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Pharm Exam 3 > 41: Opiod Analgesics > Flashcards

41: Opiod Analgesics Flashcards

1
Q

what 5 things are opiods traditionally used for?

A 
euphoria
analgesia
sedation
relief from diarrhea
cough suppression
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2
Q

opium combined with alcohol =

A

laudanum

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3
Q

the exudate from poppy seeds containing 20 biologically active components including morphine and codeine

A

opium

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4
Q

drug extracted from the exudate of the poppy

A

opiate

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5
Q

natural or synthetic drug that binds to opiod receptors producing agonist effects

A

opioid

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6
Q

term used to characterize pharmacological compounds used to treat moderate to severe pain

A

narcotic

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7
Q

natural opiods occur …

A
  • in the exudate of the opium poppy

- as endogenous endorphins, enkephalins and dynorphins

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8
Q

all non-natural opiods are derived from…

A

morphine and precursor compounds

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9
Q

located outside the spinal cord and responsible for central interpretation of pain - supraspinal analgesia

A

Mu1

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10
Q

located throughout the CNS- brainstem and spinal cord

responsible for supraspinal and spinal analgesia, respiratory depression, constipation, physical dependence, and euphoria

A

Mu2

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11
Q

three endogenous opiod receptors

A

Mu
Kappa
Delta

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12
Q

what gprtn is assocaited with opiod receptor activation

A

Gi/Go

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13
Q

upon opiod receptor activation, the Gi/Go coupling results (3)

A
  1. inhibition of adenyly cyclase
  2. reduced opening of presynaptic voltage-gated Ca2+ channels resulting in loss of intracellular calcium and decreased release of neurotransmitters
  3. increase postsynaptic opening of K+ channels (hyperpolarization and decreased firing)
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14
Q

mechanisms of analgesia on the ascending pain pathways (3)

A

1) inhibition of afferent pain transmission (blockade of pain impulses from the periphery to the brain)
2) peripheral effects (activation of opiod receptors on distal ends of afferent neurons decreases their activation and excitability)
3) dorsal horn of the spinal cord (reduction in incoming pain signaling and reduction in pain signaling up the spinal cord)

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15
Q

how do opiods work presynaptically v. postsynaptically?

A

presynaptic : opiods block release of pain-mediating Nt from afferent neurons via inhibtion of Ca channels

postsynaptic: opioids inhibit activation of afferent neurons via increased K conductance that leads to hyperpolarization

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16
Q

how do opioids work in descending pathways?

A

opiods block inhibtior GABAergic interneurons to produce disinhibiton

leads to enhanced inhibition of nociceptive processing in the spinal cord and overall pain relief

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17
Q

site of action of opioids

A

periaqueductal gray-midbrain

rostral ventral medulla - brainstem

locus coeruleus - pons in brainstem

18
Q

reduce both sensory and affective aspects of pain

A

analgesia

19
Q

what special precaution needs to be taken with use of opiods in head trauma?

A

increased pCO2 –> reflexive cerebral vasodilation

respiratory depression is a general pharmacological effect of opioids and leads to reduction in respiratory center sensitivity to pCO2 tension

20
Q

do opioids cause dilated or constricted pupils?

A

miosis - constriction of pupils

21
Q

why do opiods cause cough suppression?

A

suppress the cough center in the brain – action is predominately via the brainstem chemoreceptor trigger zone

22
Q

what is the main GI effect of opioids?

A

constipation

relieve diarrhea by decreasing gut motility and increasing the tone of intestinal smooth muscle

23
Q

how do opioids affect the uterus and urinary tract?

A

diminished force of contractions in labor

urinary retention

24
Q

what are the cardiovascular effects of opioids?

A

hypotension

bradycardia

25
Q

urticaria (hives) may be a side effect of opioid use. why?

A

histamine release – stimulates mast cell degranulation and release of histamin causing urticaria, itching, diaphoresis and vasodilation

26
Q

what is a contraindication for meperidine use?

A

MAOi drug interaction with opioids

hyperpyrexic rxn including hypertension

27
Q

dextromethorphan

A

cough suppressant

28
Q

diphenoxylate

A

antidiarrheal agent

29
Q

loperamide

A

antidiarrheal agent

30
Q

tramadol

A

mu agonist plus 5HT/Ne uptake inhibitor

31
Q

pros and cons of mixed opioid agonist-antagonists

A

mixed act differently at specific opioid receptors

pros: provide adequate analgesia with less risk of side effects and addiction
cons: enhanced psychotropic effects

32
Q

which mixed opioid agonist-antagonist is a partial activator of mu rec, blocks kappa rec.

A

buprenorphine

all the others activate kappa rec. and block or partially activate mu rec

33
Q

which receptors does morphine work on?

A

mu
kappa
delta

34
Q

latency to onset and duration of action for morphine

A

15-60;
3-6 hrs

PO administration -other routes are preferred

35
Q

7-10x more potent analgesic than morphine

A

hydromorphone

36
Q

which opioid is transdermal?

A

fentanyl

works 72 hours transdermal

more potent than morphine and hydromorphone

37
Q

what happens when a normal person takes opioid antagonists?

A

in normal individuals with no opiates present, these drugs produce no effects

38
Q

what drug would you use to reverse effects of acute opioid overdose?

A

naloxone (opioid antagonist)

IV produces a reversal of CNs and respiratory depression within 30 sec

39
Q

what drug might be used as a maintenance drug for addicts in treatment programs?

A

naltrexone (opioid antagonist)

PO administration with long duration of inhibitory action

40
Q

physiological tolerance involves changes in…

A

decrease in number and sensitivity of opioid receptors

41
Q

what is cross-tolerance?

A

tolerance to one drug produces tolerance for another drug

one who is tolerant to morphine will also be tolerant to the analgesic effect of fentanyl and other opioids

42
Q

primary pharmacologic intervention used to treat opioid addiction

A

methadone

substituted for heroin and slowly withdrawn with milder withdrawal symptoms

Pharm Exam 3 (11 decks)

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