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23 Cards in this Set
- Front
- Back
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Do opioids have a ceiling effect? DO NSAIDs have a ceiling effect?
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1. Opioids do NOT have a ceiling effect while NSAIDs do have a ceiling effect
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Name the opioid receptor families and what responses they facillitate.
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1, Mu- analgesia, resp depression, euphoria/sedation, physical dependance, decrease GI motility, and pupillary constriction
2. kappa- spinal analgesia, sedation, pupil constriction 3. sigma- hallucination, dysphoria |
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Morphine- MOA
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- strong agonist, w/ highest affinity for mu receptors
- inhibits transmission of nocicepetive info from ASCENDING pain pathway - relieves pain by raising the pain threshold at the spinal cord level - alters brains perception to pain |
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Morphine- SE
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- euphoria (mediated by dopamine release)
- resp depression- dec sensitivity of resp center to CO2 - cough reflex depression- morphine and codiene have anti tussive effects - miosis- pinpt pupils - emesis- NOT allergic rxn - GI tract- decreases motility but pt will develop tolerance to these sx - CV- at high doses hypotension and bradycardia - histamine release- vasodilation, sweating, urticaria- may seem like allergic rxn but it is not - hormonal actiong- inc ADH-- urinary retention - labor- prolongs labor by decreasing uterine contractions |
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Morphine- Use, PK, DI
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Use- analgesia, cough, diarrhea
PK- slow and erratic orally. Sig hepatic first pass metabolism, active metabolite--morphine activated by liver and eliminated by kidney. Also crosses placenta DI-MAOIs, TCAs, sedative hypnotics |
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Meperidine- MOA, Use
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- binds to mu and kappa sites, for ACUTE pain
- should NOT be used long term - does not tx cough or diarrhea |
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Meperidine- SE, PK
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- SE: resp depression, constipation, pupil DILATION. accumulation of toxic metabolite-- muscle twitches, convulsions
- PK: SHORTER duration of action than morphine, metabolized by liver to TOXIC metabolite |
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Methadone- Use (diff from morphine), SE, PK
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- analgesia through mu receptor, also used to control withdrawal of addicts
SE: resp depression, constipation, dependance, less euphoria than others, PK better absorption, longer duration of action |
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Fentanyl- PK, Use
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PK: very potent, highly lipophillic, RAPID onset and short duration of action, patch formulation has longer duration of action
Use: anesthesia |
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Hydromorphone- PK, SE
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PK: 10x more potent than morphine in analgesic effect
SE: sig more resp depression, less N & V, itching and constipation |
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hydrocodone and oxycodone- use
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- potency and AE similar to morphine
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codiene- PK, SE
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- less potent analgesia than morphine, low affinity for op receptors, converted to morphine by cyt p450 enzymes ( has polymorphic variability)
SE: much less euphoria Use: anti tussive agent at lower doses, at higher doses analgesia |
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Tramodol- MOA, PK, DI
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- central acting analgesic, binds ot mu receptor and inhibits reuptake of NE and 5HT
- mild to mod severe pain PK: hep metab to active metab, DI: SSRI- can cause serotonin syndrome |
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Tramodol- AE/precautions
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- low seizure threshold
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Mixed agonist-antagonists- use, drugs, which receptors do they work at?
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- teazcine- agonist at kappa receptors, antagonist at mu and sigma receptors
- buprenorphine- partial agonist at mu receptors |
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What are the sx of acute opioid tox? What is the tx?
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- stuporous to coma, low resp rate, low bp, symmetric and pinpt puils, low body temp
- tx: naloxone- comp antag of mu receptors |
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What level of pain should opioids be used? Which is DOC?
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1. moderate to severe pain
2. morphine- dosing and time to pk effect is crucial |
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Peak effect- parenteral, immediate release, sustained/ transdermal patch- initiation of analgesia
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- parenteral- 15-30 min
- immediate release- 1 hr - sustained release- 4 hrs |
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What are the 2 main ways to titrate analgesia?
When converting from IV to oral what should you do w/ dosing? What abt when switching to different opioids? |
1. titrate morphine dose till steady state
2. PCA- pt controlled analgesia w/ 4 hr limit on am tof drug delivered - need more orally - give at lower dose |
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Transdeermal fentanyl- PK
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- absorption is tem dependant- fever increases rate of absorption, subcut fat adn hydration stat dependant
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What is one prophylactic tx that should be given w/ all opioids almost?
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- stool softener b/c constipation is problem w/ all opioids
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W/ chronic opioid tx what needs ot be done to the dosing for the same analgesic effects?
Over what time course will opioid dependance develop? |
1. increase dosing
2. > 7-10 days |
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Is opioid allergy common? When can you dx someone w/ opioid allergy?
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1. is uncommon-- may seem like allergy when its actually just the histamine release
2. after you take a good hx, should use agent from different class |
