Term
| What are the endogenous opiods of our nervous system? |
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Definition
| endorphins, dynorphins (A and B), and leu-enkephalin |
|
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Term
| What protein gives rise to endorphins? |
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Definition
|
|
Term
| What protein gives rise to leu-enkephalin? |
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Definition
|
|
Term
| What protein gives rise to dynorphins? |
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Definition
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Term
| Activation of what receptor is responsible for the therapeutic and side effects of morphine? |
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Definition
|
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Term
| What two nerve membrane channels does morphine affect? What second mesenger signaling molecule? |
|
Definition
| potassium (increased opening) and calcium (reduced opening) -> decreased nerve transmission; Adenylate cyclase is inhibited |
|
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Term
| Which receptors mediate the psychotomimetic effects of opiate analgesics? do endogenous opiods activate them as well? |
|
Definition
| sigma and phencyclidine receptors; no |
|
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Term
| Which receptors are responsible for the antitussive effect of codeine |
|
Definition
|
|
Term
| How are codeine and heroin related to morphine? |
|
Definition
| they are prodrugs that are converted into morphine |
|
|
Term
| what is allodynia and what cuases it? |
|
Definition
| pain caused by previously innocuous stimuli due both to perihperal sensitization and to longer term changes in spinal mechanisms |
|
|
Term
| What are the sites for opiate analgesia? |
|
Definition
| primary afferents (peripheral nociceptors); opiod interneurons in dorsal horn of spinal cord (they gate nociceptive inputs) |
|
|
Term
| Thinking about the sites where morphine and opiod analgesics are active, what are the implications in terms of how you'd administer opiates? |
|
Definition
| intrathecally or epidural routes |
|
|
Term
| How come TCAs and SSRIs are able to potentiate opiate analgesia? |
|
Definition
| there are descending pathways from pons that potentiate spinal analgesia that use serotonin and noradrenaline as NTs |
|
|
Term
| What role do PGE2 and PGI2 play in the role of pain? |
|
Definition
| they sensitive the peripheral nerve endings |
|
|
Term
How does morphine affect:
consciousness;
Other sensory modalities;
dull & shrap intermittent pain;
affective (suffering) component of pain |
|
Definition
Occurs w.out loss of consciousness;
other sesnory modalities less altered;
continusous dull > sharp intermittent;
alleivates snesory and affective component |
|
|
Term
| What are morphines physiologic actions? |
|
Definition
| Morphine gives you one "HECC of a DREAM" Hisamine and Hormonal actions; Emesis; Contraction of biliary smooth muscle (biliary colic) and Cardiovascular changes (hypotension); Decreased cough reflex, Decreased GI motility, Depression of mental functioning; Respiratory depression; Eurphoria; Analagesia; Miosis |
|
|
Term
| Why is it dangerous to administer oxygen to a person under morphine administration? |
|
Definition
| Morphine depresses the brain-stem respiratory generator, so respiration becomes soley dependent on the carotid chemoreceptors which are stimulated by HYPOXIA and a higher than normal PCO2 to keep respiration going. |
|
|
Term
| What are pin point pupils a sign of? |
|
Definition
| possible morphine toxciity (due to central effect on EW nucleus of oculomotor nerve) |
|
|
Term
| How would you treat hypoxia in an overdose morphinated patient? |
|
Definition
| ventilation only (administering oxygen will decrease respiratory drive) |
|
|
Term
| Name an opiod receptor antagonist |
|
Definition
|
|
Term
| Naloxone is what kind of drug? |
|
Definition
| opiate receptor antagonist |
|
|
Term
| What can naloxone be used for? |
|
Definition
| treatment of morphine overdose |
|
|
Term
|
Definition
|
|
Term
|
Definition
| oral, subcutaenous, IM, IV |
|
|
Term
| How well does morphine penetrate the CNS? What is it about its structure that determines its ability to penetrate? |
|
Definition
| poorly in comparison to other opiod analgesics; it's highly hydroxylated |
|
|
Term
| Metabolism and Excretion: morphine |
|
Definition
| conjugated with glucoronic acid in the liver and excreted via urinary and 10% biliary |
|
|
Term
| What type of tolerance is seen in morphine? |
|
Definition
|
|
Term
| physical dependence: morphine |
|
Definition
|
|
Term
| codeine is what kind of drug? |
|
Definition
| opiod agonst like morphine |
|
|
Term
| hydromorphone is what kind of drug? |
|
Definition
|
|
Term
| oxymorphone is what kind of drug? |
|
Definition
|
|
Term
| oxycodone is what kind of drug? |
|
Definition
|
|
Term
| hydrocodone is what kind of drug? |
|
Definition
|
|
Term
| heroin is what kind of drug? |
|
Definition
|
|
Term
| levorphanol is what kind of drug? |
|
Definition
|
|
Term
| meperidine is what kind of drug? |
|
Definition
| phenylpiperidine drivative opiate |
|
|
Term
| Preferred opiate for obstetrical analgesia? |
|
Definition
| meperidine as it produces less respiratory depression in the newborn |
|
|
Term
| What side fx does meperidine lack compared to morphine? |
|
Definition
| less spasmogenic, less constipation and urine retention, doesn't inhibit coug |
|
|
Term
| Which opiates are virtually insoluble in waterand so can't be administered IV or parenterally? |
|
Definition
|
|
Term
| diphenoxylate is what kind of drug? |
|
Definition
| an opiate that at low doses tx diarrhea and at higher doses show typical opiod activity |
|
|
Term
| fentanyl and sufentanyl are what kinds of drugs? |
|
Definition
|
|
Term
| which opiates are 80x more potent than morphine |
|
Definition
|
|
Term
|
Definition
| long - 15 hrs (compare with morphines 4 hrs) |
|
|
Term
| what kind of drug is methadone? |
|
Definition
| opiate agonist that has identical pharmacology as morphine |
|
|
Term
| How is methadone superior to morphine? |
|
Definition
| oral absorption, larger T 1/2, lesser withdrawal sx |
|
|
Term
| propoxyphene is what kind of drug? |
|
Definition
|
|
Term
| compare effectiveness of propoxyphene and codeine as well as abuse libaility |
|
Definition
| codeine is more effective but greater abuse potential |
|
|
Term
| 1- acetylmethadol is what kind of drug? |
|
Definition
| opiod that produces methadone |
|
|
Term
| What is so special about 1-acetylmethadol? |
|
Definition
| because it can be given as a depot and is structurally modified version of methadone, it is very long lasting and only needs to be admin. ever 2 or 3 days |
|
|
Term
| Pentazocin is what kind of drug? |
|
Definition
|
|
Term
| Mechanism of action: pentazocin |
|
Definition
| weak antagonist a mu receptors, powerful kappa agonist |
|
|
Term
| What are particular side effects of pentazocin? |
|
Definition
| at doses requried to tx intense pain: anxiety, disturbing thoughts, nightmares, hallucinations |
|
|
Term
| T or F: pentazocin can produce analgesia and morphinmimetic fx? |
|
Definition
| when administered alone, yes |
|
|
Term
| T or F: pentazocin reduces morphine analgesia (but not its respiratory depression) |
|
Definition
| true. it can precipitate withdrawal sx in morphine tolerant individuals |
|
|
Term
| buprenorphine is what kind of drug? |
|
Definition
|
|
Term
| naloxone is what kind of drug? |
|
Definition
|
|
Term
| naltrexone is what kind of drug? |
|
Definition
|
|
Term
| Route of administration: naloxone |
|
Definition
| only iv (zero oral bioavailability) |
|
|
Term
|
Definition
|
|
Term
| route of admin: naltrexone |
|
Definition
|
|
Term
|
Definition
| longer than naloxone (b/c oral administered) |
|
|
Term
| dextromethorphan is what kind of drug? |
|
Definition
| antitussive; optical isomer of levorphanol is dextrorphan - this drug is the methoxylated for of dextrorphan |
|
|
Term
| t or f. dextromethorphan has zero analgesic potentcy, zero affinity for opiod receptor, and minimal toxicity? |
|
Definition
|
|
Term
| What are the 3 main criteria in guiding selection of opiod analgesic? |
|
Definition
| type of pain, required duration of action, intensity of pain |
|
|
Term
| Opiods not only act on the CNS but on the... |
|
Definition
| gut! it is sensitive to doses of opiates FAR below those requried to produce analgesia |
|
|
Term
| which opiate can be used a low dose to tx diarrhea? |
|
Definition
|
|
Term
| What are 4 ways to tx opiate abuse? |
|
Definition
| replacement therapy with agonists (methaone, acetyl-methadol); antagonist (naltrexone - longer duration of action); partial agonists (buprenex); clonidine |
|
|
Term
| How does this drug tx opiate abuse: clonidine |
|
Definition
| this is an alpha 2 agonist so it reduces some of the withdrawal effects of opiates by attenuating intesnity of autonomic components and by producing sedation |
|
|
Term
| How does this drug tx opiate abuse: methadone; acetyl-methadol |
|
Definition
| breaks habit of injecting drugs, no withdrawal fear, no buying of illegal drugs, long T1/2 (so less serious withdrawal) |
|
|
Term
| How does this drug tx opiate abuse: naltrexone |
|
Definition
| long last antagonist which can be good during early detoxification phase |
|
|
Term
| How does this drug tx opiate abuse: buprenorphine |
|
Definition
| a u-receptor partial agonist antagonizes high potency agonists but keeps opiate receptors somewhat stimulated |
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