Opioids (Exam 1 Material) Flashcards
Opioids include all drugs (natural and synthetic) with ______ like properties, including _______
Morphine like properties
Including endogenous peptides
The standard of comparison for all opioid drugs is ____
Morphine
Opioids include all exogenous substances that bind specifically to _______ and produce
Opioid receptors & produce some agonistic response
**whether it is full or partial
In anesthesia, the standard of comparison is ____
Fentanyl
Most common use for opioid is:
Pain relief
Other uses for opioids include:
Premedication
Anesthesia supplement Primary anesthetic (not given often because so much would be needed)
Although opioids have some sedative properties, _____ is the primary use for opioids
Analgesia
Most common pre-op medication is ____
Morphine
Most common post-op medications are:
Morphine, Hydromorphone, and Fentanyl
Most common anesthesia opioids are:
Fentanyl, remifentanil, sufentanil, and alfentanil
What is special about Sufentanil?
Most potent, must be given under extreme caution
What are the most common opioids used in anesthesia? (2)
Fentanyl and Remifentanil
What is special about Alfentanil?
It is not as reliable, not given as much
What are the most common opioids given for chronic pain?
Morphine, oxycodone, and hydrocodone
What is Meperidine (Demerol) given for?
Used to be given for pain (less common now), but has anti-shivering properties
Oxycodone is most similar to what other PO med?
Hydrocodone
ALL opioid receptors belong to a superfamily of __________
SEVEN transmembrane-segment GPCRs
All opioid receptors are ____ and belong to the ______
GPCRs and belong to the Rhodopsin family of g proteins
By nature, opioid receptors are excitatory/inhibitory?
Inhibitory
Mechanism of action of the opioid receptor: (6)
Opioid binds to opioid receptor
GPCR is activated Adenyl cyclase is inhibited
Less cAMP is produced Ca++ is decreased
K++ is increased
Opioids action on the CNS is ____ and the _____
Presynaptic
Action of opioids is to inhibit neurotransmitter release
Opioid mechanism:
Act as _______ in the ____ and other tissues
Act as agonists with opioid receptors in the CNS & in other tissues
Opioid receptors are normally activated by ____
3 endogenous peptide opioid receptor ligands
Analgesia is mediated through a complex interaction of ____
Opioid receptors
Analgesia is mediated through which opioid receptors?
Morphine (Mμ) MOP receptor
Delta (ε) DOP receptor
Kappa (κ) KOP receptor
What is the fourth opioid receptor?
ROL1
Where are opioid receptor systems found at?
Supra-spinal sites (brain)
Spinal sites
Spinal cord
Peripheral sites (peripheral nerves)
Supraspinal analgesia occurs when opioids act at _____
The brain (high concentrations here)
***Limbic, hypothalamus, and thalamus
____ receptors are dominant in mediating supraspinal anesthesia & analgesia
Mμ receptors
Supra-spinal anesthesia & analgesia produces a ____
Change in response to pain
Supraspinal anesthesia develops following _____
IV administration of opioids
All opioids are additive/synergistic?
Synergistic when giving more than one
Mμ were the _____ to be identified
First
Supraspinal routes of analgesia also include:
Oral, intrathecal, transdermal, etc
Spinal anesthesia occurs when _____
Pain impulse transmission is suppressed through the substantia gelatinosa
The substantia gelatinosa is also called the
Rexed’s Lamina II
Mμ receptors are dominant in mediating _____ and _____
Spinal anesthesia & analgesia
____ receptors are principally responsible for supraspinal and spinal analgesia
Mμ receptors
Spinal anesthesia produces a _____ in _____
Decrease in pain perception
In spinal anesthesia, a pt would feel less pain because ____
Fewer action potentials are relayed in the brain (perception of pain is diminished)
Spinal analgesia results from opioids acting in the region of the brain referred to as the _____
Periventricular/periaqueductal gray
_____ results from the action of opioids in the substantia gelatinosa after epidural/intrathecal administration
Spinal analgesia
The role of opioid receptors and endorphins is to function as an _____
Endogenous pain suppression system
Opioid receptor locations are in areas of the brain/spinal cord involved with:
Pain perception
Pain impulse integration (sending it back and forth)
Pain response
***Location does matter
Pain receptors are located where pain sensations ____
Occur and are modulated
We each have an endogenous pain suppression system that produces _____
Endogenous opioids
**helps us in fight/flight situations, serious injury
another example is runners high, can become addictive
The term endorphin is a combination of
Endogenous & morphine
____ are an endogenous morphine analgesic system
Endorphins
ALL endogenous opioids are derived from 3 families of pro hormones/opioid peptides:
- Pro enkephalin
- Pro dynorphine
- Pro opio melano cortin (POMC)
All pro hormones are GPCRs that share the amino terminal sequence of:
Try-Gly-Gly-Phe-(Met or Leu)
Because opioid receptors are GPCRs, they utilize a
Second messenger system
Endogenous opioid amino acid sequences differ in 3 ways:
Distribution
Receptor selectivity
Neurochemical role (how they act/what they produce)
**Important to note, that while they differ… they all share many features
Endogenous opioids from all families begin with the ____
Penta peptide sequence of leu or met – enkepehalin
*** Lu-met-tic sarah palin
The term endorhin is exclusive to peptides of the ______
Pro opio melano cortin (POMC) family
*** Endor(se)phin Kamala (melano)
Pro opio melano cortin is the common precursor of: (3)
β-endorphin (most active of endorphins)
Adreno cortico tropic hormone (ACTH)
Melanocyte-stimulating hormone (MSH)
Which endorphin is responsible for giving the most analgesia?
β-endorphin
Which endorphin is produced in the pituitary gland?
Adreno CORTIco tropic hormone – where CORTIsol ends up being released
Which endorphin is produced in the skin/pituitary gland/hypothalamus that controls skin pigmentation?
Melanocyte-stimulating hormone
The pro enkephalin family includes the penta peptide sequence of: (2)
Leu-enkephalin & Met-enkephalin
*** Lu-met-tic sarah palin
Cells that synthesize pro enkephalin are widely distributed through the _____, ______, ______, and ESPECIALLY the ________
Brain, spinal cord, peripheral sites, and ADRENAL MEDULLA
**may play a role in explaining withdrawal signs of addiction to opioids
Pro dynorphin family consists of: (3)
Dynorphin A
Dynorphin B
Neo-dynorphin
Pro-dynorphin family is widely distributed throughout the ______
Brain, spinal cord and peripheral sites
The pro-dynorphin
