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30 Cards in this Set
- Front
- Back
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Where are opiod receptors found?
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CNS, GI tract, adrenal medulla
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Analgesic efficacy is mediated primarily through which receptor?
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Mu
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What is the MOA of mu receptors?
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7 TM GPCRs that hyperpolarize postsynaptic membranes and decrease presynaptic Ca2+ currents thus blocking or reducing neurotransmission in the pain pathways..
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which opiod receptor, when activated, decreases respiration?
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mu
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which opiod receptor, when activated, can be a psychomimetic?
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kappa
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What is the "reward pathway"?
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mesolimbic dopamine pathway from the ventral tagmental area projecting to the nucelus accumbens and terminating in the prefortal cortex.
- opiod receptors are highly concentrated in the nucleus accumbens. |
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What is the MOA of opioids?
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inhibit ascending pain transmission through the activation of opioids receptors in the dorsal horn AND activate the descending pan control circuits which inhibit the ascending pathway.
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What is the most likely cause of death in opiod overdose?
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respiratory depression
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Which opioid is a full k agonist and u antagonist?
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Nalbuphine (Nubain)
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Which opioid is a partial u agonist and full k agonist?
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Pentacozine (Talwin)
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Which opioid is a partial u agonist and k antagonist?
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Buprenorphine (Buprenex)
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What are the post synaptic and pre synaptic actions of opioids?
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Post-synapse:
- decrease adenyl cyclase - increase K+ Presynapse: decrease Ca2+ |
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What receptor mediates hyperalgesia?
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kappa. (dynorphin ligand)
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What are the preferential endogenous ligands for u, k, and delta?
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u - endorphins
delta -enkephalin k - dynorphin |
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Are tolerance and dependence predictors of addiction?
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NO.
Tolerance- reduced efficacy w/ repeated use Dependence- altered hemostatic balance which leads to withdrawal Addiction- BEHAVIORAL COMPULSIVE act of seeking and using drug. |
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What type of pain responds well to opiods?
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Nociceptive
- neuropathic pain does not. |
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What is the preferred method of giving opioids for labor?
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Spinal - ledd adverse effect!
- Meperidine (Damerol) |
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What drug is given IV for left ventricular failure/Acute pulmonary edema?
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Morphine
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What opioid is used as a cough suppressant and +Chlorpheniramine = Penntuss?
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Codeine
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What CNS effect is indicative on an addict because effect doen't go away?
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Miosis - pinpoint pupils.
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Opioids develop little or no tolerance to what side effects?
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Miosis, Constipation, Convulsant action.
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What drug is contraindicated in CLOSED HEAD INURIES because it increases intercranial pressure?
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Morphine
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What do you use to tx opioid dependent patients?
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Methadone
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What opioid is combined with chlorpromazine for preeclampsia?
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Meperidine
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If antagonist or partial agonist of mu is given to someone dependent on opioids, what happens?
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triggers opioid withdrawal syndrome
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What is the tx use of giving Naloxone + Buprenorphine SUBLINGUAL?
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Detoxification of opioid abuse
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What is the effect of amphetamines and opioid agonists?
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increased analgesia and euphoria
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What is the effect of combining weak opioid agonist and full opioid agonist ?
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weak agonist can antagonize the effects of the stronger agonist leading to DECREASE in analgesic effect
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What is the BEST drug for treating an opioid addict?
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Naltrexone (reVIA) - long action - 48hrs
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Pts comes in with pinpoint pupils, resp. dep, and tracks on arm, what do you do?
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give them Naloxone and monitor!
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