Identification

Name
Alfentanil
Accession Number
DB00802  (APRD00726)
Type
Small Molecule
Groups
Approved, 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
  • Alfentanilo
  • Alfentanilum
  • Alfentanyl
  • N-(1-(2-(4-Ethyl-5-oxo-2-tetrazolin-1-yl)ethyl)-4-(methoxymethyl)-4-piperidyl)propionanilide
External IDs
IDS-NA-014
Product Ingredients
IngredientUNIICASInChI Key
Alfentanil hydrochloride11S92G0TIW70879-28-6YYESXRRYBUERKF-UHFFFAOYSA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
AlfentaInjection500 ug/1mLIntravenousTaylor Pharmaceuticals2008-02-25Not applicableUs
Alfenta Inj 500mcg/mlSolution500 mcgIntravenousJanssen Pharmaceuticals1988-12-312008-09-05Canada
AlfentanilInjection500 ug/1mLIntravenousAkorn2013-07-19Not applicableUs
Alfentanil HydrochlorideInjection500 ug/1mLIntravenousAkorn2010-02-01Not applicableUs
Alfentanil Injection USPSolution500 mcgIntravenousSandoz Canada Incorporated2004-11-01Not applicableCanada
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Alfentanil HydrochlorideInjection, solution500 ug/1mLIntravenousHospira, Inc.2005-08-30Not applicableUs
International/Other Brands
Rapifen (Janssen)
Categories
UNII
1N74HM2BS7
CAS number
71195-58-9
Weight
Average: 416.5172
Monoisotopic: 416.25358892
Chemical Formula
C21H32N6O3
InChI Key
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

Pharmacology

Indication

For the management of postoperative pain and the maintenance of general anesthesia.

Associated Therapies
Pharmacodynamics

Alfentanil 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 action

Opiate 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.

TargetActionsOrganism
AMu-type opioid receptor
agonist
Human
Absorption

For intravenous injection or infusion only.

Volume of distribution
  • 0.4 to 1 L/kg
Protein binding

92%

Metabolism

The liver is the major site of biotransformation.

Route of elimination

Only 1.0% of the dose is excreted as unchanged drug; urinary excretion is the major route of elimination of metabolites.

Half life

90-111 minutes

Clearance
  • 5 mL/kg/min
Toxicity

Symptoms 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
PathwayCategory
Alfentanil Action PathwayDrug action
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
(R)-warfarinThe metabolism of Alfentanil can be decreased when combined with (R)-warfarin.
(S)-WarfarinThe metabolism of Alfentanil can be decreased when combined with (S)-Warfarin.
2,5-Dimethoxy-4-ethylamphetamineThe risk or severity of serotonin syndrome can be increased when Alfentanil is combined with 2,5-Dimethoxy-4-ethylamphetamine.
2,5-Dimethoxy-4-ethylthioamphetamineThe risk or severity of serotonin syndrome can be increased when Alfentanil is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
3,4-MethylenedioxyamphetamineThe risk or severity of serotonin syndrome can be increased when Alfentanil is combined with 3,4-Methylenedioxyamphetamine.
3,5-diiodothyropropionic acidThe metabolism of Alfentanil can be decreased when combined with 3,5-diiodothyropropionic acid.
4-Bromo-2,5-dimethoxyamphetamineThe risk or severity of serotonin syndrome can be increased when Alfentanil is combined with 4-Bromo-2,5-dimethoxyamphetamine.
4-hydroxycoumarinThe metabolism of 4-hydroxycoumarin can be decreased when combined with Alfentanil.
4-MethoxyamphetamineThe risk or severity of adverse effects can be increased when Alfentanil is combined with 4-Methoxyamphetamine.
5-androstenedioneThe metabolism of Alfentanil can be decreased when combined with 5-androstenedione.
Food Interactions
Not 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 References
Not Available
External Links
Human Metabolome Database
HMDB0014940
KEGG Compound
C08005
PubChem Compound
51263
PubChem Substance
46505618
ChemSpider
46451
BindingDB
83450
ChEBI
2569
ChEMBL
CHEMBL634
Therapeutic Targets Database
DAP001134
PharmGKB
PA448084
RxList
RxList Drug Page
Wikipedia
Alfentanil
ATC Codes
N01AH02 — Alfentanil
AHFS Codes
  • 28:08.08 — Opiate Agonists
MSDS
Download (51.3 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
3CompletedTreatmentBronchoscopy / Sedation, Conscious1
3CompletedTreatmentChild Comfort / Intensive Care Units / Morphine / Pediatric1
4CompletedNot AvailableDigestive System Diseases / Disorientation1
4CompletedPreventionAnesthesia Intubation Complications1
4CompletedPreventionEmergence Agitation1
4CompletedPreventionLower Esophageal Sphincter1
4CompletedTreatmentHypoxemia1
4CompletedTreatmentLung Cancers1
4CompletedTreatmentFunctional disorders of the biliary tract / Pancreatic Diseases1
4CompletedTreatmentProcedural Sedation1
4CompletedTreatmentSedation therapy2
4RecruitingTreatmentBlood Pressures / Electroconvulsive Therapy1
Not AvailableCompletedNot AvailablePain NOS1
Not AvailableCompletedBasic ScienceHyperalgesia1
Not AvailableCompletedBasic SciencePain Measurement1
Not AvailableCompletedDiagnosticAnaesthesia therapy / Pain NOS1
Not AvailableCompletedOtherAirway Response1
Not AvailableCompletedPreventionIschemia, Cerebral1
Not AvailableCompletedPreventionPost-Operative Nausea and Vomiting (PONV)1
Not AvailableCompletedSupportive CareMalignancies1
Not AvailableCompletedTreatmentAdverse Effect of Other General Anesthetics1
Not AvailableCompletedTreatmentCalcium Nephrolithiasis1
Not AvailableCompletedTreatmentChronic Lung Diseases1
Not AvailableCompletedTreatmentColonoscopy1
Not AvailableRecruitingNot AvailableAcute Bacterial Exacerbation of Chronic Bronchitis (ABECB) / Acute Bacterial Sinusitis (ABS) / Acute Decompensated Heart Failure (ADHF) / Acute Pyelonephritis / Adenovirus / Adjunct to general anesthesia therapy / Adrenal Insufficiency / Airway Swelling / Anaesthesia therapy / Anxiolysis / Arterial Hypotension / Autism, Early Infantile / Autistic Disorder / Bartonellosis / Benzodiazepine Withdrawal / Benzodiazepines / Bipolar Disorder (BD) / Bloodstream Infections / Bone and Joint Infections / Brain Swelling / Bronchospasm / Brucellosis / Cardiac Arrest / Central Nervous System Infections / Cholera / Chronic Bacterial Prostatitis / Community Acquired Pneumonia (CAP) / Complicated Urinary Tract Infections / Convulsions / Cytomegalovirus Retinitis / Drug hypersensitivity reaction / Early-onset Schizophrenia Spectrum Disorders / Edema / Epilepsies / Feeling Anxious / Flu caused by Influenza / Gastroparesis / Gynaecological infection / Headaches / Herpes Simplex Virus / High Blood Pressure (Hypertension) / High Cholesterol / Hospital-acquired bacterial pneumonia / Hyperlipidemias / Infantile Hemangiomas / Infection NOS / Inflammatory Conditions / Inflammatory Reaction / Influenza Treatment or Prophylaxis / Inhalational Anthrax (Post-Exposure) / Intra-Abdominal Infections / Life-threatening Fungal Infections / Lower Respiratory Tract Infection (LRTI) / Meningitis, Bacterial / Migraines / Muscle Spasms / Nausea / Opioid Addiction / Pain NOS / Plague / Pneumonia / Prophylaxis / Psittacosis / Q Fever / Reflux / Relapsing Fever / Rocky Mountain Spotted Fever / Schizophrenic Disorders / Sedation therapy / Seizures / Sepsis / Skeletal Muscle Spasms / Skin and Subcutaneous Tissue Bacterial Infections / Skin Structures and Soft Tissue Infections / Stable Angina (SA) / Thromboprophylaxis / Thrombotic events / Toxic effect of hydrocyanic acid and cyanides / Trachoma / Treatment-resistant Schizophrenia / Tularemia / Typhus Fever / Uncomplicated Skin and Skin Structure Infections / Uncomplicated Urinary Tract Infections / Urinary Tract Infections (UTIs) / Vomiting / Withdrawal1
Not AvailableUnknown StatusSupportive CareAdjunct to general anesthesia therapy1
Not AvailableUnknown StatusTreatmentChronic Lung Diseases1

Pharmacoeconomics

Manufacturers
  • Akorn inc
  • Hospira inc
Packagers
  • Akorn Inc.
  • Baxter International Inc.
  • Hospira Inc.
  • Taylor Pharmaceuticals
Dosage forms
FormRouteStrength
InjectionIntravenous500 ug/1mL
Injection, solutionIntravenous500 ug/1mL
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.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)140.8Janssens, 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 RuleNoChemAxon
MDDR-like RuleYesChemAxon
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)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-014i-0000900000-a802cc961dad7c6326a5
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-014i-0395300000-498fafc6962b6fd82e9c
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-00kb-0912000000-43c2343a5fa4997ca93a
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-015a-2900000000-16b845b2c742175e38cd
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-015a-7900000000-e9bd243460dd40507619

Taxonomy

Description
This 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.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Benzene and substituted derivatives
Sub Class
Anilides
Direct Parent
Anilides
Alternative Parents
Piperidines / Tetrazoles / Tertiary carboxylic acid amides / Heteroaromatic compounds / Trialkylamines / Amino acids and derivatives / Dialkyl ethers / Azacyclic compounds / Organopnictogen compounds / Organic oxides
show 2 more
Substituents
Anilide / Piperidine / Azole / Heteroaromatic compound / Tertiary carboxylic acid amide / Tetrazole / Amino acid or derivatives / Carboxamide group / Tertiary amine / Tertiary aliphatic amine
show 15 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
piperidines, monocarboxylic acid amide (CHEBI:2569)

Targets

Details
1. Mu-type opioid receptor
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...
Gene Name
OPRM1
Uniprot ID
P35372
Uniprot Name
Mu-type opioid receptor
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 react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
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 un...
Gene Name
CYP3A7
Uniprot ID
P24462
Uniprot Name
Cytochrome P450 3A7
Molecular Weight
57525.03 Da
References
  1. 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 un...
Gene Name
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
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]

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...
Gene Name
ORM1
Uniprot ID
P02763
Uniprot Name
Alpha-1-acid glycoprotein 1
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 colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
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
Uniprot Name
Multidrug resistance protein 1
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]

Drug created on June 13, 2005 07:24 / Updated on December 12, 2018 07:09