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Category
|
Drug
Name
|
Potency
|
Potential
Side effects
|
Cautions
|
|||||
1. Non-opioids
|
Acetaminophen
|
It should be the first step of the
treatment if the pain level is mild. It may also be considered a good
medication to add to an opioid treatment.
|
Hepatic toxicity. Light-headedness, sedation,
constipation, dizziness, nausea, vomiting, respiratory depression
|
severe liver failure. Lower dose
to 2 gms in liver disease.
|
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NSAIDs:
The options which are considered
as the safest nowadays are ibuprofen and naproxen.
|
May
have a benefit in pain mediated by inflammation (e.g., bone metastases,
musculoskeletal or skin pain) through the blockage of prostaglandins
biosynthesis
|
Gastrointestinal
irritation, bleeding
|
Renal
failure
|
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2. Weak Opioids
|
Codeine
|
converted to its active agents
(among them morphine) through the enzyme CYP2D6. 10 mg codeine usually
equivalent to 1 mg of morphine.
|
Ultra-rapid metabolizers and
may have an increased risk of side effects. Sedation, nausea, vomiting,
dizziness, constipation, CNS depression, sweating, headache, lethargy,
confusion, light-headedness.
|
The only indication for codeine
remains its action against cough, probably through its pro-drug.
|
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Tramadol
|
synthetic
opioid, about five times less potent than morphine. Not considered to be
"at risk" for addiction due its weak action on the mu opioid
receptors.Due to its blockage of serotonin and norepinephrine reuptake, may
have an additional benefit in neuropathic pain.
|
There
are several limitations: a ceiling dose of 400 mg/day, an increased risk of
seizures in predisposed patients, and more adverse effects than other opioids
such as nausea and vomiting, especially in the geriatric population.
|
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3. Strong Opioids
|
Morphine
|
Remains the “gold standard” as it
has been the most extensively studied.
|
Lead to opioid-related
toxicity. Sedation, hypotension, increased sweating, constipation, dizziness,
drowsiness, nausea, vomiting, dry mouth, somnolence, respiratory depression.
|
Renal impairment
|
|||||
Hydrocodone
|
slightly
less potent than morphine. Unfortunately, it is only available in combination
with APAP or NSAIDs. It is metabolized to hydromorphone.
|
Sedation,
hypotension, increased sweating, constipation, dizziness, drowsiness, nausea,
vomiting, dry mouth, somnolence, respiratory depression.
|
|||||||
Hydromorphone
|
similar properties than morphine
but around five times more potent
|
Lead to neurotoxicity at
high doses
|
Renal impairment
|
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Oxycodone
|
synthetic
opioid. Unfortunately not available as parenteral formulation. Slightly more
potent than morphine (10 mg morphine=7.5 mg oxycodone). Targets not only mu
receptors as other usual opioids but also kappa receptors, which explains why
it may have a better action on neuropathic pain and may produce less nausea
and vomiting.
|
Light-headedness,
sedation, constipation, dizziness, nausea, vomiting, sweating, respiratory
depression
|
Kidney,
Renal impairment
|
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Oxymorphone
|
semisynthetic. Twice as potent as
morphine
|
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Fentanyl
|
Highly
lipid soluble opioid which can be administered parenterally, transdermally, transmucosally,
buccally, intranasally but not orally. Extremely potent (around 100 times
morphine)
|
Sedation,
sweating, headache, vertigo, lethargy, confusion, light-headedness, nausea,
vomiting, respiratory depression.
|
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Meperidine
|
Analgesic, preoperative,
medication, support of anesthesia
|
Not recommended because of the
neurotoxic effects of its metabolites (increased risk of seizures in
predisposed population) and its high risks of addiction.
|
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Methadone
|
synthetic
opioid. Poor reputation due to the variability in half-life for individuals
requiring careful titration and optimal compliance (half-life prolonged with
prolonged use).
|
Light-headedness,
dizziness, sedation, nausea, vomiting, constipation, respiratory depression
|
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4.
Coanalgesics or adjuvant analgesics
|
Antidepressants: desiprimine and nortriptyline are
better tolerated, antiepileptic
and drugsanticonvulsants: gabapentin and pregabalin for neuropathic
pain
|
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