| Absorption | For intravenous injection or infusion only. |
| Volume of distribution | |
| Protein binding | 92% |
| Metabolism | The liver is the major site of biotransformation.
| Enzyme | Metabolite | Reaction | Km | Vmax |
| Cytochrome P450 3A4 | AMX | amide N-dealkylation | 18.9 | 17.96 |
| Cytochrome P450 3A4 | noralfentanil | piperidine N-dealkylation | 14.1 | 1.05 |
|
| 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 | |
| Toxicity | Symptoms of overexposure include characteristic rigidity of the skeletal muscles, cardiac and respiratory depression, and narrowing of the pupils. |
| Affected organisms | |
| Pathways |
| Pathway | Name | SMPDB ID |
 | Alfentanil Pathway |
|
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