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Opioid Analgesics
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How are opioid analgesics classified?
By how
effectively
they relieve pain
What are the categories of opioid analgesics and their key features?
Strong opioids
:
Morphine
,
Fentanyl
,
Oxycodone
Best for severe pain, higher side effects
Intermediate efficacy
:
Dihydrocodeine
Suitable for moderate pain, often combined with NSAIDs
Partial agonists
: Buprenorphine,
Pentazocine
Less potent, lower abuse potential
What is the analogy used to describe strong opioids?
Like taking an
elevator
to the top floor
What is the analogy used for intermediate efficacy agents?
Like using the stairs for
moderate
relief
How are partial agonists compared in the analogy?
Like taking a few steps for
mild relief
What are the strong opioids mentioned?
Morphine
,
Fentanyl
,
Oxycodone
What is the primary function of strong opioids?
To relieve
severe
and
chronic pain
How do strong opioids work?
By binding to
opioid receptors
in the brain
What are the key properties of morphine?
Potent
pain reliever, effective orally or
parenterally
What are the key uses of morphine?
Acute pain
in hospitals,
chronic pain management
What is a key property of fentanyl?
Extremely
potent
, available in
transdermal
patches
What are the key uses of fentanyl?
Post-operative
pain, breakthrough pain in
cancer
patients
What is a key property of oxycodone?
Strong
efficacy
, often combined with other
analgesics
What are the key uses of oxycodone?
Moderate to
severe
pain, often after surgery
What is the key feature of dihydrocodeine?
More effective than codeine, not as strong as
morphine
How is dihydrocodeine often used?
Combined with
paracetamol
or
NSAIDs
What is the comparison of opioid types based on efficacy?
Strong:
Morphine
, High efficacy, No combination needed
Intermediate
: Dihydrocodeine, Medium efficacy, Combined with
Paracetamol/NSAIDs
Weak
:
Codeine
, Low efficacy, Combined with Paracetamol/NSAIDs
What are the key properties of partial agonists?
Relieve pain but not as much as
strong opioids
What are the key uses of buprenorphine?
Chronic
musculoskeletal
pain
What are the key uses of pentazocine?
Moderate
pain relief when needed
What are the phases of pharmacokinetics for opioid analgesics?
Absorption: How the drug enters the
bloodstream
Distribution: How the drug spreads throughout the
body
Metabolism: How the drug is broken down in the
liver
Excretion: How the drug is
removed
from the body
What is the implication of absorption for opioids?
Routes affect speed and amount entering
circulation
How do opioids distribute in the body?
They cross the
blood-brain barrier
to
target
pain receptors
What is the role of metabolism in opioids?
The
liver
metabolizes opioids, reducing
potency
How are opioids excreted from the body?
Kidneys excrete
metabolites
in
urine
What is the mechanism of action of opioid analgesics?
Interact with
opioid receptors
:
μ, δ, κ
Affect neurotransmission and modulate pain signals
Bind to
endogenous peptides
:
endorphins
,
enkephalins
,
dynorphins
What are the effects of the μ receptor?
Antinociception
,
analgesia
,
respiratory depression
What are the effects of the δ receptor?
Antinociception
, analgesia, may play a role in
tolerance
What are the effects of the κ receptor?
Analgesia
, diuresis, sedation,
dysphoria
What are the acute effects of opioid analgesics?
Analgesia
: Pain relief
Sedation & Euphoria: Relaxation and well-being
Respiratory Depression
: Reduced respiratory rate
Nausea & Vomiting: Stimulation of chemoreceptor trigger zone
GI Effects
: Constipation
Smooth Muscle Changes: Contraction of biliary tract
Miosis
: Pupillary constriction
Miscellaneous:
Truncal rigidity
, histamine release
What causes respiratory depression in opioid use?
Reduced
respiratory rate
at high doses
What GI effects do opioids have?
Decreased
intestinal
peristalsis causing
constipation
What is the effect of opioids on smooth muscles?
Contraction of
biliary tract
and increased
bladder tone
What is miosis in relation to opioid use?
Pupillary constriction characteristic of
opioids
What are the chronic effects of opioid analgesics?
Tolerance
: Higher doses needed for pain relief
Dependence
: Physical reliance on opioids
Hyperalgesia
: Increased pain sensitivity after prolonged use
What is tolerance in opioid use?
Decreased sensitivity requiring
higher doses
What is dependence in opioid use?
Physical reliance leading to
withdrawal symptoms
What is hyperalgesia in relation to opioids?
Increased
pain sensitivity
after prolonged use
What are the clinical uses of opioid analgesics?
Analgesia:
Morphine
, Oxycodone for
severe pain
Cough Suppressant:
Codeine
,
Dextromethorphan
Treatment of
Diarrhea
:
Diphenoxylate
,
Loperamide
Pulmonary Edema
: Morphine for calming effects
Anesthesia:
Fentanyl
, Morphine as
preoperative
medications
Opioid Dependence:
Methadone
,
Suboxone
for withdrawal management
What opioids are used for cough suppression?
Codeine
,
Dextromethorphan
See all 54 cards
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