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Pharm Exam 3 > Opiate Analgesics > Flashcards

Opiate Analgesics Flashcards

1
Q

General therapeutic strategies for chronic pain:

A

1) relief of pain

2) Delay or arrest of disease process

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2
Q

What is prototype opioid drug?

A

morphine

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3
Q

What level of pain are opioids used to treat?

A

moderate to severe pain

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4
Q

Opioids historically used for:

A 
euphoria
analgesia
sedation
relief from diarrhea
cough suppresion
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5
Q

opium definition -

A
  • greek for “juice”

- the exudate from poppy seeds containing 20 bilogically acting components including morphine and codeine

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6
Q

Opiate definition -

A

drug extracted from the exudate of the poppy

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7
Q

opioid definition:

A

natural or synthetic drug that binds to opioid receptors producing its agonist effects

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8
Q

narcotic definition:

A

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

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9
Q

Only two natural opioids that come directly from poppy?

A

morphine and codein

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10
Q

endogenous opioids?

A

endorphins
enkephalins
dynorphins

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11
Q

All other non-natural opioids are prepared from?

A
  • morphine

- other precursor compounds

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12
Q

Three endogenous opioid receptors:

A

1) Mu -two types: Mu1 & Mu2
2) Kappa (k)
a) supraspinal and spinal analgesia
b) little or no respiratory depression
c) little or no dependence
d) dysphoric and general psychomimetic effects
3) Delta-
a) modest supraspinal and spinal analgesia
b) little addictive potential
c) modulation of hormone and neurotransmitter release
d) may regulate Mu receptor activity

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13
Q

**Two types of Mu receptors and effects:

A

a) Mu1-outside spinal cord= responsible for central interpretation of pain - supraspinal analgesia
b) Mu2-located throughout CNS-brainstem and spinal cord=responsible for supraspinal and spinal analgesia, respiratory depression, constipation, physical dependence and euphoria

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14
Q

general pharmacokinetics for all opioids:

ABSORPTION

A
  • well absorption from GI tract
  • first pass effect (morphine)
  • low oral bioavailability (low oral:parenteral ratio)
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15
Q

general pharmacokinetics for all opioids:

METABOLISM

A
  • hepatic - primary process- glucuronidation
  • *-Morphine –> morphine-6-glucuronide (M6G = even more active than morphine!); M3G
  • heroin and codein both metabolized to morphine
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16
Q

general pharmacokinetics for all opioids:

LATENCY TO ONSET

A
  • transdermal >12hr
  • oral 15-30 min
  • intranasal 2-3min
  • intravenous 15-30 sec
  • pulmonary inhalation 6-12 sec
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17
Q

What is morphine 6 glucuronide?

A

metabolite of morphine = even more active than morpine

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18
Q

MOA for opioids?

A

hit Mu receptors

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19
Q

What kind of receptor is Mu?

A

Gi/Go coupled

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20
Q

MOA at the receptor level:

A

Mu receptor - Gi/Go coupled

1) inhibition of adenylyl cyclase = dec production of cAMP
2) reduced opening of presynaptic voltage gated Ca channels =in **loss of intracellular Ca and dec release of neurotransmitters
3) Inc postsynaptic opening of K channels = loss of intracellular K and neuronal hyperpolarization (less firing)

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21
Q

Mechanism of analgesia - ascending pain paths:

A

1) inh of afferent pain transmission-block pain impulse from the periphery to the brain
2) peripheral effects-activate opioid receptors on distal ends of primary afferent (sensory) neurons decreasing their activation and excitability
3) Dorsal horn of the spinal cord-
a) presynaptic=opioids block release of pain mediating neurotransmitters from primary afferent neurons via inhibition of Ca channels=reduction in incoming pain signaling
b) postsynaptic=opioids inhibit activation of 2nd afferent neurons via inc K conductance that leads to hyperpolarization
c) activate GABA (inhibitory) neurons in the spinal cord leading to reduced activation of teh secondary afferent neurons

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22
Q

**Mechanisms of analgesia- descending pain paths

A

-Opioisd block inhibitory GABAergic interneurons (disinhibition) = enhanced inhibition of nociceptive processing in the spinal cord and overall pain relief

Descending pathways regulate/lower our pain subconsciously!

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23
Q

Site of action of opioids:

A

1) periaqueductal gray area - midbrain-activates enkephalin releasing neurons that projects to the raphe nuclei in the brainstem
2) Rostral ventral medulla -brainstem-nuceus raphe magnus; serotonergic projections to the dorsal horn of the spinal cord
3) Locus ceoruleus-pons in brainstem-noradrenergic projections to the dorsal horn of the spinal cord

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24
Q

General pharmacological effects of opioids: ANALGESIA

A

**-reduce both sensory and affective aspects of pain

both spinal and supraspinal (u,k,delta) sites

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25
Q

General pharmacological effects of opioids: EUPHORIA

A
  • *-pleasant floating sensation with reduced anxiety and distress
  • more common in abuse situations
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26
Q

General pharmacological effects of opioids: SEDATION

A
  • -drowsiness and lethargy, cognitive impairment and sense of tranquility
  • more prominent effect in elderly
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27
Q

General pharmacological effects of opioids: RESPIRATORY DEPRESSION

A

-**inh of brainstem respiratory mechanism (less sensitivity to pCO2 tension

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28
Q

General pharmacological effects of opioids: MIOSIS

A

*-constriction of pupis (pin point pupils)

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29
Q

Do not use opioids with what presenting patient condition

A

head trauma-bc inc cerebral vasodilation due to increased pCO2 since body is not sensitive to pCO2 tension anymore with drug

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30
Q

General pharmacological effects of opioids: COUGH SUPPRESSION:

A
  • suppression of cough center

* -action is predominantly via the brainstem chemoreceptor trigger zone

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31
Q

Other pharmacological effects of opioids: EMESIS:

A
  • nausea and vomiting
  • **-directly stimulate chemoreceptor trigger zone in brainstem
  • effect reduced with continued use
32
Q

Other pharmacological effects of opioids: GI:

A
  • ***CONSTIPATION
  • increased tone and decreased motility
  • *Relieve diarrhea by decreasing gut motility and increasing the tone of intestinal smooth muscle
33
Q

Other pharmacological effects of opioids:RENAL:

A
  • inc tone of muscle in bladder and ureters
  • enhanced release of ADH
  • urinary retention
34
Q

Other pharmacological effects of opioids: UTERUS:

A

diminished force of contractions in labor

35
Q

Other pharmacological effects of opioids: CARDIOVASCULAR:

A
  • -hypotension - dec symp tone

* -bradyvcardia- decreased preload and afterload

36
Q

Other pharmacological effects of opioids: HISTAMINE RELEASE:

A

-*stimulates mast cell degranulation and release of histamine = utricaria (hives), itching, diaphoresis, and vasodilation

37
Q
  • Main therapeutic indication for opioids?
A

Analgesia! - mod to severe pain that is constant in duration

38
Q

**Therapeutic indications for opioids?

A
  • 1) analgesia (acute post surgical/trauma pain; post MI pain; severe inflammatory and neuropathic pain; cancer)
  • 2) anesthetic (pre-med/adjunct to general anasthetic)
  • 3) cough suppresant (codeine, dextromethorphan)
  • 4) diarrhea (loperamide)
  • 5) acute pulmonary edema (reduce intense panic and anxiety)
39
Q

opioids side effects/toxicities:

A
  • -sedation
  • -respiratory depression
  • -nausea and vomit
  • -beh restlessness
  • -seizures
  • -hypotension
  • -constipation
  • -increased intracranial pressure
  • -urinary retention
  • -utricaria
40
Q

usual first step to managing a side effect or toxicity for opioids?

A

switch opioids!

41
Q

*Opioids - Drug interaction:

A
  • *-CNS depressants - esp respiratory
  • *-MES liver metabolism enzymes
  • *****-MAOI - CONTRAINDICATION MOST ASSOCIATED WITH MEPERIDINE - USE CAUTION! hyperpyrexic (inc in body temperature) reaction including hypertension
  • *-mixed agonist-antagonist
  • *-antagonist
42
Q

**Which opioid should never be used with MAOIs?

A

**meperidine!

43
Q

strong agonist for severe pain opioids - list drugs?

A
  • morphine
  • hydromorphone
  • oxymorphone
  • methadone
  • meperidine
  • fentanyl
  • levorphanol
  • sufentanil
  • heroin
44
Q

moderate agonist for moderate pain opioids?

A
  • codeine
  • hydrocodone
  • oxycodone
  • propoxyphene
  • tramadol
45
Q

Mixed Agonist/Antagonists for moderate pain opioids?

A
  • buprenorphine
  • butorphanol
  • balbuphine
  • pentazocine
  • nalbuphine
46
Q

Opioid antagonist drugs?

A
  • naloxone
  • naltrexone
  • nalmefene
47
Q

morphine -

  • belongs to which category of opioids?
  • hits what receptor
A
  • strong opioid agonsit

- prototype stong Mu agonist

48
Q

fentanyl -

  • belongs to which category of opioids?
  • solubility
  • hits what receptor?
A
  • strong opioid agonsit

- strong lipophilic Mu agonist

49
Q

meperidine

  • belongs to which category of opioids?
  • what is it?
A
  • strong opioid agonsit

- active metabolite of morphine

50
Q

methadone

  • belongs to which category of opioids?
  • how long do effects last?
  • what is it used for?
A
  • strong opioid agonsit
  • long duration
  • tx patients with opiate addiction
51
Q

sufentanil

  • belongs to which category of opioids?
  • solubility
  • hits what receptor?
A
  • strong opioid agonsit

- strong lipophilic Mu agonist - even more potent that fentanyl - extended action

52
Q

Codeine

  • belongs to which category of opioids?
  • how used/combo with what?
  • usually used for?
A
  • prototype moderate opioid agonist
  • used in combo with acetominophen and others
  • used as an antitussive
53
Q

oxycodone

  • belongs to which category of opioids?
  • used in what kind of cases?
A
  • moderate opioid agonist

- used for breakthrough pain such as post-surgery

54
Q

hydrocodone

  • belongs to which category of opioids?
  • how is this prepped for use?
A
  • moderate opioid agonist

- only available combined with acetaminophen, NSAIDS, etc

55
Q

Other opioid agonist: Dextromethorphan:

-used for

A

cough suppresant

56
Q

Other opioid agonist: Diphenoxylate: use for?

A

-antidiarrheal agent

57
Q

Other opioid agonist: Loperamide: used for?

A

-antidiarrheal agent

58
Q

Other opioid agonist: tramadol: receptors??

A

Mu agonist plut 5-HT/NE uptake inh

59
Q

Buprenorphine

  • which class of opioid?
  • hits which receptors?
A
  • mixed agonist-antagonist

- partial activators of Mu receptors and block kappa receptors

60
Q

butorphanol

  • which class of opioid?
  • hits which receptors?
A
  • mixed agonist-antagonist

- activate kappa receptors and block or partially activate mu receptors

61
Q

nalbuphine

  • which class of opioid?
  • hits which receptors?
A
  • mixed agonist-antagonist

- activate kappa receptors and block or partially activate mu receptors

62
Q

pentazocine

  • which class of opioid?
  • hits which receptors?
A
  • mixed agonist-antagonist

- activate kappa receptors and block or partially activate mu receptors

63
Q

which mixed agonist/antagonists activate kappa receptors and block or partially activate mu receptors

A

pentazocine
nalbuphine
butorphanol

64
Q

What are the two antitussive opioids?

A

codeine

dextromethorphan (

65
Q

What is an advantage of which mixed agonist/antagonists that activate kappa receptors and block or partially activate mu receptors?

A

provide adequate analgesia with less risk of side effects and addiction

66
Q

Cons for mixed agonist-antagonist drugs?

A

more psychotropic effects - hallucinations

67
Q

**potency of hydromorphone compared to morphine?

A

**7-10x more potent analgesic!!

68
Q
  • *fentanyl
  • what strength opioid is it?
  • special thing about this drug?
A
  • *-strong!!

* **-available as transdermal patch = Duration is 72 hours (compared to 1-2 hours duration if oral)

69
Q

Codine potency related to morphine?

-why is codeine better in some aspects?

A

-codeine is much LESS potent than morphine

  • less euphoria
  • lower abuse potential
  • rare physical dependence

BUT can produce significant sedation

70
Q

opioid antagonists are generally used for?

name the drugs?

A

opioid overdose!

  • naloxone
  • naltrexone
  • nalmefene
71
Q

**acute opioid overdose need to give what drug? Why?

A

naloxone - if given IV reverses respiratory and CNS depression within 30 seconds!!! But short duration of action (not maintenance - use naltrexone for maintenance)

72
Q

**What drug is used as maintenance drug for addicts in treatment programs? Why?

A

naltrexone - duration of action is much longer than naloxone (which is used for acute opioid overdose and duration of action is super short relatively)

73
Q

What effect of opioids is the leading cause of opiate dependence and abuse?

A

Euphoria - reward pathway (DA-pathway) - addiction

74
Q

Primary drug used to treat opioid addiction?

A

methadone - development of withdrawl symptoms are slower and not as bad with methadone but still sucks

75
Q

acute opioid drug actions:

withdrawal symptoms?

A

Withdrawl symptom just opposite of opioid effects:

  • analgesia–>pain/irritability
  • respir depression–>hyperventil
  • euphoria–>dysphoria/depression
  • relaxation/sleep–> restlessness/insomnia
  • tranquilization–>fear/hostiity
  • dec BP–>inc BP
  • constipation–>diarrhea
  • pulillary constriction–>dilation
  • hypothermia–>hyperthermia
  • dry of secretion–>lacrimation,runnynose
  • reduced sex drive–>spontaneous ejaculation
  • flushed/warm skin–> chills/gooseflesh

Pharm Exam 3 (11 decks)

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