Term
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Definition
Mu receptor agonist
Crosses BBB - CNS effects in brain
Poor lipid solubility, 60% charged
Slow onset (4hours), 2hr half life
Accentuates inhibitory system
Analgesia, euphoria, RR depression, sedation, urinary retention
Metabolism:
M-6 glucuronide - 10x active
M-3 glucuronide - inactive
Liver disease has little effect
RENAL effects are significant due to M-6
3xOral = IV dosage
Can dose into spinal cord - side effects are dampened |
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Term
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Definition
5x more potent than morphine, faster onset
IV or oral
H-6 glucuronide is less active than M-6
H-3 is still inactive
Greater euphoria, greater risk of abuse |
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Term
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Definition
CYP2D6 metabolism in liver (prodrug)
Prodrug metabolized to hydromorphone
Given w/ acetamenophin (Vicodin/Lortab) |
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Term
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Definition
CYP2D6 metabolism in liver (prodrug)
Prodrug metabolized to oxymorphone
Given w/ acetamenophin (Percocet)
Available in extended release |
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Term
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Definition
CYP2D6 metabolism in liver to morphine (prodrug)
Given with acetaminophen
Weak/mild analgesia |
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Term
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Definition
DO NOT USE
Prodrug converted to morphine
W/ acetaminophen (Darvocet) |
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Term
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Definition
Diacetyl Morphine
Very lipid soluble
Converted to morphine in the brain and monoacetyl morphine via deacetylation
Rapid onset |
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Term
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Definition
Oral - nonactive half metabolite
VERY long half life - 15-60 hrs
Drug addiction treatment, mild pain management |
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Term
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Definition
Oral/IV (Demerol) - active metabolite
Lipid soluble, fast onset
10x less potent than morphine
(7.5mg morphine = 75 meperidine)
Liver -> nor-meperidine (CNS/convulsions)
Nor-meperidine - severe effects with KIDNEYS
Side effects with MAOIs - seretonin syndrome (clonus, hyperactive autonomics, mental status effect) |
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Term
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Definition
Patch for chronic pain
Oral - lollipop or sublingual
Epidural
Non-active metabolite |
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Term
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Definition
Mixed agnoist/antagonist
Partial mu agonist and monoamine (seretonin/NE) uptake inhibitor
w/ acetaminophen
Mild/moderate pain |
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Term
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Definition
Mixed agnoist/antagonist at mu receptors
kappa agnoist
mu agnoist/antagonist
opioid
NOT for chronic pain, only short term and managing side effects |
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Term
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Definition
Mixed agnoist/antagonist at mu receptors
kappa agnoist
mu agnoist/antagonist
opioid
NOT for chronic pain, only short term and managing side effects |
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Term
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Definition
Mixed agnoist/antagonist at mu receptors
kappa agnoist
mu agnoist/antagonist
opioid
NOT for chronic pain, only short term and managing side effects |
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Term
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Definition
Mixed mu agonist/antagonist
High agonist affinity for mu, some for kappa
Used for addiction: difficult to reverse agonist, inhibits analgesia for surgery |
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Term
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Definition
Opioid agnoist
Antidiarrheal |
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Term
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Definition
Opioid agonist
antidiarrheal (imodium) |
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Term
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Definition
Opioid antagonist - save lives
Parenteral |
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Term
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Definition
Opioid antagonist - save lives
Oral |
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Term
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Definition
Opioid antagonist - Oral
Poorly absorbed - good for GI side effects of opioids |
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