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50 Cards in this Set
- Front
- Back
Name opiod agonists, antagonists, agonist-antagonists
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Agonist-Morphine
Antagonist- Naloxone Agonist-antagonist- Nalorphine |
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Name 6 characteristics of Morphine
1-effective for what kind of pain 2- reversed by 3- more effective dull or sharp? 4-selective or non-specific? 5-does or does not alter pain perception 6 blocks |
1-severe pain
2-reversed by naloxone 3-effective on dull pain 4-selective 5-dose NOT alter perception 6-blocks spinal reflex |
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Will a patient on morphine respond to a pin prick?
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yes
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What is the neurophysiology mode of action of opiates
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reduces neuronal firing rate
in regions like dorsal horn, periaquiductal gray matter, limbic system, thalamus |
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Mu receptors
name endogenous ligand and distribution (6) |
Ligand- beta-endorphin
Distribution- thalamus, PAG, dorsal horn, accumbens, brainstem (respiration), basal ganglia |
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Endogenous ligand and distribution of delta receptor (4 regions)
importantly not located in - |
ligand-enkephalin
Distribution: amygdala, accumbens, dorsal horn, BG Importantly NOT in the thalamus or brainstem |
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Delta receptors use what ligand and distribution
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Ligand- enkephalin
Distribution- amygdala, accumebs dorsal horn, basal ganglia NOT in brainsteam |
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Kappa receptors have what endogenous ligand and distribution?
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Ligand-dynorphin
Disribution analgesia areas (thalamus, PAG) basal ganglia NOT in the brainstem |
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Of enkephalin, B-Endorphin, and Dynorphin which is the most rapidly degraded?
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Enkephalin, its a pentapeptide
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Of enkephalin, B-Endorphin, and Dynorphin which is released from pituitary during stress
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B-Endorphin
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Which opiate is commonly used orally?
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Codeine, it is absorbed in GI
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Name 6 central effects of Morphine (non-alalgestic)
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1- Respiratory Depression
2- Miosis 3-Nausea 4-Anti Tussive 5-Sedation/euphoria 6-Increase in ADH |
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What are 4 peripheral effects of morphine?
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Anti Diarrheal
Decreased Uterus Contraction Bile (bilosis?) Orthostatic hypotension |
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Why does morphine cause respiratory depression?
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There are mu receptors in the brainstem nuclei for respiratory control
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Name two moderate analgesic opiate agonists
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Oxycodone (Percodan) and Meperidine (Demerol)
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Name two very weak opiate agonists
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Diphenoxylate (lomotil) and Propoxyphene (Darvon)
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Name a very strong opiat agonist (mostly used in veterinary setting)
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Etorphine (Immobilon)
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Name 3 strong opiate agonists
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Morphine, Heroin, and Methadone
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Which opiate agonist is a useful clinical anti diarrheal?
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Diphenoxylate (tradename- Lomotil)
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Drug that is as potent as morphine but more orally available?
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Methadone (Dolophine)
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Which opiate agonist is highly abused by over prescription?
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Oxycodone (Percodone)
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Name 2 opiod antagonists, which one is oral
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Naloxone and Naltrexone (oral)
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Name two opiate agonist-antagonists
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Nalorphine and Pentazocine
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Which opiate antagonist would you use in the Emergency Room for drug OD and which to treat addiction?
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Naloxone in the ED bc it is fast acting IV
Naltrexone in addiction bc it's a pill |
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Why doesn't Pentazocine work that well to treat addiction? What has more success in this setting?
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It causes dysphoric side effects
Nalorphine has more success |
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3 properties usually noticed with addictive drugs
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Tolerance
Physical Dependence Psychological Dependence |
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As a class the tricyclic antidepressants have this mechanism
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Inhibit the reuptake of NE and 5-HT
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Monoamina oxidase inhibitors have this mechanism of action
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Stop the breakdown of NE, 5HT and DA through inhibition of MOA
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Name 3 prominent tricyclic antidepressants
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Imipramine
Amytryptiline Desipramine |
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Name 3 prominent MAOis
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Tranycypramine
Phenezlzine Isocarboxazid |
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What is Buproprion used for and how does it work
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It's an atypical antidepressant
weak DA, NE uptake inhibitor |
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What is Mitrazapine used for and how does it work
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It's an atypical antidepressant
Increases release of 5-HT and NE |
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What is Lithium used for and how do we think it works?
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Mood stabilizer/anti manic
decreases synthesis and release of DA/NE |
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Valproate is what type of drug and how does it work?
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Anticonvulsant
Sodium Channel blocker that blocks breakdown of GABA |
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What kind of drug is carbamezepine and how does it work?
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Anticonvulsant
Sodium channel blocker Can be a GABA agonist at some receptors |
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What is Lamotrigine and how does it work
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Anticonvulsant
Sodium channel blocker blocks glutamate release |
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Name 3 drugs in the valproate class
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Divalproex, Depokate, and Depakene
these are anticonvulsants |
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Name 2 drugs in the Carbazepine class
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Tegretol, Trileptal
These are anticonvulsants |
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What drug is in the Lamotrigine class
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Lamictal
Anticonvulsant |
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Why do antidepressants take 2-3 weeks to work?
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There is a compensatory decrease in firing rate
There can be a downregulation of autoreceptors |
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What are side effects of TCAs?
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Anticholinergic effects- dry mouth, constipation, urinary retention
Alpha 1 blockade-hypotension |
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Common side effects of SSRI
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GI disturbance and insomnia
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What kind of drugs potentiate side effects of TCAs?
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protein-bound like aspirin or scopolamine
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What kind of drugs interfere with metabolism and increase TCA concentration?
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Neuroleptics, oral contraceptives
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What drugs induce liver enzymes to decrease plasma concentration of TCAs
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barbiturates, sedatives, cigarette smoking
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Describe a toxic food and drug interaction with MAOis
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Hypertensive crisis- the inhibited MAOi cannot metabolize tyramine from diet which promotes release of catecholamines
Treat with alpha blocker like prazosin or phentolamine |
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What kind of foods need to be monitored on patients taking MAOis
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tyramine containing ones like cheese, bananas, liver, smoked fish, avacado, beer/wine, and chocolate
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What is the class and action of luoxetine (prozac)
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Inhibits reuptake of monoamines
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Name 3 SSRIs and their mechanism of action
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Sertaline, Paroxetine, and Citolpram
Block 5-HT transporter |
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Name a SNRI
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Duloxetine
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