test 5 Flashcards
morphine pharmikokinetics
t1/2=2/3 hours, metabolized in the liver(glucuronide formation), readily cross placenta-> respiratory depress the fetus
-standard dose is 10mg SC or IM
morphine drug interactions
addative defect with ethos, barbituates, bento, anti psychotics and into depress and anti Histamine
-MAOI- can cause severe hyperpyrexia(esp meperidine)
some anti histamines can increase the analgesic effects of morphine
-same as^ with tricyclic anti depress
opioid drug poisioning
triad-
cns depression(stupor or coma)
depressed depth and rate of breathing
pin point pupils (if pt severely hypoxic and near death pupils may dilate)
Treat- respiratory support and ventilation and naloxone (narcotic antagonist)
codiene
on list
oral admin
1/12 of morphine- dose 30-60 mg
analgesic for mild to moderate pain, antitusive
only a weak opioid agonist, but in most pts it is demethylated and converted to morphine to give its effect (genetic polymorphism)
Hydromorphone on list
similar to morphine but more potent
oxycodone
on list
oral admin, (alone or in combination with acetaminophen)
OXYcontin is a sustained release oral prep for chronic pain
hydrocodone
on list
orally in combination with acetaminophen for mild-mod pained anti tussive
very highly prescribed
Zohydro is an oral sustained release w/o acetamenophen
meperidine
on list
synthetic drug, oral and parenteral admin
1/10 morphine
-though to have less SM effect and less constapation and urine retention( weak support)
-short acting and not used for chronic pain
-used in OB b/c less rest depression of the fetus
Heroine
on list
more potent and euphoric than morphine, lasts 4-6 hours
not available for med use in US
injected or snorted
Methadone
on list
less euphoric and long-lasting(12-24 hours) than morphine(4-6) or heroine(4-6)
used an analgesic and treat opioid addiction
carefull dosing with monitoring
fentenyl
on list
very potent mu agonist(100x morphine)
used in surgery
neuroleptic anesthesia when used with NO gas and dropiridol(inovor)
pentazocine
on list
mixed opioid agonist and antagonist
agonist effects dominate- acts at K receptor but only partially at the mu receptor
mu antagonist at high doses
less effective for pain than morphine, less sedation and rest depression
more comon cns stim and hallucination
can ppct withdrawal in opioid addicts
given parenteral
Butorphanol
similar to pentazocine mixed opioid agonist and antagonist agonist effects dominate- acts at K receptor but only partially at the mu receptor mu antagonist at high doses less effective for pain than morphine, less sedation and rest depression more comon cns stim and hallucination can ppct withdrawal in opioid addicts can be given intranasally
buprenorphine
on list
partial agonist at mu R, antagonist at high dose
only slightly less analgesic effect than morphine but MUCH lower abuse potential
reduce craving of heroine addicts ( suboxone- combination this and naloxone to prevent abuse)
injected, sublingual, or intranasal
“Office based treatment of opioid addiction”
Tramadol
on list
partial mu agonist
mild to moderate pain used
inhibits synaptic repute of NE and serotonin like tricyclic anti depress
SE resemble other opioids( dizzy,sedate,nausea,constipation)
tapentadol
newer drug, like tramadol but higher activity at the Mu R
inhibits NE and 5-HT reuptake
used for moderate to severe pain, schedule 2
high abuse potential
Naloxone
on list
pure opioid antagonist- block most mu R, can pact withdrawal
drug for opioid poisioning, can reverse the rest depression
must be parenteral b/c of first pass metabolism
short acting 1-2 hrs
naltrexone
on list
Pure opioid antagonist long acting (24 hours) and orally given risk of hepatotox compliance is problem must be brought the withdrawal fist before treatment used for alcoholics to block cravings
clonidine
centrally acting adrenergic neuronal inhibitor
not a prodrug
similar action to methyl dopa as a a2 agonist to dampen simp outflow
lower doses than methyldopa, in patch form
no autoimmune SE, rebound HTN
treatment of: adhd, meno hot flash, stress disorder, nicotine and ethos withdrawal, ALSO TREAT OPIOID WITHDRAWL
methylnaltrexone
quaternary salt of naltrexone used specifically for opioid induce constipation
only given parenteral
post operative paralytic ileus
alvimopan and NAloxegol are similar
Acetyl Salicylic Acid
on list
Salicyclic Acid Derivatives
irreversible COX-1 and COX 2 inhibitors pKa=3.5
Mesalamine
Salicyclic Acid Derivatives
5-amino salicylic acid
Diflunisal
on list
Salicyclic Acid Derivatives-REVERSIBLE INHIBITS tisue COX
similar analgesic and anti inflame to aspirin
NO ANTI PYRETIC EFFECTS
t1/2=8-12(3-4x asprin)
acute to long term pain mild to moderate pain management
Indomethacin [IndocinR]
on list
Acetic Acid Derivatives
reversible COX1 and COX 2 inhibitors
not recommended in children under 14 b/c hepatotoxicity
aggrevate depressin
SE: headache, CNS disturbances
FDA approved for closing patent ductus arteriosus
Etodolac
Acetic Acid Derivatives
reversible COX1 and COX 2 inhibitors
Diclofenac
on list
Acetic Acid Derivatives
reversible COX1 and COX 2 inhibitors
Tolmetin
on list
Acetic Acid Derivatives
reversible COX1 and COX 2 inhibitors
indicated for JRA
SE:autoimmune hemolytic anemia
Ketorolac
on list
Acetic Acid Derivatives
reversible COX1 and COX 2 inhibitors
SE: strong headache
NO USE in RA or OA
Ibuprofen
on list
Propionic Acid Derivatives
reversible COX1 and COX 2 inhibitors
SE: high hypersensitivity triad of risk-fever rash, internal organ involvement
others: ab pain, headache, nausea, vomit, liver damage, meningitis in SLE pts
FDA aproved for closing patent ductus arteriosus
Naproxen
on list
Propionic Acid Derivatives
reversible COX1 and COX 2 inhibitors
indicated for JRA
Ketoprofen
on list
Propionic Acid Derivatives
reversible COX1 and COX 2 inhibitors
Oxaprozin
on list
Propionic Acid Derivatives
reversible COX1 and COX 2 inhibitors
Piroxicam (oxicams)
on list
enolic acid derivatives
reversible COX1 and COX 2 inhibitors
Meloxicam (oxicams)
on list
enolic acid derivative
reversible COX1 and COX 2 inhibitors
