Analgesics Flashcards
What receptors are responsible for the analgesic effects of opiates
Mu receptors
What drug class is morphine
opioid
What is a narcotic
A narcotic is an opioid (opiate) drug- dervived from unripe opium poppy (papaver somniferum)
What is the administration route of morphine
PO, PR, IM, IV
In which acute situation is morphine often used
acute MI because of the vasodilation, anxiolytic, and pain relief effects
What are common side effects of morphine (7)
respiratory depression, miosis, itching, constipation, paralytic ileus, N/V, dependence
What category is morphine
category C (may have adverse effects on fetus, but no human studies) Morphine crosses placenta and can cause dependance in fetus
How does Fentanyl (duragesic) differ from morphine
It is 80x more potent, which means it has a much greater respiratory depression
how is fentanyl administered
transdermal patch, lollipop or lozenge (sublingual), IV
what are side effects of fentanyl
constipation and paralytic ileus, N/V, addiction
What drug type cannot be used with fentanyl
concomitant CYP450 inhibitors can lead to fatal blood levels of fentanyl (like grapefruit juice)
What can effect the efficacy of the fentanyl patch
cutting the patch will mess up the timed release, and heating the patch affects the dose delivered as well
What are the uses of codeine
It is an anti-tussive in addition to being an analgesic
How does codeine compare to morphine
It is converted to morphine by the body, but is a much weaker analgesic. codeine is much better at cough relief.
what category is codeine
category C
what are common side effects of codeine
sedation, constipation, itching. ultra-rapid metabolizers can die from normal doses of codeine, essentially a morphine OD
What neuro effect does tramadol (Ultram) have
affects dopamine and serotonin as well as weak mu-receptor agonist, which makes the person tolerate pain better, as well as reducing pain
how does heroin differ from morphine
it is more lipid soluble, and thus crosses BBB and induces a greater euphoric effect. it is 2x as potent, and way more addictive than morphine
What is methadone used for
opioid used in the controlled withdrawal of heroin and morphine in addicted patients
What is Naloxone (narcan) used for
opioid OD, reverses coma and respiratory depression
What is the MOA of Naloxone (narcan)
Opioid ANTAGONIST bind with high affinity to opioid receptors but do not activate the receptor mediated response.
What is dextromethorphan
The dextro-isomer of codeine
How does dextromethrophan differ from codeine
It has little to no analgesic, sedative, or GI effects (non constipating)
what drug class is Aspirin/ Acetylsalicylic acid (ASA)
NSAID
Is aspirin a reversible or irreversible COX inhibitor
it is irreversible, thus no aspirin 14 days before surgery
What is a risk of kids using aspirin
Reye’s syndrome, salicylism (dizziness, tinnitus, hyperventilation, craziness)
Is ibuprofen (motrin, advil) reversible or irreversible COX inhibitor
reversible, so no platelet aggregation issues
What drug class is celecoxib (celebrex)
NSAID, selective COX-2 inhibitor
Why was vioxx (rofecoxib) pulled from the market
increased cardiovascular events after 7 months of use
What class is acetaminophen (tylenol)
NSAID, inhibits COX-3
What NEVER mixes with tylenol
alcohol
What happens in an acetaminophen overdose
The byproduct NAPQI builds up in the liver and binds to vital proteins in the lipid bilayer in hepatocytes, causing cell death and necrosis
What category is acetaminophen
category B
How is acetaminophen antidoted
N-acetylcysteine administration ASAP
What is the maximum dose of tylenol in the absence of any alcohol or liver disease (considered safe adult dose)?
4 grams/ 24 hours
What is considered an overdose of tylenol?
> 7 grams/24 hours
indication for celebrex?
inflammation, pain, treatment of adenomatous polyps, can also be used in people with peptic ulcers
Which analgesic agent would not cause constipation?
dextromethorphan
What DEA category is Heroin?
DEA category CI
What are endogenously made opiates called?
Opiopeptins : endorphins, enkephalins
