Narcotic Analgesic Drugs - ChemWiki

June 14, 2014 – 06:33 pm

673analgesicrecep.gif Narcotic agents are potent analgesics which are effective for the relief of severe pain. Analgesics are selective central nervous system depressants used to relieve pain. The term analgesic means "without pain". Even in therapeutic doses,narcotic analgesics can cause respiratory depression,nausea,and drowsiness. Long term administration produces tolerance,psychic,and physical dependence called addiction.

Introduction

Narcotic agents may be classified into four categories:

  1. Morphine and codeine - natural alkaloids of opium.
  2. Synthetic derivatives of morphine such as heroin.674morphine.jpg
  3. Synthetic agents which resemble the morphine structure.
  4. Narcotic antagonists which are used as antidotes for overdoses of narcotic analgesics.

The main pharmacological action of analgesics is on the cerebrum and medulla of the central nervous system. Another effect is on the smooth muscle and glandular secretions of the respiratory and gastro-intestinal tract. The precise mechanism of action is unknown although the narcotics appear to interact with specific receptor sites to interfere with pain impulses.

Receptor Site

A schematic for an analgesic receptor site may look as shown in the graphic below with morphine. Three areas are needed: a flat areas to accommodate a flat nonpolar aromatic ring,a cavity to accept another series of rings perpendicular,and an anionic site for polar interaction of the amine group.

Enkephalins

Recently investigators have discovered two compounds in the brain called enkephalins which resemble morphine in structure. Each one is a peptide composed of 5 amino acids and differ only in the last amino acid. The peptide sequences are: tyr-gly-gly-phe-leu and tyr-gly-gly-phe-met. Molecular models show that the structures of the enkephalins has some similarities with morphine. The main feature in common appears to be the aromatic ring with the -OH group attached (tyr). Methadone and other similar analgesics have 2 aromatic rings which would be similar to the enkephalins (tyr and phe).

Analgesics may relieve pain by preventing the release of acetylcholine. Enkephalin molecules are released from a nerve cell and bind to analgesic receptor sites on the nerve cell sending the impulse.674methadone.gifThe binding of enkephalin or morphine-like drugs changes the shape of the nerve sending the impulse in such a fashion as to prevent the cell from releasing acetylcholine. As a result,the pain impulse cannot be transmitted and the brain does not preceive pain.

Morphine and Codeine

Morphine exerts a narcotic action manifested by analgesia,drowsiness,changes in mood,and mental clouding. The major medical action of morphine sought in the CNS is analgesia. Opiates suppress the "cough center" which is also located in the brain stem,the medulla. Such an action is thought to underlie the use of opiate narcotics as cough suppressants. Codeine appears to be particularly effective in this action and is widely used for this purpose.

674heroin.jpg

Source: chemwiki.ucdavis.edu


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