Opioid analgesics Flashcards
(140 cards)
1
Q
What drugs can be used in pain treatment? (3)
A
I. Opioid analgesics
II. Analgesics and NSAIDs
III. Specific analgesics (adjuvants)
2
Q
Mechanism of action for opiod analgesics, opioids or narcotics?
A
-specific CNS receptors (opiates or opioids receptors changing perception of pain)
3
Q
What is the effect of opiod analgesics, opioids or narcotics? (6)
A
- produce analgesia (Strong)
- sedation
- somnolence (sleepyness)
- tolerance
- addiction
- abstinence
4
Q
What is somnolence?
A
sleepyness
5
Q
Mechanism of action for non-opioid analgesics (NSAIDS + Analgesics)? (2)
A
- Cox inhibitors
- inhibit prostaglandin synthesis (vasodialator
6
Q
What is protaglandin? (2)
A
a vasodilator.
Needs the COX enzyme
7
Q
What is the effect of non-opioid analgesics (NSAIDS + Analgesics)?
A
- analgesia (moderate)
- antipyretic
- nonaddictive
SOME:
- anti-inflammatory
- antiplatlet
8
Q
What are the adjuvant analgesic drug types? (3)
A
- anti-epileptic
- anti-depressants
- neuroleptics
9
Q
What do you prescribe in the first step of pain management? (3)
A
- Mild to moderate pain
- NSAIDs (ibuprofen…)
- paracetamol
10
Q
What do you prescribe in the 2nd step of pain management? (3)
A
- Moderate to intense pain
- NSAIDs + Weak opioids (tramadol, codeine)
11
Q
What do you prescribe in the 3rd step of pain management? (2)
A
- Intense pain uncontrolled with previous drugs
- Strong opioid (morphine)
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
13
Q
In which step of pain management do you add adjuvant drugs?
A
-can be added in all steps depending on the pain
14
Q
What kind of pain do opioid analgesics treat? (2)
A
- moderate to severe
- acute or chronic
15
Q
What kind of analgesic effect do opioid analgesics have?
A
intense
16
Q
Opioid analgesics have an affinity for ______ receptors
A
opioid
17
Q
NSAID indications? (3)
A
- headache
- arthralgia (joint pain)
- myalgia (muscle pain)
18
Q
What is arthralgia?
A
joint pain
19
Q
What is myalgia?
A
pain in a muscle or muscle group
20
Q
Opioid indications?
A
- visceral pain
- intense pain
21
Q
NSAID pain effectiveness?
A
moderate
22
Q
opioids pain effectiveness?
A
intense
23
Q
NSAID analgesic location?
A
peripheral
24
Q
Opioid analgesic location?
A
central
25
Opioids are also called.... (2)
opiates & narcotics
26
Opioids come from...
Juice of the poppy (Papaver somniferum)
27
The poppy's latin name is
Papaver somniferum
28
The most significant natural alkaloid obtained from opium is
morphine
29
Which drug is used as a reference or standard to compare with the rest of the opioids?
morphine
30
First preparation that demonstrated analgesic, sedative and euphoric properties was?
- Juice of the poppy (Papaver somniferum)
| - 1st "opioid"
31
Opiate vs opioid?
- Opiate: products obtained from poppy juice and derivatives
- Opioid: any substance endogenous or exogenous with affinity for the
specific receptors.
32
What are the opioid receptors? (4)
- μ
- δ
- κ
- ORL-1
33
What is the mechanism of action for opioid receptors?
- affinity to opioid receptors
- DECREASE painful sensation
- DECREASE affective component of pain
34
What endogenous substances stimulate opioid receptors?
- beta-endorphins
| - enkephalins
35
Location of opioid receptors? (5)
- C.N.S. : medulla, midbrain, thalamus, cortex
| - PERIPHERAL N.S.
36
How do opioid analgesics work?
- act on receptors mu (μ),
37
What is the action of the mu (μ) receptors
- analgesic effect
| - respiratory depression
38
What are the different types of opioids?
- major opioids
- minor opiates
- partial agonists
- agonist-antagonists
39
What are the major opioids? (4)
- MORPHINE
- FENTANYL
- PETHIDINE (meperidine)
- METADONE
40
What are the minor opiates? (3)
- CODEINE / DIDYDROCODEINE
- TRAMADOL
- DEXTROPOPOXYPHENE
41
What are the opioid antagonists?
- Naloxone
| - Naltrexone
42
What is the opioid partial agonist?
Buprenorphinie
43
What is the opioid agonist-antagonist?
Pentazocine
44
Opioid route of administration? (3)
- oral
- sublingual (buprenorphine)
- Transdermal (buprenorphine, fentanyl)
- Parentreral (IM, IV, SC, epidural)
45
Why are opioids used orally?
good absorption
46
Opioid bioavailability orally? (2)
- low
| - high hepatic first pass
47
Which opioids are used sublingually? why? (2)
- buprenorphine
| - avoids hepatic first pass
48
Which opioids are used transdermally? why? (3)
- buprenorphine
- fentanyl
- avoids hepatic first pass
49
Describe opioid biotransformation and excretion
- elevated hepatic biotransformation
| - renal excretion
50
Do opioids cross placenta and BBB?
yes
51
Opioid half life?
4-6 hrs
| * can have controlled release preparations
52
define stupor
a state of near-unconsciousness or insensibility.
53
Pharmacologic actions of morphine
- Decreased level of consciousness: sedation and stupor
- Respiratory depression (dose + route dependent)
- hypothermia
- miosis (pupillary constriction)
- nausea + vomitting
- incr. muscle tone (high doses)
54
Morphine: acute or chronic?
both
| depends on dose
55
What are the cardiovascular effects of morphine? (3)
- hypotension
- bradycardia (slow heart action)
- Vasodilation (decreasing vascular tone)
56
What are the GI effects of morphine? (4)
- delayed gastric emptying
- constipation
- increased pressure in bile ducts (hypertonic sphincter of oddi)
57
What are the urinary effects of morphine?
- increased bladder tone
| - less urination (?)
58
Morphine and tolerance? (4)
- quick development of tolerance
- duration of action shortened
- response intensity decreases
- dose increase required
59
Morphine and dependence? (2)
- withdrawl =severe central and vegetative symptoms
| - mostly sympathetic
60
Morphine withdrawal is mostly _______
sympathetic
61
ANALGESIC DOSE _______ ALTER THE LEVEL OF CONCIOUSNESS
does not
62
Morphine analgesic indications (4)
-reduces emotional response to pain
IV-SC for a few days:
- surgical interventions
- polytrauma
IV few days or SC (oral) chronic:
-tumors
63
When do you use subcutaneous or oral morphine?
chronic treatment of tumors
64
How/why do we use morphine for surgical interventions? (3)
analgesic
| IV or SC for a few days
65
How/why do we use morphine for polytrauma? (3)
analgesic
| IV or SC for a few days
66
How/why do we use morphine for tumors? (3)
analgesic
- IV few days or
- SC (oral) for chronic
67
What are the morphine vasodilator indications? (2)
- Acute pulmonary edema (iv-sc) (heart failure)
| - Acute myocardial infarction (AMI)
68
How / why do we use morphine for Acute pulmonary edema? (3)
- vasodilator for heart failure
| - IV or SC
69
Why do we use morphine for acute myocardial infarction?
vasodilator
70
What are the morphine sedative indications?
Mechanical ventilation (i.v-s.c..)
71
How / why do we use morphine for Mechanical ventilation?
- sedative
| - IV or SC
72
Describe morphine respiratory depression (3)
- adverse effect
- can be used to relief respiratory effort in terminal situations
- maximum IV
- minimum oral
73
Morphine adverse effects (4)
- 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
How does morphine act on the bronchus?
bronchoconstriction
75
Antidote for acute morphine poisoning?
naloxone
76
Morphine contraindications (8)
-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
What drug is the exception for opioid contradiction for Biliary pancreatic colic pain
MEPERIDINE = PETHIDINE
78
What is the sphincter of Oddi?
-controls flow of bile and pancreatic juice into the second part of duodenum
79
Morphine has drug interactions with... (6)
- CNS depressants (incr.)
- Diuretics (decr.)
- Tricyclic antidepressants (incr. analgesic)
- CA-antagonists (incr. analgesic)
- rifampicin (incr. metabolism)
- delayed absorption of other drugs
80
Morphine interaction with CNS depressants causes....? Which drugs? (5)
- (opiates) increased effect
- neuroleptics
- antidepressants
- benzodiazepines
- ethanol
81
Morphine interaction with diuretics causes....?
a decreased effect
82
Morphine interaction with tricyclic anti-depressants causes....?
increase in the analgesic activity
83
Morphine interaction with CA-antagonists causes....?
increase in the analgesic activity
84
Morphine interaction with rifampicin causes....?
increased metabolism of morphine
85
Morphine interaction with other drugs causes...?
delayed absorption of the other drugs
86
opioid analgesics ______ the cough reflex (2)
decrease
| ex. codiene
87
opioid analgesics ______ secretions. which ones?
decrease
- intestinal
- biliary
- saliva
88
Can opioid analgesics be used pulmonary edema? (4)
- yes
- reduces preload and afterload
- relieves pulmonary and cardiac congestion
89
Can opioids be used for narcosis hypnosis and coma?
yes
90
Codiene/dihydrocodeine is a _____ derivative
morphine
91
Codiene/dihydrocodeine has ____ affinity for _____ receptor
less affinity
| μ receptors.
92
Codiene/dihydrocodeine effects? (3)
- Antitussive: central action
- Analgesic: association with acetaminophen or ASA
- Antidiarrheal: constipation
93
Codiene/dihydrocodeine has analgesic associations with ...? (2)
- acetaminophen
| - aspirin
94
What has a higher risk of addiction? morphine or codeine?
morphine
95
What has a higher risk of respiratory depression? morphine or codeine?
morphine
96
DEXTROPROPOXYPHEN is a ______ opioid
minor
97
DEXTROPROPOXYPHEN has analgesic efficacy similar to ______
codiene
98
Which is better, dextropropoxyphen or codiene?
both have same advantages
99
When do we use tramadol?
moderate pain
100
What is the duration of action for tramadol?
6-8hrs
101
Tramadol has a low risk of .. (3)
- respiratory depression
- constipation
- urinary retention
102
Tramadol adverse effect
tachycardia (high HR)
103
Tramadol contraindications
myocardial infarction
104
What is the alternative to morphine but 10 times less potent?
MEPERIDINE = PETHIDINE
105
Which opioid is useful in biliary-pancreatic colic pain?
MEPERIDINE = PETHIDINE
106
Which opioid is useful in lower myocardial infarction
MEPERIDINE = PETHIDINE
107
Which opioid has a higher risk of respiratory depression and dependence?
MEPERIDINE = PETHIDINE
108
After metabolism, MEPERIDINE = PETHIDINE metabolites can cause.. (2)
- Cardiotoxicity: tachycardia
| - Neurotoxicity: convulsions.
109
Which opioid does not cross the placental barrier?
MEPERIDINE = PETHIDINE
110
Which drug is 100 times more potent than morphine
fentanyl
111
Fentanyl treats what kind of pain?
Moderate to severe pain
112
fentanyl has ___ lipid solubility
high
113
fentanyl has ___ cardiotoxicity
little
114
Which opioid is frequently used in anesthesia?
fentanyl
115
What are the routes of administration for fentanyl? (2)
- IV
| - transdermal (90% biodisponibility) every 2-3 days
116
Describe the fentanyl transdermal patch
- 90% biodisponibility
| - path changes 2-3 days
117
Fentanyl is used as an alternative in elderly and pain oncology patients because...
less constipation than morphine
118
Which opioid causes less constipation than morphine?
fentanyl
119
Which opioid is similar to morphine, but with less cardiovascular effects?
buprenorphine
120
Buprenorphine is useful in treating what type of pain?
moderate-severe (transdermal 35-70 mcg/h)
121
What opioid is useful in treating opioid dependence and through what route?
- buprenorphine
| - sublingual
122
Describe buprenorphine absorption
- oral =low
| - better sublingual, dermal and IV
123
Where is buprenorphine metabolized?
-liver
124
How is buprenorphine eliminated?
biliary elimination
125
Burenorphine adverse reactions:
Same adverse reactions as morphine but less intense
126
How does Naloxone work?
-immediate reversal of CNS depression
127
How does Naltrexone work?
Prevention of opioids subjective effects
128
What is the route of administration for naloxone?
Parenteral
129
What is the route of administration for naltrexone?
oral
130
When is naloxone used? (2)
acute treatment
| -respiratory depression from full agonist intoxication/overdose
131
When is naloxone used?
patient detoxification and addiction to opioids and
| in chronic alcoholism
132
Intoxication/overdose of opioids appears in ... (3)
- heroin addicts
| - after IV adminsitration of potent opioids (ex. morphine or fentanyl)
133
Symptoms of opioid intoxication/overdose? (3)
- Decreased level of consciousness
- Respiratory depression
- Miosis ( Pinpoint pupils)
134
opioid antidote
Naloxone IV bolus
135
Which opioid is used to treat opioid dependence
| and as an analgesic
Methadone
136
Methadone route of administration
oral
137
methadone is what type of opioid?
opioid agonsist
138
Which opioid has a longer duration?
methadone
139
Which opioid Doesn ́t have the euphoric effects associated with opiates?
methadone
140
Do we need to worry about overdose with methadone?
yes
