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Pharm.Opioids
| Question | Answer |
|---|---|
| the3 different families of opioids | Mu, Kappa, Delta |
| Name of receptors of the 3 families of opioids | Mu1, Mu1, Kappa1, Kappa3, Delta1, Delta2 |
| What is different about the Pro-opiomelanocortin peptides (POMC) (ie B-endorphin) | They can serve as both a hormone and a neurotransmitter. The others are only neurotransmitters |
| primary endogenous opioid for Mu receptors | endomorphins |
| what will bind to Mu, Kappa, and Delta receptors | B-endorphin (promiscuous transmitter) |
| Kappa receptors - think of the _______ | dynomorphins |
| If dynorphin is released from one side of the synapse, you can bet there's a _________receptor on the other side | Kappa |
| For delta receptors, the primary transmitters are the __________ | enkephalins |
| 3 desireable properties of morphine | effective over a wide range of properties (can increase/decrease dose, no ceiling to the effect), + mood, sedation |
| Morphine is named after __________ and so that was the first property of Morphine that was noted | Morpheus who was the God of dreams |
| Adverse affects of Morphine (* indicates desirable/undesirable depending on the treatment) | Sedation*, Mental Clouding, Dysphoria, Constipation*, Dizziness, Nausea and vomiting, Respiratory depression*, Cough reflex depression*, Pruritis |
| With morphine the _______ effect decreases slower than the ______ effect with time | analgesic, sedative |
| With morphine the symptom of ________ goes away fairly quickly - you develop a tolerance and its no longer a problem. | mental clouding, dysphoria, N&V |
| Opioid agonists: Opium alkaloids and derivatives (2) | morphine and codeine |
| T/F using an opioid agonist with time leads to a constipation tolerance (decrease in those symptoms) | false - your always going to have constipation while your taking opioids |
| Great Mu agonist for an antidiarhheal | Loperamide |
| If Loperimide is an opioid why is it over the counter | Does not cross the BBB - only has affects on the gut |
| hyperventilation can be treated with a small dose of ________ | morphine (think respiratory depression) |
| patient gets pruritis from morphine - how are you going to treat | antihistamines |
| Opioids: Two adverse affects your not going to develop a tolerance to (decrease of the affect over time) | constipation, meiosis |
| patient is taking opioids and pees their pants - why | opioids can cause smooth muscle spasms - it can also cause urinary retention! |
| morphine - meiosis or mydriasis | meiosis (mydriasis if withdrawing) |
| at what point is too much morphine too much in the case of tolerance | there is no ceiling |
| T/F - tolerance to opioids is life-threatening | false |
| active metabolite of morphine that accounts for much of the affect attibuted to morphine | morphine-6B-glucuronide |
| inactive metabolite of morphine | Morphine-3B-glucuronide |
| Which patient population would you be careful of when giving morphine | renal failure - the active metabolite (morphine-6B-glucuronide) needs to be cleared through the kidneys - so renal compromise means build-up of the metabolite |
| Definition: cues that a drug is going to be given which leads to the body resisting it (tolerance) | associative/behavioral tolerance |
| Definition: repeatedly stimulate the receptors, they have less and less of an effect on the signaling | Nonassociative/pharmacologic tolerance |
| Definition: if you're tolerant to one Mu agonist, you're tolerant to all the Mu agonists. If you're tolerant to one kappa agonist, you're tolerant to all the kappa agonists. | Cross-tolerance |
| How is the potency of codeine by comparison to morphine | 1/10 the potency of morphine - need much higher doses |
| active metabolite of codeine | morphine |
| For patients without the CYP450 2D6 enzyme - what affect does codeine have | no effect - cant be metabolized into morphine |
| potency of oxycodone by comparison to codeine | 10X - about the same potency as morphine! |
| oxycodone is metabolized by | CYP450 2D6 |
| Controlled release formulation of oxycodone | oxycontin |
| pretty much the same drugs as oxycodone | Hydrocodone and dihydrocodeine |
| Which two drugs are often combined with hydrocodone, dihydrocodeine, and oxycodone? | acetaminophen or ibuprofen |
| why would acetaminophen or ibuprofen be added with an opioid | additive analgesia effect was synergistic |
| heroine by comparison to morphine is _______ potency | 2-4X |
| What is the metabolite of heroine? | morphine |
| Hydromorphone is about _____ more potent than morphine | 8-10X |
| Hydromorphone has a _______ duration than morphine | shorter |
| T/F - hydromorphone is only available IV | False - offered also as a suppository |
| Drug thats considered the same as hydromorphone | Oxymorphone |
| Synthetic opioid compounds (3) | Meperidine, Fentanyl, Methadone |
| merperidine is about what potency when compared to morphine | 1/8th |
| only use for merperidine | post-surgical analgesia |
| who would you never give merperidine to? | recommended not to give it period - but especially to brain damaged or epilepsy patients because the metabolite builds up and can cause seizures |
| Fentanyl is how potent by comparison to morphine | 80 - 100X |
| Fentanyl onset and duration | fast and short |
| What forms of delivery do we have for Fentanyl | IV, patch, oral slow release |
| Anything with fentanyl in the name, check ______ | your doses! |
| what advantage does methadone have over morphine | longer plasma half-life, 4X more potent orally, slow onset (no rush for the druggies), duration of action INCREASES with repeated use |
| Methadone is used for what | treatment of narcotic dependance |
Created by:
mmw562