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50 Cards in this Set

  • Front
  • Back
Name opiod agonists, antagonists, agonist-antagonists
Agonist-Morphine
Antagonist- Naloxone
Agonist-antagonist- Nalorphine
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
Will a patient on morphine respond to a pin prick?
yes
What is the neurophysiology mode of action of opiates
reduces neuronal firing rate
in regions like dorsal horn, periaquiductal gray matter, limbic system, thalamus
Mu receptors
name endogenous ligand and distribution (6)
Ligand- beta-endorphin
Distribution- thalamus, PAG, dorsal horn, accumbens, brainstem (respiration), basal ganglia
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
Delta receptors use what ligand and distribution
Ligand- enkephalin
Distribution- amygdala, accumebs dorsal horn, basal ganglia
NOT in brainsteam
Kappa receptors have what endogenous ligand and distribution?
Ligand-dynorphin
Disribution analgesia areas (thalamus, PAG) basal ganglia
NOT in the brainstem
Of enkephalin, B-Endorphin, and Dynorphin which is the most rapidly degraded?
Enkephalin, its a pentapeptide
Of enkephalin, B-Endorphin, and Dynorphin which is released from pituitary during stress
B-Endorphin
Which opiate is commonly used orally?
Codeine, it is absorbed in GI
Name 6 central effects of Morphine (non-alalgestic)
1- Respiratory Depression
2- Miosis
3-Nausea
4-Anti Tussive
5-Sedation/euphoria
6-Increase in ADH
What are 4 peripheral effects of morphine?
Anti Diarrheal
Decreased Uterus Contraction
Bile (bilosis?)
Orthostatic hypotension
Why does morphine cause respiratory depression?
There are mu receptors in the brainstem nuclei for respiratory control
Name two moderate analgesic opiate agonists
Oxycodone (Percodan) and Meperidine (Demerol)
Name two very weak opiate agonists
Diphenoxylate (lomotil) and Propoxyphene (Darvon)
Name a very strong opiat agonist (mostly used in veterinary setting)
Etorphine (Immobilon)
Name 3 strong opiate agonists
Morphine, Heroin, and Methadone
Which opiate agonist is a useful clinical anti diarrheal?
Diphenoxylate (tradename- Lomotil)
Drug that is as potent as morphine but more orally available?
Methadone (Dolophine)
Which opiate agonist is highly abused by over prescription?
Oxycodone (Percodone)
Name 2 opiod antagonists, which one is oral
Naloxone and Naltrexone (oral)
Name two opiate agonist-antagonists
Nalorphine and Pentazocine
Which opiate antagonist would you use in the Emergency Room for drug OD and which to treat addiction?
Naloxone in the ED bc it is fast acting IV

Naltrexone in addiction bc it's a pill
Why doesn't Pentazocine work that well to treat addiction? What has more success in this setting?
It causes dysphoric side effects

Nalorphine has more success
3 properties usually noticed with addictive drugs
Tolerance
Physical Dependence
Psychological Dependence
As a class the tricyclic antidepressants have this mechanism
Inhibit the reuptake of NE and 5-HT
Monoamina oxidase inhibitors have this mechanism of action
Stop the breakdown of NE, 5HT and DA through inhibition of MOA
Name 3 prominent tricyclic antidepressants
Imipramine
Amytryptiline
Desipramine
Name 3 prominent MAOis
Tranycypramine
Phenezlzine
Isocarboxazid
What is Buproprion used for and how does it work
It's an atypical antidepressant
weak DA, NE uptake inhibitor
What is Mitrazapine used for and how does it work
It's an atypical antidepressant
Increases release of 5-HT and NE
What is Lithium used for and how do we think it works?
Mood stabilizer/anti manic
decreases synthesis and release of DA/NE
Valproate is what type of drug and how does it work?
Anticonvulsant
Sodium Channel blocker that blocks breakdown of GABA
What kind of drug is carbamezepine and how does it work?
Anticonvulsant
Sodium channel blocker
Can be a GABA agonist at some receptors
What is Lamotrigine and how does it work
Anticonvulsant
Sodium channel blocker
blocks glutamate release
Name 3 drugs in the valproate class
Divalproex, Depokate, and Depakene
these are anticonvulsants
Name 2 drugs in the Carbazepine class
Tegretol, Trileptal
These are anticonvulsants
What drug is in the Lamotrigine class
Lamictal
Anticonvulsant
Why do antidepressants take 2-3 weeks to work?
There is a compensatory decrease in firing rate
There can be a downregulation of autoreceptors
What are side effects of TCAs?
Anticholinergic effects- dry mouth, constipation, urinary retention
Alpha 1 blockade-hypotension
Common side effects of SSRI
GI disturbance and insomnia
What kind of drugs potentiate side effects of TCAs?
protein-bound like aspirin or scopolamine
What kind of drugs interfere with metabolism and increase TCA concentration?
Neuroleptics, oral contraceptives
What drugs induce liver enzymes to decrease plasma concentration of TCAs
barbiturates, sedatives, cigarette smoking
Describe a toxic food and drug interaction with MAOis
Hypertensive crisis- the inhibited MAOi cannot metabolize tyramine from diet which promotes release of catecholamines

Treat with alpha blocker like prazosin or phentolamine
What kind of foods need to be monitored on patients taking MAOis
tyramine containing ones like cheese, bananas, liver, smoked fish, avacado, beer/wine, and chocolate
What is the class and action of luoxetine (prozac)
Inhibits reuptake of monoamines
Name 3 SSRIs and their mechanism of action
Sertaline, Paroxetine, and Citolpram
Block 5-HT transporter
Name a SNRI
Duloxetine