibitor0.5893
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Akorn inc
  • Hospira inc
Packagers
Dosage forms
FormRouteStrength
Injectionintravenous500 ug/mL
Injection, solutionintravenous500 ug/mL
Solutionintravenous500 mcg
Prices
Unit descriptionCostUnit
Alfenta 500 mcg/ml ampul5.26USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point140.8Janssens, F.; US. Patent 4,167,574; September 11, 1979; assigned to Janssen Pharmaceutica NV.
water solubility34.6 mg/LNot Available
logP2.16HANSCH,C ET AL. (1995)
Predicted Properties
PropertyValueSource
Water Solubility0.252 mg/mLALOGPS
logP2.2ALOGPS
logP2.81ChemAxon
logS-3.2ALOGPS
pKa (Strongest Basic)7.5ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area81.05 Å2ChemAxon
Rotatable Bond Count9ChemAxon
Refractivity118.59 m3·mol-1ChemAxon
Polarizability45.57 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
References
Synthesis Reference

Jacob Mathew, J. Killgore, “New methods for the synthesis of alfentanil, sufentanil, and remifentanil.” U.S. Patent US20060149071, issued July 06, 2006.

US20060149071
General ReferencesNot Available
External Links
ATC CodesN01AH02
AHFS Codes
  • 28:08.08
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (51.3 KB)
Interactions
Drug Interactions
Drug
AcepromazineAcepromazine may increase the hypotensive activities of Alfentanil.
AcetazolamideThe risk or severity of adverse effects can be increased when Alfentanil is combined with Acetazolamide.
AlvimopanThe risk or severity of adverse effects can be increased when Alfentanil is combined with Alvimopan.
AmilorideThe risk or severity of adverse effects can be increased when Alfentanil is combined with Amiloride.
Ammonium chlorideAmmonium chloride may increase the excretion rate of Alfentanil which could result in a higher serum level.
AmphetamineAmphetamine may increase the analgesic activities of Alfentanil.
AprepitantThe serum concentration of Alfentanil can be increased when it is combined with Aprepitant.
AzelastineAlfentanil may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
BaclofenThe risk or severity of adverse effects can be increased when Baclofen is combined with Alfentanil.
BendroflumethiazideThe risk or severity of adverse effects can be increased when Alfentanil is combined with Bendroflumethiazide.
BepridilAlfentanil may increase the bradycardic activities of Bepridil.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Alfentanil.
BumetanideThe risk or severity of adverse effects can be increased when Alfentanil is combined with Bumetanide.
ButorphanolButorphanol may decrease the analgesic activities of Alfentanil.
CathinoneCathinone may increase the analgesic activities of Alfentanil.
ChlorothiazideThe risk or severity of adverse effects can be increased when Alfentanil is combined with Chlorothiazide.
ChlorthalidoneThe risk or severity of adverse effects can be increased when Alfentanil is combined with Chlorthalidone.
CimetidineThe serum concentration of Alfentanil can be increased when it is combined with Cimetidine.
ClarithromycinThe serum concentration of Alfentanil can be increased when it is combined with Clarithromycin.
ConivaptanThe serum concentration of Alfentanil can be increased when it is combined with Conivaptan.
CrizotinibThe serum concentration of Alfentanil can be increased when it is combined with Crizotinib.
CyclothiazideThe risk or severity of adverse effects can be increased when Alfentanil is combined with Cyclothiazide.
DasatinibThe serum concentration of Alfentanil can be increased when it is combined with Dasatinib.
DesmopressinThe risk or severity of adverse effects can be increased when Alfentanil is combined with Desmopressin.
DiazepamDiazepam may increase the central nervous system depressant (CNS depressant) activities of Alfentanil.
DiltiazemThe serum concentration of Alfentanil can be increased when it is combined with Diltiazem.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Alfentanil.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Alfentanil.
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Alfentanil.
EluxadolineAlfentanil may increase the activities of Eluxadoline.
EnzalutamideThe serum concentration of Alfentanil can be decreased when it is combined with Enzalutamide.
ErythromycinThe serum concentration of Alfentanil can be increased when it is combined with Erythromycin.
Etacrynic acidThe risk or severity of adverse effects can be increased when Alfentanil is combined with Ethacrynic acid.
EthanolAlfentanil may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
EthoxzolamideThe risk or severity of adverse effects can be increased when Alfentanil is combined with Ethoxzolamide.
FluconazoleThe metabolism of Alfentanil can be decreased when combined with Fluconazole.
FosaprepitantThe serum concentration of Alfentanil can be increased when it is combined with Fosaprepitant.
FurosemideThe risk or severity of adverse effects can be increased when Alfentanil is combined with Furosemide.
Fusidic AcidThe serum concentration of Alfentanil can be increased when it is combined with Fusidic Acid.
HydrochlorothiazideThe risk or severity of adverse effects can be increased when Alfentanil is combined with Hydrochlorothiazide.
HydrocodoneAlfentanil may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
HydroflumethiazideThe risk or severity of adverse effects can be increased when Alfentanil is combined with Hydroflumethiazide.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Alfentanil.
IdelalisibThe serum concentration of Alfentanil can be increased when it is combined with Idelalisib.
IndapamideThe risk or severity of adverse effects can be increased when Alfentanil is combined with Indapamide.
IvacaftorThe serum concentration of Alfentanil can be increased when it is combined with Ivacaftor.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Alfentanil.
LuliconazoleThe serum concentration of Alfentanil can be increased when it is combined with Luliconazole.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Alfentanil.
MethotrimeprazineAlfentanil may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
MetolazoneThe risk or severity of adverse effects can be increased when Alfentanil is combined with Metolazone.
MetyrosineAlfentanil may increase the sedative activities of Metyrosine.
MifepristoneThe serum concentration of Alfentanil can be increased when it is combined with Mifepristone.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Alfentanil.
MirtazapineAlfentanil may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Alfentanil.
NadololAlfentanil may increase the bradycardic activities of Nadolol.
NaltrexoneThe therapeutic efficacy of Alfentanil can be decreased when used in combination with Naltrexone.
NelfinavirThe metabolism of Alfentanil can be decreased when combined with Nelfinavir.
NetupitantThe serum concentration of Alfentanil can be increased when it is combined with Netupitant.
OrphenadrineAlfentanil may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
PalbociclibThe serum concentration of Alfentanil can be increased when it is combined with Palbociclib.
ParaldehydeAlfentanil may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParoxetineAlfentanil may increase the serotonergic activities of Paroxetine.
PegvisomantThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Alfentanil.
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Alfentanil.
PhenelzineAlfentanil may increase the serotonergic activities of Phenelzine.
PramipexoleAlfentanil may increase the sedative activities of Pramipexole.
ProcyclidineThe risk or severity of adverse effects can be increased when Procyclidine is combined with Alfentanil.
PropofolThe risk or severity of adverse effects can be increased when Alfentanil is combined with Propofol.
RamosetronAlfentanil may increase the activities of Ramosetron.
RifabutinThe serum concentration of Alfentanil can be decreased when it is combined with Rifabutin.
RifampicinThe serum concentration of Alfentanil can be decreased when it is combined with Rifampicin.
RifapentineThe serum concentration of Alfentanil can be decreased when it is combined with Rifapentine.
RitonavirThe serum concentration of Alfentanil can be increased when it is combined with Ritonavir.
RopiniroleAlfentanil may increase the sedative activities of Ropinirole.
RotigotineAlfentanil may increase the sedative activities of Rotigotine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Alfentanil.
SimeprevirThe serum concentration of Alfentanil can be increased when it is combined with Simeprevir.
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Alfentanil.
SpironolactoneThe risk or severity of adverse effects can be increased when Alfentanil is combined with Spironolactone.
StiripentolThe serum concentration of Alfentanil can be increased when it is combined with Stiripentol.
SuccinylcholineSuccinylcholine may increase the bradycardic activities of Alfentanil.
SuvorexantAlfentanil may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Alfentanil.
TelithromycinThe serum concentration of Alfentanil can be increased when it is combined with Telithromycin.
ThalidomideAlfentanil may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
TicrynafenThe risk or severity of adverse effects can be increased when Alfentanil is combined with Ticrynafen.
TorasemideThe risk or severity of adverse effects can be increased when Alfentanil is combined with Torasemide.
TranylcypromineAlfentanil may increase the serotonergic activities of Tranylcypromine.
TriamtereneThe risk or severity of adverse effects can be increased when Alfentanil is combined with Triamterene.
TrichlormethiazideThe risk or severity of adverse effects can be increased when Alfentanil is combined with Trichlormethiazide.
ZolpidemAlfentanil may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Voltage-gated calcium channel activity
Specific Function:
Receptor for endogenous opioids such as beta-endorphin and endomorphin. Receptor for natural and synthetic opioids including morphine, heroin, DAMGO, fentanyl, etorphine, buprenorphin and methadone. Agonist binding to the receptor induces coupling to an inactive GDP-bound heterotrimeric G-protein complex and subsequent exchange of GDP for GTP in the G-protein alpha subunit leading to dissociati...
Gene Name:
OPRM1
Uniprot ID:
P35372
Molecular Weight:
44778.855 Da
References
  1. Garrido M, Gubbens-Stibbe J, Tukker E, Cox E, von Frijtag J, Kunzel D, IJzerman A, Danhof M, van der Graaf PH: Pharmacokinetic-pharmacodynamic analysis of the EEG effect of alfentanil in rats following beta-funaltrexamine-induced mu-opioid receptor "knockdown" in vivo. Pharm Res. 2000 Jun;17(6):653-9. [PubMed:10955836 ]
  2. Lotsch J, Geisslinger G: Are mu-opioid receptor polymorphisms important for clinical opioid therapy? Trends Mol Med. 2005 Feb;11(2):82-9. [PubMed:15694871 ]
  3. Oertel BG, Schmidt R, Schneider A, Geisslinger G, Lotsch J: The mu-opioid receptor gene polymorphism 118A>G depletes alfentanil-induced analgesia and protects against respiratory depression in homozygous carriers. Pharmacogenet Genomics. 2006 Sep;16(9):625-36. [PubMed:16906017 ]
  4. Leung A, Wallace MS, Ridgeway B, Yaksh T: 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. [PubMed:11240090 ]
  5. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  2. Klees TM, Sheffels P, Dale O, Kharasch ED: Metabolism of alfentanil by cytochrome p4503a (cyp3a) enzymes. Drug Metab Dispos. 2005 Mar;33(3):303-11. Epub 2004 Nov 22. [PubMed:15557344 ]
  3. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxygen binding
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A5
Uniprot ID:
P20815
Molecular Weight:
57108.065 Da
References
  1. Kharasch ED, Walker A, Isoherranen N, Hoffer C, Sheffels P, Thummel K, Whittington D, Ensign D: 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. Epub 2007 Jun 6. [PubMed:17554244 ]
  2. Klees TM, Sheffels P, Dale O, Kharasch ED: Metabolism of alfentanil by cytochrome p4503a (cyp3a) enzymes. Drug Metab Dispos. 2005 Mar;33(3):303-11. Epub 2004 Nov 22. [PubMed:15557344 ]
  3. Klees TM, Sheffels P, Thummel KE, Kharasch ED: Pharmacogenetic determinants of human liver microsomal alfentanil metabolism and the role of cytochrome P450 3A5. Anesthesiology. 2005 Mar;102(3):550-6. [PubMed:15731592 ]
  4. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  5. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxygen binding
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A7
Uniprot ID:
P24462
Molecular Weight:
57525.03 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]

Carriers

Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Not Available
Specific Function:
Functions as transport protein in the blood stream. Binds various ligands in the interior of its beta-barrel domain. Also binds synthetic drugs and influences their distribution and availability in the body. Appears to function in modulating the activity of the immune system during the acute-phase reaction.
Gene Name:
ORM1
Uniprot ID:
P02763
Molecular Weight:
23511.38 Da
References
  1. Belpaire FM, Bogaert MG: Binding of alfentanil to human alpha 1-acid glycoprotein, albumin and serum. Int J Clin Pharmacol Ther Toxicol. 1991 Mar;29(3):96-102. [PubMed:2071261 ]
  2. Kumar K, Crankshaw DP, Morgan DJ, Beemer GH: The effect of cardiopulmonary bypass on plasma protein binding of alfentanil. Eur J Clin Pharmacol. 1988;35(1):47-52. [PubMed:3146505 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Toxic substance binding
Specific Function:
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloidal osmotic pressure of blood. Major zinc transporter in plasma, typically binds about 80% of all plasma zinc.
Gene Name:
ALB
Uniprot ID:
P02768
Molecular Weight:
69365.94 Da
References
  1. Belpaire FM, Bogaert MG: Binding of alfentanil to human alpha 1-acid glycoprotein, albumin and serum. Int J Clin Pharmacol Ther Toxicol. 1991 Mar;29(3):96-102. [PubMed:2071261 ]
  2. Kumar K, Crankshaw DP, Morgan DJ, Beemer GH: The effect of cardiopulmonary bypass on plasma protein binding of alfentanil. Eur J Clin Pharmacol. 1988;35(1):47-52. [PubMed:3146505 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Molecular Weight:
141477.255 Da
References
  1. Wandel C, Kim R, Wood M, Wood A: Interaction of morphine, fentanyl, sufentanil, alfentanil, and loperamide with the efflux drug transporter P-glycoprotein. Anesthesiology. 2002 Apr;96(4):913-20. [PubMed:11964599 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23