Rx00010 - Alfentanil


Name:
Alfentanil
Rx ID:
Rx00010
Validation Level:
Reference ID:
DB00802
Primary Indications:
Anesthesia
Orphan Indications:
HIV-associated neuropathy; postherpetic neuralgia
Rare Indications:
No annotated rare indications.
Common Indications:
No annotated common indications.
Drug Interactions:
Alvimopan; Cimetidine; Erythromycin; Fluconazole; Itraconazole; Ketoconazole; Rifampicin; Telithromycin; Tranylcypromine; Triprolidine; ...
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Food Interactions:
No annotated food interactions in DrugBank.

Interactive 3D Model

Interactive Drug Target Network

Interactive Bipartite Drug Repurposing Graph

Rx00010
Primary Indication
Secondary Indication

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Chemical, Pharmacological and Biological Annotations


ATC Code:
N01AH02
Brand:
Rapifen (Janssen)
Categories:
Anesthetics, Intravenous; Analgesics, Opioid; Narcotics
ChEBI ID:
2569
PubChem ID:
51263
SMILE:
CCN1N=NN(CCN2CCC(COC)(CC2)N(C(=O)CC)C2=CC=CC=C2)C1=O
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
Classification:
Kingdom:
Organic Compounds
Superclass:
Benzenoids
Class:
Benzene and Substituted Derivatives
Subclass:
Anilides
Indication:
For the management of postoperative pain and the maintenance of general anesthesia.
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, alfentan...
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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 ...
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Mechanism:
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 GD...
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Adsorption, Distribution, Metabolism, Excretion and Toxicity


Human Intestinal Absorption:
+
Blood Brain Barrier:
+
Caco-2 permeable:
-
P-glycoprotein substrate:
Substrate
P-glycoprotein inhibitor I:
Inhibitor
P-glycoprotein inhibitor II:
Non-inhibitor
Renal organic cation transporter:
Non-inhibitor
CYP450 2C9 substrate:
Inhibitor
CYP450 2D6 substrate:
Non-inhibitor
CYP450 2C19 substrate:
Non-inhibitor
CYP450 inhibitory promiscuity:
Low CYP Inhibitory Promiscuity
Ames test:
AMES toxic
Carcinogenicity:
Non-carcinogens
Biodegradation:
Not ready biodegradable
Rat acute toxicity:
2.9997 LD50, mol/kg
hERG inhibition (predictor I):
Strong inhibitor
hERG inhibition (predictor II):
Inhibitor

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Dudley Laboratory
Department of Genetics and Genomic Sciences
Icahn Institute for Genomics and Multiscale Biology
Icahn School of Medicine at Mount Sinai
One Gustave L. Levy Place, Box 1498
Manhattan, New York City, NY
repurposedb@dudleylab.org