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chap 19
narcotic
51
Pharmacology
Undergraduate 1
05/05/2011

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Term
Analgesic
Definition
pain reliever. A drug that inhibits painful stimuli or the perception of pain.
Term
Narcotic
Definition
a drug that is physically addictive with repeated use. Narcotic analgesics are similar to opium (opiate drugs).
Term
Opiate drugs
Definition
are derived from the poppy plant
Term
Opiate drugs
Definition
similar in structure to morphine
Term
Clinical Indication
Definition
Prevent or interrupt moderate to severe pain of any origin without a loss of consciousness
Term
Acute pain
Definition
during or after surgical procedures
Term
Chronic pain
Definition
any etiology from back pain to cancer pain
Term
Opium
Definition
extracted from poppy seeds (Papaver somniferum)
Term
Opium uses
Definition
Euphoria Analgesia Sedation
Relief from diarrhea Cough suppression
Term
opiate
Definition
drug extracted from the exudate of the poppy
Term
“opioid”
Definition
is a natural or synthetic drug that binds to opioid receptors prod“opioid” ucing agonist effects
Term
Opioid analgesics
Definition
derivatives of thenaturally occurring plant substance opium (semi-synthetic) OR
synthetic substances that produce the same pharmacologic effects as opium
Term
Natural opiate
Definition
phenanthrene
morphine 10%
codeine 0.5%
thebaine 0.2%
Term
semisynthetic opiate
Definition
heroin
oxymorphone
Hydromorphone
Term
synthetic opiate
Definition
meperidine
methadone
morphinians
benzamorphans
Term
Opinoids
Definition
Morphine
Heroin
Hydromorphone
Fentanyl
Codeine
Hydrocodone
Term
Pain is composed of two elements
Definition
localized stimulation of peripheral nerves through damage or inflammation
and recognition of pain within the CNS that
can intensify the reaction to pain
Term
Nociception
Definition
the mechanism whereby pain peripheral stimuli are transmitted to the central nervous system.
Term
Polymodal nociceptors (PMN)
Definition
the main type of peripheral sensory neuron that responds to pain stimuli.
Term
non-myelinated C-fibres
Definition
endings respond to thermal, mechanical and chemical stimuli.
Term
Activation of peripheral nociceptive fibers
Definition
causes release of substance P and other pain-signaling neurotransmitters from nerve terminals in the dorsal horn of the spinal cord
Term
Release of pain-signaling neurotransmitters
Definition
regulated by endogenous endorphins or by exogenous opioid agonists by acting presynaptically to inhibit substance P release, causing analgesia
Term
Opioid analgesics
Definition
analgesics relieve pain by
selectively acting on receptors within the
CNS
Term
Opioid analgesics in cns
Definition
decrease anxiety
reduce the reaction to pain
interrupt pain signal transmission within the spinal cord
Term
Opioid Receptors
Definition
they are at areas concerned with pain
and receptor locations beginning with highest concentration areas
Term
Opioid Receptors location
Definition
cerebral cortex,amygdala, septum, thalamus, hypothalamus, midbrain, spinal cord
Term
Three Opioid Receptors
Definition
Mu,Kappa,Delta
Term
Opioid analgesics mimic
Definition
action of endorphins
produced in the brain and spinal cord by
selectively stimulating receptors
Term
mu (µ)
Definition
receptors mediate analgesia, euphoria, and respiratory depression
Term
kappa (κ)
Definition
receptors mediate sedation, dysphoria
Term
delta (δ)
Definition
receptors mediate hallucinations, and increased respiration and blood pressure
Term
Delta agonists
Definition
show poor analgesia and little addictive potential
Term
delta receptor
Definition
May regulate mu receptor activity
Believed to cause hallucinations
Term
Mu-Receptor: Two Types
Definition
Mu-1
Mu-2
Term
Mu-1
Definition
Located outside spinal cord
Responsible for central interpretation of pain
Term
Mu-2
Definition
Located throughout CNS
Responsible for respiratory depression, spinal analgesia, physical dependence, and euphoria
Term
Kappa Receptor
Definition
Only modest analgesia
Little or no respiratory depression
Little or no dependence
Dysphoric effects
Term
Pure Agonist
Definition
has affinity for binding plus efficacy
Term
Pure Antagonist
Definition
has affinity for binding but no efficacy; blocks action of endogenous and exogenous ligands
Term
Mixed Agonist-Antagonist
Definition
produces an agonist effect at one receptor and an antagonist effect at another
Term
Partial Agonist
Definition
has affinity for binding but low efficacy
Term
AGONISTS
Definition
Morphine
*Heroin
*Hydromorphone
*Fentanyl
*Codeine
Term
Sedation and anxiolysis
Definition
Drowsiness and lethargy
Apathy
Cognitive impairment
Sense of tranquility
Term
Depression of respiration
Definition
Main cause of death from opioid overdose
Combination of opioids and alcohol is especially dangerous
Term
Cough suppression
Definition
Opioids suppress the “cough center” in the brain
Term
Pupillary constriction
Definition
pupillary constriction in the presence of analgesics is characteristic of opioid use
Term
Nausea and vomiting
Definition
Stimulation of receptors in an area of the medulla called the chemoreceptor trigger zone causes nausea and vomiting
Unpleasant side effect, but not life threatening
Term
Gastrointestinal symptoms
Definition
Opioids relieve diarrhea as a result of their direct actions on the intestines
Term
Other effects
Definition
Opioids can release histamines causing itching or more severe allergic reactions including bronchoconstriction
Opioids can affect white blood cell function and immune function
Term
Pharmacological Effects on
CNS
Definition
Change in mental alertness, sedation (μ, κ)
Change mood, euphoria (µ) or dysphoria (κ)
Stimulation of chemoreceptor trigger zone
initiating nausea and vomiting
Dose dependent depression of the vomiting center
Depression of respiratory centers (µ)
Headache
Cough suppressant (antitussive)
Secretion of antidiuretic hormone
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