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83 Cards in this Set
- Front
- Back
What are all opioid receptors coupled to?
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Gi/o proteins
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What Do opioids do when the bind the receptors? (2 phases, both pre and post synaptic)
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1) closes voltage gated Ca2+ channels presynaptically, decreasing NT release
2) Opens post synaptic K+ channels, hyperpolarizing and inhibiting neurones |
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What does activation of u (MU) receptors by opioids do?
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this produces analgesic, sedative, and euphoric effects.
as well as the side effects |
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What does activation of k (Kappa) receptors by opioids do?
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this contributes to analgesia, and also dysphoria
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How do opioids act in the dorsal horn of the spine?
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these directly inhibit pain transmission in the dorsal horn.- called spinal analgesai
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how do opioid agonists affect the ascending pain pathways?
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inhibition
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How do opioid agonists affect the descending systems of pain transmission?
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these stimulate the inhibition systems
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In general how do opioids affect analgesia?
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these induce both sensory and affective (emotional) components of pain
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In general how do opioids sedation?
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these cause drowsiness, and in overdose can cause CNS depression
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In general how do opioids euphoria?
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people may experience euphoria, a decrease in anxiety or distress
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In general how do opioids cause nausea?
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this directly stimulates the CTZ in the brain causing nausea
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In general how do opioids affect cough?
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low doses suppress cough
codeine and dextromethorphan are commonly used |
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In general how do opioids the respiratory system?
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there is decreased respiratory drive, which is good for pulmonary edema.
But bad for asthma/COPD as there is an overall PaCO2 increase |
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In general how do opioids affect intracrainal pressure?
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these increase intracrainal pressure, as the increased PaCO2 in the blood increases vasodilation
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In general how do opioids affect the eyes?
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this causes miosis (pupil constriction)
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In general how do opioids body temp?
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lowers it
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In general how do opioids the trunk muscle tone?
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this causes truncal rigidity
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In general what do opioids to the heart?
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Bradycarida
(except for meperidine- tachycardia) |
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In general how do opioids the GI system?
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constipation
decreased gastric motility biliary colic |
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In general how do opioids the GU system?
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lower urine output
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In general how do opioids affect histamine?
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these cause histamine release-
itching, usually due to injected opioids |
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What are the signs of opioid overdose?
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CNS depression
depressed respiration pin point pupils (may be dilated near death) |
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What do you do to treat opioid overdose?
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support respiration
administer naloxone (Narcan) |
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What happens when opioids are given with MAO inhibitors?
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this causes a hyperpyrexic coma
should be avoided! |
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What may decrease the analgesic effect of codeine derievtives?
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anything that inhibits CYP2D like SSRI's
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What is the prototype strong agonist opioid?
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Morphine (MSContin)
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What receptors does Morphine (MSContin) stimulate?
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this stimulates all opiate receptors
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What is the least effective way to dose Morphine (MSContin)?
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orally- due to high first pass metabolism
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How is Morphine (MSContin) metabolized in the body?
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this is metabolized in the liver by CYP2D6
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How long is the half life of Morphine (MSContin)?
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about 1.5-2 hours
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What is the more potent analgesic version of morphine, and how is it made?
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this is morphine 6-glucuronide
this is formed by conjugation with glucuronic acid |
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How potent is hydromorphone (Dilaudid)
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this is MORE potent than morphine, and as effective
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What is hydromorphone (Dilaudid) less likely to cause than morphine?
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this is less likely to cause itching
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How long is the duration of action of Methadone (dolophine)
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this has a longer duration of action than morphine. its half life is 15-60 hours
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What is Methadone (dolophine often used to treat?
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hard to treat pain from cancer/neruopathic pain. help with withdrawal
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What is the withdrawl from Methadone (dolophine) like?
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this is milder and longer than other opioids
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What is meperidine (demerol) used for?
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this is used for very brief course in pts who are healthy, and are undergoing short painful procedures
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Why is meperidine (demerol) not used for long term use?
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this has metabolite accumulation which leads to seizures in patients with renal failure
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How does meperidine (demerol) affect the heart?
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this has antimuscarinic activity- so may cause tachycardia
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how does meperidine (demerol) affect the eyes?
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this may causes pupil dilation due to muscarinic block
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How does meperidine (demerol) affect cough?
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this does NOT suppress cough
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how does meperidine (demerol) affect the brain? What interaction does this have?**
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this blocks neuronal reuptake of serotonin
this can causes serotonin syndrome when given with SSRI's, TCA's, or MAO inhibitors |
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How potent is fentanyl (sublimaze)?
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this is 100x more potent than morphine due to its high lipid solubility
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What is fentanyl used for?
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this is used for anesthesia induction and maintenance
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What metabolizes fentanyl?
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CYP3A4- so high interaction potential
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What schedule is heroin?
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schedule 1, not available in US
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What kind of drug is hydrocodone (codan)
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this is a moderate to strong opioid agonist
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How is hydrocodone (codan) metabolized?
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this undergoes complex hepatic metabolism
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What is the important metabolite produced by hydrocodone (codan)? by what enzyme?
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CYP2D6 a cytochrome P450.
this produces hydromorphone (dilaudid) which produces some of the analgesic effect |
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What kinds of drug is oxycodone?
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this is a moderate to strong opioid
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What is oxycodone (oxycontin) used for?
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this is used to control moderate to severe pain
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What is Percodan?
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this is oxycodone (oxycontin) and aspirin
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What is Percoset?
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this is oxycodone (oxycontin) and acetaminophen
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What must happen in the body for oxycodone (oxycontin) to produce analgesia?
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this must be metabolized by CYP2D6
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What is Codeine used for?
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this is a moderate opioid agonist that is used as an antitussive agent
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What is Codenie metabolized into?
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this is metabolized into morphine by CYP2D6
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What does codeine do?
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this is an antitussive agent
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How is codeine metabolized?
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this is metabolized to morphine by CYP2D6
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What is Propoxyphene (Darvon)
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this is a weak analgesic
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What do high doses of Propoxyphene (Darvon) cause?
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these lead to seizures and toxic psychosis
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What is Pentazocine (Talwin)?
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this is an agonist at kappa receptors, and partial agonist at Mu receptors
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What is Pentazocine (Talwin) given for?
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this is a mixed agonist-antagonists
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What can happen when taking Pentazocine (Talwin) in opioid addicts?
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this can precipitate withdrawal symptoms
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What is Buprenorphine (Buprenex, suboxone)
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this is a mixed agonist -antagonists
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What is Buprenorphine (Buprenex, suboxone) given for?
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this is used to reduce drug craving in addicts (subutex)
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What receptors does Tramadol (Ultram) affect
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this is a weak Mu agonist
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What does Tramadol (Ultram) do?
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this inihibits reuptake of NE and 5-HT, like TCA's
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What happens with you combine Tramadol (Ultram) with antidepressants?
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this may result in seizures
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What side effect should you be aware of for Tramadol (Ultram)?
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serotonin syndrome
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What is Dextromethorphan given for?
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this is an antitussive
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What happens when combining Dextromethorphan with MAOI's
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this can cause serotonin syndrome
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What happens when ingesting pure Dextromethorphan in powdered form?
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this causes death, brain damage, seizures
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What is Naloxone (Narcan)?
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this is a pure opioid antagonist
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How long does Naloxone (Narcan) last? why is this important?
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this only lasts about 2 hours, so may requires repeated doses
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How does Naloxone (Narcan) affect addicts?
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this can precipitate withdrawal symptoms
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What is Naltrexone (ReVia)
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this is a long acting opioid antagonist
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What is Naltrexone (ReVia) used for?
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this is used to prevent recovering addicts from getting high
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What receptors does methadone block or bind?
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this blocks NMDA receptors, inhibits monoamine reuptake
strongly binds opioid receptors |
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What receptors does Meperidine (demerol) bind or block?
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blocks serotonin ruptake
binds opioids |
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What are the risks of long term meperidine (demerol) use?
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seizures
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What receptors does fentanyl binds?
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Opioid receptors
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What receptor does codeine bind?
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this does NOT bind MU- important because that limits the mu effects (analgesia, sedation, respiratory depression and side effects)
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What receptors does Tramadol bind or block?
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weak Mu agonist
blocks serotinin and NE reuptake |