Term
| What are the opioid receptor subtypes? |
|
Definition
| Mu (1 and 2), kappa (1 and 3), and delta (1 and 2) |
|
|
Term
| What is the kappa 2 receptor? |
|
Definition
| thought to be an opioid receptor but there is no effect when opiates bind |
|
|
Term
| Name the different types of endogenous opioids. |
|
Definition
| pro-opiomelanocortin peptides, pro-enkephalin, prodynorphin, endomorphins |
|
|
Term
| Name the pro-opiomelanocortin peptide that acts as an endogenous opioid? |
|
Definition
|
|
Term
| Name the pro-enkephalin peptides that act as endogenous opiods? |
|
Definition
| met-enkephalin and leu-enkephalin |
|
|
Term
| What are the prodynorphin peptides? |
|
Definition
| dyn-A, dyn-B, and alpha-neo-endorphin |
|
|
Term
| Name the endomorphins that act as endogenous opioids? |
|
Definition
| endomorphin-1 and endomorphin-2 |
|
|
Term
| What endogenous opioid act on mu 1 receptors? |
|
Definition
| endomorphin (beta-endorphin, enkephalin) |
|
|
Term
| What are teh endogenous ligands of the Mu 2 receptors? |
|
Definition
| endomorphin (beta-endorphin) |
|
|
Term
| What are the endogenous ligands of kappa 1 receptors? |
|
Definition
|
|
Term
| What are the endogenous receptors of kappa 2 and 3 receptors? |
|
Definition
|
|
Term
| What are the endogenous ligands of delta 1 receptors? |
|
Definition
|
|
Term
| What are the endogenous ligands of delta 2 receptors? |
|
Definition
|
|
Term
| Name the cloned opiod receptors. |
|
Definition
| MOR, DOR, KOR (aka MOP, DOP, KOP) |
|
|
Term
| Describe the cloned opioid receptors. |
|
Definition
| 7 transmembrane domains, G-protein linked (Gi or Go) to adenylyl cyclase or potassium channels (GIRKS) |
|
|
Term
| What kinds of systemic effects of opioids are measured in in vivo assays using rats? |
|
Definition
| analgesic properties, reinforcing properties, stimulus properties |
|
|
Term
| What are the different ways to measure analgesic effects of opioids? |
|
Definition
| thermal stimuli, tactile stimuli, inflammation, neuropathy |
|
|
Term
| How are reinforcing propterties of opioids measured in rats? |
|
Definition
| self-administration and conditioned place preferance |
|
|
Term
| How are the stimulus properties of endogenous opiods measured? |
|
Definition
| discrimination tasks and addiction research center inventory |
|
|
Term
| What makes morphine a good analgesic? |
|
Definition
| effective over a wide range of doses, effect on mood, sedation |
|
|
Term
| What effects of morphine do you not develop tolerance to? |
|
Definition
|
|
Term
| What are the undesirable properties of morphine as an analgesic? |
|
Definition
| physical/behavior dependence and tolerance, mental clouding, dysphoria, miosis, constipation, N/V, biliary tract spasms, dizziness/circulatory depression, respiratory depression/cough reflex depression, puriritis and rash, ureter and vesical spasms, urinary retention, sexual dysfunction |
|
|
Term
| T/F Small dose of morphine can treat hyperventillation. |
|
Definition
|
|
Term
| WHat effect do opiods have on urination? |
|
Definition
| at low doses you cause urinary retention but at higher and higher doses you start binding the kappa receptor to cause diuresis |
|
|
Term
| What does it mean to have behavioral dependence? |
|
Definition
| person develops drug seeking behavior |
|
|
Term
| In patients taking opioids for a majorly painful symptom for a short while, what percent will become addicted? |
|
Definition
|
|
Term
| Where are the opioid acting on receptors? |
|
Definition
| dorsal horn of the spinal cord, activate descending inhibitory system, peripheral receptors |
|
|
Term
| When are opoids indicated? |
|
Definition
| acute or chronic moderate to severe pain due to surgery, post-surgical pain, or cancer |
|
|
Term
| T/F Morphine is very effective for neuropathic pain. |
|
Definition
| false; opoids are often less effective for neuropathic pain |
|
|
Term
| When are opoids contraindicated? |
|
Definition
| asthma, COPD, apnea, or other breathing disorders, liver or kidney disease, underactive thyroid, curvature of the spine, a history of head injury or brain tumor, epilepsy or other seizures disorder, low blood pressure, gallbladder disease, addison's disease/other adrenal disorders, enlarged prostate, urination problems, mental illness, a history of drug or alcohol abuse |
|
|
Term
| What are teh metabolites of morphine? |
|
Definition
| morphpine-3beta-glucuronide (inactive) and morphine-6beta-glucuronide (active) |
|
|
Term
| Morphine metabolites accumulate in patients with _________. |
|
Definition
|
|
Term
| What's the difference between heroin and morphine? |
|
Definition
| heroion crosses the blood-brain barrier more rapidly than morphine, has 2-4x greater potency than morphine and is actually converted to morphine |
|
|
Term
| What's the difference between hydromorphone and morphine? |
|
Definition
| hydromorphone has 8-10x the potency of morphine, slightly shorter duration than morphine, and available as suppository |
|
|
Term
| How does morphine cause pruritis/rash? |
|
Definition
| psuedoallergic reaction in which morphine causes degranulation of mast cells |
|
|
Term
| What pharmacologic considerations must be taken into account when administering naloxone? |
|
Definition
| short half life and not effective orally |
|
|
Term
| How long do withdrawal symptoms last after you stop taking morphine? |
|
Definition
| starts in 12 hours and lasts for 72 hours |
|
|
Term
| What are the sexual side effects of opioids? |
|
Definition
| females lose desire, males can't orgasm |
|
|
Term
| What is associative tolerance? |
|
Definition
| when your tolerance to a certain amount of drug is dependent upon you taking the drug in the same environment |
|
|
Term
| What drug is similar to hydromorphone? |
|
Definition
|
|
Term
| Hydrocodone is metabolized into ______. |
|
Definition
|
|
Term
| What is oxycodone converted into? |
|
Definition
|
|
Term
| What is the difference between codeine and morphine? |
|
Definition
| about 1/10th the potency of morphine, lower efficacy than morphine, about 10% converted to morphine by CYP 2D6 |
|
|
Term
| Why is codeine ineffective in some patients? |
|
Definition
| 7-10% of patients are poor metabolizers of codeine so it is not efficiently converted into morphine |
|
|
Term
| What opiate must you be careful in giving to northern pacific islanders? |
|
Definition
| codeine because some populations of northern pacific islanders are "super metabolizers" |
|
|
Term
| What's another name for codeine? |
|
Definition
|
|
Term
| What's the difference beween oxycodone and codeine? |
|
Definition
| oxycodone has about 10x the potency of codeine, also metabolized by CYP-2D6 |
|
|
Term
|
Definition
| controlled release formulation of oxycodone |
|
|
Term
|
Definition
|
|
Term
| Name two drugs similar to oxycodone? |
|
Definition
| hydrocodone and dihydrocodeine |
|
|
Term
| What opoids are added to acetaminophen or NSAIDS? |
|
Definition
| codeine, hydrocodone, dihydrocodeine, or oxycodone |
|
|
Term
| What is the logic behind mixing opiods with acetaminophen/NSAIDS? |
|
Definition
| additive or synergistic analgesia without concomitant increase in adverse effects |
|
|
Term
| Name some synthetic compounds that are opioids? |
|
Definition
| meperidine, fentanyl, sufentanyl, alfentanyl, remifentanyl, methadone, L-alpha-acetyl-methadol: LAAM, propoxyphene |
|
|
Term
| What is the difference beween meperidine and morphine? |
|
Definition
| meperidine has 1/8th the potency of morphine, shorter duration, fewer smooth muscle spasms than morphine, no miosis |
|
|
Term
| What are the side effects of demerol? |
|
Definition
| biotransformed to a toxic metabolite that builds up and can cause seizures |
|
|
Term
| What opioid is contraindicated in patients who are poisoned by gila monster venom? |
|
Definition
|
|
Term
| How does fentanyl compare to morphine? |
|
Definition
| 80-100x potency of morphine; fast onset, short duration |
|
|
Term
| How is fentanyl administered? |
|
Definition
| used IV for anesthesia, available as patch (duragesic), and available as oral slow release device (Actiq) |
|
|
Term
| Name the drugs that are derivatives of fentanyl |
|
Definition
| alfentanil, sufentanil, remifentanil, carfentanil, lofentanil |
|
|
Term
| How does methadone compare to morphine? |
|
Definition
| potency similar to morphine for IV administration but 4x more potent orally; long plasma half life |
|
|
Term
| When is methadone indicated? |
|
Definition
| used in treatment of narcotic dependence |
|
|
Term
| What changes about the pharmacokinetics with repeated use of methadone? |
|
Definition
| duration of action increases with repeated use |
|
|
Term
| What is the plasma half life of LAAM? |
|
Definition
| >72 hours; extermely long plasma half-life |
|
|
Term
|
Definition
| suppresses opiate withdrawal for 4-5 days |
|
|
Term
| Why was propoxyphene withdrawn from the market? |
|
Definition
| produces cardiotoxicity and pulmonary edema; active metabolite produces convulsions |
|
|
Term
| Name the opoid antagonists. |
|
Definition
| naloxone, naltrexone, nalmefene |
|
|
Term
| What are the signs of opoid overdose? |
|
Definition
| stuporous or in coma, respiratory rate extremely low, pinpoint pupils, low body temperature, flacid skeletal muscles, jaw relaxed |
|
|
Term
| What are the pharmacokinetic properties of naltrexone? |
|
Definition
| long half life; effective orally or injected but available in oral form only |
|
|
Term
| When are are the indications of naltrexone? |
|
Definition
| used for treatment of dependence |
|
|
Term
| What are the adverse effects of naltrexone? |
|
Definition
| can produce hepatotoxicity with long-term use |
|
|
Term
| What are the pharmacokinetic properties of nalmefene? |
|
Definition
| intermediate duration (4-6 hours) and orally active |
|
|
Term
| Which opioid antagonist has no hepatotoxicity with long term use? |
|
Definition
|
|
Term
| What are mixed agonists-antagonists? |
|
Definition
| nalorphine and cyclazocine, pentazocine, butorphanol, nalbuphine |
|
|
Term
| What effect does nalorphine have on the opioid receptors? |
|
Definition
| kappa 3 receptor agonist and mu receptor antagonist |
|
|
Term
| What action does cyclazocine have on the opioid receptors? |
|
Definition
| kappa 3 receptor agonist; mu receptor antagonist |
|
|
Term
| What are the effects of nalorphine? |
|
Definition
| produces psychotomimetic effects, produces dysphoria |
|
|
Term
| What are the effects of cyclazocine? |
|
Definition
| produces psychotomimetic effects; produces dysphoria |
|
|
Term
| What effect does pentazocine have on opioid receptors? |
|
Definition
|
|
Term
|
Definition
|
|
Term
| What effect does butorphanol have on opioid receptors? |
|
Definition
| kappa receptor agonist, mu receptor antagonist |
|
|
Term
| How is butorphanol administered? |
|
Definition
|
|
Term
| Which patients is butorphanol more effective in? |
|
Definition
| butorphanol is 5x more efficacious in women than men |
|
|
Term
| Why might butorphanol be more effective in women? |
|
Definition
| there is some evidence that this is linked to the melanocortin-1 receptor gene, which is regulated by LH |
|
|
Term
| What effect does nalbuphine have on opioid receptors? |
|
Definition
| kappa receptor agonist, mu receptor antagonist |
|
|
Term
| What is the difference between nalbuphine and nalorphine? |
|
Definition
| nalbuphien has little dysphoria compared to nalorphine |
|
|
Term
| In what medical setting is nalbuphine frequently used? |
|
Definition
|
|
Term
| Why might nalbuphine be preferable to use over morphine? |
|
Definition
|
|
Term
| What action does buprenorphine have at opioid receptors? |
|
Definition
| partial agonist at mu receptors, partial agonists at kappa 3 receptors; antagonist at kappa 1 receptors |
|
|
Term
| Ho does buprenorphine compare to morphine? |
|
Definition
| lower efficacy analgesic than morphine |
|
|
Term
|
Definition
|
|
Term
| What is the MOA of tramadol? |
|
Definition
| opioid receptor agonist (mu and delta); NE and 5-HT reuptake blocker (antidepressant), alpha 2 adrenoceptor agonist --> these actions are synergistic for analgesia |
|
|
Term
| What is the MOA of tapentadol? |
|
Definition
| opioid receptor agonist (mu and delta), NE reuptake blocker (antidepressant)--> thse actions are synergistic for analgesia |
|
|
Term
| Degree of dependence depends upon... |
|
Definition
| dose and frequency of drug |
|
|
Term
| T/F Withdrawal from opioids can be life threatening. |
|
Definition
|
|
Term
| What factors influence the effectiveness of opioid treatment? |
|
Definition
| progression of tissue-damaging disease, sensitization of CNS neurons, collateral transmission |
|
|
Term
| What is the active ingredient in salvia divinorum? |
|
Definition
|
|
Term
| What is the MOA and effect of salvinorin A? |
|
Definition
| very selective kappa opioid agonist, hallucinogen |
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