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Opioid Analgesics

Pharmacology OHSU NRS 230

QuestionAnswer
What are the names of the four types of opioid receptors that endogenous opioids bind to? mu, kappa, delta, and N/OFQ (orphan)
What are the names of the three types of opioid receptors that opioid agonist drugs can bind to? mu, kappa, and sometimes delta
Which opioid receptor do all opioid agonists bind to? mu
What type of opioid analgesic is morphine? (agonist, agonist-antagonist, partial agonist, or antagonist) opioid agonist
What type of opioid analgesic is codeine? (agonist, agonist-antagonist, partial agonist, or antagonist) opioid agonist
What type of opioid analgesic is fentanyl? (agonist, agonist-antagonist, partial agonist, or antagonist) opioid agonist
What type of opioid analgesic is hydrocodone? (agonist, agonist-antagonist, partial agonist, or antagonist) opioid agonist
What type of opioid analgesic is hydromorphone? (agonist, agonist-antagonist, partial agonist, or antagonist) opioid agonist
What type of opioid analgesic is methadone? (agonist, agonist-antagonist, partial agonist, or antagonist) opioid agonist
What type of opioid analgesic is oxycodone? (agonist, agonist-antagonist, partial agonist, or antagonist) opioid agonist
What type of opioid analgesic is meperidine? (agonist, agonist-antagonist, partial agonist, or antagonist) opioid agonist
What type of opioid analgesic is butorphanol? (agonist, agonist-antagonist, partial agonist, or antagonist) opioid agonist-antagonist
What type of opioid analgesic is buprenorphine? (agonist, agonist-antagonist, partial agonist, or antagonist) partial opioid agonist
What type of opioid analgesic is naloxone? (agonist, agonist-antagonist, partial agonist, or antagonist) opioid antagonist
What type of opioid analgesic is methylnaltrexone? (agonist, agonist-antagonist, partial agonist, or antagonist) opioid antagonist
Which opioid agonist is the standard against which other opioid agonists are compared? morphine
What term refers to a drug that binds to a receptor and makes it do its job? agonist
What term refers to a drug that binds to a receptor and blocks it from doing its job? antagonist
Which opioid agonist is a pro drug that metabolizes to morphine and is commonly used for its antitussive action? codeine
Which opioid agonist can be administered in the form of a transdermal patch or as a "lollipop" (lozenge)? fentanyl
How should you teach a patient to dispose of their fentanyl patch? Flush it down the toilet (if a child were to find it in the garbage and put it on it would be fatal).
Why is the half-life of a fentanyl patch so much longer than a fentanyl lollipop? With the patch there is a continued release of the drug from deposition in skin layers.
What would increase the absorption of a fentanyl patch? Heat (e.g. heating pads, electric blankets, hot baths, fever)
What type of pain is the fentanyl patch indicated for and for which type of patient? Chronic pain in opioid-tolerant patients that is not well controlled by shorter-acting analgesics
What would happen if a fentanyl patch was given to a patient who was opioid-naive? Overdose and possibly death
What types of pain are NOT indications for fentanyl patch use? Postoperative pain, acute pain, intermittent pain, mild pain
What in particular makes hydrocodone controversial? The high rate of misuse associated with it
Which drug is stronger on a per milligram basis--hydromorphone or morphine? hydromorphone (1.5 mg of hydromorphone parenterally is equivalent to 10 mg of morphine parenterally)
Which opioid agonist has the longest half-life? methadone
Why does oxycodone receive a lot of publicity? There is a high amount of drug abuse associated with it.
Which opioid analgesic is on the Beers list (not recommended for older adults)? meperidine
Which non-opioid analgesic is frequently combined with hydrocodone in a combination drug? acetaminophen (Vicodin is hydrocodone with acetaminophen)
Which opioid agonist is frequently combined with acetaminophen as part of a combination drug used to treat pain as well as suppress coughing? codeine (Tylenol with Codeine number 3 or number 4)
What is the most common route for butorphanol to be administered? nasal spray
What are three responses to activation of mu receptors that are not part of the response to activation of kappa receptors? respiratory depression, euphoria, and physical dependence
Why does the opioid agonist-antagonist butorphanol have a lower abuse potential than opioid agonists? The kappa receptor gets the agonist and the mu receptor the antagonist, blocking the responses more likely to lead to addiction (i.e. euphoria and physical dependence)
Which three responses are activated by both the mu and the kappa receptors? analgesia, sedation, and decreased GI motility (constipation)
Other than pain, what can the partial opioid agonist buprenorphine be used to treat? Opioid addiction (by suppressing the withdrawal symptoms during detoxification)
What is the opioid antagonist naloxone typically used for? As an antidote for opioid overdose
Why is it important to know that naloxone, used to treat opioid overdose, has a shorter duration of action than morphine? When it wears off, the patient could re-overdose on the morphine. Naloxone needs to be administered again.
What can happen to a patient who is physically dependent on opioids if he is given naloxone? Rapid onset of abstinence syndrome (withdrawal)
What form of naloxone was approved for use by the public in 2014? A hand-held auto-injector.
What important side of effect of opioid use does the opioid antagonist methylnaltrexone treat? constipation
Why does methylnatrexone block the mu receptors that affect constipation, but not the mu receptors that affect analgesia? It works peripherally rather than centrally. It does not interfere with the brain.
How is tramadol different than the other analgesics for moderate to severe pain? It is not an opioid, but it does have some opioid-like action
Which receptors does tramadol bind to? mu receptors (peripherally and centrally)
What neurotransmitters does tramadol inhibit the reuptake of in the central nervous system? norepinephrine and serotonin
Can naloxone block tramadol's effects? Only partly
Can tramadol cause respiratory depression, physical dependence, or abuse? Generally no and it is not included in the Controlled Substances Act.
What is the indication for use of opioid analgesics? Management of moderate to severe pain
Which type of opioid can activate mu receptors, kappa receptors, and possibly delta receptors? Opioid agonists
Which types of opioid activates some types of opioid receptors while blocking (or partially blocking) other types? Opioid agonist/antagonists and partial agonists
Which type of opioid blocks mu and kappa receptors? Opioid antagonists
What effect does blocking mu and kappa receptors on neurons have on neurotransmitter release and neurotransmission? It reduces release and transmission in many neural pathways
Activating mu and kappa receptors is the mechanism for what kinds of effects of opioids? Both therapeutic and side effects
Activating mu receptors on neurons in the brain can cause what pleasurable side effect that may lead to psychological dependence? Euphoria
Neurons exposed to chronic opioid use alter their chemistry to function normally with the drug. This mechanism leads to what two effects? Tolerance and physical dependence
Where are most opioids metabolized? Liver
Which three opioids are metabolized heavily by CYP450 enzymes? fentanyl, oxycodone, and methadone
What are the four most common side effects of opioid agonists? confusion, sedation, hypotension, and constipation
Name as many common opioid-induced side effects in the central nervous system as you can. sedation, disorientation, euphoria, dysphoria, miosis, lowered seizure threshold, tremors, tolerance, physical dependence, psychological dependence
What are some common opioid-induced side effects in the cardiovascular system? lightheadedness, hypotension, palpitations, flushing
What is a common opioid-induced side effect in the respiratory system? Respiratory depression (can lead to death)
What are some common opioid-induced side effects in the gastrointestinal system? nausea, vomiting, constipation
What is a common opioid-induced side effect in the genitourinary tract? urinary retention
Which opioid is more likely than the others to cause itching as a side effect due to histamine release? morphine
Why is it important that many opioids have active metabolites that are excreted renally? If the patient has oliguria or renal disease the drug could build up in the body to unsafe levels
Why should opioids be given cautiously in someone with severe pulmonary disease? They are more prone to the side effect of respiratory depression because of decreased respiratory reserve
Why should opioids be given cautiously in someone with severe hepatic disease? The liver metabolizes most opioids. If not as much is metabolized the dose of drug left in the body could be too high, increasing potentially dangerous side effects
Why should opioids be given cautiously in someone with severe renal disease? There is increased risk of neurotoxicity and other side effects with oliguria because active metabolites are not being excreted
Why should opioids be given cautiously in someone with benign prostatic hypertrophy? They are more likely to experience urinary hesitancy or retention, which may require catheterization.
Why should opioids be given cautiously in someone with undiagnosed abdominal pain? Opioids can cause biliary colic. If the abdominal pain is caused by this, pain could intensify instead of being relieved. Also, in patients with IBD morphine can cause toxic megacolon or paralytic ileus
What are four types of drugs that cause CNS depression which may interact with opioids? alcohol, sedatives/hypnotics, antihistamines, and barbituates
What are three natural products that cause CNS depression which may interact with opioids? valerian, chamomile, kava-kava
What are two types of drugs specifically that may cause constipation, which would be worsened if taking with opioids? anticholinergics and calcium channel blockers (many other drugs and natural products can also cause constipation)
What are some other substances that, like opioids, can cause hypotension and could increase this effect if given with opioids? alcohol, diuretics, most antihypertensives (as well as many other drugs and natural products)
What could the following signs indicate to you if you observed them in a patient? Respiratory depression, coma, and miosis Opioid overdose
Name as many signs and symptoms of opioid withdrawal (acute abstinence) as you can think of. anxiety, runny nose, watery eyes, sneezing, yawning, dyspnea, diarrhea, nausea, vomiting, chills, goose bumps, dilated pupils, cramps, restlessness, tachycardia, hypertension, fever
Is opioid withdrawal dangerous? Not generally (unlike withdrawal from CNS depressants like alcohol and barbitutates, which can be deadly, but it feels awful)
How long will opioid withdrawal usually take without treatment? 7-10 days (with peak symptoms at about 72 hours)
What term is defined as a drug that depresses the central nervous system and produces stupor or sleep? narcotic (opioids may be included in this category)
What term is defined as a compound related to opium with an action similar to morphine? opioid
What term is defined as an agent that prevents or relieves coughing? antitussive
What term is defined as a situation where a person has developed decreased sensitivity to subsequent doses of the same substance? The dose would need to be increased to achieve the same effect. tolerance
What term is defined as the condition when adaptive cellular changes to the presence of a drug leads to withdrawal if the drug is discontinued physical dependence
What term refers to the side effects that occur when a drug has been discontinued to which the patient is physically dependent? abstinence syndrome (withdrawal)
What term refers to the preoccupation with a drug and drug-seeking behaviors and compulsively using a drug even when causing harm to self and others addiction
What term refers to the use of a drug that is not in accordance with accepted norms of society drug abuse
What does ER mean as part of a drug name? extended release
What is the classification of drugs with dependence and abuse potential according to the Controlled Substances Act, which includes opioids? Schedule of Controlled Substances
Who regulates the Schedule of Controlled Substances? The Drug Enforcement Administration (DEA)
What term is defined as the psychic desire or craving for the effect of a drug? Psychological dependence
Do most people who use opioids for analgesia develop pscyhological dependence or addiction? What is important about this? No, in fact it is uncommon. Patients should be treated appropriately for their pain and not withheld medication because of fear of addiction.
Do most people who use opioids long term develop physical dependence or tolerance? What is important about this? Yes. When it is time to stop taking the drug it should be tapered gradually to avoid severe side effects of withdrawal.
What does cross tolerance mean with opioids? A patient that has become tolerant to one opioid will also have increased tolerance to other opioids. (There is no cross tolerance between opioids and general CNS depressants like barbituates or alcohol.)
What is PCA? patient-controlled analgesia, where analgesia is administered via a pump that allows the patient to self-administer up to a limit.
What term refers to a dose of an opioid that should provide the same analgesic effect as a different dose of another analgesic? Equianalgesic dose
What is the standard against which opioids are compared in the equianalgesic chart? 10 mg of morphine parenterally
When would you need to use an equianalgesic chart? If a patient is switching to another opioid, to determine the appropriate dose
Why are most opioids called high alert drugs? They are known to cause the most patient harm with errors. Too much can lead to respiratory depression and death. A decimal point error can lead to 10x the correct dose, likely a fatal error.
Created by: k_duff