| Indication |
For use during the induction and maintenance of general anesthesia. |
| Pharmacodynamics |
Remifentanil is an opioid agonist with rapid onset and peak
effect and ultra-short duration of action. The opioid activity of
remifentanil is antagonized by opioid antagonists such as naloxone. The
analgesic effects of remifentanil are rapid in onset and offset. Its
effects and side effects are dose dependent and similar to other
opioids. Remifentanil in humans has a rapid blood-brain equilibration
half-time of 1 ± 1 minutes (mean ± SD) and a rapid onset of action. |
| Mechanism of action |
Remifentanil is a µ-opioid agonist with rapid onset and peak
effect, and short duration of action. The µ-opioid activity of
remifentanil is antagonized by opioid antagonists such as naloxone. |
| Absorption |
Not Available |
| Volume of distribution |
- 350 mL/kg
- 452 ± 144 mL/kg [neonates]
- 223 ± 30.6 mL/kg [adolescents]
|
| Protein binding |
70% (bound to plasma proteins) |
| Metabolism |
By hydrolysis of the propanoic acid-methyl ester linkage by nonspecific blood and tissue esterases. |
| Route of elimination |
Remifentanil is an esterase-metabolized opioid. The carboxylic
acid metabolite is essentially inactive (1/4600 as potent as
remifentanil in dogs) and is excreted by the kidneys with an elimination
half-life of approximately 90 minutes. |
| Half life |
1-20 minutes |
| Clearance |
- 40 mL/min/kg [young, healthy adults]
|
| Toxicity |
Not Available |
