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rhodes 3b
opioid analgesics and antagonists
| Question | Answer |
|---|---|
| What's a "true" narcotic? | having a tendance to induce narcosis/hypnosis |
| How do you get an opiate? | plant alkaloid (or synthetic modification) from Opium Poppy |
| There are four chemical classes of Opioids: | Natural "ine", Semi-synthetic {ET phone home}, Synthetic "phine, phene, fent, nyl, nil" and SYNTHETIC ANTAGONISTS |
| 2 Natural analgesics | codeine, morphine |
| other NATURAL medication used for vasospasm | papaverine |
| other NATURAL medication that's the precursor for development of many other opioids | thebaine |
| 4 semi-synthetic analgesics | hydrocodone (vicodin); hydromorphone (dilaudid); oxycodone (Percodan, percocet); oxymorphone (numorphan) |
| 1 OTHER semi-synthetic drug | Heroin (diacetylmorphine) |
| 8 Synthetic analgesics (that end in "phine or phene") and 4 that end in "fent, nyl or nil" | BUTORPHANOL (stadol); bupremorphine (buprenex); levorphanol (levo-dromoran); MEPERIDINE; METHADONE; nalbuphine (nubain); PENTAZOCINE (talwin); PROPOXYPHENE (darvon); Fentanyl, sufentanil, alfentanil, remifentanil |
| 3 other synthetic drugs: | diphenoxylate; loperamide; dextromethorphan |
| 3 synthetic antagonists | nalmefene (revex); naloxone (narcan); naltrexone (revia) |
| What's alvimopan (Entereg)? | a miu opioid antagonist that's used after bowel surgery (opioid receptor blacker) |
| What's methylnaltrexone (Relistor) | treats constipation or ileus caused by opioids |
| What't pain? | distressing feeling: burning, aching, throbbing, sharp, dull |
| What are the 5 receptors involved? | Opioid, GABA, NMDA, tachykinin and bradykinin |
| Pain receptors: Where are most of them and where's the arousal center | skin; brain (RAS) |
| Name the three opioid peptides: | Endorphins, Enkephalins, Dynormphins |
| There are 3 opioid receptor subtypes: name the first one, it's function and it endogenous opioid peptide affinity | (Mu)EUPHORIA & DEPENDENCE, spinal analgesia, sedation, inhib of resps, slowed GI - Endorphins > enkephalins > dynorphins |
| The second one, it's function and it's endogenous opioid peptide affinity | DELTA: spinal analgesia, modulation of hormone and NT release - Enkephalins > |
| The third one, it's function and it's endogenous opioid peptide affinity | KAPPA: spinal analgesia, psychotomimetic effects, slowed gi transit - Dynorphins >> endorphins > enkephalins |
| When are endogenous substances released? | In response to or in anticipation to pain |
| The precursors that give rise to Opioid peptides are made where? | the Pituitary |
| Most opioid analgesics have a DOA of how long? | 2-6 hours |
| Many opioids have effects on which receptor? | Mu |
| Which opioid has effects on MU, DELTA and KAPPA? | Sufentanil |
| Which receptors does morphine effect? | Most Mu but also Kappa |
| Which drug has a high affinity to Kappa receptor? | Butorphanol |
| Which other drug has a pretty stong affinity to Kappa receptor? | Nalbuphine (also is Mu antagonist) |
| Overall, how is the oral potency of opioids and why is it that way? | Oral potency is low d/t first pass effect |
| What is the mechanism of excretion? | Metabolism: glucoronidation (more h2o soluble) |
| PHARM EFFECTS OF OPIOIDS: CNS a. Analgesia b. Euphoria c. Sedation d. Respiratory depression | a. better effects on dull, aching pain; b. sense of well being (1st time = great, every subsequent dose is trying to catch up to 1st dose effect) - c. morphine>meperidine>fentanyl - d. medulla; adicts usually don't present w/this d/t tolerance |
| CNS effects cont: e. cough suppres. f. miosis g. emesis h. trunk rigidity | e. codeine, dextromet. f. hallmark sign of opiate toxicity NO TOLERANCE g. activates CTZ chemo triggers (medulla) h. reversed by NM blocker |
| Opioid effects on GI tract: | Constipation (no tolerance) |
| Opioid effects on CVS: | All opioids cause: muscarinic bradycardia |
| Which drug causes a paradoxical, antimuscarinic tacycardia? | Meperidine |
| There are three degrees of tolerance that may develop to some of the effects of the opioids; name them and give a few examples | HIGH: Analgesia, euphoria, mental clouding, sedation, resp depress, n/v, cough suppression - MODERATE: Bradycardia - MINIMAL: Miosis, constipation, convulsions |
| Hospice patients may develop what degree of tolerance? | Minimal or none |
| SOME SPECIFIC AGENTS: What is a precursor that is metabolized to morphine and has antitussive effects? | Codeine |
| What's Darvon used in combo with? | Aspirin and acetaminophen |
| Tell a little about Talwin and Talwin N | Talwin - IV also: Talwin N is oral form which gets metabolized 1st pass effect - not effective if crushed up into IV form d/t it's quaternary form - IV drug users try to crush opioid tablets and try to use IV (this specific drug they're unable) |
| What's Heroin metabolized to? | Morphine |
| What are the triad of symptoms in acute opioid toxicity? | Pinpoint pupils, resp depression, pul edema, coma |
| What are some other symptoms of toxicity? | hypotension, icp, constipation, urinary retention, itching(more common w/ natural opioids rather than synthetics) |
| What's the treatment for Opiate toxicity? | Opioid antagonist (narcan, etc) |
| Narcotic abuse and treatment: what three things can be done? | 1. transf to an oral prescription w/ gradual dose reduction (methadone, buprenorphine + nalaxone= subonone 2. Clonidine (A2 agonist) - decreases w/d response but not cravings 3. electrostimulation techniques |
Created by:
kelbj819
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