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Clinical Neurosciences > Pharmacology Opiods and Anlgesics > Flashcards

Pharmacology Opiods and Anlgesics Flashcards

1
Q

What are the three ways NSAIDS are involved with reducing/treating Pain

A

reduce activation threshold at peripheral terminals of primary afferent nociceptor neurons
decrease recruitment of leukocytes
crosses the blood brain barrier to prevent generation of prostaglandins that act as a pain producing neuromodulators in the spinla cord dorsal horn

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2
Q

what are the three endogenous opiods

A

endorphin, enkephalin, and dynorphin

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3
Q

endorphins use what receptor subtype mainly

A

mu

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4
Q

enkephalins use what receptor subtype maiinly

A

delta

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5
Q

dynorphin use what receptor subtype mianly

A

kappa

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6
Q

which two receptors can undergo desentiziation

A

mu and delta

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7
Q

is the decrease in apparent effectiveness if a drug with continuous or repeated administration

A

tolerance

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8
Q

is the state of adaptation manifested by receptor specific withdrawal syndrome produced by cessation of drug exposure

A

dependence

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9
Q

the CNS effects associated with opioids are mostly associated with what receptor

A

mu

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10
Q

what are the CNS effects of opioids

A

analgesia, euphoria, sedation, respiratory depression, cough suppresion, miosis, and nausea and vomitting

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11
Q

peripheral effects of opioids

A

constipation, bradycardia, and hypotension

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12
Q

how can tolerance be minimized

A

small amounts with longer dosing intervals (drugs with LONGER t1/2)

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13
Q

examples of strong opioid agonists

A

morphine, hydropmorphone, oxymorphone, methadone, meperidine, and fetanyl

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14
Q

examples of mild to moderate opioid agonists

A

codeine, hydrocodone, oxycodone and tramadol

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15
Q

examples of mixed agonist-antagonists

A

nalbuphine, butorphanol and buprenorphine

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16
Q

examples of pure opioid antagonists

A

nalozone and naltrexone

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17
Q

2D62X2 polymophism

A

increased conversion of codeine to morphine

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18
Q

2D6 polymorphism

A

decreased conversion of codeine to morphine

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19
Q

in what type of patients should you use caution for opioids

A

liver and kidney pts

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20
Q

what is the effect of the use of a pure agonist with a partial agonist

A

it may diminish analgesia and or induce a state of withdrawal

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21
Q

if you use opioids in patients with impaired pulmonary function it may…

A

lead to acute respiratory failure (due to the effect of respiratory failure)

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22
Q

if you use opioids during pregnancy….

A

may result in fetal physical dependence, shrill crying, irritability, diarrhea, and or seizures

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23
Q

use of opioids in patients with endocrine disease

A

prolonged and exaggerated response to opioids in patients with ardrenal insufficiency or hypothryoidism

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24
Q

what has a higher bioavailability than morphine

A

methadone

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25
its isomers can block both NMDA and monoaminergic reuptake transporters
methadone
26
what is very effective for treating difficult to treat pain (neuropathic and cancer pain)
methadone
27
half live of methadone
long (25-52 hours)
28
what is widely used for treatment of opioid abuse
methadone
29
what is unique about methadone
prolonged QT syndrome
30
has signifncant antimuscarinic effects
meperidine
31
causes mydriasis and sometimes IV administration can cause increase heart rate
meperidine
32
what are the two severe reactions to meperidine
serotonin syndrome and acute narcotic overdose
33
serotonin syndrome
can block neuronal reuptake of 5HT, resulting in serotonergic overactivity
34
acute narcotic overdose
due to inhibition of hepatic CYP's by MAO inhibitors
35
meperidine is metabolized to _________- and can cause increased CNS excitability and _________
normeperidine, seizures
36
most widely used in anesthesia applications
fetanyl
37
what is the most lipid soluble of the strong mu agonists ?
fetanyl
38
what has a high abuse potential among the strong mu agonists ?
fetanyl
39
which has a rapid termination among the strong mu agonists ?
fetanyl
40
examples of mild to moderate mu agonists ?
codeine, hydrocodone, and oxycodone
41
codeine metabolism is variable and is not recommended for
cancer pain management
42
is synthetic codeine
tramadol
43
what is the mechanism of action of tramadol ?
based on MOR activity and NE and 5HT reuptake blockade
44
what are the contraindications of tramadol ?
pts. taking MAO inhibitors and SSRI's
45
what drugs are not easily reversible with mu receptor antagonists ?
mixed agonist antagonists
46
causes psychotomimetic side effects (dysphoria, racing thoughts, and distortions of body image)
butorphanol
47
analgesia through KOR is more effective in
women
48
has a long duration of action and is effective in treating for opioid abuse
buprenophrine (high dose results in mu receptor antagonist action)
49
naloxone
short duration of action, administered parenterally but the pt. must be monitored until it is certain that the offending opioid is NO longer in the system
50
naltrexone
patient must be monitored until ALL opoids have been eliminated, long half life (10 Hours), administered orally in outpatient settings and is used in maintainence programs)
51
amitriptyline and nortryptline do what
block sodium channels and decrease NE and 5HT reuptake
52
duloxetine and venlafaxine
inhibit 5HT and NE reuptake
53
gabapentin and pregabalin
inhibit voltage gated calcium channels (calcium channel ligands GABA analogs)
54
blocks sodium channels and prevents generation of action potential responsible for nerve conduction (pain)
lidocaine
55
what is the first line treatment for trigeminal neuralgia
carbamazepine
56
carbamazepine is associated with risk for what
aplastic anemia
57
used for chronic pain and postoperative pain and is a NMDA receptor antagonist
dextromethorphan and ketamine
58
dextromethorphan and ketamine produce
psychomimetic side effects
59
clonidine
acts on alpha 2 receptors in the DRG of spinal cord to produce anti-nociceptive state
60
clonidine is associated with what which limits its usefulness in pain management
postural hypotension

Clinical Neurosciences (16 decks)

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