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Pharm > Opioid analgesics > Flashcards

Opioid analgesics Flashcards

1
Q

What drugs can be used in pain treatment? (3)

A

I. Opioid analgesics
II. Analgesics and NSAIDs
III. Specific analgesics (adjuvants)

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2
Q

Mechanism of action for opiod analgesics, opioids or narcotics?

A

-specific CNS receptors (opiates or opioids receptors changing perception of pain)

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3
Q

What is the effect of opiod analgesics, opioids or narcotics? (6)

A
  • produce analgesia (Strong)
  • sedation
  • somnolence (sleepyness)
  • tolerance
  • addiction
  • abstinence
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4
Q

What is somnolence?

A

sleepyness

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5
Q

Mechanism of action for non-opioid analgesics (NSAIDS + Analgesics)? (2)

A
  • Cox inhibitors

- inhibit prostaglandin synthesis (vasodialator

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6
Q

What is protaglandin? (2)

A

a vasodilator.

Needs the COX enzyme

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7
Q

What is the effect of non-opioid analgesics (NSAIDS + Analgesics)?

A
  • analgesia (moderate)
  • antipyretic
  • nonaddictive

SOME:

  • anti-inflammatory
  • antiplatlet
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8
Q

What are the adjuvant analgesic drug types? (3)

A
  • anti-epileptic
  • anti-depressants
  • neuroleptics
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9
Q

What do you prescribe in the first step of pain management? (3)

A
  • Mild to moderate pain
  • NSAIDs (ibuprofen…)
  • paracetamol
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10
Q

What do you prescribe in the 2nd step of pain management? (3)

A
  • Moderate to intense pain

- NSAIDs + Weak opioids (tramadol, codeine)

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11
Q

What do you prescribe in the 3rd step of pain management? (2)

A
  • Intense pain uncontrolled with previous drugs

- Strong opioid (morphine)

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12
Q

What do you prescribe in the 4th step of pain management? (3)

A

-Very intense pain

Invasive analgesic actions:

  • intrathecal or epidural morphine
  • infiltrations of local anesthetics
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13
Q

In which step of pain management do you add adjuvant drugs?

A

-can be added in all steps depending on the pain

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14
Q

What kind of pain do opioid analgesics treat? (2)

A
  • moderate to severe

- acute or chronic

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15
Q

What kind of analgesic effect do opioid analgesics have?

A

intense

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16
Q

Opioid analgesics have an affinity for ______ receptors

A

opioid

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17
Q

NSAID indications? (3)

A
  • headache
  • arthralgia (joint pain)
  • myalgia (muscle pain)
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18
Q

What is arthralgia?

A

joint pain

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19
Q

What is myalgia?

A

pain in a muscle or muscle group

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20
Q

Opioid indications?

A
  • visceral pain

- intense pain

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21
Q

NSAID pain effectiveness?

A

moderate

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22
Q

opioids pain effectiveness?

A

intense

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23
Q

NSAID analgesic location?

A

peripheral

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24
Q

Opioid analgesic location?

A

central

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25
Q

Opioids are also called…. (2)

A

opiates & narcotics

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26
Q

Opioids come from…

A

Juice of the poppy (Papaver somniferum)

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27
Q

The poppy’s latin name is

A

Papaver somniferum

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28
Q

The most significant natural alkaloid obtained from opium is

A

morphine

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29
Q

Which drug is used as a reference or standard to compare with the rest of the opioids?

A

morphine

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30
Q

First preparation that demonstrated analgesic, sedative and euphoric properties was?

A
  • Juice of the poppy (Papaver somniferum)

- 1st “opioid”

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31
Q

Opiate vs opioid?

A
  • Opiate: products obtained from poppy juice and derivatives
  • Opioid: any substance endogenous or exogenous with affinity for the
    specific receptors.
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32
Q

What are the opioid receptors? (4)

A
  • μ
  • δ
  • κ
  • ORL-1
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33
Q

What is the mechanism of action for opioid receptors?

A
  • affinity to opioid receptors
  • DECREASE painful sensation
  • DECREASE affective component of pain
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34
Q

What endogenous substances stimulate opioid receptors?

A
  • beta-endorphins

- enkephalins

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35
Q

Location of opioid receptors? (5)

A
  • C.N.S. : medulla, midbrain, thalamus, cortex

- PERIPHERAL N.S.

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36
Q

How do opioid analgesics work?

A
  • act on receptors mu (μ),
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37
Q

What is the action of the mu (μ) receptors

A
  • analgesic effect

- respiratory depression

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38
Q

What are the different types of opioids?

A
  • major opioids
  • minor opiates
  • partial agonists
  • agonist-antagonists
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39
Q

What are the major opioids? (4)

A
  • MORPHINE
  • FENTANYL
  • PETHIDINE (meperidine)
  • METADONE
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40
Q

What are the minor opiates? (3)

A
  • CODEINE / DIDYDROCODEINE
  • TRAMADOL
  • DEXTROPOPOXYPHENE
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41
Q

What are the opioid antagonists?

A
  • Naloxone

- Naltrexone

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42
Q

What is the opioid partial agonist?

A

Buprenorphinie

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43
Q

What is the opioid agonist-antagonist?

A

Pentazocine

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44
Q

Opioid route of administration? (3)

A
  • oral
  • sublingual (buprenorphine)
  • Transdermal (buprenorphine, fentanyl)
  • Parentreral (IM, IV, SC, epidural)
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45
Q

Why are opioids used orally?

A

good absorption

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46
Q

Opioid bioavailability orally? (2)

A
  • low

- high hepatic first pass

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47
Q

Which opioids are used sublingually? why? (2)

A
  • buprenorphine

- avoids hepatic first pass

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48
Q

Which opioids are used transdermally? why? (3)

A
  • buprenorphine
  • fentanyl
  • avoids hepatic first pass
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49
Q

Describe opioid biotransformation and excretion

A
  • elevated hepatic biotransformation

- renal excretion

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50
Q

Do opioids cross placenta and BBB?

A

yes

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51
Q

Opioid half life?

A

4-6 hrs

* can have controlled release preparations

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52
Q

define stupor

A

a state of near-unconsciousness or insensibility.

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53
Q

Pharmacologic actions of morphine

A
  • Decreased level of consciousness: sedation and stupor
  • Respiratory depression (dose + route dependent)
  • hypothermia
  • miosis (pupillary constriction)
  • nausea + vomitting
  • incr. muscle tone (high doses)
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54
Q

Morphine: acute or chronic?

A

both

depends on dose

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55
Q

What are the cardiovascular effects of morphine? (3)

A
  • hypotension
  • bradycardia (slow heart action)
  • Vasodilation (decreasing vascular tone)
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56
Q

What are the GI effects of morphine? (4)

A
  • delayed gastric emptying
  • constipation
  • increased pressure in bile ducts (hypertonic sphincter of oddi)
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57
Q

What are the urinary effects of morphine?

A
  • increased bladder tone

- less urination (?)

58
Q

Morphine and tolerance? (4)

A
  • quick development of tolerance
  • duration of action shortened
  • response intensity decreases
  • dose increase required
59
Q

Morphine and dependence? (2)

A
  • withdrawl =severe central and vegetative symptoms

- mostly sympathetic

60
Q

Morphine withdrawal is mostly _______

A

sympathetic

61
Q

ANALGESIC DOSE _______ ALTER THE LEVEL OF CONCIOUSNESS

A

does not

62
Q

Morphine analgesic indications (4)

A

-reduces emotional response to pain

IV-SC for a few days:

  • surgical interventions
  • polytrauma

IV few days or SC (oral) chronic:
-tumors

63
Q

When do you use subcutaneous or oral morphine?

A

chronic treatment of tumors

64
Q

How/why do we use morphine for surgical interventions? (3)

A

analgesic

IV or SC for a few days

65
Q

How/why do we use morphine for polytrauma? (3)

A

analgesic

IV or SC for a few days

66
Q

How/why do we use morphine for tumors? (3)

A

analgesic

  • IV few days or
  • SC (oral) for chronic
67
Q

What are the morphine vasodilator indications? (2)

A
  • Acute pulmonary edema (iv-sc) (heart failure)

- Acute myocardial infarction (AMI)

68
Q

How / why do we use morphine for Acute pulmonary edema? (3)

A
  • vasodilator for heart failure

- IV or SC

69
Q

Why do we use morphine for acute myocardial infarction?

A

vasodilator

70
Q

What are the morphine sedative indications?

A

Mechanical ventilation (i.v-s.c..)

71
Q

How / why do we use morphine for Mechanical ventilation?

A
  • sedative

- IV or SC

72
Q

Describe morphine respiratory depression (3)

A
  • adverse effect
  • can be used to relief respiratory effort in terminal situations
  • maximum IV
  • minimum oral
73
Q

Morphine adverse effects (4)

A
  • dry mouth (dental caries, periodontal disease, oropharyngeal candidiasis)
  • allergic skin reactions (rare)
  • tolerance to more depressant actions
  • acute poisoning (coma respiratory depression, pinpoint pupils)
74
Q

How does morphine act on the bronchus?

A

bronchoconstriction

75
Q

Antidote for acute morphine poisoning?

A

naloxone

76
Q

Morphine contraindications (8)

A

-respiratory failure
-billiary pancreatic colic pain (ONLY use
meperdine - anticholinergic effect)
-liver failure
-inferior myocardial infarction (incr. vagal tone, better meperidine)
-childbirth (risk of fetal respiratory depression)
-pregnancy (fetal abstinence syndrome)
-breastfeeding
-elderly

77
Q

What drug is the exception for opioid contradiction for Biliary pancreatic colic pain

A

MEPERIDINE = PETHIDINE

78
Q

What is the sphincter of Oddi?

A

-controls flow of bile and pancreatic juice into the second part of duodenum

79
Q

Morphine has drug interactions with… (6)

A
  • CNS depressants (incr.)
  • Diuretics (decr.)
  • Tricyclic antidepressants (incr. analgesic)
  • CA-antagonists (incr. analgesic)
  • rifampicin (incr. metabolism)
  • delayed absorption of other drugs
80
Q

Morphine interaction with CNS depressants causes….? Which drugs? (5)

A
  • (opiates) increased effect
  • neuroleptics
  • antidepressants
  • benzodiazepines
  • ethanol
81
Q

Morphine interaction with diuretics causes….?

A

a decreased effect

82
Q

Morphine interaction with tricyclic anti-depressants causes….?

A

increase in the analgesic activity

83
Q

Morphine interaction with CA-antagonists causes….?

A

increase in the analgesic activity

84
Q

Morphine interaction with rifampicin causes….?

A

increased metabolism of morphine

85
Q

Morphine interaction with other drugs causes…?

A

delayed absorption of the other drugs

86
Q

opioid analgesics ______ the cough reflex (2)

A

decrease

ex. codiene

87
Q

opioid analgesics ______ secretions. which ones?

A

decrease

  • intestinal
  • biliary
  • saliva
88
Q

Can opioid analgesics be used pulmonary edema? (4)

A
  • yes
  • reduces preload and afterload
  • relieves pulmonary and cardiac congestion
89
Q

Can opioids be used for narcosis hypnosis and coma?

A

yes

90
Q

Codiene/dihydrocodeine is a _____ derivative

A

morphine

91
Q

Codiene/dihydrocodeine has ____ affinity for _____ receptor

A

less affinity

μ receptors.

92
Q

Codiene/dihydrocodeine effects? (3)

A
  • Antitussive: central action
  • Analgesic: association with acetaminophen or ASA
  • Antidiarrheal: constipation
93
Q

Codiene/dihydrocodeine has analgesic associations with …? (2)

A
  • acetaminophen

- aspirin

94
Q

What has a higher risk of addiction? morphine or codeine?

A

morphine

95
Q

What has a higher risk of respiratory depression? morphine or codeine?

A

morphine

96
Q

DEXTROPROPOXYPHEN is a ______ opioid

A

minor

97
Q

DEXTROPROPOXYPHEN has analgesic efficacy similar to ______

A

codiene

98
Q

Which is better, dextropropoxyphen or codiene?

A

both have same advantages

99
Q

When do we use tramadol?

A

moderate pain

100
Q

What is the duration of action for tramadol?

A

6-8hrs

101
Q

Tramadol has a low risk of .. (3)

A
  • respiratory depression
  • constipation
  • urinary retention
102
Q

Tramadol adverse effect

A

tachycardia (high HR)

103
Q

Tramadol contraindications

A

myocardial infarction

104
Q

What is the alternative to morphine but 10 times less potent?

A

MEPERIDINE = PETHIDINE

105
Q

Which opioid is useful in biliary-pancreatic colic pain?

A

MEPERIDINE = PETHIDINE

106
Q

Which opioid is useful in lower myocardial infarction

A

MEPERIDINE = PETHIDINE

107
Q

Which opioid has a higher risk of respiratory depression and dependence?

A

MEPERIDINE = PETHIDINE

108
Q

After metabolism, MEPERIDINE = PETHIDINE metabolites can cause.. (2)

A
  • Cardiotoxicity: tachycardia

- Neurotoxicity: convulsions.

109
Q

Which opioid does not cross the placental barrier?

A

MEPERIDINE = PETHIDINE

110
Q

Which drug is 100 times more potent than morphine

A

fentanyl

111
Q

Fentanyl treats what kind of pain?

A

Moderate to severe pain

112
Q

fentanyl has ___ lipid solubility

A

high

113
Q

fentanyl has ___ cardiotoxicity

A

little

114
Q

Which opioid is frequently used in anesthesia?

A

fentanyl

115
Q

What are the routes of administration for fentanyl? (2)

A
  • IV

- transdermal (90% biodisponibility) every 2-3 days

116
Q

Describe the fentanyl transdermal patch

A
  • 90% biodisponibility

- path changes 2-3 days

117
Q

Fentanyl is used as an alternative in elderly and pain oncology patients because…

A

less constipation than morphine

118
Q

Which opioid causes less constipation than morphine?

A

fentanyl

119
Q

Which opioid is similar to morphine, but with less cardiovascular effects?

A

buprenorphine

120
Q

Buprenorphine is useful in treating what type of pain?

A

moderate-severe (transdermal 35-70 mcg/h)

121
Q

What opioid is useful in treating opioid dependence and through what route?

A
  • buprenorphine

- sublingual

122
Q

Describe buprenorphine absorption

A
  • oral =low

- better sublingual, dermal and IV

123
Q

Where is buprenorphine metabolized?

A

-liver

124
Q

How is buprenorphine eliminated?

A

biliary elimination

125
Q

Burenorphine adverse reactions:

A

Same adverse reactions as morphine but less intense

126
Q

How does Naloxone work?

A

-immediate reversal of CNS depression

127
Q

How does Naltrexone work?

A

Prevention of opioids subjective effects

128
Q

What is the route of administration for naloxone?

A

Parenteral

129
Q

What is the route of administration for naltrexone?

A

oral

130
Q

When is naloxone used? (2)

A

acute treatment

-respiratory depression from full agonist intoxication/overdose

131
Q

When is naloxone used?

A

patient detoxification and addiction to opioids and

in chronic alcoholism

132
Q

Intoxication/overdose of opioids appears in … (3)

A
  • heroin addicts

- after IV adminsitration of potent opioids (ex. morphine or fentanyl)

133
Q

Symptoms of opioid intoxication/overdose? (3)

A
  • Decreased level of consciousness
  • Respiratory depression
  • Miosis ( Pinpoint pupils)
134
Q

opioid antidote

A

Naloxone IV bolus

135
Q

Which opioid is used to treat opioid dependence

and as an analgesic

A

Methadone

136
Q

Methadone route of administration

A

oral

137
Q

methadone is what type of opioid?

A

opioid agonsist

138
Q

Which opioid has a longer duration?

A

methadone

139
Q

Which opioid Doesn ́t have the euphoric effects associated with opiates?

A

methadone

140
Q

Do we need to worry about overdose with methadone?

A

yes

Pharm (14 decks)

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