PK
ABSORPTION
GI tract
nasal mucosa
Lungs
Subcutaneous
IM
IV
DISTRIBUTION
morphine accumulates in kidney, lung, liver, and spleen
CNS: primary site of action (analgesia/sedation)
METAB./excrete
metab: liver
conjugate w/glucuronic acid
excrete: kidney
T1/2: 2.5 to 3 hours (x stay in body tissue)
main excretion product : morphine-3-glucoronide
DOA 10mg : 3 to 5 hrs
ADMINISTRATION
x oral- erratic
1st pass efect varies in person
Subtopic 3
iv- works fast
main effect: CNS
EFFECT in cns
analgesia
rxn & perception
cancer pts tolerate more
most effective dull aching pain
sharp
stabbing
shooting pain
pain-free person. 1-> dysphoric
sedation
sedation. yes!
LOC no!
euphoria
mood change
mental cloudiness
Respiratory depression
< rate
< vol
< tidal volume
mu recep. activxn
< responsive to PCO2. build up PCO2
irregular breathing patern. apnea
nausea & vomiting
activxn of CTZ
afferent: ear & gut
motion sickness
pupil size
miosis (pinpoint pupil)
kappa recept.
oculomotor (CNIII) stimulated)
cough supression
EFFECT on CVS
vasodilation -> < bp
release of histamine
suppression of central adrenergic tone
supress reflex vasoconstriction
EFFECT on GIT
> tone, < motility= constipation
< HCL in stomach
x tolerance
EFFECT on SMOOTH MUSCLE
biliary tract
> pressure biliary tract
> contraction Sphincter of Oddi
bladder
tone of detrusor muscle increased
urinary urgency
urinary retention -> > muscle tone ? sphincter closed off
bronchial muscle
bronchoconstriction
contraI: asthmatic
uterus
> tone, prolong labor
EFFECT on neuroendocrine
< GNRH, < CRF
< LH ,FSH, ACTH
< cortisol & testosterone
TOLERANCE
YES
nausea
analgesia
sedation
respiratory depression
cardiovascular
euphoric
NO
miosis
constipation
TOXICITY
excitatory and spinal reflexes
>OPIOID = convulsions (agonist antagonist)
Respiratory depression
pinpoint pupils
coma
TX
1. establish adequate ventilation
2. give OPIOID antagonist (naloxone)