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Pharm1 Test2 Opioids Barry University

Where are mu-Receptors located? Mainly found in the brainstem and medial thalamus. Some located in spinal cord.
Where are the kappa-Receptors located? Mainly in the dorsal horn of the spinal cord and some in the brainstem medullary reticular formation.
Where are the delta-Receptors located? Mainly in the limbic system.
Where are the sigma-Receptors located? Mainly in the hippocampus and amygdala of the limbic system.
What are the functions of the mu-Receptor? analgesia, respiratory depression, euphoria, miosis, physical dependence, decreased GI motility.
What are the functions of the kappa-Receptor? supraspinal analgesia, sedation, dysphoria (psychoses).
What are the functions of the delta-Receptor? analgesia (spinal?).
What are the functions of the sigma-Receptor? dysphoria, hallucinations.
From what substance are endogenous opioids derived? precursor polypeptides
What are the three types of endogenous opioids? endorphins, dynorphins, and enkephalins.
All endogenous opioids differ in length, but what do they have in common? The first few (61-65) amino acids.
What are endomorphines? newly discovered m-receptor selective tetrapeptides.
As the body's main painkillers, what are the three modes of action of endogenous opioids? They act as neurotransmitters, neuromodulators, or neurohormones.
About how much homology exists among opioid receptors mu, kappa, and delta? About 65%.
Where are the receptors that mediate analgesia located? Dorsal horn of the spinal cord, periaqueductal gray matter, and the thalamus.
What do opioid receptors in the ventral brainstem do? Mediate effects on coughing, vomiting, respiration, and pupillary diameter.
Where are opioid receptors that control neuroendocrine function located? In the hypothalamus.
Where are opioid receptors that control mood and behavioral effects located? Mainly in the limbic system.
What receptors mainly affect the GI tract and where are they located? Peripheral mu-Receptors.
Agonist: bind to and activate receptor.
Antagonist: binds to the receptor, but does not activate it.
Partial Agonist: binds to the receptor, but produces less than maximal response.
Mixed Agonist/Antagonist: binds to more than one type of opioid receptor, acting as an agonist at one, and an antagonist at others.
In the CNS, where do opioids primarily act? brainstem/spinal cord
In the PNS, where do opioids primarily act? Peripheral afferent neurons.
In what form do opioids bind to receptors? Ionized form
What is the primary mode of action of opioids? decreased neurotransmission by presynaptic inhibition of neurotransmitter release (NE, ACh, DA, SubP)
Opioids act by decreasing neurotransmission by presynaptic inhibition of what neurotransmitters? NE, Ach, DA, SubP (Norepinephrine, Acetylcholine, Dopamine, and Substance P)
How do opioids decrease neurotransmission by inhibiting release of neurotransmitters at the presynapse? Causes increased potassium conductance and/or calcium channel inactivation.
Other than at the presynapse, where do opioids act to decrease neurotransmission? At the postsynapse.
What are the central opioid effects? Decreased neuronal activity, analgesia, respiratory depression, mood alteration, sedation, miosis, N/V, and endocrine effects.
How do opioids cause analgesia? Raises pain perception threshold and increases pain tolerance?
How do opioids cause respiratory depression? Decreases respiratory center sensitivity to CO2, and can lead to Cheyne-Stokes resp.
What effects do opioids have on the endocrine system? Inhibit LHRH (leutinizing hormone-releasing hormone, aka gonadotropin-releasing hormone)
What are the peripheral opioid effects? Histamine release, venous dilatation, smooth muscle contraction, inhibition of ACh release.
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).
In what way do opioids affect the venous system? besides histaminic component, there is a direct opioid receptor action to cause venous dilatation.
Where do opioids mainly affect smooth muscle contraction? cause contraction in biliary and bladder sphincter muscles.
Where do opioids inhibit ACh release? in mesentery, this decreases peristalsis, and causes constipation.
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).
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).
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.
Opioids distribute well. Which types reach higher CNS concentrations faster? More lipid-soluble opioids reach higher CNS concentrations faster.
What are the implications of opioids on a fetus? Most cross placenta well, but fetus can not metabolize much, so conc. is high.
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.
What are the two chemical classes of opium alkaloids? Phenanthrenes and benzolisoquinolines.
What is the structure of phenanthrenes? 4 ring-system with a tertiary amine with pKa of >8.0, so mostly ionized at physiologic pH
Levo isomers of phenanthrenes are more active. What are the three levo isomers of phenanthrenes? Morphine, codeine, and thebain.
The benzolisoquinolines lack standard opioid activity. What are the two benzolisoquinolines? Papavarine and noscapine.
Papavarine is a benzolisoquinoline. What does it do? a smooth muscle relaxant – phosphodiesterase inhibitor, increases cAMP.
Noscapine is a benzolisoquinoline. What does it do? antitussive and anticancer(?) – sigma-activity?
What are the three opioid agonists that begin with the letter "M?" Morphine(MS Contin), Meperidine(Demerol), Methadone(Dolophine).
What are the three opioid agonists that begin with the letter "H?" Hydromorphone(Dilaudid), Hydrocodone (Vicoden), and Heroin.
What are the three opioid agonists with "fent" in their names? Fentanyl (Sublimaze), Sufentanil(Sufenta), and Alfentanil(Alfenta).
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
A natural alkaloid, Morphine is derived from what plant? Papaver somniferum.
At what receptors does Morphine act? Primarily mu (some kappa).
True or false: It takes a long time to develop tolerance to Morphine. False. Morphine users quickly develop tolerance.
There has been a recent resurgence in the use of Morphine. What is it most commonly used for? Analgesia.
What is the chemical name of Heroin? Diacetylmorphine
Heroin is a synthetic compound. How is it prepared. Easily prepared from Morphine.
How does Heroin compare to Morphine? Approximately twice as potent as morphine, but much more lipid-soluble.
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.
How does Codeine compare to Morphine? For analgesia, about 1/10th the potency.
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.
How does Oxycodone(Oxycontin) compare to Morphine? It is about twice as potent as an analgesic.
What drug comes in a 160mg extended release tablet form and is widely abused as "Hillbilly Heroin?" Oxycodone(Oxycontin).
What do idiots do to Oxycodone(Oxycontin) to make it more lethal? Chewing up the extended release form.
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.
What is Dextromethorphan(Dimetane)? A dextro-rotary isomer, which means it has no analgesic activity, but is an effective antitussive.
What is the most widely used synthetic congener? Meperidine(Demerol).
Compare Meperidine(Demerol) to Morphine. Only one-tenth the mg. potency of morphine as an analgesic, and has a shorter duration of action.
Why is Meperidine(Demerol) abuse more difficult to detect? It does not cause miosis.
How can Meperidine(Demerol) cause seizures? Metabolized to Normeperidine, a CNS stimulant. Decreased renal function can allow metabolite build-up, and potential seizures.
What is a contraindication of Meperidine(Demerol)? MAOI therapy.
Compare Methadone(Dolophine) with Morphine. About the same analgesic potency, but Methadone(Dolophine) causes much less sedation.
Why is Methadone used to counter withdrawal symptoms? Longer duration of action, due to slower elimination.
Compare Propoxyphene(Darvon) to Methadone. Structurally related to Methadone, but less than one-tenth as potent per mg.
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.
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).
What is the main advantage of Fentanyl(Sublimaze)? Main advantage is its short half-life of redistribution (12.5 min.).
What common opioid is also used for continuous epidural and transdermal analgesia? Fentanyl(Sublimaze).
What drugs are used similarly to Fentanyl(Sublimaze)? Sufentanil (Sufenta) (800X), Remifentanil (Ultiva) (80X), and Alfentanil (Alfenta) (20X) have similar uses.
Fentanyl(Sublimaze) is often used in conjunction with what? Often combined with other agents for anesthesia such as neuroleptics.
Remifentanyl(Ultiva) is selective to what? Selective mu-Receptor agonist.
How does Remifentanyl(Ultiva) differ from other Fentanyl(Sublimaze) derivatives? Differs from other Fentanyl derivatives by having an ester-linkage.
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.
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.
Compare Etorphine(Immobilion, M99) to Morphine. 1000X Morphine potency.
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.
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(??)
Define Opioid Antagonists: Have receptor affinity but no intrinsic activity.
What receptors do Opioid Antagonists mainly block? Act by blocking mu-Receptors mainly (some kappa blockade also).
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.
What is the clinical use of Opioid Antagonists? Used clinically to reverse opioid-induced respiratory depression and in the treatment of “addicts”.
What is a pure opioid antagonist given IV? Naloxone (Narcan) is a pure antagonist normally given IV.
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).
What is the partial opioid agonist? Buprenorphine (Buprenex) shares structural components of Codeine and Naltrexone.
How does Buprenorphine(Buprenex) work? Binds to mu-Receptors, and elicits a weaker maximal response than other agonists.
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.
What are the mixed opioid agonist/antagonists? Nallorphine(Nalline), Pentazocine(Talwin), and Nalbuphine(Nubain).
What are Nallorphine(Nalline)'s agonist/antagonist properties? Is a mu-Receptor antagonist and a weak agonist at kappa-Receptors.
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.
What are some side effects of large doses of the mixed opioid agonist/antagonist Nallorphine(Nalline)? Large doses may cause dysphoria and hallucinations.
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.
Tramadol(Ultram) is a newer analgesic with similarities to what two drugs? Opioids and NSAIDs.
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.
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.
True or False: Tramadol(Ultram) is similar in strength to Fentanyl? False. Its analgesic strength is similar to Codeine-Acetaminophen agents.
What are some SE of Tramadol(Ultram)? Can cause dizziness, sedation, seizures and hallucinations.
What opioid effects cause its high abuse potential? Euphoria and sedation.
Opioids are physically and (blank) addictive. Psychologically.
What does rapid tolerance mean? Rapid tolerance development means higher and higher doses requires to achieve same euphoria.
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.
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).
What are the three main ways opioids are used in anesthesia? 1. Spinal analgesia/anesthesia 2. Pre-op 3. Surgical adjuvant(assistant).
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.
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.
What is a neuroleptic? A tranquilizer used to treat psychotic conditions when a calming effect is desired.
What is neuroleptic anesthesia? butyrophenone i.e. droperidol – a D2 blocker with antiemetic properties + opioid i.e. fentanyl + nitrous oxide), etc.
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.
Why are peptide-type opioid receptor agonists for pain relief being developed? These are being designed to target specific receptor sub-types.
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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