• Shuffle
    Toggle On
    Toggle Off
  • Alphabetize
    Toggle On
    Toggle Off
  • Front First
    Toggle On
    Toggle Off
  • Both Sides
    Toggle On
    Toggle Off
  • Read
    Toggle On
    Toggle Off
Reading...
Front

Card Range To Study

through

image

Play button

image

Play button

image

Progress

1/45

Click to flip

Use LEFT and RIGHT arrow keys to navigate between flashcards;

Use UP and DOWN arrow keys to flip the card;

H to show hint;

A reads text to speech;

45 Cards in this Set

  • Front
  • Back
Medication Overuse Headache - MOH
“Rebound headache”
Analgesics, ergotamines, caffeine, & triptans
Limit use to 2-3 days per week for abortive therapy
Withdrawal symptoms on discontinuation
Toxic effects from the medications
Escalating use, escalating headaches, dependence & habituation to symptomatic management
the body creates a circuit and gets used to it, so it will take a particular path that results in pain
the pattern of these patients are ones that take more and more meds tog get the same effects
best way to get rid of MOH
stop using meds cold turkey
#1 medication that causes MOH (know)
excedrin for migraine
it is the most overused
scotomata
aura term
hazy or lost vision
visual field is cut
Narcotic
drug that induces stupor or insensibility
opiate
naturally-occurring alkaloids found in the opium poppy
opiopeptidins
endogenous neurotransmitter peptides that exhibit opiate-like activity
opioids
Narcotic: drug that induces stupor or insensibility
• Opiate: naturally-occurring alkaloids found in the opium poppy
• Opiopeptins: endogenous neurotransmitter peptides that exhibit opiate-like activity
• Opioids: general term that covers all of the above
nociceptions
the perception of traumatic stimuli
analgesia
the absence of sensibility to pain or the relief of pain
First endogenous opioid peptides were discovered
40 years ago and act as agonists on endogenous opioid receptors
Opiates and synthetic opioid drugs are either .....
agonists, partial agonists, or antagonists of endogenous opioid receptors
Endogenous opioid peptides Implicated in many bodily functions including:
Analgesia
Modulation of stress and anxiety
Regulation of hormonal functions
Thermoregulation
Maintain homeostasis
Endogenous Opioid Peptides
Endogenous opioid peptides comprise a family of small, structurally related peptides that are encoded by three different genes. A large precursor peptide is made from the gene (a “prohormone”) and the smaller opioid peptides are cleaved from this precursor (from 5-32 amino acids in length).
The three opioid peptide gene families are:
Proenkephalin
• Leu-enkephalin, Met-enkephalin (generally referred to simply as “enkephalin”)
common structure of opioids
try-Gly-Gly-Phe-Met/Leu
The Anatomical distribution of opioid peptides:
what are the smallest opioid peptides
met and leu enkephalin
5 amino acids long and differ in the terminal amino acid met and leu
Opioid Receptors
There are at least 8 subtypes of opioid receptors each of which has seven membrane-spanning regions. All of them modulate intracellular signaling cascades through coupling to G-proteins.
are opioid receptors inhibitory or stimulatroy
inhibitory
Opioid receptors are inhibitory and cause
There are at Least 8 Different Opioid Receptor Subtypes
 u (1, 2)
Main receptor in the Descending Pain Pathway
 gama (1, 2)
 kapa(1, 2, 3)
Activation of k receptors thought to antagonize u receptor activity
 e
(possibly others)
•Opioid receptor subtypes: that are important pharmocologically
Anatomical distribution of opioid receptors
What determines the specific effects of endogenous and exogenous opioid ligands?
pain
Unpleasant sensory and emotional experience associated with actual or potential tissue damage, or
described in terms of such damage.”
(International Association for the Study of Pain)
Pain is a reaction to harmful stimuli. It can be acute, the result of sudden injurious event or it can be chronic which could be the result of disease or injury and is rather long-lasting. It serves as warning to the organism, but inhibition of pain is also adaptive. For example, excessive pain could prevent one from appropriately dealing with a potentially dangerous or life-threatening situation.
Opioid Receptors are Inhibitory
Primary effect is to inhibit adenylyl cyclase activity (decreases formation of cAMP)
This causes a decrease in voltage-gated Ca2+ currents with a concomitant increase in K+ efflux
The end result is hyperpolarization of the neuron leading to a decrease in neurotransmitter release
Anatomical distribution of opioid receptors
Broadly distributed in CNS
Peripheral sensory neurons
Others:
pituitary, small intestine, vas deferens, possibly elsewhere
There is not a particular correspondence between specific endogenous opioid peptides and specific opioid receptors (except possibly dynorphin and k receptors)
Summary of the Endogenous Opioid System
Endogenous opioid peptides
Enkephalins
Dynorphins
B-endorphin
Opioid receptors



Main effect is to inhibit neurotransmitter release (i.e., other neurotransmitters like substance P)
g protein coupled receptor
picture of the endogenous opiod system
Acute pain
The first component in the perception of pain
Sensory
Stimulation of pain receptors
Transmitted from sensory neurons to the CNS via the Ascending Pain Pathway
Is modulated via the Descending Pain Pathway and at Peripheral Nerve Endings
The second component in the perception of pain
Psychological (“affective”)
Related to a person’s state of mind which is modulated by many intrinsic and extrinsic factors
Chronic pain
Neuropathic pain
A FEW EXAMPLES OF PROTOTYPICAL OPIOID DRUGS
Because of the many effects in which endogenous opioid receptors are involved, opioid drugs have many clinical applications, the primary one being as an analgesic. In addition, opioids are used for preoperative sedation, antidiarrheal medications, cough suppression, replacement therapy for opiate dependence, treatment of opiate overdose, and reversal of opiate-induced respiratory depression. In addition to the therapeutic effect being sought, the specific drug used will depend on such factors as intended time of duration, desired magnitude of effect (potency), ease of administration, and the presence of additional health problems (for example, head injury, pulmonary disease, asthma). The following is a brief description of but a few of the more commonly used therapeutic opioids.
Clinical Uses of Opioid Drugs
Analgesia
Preoperative sedation
Antidiarrheal
Cough suppression
Replacement therapy for opioid dependence
Opioid overdose or reversal of opioid-induced respiratory depression (antagonists)
Pentazocine
Partial agonist; unique structure
Less constipation, less nausea and vomiting than morphine
Pentazocine clinical uses
Premedication and supplement to surgery
Pentazocine SE
Heavy sedation
Psychotomimetic effects
Increased heart rate and cardiac load
Epilepsy
Psychosis
Naloxone
Pure antagonist; morphine analogue
Half-life of 1 hour; must be repeatedly administered
Reduced oral bioavailability

doesn't activate the receptor just prevents other ligand from binding it
Naloxone clinical uses
Reversal of opioid overdose
Naloxone SE
“Overshoot” in opioid dependent patients

the patien is tolerant and therefore sensitive to the blocking affect and the endogenous ligand (which is reduced) and the drug are being blocked so can into withdrawl
Dextromethorphan
Agonist
2-fold less potent than codeine
OTC
Clinical uses:
Antitussive