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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
Q

its isomers can block both NMDA and monoaminergic reuptake transporters

A

methadone

26
Q

what is very effective for treating difficult to treat pain (neuropathic and cancer pain)

A

methadone

27
Q

half live of methadone

A

long (25-52 hours)

28
Q

what is widely used for treatment of opioid abuse

A

methadone

29
Q

what is unique about methadone

A

prolonged QT syndrome

30
Q

has signifncant antimuscarinic effects

A

meperidine

31
Q

causes mydriasis and sometimes IV administration can cause increase heart rate

A

meperidine

32
Q

what are the two severe reactions to meperidine

A

serotonin syndrome and acute narcotic overdose

33
Q

serotonin syndrome

A

can block neuronal reuptake of 5HT, resulting in serotonergic overactivity

34
Q

acute narcotic overdose

A

due to inhibition of hepatic CYP’s by MAO inhibitors

35
Q

meperidine is metabolized to _________- and can cause increased CNS excitability and _________

A

normeperidine, seizures

36
Q

most widely used in anesthesia applications

A

fetanyl

37
Q

what is the most lipid soluble of the strong mu agonists ?

A

fetanyl

38
Q

what has a high abuse potential among the strong mu agonists ?

A

fetanyl

39
Q

which has a rapid termination among the strong mu agonists ?

A

fetanyl

40
Q

examples of mild to moderate mu agonists ?

A

codeine, hydrocodone, and oxycodone

41
Q

codeine metabolism is variable and is not recommended for

A

cancer pain management

42
Q

is synthetic codeine

A

tramadol

43
Q

what is the mechanism of action of tramadol ?

A

based on MOR activity and NE and 5HT reuptake blockade

44
Q

what are the contraindications of tramadol ?

A

pts. taking MAO inhibitors and SSRI’s

45
Q

what drugs are not easily reversible with mu receptor antagonists ?

A

mixed agonist antagonists

46
Q

causes psychotomimetic side effects (dysphoria, racing thoughts, and distortions of body image)

A

butorphanol

47
Q

analgesia through KOR is more effective in

A

women

48
Q

has a long duration of action and is effective in treating for opioid abuse

A

buprenophrine (high dose results in mu receptor antagonist action)

49
Q

naloxone

A

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
Q

naltrexone

A

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
Q

amitriptyline and nortryptline do what

A

block sodium channels and decrease NE and 5HT reuptake

52
Q

duloxetine and venlafaxine

A

inhibit 5HT and NE reuptake

53
Q

gabapentin and pregabalin

A

inhibit voltage gated calcium channels (calcium channel ligands GABA analogs)

54
Q

blocks sodium channels and prevents generation of action potential responsible for nerve conduction (pain)

A

lidocaine

55
Q

what is the first line treatment for trigeminal neuralgia

A

carbamazepine

56
Q

carbamazepine is associated with risk for what

A

aplastic anemia

57
Q

used for chronic pain and postoperative pain and is a NMDA receptor antagonist

A

dextromethorphan and ketamine

58
Q

dextromethorphan and ketamine produce

A

psychomimetic side effects

59
Q

clonidine

A

acts on alpha 2 receptors in the DRG of spinal cord to produce anti-nociceptive state

60
Q

clonidine is associated with what which limits its usefulness in pain management

A

postural hypotension

Clinical Neurosciences (16 decks)

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