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27 Cards in this Set
- Front
- Back
opioid ladder
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step 1 - pain ~ asprin
step 2 - persistant pain/increase ~ codeine (weak opioid) step 3 - severe pain ~ morpheine (Strong opioid) |
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drugs to know
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morphine
fentanyl methadone meperdine buprenophrine tramadol |
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natural ops
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morphine
codeine |
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semisyn ops
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heroin
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synthetic ops
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fentanyl
methodone bupreophine |
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ops ANTAG
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naloxone (narcan)
naltreone (trexan) |
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Use of ops
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acute/chronic pain
~ acute pulm edema ~ cough (non-produc) ~ diarrhea ~ regional analgesics (epidural/subarach) |
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MOA
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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 |
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Mu receptor
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supraspinal analgisia
Visc SM phyiscal depend liability |
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Kappa
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spinal analgeisa
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affinty of ops to receptors - Mu
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all ag except codeine are strong
~ buprenopine (PAg) ~ both antag |
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effects on organs
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CNS
~ N/V ~ miosis ~ resp depression ~ polikothermia Periph effects ~ decreased GI ~ vasodilation/ inhib baroreceptors ~ decreaesd CRF and GnRH ~ increaesd tone of detrusor/spintcter (bladder) |
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MORPHINE effects
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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 |
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Analgesic ~ morphine
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STRONGEST
~ all types of pain ~ dull pain relieved more then sharp ~ nociceptive >> neuropathic (damaged neurals) ~ moder. affec on pain threshold ~ releive discomfort/suffering |
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morph - MOA
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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 |
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moprh- GI
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~ increase in tone
~ decrease in propulsive contractions ~ N/V |
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morph - resp
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~ all phases of resp activity depressed
~ reduced resp to Co2 in brain ~ pons/medulla depressed ~ broncoconstrtion ~ depress in cough reflex |
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morph - other effects
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indirectly inhibits gaba in some CNS neurons - excititory
decreased PIH, CRH, GnRH incread prolactin/GH depression of IMMUNE w/ LT use |
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morph - pharmokinetics
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biotransformed w/ gluconronic A
M-6-glucuronide ~ ACTIVE (longer t1/2 then morphine) - excerted by kidney |
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Fentanyl
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potent then morph
~ maintain cardiac stab (minimal vaso D) ~ maintain gen anestheisa ~ can stay in lipid tissues...leech out later |
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meperidine & congeners
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mu/kappa ag
~ less effect on smooth musc ~ more freq CNS excite ~ stimulent on utuerus |
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loperamide
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excerts only constp effect ~ unless highdose then op effect
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pentazocine
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kappa/siggma (weak mu)
~ increase BP/hr ~ less constp/vomit |
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bupreorphine
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partial mu
~ dissoc slow from receptors ~ longer duration ~ lower dependence liability |
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tramadol
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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 |
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opiod resistance pains
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phantom limb
skeletal m spasm tension headaches increase ICP |
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contra indications
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respitory is decreased
impaired liver/kidney Crohn's, constipation prostatic hypertrop |