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121 Cards in this Set
- Front
- Back
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What are the ONLY agents able to pass through the BBB? How?
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lipid soluble agents; specific transport system
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What characteristic of the CNS results in weeks before there is a noticable therapeutic effect?
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the CNS takes time to make adapative changes for the drug
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What is unique about the SEs of CNS medications?
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they subside after therapeutic effect is achieved related to the adaptive changes made by the CNS
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What is a negative effect of the CNS adaptation process?
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is can result in tolerance or physical dependence and cause withdrawal symptoms
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How should opioids be dosed?
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fixed schedule
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What are the 3 types of opioid recetpors?
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Mu, Kappa, Delta
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Which opioid receptor IS activated most often by exogenous opioids?
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Mu
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Which opioid receptor IS NOT activated by exogenous opioids?
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Delta
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Which receptors are receptive to endogenous opioids?
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Mu, Kappa, Delta (all 3)
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Mu receptor activation has what 7 effects?
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analgesia, respiratory depression, euphoria, sedation, cough suppression, physical dependence, decreased GI motility (constipation and urinary retention)
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Kappa receptor activation has what 3 effects?
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analgesia, sedation, decreaseed GI motility (constipation)
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What receptors do pure opioid agonists activate?
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Mu and Kappa
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What receptors do agonist-antagonist opioids activate?
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low to moderate Mu and Kappa
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What do pure opioid antagonists do to opioid agonists?
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the antagonist blocks the effects of the agonist
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Which opioid takes receptor precedence, agonist or antagonist?
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antagonist
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What are pure opioid antagonists used for?
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to reverse respiratory and CNS depression caused by opioid agonists
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What drug class is morphine in?
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pure opioid agonist
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What pure opioid agonist is 100 times stronger than morphine?
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fentanyl
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What pure opioid agonist is 1000 times stronger than morphine?
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alfentanil and sufentanil
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What drug class is methadone in? What is it used for?
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pure opioid agonist; treats heroin addiction
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Some of the names of pure opioid agonists have what in common (2)?
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they have “morph” in the name (e.g. hydroMORPHone); they end in “-fentanil”
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What type of sensations is morphine more effective against?
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constant, dull pain
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What is the most common cause of death with regards to morphine?
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respiratory depression
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What respiratory rate indicates that morphine should be delayed?
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< 12 breaths per minute
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What drug class can be used to reverse morphine-induced respiratory depression?
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opioid antagonist
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How is morphine-induced constipation treated (3)?
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stool softener, laxative, or osmostic laxative
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Morphine does NOT cause a cross tolerance in which of these (4): gernal anesthetics, heroin, oxycontin, ethanol, benzos, codeine, oxycodeine, barbituates
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barbituates, ethanol, benzos, general anesthetics
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Morphine does or does not cause birth defects in pregnancy?
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does NOT
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What is the 1st pass effect?
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PO meds are metabolized before they enter systemically
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Why is PO morphine given in higher doses than parenteral routes?
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first pass effect
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How is morphine dosed?
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dosing is individualized
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Which type of pain requires a higher morphine dose, sharp stabbing or dull?
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sharp stabbing
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When in particular should morphine be withheld?
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when respiration rate is less than 12 br/min
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What schedule is heroin?
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Schedule I - no medicinal value
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What schedule is morphine?
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Schedule II
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How does morphine affect a fetus?
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no birth defects but does cause physical dependence
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What are two differences between strong opioid agonists and moderate opioid agonists?
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amount of analgesia and level of respiration depression produced
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What drug class is pentazocine?
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agonist-antagonist opioid
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What drug class is nalbuphine?
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agonist-antagonist opioid
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What drug class is butorphanol?
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agonist-antagonist opioid
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What drug class is buprenorphine?
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agonist-antagonist opioid
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What receptors are affected by agonist-antagonist opioids? How?
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Mu - antagonist; Kappa - agonist
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What condition do pure opioid agonists treat that pentazocine does not?
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MI (due to increased CO)
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Do agonist-antagonist opioids produce euphoria? Why?
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no; due to the anatagonist effect at Mu receptors
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What is the most common drug used in a PCA?
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morphine
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What is required before PCA use?
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loading dose
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What is the primary use of opioid antagonists?
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used to treat overdose or reverse respiratory depression after post-op and addiction treatment
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The names of opioid antagonists have what in common?
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they start with “nal-“ (e.g. NALtreone)
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What happens if opioid antagonists are administered to patients WITHOUT opioid physical dependence?
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nothing
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What happens if opioid antagonists are administered to patients WITH opioid physical dependence?
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it can trigger withdrawal symptoms
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What happens if opioid antagonists are administered before opioid agonists?
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it will block the effects
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What happens if opioid antagonists are administered after opioid agonists?
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it well reverse the effects
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Which drug class relieves pain by mechanisms unrelated to opioid receptors?
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nonopioid centrally acting analgesics
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What are 3 benefits of nonopioid centrally acting analgesics?
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they do NOT cause respiratory depression, dependence, or abuse
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What drug class is tramadol (Ultram)?
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nonopioid centrally acting analgesics
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What is the MOA of tramadol (Ultram)?
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blocks uptake of serotonin and NE thereby activating spinal inhibition of pain
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Does naloxone block the effects of tramadol?
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only partially
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What drug class is clonidine (Duraclon)?
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nonopioid centrally acting analgesics
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What is the MOA of clonidine (Duraclon)?
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relieves pain by binding to pre and postsynaptic alpha 2 receptors in the spinal cord
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What route is clonidine delivered?
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continuous epidural infusion
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What 2 conditions do muscle relaxants treat?
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muscle relaxants either treat muscle spasticity or acute muscle spasm but NOT both
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What are 4 causes of muscle spasm?
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epilepsy, hypocalcemia, acute or chronic pain from muscle injury, trauma
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What is the MAIN cause of muscle spasm?
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acute and chronic pain from muscle injury
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What drug class is diazepam (Valium)?
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muscle relaxants - spasticity
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What drug class is tizanidine (Zanaflex)?
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muscle relaxants
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What drug class is baclofen?
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muscle relaxants - spasticity
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What drug class is carisoprodol (Soma)?
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muscle relaxants
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What drug class is chlorphenesin (Maolate)?
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muscle relaxants
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What drug class is cyclobenazaprine (Flexeril)?
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muscle relaxants
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What drug class is dantrolene?
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muscle relaxants - spasticity
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What drug class is metaxolone (Skelaxin)?
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muscle relaxants
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What drug class is methocarbamol (Robaxin)?
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muscle relaxant
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What drug class is orphenadrine (Norflex)?
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muscle relaxant
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What is thought to be the MOA of muscle relaxants?
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relaxation is due to its sedative properties
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What muscle relaxant causes liver damage?
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tizanidine; make sure to check LFTs
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Do muscle relaxants cause physical dependence?
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yes, with life-threatening withdrawal if not done slowly
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Which 3 of these muscle relaxants treat spasticity? dantrolene, chlorphenesin, baclofen, tizanidine, carisoprodol, diazepam
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dantrolene, baclofen, diazepam
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How is insomnia defined?
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difficulty falling or staying asleep; early morning awakening or non-refreshing sleep
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How much of sleep is Stage I?
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5%
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How much of sleep is Stage II?
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50-60%
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How much of sleep is Stage III?
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10-20%
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How much of sleep is Stage IV?
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20-35%
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What is Stage V sleep?
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REM sleep
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What is REM?
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rapid eye movement DELTA waves
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What is NREM?
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non-rapid eye movement ALPHA waves
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What are the stages of NREM?
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I - light sleep, II - light sleep, III - deep sleep, IV - deepest sleep
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What drug class is used to treat anxiety and insomnia?
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sedative-hypnotics
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What are drugs that relieve anxiety called (2)?
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anxiolytics, tranquilizers
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What are drugs that given to promote sleep called?
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hypnotics
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What do sedative-hypnotics treat at low doses?
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anxiety
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What do sedative-hypnostics treat at high doses?
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insomnia (they induce sleep)
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What are the 3 classes of sedative-hypnotics?
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barbituates, benzos, benzo-like drugs
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Why are barbituates rarely used (4)?
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strong respiratory depression, high potential for abuse, tolerance buildup, physical dependence
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What drug class is preferred to barbituates?
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benzodiazepines
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What do some of the names of benzos have in common?
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they end in “-zepam” or “-zolam” (e.g. loraZEPAM, alpraZOLAM)
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Which sedative-hypnotic benzo is also a muscle relaxant?
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diazepam
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What are the 3 uses of benzos?
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reduce anxiety, promote sleep, induce muscle relaxation
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When given PO, what effect do benzos have on the cardiovascular system?
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none
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When given IV, what effect do benzos have on the cardiovascular system?
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profound hypoTN, cardiac arrest
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What condition to benzos exacerbate?
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obstructive sleep apnea (snoring may turn to OSA)
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How likely are benzos to produce respiratory depression?
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death from overdose has never been documented
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Do benzos have the potential for abuse?
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yes
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Which inhibitory neurotransmitter do benzos increase the action of?
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GABA
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Do benzos cross the BBB? How?
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yes, they are highly lipid soluble
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Which benzos are preferred in patients with liver disease?
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LOT (lorazepam, oxazepam, temazepam)
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Which benzos are preffered in patients with liver disease? alprazolam, lorazepam, diazepam, clonazepam, oxazepam, temazepam, midazolam
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LOT - lorazepam, oxazepam, temazepam
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Which drug counteracts benzo overdose?
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flumazenil (Romazicon)
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What is the route and dose for flumazenil?
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IV over 30 sec and every min PRN, taper 4 doses from 0.2mg to 0.5mg
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Ambien and Lunesta are in which drug class?
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sedative-hypnotic benzo-like drugs
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What are 3 therapeutic effects of zolpidem (Ambien)?
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reduces sleep latency, reduces wakenings, produces longer sleep
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How does Ambien affect REM?
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it does NOT significantly reduce REM sleep
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How is Ambien different from benzos (3)?
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has no effect on anxiety and is not a muscle relaxant or anticonvulsant
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Which benzo-like drug has no limitation to how long it can be taken?
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Lunesta
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What drug class is zaleplon (Sonata)?
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pyrazolopyrimidines
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What drug schedule is Sonata?
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Schedule IV
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What is the brand name for zolpidem?
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Ambien
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What is the brand name for zaleplon?
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Sonata
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What is the brand name for eszopiclone?
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Lunesta
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Which of these is NOT a controlled substance? ramelteon (Rozerem), zolpidem (Ambien), zaleplon (Sonata)
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ramelteon (Rozerem)
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What drug class is ramelteon (Rozerem)?
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melatonin agonist
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What hormones are affected by ramelteon (2)?
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increases prolactin, decreases testosterone
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