Opioids (Exam 1 Material)

Question 1

Opioids include all drugs (natural and synthetic) with ______ like properties, including _______

Answer 1

Morphine like properties

Including endogenous peptides

Question 2

The standard of comparison for all opioid drugs is ____

Answer 2

Morphine

Question 3

Opioids include all exogenous substances that bind specifically to _______ and produce

Answer 3

Opioid receptors & produce some agonistic response

**whether it is full or partial

Question 4

In anesthesia, the standard of comparison is ____

Answer 4

Fentanyl

Question 5

Most common use for opioid is:

Answer 5

Pain relief

Question 6

Other uses for opioids include:

Answer 6

Premedication
Anesthesia supplement Primary anesthetic (not given often because so much would be needed)

Question 7

Although opioids have some sedative properties, _____ is the primary use for opioids

Answer 7

Analgesia

Question 8

Most common pre-op medication is ____

Answer 8

Morphine

Question 9

Most common post-op medications are:

Answer 9

Morphine, Hydromorphone, and Fentanyl

Question 10

Most common anesthesia opioids are:

Answer 10

Fentanyl, remifentanil, sufentanil, and alfentanil

Question 11

What is special about Sufentanil?

Answer 11

Most potent, must be given under extreme caution

Question 12

What are the most common opioids used in anesthesia? (2)

Answer 12

Fentanyl and Remifentanil

Question 13

What is special about Alfentanil?

Answer 13

It is not as reliable, not given as much

Question 14

What are the most common opioids given for chronic pain?

Answer 14

Morphine, oxycodone, and hydrocodone

Question 15

What is Meperidine (Demerol) given for?

Answer 15

Used to be given for pain (less common now), but has anti-shivering properties

Question 16

Oxycodone is most similar to what other PO med?

Answer 16

Hydrocodone

Question 17

ALL opioid receptors belong to a superfamily of __________

Answer 17

SEVEN transmembrane-segment GPCRs

Question 18

All opioid receptors are ____ and belong to the ______

Answer 18

GPCRs and belong to the Rhodopsin family of g proteins

Question 19

By nature, opioid receptors are excitatory/inhibitory?

Answer 19

Inhibitory

Question 20

Mechanism of action of the opioid receptor: (6)

Answer 20

Opioid binds to opioid receptor
GPCR is activated Adenyl cyclase is inhibited
Less cAMP is produced Ca++ is decreased
K++ is increased

Question 21

Opioids action on the CNS is ____ and the _____

Answer 21

Presynaptic
Action of opioids is to inhibit neurotransmitter release

Question 22

Opioid mechanism:

Act as _______ in the ____ and other tissues

Answer 22

Act as agonists with opioid receptors in the CNS & in other tissues

Question 23

Opioid receptors are normally activated by ____

Answer 23

3 endogenous peptide opioid receptor ligands

Question 24

Analgesia is mediated through a complex interaction of ____

Answer 24

Opioid receptors

Question 25

Analgesia is mediated through which opioid receptors?

Answer 25

Morphine (Mμ) MOP receptor Delta (ε) DOP receptor Kappa (κ) KOP receptor

Question 26

What is the fourth opioid receptor?

Answer 26

ROL1

Question 27

Where are opioid receptor systems found at?

Answer 27

Supra-spinal sites (brain) Spinal sites Spinal cord Peripheral sites (peripheral nerves)

Question 28

Supraspinal analgesia occurs when opioids act at _____

Answer 28

The brain (high concentrations here) ***Limbic, hypothalamus, and thalamus

Question 29

____ receptors are dominant in mediating supraspinal anesthesia & analgesia

Answer 29

Mμ receptors

Question 29

Supra-spinal anesthesia & analgesia produces a ____

Answer 29

Change in response to pain

Question 30

Supraspinal anesthesia develops following _____

Answer 30

IV administration of opioids

Question 31

All opioids are additive/synergistic?

Answer 31

Synergistic when giving more than one

Question 32

Mμ were the _____ to be identified

Answer 32

First

Question 33

Supraspinal routes of analgesia also include:

Answer 33

Oral, intrathecal, transdermal, etc

Question 34

Spinal anesthesia occurs when _____

Answer 34

Pain impulse transmission is suppressed through the substantia gelatinosa

Question 35

The substantia gelatinosa is also called the

Answer 35

Rexed's Lamina II

Question 36

Mμ receptors are dominant in mediating _____ and _____

Answer 36

Spinal anesthesia & analgesia

Question 37

____ receptors are principally responsible for supraspinal and spinal analgesia

Answer 37

Mμ receptors

Question 38

Spinal anesthesia produces a _____ in _____

Answer 38

Decrease in pain perception

Question 39

In spinal anesthesia, a pt would feel less pain because ____

Answer 39

Fewer action potentials are relayed in the brain (perception of pain is diminished)

Question 40

Spinal analgesia results from opioids acting in the region of the brain referred to as the _____

Answer 40

Periventricular/periaqueductal gray

Question 41

_____ results from the action of opioids in the substantia gelatinosa after epidural/intrathecal administration

Answer 41

Spinal analgesia

Question 42

The role of opioid receptors and endorphins is to function as an _____

Answer 42

Endogenous pain suppression system

Question 43

Opioid receptor locations are in areas of the brain/spinal cord involved with:

Answer 43

Pain perception Pain impulse integration (sending it back and forth) Pain response ***Location does matter

Question 44

Pain receptors are located where pain sensations ____

Answer 44

Occur and are modulated

Question 45

We each have an endogenous pain suppression system that produces _____

Answer 45

Endogenous opioids **helps us in fight/flight situations, serious injury another example is runners high, can become addictive

Question 46

The term endorphin is a combination of

Answer 46

Endogenous & morphine

Question 47

____ are an endogenous morphine analgesic system

Answer 47

Endorphins

Question 48

ALL endogenous opioids are derived from 3 families of pro hormones/opioid peptides:

Answer 48

1. Pro enkephalin 2. Pro dynorphine 3. Pro opio melano cortin (POMC)

Question 49

All pro hormones are GPCRs that share the amino terminal sequence of:

Answer 49

Try-Gly-Gly-Phe-(Met or Leu)

Question 50

Because opioid receptors are GPCRs, they utilize a

Answer 50

Second messenger system

Question 51

Endogenous opioid amino acid sequences differ in 3 ways:

Answer 51

Distribution Receptor selectivity Neurochemical role (how they act/what they produce) **Important to note, that while they differ... they all share many features

Question 52

Endogenous opioids from all families begin with the ____

Answer 52

Penta peptide sequence of leu or met -- enkepehalin *** Lu-met-tic sarah palin

Question 53

The term endorhin is exclusive to peptides of the ______

Answer 53

Pro opio melano cortin (POMC) family *** Endor(se)phin Kamala (melano)

Question 54

Pro opio melano cortin is the common precursor of: (3)

Answer 54

β-endorphin (most active of endorphins) Adreno cortico tropic hormone (ACTH) Melanocyte-stimulating hormone (MSH)

Question 55

Which endorphin is responsible for giving the most analgesia?

Answer 55

β-endorphin

Question 56

Which endorphin is produced in the pituitary gland?

Answer 56

Adreno CORTIco tropic hormone -- where CORTIsol ends up being released

Question 57

Which endorphin is produced in the skin/pituitary gland/hypothalamus that controls skin pigmentation?

Answer 57

Melanocyte-stimulating hormone

Question 58

The pro enkephalin family includes the penta peptide sequence of: (2)

Answer 58

Leu-enkephalin & Met-enkephalin *** Lu-met-tic sarah palin

Question 59

Cells that synthesize pro enkephalin are widely distributed through the _____, ______, ______, and ESPECIALLY the ________

Answer 59

Brain, spinal cord, peripheral sites, and ADRENAL MEDULLA **may play a role in explaining withdrawal signs of addiction to opioids

Question 60

Pro dynorphin family consists of: (3)

Answer 60

Dynorphin A Dynorphin B Neo-dynorphin

Question 61

Pro-dynorphin family is widely distributed throughout the ______

Answer 61

Brain, spinal cord and peripheral sites

Question 62

The pro-dynorphin