Pharm1 Test2 Opioids Barry University
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| Where are mu-Receptors located? | Mainly found in the brainstem and medial thalamus. Some located in spinal cord.
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| Where are the kappa-Receptors located? | Mainly in the dorsal horn of the spinal cord and some in the brainstem medullary reticular formation.
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| Where are the delta-Receptors located? | Mainly in the limbic system.
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| Where are the sigma-Receptors located? | Mainly in the hippocampus and amygdala of the limbic system.
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| What are the functions of the mu-Receptor? | analgesia, respiratory depression, euphoria, miosis, physical dependence, decreased GI motility.
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| What are the functions of the kappa-Receptor? | supraspinal analgesia, sedation, dysphoria (psychoses).
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| What are the functions of the delta-Receptor? | analgesia (spinal?).
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| What are the functions of the sigma-Receptor? | dysphoria, hallucinations.
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| From what substance are endogenous opioids derived? | precursor polypeptides
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| What are the three types of endogenous opioids? | endorphins, dynorphins, and enkephalins.
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| All endogenous opioids differ in length, but what do they have in common? | The first few (61-65) amino acids.
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| What are endomorphines? | newly discovered m-receptor selective tetrapeptides.
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| As the body's main painkillers, what are the three modes of action of endogenous opioids? | They act as neurotransmitters, neuromodulators, or neurohormones.
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| About how much homology exists among opioid receptors mu, kappa, and delta? | About 65%.
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| Where are the receptors that mediate analgesia located? | Dorsal horn of the spinal cord, periaqueductal gray matter, and the thalamus.
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| What do opioid receptors in the ventral brainstem do? | Mediate effects on coughing, vomiting, respiration, and pupillary diameter.
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| Where are opioid receptors that control neuroendocrine function located? | In the hypothalamus.
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| Where are opioid receptors that control mood and behavioral effects located? | Mainly in the limbic system.
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| What receptors mainly affect the GI tract and where are they located? | Peripheral mu-Receptors.
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| Agonist: | bind to and activate receptor.
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| Antagonist: | binds to the receptor, but does not activate it.
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| Partial Agonist: | binds to the receptor, but produces less than maximal response.
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| Mixed Agonist/Antagonist: | binds to more than one type of opioid receptor, acting as an agonist at one, and an antagonist at others.
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| In the CNS, where do opioids primarily act? | brainstem/spinal cord
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| In the PNS, where do opioids primarily act? | Peripheral afferent neurons.
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| In what form do opioids bind to receptors? | Ionized form
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| What is the primary mode of action of opioids? | decreased neurotransmission by presynaptic inhibition of neurotransmitter release (NE, ACh, DA, SubP)
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| Opioids act by decreasing neurotransmission by presynaptic inhibition of what neurotransmitters? | NE, Ach, DA, SubP (Norepinephrine, Acetylcholine, Dopamine, and Substance P)
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| How do opioids decrease neurotransmission by inhibiting release of neurotransmitters at the presynapse? | Causes increased potassium conductance and/or calcium channel inactivation.
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| Other than at the presynapse, where do opioids act to decrease neurotransmission? | At the postsynapse.
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| What are the central opioid effects? | Decreased neuronal activity, analgesia, respiratory depression, mood alteration, sedation, miosis, N/V, and endocrine effects.
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| How do opioids cause analgesia? | Raises pain perception threshold and increases pain tolerance?
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| How do opioids cause respiratory depression? | Decreases respiratory center sensitivity to CO2, and can lead to Cheyne-Stokes resp.
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| What effects do opioids have on the endocrine system? | Inhibit LHRH (leutinizing hormone-releasing hormone, aka gonadotropin-releasing hormone)
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| What are the peripheral opioid effects? | Histamine release, venous dilatation, smooth muscle contraction, inhibition of ACh release.
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| What are the effects of opioid-induced histamine release? | causes peripheral arteriole and venous dilatation, which can decrease blood pressure (sensitive individuals may enter shock following IV dose).
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| In what way do opioids affect the venous system? | besides histaminic component, there is a direct opioid receptor action to cause venous dilatation.
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| Where do opioids mainly affect smooth muscle contraction? | cause contraction in biliary and bladder sphincter muscles.
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| Where do opioids inhibit ACh release? | in mesentery, this decreases peristalsis, and causes constipation.
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| What are the most common therapeutic opioid uses? | 1. Analgesia – both acute and chronic.
2. Pre-op sedation, anesthesia, epidural analgesia.
3. Diarrhea.
4. Cough suppression.
5. Opioid addiction withdrawal.
6. Opioid overdose (antagonist).
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| What are the major opioid side effects? | 1. Respiratory depression.
2. Nausea and vomiting.
3. Hypothermia.
4. Constipation.
5. Histamine release and its effects.
6. Muscular rigidity due to inhibition of dopamine release in the striatum (Parkinson-like).
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| True or False: While opioids are well absorbed from the GI system, they do not have much first-pass effect. | False. Because they are well absorbed from the GI, most undergo large first-pass metabolism following oral dosing.
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| Opioids distribute well. Which types reach higher CNS concentrations faster? | More lipid-soluble opioids reach higher CNS concentrations faster.
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| What are the implications of opioids on a fetus? | Most cross placenta well, but fetus can not metabolize much, so conc. is high.
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| Metabolism varies among each compound, however all are metabolized to some extent. Where are most metabolites excreted? | Excretion mainly via renal and biliary mechanisms of metabolized forms.
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| What are the two chemical classes of opium alkaloids? | Phenanthrenes and benzolisoquinolines.
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| What is the structure of phenanthrenes? | 4 ring-system with a tertiary amine with pKa of >8.0, so mostly ionized at physiologic pH
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| Levo isomers of phenanthrenes are more active. What are the three levo isomers of phenanthrenes? | Morphine, codeine, and thebain.
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| The benzolisoquinolines lack standard opioid activity. What are the two benzolisoquinolines? | Papavarine and noscapine.
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| Papavarine is a benzolisoquinoline. What does it do? | a smooth muscle relaxant – phosphodiesterase inhibitor, increases cAMP.
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| Noscapine is a benzolisoquinoline. What does it do? | antitussive and anticancer(?) – sigma-activity?
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| What are the three opioid agonists that begin with the letter "M?" | Morphine(MS Contin), Meperidine(Demerol), Methadone(Dolophine).
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| What are the three opioid agonists that begin with the letter "H?" | Hydromorphone(Dilaudid), Hydrocodone (Vicoden), and Heroin.
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| What are the three opioid agonists with "fent" in their names? | Fentanyl (Sublimaze), Sufentanil(Sufenta), and Alfentanil(Alfenta).
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| List all opioid agonists: | Morphine(MS Contin), Hydromorphone(Dilaudid), Oxymorphone,
Codeine, Hydrocodone(Vicodin), Oxycodone (Oxycontin), Heroin, Levorphanol(Levo-Dromoran), Dextromethorphan,
Meperidine(Demerol), Methadone,
Propoxyphene(Darvon), Fentanyl,
Sufentanil, Alfentan
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| A natural alkaloid, Morphine is derived from what plant? | Papaver somniferum.
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| At what receptors does Morphine act? | Primarily mu (some kappa).
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| True or false: It takes a long time to develop tolerance to Morphine. | False. Morphine users quickly develop tolerance.
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| There has been a recent resurgence in the use of Morphine. What is it most commonly used for? | Analgesia.
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| What is the chemical name of Heroin? | Diacetylmorphine
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| Heroin is a synthetic compound. How is it prepared. | Easily prepared from Morphine.
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| How does Heroin compare to Morphine? | Approximately twice as potent as morphine, but much more lipid-soluble.
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| Heroin is not approved for clinical use due to high addiction probability. It enters the CNS quickly to cause euphoria due to what property? | High lipid-solubility.
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| How does Codeine compare to Morphine? | For analgesia, about 1/10th the potency.
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| Codeine is a potent antitussive and has little risk for addiction or respiratory depression. What accounts for its analgesic qualities? | It is partially converted to Morphine in the body.
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| How does Oxycodone(Oxycontin) compare to Morphine? | It is about twice as potent as an analgesic.
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| What drug comes in a 160mg extended release tablet form and is widely abused as "Hillbilly Heroin?" | Oxycodone(Oxycontin).
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| What do idiots do to Oxycodone(Oxycontin) to make it more lethal? | Chewing up the extended release form.
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| Levorphanol(Levo-Dromoran) is a congener of Morphine, which means it is in the same chemical class. How do they compare? | Very potent synthetic morphine analgesic congener (5X). Less constipating and longer lasting.
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| What is Dextromethorphan(Dimetane)? | A dextro-rotary isomer, which means it has no analgesic activity, but is an effective antitussive.
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| What is the most widely used synthetic congener? | Meperidine(Demerol).
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| Compare Meperidine(Demerol) to Morphine. | Only one-tenth the mg. potency of morphine as an analgesic, and has a shorter duration of action.
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| Why is Meperidine(Demerol) abuse more difficult to detect? | It does not cause miosis.
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| How can Meperidine(Demerol) cause seizures? | Metabolized to Normeperidine, a CNS stimulant. Decreased renal function can allow metabolite build-up, and potential seizures.
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| What is a contraindication of Meperidine(Demerol)? | MAOI therapy.
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| Compare Methadone(Dolophine) with Morphine. | About the same analgesic potency, but Methadone(Dolophine) causes much less sedation.
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| Why is Methadone used to counter withdrawal symptoms? | Longer duration of action, due to slower elimination.
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| Compare Propoxyphene(Darvon) to Methadone. | Structurally related to Methadone, but less than one-tenth as potent per mg.
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| Propoxyphene(Darvon) has properties similar to other Opioid analgesics. Why has its benefit been questioned? | Questions have been raised concerning its benefit in dose strengths found in most products.
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| Fentanyl(Sublimaze) is chemically related to Meperidine. Compare Fentanyl(Sublimaze) to Morphine. | Approximately 80X as potent an analgesic as Morphine (similar potency among its other effects also).
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| What is the main advantage of Fentanyl(Sublimaze)? | Main advantage is its short half-life of redistribution (12.5 min.).
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| What common opioid is also used for continuous epidural and transdermal analgesia? | Fentanyl(Sublimaze).
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| What drugs are used similarly to Fentanyl(Sublimaze)? | Sufentanil (Sufenta) (800X), Remifentanil (Ultiva) (80X), and Alfentanil (Alfenta) (20X) have similar uses.
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| Fentanyl(Sublimaze) is often used in conjunction with what? | Often combined with other agents for anesthesia such as neuroleptics.
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| Remifentanyl(Ultiva) is selective to what? | Selective mu-Receptor agonist.
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| How does Remifentanyl(Ultiva) differ from other Fentanyl(Sublimaze) derivatives? | Differs from other Fentanyl derivatives by having an ester-linkage.
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| How does Remifentanyl(Ultiva)'s ester-linkage cause its short duration of action? | Causes short duration of action due to hydrolysis by non-specific esterases.
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| What are the benefits of Remifentanyl(Ultiva)? | This allows an agent of short duration that can be more carefully titrated to needs and allows rapid recovery.
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| Compare Etorphine(Immobilion, M99) to Morphine. | 1000X Morphine potency.
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| Why is Etorphine(Immobilion, M99) is a large animal immobilizer. Why is it veterinary use only? | Toxic to humans, one drop on skin can be fatal.
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| What relative of Etorphine(Immobilon, M99) is used on humans in China? | Dihydroetorphine used in China as a painkiller, it appears to be less addictive(??)
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| Define Opioid Antagonists: | Have receptor affinity but no intrinsic activity.
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| What receptors do Opioid Antagonists mainly block? | Act by blocking mu-Receptors mainly (some kappa blockade also).
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| What actions do Opioid Antagonists usually block? | Blocks analgesic, respiratory, euphoric, miosis, hypotension, and smooth muscle actions of the Opioids and endogenous b-endorphin and enkephalins.
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| What is the clinical use of Opioid Antagonists? | Used clinically to reverse opioid-induced respiratory depression and in the treatment of “addicts”.
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| What is a pure opioid antagonist given IV? | Naloxone (Narcan) is a pure antagonist normally given IV.
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| Compare the opioid antagonist Naltrexone(Trexan) to Naloxone(Narcan). | Naltrexone (Trexan) is similar, but has a longer half-life, and can be given orally (Nalmefene (Revex) too).
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| What is the partial opioid agonist? | Buprenorphine (Buprenex) shares structural components of Codeine and Naltrexone.
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| How does Buprenorphine(Buprenex) work? | Binds to mu-Receptors, and elicits a weaker maximal response than other agonists.
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| Buprenorphine(Buprenex) binds to mu-Receptors and elicits a weaker maximal response than other agonists. How is it used? | It has less abuse potential, and has been used to counteract Heroin and Morphine addiction without causing full-blown withdrawal symptoms.
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| What are the mixed opioid agonist/antagonists? | Nallorphine(Nalline), Pentazocine(Talwin), and Nalbuphine(Nubain).
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| What are Nallorphine(Nalline)'s agonist/antagonist properties? | Is a mu-Receptor antagonist and a weak agonist at kappa-Receptors.
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| What is the outcome of Nallorphine(Nalline)'s antagonism at mu-Receptors and agonism at kappa-Receptors? | While it blocks mu-Receptor-mediated analgesia and euphoria, it also stimulates kappa-Receptor induced analgesia and sedation.
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| What are some side effects of large doses of the mixed opioid agonist/antagonist Nallorphine(Nalline)? | Large doses may cause dysphoria and hallucinations.
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| How do Pentazocine(Talwin) and Nalbuphine(Nubain) compare to Nallorphine(Nalline)? | Pentazocine (Talwin) and Nalbuphine (Nubain) have similar actions, but are stronger kappa mediated analgesics.
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| Tramadol(Ultram) is a newer analgesic with similarities to what two drugs? | Opioids and NSAIDs.
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| True or False: Both the parent compound and an active metabolite have weak affinity for mu-Receptors, however, their analgesic effect is not entirely reversed by Naloxone. | True.
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| In addition to Tramadol(Ultram)'s affinity for mu-Receptors, how else does it cause analgesia? | Also acts to block re-uptake of serotonin and norepinephrine in central synapses, which then decreases pain information transmission in the brain.
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| True or False: Tramadol(Ultram) is similar in strength to Fentanyl? | False. Its analgesic strength is similar to Codeine-Acetaminophen agents.
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| What are some SE of Tramadol(Ultram)? | Can cause dizziness, sedation, seizures and hallucinations.
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| What opioid effects cause its high abuse potential? | Euphoria and sedation.
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| Opioids are physically and (blank) addictive. | Psychologically.
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| What does rapid tolerance mean? | Rapid tolerance development means higher and higher doses requires to achieve same euphoria.
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| Because rapid tolerance causes opioids to become less pleasurable, why do addicts continue to use them? | Many “addicts” only continue to take the opioids to avoid the uncomfortable withdrawal symptoms.
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| In addition to pharmacologic therapy (Methadone), what do many addicts require? | Proper addiction therapy often requires years of psychological therapy as well as pharmacologic therapy (ex.- Methadone).
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| What are the three main ways opioids are used in anesthesia? | 1. Spinal analgesia/anesthesia
2. Pre-op
3. Surgical adjuvant(assistant).
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| Why are opioids used in pre-op? | To decrease pre-surgical pain, surgical pain, and to provide mild sedative effects.
Use allows the amount of general anesthetic required to be decreased.
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| Why are opioids used as surgical adjuvant? | Can be used alone in some cases, or provided with lower doses of other agents such as anesthetics, muscle relaxants, neuroleptics.
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| What is a neuroleptic? | A tranquilizer used to treat psychotic conditions when a calming effect is desired.
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| What is neuroleptic anesthesia? | butyrophenone i.e. droperidol – a D2 blocker with antiemetic properties + opioid i.e. fentanyl + nitrous oxide), etc.
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| What are some future opioid therapeutic possibilities? | Use of peptide-type opioid receptor agonists for pain relief, and transplantation of adrenal medullary chromaffin cells (which secrete opioid peptides) into the spinal subarachnoid space.
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| Why are peptide-type opioid receptor agonists for pain relief being developed? | These are being designed to target specific receptor sub-types.
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| Why would you transplant adrenal medullary chromaffin cells into the spinal subarachnoid space? | Because they secrete opioid peptides and could theoretically provide long-term pain relief to chronic pain sufferers without exogenous opioid SE’s.
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