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58 Cards in this Set
- Front
- Back
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Top 2 effects of mu receptor
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#1 respiratory depression
#2 GI disturbances |
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Kappa receptor effects
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analgesia (supraspinal, spinal)
dysphoria sedation low abuse potential miosis |
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Delta receptor effects
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analgesia (supraspinal, spinal)
depression of ventilation physical dependence constipation urinary retention |
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Antagonist at opiate receptors
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Naloxone (narcan)
Naltrexone Nalmefene |
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Reason for ventilatory depression
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opiates are resp. depressants the degree of resp. depression is always equal to the amt of analgesia the drug is producing. produce Resp Depression by depressing the respiratory centers sensitivity to CO2. "shifts CO2 respose curve to R"
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Cardiac Effects
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mild bradycardia
small amount of hypotension in dry, elderly or comorbid patients demerol causes tachycardia "atropine-like" |
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Phenanthrine drugs can produce?
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Modest amt of vasodilation
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How cough suppression?
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depress cough center in the brain
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Cough suppressants in decreasing order of potency
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heroin=fentanyl=hydromorphone=hydrocodone
methadone codeine morphine levorphanol meperidine=pentazocine |
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How Miosis?
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opioids abolish cortical inhibition of Edinger Westphal nucleus, thereby resulting in papillary constriction
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4 groups of endogenous chemicals in body that are able to produce pain relief?
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enkephalins
endorphins dynorphins endomorphins |
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Precursor: proenkephalin A
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enkephalins:
Leuenkephalin metenkephalin |
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Precursor: Pro-opiomelanocortin
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B-endorphin
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Precursor: Prodynorphin
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Dynorphins:
dynorphin alpha-neoendorphin |
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Precursor: unk
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Endormorphin 1
Endormorphin 2 |
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key goal to multi-modal treatment?
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opioid sparing
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Why dose pain go away?
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Endorphins produce agonist response, they stimulate inhibition of pain pathways, they are not antagonist, they are agonist.
Agonist at opiate receptors and inhibit pain pathways. |
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3 subtypes of opiate receptors
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Mu
Kappa Delta |
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Primary or main effect of all opiates are produced at what receptor?
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Mu
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Mu Receptor Effects
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analgesia (supraspinal, spinal)
euphoria low abuse potential miosis bradycardia hypothermia urinary retention pruritus skeletal muscle rigidity biliary spasm depression of ventilations physical dependence constipation |
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Nausea/vomiting
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opiates are biphasic response stimulate the CTZ but they inhibit the vomiting center. Therefore, with subsequent doses the potential for vomiting decreases. incidence goes down with duration of treatment.
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opiates are the most emetic drugs
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incidence decreases with longer duration of treatment
more common in ambulatory patients stimulate CTZ, inhibit vomiting center antiemetic in long run |
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Skeletal muscle rigidity "tight chest" when do we see?
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high dose of narcotic
speed of administration quick use of N2O at same time Use of narcotics in older patients Absence of muscle relaxants (Give Now!) rigidity almost always occurs after LOC |
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effect of smooth muscle spasm
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increase biliary pressure, constrict sphincter of Oddi, increase bile, increase biliary pressure
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Reverse smooth muscle effect
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atropine or glypyrrolate
NTG glucagon naloxone (narcan) |
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GI effects
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delayed digestion
hard, dry stools incomplete evacuation |
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Urinary retention
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opiates constrict vessels in urinary system, makes voiding difficult
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Pruritis
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most common when given intrathecal
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antishivering
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meperidine is unique in its ability to effectively terminate or attenuate shivering, primarily a kappa receptor effect
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Tolerance/Physical dependence
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if someone develops tolerance more than likely have some physical dependence, if not just psychological dependence. chronic administration of opiates leads to tolerance (requiring higher and higher doses for same effect)
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opiates do not produce___, they produce___. Need to watch out for ____.
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anesthesia, analgesia, pt being awake
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amount of analgesia you get is always equivalent to the amount of ___ and ___.
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respiratory depression, addiction liability
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Most potent opioid
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sufentanil
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Phenanthrene Alkaloids (naturally occurring)
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morphine
codeine thebaine (not used anymore) |
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Phenanthrene (semisynthetic)
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diacetylmorphine (heroin)
hydrocodone (vicoden) hydromorphone (dilaudid) oxycodone (oxycontin) oxymorphone |
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Synthetic Opioids
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Morphinan derivatives
Leorphanol |
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Phenylpiperidine derivatives
(All synthetic) |
meperidine (demerol)
fentanyl sufentanil alfentanil remifentanil |
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Propionilide (methadone derivatives)
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methatdone
propoxyphene |
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Can I give fentanyl if patient is allergic to codeine?
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Yes
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Can I give vicoden if allergic to codeine?
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No, bad idea
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Enzyme that metabolizes Remi
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nonspecific esterase enzymes
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where is remi metabolized?
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plasma
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What should I think about before turning off Remi infusion?
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Pt is going to need a longer acting analgesic
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3 chemical things we need to know about opiates
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1-All opioids are metabolized in liver except REMI
2- remi is broken down by nonspecific esterases by hydrolysis in the plasma 3- demerol gets metabolized into an active metabolite (normeperidne) causes seizures with prolonged use |
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Do opioids increase ICP?
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No, if pCO2 elevates then increase in CBF may increase ICP but it was not the opioid it was they hypercarbia
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Complications of Narcan
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HTN
CVA pulmonary edema cardiac arrest/Death Vfib/Vtach |
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Trexane (naltrexone) is also used as what
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appetitie suppressant
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Duration of action of Narcan
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30-60 minutes
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What should you look for after you give narcan to a patient.
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could re-narcosize (is that really a word?) pt could go apneic again if narcotic is still on board and narcan has redistributed
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How best to give opioids?
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Front load, want pt breathing at end of case, but still want analgesic effects working. Do not want to have to give narcan to get pt to breathe.
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when tolerance to an opioid occurs there is simultaneous ____ tolerance to other opioid agonists
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cross
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why is merperidine CONTRAINDICATED with pts that are on MAOIs?
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they may suffer a sertoninergic crisis manifested as clonus, agitation, hyperrefllexia and hyperthermia. (seizure)
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repeated doses of methadone do what?
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subsequent doses of methadone appear to last much longer than the initial dose. used for chronic pain, has low euphoric effect
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How are larger doses of fentanyl different?
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in doses of fentanyl >20mcg/kg redistribution may be insufficient to bring plasma conc. to subtherapeutic levels. In this circumstance, termination of effect depends on the much slower elimination process and the drug appears long-acting.
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How do opiates affect inhaled anesthetics?
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Opioids produce a dramatic dose-related decrease in the need for inh. anesthetics, they are frequently used for this reason.
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what drugs do opiates potentiate?
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barbiturates, benzodiazepines and propofol
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Which opiates cause histamine release?
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morphine and meperidine
really all phenanthranes and meperidie |
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opioid-induced nausea can be exacerbated by?
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vestibular input, problematic in ambulatory patients
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