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64 Cards in this Set

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what are opioids?
opioid refers to all agonists adn antagonists with morphine like activity as well as to naturally occurring and synthetic opioid peptides.
what are the 3 classes of opioid receptors and where are they located?
mu, kappa, and delta; throughout the CNS, including cortex, thalamus, brainstem, and spinal cord
what are the effects of mu receptors?
produce spinal/supraspinal analgesia, euphoria, respiratory depression, miosis, and constipation
what receptor is responsible for producing spinal analgesia, sedation, dysphoria, and miosis?
waht receptor is just responsible for producing supraspinal/spinal analgesia?
how do opioids help reduce pain?
they cause hyperpolarization of nerve cells by activating K+ channels, and inhibit both nerve firing and presynaptic transmitter release by inhibiting voltage-operated calcium and NT release
names some classes of analgesic agents.
NON-OPIOIDS (NSAIDs)good for mild pain alone, good for moderate if given with low-dose opioids; OPIOIDS: choice for severe pain; ANALGESIC ADJUVANTS (muscle relaxers, antidepres, antianxiety): alone little effect, but significantly enhance the action of other pain killers
what does opium contain?
morphine, codeine, thebaine
what drugs are considered strong opioid agonists?
morphine, meperidine, methadone, fentanyl, heroin, hydromorphone
what would a heroin user's urine reveal?
free morphine, morphine glucuronide, free codeine, 6-monoacetylmorphine (specific for heroin use)
what legal food can reveal a positive test for morphine and codeine?
poppy seeds
what receptors are activated by mechanical, thermal, and/or chemical stimuli (respond to damaging stimuli)?
where do nociceptor fibers terminate?
in the dorsal horn of the spinal cord
what fibers localize pain fast, which slow?
small fibers - fast response; larger fibers - slow transfer of info, delayed response
what are the 3 types of pain?
nociceptive pain, inflammatory pain, and neuropathic pain
define absence of pain sensation.
deine absence of sensation.
what two tracts are involved in pain?
anterolateral spinothalamic tract and the dorsalcolumn medial leminsical tract
what channel do anticonvulsants and local anesthetics inhibit?
Na+ channels
what are the two types of afferent nociceptor pain fibers that stimulate the spinothalamic tract?
fast-conducting, myelinated a-delta fibers and slow, visceral, unmyelinated C fibers
give 3 examples of endogenous (naturally occuring) opioids.
enkephalins (short interneurons associated with pain pathways, emotional behavior and motor control), endorphins (selective for mu; co-released with ACTH, stress hormone), and dynorphins (co-localized with vasopressin, may have role in fluid homeostasis)
how does the body modulate pain with neurotransmitters?
1. when stimulated the descending projects or the inhibitory interneuron will release various NTs: GABA, NE or endogenous opioids (ie. enkephalin); 2. bind receptors on presynapse, inhibit Ca2+ leading to reduced vesicle release; 3. bind post-synaptically, cause efflux of K+ or Cl- to hyperpolarize
what do opioids cause?
analgesia, eurphoria, respiratory depression, cough suppression, miosis, emesis, reduced GI motility, histamine release from mast cells, sedation
what seems to play a role in endogenous opioid release?
emotional stress, esp. fear/stress
Opioids are used for therapeutic purposes, name them.
analgesia with sedation; treatment of diarrhea; cough suppressant (dextromethorphan); opioid withdrawal (methadone); opioid overdose (naloxone); and anesthesia
substantia gelatinosa/dorsal horn, the limbic system/thalamus, and the periaqueductal grey area(receives info from the ascending spinothalamic tract) are all areas that contain what?
opioid receptors
stimulation of the periaqueductal grey matter of the midbrain results in release of what?
serotonin in the dorsal horn of the spinal cord, profound analgesia, activation of interneurons containing enkephalin, and release of norE in dorsal horn
which opioid receptor is responsible for being the main pharmacological site?
mu receptor; mu1: supraspinal analgesia, physical dependence, and euphoria, inhibits ACh release; mu2: spinal analgesia, respiratory depression, miosis, and decrease GI motility
which receptor is predominately associated with endogenous opiates that produces spinal analgesia, miosis, sedation, and dysphoria?
name some moderate agonists of opiates.
codeine and propoxyphene, tramadol is a synthetic codeine analog that is a weak mu agonist
name some antagonists of opiates.
naloxone and naltrexone
what does the delta receptor responsible for doing?
enhances mu agonists and reinforces supraspinal analgesia
tolerance develops to most of morphine's effects, except with:
miosis, constipation, and pruritis
morphines main MOA:
activation of mu receptors
when is morphine indicated?
acute pain (do not use in chronic non-malignant pain); dyspnea and pulmonary edema, pre-anesthetic medication, open heart surgery, decrease fear in dying
is morphine equally effective orally vs parentally?
no, only 25% for oral
what does morphine do to respiration? does it make people nauseated?
decreases rate, volume and tidal exchange: respiratory depression is dose related; morphine stimulates CTZ and may cause nausea and vomiting
what are the cardiovascular effects of morphine?
vasodilation, thus a decrease in blood pressure (histamine causes vasodilation and morphine suppresses the reflex vasoconstriction)
what are the GI effects of morphine?
increased tone and decreased mobility - constipation
name the drug that is 10 times more potent than morphine, more expensive, lasts longer, and has less tendency to induce N/V, less effect on respiratory center and doesn't cause histamine release.
oxymorphone - to prevent severe bradycardia, an anticholinergic should be given
name the opioid that produces less sedation, shorter duration of action, and less vomiting occurs; it is the only opioid that will directly depress the myocardium.
meperidine (Demerol) activates mu receptors; only 1/3 potency of morphine,(not recommended for alleviated post-op pain b/c its short duration of action)
name some meperidine analogues used to treat diarrhea.
loperamide (imodium) and diphenoxylate
codeine gets turned into what in the liver?
what opioid drug is 75-125 times more potent than morphine, be active for only 45-60min, with MINIMAL CARDIO effects except for bradyarrhythmias, however, more severe respiratory depression.
Name some fentanyl congeners.
sufentanyl (1000xs more potent than morphine); alfentanil and remifentail (rapid onset of analgesia)
what two piperidines are used for short, painful procedures that need intense analgesia and suppressing stress response?
alfentanil and remifentanil
explain the pharmacokinetics of opiates.
ABSORPTION: RAPIDLY ABSORBED in GI, high rate of 1st metabolism, highly lipophilic can be absorbed transdermally; DISTRIBUTION: all bind to plasma proteins; will rapidly leave the blood to go into other tissues; METABOLISM: first pass effect; most are converted to more polar metabolites in the liver, turned into glucuronides or N-demethylated; 6-glucuronide is more potent; 3-glucuronide is inactive and found in urine; EXCRETION: kidneys
what signifies acute morphine poisoning?
Triad of Coma, miosis, cyanosis (decreased respirations); respiratory failure
what would be a good way to painlessly administer an analgesic to a child for a surgical procedure. it takes effect within 15-20min and lasts 1-2hrs?
intrabuccal fentanyl (Oralet and Actiq-used for CA pts with breakthrough pain)
what is a good way to manage chronic malignant pain, duration of action of 72hrs
transdermal fentanyl
what drug is commonly abused by crushing the extended release opioid?
describe codeine's effects and indications.
10% gets converted to morphine, has a higher oral efficiency and slower development of tolerance than morphine, less respiratory depression, less dependence, less euphoria; INDICATIONS: moderate pain and as an antitussive
name a codeine analog that is for mild to mod pain and is excreted renally;and describe its MOA.
tramadol (Ultram); blocks reuptake of NorE and 5-HT
name the most prescribed drug that is highly abused and more potent than codeine.
what type of drugs may be used to reverse depressant effects of opioid while preserving it's analgesic qualities?
any non-pure mu agoinst: ie. partial mu agonist, poor mu antagonist, and kappa agonist
name the drug that is 1/3 as potent as morphine wiht faster onset and shorter duration; and is a kappa agonist, mu and delta antagonist
name a long acting, potent opioid , mu and kappa partial agonist, delta antagonist
buprenorphine - PARTIAL AGONIST 20-50x potency of morphine; used to in tx of opiate addicts; available worldwide(less physical depend. ceiling effect on respiratory depression)
high doses of this drug can cause CNS stimulation with convulsions, respiratory depression, haluucinations, confusion, and coma (chemically related to methadone with <1/2 the analgesic potency of codeine.
name the drug that antagonizes most opioid receptors agonists (almost pure antagonist) that is used to reverse opiod overdose.
naloxone (Narcan) - short half-life; observe for recurrent signs of opiate intoxication (given IV)
name the longer acting derivative of the opiate antagonist naloxone?
naltrexone (clinically used to tx opiate addicts - it reduces pleasure from opiates)
what is the purpose of combining a low dose opioid antagonist with an opiate agonist?
pain relief is more easily achieved, enhances the analgesic effect
name 4 drugs that are used to treat opiate dependence.
methadone (full agonist at the mu receptor; its long half-life helps prevent withdrawal), buprenorphine (suppresses withdrawal, blocks subsequent opiate use), LAAM, and naltrexone
name some common OTC meds that contain dextromethorphan.
vicks 44 cough relief; Robitussin DM, Coricidin cough & cold
how would someone present clinically with a dextromethorphan overdose?
slurred speech, restlessness, poor coordination, difficulty breathing, seizures