Levorphanol: Difference between revisions

Levorphanol
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Revision as of 05:40, 16 February 2025

An opioid medication used for pain management

Levorphanol is a synthetic opioid used primarily in the management of moderate to severe pain. It is known for its potent analgesic properties and is often utilized in cases where other pain management strategies are ineffective.

Pharmacology

Levorphanol is a morphinan derivative and acts as an agonist at the mu-opioid receptor, which is responsible for its analgesic effects. It also has activity at the kappa-opioid receptor and delta-opioid receptor, contributing to its efficacy in pain relief. Additionally, levorphanol inhibits the reuptake of norepinephrine and serotonin, which may enhance its analgesic properties.

Medical uses

Levorphanol is primarily indicated for the treatment of moderate to severe pain. It is particularly useful in chronic pain conditions where other opioids may not be effective. Due to its long half-life, levorphanol can provide sustained pain relief with less frequent dosing compared to other opioids.

Side effects

Common side effects of levorphanol include nausea, vomiting, constipation, drowsiness, and dizziness. Like other opioids, it carries a risk of respiratory depression, especially at higher doses or when combined with other central nervous system depressants.

History

Levorphanol was first synthesized in the 1940s and has been used clinically since the 1950s. It was developed as part of efforts to find effective analgesics with fewer side effects than morphine.

Stereochemistry

Levorphanol is the levorotatory isomer of racemorphan, with the dextrorotatory isomer being dextrorphan, which is an antitussive and NMDA receptor antagonist. The stereochemistry of levorphanol contributes to its potent opioid activity.

Related pages

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-{{intro}}
+{{Short description|An opioid medication used for pain management}}
-Hydromorphone and oxymorphone are semisynthetic derivatives of morphine and potent opiate agonists which are used predominantly to treat moderate-to-severe pain.
+{{Drugbox
+| verifiedfields = changed
+| verifiedrevid = 477002123
+| image = Levorphanol_and_dextrorphan.png
+| image_size = 250px
+| image_caption = Chemical structure of Levorphanol (left) and Dextrorphan (right)
+}}
-{{livtox}}
+'''Levorphanol''' is a [[synthetic opioid]] used primarily in the management of moderate to severe [[pain]]. It is known for its potent analgesic properties and is often utilized in cases where other pain management strategies are ineffective.
-Neither hydromorphone nor oxymorphone have been linked to serum enzyme elevations during therapy or to clinically apparent liver injury.
-{{moa}}
-Hydromorphone and oxymorphone are semisynthetic derivatives that both act by engagement in cell surface opiate receptors (predominant µ type receptors) that are found in the central nervous system, but also heart, lung, vascular and intestinal cells.  Current indications are for moderate to severe pain, pre- and postoperative analgesia, and as an adjunct to anesthesia.
-{{fda}}
+==Pharmacology==
-Hydromorphone was approved for use in the United States in 1984 and is still widely used in treatment of moderate-to-severe pain and, in low doses, as an antitussive.  Hydromorphone is available generically and under the brand name Dilaudid as tablets of 2, 4 and 8 mg, as an oral solution of 5 mg/5 mL and as suppositories of 3 mg.  Solutions for injection (1 to 10 mg/mL) are also available.  The usual dose of hydromorphone in adults is 2 to 10 mg orally every 3 to 6 hours or 2 to 4 mg by injection every 4 to 6 hours.  Lower doses (1 mg orally) are used for treatment of cough.
+Levorphanol is a [[morphinan]] derivative and acts as an agonist at the [[mu-opioid receptor]], which is responsible for its analgesic effects. It also has activity at the [[kappa-opioid receptor]] and [[delta-opioid receptor]], contributing to its efficacy in pain relief. Additionally, levorphanol inhibits the reuptake of [[norepinephrine]] and [[serotonin]], which may enhance its analgesic properties.
-{{fda}}
+==Medical uses==
-Oxymorphone was approved for use in the United States in 1959 and remains in clinical use.  Current indications are for treatment of moderate to severe pain, alleviation of anxiety associated with dyspnea of pulmonary edema and as an adjunct to general anesthesia and preoperative sedation.
+Levorphanol is primarily indicated for the treatment of moderate to severe pain. It is particularly useful in chronic pain conditions where other opioids may not be effective. Due to its long half-life, levorphanol can provide sustained pain relief with less frequent dosing compared to other opioids.
-{{brand}}
+==Side effects==
-Oxymorphone is available generically and under the brand name Numorphan and Opana in standard tablets of 5 and 10 mg, extended release tablets of 5 to 40 mg, suppositories of 5 mg and as a solution for injection of 1 mg/mL.
+Common side effects of levorphanol include [[nausea]], [[vomiting]], [[constipation]], [[drowsiness]], and [[dizziness]]. Like other opioids, it carries a risk of [[respiratory depression]], especially at higher doses or when combined with other central nervous system depressants.
-{{dose}}
+==History==
-The usual dose of oxymorphone is 5 to 20 mg orally of the standard tablets every 4 to 6 hours or 1 to 1.5 mg by injection every 4 to 6 hours.
+Levorphanol was first synthesized in the 1940s and has been used clinically since the 1950s. It was developed as part of efforts to find effective analgesics with fewer side effects than [[morphine]].
-{{se}}
+==Stereochemistry==
-The side effects of hydromorphone and oxymorphone are similar to those of other opiates and include sedation, respiratory depression, confusion, euphoria, agitation, constipation, abdominal bloating, nausea, vomiting and constipation.  Both drugs are controlled substances and classified as Schedule II drugs, indicating that it has medical usefulness, but also a high potential for physical and psychological dependency and abuse.
+Levorphanol is the levorotatory isomer of [[racemorphan]], with the dextrorotatory isomer being [[dextrorphan]], which is an [[antitussive]] and [[NMDA receptor antagonist]]. The stereochemistry of levorphanol contributes to its potent opioid activity.
-{{opiods}}
+==Related pages==
+* [[Opioid]]
+* [[Pain management]]
+* [[Morphinan]]
+* [[Mu-opioid receptor]]
-{{coststubd}}
+[[Category:Opioids]]
+[[Category:Analgesics]]
+[[Category:Morphinans]]