What is the mechanism of action of Levopront (generic name), in a patient with an unspecified medical condition and no provided demographic or medical history?

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Mechanism of Action of Levopront (Levorphanol)

Primary Mechanism

Levorphanol is a full mu-opioid receptor agonist that produces analgesia through direct activation of CNS opioid receptors, with additional activity at delta- and kappa-opioid receptors at higher doses, and functions as an N-methyl-D-aspartate (NMDA) receptor antagonist. 1

Detailed Pharmacological Actions

Opioid Receptor Activity

  • Levorphanol is relatively selective for the mu-opioid receptor, which mediates its primary analgesic effects 1
  • At higher doses, it binds to delta- and kappa-opioid receptors, providing broader pain modulation 2
  • As a full opioid agonist, there is no ceiling effect for analgesia—dosage can be titrated upward as needed, limited only by adverse effects including respiratory and CNS depression 1

NMDA Receptor Antagonism

  • Like methadone, levorphanol acts as an antagonist at N-methyl-D-aspartate receptors, which may provide additional benefit for neuropathic pain 2
  • This dual mechanism (opioid agonism + NMDA antagonism) distinguishes levorphanol from simpler opioid analgesics 2

Central Nervous System Effects

  • Levorphanol produces analgesia through direct action on specific CNS opioid receptors identified throughout the brain and spinal cord 1
  • It causes respiratory depression by reducing the responsiveness of brain stem respiratory centers to both carbon dioxide retention and electrical stimulation 1
  • The drug produces miosis (pinpoint pupils) even in total darkness through direct CNS action 1

Pharmacokinetic Advantages

  • Levorphanol has a shorter half-life and more predictable metabolism compared to methadone 2
  • The morphine-to-levorphanol conversion ratio varies based on baseline morphine dose: 12:1 for <100 mg morphine, 15:1 for 100-299 mg, 20:1 for 300-599 mg, and 25:1 for >600 mg morphine 2

Additional Physiological Effects

Gastrointestinal System

  • Levorphanol reduces motility and increases smooth muscle tone in the stomach and duodenum 1
  • It decreases propulsive peristaltic waves in the colon while increasing tone to the point of spasm, resulting in constipation 1
  • May reduce biliary and pancreatic secretions and cause sphincter of Oddi spasm 1

Cardiovascular System

  • Produces peripheral vasodilation that may result in orthostatic hypotension or syncope 1
  • Manifestations of histamine release include pruritus, flushing, red eyes, sweating, and orthostatic hypotension 1

Endocrine System

  • Inhibits secretion of ACTH, cortisol, and luteinizing hormone 1
  • Stimulates prolactin and growth hormone secretion 1
  • Extended use may lead to hypogonadism with symptoms including low libido, impotence, erectile dysfunction, amenorrhea, or infertility 1

References

Guideline

Guideline Directed Topic Overview

Dr.Oracle Medical Advisory Board & Editors, 2025

Professional Medical Disclaimer

This information is intended for healthcare professionals. Any medical decision-making should rely on clinical judgment and independently verified information. The content provided herein does not replace professional discretion and should be considered supplementary to established clinical guidelines. Healthcare providers should verify all information against primary literature and current practice standards before application in patient care. Dr.Oracle assumes no liability for clinical decisions based on this content.

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