Remifentanil: Difference between revisions

Latest revision as of 11:05, 23 March 2025

Remifentanil[edit]

Remifentanil is a potent, short-acting synthetic opioid analgesic drug. It is used in anesthesia to provide analgesia during surgical procedures. Remifentanil is known for its rapid onset and short duration of action, which makes it particularly useful in settings where quick recovery from anesthesia is desired.

Pharmacology[edit]

Remifentanil is a μ-opioid receptor agonist, which means it binds to and activates the μ-opioid receptors in the central nervous system. This action results in analgesia, sedation, and respiratory depression. The unique feature of remifentanil is its rapid metabolism by nonspecific blood and tissue esterases, leading to a very short half-life of approximately 3 to 10 minutes. This rapid metabolism allows for precise control over the drug's effects, making it ideal for use in surgical anesthesia.

Clinical Use[edit]

Remifentanil is primarily used in anesthesia for its analgesic properties. It is often administered as a continuous intravenous infusion during surgery to maintain a stable level of analgesia. Due to its short half-life, remifentanil is not suitable for postoperative pain management, as its effects dissipate quickly once the infusion is stopped.

Side Effects[edit]

The side effects of remifentanil are similar to those of other opioids and include respiratory depression, bradycardia, hypotension, and muscle rigidity. Because of its rapid onset and offset, careful monitoring is required to avoid complications such as respiratory depression.

Chemical Structure[edit]

Remifentanil is chemically related to fentanyl, but it has a unique ester linkage that is rapidly hydrolyzed by esterases. This structural feature is responsible for its rapid metabolism and short duration of action. The chemical name of remifentanil is 1-(2-methoxycarbonyl-ethyl)-4-(phenylpropionylamino)-piperidine-4-carboxylic acid methyl ester.

Derivatives[edit]

Several derivatives of remifentanil have been synthesized to explore variations in pharmacokinetics and pharmacodynamics. One such derivative is tert-butyl remifentanil, which has been studied for its potential use in clinical settings.

Related Pages[edit]

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-{{intro}}
+== Remifentanil ==
-Fentanyl is a fully synthetic opioid that is more potent that morphine and is commonly used for management of severe [[pain]] and as an adjunct to general anesthesia.
-{{livtox}}
+[[File:Remifentanil2DCSDS.svg|Remifentanil 2D Chemical Structure|thumb|right]]
-Alfentanil, remifentanil and sufentanil are phenylpiperidine analogues of fentanyl and have a similar spectrum of activity, but differ in their pharmacokinetics, potency and routes of administration, and are used only in anesthesia. None of the phenylpiperidine opioids have been implicated in causing serum enzyme elevations or clinically apparent [[liver injury]].
-{{moa}}
+'''Remifentanil''' is a potent, short-acting synthetic opioid analgesic drug. It is used in anesthesia to provide analgesia during surgical procedures. Remifentanil is known for its rapid onset and short duration of action, which makes it particularly useful in settings where quick recovery from anesthesia is desired.
-Fentanyl (fen’ tan il) is a synthetic phenylpiperidine which shares similar [[pain]] relieving activities with morphine, but is 50 to 100 times more potent. Like morphine, fentanyl is an agonist for the µ type opiate receptors which are found in the central nervous system but also on heart, lung, vascular and intestinal cells. Fentanyl has a rapid onset and short duration of action, making it particularly effective in anesthesia induction as well as maintenance.
-{{fda}}
+=== Pharmacology ===
-Fentanyl was approved for use in general anesthesia in the United States in 1968 and is still widely used in anesthesia practice. With the development of transdermal and buccal formulations of fentanyl, it was approved for use in [[pain]] management and has become the most widely used synthetic opioid in clinical practice. Current indications are as an adjunct to general anesthesia (intravenous, epidural or intrathecal) and for management of moderate-to-severe [[pain]] that is not responsive to nonopiate analgesics.
-{{dose}}
+Remifentanil is a [[μ-opioid receptor]] agonist, which means it binds to and activates the μ-opioid receptors in the central nervous system. This action results in analgesia, sedation, and respiratory depression. The unique feature of remifentanil is its rapid metabolism by nonspecific blood and tissue esterases, leading to a very short half-life of approximately 3 to 10 minutes. This rapid metabolism allows for precise control over the drug's effects, making it ideal for use in [[surgical anesthesia]].
-Fentanyl is available in multiple formulations, including solutions for injection in multiple concentrations for anesthesia and acute [[pain]] management, and as transdermal patches, oral tablets and lozenges and nasal sprays for management of chronic [[pain]]. Fentanyl is available generically and under commercial names including Sublimaze (solution for injection), Duragesic and Ionsys (transdermal patches), Actiq and Fentora (lollipop and tablets for transmucosal delivery) in multiple dose formulations.
-{{se}}
+=== Clinical Use ===
-Side effects of fentanyl resemble those of other opioids and include [[sedation]], [[respiratory depression]], [[confusion]], [[euphoria]], [[agitation]], [[headache]], [[dizziness]], [[constipation]], [[diarrhea]], [[abdominal bloating]], [[nausea]] and [[vomiting]]. Fentanyl and its congeners are controlled substances and classified as Schedule II drugs, indicating that they have medical usefulness, but also a high potential for physical and psychological [[dependency]] and abuse. Indeed, deaths have been reported due to fentanyl patches and transbuccal formulations either from inadvertent overdose, accidental ingestion (by children for instance) or abuse.
-Alfentanil (al fen’ ta nil) is a structural analogue of fentanyl, which has a very short onset of action (5 to 10 minutes) and is approved for use as an adjunct to general anesthesia. Alfentanil is available as a solution for intravenous use in anesthesia generically and under the trade name Alfenta. It has similar adverse effects as fentanyl, but is not used for chronic [[pain]] management and should be used only by medical personnel trained in the use of intravenous anesthesia.
+Remifentanil is primarily used in [[anesthesia]] for its analgesic properties. It is often administered as a continuous intravenous infusion during surgery to maintain a stable level of analgesia. Due to its short half-life, remifentanil is not suitable for postoperative pain management, as its effects dissipate quickly once the infusion is stopped.
-Remifentanil (rem” i fen’ ta nil) is a structural analogue of fentanyl, but has a very short onset and duration of action with a rapid dissipation of activity even after prolonged infusions. Remifentanil is available as a solution under the brand name Ultiva for intravenous use in anesthesia. It has similar adverse effects as fentanyl, but is not used for chronic [[pain]] management and should be used only by medical personnel trained in the use of intravenous anesthesia.
+=== Side Effects ===
-Sufentanil (soo fen’ ta nil) is a structural analogue of fentanyl, which is 10 times more potent and is generally reserved for anesthesia in patients with opioid tolerance or opioid dependence. It is potent enough to overcome the actions of partial opiate [[antagonist]]s such as buprenorphine. Sufentanil was approved for use in the United States in 1984. Sufentanil is available as a solution for intravenous and epidural use in anesthesia generically and under the brand name Sufenta. It has similar adverse effects as fentanyl, but is not used for chronic [[pain]] management and should be used only by medical personnel trained in the use of intravenous anesthesia.
+The side effects of remifentanil are similar to those of other opioids and include respiratory depression, bradycardia, hypotension, and muscle rigidity. Because of its rapid onset and offset, careful monitoring is required to avoid complications such as respiratory depression.
-{{opiods}}
+=== Chemical Structure ===
-{{coststubd}}
-<gallery>
+[[File:R-30490.png|R-30490|thumb|left]]
-File:Remifentanil2DCSDS.svg|Remifentanil 2D Chemical Structure
-File:R-30490.png|R-30490
+Remifentanil is chemically related to [[fentanyl]], but it has a unique ester linkage that is rapidly hydrolyzed by esterases. This structural feature is responsible for its rapid metabolism and short duration of action. The chemical name of remifentanil is 1-(2-methoxycarbonyl-ethyl)-4-(phenylpropionylamino)-piperidine-4-carboxylic acid methyl ester.
-File:Tert-butyl remifentanil.png|Tert-butyl Remifentanil
-</gallery>
+=== Derivatives ===
-<gallery>
-File:Remifentanil2DCSDS.svg|Remifentanil 2D Chemical Structure
+[[File:Tert-butyl_remifentanil.png|Tert-butyl Remifentanil|thumb|right]]
-File:R-30490.png|R-30490
-File:Tert-butyl remifentanil.png|Tert-butyl Remifentanil
+Several derivatives of remifentanil have been synthesized to explore variations in pharmacokinetics and pharmacodynamics. One such derivative is tert-butyl remifentanil, which has been studied for its potential use in clinical settings.
-</gallery>
+== Related Pages ==
+* [[Fentanyl]]
+* [[Opioid]]
+* [[Anesthesia]]
+* [[Analgesic]]
+[[Category:Opioids]]
+[[Category:Anesthesia]]
+[[Category:Analgesics]]