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45 Cards in this Set
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Medication Overuse Headache - MOH
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“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 |
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best way to get rid of MOH
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stop using meds cold turkey
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#1 medication that causes MOH (know)
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excedrin for migraine
it is the most overused |
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scotomata
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aura term
hazy or lost vision visual field is cut |
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Narcotic
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drug that induces stupor or insensibility
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opiate
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naturally-occurring alkaloids found in the opium poppy
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opiopeptidins
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endogenous neurotransmitter peptides that exhibit opiate-like activity
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opioids
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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 |
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nociceptions
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the perception of traumatic stimuli
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analgesia
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the absence of sensibility to pain or the relief of pain
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First endogenous opioid peptides were discovered
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40 years ago and act as agonists on endogenous opioid receptors
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Opiates and synthetic opioid drugs are either .....
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agonists, partial agonists, or antagonists of endogenous opioid receptors
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Endogenous opioid peptides Implicated in many bodily functions including:
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Analgesia
Modulation of stress and anxiety Regulation of hormonal functions Thermoregulation Maintain homeostasis |
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Endogenous Opioid Peptides
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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).
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The three opioid peptide gene families are:
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Proenkephalin
• Leu-enkephalin, Met-enkephalin (generally referred to simply as “enkephalin”) |
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common structure of opioids
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try-Gly-Gly-Phe-Met/Leu
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The Anatomical distribution of opioid peptides:
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what are the smallest opioid peptides
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met and leu enkephalin
5 amino acids long and differ in the terminal amino acid met and leu |
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Opioid Receptors
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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.
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are opioid receptors inhibitory or stimulatroy
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inhibitory
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Opioid receptors are inhibitory and cause
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There are at Least 8 Different Opioid Receptor Subtypes
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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) |
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•Opioid receptor subtypes: that are important pharmocologically
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Anatomical distribution of opioid receptors
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What determines the specific effects of endogenous and exogenous opioid ligands?
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pain
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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. |
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Opioid Receptors are Inhibitory
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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 |
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Anatomical distribution of opioid receptors
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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) |
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Summary of the EndogenousOpioid System
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Endogenous opioid peptides
Enkephalins Dynorphins B-endorphin Opioid receptors Main effect is to inhibit neurotransmitter release (i.e., other neurotransmitters like substance P) |
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g protein coupled receptor
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picture of the endogenous opiod system
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Acute pain
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The first component in the perception of pain
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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 |
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The second component in the perception of pain
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Psychological (“affective”)
Related to a person’s state of mind which is modulated by many intrinsic and extrinsic factors |
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Chronic pain
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Neuropathic pain
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A FEW EXAMPLES OF PROTOTYPICAL OPIOID DRUGS
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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.
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Clinical Uses of Opioid Drugs
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Analgesia
Preoperative sedation Antidiarrheal Cough suppression Replacement therapy for opioid dependence Opioid overdose or reversal of opioid-induced respiratory depression (antagonists) |
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Pentazocine
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Partial agonist; unique structure
Less constipation, less nausea and vomiting than morphine |
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Pentazocine clinical uses
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Premedication and supplement to surgery
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Pentazocine SE
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Heavy sedation
Psychotomimetic effects Increased heart rate and cardiac load Epilepsy Psychosis |
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Naloxone
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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 |
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Naloxone clinical uses
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Reversal of opioid overdose
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Naloxone SE
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“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 |
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Dextromethorphan
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Agonist
2-fold less potent than codeine OTC Clinical uses: Antitussive |