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Phar300 > lect 13 opioid analgesics > Flashcards

lect 13 opioid analgesics Flashcards

1
Q

major use of opioids

A

handle extreme pain

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2
Q

two major locations involved in pain sensation

A

peripheral nervous system and central nervous system

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3
Q

what drugs act mainly on peripheral nervous system

A

NSAIDS

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4
Q

peripheral nervous system trajectory of pain

A
  1. nociceptors pick up pain impulse
  2. impulse travels to spinal cord where we have basic relay
  3. second relay from spinal cord to thalamus through spinothalamic tract
  4. final relay from thalamus to cortex
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5
Q

major system site of action for opioids

A

central nervous system

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6
Q

pain transmission pathway of CNS (ascending)

A

first relay in spinal cord, then thalamus, and then cortex

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7
Q

pain supression pathway in CNS descending

A

pain inhibitory tract in dorsolateral funiculus caused by endogenous opioids or ingested opioids

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8
Q

true or false? theres a vast distribution of opioid synthesizing neurons and opioid receptors throughout the brain and spinal cord

A

True

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9
Q

names of endogenous opioids (3)

A

beta-endorphins, enkephalins, dynorphins

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10
Q

types of opioid receptors (3)

A

Mu, Delta, Kappa

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11
Q

main sites for opioid analgesics

A

spinal cord and brain

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12
Q

what are opiates

A

alkaloids found in opium poppy

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13
Q

what are opioids

A

compounds with opiate-like actions ex synthetic, endogenous opioids

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14
Q

two Types of opioids

A

naturally occuring and synthetic

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15
Q

naturally occuring opioids and percentages in opium

A

morphine (10% opium by weight) and codeine (methylmorphine, 0.5% of opium)

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16
Q

derivative of morphine for anticough in 1898

A

heroin

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17
Q

hypodermic syringe 1860s

A

injection of heroin into veins as cough supressant

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18
Q

most prevalent opioid receptor in CNS

A

Mu receptor

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19
Q

true or false? different opioids have different potencies to relieve pain

A

True

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20
Q

Synthetic opioids and use

A

drugs with morphine like action. Altered basic structure. Synthesized in a way to relieve pain but not be addictive. Most sythetic opioids are addictive though

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21
Q

synthetic opioid that is an opioid antagonist that can save an overdose

A

Naltrexone

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22
Q

synthetic opioid that is a weak agonist that can save help people quit (2)

A

methadone, buprenorphine

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23
Q

both agonist and antagonist of opioid. explanation?

A

Pentazocine. can activate receptor a bit, but also blocks access of other more powerful drugs to receptor

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24
Q

2 kinds of opioid analgesia mechanism for pain

A
  1. Decrease pain signal

2. increase descending inhibition

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25
Q

decrease pain signal of opioid analgesia mechanism

A

afferent transmission is at presynaptic and postsynaptic sites. opioids act on opioid recetors both at presyn. and post synapt.

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26
Q

presynaptic decrease pain signal for opioid analgesia

A

block of Ca channels so decreased calcium influx presynapt. Decreased transmitter release

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27
Q

postsynaptic decrease pain signal for opioid analgesia

A

increase K channel opening so hyperpolarizes postsynaptic membrane. cell less likely to fire.

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28
Q

increase inhibition of opioid analgesia mechanism

A

block gaba release onto noradrenergic and serotonergic neurons. These neurons can now release tranmitters that will block Ca channel and decrease transmitter release

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29
Q

primary afferent system ascending and releasing glutamate combined with descending inhibition by 5-ht and NA release increases what as a combine result

A

increased pain threshold

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30
Q

opioids decreases what in people when it comes to pain (2)

A

physical sensation of pain and stressful emotions related to pain

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31
Q

high prevalence of mu receptors where? (3)

A

limbic system, spinal cord, brain stem

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32
Q

what type of receptor is opioid receptors and describe activation

A

GCPR, activation of it starts a signaling cascade. Alpha subunit activates adenylyl cyclase, beta and gamma subunit acts on Ca and K channels

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33
Q

mu delta and kappa receptors can all decrease what

A

calcium conductance so decreased transmitter release presynaptically

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34
Q

opioid receptor good at increase K conductance in postsynaptic to get IPSP

A

mu receptor

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35
Q

receptor plasticity

A

receptors are constantly recycled. after bound to agonist and GCPR activation, receptor is endocytosed after being phosphylated and binding to beta arrestin

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36
Q

changes to tolerance of opioids

A

receptors decrease, rapid desensitization because more phosphorylation and more rapid endocytosis

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37
Q

chronic tolerance effect on number of receptors synthesized and put into plasma membrane

A

increased insertion of receptors on PM but also increased degradation of receptors such that overall numbers are decreased

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38
Q

what area affected by opiates controls automatic body functions and depress breathing but symptoms cannot be separated from pain relief

A

brain stem

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39
Q

area affected by opiates that controls emotions to increase feelings of pleasure

A

limbic system

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40
Q

psychomimetic and aversive in human. not self administrated

A

K compounds

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41
Q

traditional functional model of GPCR widely applied to gpcr drug discovery

A

GPCR monomers

42
Q

physiological effects of exogenous opioids (7)

A

analagesia, gastrointestinal (constipation), cough suppression, euphoria, respiratory depression, miosis, seizures

43
Q

receptors involved in analgesia

A

mu delta and kappa

44
Q

receptors involved in GI, sedation

A

mu and kappa

45
Q

receptors involved in depressed respiration

A

mu

46
Q

tolerance where different targets of opioid drugs do not develop tolerance at the same speed and to the same degree. receptors respond differently with chronic use

A

differential tolerance

47
Q

absorption of morphine

A

oral, rectal, injection.

GI absorption slow and incomplete. intramuscular injection most common.

48
Q

way of administrating morphine that gets big peak in blood but falls rapidly due to redistribution. more dangerous

A

intravenous injection

49
Q

lower peak level administration of morphine but lower decline and stays in therapeutic window

A

Intramuscular injection

50
Q

oral absorption of morphine

A

absorbed in intestine and then liver. first pass effect then brain and spinal cord

51
Q

distribution of morphine

A

only 20% crosses blood brain barrier

52
Q

metabolism of morphine

A

in liver. half life of 2-4 hours.
some metabolites are highly active. different metabolites for oral and parental. once conjugated, metabolites are water soluble

53
Q

excretion of morphine

A

metabolites in urine.

54
Q

parental metabolites of morphine

A

3-glucuronide (60%) and 6-glucuronide (40%)

55
Q

non active parental metabolite of morphine

A

3-glucuronide (60%)

4 hours half life

56
Q

active parenteral metabolite of morphine

and renal failure

A

6-glucuronide (40%)
3 hours half life

renal failure>50% takes a long time to clear so dangerous

57
Q

oral metabolite that can have negative psychoactive effects and can be neurotoxic

A

Normorphine

58
Q

the two layers of neurons of intestines

A

myenteric plexus and submucosal plexus

59
Q

Impairing motility of Gi tract by morphine

A

morphine relieves diarrhea and increases constipation

60
Q

Opioid-induced constipation mechanism

A

morphine binds to opioid receptors in myenteric plexus. high circular contraction so things stay in intestine longer, more fluid absorption, decreased perilstasis, increased rectal sphincter tone, decreased colonic mucosal secretion, decreased sensitivity to rectal distension

61
Q

morphine nausea effects (2)

A
  1. stimulates chemoreceptor trigger zone

2. motion (keep person horizontally)

62
Q

main respiratory action of morphine

A

morphine depresses respiratory center sensitivity too CO2

63
Q

miosis effect of morphine

A

depress tonic inhibition, release ability to constrict pupil all the time

64
Q

no tolerance of morphine to what side effects

A

miosis and constipation

65
Q

decreased urine effect of morphine

and effects

A

decreases by enhancing anti-diuretic hormone ADH

spasm, pain, rentention

66
Q

what is combined with codeine for greater effects

synergestic

A

NSAIDS

67
Q

codeine is metabolized to morphine in BBB by which enzyme

A

CYP2D6

68
Q

percentage of poor metabolizers to CYP2D6 so not responsive to codeine

A

5-10%

69
Q

percentage of people with high levels of CYP2D6 so high response to codeine

A

5-10%

70
Q

what enzyme is highly polymorphic

A

CYP2D6

71
Q

anti breast cancer drug whos metabolite is created by CYP2D6

A

Tamoxifen

72
Q

other opioid agonists (4)

A

meredipine (full agonist), fentanyl (very powerful opioid), hydromorphone (Dilaudid) (mu agonist, absorbed orally, used for chronic severe pain)
oxycodone

73
Q

partial agonists of opioids

A

buprenorphine, methadone

74
Q

meperidine absorption

its metabolite and effect on CNS

A 
taken orally and better absorbed orally than morphine, longer half life
metabolite is normedipine
CNS excitation (balances some of the depression, so less depression)
75
Q

dose response curve of meredipine vs morphine

A

curve on right side from morphine, equally effective but longer time for meredipine so have to take several time

76
Q

fentanyl absorption and methods of taken it

A

very fast action, highly lipid soluble so given in skin patches for slow absorption, longer duration.
given as lollipops for children.
gets to the blood stream fast, so fast action

77
Q

oral mucosa physiology benefits for drugs given orally (5) oral transmucosal technology

A
  1. large surface area
  2. uniform temperature
  3. high permeability
  4. well-vascularized
  5. no first pass effect
78
Q

opioid with minimal penetration of BBB. used to treat diarrhea. cannot get to CNS so no analgesia

A

loperamide (trade name: Imodium)

79
Q

treat withdrawal of opioids using what

A

weak partial agonists

80
Q

methadone absorption
and benefits
and ex of what happens if we use it with heroin

A

oral, long half life
block withdrawal in opioid addict
stabilize maintenance therapy
if use heroin and then take methadone, it wont give a high

81
Q

naloxone mechanism and metabolism for overdose and what kind of overdose

A

bind to mu receptor. is injected and half life is short (minutes) (injected several time if not able to get to hospital). Metabolizes quickly

for acute overdose

82
Q

naltrexone mechanism for overdose and used for what

A

oral, half life a day. not for acute overdose

used by addicts to prevent drug effects, so cant get the high

83
Q

mechanism of pentazocine for overdose and difference in dose repsonse curve then meredipine

A

lowers abuse potential. Less pain relief.

Curve is lower than meredipine curve

84
Q

opioid importance in three types of pain when clinically used as analgesic

A

nociceptive, neuropathic and psychogenic

85
Q

in what case we do not care of addictive potential for opioids

A

in cancer patients we just want pain relief

86
Q

addiction in america of which opioids and effects on babies

A

oxycodone, fentanyl, babies exposed to opioids in utero can have withdrawal effects

87
Q

classical drugs of abuse prefer what receptor

A

mu sites

88
Q

prototype drugs

A

morphine and heroin

89
Q

other name for heroin

A

diacetylmorphine

90
Q

which is more potent between morphine and heroin

A

heroin is 10 times more potent

91
Q

BBB in heroin

A

crosses BBB faster than morphine and converted to morphine

92
Q

effects of heroin when smoking it and acute effects

how long it lasts

A

state of stupor (smoking it absorbs and easy state of sleepiness).
acute effects: euphoria–> rush followed by high; tranquility and sleepiness-“nod”
lasts about 3 to 5 hours

93
Q

permanent miosis is seen in who

A

chronic addicts

94
Q

drugs cause for biggest deaths of opioids

A

Fentanyl, Carfentanil

95
Q

large animal tranquilizer causing 72% of overdose

A

Carfentanil

96
Q

morphine, fentanyl, heroin and carfentanil from lowest to highest potency

A

morphine

97
Q

opioids better for oral administration because people prefer this route (3)

A

meperidine, methadone, codeine

98
Q

ability to treat diarrhea with opioids is proportional to what

A

to the ability of the drug to bind to the receptors

99
Q

opiate receptors are in which pathway

A

reward pathway

100
Q

deaths of opioid overdose is mostly in what category of age

A

people in their 20s

Phar300 (18 decks)

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