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BMS60047
Drugs acting at the Opiod Receptors
| Question | Answer |
|---|---|
| Activators of pain receptors | capsaicin, pH < 7 (increase H ions); increased temperature |
| what are the endogenous pain killers? | enkephaline, endorphine, dynorphine |
| how do the endogenous pain killers work? | they are released and act at the synaptic sites in the dorsal horn and thalamus; they interact with endogenous opioid receptors |
| endorphines (receptor, action, location) | mu-opioid receptor; open K channels leading to hyperpolarization; supraspinal/brain |
| mu-opioid receptor effects | spinal and supraspinal analgesia; euphoria, respiratory depression, bradykardia, constipation, urinary retention, miosis, high addiction potential |
| enkaphalines (receptor, action, location) | delta-opioid receptors, modulate mu-receptor activity; everywhere mu is |
| dynorphines (receptor, action, location) | kappa-opioid receptor; inhibit Ca channels (decrease transmitter release); spinal |
| kappa opioid receptor effects | spinal analgesia; dysphoria, psychoto-mimetic effects; low addiction potential |
| how are the endogenous opioid-peptides metabolized? | via neuropeptidases; cleave the amino-terminal tyrosine residue (have ultra short t1/2) |
| morphine (receptor, effects, metaboilism, t1/2; analgesic potency) | mu agonist; histamine release (itching), activates dopamine receptors (emesis); hepatic metab to M6G; t1/2 = 3 h; analgesic potency = 1 |
| piritramid | morphine with less SE (less histamine release), 0.8 Mo |
| codeine | hepatic metabolism (3A4 & 2D6) to 10% morphine; analgesic potency 1/10 Mo |
| tramadol (metabolism, receptor, mode of action) | 2D6 metabolism to mu-opioid agonist; NaSRI; alpha-2-agonist (clonidine-like); slows you down |
| pentazocine | kappa agonist, weak mu antagonist; can cause withdrawal syndrome in morphine abuser |
| methadone | mu agonist and NMDA antagonist (double analgesic); slow onset and variable t1/2; active metabolite with long t1/2; accumulation/sedation; 4-12 Mo |
| what are the i.v. opioids in decreasing order of potency? | morphine (10^0); alfentanil (10^1); fentanyl (10^2); remifentanil (10^2); sufentanil (10^3) |
| what is the mode of action of the i.v. opioids? | selective mu agonists |
| which of the i.v. opioids is the shortest acting? | remifentanil is ultra short (infusion) |
| meperidine/pethidine (analgesic potency, t1/2, metabolite, actions, effects) | 1/10 Mo; short t/12; normeperidine (1/20 Mo) is neurotoxic and accumulates (renal insufficiency); anticholinergic, SSRI, alpha-blocker; interacts with MAO-I; post-anesthetic shivering |
| naloxone | opioid antagonist; used for respiratory depression |
| what are the 3 things that can result in emesis? | activation of GIT afferent 5HT3; activation of dopamine receptors in CRTZ zone; activation of vestibular-nucleus which activates muscarin (acts on CRTZ) |
| what are the 3 ways one can stop emesis? | use a 5-HT3 blocker; use a dopamine2 blocker; use a muscarin-blocker |
| -setron | 5-HT2 antagonist |
| droperidol (DHB) and metoclopramid | D2 antagonist; 5-HT3 antagonist, 5-HT4 agonist |
| scopolamine | muscarine antagonist; only good for sea-sickness/ motion induced sickness |
| atropine | ROSA; not useful for vomiting; can induce bradycardia at very low doses |
| central anticholinergic syndrome | occurs from overdose of anticholinergic drug; dry as a bone (lack of perspiration), hot as a hare (body temp increases), red as a beet (periphery dilates), blind as a bat (lose ability to accommodate), mad hatter |
| poisoning of AChesterase inhibitor | Diarrhea, Urination, Miosis, Bronchorrhea/Bronchospasm, Bradykardia, Emesis, Lacrimation, Laxation, Salivation |
| diphenhydramine | H1-blocker (1st gen); anticholinergic; sleeping pill, also used for motion sickness (antimuscarinic) |
Created by:
cbart004
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