Generals on Opiods Flashcards Preview

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Flashcards in Generals on Opiods Deck (37)
1

Endogenous Opioid. Precursor: POMC (as is ACTH). Found in hypothalamus, nucleus tractus solitarius, and ant. pituitary. (Runner's high).
Acuts on mu, delta

B endorphin

2

B endorphin is endogenous opoid with precursor

POMC
(to the MD)

3

B endorphin acts on which receptors

mu and delta
(BMD) from the POMC (it's precursor)

4

B endorphins are found in:

Found in hypothalamus, nucleus tractus solitarius, and ant. pituitary

5

Endogenous Opioid Dynorphin precursor

Prodynorphin.

6

Co-localizes with ADH in magnocellular cells of hypothalamus and post. pituitary.

Dynorphin
(aDh---Dynorphin)

7

Dynorphin colocalizes with :

ADH in magnocells

8

Dynorphin binds to

kappa

9

Endogenous Opioid Precursor of Enkephalin

Prokephalin.

10

Where is Enkephalin distributed?

Widely distrubuted in interneurons.
delta

11

Somatic pain. Sharp, localized pain. Terminate in lamina 1 and use glutamate.

A-Delta fibers

12

Visceral or neuropathic pain. Dull, diffuse, aching or burning pain. Terminate in lamina 2 and use glutamate AND substance P.

C delta fibers

13

Descending pain path Originate in _______

periaqueductal gray.

14

Descentind pain path Descend in

dorsolateral funiculus.

15

Point of descending pain path

Release NE, 5-HT, and Enkephalin to inhibit the ascending pathways

16

General on opiod receptors

All G-protein coupled -> Gi -> inhibit adenylate cyclase -> decrease cAMP. Inhibit neurotransmitter release

17

Pleasure in limbic.
Endogenous ligands: enkephalins, B-endorphins.
Drugs: morphine, fentanyl, methadone, meperidine, buprehorphine, others

Mu receptor

18

Mr receptor has endogenous ligans

enkephalins, b-endorpins

19

Pleasure in limbic.
Endogenous ligands: enkephalins, B-endorphins.
NO drugs.

Delta R

20

Dysphoria in limbic. Endogenous ligands: dynorphins. Drugs: butorphanol, pentazocine, nalbuphine

Kappa Receptors
(dysphoria--kappa--dynorphin)

21

Kappa preceptors cause:

dysphoria in limibc system(dynorphin--kappa--dysphoria)

22

Endogenous ligands for Kappa R

dynorphins

23

Drugs that produce a stuporous sleeplike stage and may or may not be analgesic

Narcotics

24

Opiates

Drugs that are derived from opium or have a morphinelike pharmacological profile

25

Refers to all opiates, agonist-antagonist, and endogenous peptides. Cause: analgesia, constipation, euphoria, sedation, resp. depression.

Opiods

26

Physical dependence is strong on opioids. Thus, ONLY type of chronic pain treated w/ opioids is cancer.

Opiod physical dependence

27

Duration of action related to both l

lipophilicity and elimination rate

28

Effect of opioids:
Antidiarrheal effect and constipation
a. Effects are both
b. Delay in gastric emptying, spasmodic increases in intestinal tone and decrease in propulsive movements.
c.____receptors on GI nerves.

central and peripheral
μ-

29

Opiods cause both: Euphoria – Rush and high and -___

sedation

30

Most serious side effect of opioid analgesics.

Respiratory depression

31

Mech of respiratory depression in opiod:

Decrease in the sensitivity of chemoreceptors in the brainstem to carbon dioxide.

32

What other drugs do we need to be aware of when using opiods as far as respiratory depression is concerened?

Effect is at least additive with other CNS- depressing drugs.

33

Opioids cause Nausea
- stimulation of chemoreceptor trigger zone in

area postrema

34

Endocrine effects
decrease in

a. Decreased release of LH - μ receptor.

35

______secretion is increased by μ stimulation and decreased by Kappa stimulation.

ADH

36

Some drugs, such as morphine and naloxone undergo

extensive first-pass metabolism.

37

onset of action is related to

lipophlilicty