Opioids Flashcards
Natural opioids; which one is more potent
Morphine and codeine; morphine 6-7x more potent
Compound used to treat mod to severe pain and has sedative effects
Narcotics
Where are synthetic opioids derived from
Morphine
What endogenous receptor is mainly responsible for central interpretation of pain?
Mu1
What are the two components of analgesia
Sensory or affective
Sensory: tells you location, intensity, type of pain
Affective: need a negative perception/feeling of that pain
what are the effects for analgesic drugs
Analgesia, euphoria, sedation, respiratory depression, miosis, cough suppression, emesis, constipation(for diarrhea), renal: urinary retention, decrease force of contraction in labor, cardiovascular: hypotension, bradycardia, histamine release: urticaria (hives), itching
In what situation Do we need to be aware of when giving opioids
If patient has head trauma bc opioid cause respiratory depression which cause reflexive cerebral vasodilation
What’s the 1st sign of overdosing opioid
Pin point pupils
Main therapeutic effects of opioids
Analgesia, anesthetic, cough suppressant, diarrhea, acute pulmonary edema
What drugs should not be mixed with opioid?
CNS depressants -respiratory depression
MES inducers -meperidine formation of normeperidine
MAOI: meperidine–>hyperrexia rxn/HTN
Mixed agonist/antagonist
Strong opioid agonists binds with primarily which receptor?
Mu receptor
what agent is used to treat opioid addiction
methadone
which opioid could be used transdermally?
Fentanyl
which drug is used for immediate acute opioid overdose?
Naloxone
Which drug is used as maintenance drug for opioid overdose?
Naltrexone
which drug is the primary pharmacological use for opioid addiction?
Methadone
what is a good way to get someone off morphine?
switch morphine into methadone, and slowly taper it off
what does Gi/Go coupling do?
inhibit adenylyl cyclase activity–>loss of intracellular Ca and decrease release of NT
increase post synaptic opening of K+ channels–>hyperpolarization which decrease firing
Mu1 response
central interpretation of pain–supraspinal analgesi
Mu2 responses
supraspinal and spinal anaglesia, physical dependence, eurpho, constipation, euphoria, respiratory depression
kappa responses
NO respiratory depression and no dependence
only modest supraspinal and spinal anaglesia
inhibit dopamine release–> dysphoria
Delta
used for modest supraspinla and spinal analgesia. modulate hormone and NT release, regulate mu recetpor activity
a little addictive
what does morphine metabolize into?
morphine-6-glucuronide
what metabolizes to morphine
heroin and codeine
Ascending pathway way pain inhibition:
peripheral stimulus at site of injury–> presynaptic activation of opioid receptor to Mu receptors in dorsal horn–>decrease activation of Ca–> reduce incoming pain signaling
Post synaptic: opioids inhibit activation of afferent neurons via K+ conductance lead to hyperopolarization–>reduction in pain signaling pain up spinal cord to cortex
binding to GABA-A–> inhibition
what is dextromethophan primarily used for
cough suppressant, antitussive
diphenoxylate primary use
antidiarrheal agent
loperamide
antidiarrheal agent
Tramadol
mu agonist plus serotonin inhibitor
which drug blocks Kappa receptors
Buprenorphine
which drugs activate Kappa
pentazocine, nalbuphine butorphanol
what does morphine regulate
relief of moderate to severe pain, suppression of severe diarrhea
which opioid is used for surgical settings
hydromorphone
what are the benefits of using codeine
does not have intense respiratory depression, less chance of addiction, abuse potential. Produce less euphoria but can produce significant sedation.
what drug is used for breakthrough pain/post surgical pain
oxycodone
what is only available combined with NSAIDs
hydrocodone
