Neurological Associates

Pain Management Center

Vero Beach, Florida

H. Hooshmand, M. D.

DIPLOMATE AMERICAN BOARD OF PSYCHIATRY AND NEUROLOGY

BOARD CERTIFIED IN ELECTROENCEPHOLOGRAPHY

BOARD CERTIFIED IN ELECTROMYOGRAPHY  

BOARD CERTIFIED IN AMERICAN BOARD OF ELECTODIAGNOSTIC MEDICINE

INTRACTABLE NEUROLOGY

EPILEPSY, PAIN, MS

An International Referral Center dedicated to Treatment, Education and Research

 

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RSD PUZZLE # 38
Use and Abuse of Butorphanol (STADOL)

 

According to the Physician Desk Reference, Butorphanol Tartrate is a synthetic opioid mixed agonist/antagonist analgesic. Of the three endorphin receptors in the brain (mu, theta, and kappa receptors), Stadol has more affinity to mu and theta receptors. In therapeutic doses, the kappa receptor which is a larger sized receptor is not filled with the ligand Stadol, and as a result, the endorphin fills the kappa receptor.

This explains the fact that in therapeutic doses, the Stadol does not stop the formation of the endorphin in the brain and in the spinal cord, and as a result, the patient does not develop withdrawal (rebound) phenomenon which is the main problem with opioid agonists such as Morphine, etc. However, if the dosage is increased above the therapeutic dose, then the Stadol floods all the receptors, and the brain and the spinal cord stop forming natural endorphin. This explains the agonist as well as antagonist effect of Stadol in regard to pain relief.

Opioid antagonists (Stadol, Nubain, or Buprenex) in therapeutic dosage do not cause any serious problem. The problem comes when an opioid agonists such as morphine, methadone, etc... is added to it, then the patient gets dry mouth, has drowsiness, and has nausea. In addition, in high doses, the Stadol is as habit forming as morphine family of drugs. This causes Stadol addiction and abuse (dependence). In this regard, the opioid antagonist acts similar to Antebuse. They are supposed to make the patient very sick if the patient takes opioid agonists along with it.

The above neuropharmacological principle explains the complexity of the agonist/antagonist analgesics.



H.Hooshmand, M.D.

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Copyright © 1997-2012 H. Hooshmand, M.D. No part of this publication may be reproduced, transmitted, stored in a retrieval system other than this specific media, transcribed, or translated into any language without the expressed written permission from the author; H. Hooshmand, M.D. and Eric Phillips and CMNE. This material is for informational and education purposes. It is not meant to take the place of your physician. Before starting, changing, or stopping any treatments or medicines consult your physician.


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The material on the Neurological Associates Pain Management Center Homepage and all it's associated, linked or reference pages is for informational and education purposes. It is not meant to take the place of your physician. Before starting, changing, or stopping any treatments or medicines consult your physician. H. Hooshmand, M.D., Neurological Associates Pain Management Center and Associates will not be held liable for any damage or loss as a result of information provided on this page or associated documentation. Again, this WEB SITE is simply published as an information source and should not be used to treat or make judgments on RSD/CRPS. All associated material on this web site may not be copied, reproduced or quoted without expressed written permission from the owner; Copyright © 1999-2012 H. Hooshmand, M.D.

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Web Site designed and maintained by:

Eric M. Phillips; E-mail: EricmP9512@aol.com

This page was last updated on 3/11/2000.

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