Phenomorphan
Phenomorphan is a synthetic opioid analgesic, belonging to the larger family of opioid drugs. Despite its potent analgesic properties, it is not employed in current medical practice. However, understanding its pharmacological properties, structural activity relationship, and its relation to other opioids can provide insights into drug development and opioid pharmacology.
Historical Context[edit | edit source]
Opioid analgesics have been in use for centuries, primarily derived from the poppy plant. The need for potent and effective pain relief, coupled with attempts to reduce side effects, has driven the synthesis of various opioids, including Phenomorphan.
Pharmacodynamics and Mechanism of Action[edit | edit source]
Phenomorphan exerts its analgesic effects through its interaction with the μ-opioid receptor. The presence of the N-phenethyl group in its structure significantly enhances its affinity to this receptor.
- Its potency is roughly 10 times that of levorphanol, which itself possesses a potency 6-8 times greater than morphine, a widely recognized opioid benchmark[1].
- Other analogs of Phenomorphan, in which the N-(2-phenylethyl) group has been substituted with different aromatic rings, have demonstrated even greater potency. Specifically, the N-(2-(2-furyl)ethyl) and the N-(2-(2-thienyl)ethyl) analogues are found to be 60 times and 45 times more potent than levorphanol, respectively[2].
Clinical Profile and Side Effects[edit | edit source]
Like other opioids, Phenomorphan is associated with a range of side-effects, which include:
- Itching.
- Nausea.
- Respiratory depression, which can be life-threatening in overdose scenarios.
Despite its potency and potential therapeutic value, Phenomorphan is not employed in contemporary medical treatments due to concerns over its side-effect profile and the availability of safer alternatives.
Conclusion[edit | edit source]
Phenomorphan offers an illustrative example of how chemical modifications can significantly enhance the potency of opioids. Its potent interaction with the μ-opioid receptor, because of structural attributes, highlights the intricate balance between desired therapeutic effects and unintended adverse reactions. While not in medical use, it stands as a testament to the complexities of drug development and the need for thorough evaluation of potential therapeutic agents.
References[edit | edit source]
Search WikiMD
Ad.Tired of being Overweight? Try W8MD's physician weight loss program.
Semaglutide (Ozempic / Wegovy and Tirzepatide (Mounjaro / Zepbound) available.
Advertise on WikiMD
|
WikiMD's Wellness Encyclopedia |
| Let Food Be Thy Medicine Medicine Thy Food - Hippocrates |
Translate this page: - East Asian
中文,
日本,
한국어,
South Asian
हिन्दी,
தமிழ்,
తెలుగు,
Urdu,
ಕನ್ನಡ,
Southeast Asian
Indonesian,
Vietnamese,
Thai,
မြန်မာဘာသာ,
বাংলা
European
español,
Deutsch,
français,
Greek,
português do Brasil,
polski,
română,
русский,
Nederlands,
norsk,
svenska,
suomi,
Italian
Middle Eastern & African
عربى,
Turkish,
Persian,
Hebrew,
Afrikaans,
isiZulu,
Kiswahili,
Other
Bulgarian,
Hungarian,
Czech,
Swedish,
മലയാളം,
मराठी,
ਪੰਜਾਬੀ,
ગુજરાતી,
Portuguese,
Ukrainian
Medical Disclaimer: WikiMD is not a substitute for professional medical advice. The information on WikiMD is provided as an information resource only, may be incorrect, outdated or misleading, and is not to be used or relied on for any diagnostic or treatment purposes. Please consult your health care provider before making any healthcare decisions or for guidance about a specific medical condition. WikiMD expressly disclaims responsibility, and shall have no liability, for any damages, loss, injury, or liability whatsoever suffered as a result of your reliance on the information contained in this site. By visiting this site you agree to the foregoing terms and conditions, which may from time to time be changed or supplemented by WikiMD. If you do not agree to the foregoing terms and conditions, you should not enter or use this site. See full disclaimer.
Credits:Most images are courtesy of Wikimedia commons, and templates, categories Wikipedia, licensed under CC BY SA or similar.
Contributors: Prab R. Tumpati, MD
