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25 Cards in this Set
- Front
- Back
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What is the prototypical example of a member of the opiod analgesic class?
What type of pain does this drug control? |
morphine
moderate/severe pain |
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What are other uses for morphine?
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- cough suppression
- anesthesia - decrease GI motility - adjunct for pulmonary edema - drugs of abuse |
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What are examples of endogenous opiods that are released during stress?
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- endorphins
- enkephalins - dynorphins |
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What is the opiod mechanism?
Name the three different types of receptors/ |
binds to the opiod receptors in the CNS
-Mu -Kappa -Delta |
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What is the difference between the mu, kappa, and delta opiod receptors?
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- mu -- strongest analgesic with the most severe side effects (respiratory depression, constipation, dependence)
- Kappa -- analgesic, less side effects, sedation, psychotic effects - Delta -- analgesic, increases hormone release |
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What is an example of a mixed opioid receptor?
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agonist Kappa and antagonist mu providing less chance of fatality due to respiratory depression
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Opioid bind to _________ receptors.
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opioid G-protein coupled receptors to inhibit afferent pain transmission in ascending pain pathways
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What is opioid's effect on the pain-pathway presynaptic synapses?
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G proteins inhibit calcium entry and cAMP release which causes less NT release (calcium required for NT release)
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What is opioid's effect on the pain-pathway post-synaptic synapses?
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G proteins open K+ channels (lose K+) and hyperpolarize the membrane making it harder to excite the neuron
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How does the opioid activate the descending pain control pathways via disinhibition? First, define disinhibition.
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Disinhibition -- normal act is to inhibit, something stops this disinhibition and allows the pathway to occur resulting in less pain sensation
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How are opioids administered?
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some are oral and some are parenteral (IV, epidural, intrathecal, transdermal)
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Where are the opioids metabolized (inactivated)?
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in the LIVER
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What is the important of weaning from a strong mu?
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there is a high risk of dependence so we try to get patient off morphine IV ASAP and move to orals
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Give an example of a strong opioid agonist.
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mu agonist (MORPHINE)
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Give an example of a mild-to-moderate opioid agonist.
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codeine (generic), used for moderate pain, stimulates each of the opioid receptors (lower affinity and efficacy)
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Give an example of a mixed agonist-antagonist opioid.
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stimulate kappa or delta but blocks or only partially stimulates mu
- used for recovery from dependence so mu isn't stimulated - blocks mu from causing a functional change |
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What is an opioid antagonist?
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binds to an opioid receptor without having a functional effect (no effect on respiration)
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What are some adverse affects of opioids as a class?
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sedation, euphoria, respiratory depression (mu receptor), CV problems (OH), GI distress/constipation (comorbidity for SCI patients)
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Define addiction as it relates to opioids.
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compulsive drug use, psychological dependence
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Define tolerance as it relates to opioids.
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increase of a drug dose to have the same functional effect
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Define physical dependence as it relates to opioids.
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onset of withdrawal symptoms if the drug is suddenly stopped
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What are opioid withdrawal symptoms?
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- flu-like symptoms
- insomnia - irritability - tachycardia - uncontrollable yawning - muscle aches (PT intervention to treat these) |
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What are 3 problems with opioid drug use?
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1. addiction
2. tolerance 3. physical dependance |
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What is pharmacological treatment for opioid addiction?
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1. use methadone -- strong opioid agonist, has milder withdrawal symptoms than other opioids, used instead of the drug of abuse
2. buprenophine/buprenex -- mixed agonist-antagonist, partially activates mu receptors, stronger agonist for K receptors (some pain control but without the effects of K) |
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What is enzyme induction?
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an increased ability to breakdown drug
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