Lesson B4 - Pharmacology Flashcards
Opium contains at least 20 different
chemical compounds, two of which are
morphine and codeine, are analgesic (pain-relieving) drugs.
In the early 1800’s, morphine was isolated as the major analgesic agent from
opium
The purification of morphine revolutionized the use of opiates. Since then, morphine has been used worldwide for the treatment of
pain and diarrhea.
The term “opioid” refers to
any natural or synthetic substance which exerts actions on the body
that are similar to those induced by morphine and that are antagonized (blocked) by the drug
naloxone.
Opioids include:
- Opiate narcotics (analgesic agents obtained from the opium poppy).
- Substances structurally related to morphine.
- Synthetic drugs with structures different from that of morphine.
- Endogenous brain peptides that exert analgesic actions (opioid peptides: enkephalins and
endorphins) .
There are now at least three known families of
endorphins; these are:
enkephalins, dynorphins and β-endorphins.
There are several types of opioid receptors; three will be discussed…
- Mu (µ) receptors are present in all structures in the brain and spinal cord
- Kappa (k) receptors are involved in analgesia, dysphoria and miosis (pin-point pupils)
- Delta (δ) receptors have as their endogenous ligand, the enkephalins
Opioid receptors are located in the
peripheral as well as the central nervous system-These are located in the gastrointestinal tract and are responsible for the constipation caused by opiates.
Agonists:
Illicit a full response.
Natural – morphine and codeine
Semi-synthetic – heroin
Synthetic – meperidine and methadone
Mixed Agonists/Antagonists:
Pentazocine is the best example of this group. This group can illicit a response when given alone, but can block part of the
response to morphine, when given together with morphine.
Antagonists:
These agents block the response to morphine, heroin and other
opiates at the respective receptor. Administration of an antagonist to an addict will precipitate “withdrawal”.
The prototype antagonist is naloxone. It has no analgesic activity
and is used in:
(a) Reversal of opioids overdose.
(b) Treatment of opioid dependence.
(c) Diagnosis of opioid physical dependence.
(d) Naltrexone – an opioid antagonist is used to treat alcohol dependence.
The therapeutic uses listed below apply to morphine and most of the other opiates:
Relief of severe pain (e.g. post-surgical pain and pain experienced by some terminally
ill patients). Analgesia is the major use for the opiates.
Treatment of diarrhea.
Pharmacological Effects of Opioid Agonists
- Analgesia.
- Euphoria
- Sedation.
- Hypnosis/sleep (narcotic effect).
- Relief or prevention of cough.
- Respiratory depression (basis of toxicity) → respiratory arrest.
- Decreased gastrointestinal motility (constipation).
- Constriction of the pupils of the eyes (miosis).
- Nausea, vomiting.
- Drug dependence. Develops to all opiate analgesics.
Morphine and related opioids act on specific receptors on neurons – the
opioid receptors
Morphine and related opioids act on specific receptors on neurons – the opioid receptors.
Responses are elicited when these receptors are activated. Naloxone does
not activate these
receptors. However, it occupies and blocks the opioid receptors (an antagonist).