opioids Flashcards

1
Q

analgesics

A

drugs that relieve pain WITHOUT loss of conciousness

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2
Q

opioid

A

a drug that has actions similar to morphine

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3
Q

endogenous opioid peptides

A

have opioid- like properties

found in cns and peripheral tissue

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4
Q

3 main receptors

A

mu

kappa

delta

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5
Q

most important opioid receptor to opioids.

A

MU

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6
Q

Mu receptor response to activation

A

Analgesia
Euphoria
Respiratory Depression\
related to physical dependence

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7
Q

Kappa receptors response to activation

A

analgesia and sedation

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8
Q

three groups of opioids

A

1) pure opiod agonists

2) agonist-antagonist opiods

3) pure opiod antagonists

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9
Q

pure opioid agonists

A

produce similar response to endogenous opioids
- analgesic euphoria
- sedation
-physical dependence
- respiratory depression

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10
Q

2 groups of pure opioid agonists

A

1) strong opioid agonist (morphine)

2) moderate to strong opioid agonists

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10
Q
A
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11
Q

agonist-antagonists opioids

A

administered alone = low level analgesia

administered with pure agonist = blocks pure agonists
- decrease analgesia

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12
Q

pure opioid antagonists

A

acts as antagonists on mu and kappa receptors
- stops receptor from activating a response

REVERSAL of resp. and CNS depression caused by opioid agonist overdose

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13
Q

common opioid antagonists

A

NALOXONE

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14
Q

Pure agonists

A

Morphine

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15
Q

morphine pharmalogic effects

A

analgesia
sedation
euphoria
resp depression
cough suppression

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16
Q

morphine source

A

poppy plant

extract from opium

contains codeine (analgesic)
and papaverine (smooth muscle relaxant)

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17
Q

Pharmacological Actions

A

analgesic

sense of well-being

reduces anxiety

mental clouding

  • respiratory depression, urinary retention
  • prolongued use = physical tolerance and physical dependence
18
Q

Morphine Therapeutic Uses

A

relief of moderate to serve pain without unconsciousness

19
Q

Mechanism of Analgesic action

A

mimics endogenous opiods at mu

20
Q

morphine adverse effects

A

Resp depression: ++ cause of overdose death
may last 4-5 hrs
Chronic use = resp tolerance occurs

Constipation- by activating me receptors in gut

Orthostatic hypotension
- blunts barocrecptor reflex and dilate arterioles and veins

Urinary retention
- increase tone sphincter and detrusor muscle

Cough Supression
- -acts on opioid receptors in medulla

21
Q

When should morphone not be used?

A

if resp rate is less than 12 breaths per minute

22
Q

How do you reverse morphine overdose

A

Naloxone

23
Q

Morphine pharmocokinetics

A

poor lipid solubility

cant cross BBB easily
- only a fraction reaches analgesic recptors

PO= ++ inactivated First Pass

Tolerance= analgesia, euphoria, sedation, resp depression

24
Q

Physical dependence of morphine

A

abstinence syndrome occurs when drug stopped

due to cellular changes
- once changes occur, body needs constant opioids to function normally

25
Q

How long do opioid withdrawals last?

management?

A

Exterme but not LETHAL
- begins 5 hours after final dose/ lasts 7-10 days

withdrawal gradually
- progressively smaller doses over 3 days

26
Q

Morphine Toxicity

A

classic triad

-coma
- resp. depression
- pinpoint pupils

27
Q

treatment for opioid toxicity

A

ventilatory support

opioid antagonist

28
Q

fentanyl

A

transdermal
- drug placed on skin and is absorbed into blood stream

trans mucosal: intranasal, buccal, rectal, sublingual

bucal: between gums and cheek

29
Q

Methadone

A

used to treat opioid addiction

30
Q

methadone adverse effects

A

prolongs QT interval= potentially fatal dysthmia’s

31
Q

strong opioid agonists

A

morphine (prototype)

fentanyl

methadone (treats opioid addiction)

32
Q

moderate to strong opioid agonists

A

less anglgesia, resp depression, lower potential for abuse

Codeine

33
Q

Codeine

A

For mild- moderate pain
10% converted to morphine in liver
cough suppressant

34
Q

Pure antagonist function and therapeutic uses

A

Block effects of opioid agonists

treat opioid OVERDOSES

relief opioid induced CONSTIPATION

Reversal POSTOPERATIVE opioid effects

Mgmt opioid ADDICTION

35
Q

Naloxone mechanism

A

reverses effects of opioid agonists

36
Q

how is Naloxone administered and elimiated?

A

IV
IM
Intranasally
SubQ

Elimination: liver

37
Q

Naloxone therapeutic uses

A

reversal of opioid overdose
initiate with a series of small doses until crisis has passed

reversal neonatal resp depression during birth

38
Q

Opioid antagonist

A

Narcan

Methylnaltrexone Naloxegol Naldemedine

Naltrexone

39
Q

Methylnaltrexone Naloxegol Naldemidine

A

selective mu receptor antagonists

opiod-induced constaptation relief–> try other measures first

work in periphery
- Do not block CNS

40
Q

Naltrexone

A

PO, IM

opioid abuse- prevent euphoria
alcohol abuse- prevent buzz

41
Q

Non- Opioid centrally acting analgesics

A

Tramadol

42
Q

Tramadol

A

moderately stong analgesic

low potential for dependence/ resp depression

43
Q

tramadol mechanism of action

A

weak action of mu receptors

  • works primarily by blockinh uptake of norepinephrine and serotonin
    –> inhibitory effects on pain transmission in spinal cord

less effective than morphine
more effective than codeine