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75 Cards in this Set

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