Molecule

Drug Groups

illicit; approved

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]

Indication

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

Pharmacology

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.

Toxicity

Symptoms of overexposure include characteristic rigidity of the skeletal muscles, cardiac and respiratory depression, and narrowing of the pupils.

Affected Organisms

Biotransformation

The liver is the major site of biotransformation.

Absorption

For intravenous injection or infusion only.

Half Life

90-111 minutes

Protein Binding

92%

Elimination

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

Distribution

* 0.4 to 1 L/kg

Clearance

* 5 mL/kg/min

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