Opioids Flashcards
Clinical observations in pts with morphine tolerance d/t prolonged use (physiological effects unchanged by tolerance)
miosis (pinpoint pupils)
constipation
**tolerance does not develop to the above clinical effects
Morphine is safe for use in asthmatics
True or False
False.
Morphine can cause bronchoconstriction and respiratory depression
effects of morphine on respiration
↓ Rate
↓ volume
↓ tidal exchange
CNS becomes less responsive to pCO1. Irregular breathing. Apnea. Build up of CO2
morphine can cause kappa opioid receptor to stimulate which cranial nerve causing what physiological effect ?
CNIII (Edinger-Westphal nucleus)
miosis
The drug ______ partially blocks kappa receptor reversing miosis
atropine
cardiovascular effects of morphine
vasodilation –> hypotension
GI effects of morphine
constipation
↓ HCl secretion
Effects of morphine on smooth muscle
biliary - ↑ pressure
bladder - ↑ detrusor muscle tone / urinary urgency / urinary retention
bronchioles - bronchoconstriction
*contraindication for asthmatics
uterus - contraction of uterus can prolong labor
Naloxone
displaces morphine from all receptors / immediate onset (3-5imn) / short duration (30-45min)
S/S morphine toxicity
respiratory depression
miosis
coma
Tx of morphine toxicity
ventilation
opioid antagonist (naloxone)
Contraindications for morphine
acute respiratory depression
renal failure (d/t morphine-3 and morphine-6-glucuronide metabolite accumulation
chemical toxicity
↑ intracranial pressure, head injury
biliary colic
potentiation
additive depression observed with coadministration of CNS depressants + OPIOID
buprenorphine
used in conjunction with methadone for detoxification / short and long term
mixed agonist-antagonist action
Diphenoxylate
therapeutic use: anti-diarrheal drug
little analgesic effect
similar to meperidine
methadone
similar potency to morphine
long duration = 16-20hrs
used in narcotic maintenance tx
meperidine
same potency as morphine
toxicity similar to atropine (dry mouth, dry as a bone, blind as a bat, red as a beet, mad as a hatter)
Fentanyl
synthetic
80-100X the potency of morphine
short onset (5 min) and duration (30-45min)
used as pre-op med
“china white”
Hydromorphone (Dilauded)
9X potency of morphine
less constipation
no miosis
ketone at 6 hydroxyl position of morphine
Heroin
derived from resin of poppy plant
“Lady, white girl, horse, black tar, brown sugar, smack, goods, H, junk, harry, beast”
crosses BBB rapidly (vs. morphine) and is hydrolyzed to morphine making more of the drug in the brain –> 3-4X more potent than morphine
Heroin
derived from resin of poppy plant
“Lady, white girl, horse, black tar, brown sugar, smack, goods, H, junk, harry, beast”
crosses BBB rapidly (vs. morphine) and is hydrolyzed to morphine making more of the drug in the brain –> 3-4X more potent than morphine
most lipophilic opioid
acetyl groups at 3 and 6-hydroxyl positions (instead of hydroxyl)
codeine
hydroxyl group replaces methyl group at 3 position
1/10 the potency of morphine
antitussive properties
withdrawl is relatively mild
hydroxyzine
potentiates meperidine action
unlike morphine: less constipation causes mydriasis (dilated pupils)
Mu-1 receptor
Analgesia
enhance development of physical dependence
