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Opioid/NonOpioid Pain Medications
Lecture 1 Overview
60
Audiology
6th Grade
10/17/2013

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Term
dull, aching, throbbing, localized, worse with movement
Definition
somatic pain
Term
irritable bowel pain, gas pain
Definition
visceral pain
Term
lightening, streaking, radiating, pins and needles, electrical
Definition
neuropathic pain
Term
Charlie horse, gripping, spasms
Definition
muscle spasm pain
Term
somatic pain treatment
Definition
opioids, NSAIDs, Calcitonin, bisphosphonates, Steroids, Radiation
Term
visceral pain treatment
Definition
difficult to treat; may use nerve blocks, itnrathecal w/ opioid and/or local anesthetic; epidural; octreotide; antispasmodics
Term
neuropathic pain treatment
Definition
TCAs, SNRIs, anticonvulsants, topiramate, capsaicin, Lidoderm patches, steroids, opioids
Term
drug of choice for pregnancy and patients on warfarin
Definition
acetaminophen
Term
synergistic with acetaminophen and/or opioids; ceiling effect (increased dose gives no added analgesia); not recommended to be used in heart failure ; use caution in patients on warfarin
Definition
NSAIDs
Term
Advantages include no ceiling effect; Disadvantages include GI effects and physical dependency
Definition
Opioids
Term
constipation in opioids
Definition
decreased peristalsis and intestinal secretions due to interaction with the mu-2 receptors in the GI tract
Term
pruritus in opioids
Definition
interaction with the MOR-1D receptor which subsequently connect to GRPR to relay itch signals
Term
Nausea and vomiting in opioids
Definition
activation of opioid receptors in the chemotherapy trigger zone
Term
Respiratory depression in opioids
Definition
interaction with the mu-2 (and possibly delta) opioid receptors in the brain
Term
sedation in opioids
Definition
interaction with kappa opioid receptors in the brain
Term
can be opened and sprinkled into food
Definition
Kadian (long acting morphine)
Term
Morphine clinical pearl:
Definition
used in dyspnea management and myocardial infarctions
Term
morphine 6-glucuronide (metabolite)
Definition
analgesic properties
Term
morphine 3-glucuronide (metabolite)
Definition
toxic, can accumulate in patients with renal failure and may lead to seizures
Term
Advantages include more potent and faster onset; lower SEs and once daily ER formulation, no major metabolites; Disadvantages include more expensive, less formulations, higher risk
Definition
Hydromorphone (Dilaudid)
Term
Not used orally due to erratic absorption
Definition
Meperidine (Demerol)
Term
Meperidine (Demerol) cautions
Definition
do not use for more than 48 hours; do not give more than 600 mg/day; never use for chronic pain
Term
because of fast onset of action there is an increased risk of respiratory depression and death with transmucosal forms
Definition
Fentanyl
Term
Fentanyl patches
Definition
don't use for acute pain
Term
Codeine
Definition
prodrug whose active metabolite is morphine
Term
Codeine + APAP (Tylenol #3)
Definition
10-30% of dose is metabolized into morphine by CYP2D6
Term
inhibit CYP2D6
Definition
Phenothiazine, haloperidol, fluoxetine, paroxetine
Term
several reports of death in patients who are ultra-rapid metabolizers (CYP2D6)
Definition
Tylenol #3
Term
schedule III drug; more pain relief and longer duration than codeine, better tolerated than codeine
Definition
Hydrocodone + APAP (Norco, Vicodin, Lortab)
Term
better tolerated than morphine, more potent analgesic than codeine or hydrocodone
Definition
Oxycodone (Roxycodone, Oxyccontin, Percocet)
Term
Oxycodone Pearls
Definition
contains an active metabolite with a 7-9 hour half life; risk of respiratory depression when used with CYP3A4
Term
CYP3A4 drugs
Definition
macrolides, azoles, protease inhibitors
Term
long duration of action; inexpensive, may be more effective for neuropathic pain, less euphoria, less constipation; difficult to dose-- QT prolongation at high doses
Definition
Methadone
Term
gives methadone its opioid activity
Definition
l-isomer
Term
NMDA receptor antagonist and an NE and serotonin reuptake inhibitor
Definition
d-isomer of methadone
Term
Food increases Cmax by 50%-- administer on an empty stomach; twice a potent as oxycodone;
Definition
Oxymorphone (Opana, Opana ER, Numorphan)
Term
Mixed Agonist-Antagonists
Definition
Pentazocine, Butorphanol, Nalbuphine
Term
less respiratory depression, less physical dependency, schedule IV; Ceiling effect, CNS effects
Definition
Mixed agonist-antagonists
Term
Partial Agonists
Definition
Buprenorphine (Buprenex, Subutex, Butrans)
Term
High doses = Addiction; Low Doses = Pain
Definition
Buprenorphine
Term
Buprenorphine advantages
Definition
opioid detox w/ suboxone; decreases or prevents craving; treats pain; transdermal patch 1 every 7 days
Term
Buprenorphine disadvantages
Definition
ceiling effect, high receptor affinity, can be difficult to reverse respiratory depression, can bind to opioid receptors for up to 48 hours; transdermal patch is not for acute pain
Term
Opioid antagonists
Definition
Naloxone, Naltrexone, methylnaltrexone, Alvimopan
Term
used for opioid overdose, respiratory depression reverse constipation or ileus without reversing analgesia
Definition
Naloxone (Narcan)
Term
used for opioid dependency, ethanol dependency
Definition
Naltrexone (Revia, Vivitrol)
Term
SC injection used for treatment of opioid-induced constipation when response to laxative therapy has been insufficient
Definition
Methylnaltrexone (relistor)
Term
NTE 2 grams/day if history of liver disease or alcoholism
Definition
acetaminophen (Tylenol)
Term
weak mu-receptor binding; inhibition of norepinephrine serotonin reuptake (SNRI)
Definition
Tramadol (ultram, ultram ER, ryzolt, ultracet)
Term
advantages of tramadol
Definition
non-controlled, less respiratory depression, good for neuropathic pain, minimum physical dependency
Term
disadvantages of tramadol
Definition
risk of serotonin syndrome, lowers seizure threshold, may be less effective
Term
inhibits spinal reflexes, structural analog of gamma-aminobutryric acid (GABA)
Definition
Baclofen (Lioresal)
Term
use caution in renal or liver impairment, prodrug of meprobamate, low doses may be just as effective as high doses, potential for abuse
Definition
Cansoprodol (Soma)
Term
structurally related to amitriptyline, greatest evidence for efficacy, low dose maybe just as effective, potential for abuse
Definition
Cyclobenzaprine (Flexeril)
Term
neuronal inhibition via GABA receptors; available IV/IM
Definition
Diazepam (Valium)
Term
Significant effects include urine discoloration (brown, green)
Definition
Methocarbamol (Robaxin)
Term
Significant Effects: paradoxical muscle cramps, mild withdrawal symptoms
Definition
Metaxalone (Skelaxin)
Term
dizziness, somnolence, blurred vision, edema, weight-gain; decrease dose in renal impairment
Definition
Pregabalin (lyrica)
Term
same effects as Lyrica.....not indicated for neuropathic pain, less effective
Definition
Gabapentin (Neurontin)
Term
increase BP, HR, sexual side effects, restless leg syndrome
Definition
Duloxetine (Cymbalta)
Term
can be used for suicide. doses fro pain are lower than doses for depression
Definition
Amitriptyline (Elavil)
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