Flashcards in Opioid analgesics Deck (55):
Difference between analgesia and anesthesia
Analgesia - Block pain transmission
Anesthesia - Block sensory neurotransmission
What does qd mean?
What does bid mean?
Twice a day
What does Q12 mean?
Every 12 hours
What does tid mean?
three times each day
The _____ in the brain assigns aversive or pleasurable qualities to pain
The ____ in the brain is involved in fear/pain expectation
Name the key brain regions expressing opioid receptors
Rostral ventral medulla
Dorsal Root Ganglion/Dorsal Horn
Opium contains two types of alkaloids, name them.
Phenanthrene opoids primarily show differences at
3 and 6 positions
Phenanthrene partial antagonism is conferred by....
bulky side groups
Significance of knowing which drugs are Phenanthrene and which are non-Phenanthrene?
Some patients respond better to one type than the other, so in patients struggling with pain or side effects of one, the other may help a lot.
Three examples of Phenanthrenes
Four examples of non-Phenanthrene
Name a Phenanthrene antagonist
How are Phenanthrene opioids metabolized
Glucorinidation at the 3, 6 position
With morphine-6-glucoronide, the metab. is still active
Which organ(s) runs opioid metabolism
Metab. is largely hepatic, impaired with liver disease
Metabolites are excreted through the kidneys
Name the different types of Opioid receptors
G Protein Coupled (Family A/Gio coupled)
Nociceptin, orphanin FQ receptor
Natural agonists of mu opioid receptors
Beta endorphins (endogenous morphine)
Why target mu opioid receptors therapeutically
Analgesia (NOT for sharp localized, neuropathic pain)
Antitussive (suppresses the cough reflex)
Important sid effects of mu opioid drugs
Significance of the kappa opioid receptor
Involved in negative feedback loop, inhibiting the release of dopamine. The first dopamine causes dynorphin transcription. Its release activated presynaptic kappa receptors on dopaminergic terminals, inhibiting further release
Name the endogenous kappa agonist
Delta opioid receptors are being considered for treatment of...
Anxiety, Depression, OH Abuse
Why are delta opioid so interesting in the context of chronic pain?
They are upregulated with chronic stimulation
Natural ligand for delta opioid receptor?
Why do we care about the orphanin opoid receptor like subtype 1
Debate on activity, opposes classic mu effects and mediates pain
Describe the molecular signalling of opioids
opioid binds to GPCR. They're all Gi/o coupled, which causes them to inhibit ACyc, and thus decrease cAMP. They also turn on GIRK, causing hyperpolarization and inhibiting NT release.
Presynaptic inhibition of neurotransmitter release is mediated by...
Inhibition of calcium uptake
Postsynaptic inhibition of pain transmission is medicated by...
hyperpolarization through GIRK channels
Which two opioids are typically used in surgical mu analgesia
Which opioid can be used via IV, Patch, or Lollipop
Other name for hydromorphone
Why is morphine most common
Covered by medicare
Other names for hydrocodone
Other names for oxycodone
Name as many clinically used opioids as you can
Sufentanil, Remifentanyl, Fentanyl
Codeine, Hydrocodone, Oxycodone
Tramadol, Loperamide, Propoxyphene
Other name for meperidine
Other name for tramadol
Negative effect of methadone
Meperidine is used to treat...
Problems with meperidine?
Its metabolite (normeperidine) is neurotoxic (tremors, twitches, seizures)
Loperamide is used for...
How do Tramadol and Tapentadol work?
Mild opioid analgesic
Help with management of mild neuroathic pain
Which patients is Meperidine especially dangerous in?
Patients with decreased renal function
Important details for Methadone
Primarily used for opioid dependence
It has a long duration of action/half life (15-60 hrs)
NMDA antagonist to help Chronic pain treatment
Important details on Levorphanol
Long half life (16 hr)
NMDA antagonist for neuropathic pain
Two receptors upregulated by chronic pain
Which opioids are known for NMDA action
Methadone and Levorphanol
Which drug is a partial mu agonist
Which drugs are mu antagonists
When to use Buprenorphine
Used to treat opioid withdrawl in addiction therapy
Combined with naloxone for maintenence therapy
Which opioids are used for postop, epidural. Why?
4-5X the half life of fentanyl
Which opioids are used for pain maangement. Why?
Oxycodone, Hydrocodone, Oxycontin, Zohydro
Oral bioavailability, longer halflife
Which opioid is used for terminal cancer pain? Why?
Cost, History of Knowledge, No worries about dependence