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27 Cards in this Set

  • Front
  • Back
opioid ladder
step 1 - pain ~ asprin
step 2 - persistant pain/increase ~ codeine (weak opioid)
step 3 - severe pain ~ morpheine (Strong opioid)
drugs to know
morphine
fentanyl
methadone
meperdine
buprenophrine
tramadol
natural ops
morphine
codeine
semisyn ops
heroin
synthetic ops
fentanyl
methodone
bupreophine
ops ANTAG
naloxone (narcan)
naltreone (trexan)
Use of ops
acute/chronic pain

~ acute pulm edema
~ cough (non-produc)
~ diarrhea
~ regional analgesics (epidural/subarach)
MOA
5 receptors in the brain major ones

Mu1, kappa, Delta

have ag/antag/and mix effects

GCPR (Gi/go)

presynap - mu receptors
adencyl cyclase inhib

post synp- hyperpol

inhibt nuuronal act via GABA in the sub gelationsa
Mu receptor
supraspinal analgisia
Visc SM
phyiscal depend liability
Kappa
spinal analgeisa
affinty of ops to receptors - Mu
all ag except codeine are strong
~ buprenopine (PAg)
~ both antag
effects on organs
CNS
~ N/V
~ miosis
~ resp depression
~ polikothermia

Periph effects
~ decreased GI
~ vasodilation/ inhib baroreceptors
~ decreaesd CRF and GnRH
~ increaesd tone of detrusor/spintcter (bladder)
MORPHINE effects
decreases presyn NE release in locus Cer by acting on Mu receptors - over time up reg of NE post syn receptors

w/ withdrawl...~ ADERNERGIC STORM!

no real tolerance to
vomiting, resp depression, miosis
Analgesic ~ morphine
STRONGEST
~ all types of pain
~ dull pain relieved more then sharp
~ nociceptive >> neuropathic (damaged neurals)
~ moder. affec on pain threshold
~ releive discomfort/suffering
morph - MOA
inhib sub P (excite) in spinal cord
- inhib of nociep transmission
- activation of bulbospinal (inhibit pain perception)

EFFECTS
~ feel foggy/detached
~ euphoria
~ kick/thrill in tummy
~ decrease sex, hunger, thrist
~ drowsy

CVS
~ arteriola/venous DIALATION
- histamine release
- hypercapina (due to resp depression)
- DEPRESSION of baroceptors

~ can cause hypotension
moprh- GI
~ increase in tone
~ decrease in propulsive contractions

~ N/V
morph - resp
~ all phases of resp activity depressed
~ reduced resp to Co2 in brain
~ pons/medulla depressed
~ broncoconstrtion
~ depress in cough reflex
morph - other effects
indirectly inhibits gaba in some CNS neurons - excititory

decreased PIH, CRH, GnRH
incread prolactin/GH
depression of IMMUNE w/ LT use
morph - pharmokinetics
biotransformed w/ gluconronic A

M-6-glucuronide ~ ACTIVE (longer t1/2 then morphine) - excerted by kidney
Fentanyl
potent then morph
~ maintain cardiac stab (minimal vaso D)
~ maintain gen anestheisa
~ can stay in lipid tissues...leech out later
meperidine & congeners
mu/kappa ag
~ less effect on smooth musc
~ more freq CNS excite
~ stimulent on utuerus
loperamide
excerts only constp effect ~ unless highdose then op effect
pentazocine
kappa/siggma (weak mu)
~ increase BP/hr
~ less constp/vomit
bupreorphine
partial mu
~ dissoc slow from receptors
~ longer duration
~ lower dependence liability
tramadol
syn to active metabolite
~ good for neuropathic pain

MOA ~ ne and 5ht reuptake blocker, dont use with SSRI's

~ treat labor pain
~ less neonatal resp depression
~ lowers seizure threshhold
opiod resistance pains
phantom limb
skeletal m spasm
tension headaches
increase ICP
contra indications
respitory is decreased
impaired liver/kidney
Crohn's, constipation
prostatic hypertrop