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75 Cards in this Set
- Front
- Back
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In the early 1800s these two drugs were isolated from opium
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Morphine and codeine
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Narcotic is derived from a Greek word that means:
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Stupor
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Drugs that are derived from the substances in the opioid poppy became called this to separate them from other drugs that cause stupor
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Opiates
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To include the synthetic opiate-like drugs now these are referred to as:
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Opioids
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List the opioids in the Morphine and codeine structure group
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Morphine, codeine, hydromorphone, hydrocodone, dihydrocodeine, and oxycodone
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Drugs in the Meperidine group
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Meperidine, fentanyl, diphenoxylate, loperamide
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Drugs in Methadone group
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Methadone and Propoxyphene
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Three groups of endogenous substances with opioid-like action
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Enkephalins, endorphins, and dynorphins
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Name the three receptors stimulated by opioids
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mu, kappa, and delta
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Name the 5 analgesic groups based on structure
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1. Morphine and Codeine, 2. Methadone 3. Morphinan 4. Merperidine 5. Other (Buprenorphine)
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What are the classifications of opioids by receptor agonist
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Opioid agonists; Mixed opioids (agonist antagonists and partial agonists): Antagonists
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Dosing interval for nearly all the classes of opioids is:
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4-6 hours
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Describe opioid absorption
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Most are absorbed well orally, from lungs, nasal and oral mucosa and even skin
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Describe opioid distribution
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Variable first-pass metabolism: bioavailability is 0.2 for morphine therefore oral dose of 5 mg equal to IV dose of 1 mg. plasma binding 35% for morphine/60% for meperidine: Go to fetus as well
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Describe opioid metabolism
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Primary is conjugation with glucuronic acid in liver. Duration of action of all oral opioids 4-6 hours
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Describe opioid excretion
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Metabolites and unchanged drug excreted in urin
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What opioid is used to compare other opioids
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Morphine
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Sedation and euphoria with opioids occurs via what receptor?
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Kappa
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Where is the antitussive (cough suppression) action of opioids located
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The cough center in the medulla
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Are strong opioids needed to suppress cough
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No, codeine or dextromethorphan work well
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What is effect of opioids on the gastrointestinal tract
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They increase smooth muscle tone and cause constipation
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What opioid-like agent is used to treat diarrhea?
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Lomotil (diphenoxylate)
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Adverse reactions to opioids are usually due to:
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An extension of their pharmacologic effects rather than tissue or organ damage
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List the contraindications to opioid use.
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Abuse potential, increases ICP in head injury patients, addiction in chronic pain patients, respiratory depression in those with respiratory disease or fetus, added nausea and constipation
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Opioid death is usually due to:
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Overdose which stops breathing due to decreased sensitivity to CO2
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What are the effects on respiratory rate and depth with opioids
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Both are reduced
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What is the cause of N/V with opioids
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They stimulate the chemoreceptor trigger zone (CTZ) in the medulla
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What do the pupils look like in someone using opioids
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Miosis (pupillary constriction)
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Does tolerance to constipation and miosis occur with opioid use
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No
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How do opioids affect the urinary system
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Increase smooth muscle tone making urination difficult and stimulate the release of ADH from the pituitary causing decreased uring production
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What are possible CNS effects of opioids?
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CNS stimulation, anxiety, restlessness, nervousness, sedation and dysphoria
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What are CVS effects of opioids?
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Depression of vasomotor center with vagal stimulation/bradycardia, postural hypotension, and even syncope
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Opioid effects on Biliary Tract
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Constriction of biliary duct with biliary colic(if gallstones present)
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Opioid effects on Histamine release
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Itching and urticaria at injection site or remote sites
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Pregnancy considerations
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Not teratogenic but may prolong labor/cause fetal respiratory depression near term. Infant may undergo withdrawal if born to opioid abuser
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Nursing considerations
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None at normal doses
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Degree of addiction potential of opioids is proportional to there:
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Analgesic strength
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Major symptom of overdose with opioids is:
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Respiratory depression (also pinpoint pupils and coma)
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Describe opioid withdrawal symptoms
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Yawning, lacrimation, perspiration, rhinorrhea, goosebumps, irritability, N/V, tachycardia, tremors, chills, restless legs
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Piloerection means:
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Hair "standing on end" (gooseflesh or goosebumps). This is where term "cold turkey" comes from
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How do you identify a "drug shopper"?
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Requests certain drug, states allergies to less potent opioids, cancels dental appointments, pain out of proportion to procedure, changes offices, "low pain threshold", frequent refills
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Describe four methods of treatment for opioid addiction.
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1. Substitution with methodone and gradual withdrawal. 2. "Cold turkey" and treat withdrawal symptoms. 3. Methadone maintenace. 4. Long-acting antagonist (naltrexone)
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True opioid allergy is __________
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Uncommon. Most are due to histamine releasing property of the opioid and not a true allergy. Substituting classes may help
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Giving opioids with another CNS depressant will:
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Potentiate the respiratory depression of the opioid
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Most agonist opioids commonly used affect what receptors?
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Mu and kappa
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An equivalent number of milligrams of each opioid is compared with ____mg of MSO4
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10 mg
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Morphine used for severe pain in hospital is given by what route
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Parenteral
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Chronic pain or terminal illness pain is sometimes treated with this form of oral MSO4
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Sustained-release MSO4
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Oxycodone is used alone or in combination with _______ or _______ to treat moderate-to-severe pain
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Aspirin, acetaminophen
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Hydrocodone is usually used in combination with ________
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Acetaminophen
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When prescribing an opioid with acetaminophen one must keep in mind the ________ dose of the acetaminophen
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Maximum daily
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The amount of codeine in combination codeine/acetaminophen combinations is indicated by:
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#2 = 15mg codeine, #3 = 30mg of codeine, #4 = 60mg codeine
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This opioid is synthetic and chemically similar to methadone, has little efficacy and causes many adverse effects due to a cardiotoxic metabolite
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Propoxyphene (DarvocetN-100)
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This drug requires 100 mg to equal the efficacy of 10 mg of morphine, is metabolized to normeperidine which can cause toxicity
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Demerol (meperidine)
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This drug can result in inadequate pain relief and adverse effects so morphine, hydromorphone, or oxycodone should be used instead
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Meperidine
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This oral drug is more potent than morphine and better absorbed orally. It is also best used in limited situations
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Hydromorphone (Dilaudid)
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This drug is used primarily to treat opioid addicts or for chronic pain therapy
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Methadone (Dolophine)
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Name the short-acting parenteral opioids used perioperatively
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Fentanyl, Sufentanil, and alfentanil
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This opioid can be used in a patch to provide pain relief for the terminally ill
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Fentanyl (Duragesic) Transdermal System
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The only mixed opioid availabe for oral use is the agonist-antagonist __________
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Pentazocine (Talwin)
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Another mixed opioid available as a nasal spray is ________
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Butorphanol (Stadol)
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Unlike the other opioids, increasing the dose of pentazocine does not lead to a higher risk for _________ depression
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Respiratory
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To reduce the abuse potential what drug has been added to Pentazocine tablets
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Naloxone
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Other agonist-antagonist drugs for parenteral use are often not used due to more _________ effects than the agonists
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Adverse
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The only partial agonist available is ____________
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Buprenorphine (Buprenix, subutex)
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Naloxone is also called _________
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Narcan
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Naloxone antagonizes these receptors
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Mu, kappa, and delta
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Drug of choice for agonist or mixed opioid overdoses is:
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Naloxone (Narcan)
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Naloxone should work within ___ to ______ minutes
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1 to 2 minutes
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If ____ mg of naloxone is given and no response occurs then opioid overdose may not be the problem
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10 mg
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Another drug that reverses opioid overdose is Revex or __________
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Nalmefene
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A long acting opioid antagonist that may be effect in maintenance of the opiod-free state in addicts is _______
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Naltrexone (ReVia)
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A unique drug that only affects mu receptors but is equally efficacious with codeine is ________
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Tramadol (Ultram)
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A dentist should probably pick what class of pain relievers as their first choice for dental pain
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NSAIDs
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If NSAIDs are ineffective one can proceed to these drugs until pain relief is obtained
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Codeine or hydrocodone then oxycodone
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