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The Insight Corner Hub: Palliative care: Pain Management Palliative care: Pain Management

Pharmacological options
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.
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
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.
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. 

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
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
Oxymorphone
semisynthetic. Twice as potent as morphine


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.

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.

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

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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