Term
|
Definition
drug derived from opium (semisynthetic congers)
opium like |
|
|
Term
|
Definition
all agonist and antagonists natural and synthetic
morphine like |
|
|
Term
|
Definition
strone opiate analgesic
often abused
not a pharmacological word |
|
|
Term
|
Definition
|
|
Term
| what is the ascending pain pathway |
|
Definition
| noxious stimuli > nociceptor > primary afferent neuron > dorsal horn > secondary neuron (spinothalamic) > supraspinal nuclei in thalamus > limbic system and primary somatosensory cortex |
|
|
Term
| what are the two types of primary afferent neurons / nocioceptors |
|
Definition
somatic pain A delta (Ad) fibers
visceral pain C fibers |
|
|
Term
| somatic pain A delta (Ad) fibers: size, composition, speed, location |
|
Definition
small
unmyelinated
fast, high threshold
terminate in laminae I |
|
|
Term
| somatic pain A delta (Ad) fibers: what do they sense, what do they cause |
|
Definition
sense mechanical and thermal
cause sharp localized pain |
|
|
Term
| visceral pain C fibers: size, composition, speed, location |
|
Definition
large
unmyelinated
slow
terminate in laminae II (substantia gelatinosa) |
|
|
Term
| visceral pain C fibers: what do they sense, what do they cause |
|
Definition
sense: mechanical, thermal, chemical
cause: dull, diffuse, achine, burning pain |
|
|
Term
| how do affernt neurons work |
|
Definition
| release excitatory AA into dorsal horn (C fibers also release neuropeptides) |
|
|
Term
| describe the decending pain pathway |
|
Definition
periaqueductal gray in midbrain and nuclei of rostroventral medulla > dorsal horn > NE/SE release > inhibit ascending pathway...
directly: direct synaptic inhibition
indirectly: activate inhibitory interneurons |
|
|
Term
| what are the three endogenous opioid peptides |
|
Definition
enkephalins
endorphins
dynorphin |
|
|
Term
| general locations of enkephalins |
|
Definition
in interneurons
pain areas, emotion areas, motor areas, antonomic reflex areas, inhibitory areas |
|
|
Term
| pain areas of enkephalins |
|
Definition
| laminae I and II, spinal trigeminal nuclei, PAG midbrain |
|
|
Term
| emotion areas of enkephalins |
|
Definition
|
|
Term
| motor sreas of enkephalins |
|
Definition
|
|
Term
| autonomic reflex areas of enkephalins |
|
Definition
| nucleus tractus solitaries |
|
|
Term
| inhibitory areas of enkephalins |
|
Definition
| dorsal horn causing inhibition of secondary ascending pain neurons |
|
|
Term
|
Definition
hypothalamus, nucleus tractus solitaris
anterior pituitary: Co-release with ACTH in response to stress |
|
|
Term
|
Definition
mangocellylar cells of hypothalamus
posterior pituitary: role in fluid homeostasis
CNS: all over, esp laminae I and II |
|
|
Term
| explain how opioid receptors work |
|
Definition
| Gi protein coupled receptor > adenylate cyclase > cAMP > increases K and decreases Ca conductance > inhibits neuron activity |
|
|
Term
| what do opioids cause clinically to help pain |
|
Definition
| effect transmission of pain and pain perception (I feel it but I don't care) |
|
|
Term
| what are the classes of opioid receptors |
|
Definition
Mu (m)
Kappa (k)
Delta (d)
65% homologous |
|
|
Term
| how do opioid analgesics work (the morphine model) |
|
Definition
full agonist of Mu receptors
high doses interact with other opioid receptors |
|
|
Term
| 12 CNS side effects of morphine |
|
Definition
analgesia
euphoria
mood alteration
dec cough reflex in medulla
nausea/emetic: stimulation of chemoreceptor in postrema of medulla
sleep
increased ICP (NO use in trauma!!)
hypothalamus: alters temp equlibrium
neuroendocrine: dec testosteone and cortisol
miosis
convulsions at high dose (esp kids) |
|
|
Term
| explain how opioids effect the hypothalamus |
|
Definition
alters temp equlibrium
acute: lowers
chronic: increases |
|
|
Term
| explain how opioids cause miosis |
|
Definition
| Mu and K agonists constrict pupil via parasympathetic |
|
|
Term
| what do opioids do to respiration (2) |
|
Definition
decrease response to CO2 in brainstem decreasing respiration
CAUSES DEATH IN MORPHINE POISONING
max effect 5-10 min after IV administration
cough: decreases cough reflex in medulla |
|
|
Term
| what do opioids to do GI (8) |
|
Definition
nausea/emetic: stimulation of chemoreceptor in postrema of medulla
stomach: Mu agonist dec HCl
Si: dec secretions, delay pooing, increase water absorption
LI: propulsive peristalsis stopped causing constipation
billiary: sphincter of oddi constricts and increases pressure and spasm in common bile duct
bladder: stops voiding reflex |
|
|
Term
| CV effects of opioids (2) |
|
Definition
| when standing causes histamine release leading to peripherial vasodilation and orthostatic hypotension |
|
|
Term
| effects of opioids in uterus (2) |
|
Definition
prolong labor
respiratory depression in neonate |
|
|
Term
| effects of opioids in skin (1) |
|
Definition
| dilation of cutaneous vessels in flushing |
|
|
Term
| all opioids have tolerance, cross tolerance, and physical dependence. define each |
|
Definition
tolerance: higher doses are needed to produce same response
cross tolerance: across all opioids
physical dependence: body adapts to presence of drug and requires it to function. termination causes withdrawl |
|
|
Term
| signs of withdrawl from opioids |
|
Definition
pupil dilation
hyperventilation
diarrhea
dysphoria |
|
|
Term
| interactions with opioids (3) |
|
Definition
MAOI: hyperpyrexic coma
sedative/hypnotics: increased CNS depression, respiratory depression
TCA/anti-psych: increased sedation, increased respiratory depression |
|
|
Term
| in order from least to most effective list the 9 pain killers less effective than morphine |
|
Definition
diphenyloxylate D
dextropropoxyphene 1/20
pentazocine 1/15
codine 1/12
tramadolol 1/12
mepheridine 1/10
hydrocodone 1/13
oxycothinin 2/3
oxycodone 2/3 |
|
|
Term
| what are the two drugs that have the same effectiveness as morphine |
|
Definition
|
|
Term
| what are the 6 drugs more effective than morphine from least to most potent |
|
Definition
diacetylmorphine 3-5x
butorphanol 5x
hydromorphone 7x
buprenophine 20-50x
fentynil 80x
sufentanil 800x |
|
|
Term
| what are the two "other" pain killers from least to most potent |
|
Definition
diphenyloxylate
tramadolol |
|
|
Term
| what are the 5 codine/codine derivative pain killers from least to most potent |
|
Definition
dextropropoxyphene
codine
hydrocodone
oxycotinin
oxycodon |
|
|
Term
| what are the 4 mixed pain killers from least to most potent |
|
Definition
pentazocine
nalbuphine
butorphanol
buprenophine |
|
|
Term
| what are the 7 opioid pain killers from least to most potent |
|
Definition
mepheridine
methadone
morphine
diacetylmorphine
hydromorphone
fentynil
sufentanil |
|
|
Term
| which pain killers cannot be taken oral (7) |
|
Definition
morphine* can but it sucks
nalbuphine
diacetylmorphine
butorphanol
buprenophine
fentynil
sufentanil |
|
|
Term
| what painkillers stronger than morphine or equal to can be taken oral (2) |
|
Definition
morphine* but it sucks
hydromorphone |
|
|
Term
| what painkillers can be taken IV IM (9) |
|
Definition
mepheridine
methadone
morphine
nalbuphine
butorphanol
hydromorphone
buprenophine
fentinyl
sufentanil |
|
|
Term
| which pain killers can be taken SC (3) |
|
Definition
morphine
nalbuphine
hydromorphone |
|
|
Term
| what painkiller can be taken nasal |
|
Definition
|
|
Term
| what painkiller can be taken rectal |
|
Definition
|
|
Term
| what pain killer can be taken sublingual |
|
Definition
|
|
Term
| what pain killer can be taken transdermal/transmucosal |
|
Definition
|
|
Term
| which pain killers have a different metabolism, describe it (4) |
|
Definition
codine: 10% converted to morphine
mepheridine: metabolized via N-demythylation to normepheridine
morphine: conjugated with glycorinic A to make morphine 6, excreted as morphine 3
diacetylmorphine: hydrolyzed to 6-monoacetylmorphine (lipid soluble), hydrolyzed to morphine |
|
|
Term
| MOA of the mixed opioids (4) |
|
Definition
pentazocine: partial Mu antagonist, K agonist
nalbuphine: strone K agonist, Mu antagonist
butorphanol: strong K agonist, Mu antagonist
buprenophinel: strong K agonist, Mu antagonist |
|
|
Term
|
Definition
inhibit NE/SE
weak Mu agonist |
|
|
Term
|
Definition
| oxycodone time release in higher doses |
|
|
Term
| which painkillers have a long duration (2) |
|
Definition
|
|
Term
| what pain killer has a rapid onset and short duration |
|
Definition
|
|
Term
| unique SE of dextropropxyphene |
|
Definition
not analgesic
not addictive
low toxicity
supresses CNS |
|
|
Term
| unique use of dextropropxyphene |
|
Definition
| antitussive: cough supression |
|
|
Term
|
Definition
| high dose increases catecholamines and thus BP |
|
|
Term
| unique use of pentazocine |
|
Definition
| help with withdrawl, releave some pain |
|
|
Term
|
Definition
often combined with ASA/APAP, NSAID
antitussive |
|
|
Term
|
Definition
analgesia not completely reversed by antagonist
seizure - never in epileptic!!
little respiratory depression
interacts with SSRI!! |
|
|
Term
|
Definition
|
|
Term
|
Definition
no CV/pupil effects when oral
metabolite cause tremor, twitch, convulsions
EVEN THOUGH ALL SHOULDNT GO WITH MAOI, THIS ONE REALLY SHOULDENT |
|
|
Term
| unique use of mepheridine |
|
Definition
|
|
Term
| unique use of hydrocodone |
|
Definition
| often combined with ASA/APAP, ibprofen |
|
|
Term
|
Definition
| often combined with ASA/APAP |
|
|
Term
|
Definition
|
|
Term
|
Definition
| help with withdrawl (because it has a more mild one) |
|
|
Term
|
Definition
low abuse
depresses respiration |
|
|
Term
| unique SE diacetylmorphine |
|
Definition
| fast euphoria due to lipid solubility |
|
|
Term
|
Definition
| increased workload on heart |
|
|
Term
| unique use of butorphanol |
|
Definition
| not good for chronic pain, acute only |
|
|
Term
|
Definition
| less respiratory depression |
|
|
Term
|
Definition
| added to naltrexone to make auboxone to maintain opioid dependent pt |
|
|
Term
|
Definition
| interaction with deoperidol (neuroleptic anesthesia) |
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
| which pain killers are used for cough supression |
|
Definition
|
|
Term
| what pain killers are used to help with withdrawl (3) |
|
Definition
pentazocine
methadone
buprenophine |
|
|
Term
| what pain killers are often combined with ASA/APAP, of other mild pain killer |
|
Definition
codine
hydrocodone
oxycotinin |
|
|
Term
| what are the 4 opioid antagonists |
|
Definition
naloxone
naltrexone
nalmefene
methylabaktrexibe |
|
|
Term
| naloxone: administration, duration, distribution |
|
Definition
IV, IM, SC
duration 1-4h
completely metabolized 1st pass |
|
|
Term
|
Definition
| tx opioid dependency and toxicity |
|
|
Term
| naltrexone: administration, duration |
|
Definition
|
|
Term
|
Definition
opioid toxicity and dependence
alcoholism |
|
|
Term
| nalmefene: administration, use |
|
Definition
IV
pure opioid antagonist (best) for tx opioid dependency and toxicity |
|
|
Term
| methylabaktrexible: administration, distribution and SE |
|
Definition
SC
unable to cross BBB so no pain killing |
|
|
Term
|
Definition
| prevent morphine constipation |
|
|
Term
| what is the restriction of all opioid antagonists |
|
Definition
|
|
Term
| what is the story used for pain killers less than morphine |
|
Definition
i died from phenyl
dex tried to operate
he penetrated
the code in my
tramp stamp
me phrend the dean
stole my hydrocodone
oxycotinin
and oxycodone |
|
|
Term
| what is the story used for paiin killers same sa morphine |
|
Definition
meth done
morphed into a
nail biting pheind |
|
|
Term
| what is the story used for pain killers more than morphine |
|
Definition
heroine
butt and or oral
hydrates me
but phrends no me
fender
suffers |
|
|
