Generals on Opiods Flashcards

1
Q

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

A

B endorphin

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2
Q

B endorphin is endogenous opoid with precursor

A

POMC

to the MD

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3
Q

B endorphin acts on which receptors

A

mu and delta

BMD) from the POMC (it’s precursor

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4
Q

B endorphins are found in:

A

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

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5
Q

Endogenous Opioid Dynorphin precursor

A

Prodynorphin.

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6
Q

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

A

Dynorphin

aDh—Dynorphin

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7
Q

Dynorphin colocalizes with :

A

ADH in magnocells

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8
Q

Dynorphin binds to

A

kappa

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9
Q

Endogenous Opioid Precursor of Enkephalin

A

Prokephalin.

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10
Q

Where is Enkephalin distributed?

A

Widely distrubuted in interneurons.

delta

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11
Q

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

A

A-Delta fibers

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12
Q

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

A

C delta fibers

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13
Q

Descending pain path Originate in _______

A

periaqueductal gray.

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14
Q

Descentind pain path Descend in

A

dorsolateral funiculus.

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15
Q

Point of descending pain path

A

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

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16
Q

General on opiod receptors

A

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

17
Q

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

A

Mu receptor

18
Q

Mr receptor has endogenous ligans

A

enkephalins, b-endorpins

19
Q

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

20
Q

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

A

Kappa Receptors

dysphoria–kappa–dynorphin

21
Q

Kappa preceptors cause:

A

dysphoria in limibc system(dynorphin–kappa–dysphoria)

22
Q

Endogenous ligands for Kappa R

A

dynorphins

23
Q

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

24
Q

Opiates

A

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