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Unrelived pain
- causes unecessary suffering
- stimulates sympathetic respone
- decreases immune function
- weakens already debilitated patients
- increases poor compliance with therapy
- impinges on work, family, leisure
- diminishes hope
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Assessment of Pain intensity
- Scales: 0-10
- Simple descriptor (none, mild, moderate, severe)
- Faces
- When? initiation; dose increase;peak of analgesic
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Physical dependence
a pharmacologic property causing the occurrence of withdrawal symptoms with abrupt discontinuation or administration of an antagonist
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Tolerance
the pharmacologic effect in which with repeated administration, increasing doses are necessary to provvide the same effect
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Addiction
psychological dependence, a behavioral syndrome marked by drug craving, compulsie efforts to secure a drug supply, hoarding, and drug-related interference with pyschological, social, or physical function
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Mechanisms of action
Nonopiod analgesics
- Work in periphery
- Affect prostaglandin synthesis
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Mechanisms of action
Opiod analgesics
- Work in CNS
- Bind to the mu, kappa, and delta receptors
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Acetominophen (Tylenol)
- analgesic
- antipyretic
- no anti-inflammatory effects
- max dose: 4000 mg/day
- risk of hepatotoxicity with higher doses
- Ofirmev - IV acetominophen
- Antidote: acetylcsteine (Mucomyst, Acetadote)
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Cyclooxygenase inhibitors
- COX found in all tissues, encourages synthesis of prostaglandins
- COX 1: present in all tissues, protects gastric mucosa, supports renal function
- COX 2: at site of tissue injury & brain; mediates inflammation, pain, fever response
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COX 1 inhibition
- Gastric erosion and ulceration (-)
- Bleeding tendencies (-)
- Acute renal failure (-)
- Protection against myocardial infarction (+)
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COX 2 inhibition
- Suppression of inflammation (+)
- Alleviation of pain (+)
- Reduction of fever (+)
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Salicylates
Asprin (acetylsalicyclic acid, ASA)
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Salicylates
- analgesic, antipyretic, antiinflammatory
- Initial ang effect: 1 hr
- Max anti-inflammatory effect- in 2 wks
- ADR: GI upset, bleeding
- Toxicity: tinnitus, sweating, dizziness
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NSAIDs
- Inhibit both COX1 and COX2
- Analgesic, antipyretic, anti-inflammatory
- Initial analgesic effect: 1 hr
- Maximum anti-inflammatory effect: 2 wks
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ibuprofen
- Vitamin I
- NSAID
- Advil, Nuprin, Motrin,
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Adjuvants
- Enhance efficacy of other agents
- Add analgesia
- Treat concurrent symptoms
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Most common adjuvants
- to treat neuropathic pain: (gabapentin (Neurontin)
- to treat fibromyalgia: pregabalin (Lyrica)
- Others: cyclobenzadrine (Flexaril)
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gabapentin
- adjuvant to treat neuropathic pain
- Neurontin
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pregabalin
- Adjuvant to treat fibromyalgia
- Lyrica
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Opiod classifications
- Opioid agonist
- Opioid agonist/antagonist
- Opiod antagonist
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Opioids
- Treat moderate to severe pain
- Bind to mu opioid receptors in CNS
- No ceiling effect
- No major organ disfunction
- Generally manageable side effects
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codeine
- Step 2 opioid
- more emetogenic and constipating
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hydrocodone
- Step 2 opioid
- Vicodin, Lorcet, Norco
- Stronger than codeine
- available in varying doses, limited by acetaminophen content
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oxycodone
- Step 2 opioid
- Percocet, Percodan, Tylox
- also available as a single entity?
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Tramadol
- Ultram
- Centrally acting nonopioid analgesic
- Binds to mu opioid receptor
- Inhibits uptake of serotonin and norepi in the CNS
- Indicated for moderate to moderately severe pain
- Equianalgesic to Tylenol with codeine #3
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Tramadol cont
- Ultram
- dose 50-100 mg q 4-6 hr
- Onset 1 hr
- Peak 2-3 hrs
- similar side effects to opioids
- May cause seizures with therap doses
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morphine
- Step 3 opioid
- MSO4, MS, Roxanol, MS Contin, Oramorph, Kadian, Avinza
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Meperidine (Demerol)
- Step 3 opioid
- Duration: 2-3 hours
- PO Doses: 1/4 analgesic effect
- Toxic metabolite: normeperidine (not reversible with Narcan)
- Do not use for more than 48 hrs or at doses >600 mg/24 hr
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Equianalgesic Opioid Doses
Look up in book
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Titrating opioid doses
- Increase dose 25-50% until there is either a 50% reduction in pain rating or the patient reports satisfactory pain relief
- A repeat dose can be give at time of peak if previous dose is ineffective and side effects are minimal.
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Opioid dosing
- ATC does more effective than PRN for pain that is expected to continue
- More effective if given before pain becomes severe
- Provide analgesic to allow for uninterrupted sleep
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Opioids: Routes of administration
- Noninvasive is best
- PO is effective if doses are high enough
- IV route is safest and fastest for titration
- IM is painful and unreliable: AVOID
- Transdermal useful for chronic pain
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Opioid Agonist Antagonist Analgesics
- Nor recommended for 1st line therapy
- Bind to kappa receptors
- Partial agonist
- Partial antagonist (may cause withdrawal in physically dependent patients on opioid agonists
- Greater risk of dysphoric side effects
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pentazocine
- Talwin
- Opioid Agonist Antagonist
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butorphanol
- Stadol
- Opioid Agonist Antagonist
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nalbuphine
- Nubain
- Opioid Agonist Antagonist
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buprenorphine
- Buprenex, Butrans
- Opioid Agonist Antagonist
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buprenorphine transdermal (Butrans)
- Moderate to severe chronic pain
- Transdermal patch lasts up to 7 days
- No alcohol during use
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Dosing long-acting opioids
- Treat patient with immediate-release opioids for 48 hrs to learn average daily dose
- Approximately 2/3 of estimated daily dose should be used for sustained-release
- Provide supplemental immediate release opioid for breakthrough pain
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Long acting opioids
- morphine (MS Contin, Oramorph, Avinza, Kadian)
- oxycodone (Oxycontin)
- Hydromorphone (Exalgo)
- fentanyl (Duragesic)
- oxymorphone (Opana ER)
- methadone
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Sustained-released morphine
- MS Contin & Oramorph (8-12 hrs): Do not crush or chew; swallow hole
- Kadian & Avinza (24 hrs): Caps can be opened and sprinkled on soft, moist food
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Sustained-release oxycodone
- Oxycontin (8-12 hrs)
- Do not crush or chew; swallow whole
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Hydromorphone
- Sustained release (Exalgo)
- Once every 24 hrs
- Do not crush or chew; swallow whole
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Long-acting opioids: Transdermal Fentanyl
- gradual increase in serum levels
- Steady state achieved in 12-24 hrs
- Duration of action: up to 72 hrs
- Elimination half life: ~17 hrs
- Transdermal application bypasses GI tract
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Extended-release oxymorphone
- Opana
- Titrate on short-acting form
- Then convert to long-acting form Q 12 hrs
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Methadone
- Inexpensive
- Accumulates with repeated dosing
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Breakthrough pain
- Reaches max intensity within 3 minutes
- Lasts an average of 30 min
- Doses should be equiv to about 10-20% of the 24 hr total dose. Doses may be given every 2 hrs as needed
- Do not use sustained-release meds for breakthrough pain
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Fentanyl buccal
- Fentora
- For breakthrough pain
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Opioid-induced side effects
- constipation (give stimulant lax: Senokot)
- nausea & vomiting
- sedation
- respiratory depression
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methylnaltrexone
- Relistor
- Tx for constipation caused by opioid use
- Acts peripherally as mu-opioid receptor antagonist-blocks opioid effects in GI tract
- Blocks GI tract effects without loss of analgesia
- SQ injection qod
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Sedation scale
- S=sleeping, easily aroused, Requires no action
- 1=awake and alert. Requires no action
- 2=occasionally drowsy; easy to arouse. Requires no action
- 3=frequently drowsy, arousable, drifts off to sleep during conversation. Decrease opioid dose
- 4=somnolent, minimal or no response to stimuli. Decrease opioid; consider naloxone (Narcan)
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Discontinuing opioids
- Short-acting opioids, taper doses
- 50% x 2 days
- 25% every 2 days
- Discontinue after 2 days at min dose
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hydrocodone
- Step 2 opioid
- Vicodin, Norco
- stronger than codeine
- limited by acetominophen content
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Local anesthetics
- suppress pain by blocking impulse conduction along axons
- Block Na channels
- Block all function, both sensory and motor
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Classifications: Local anesthetics
- Esters: procaine (Novocain)
- Amides: lidocaine (Xylocaine)
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lidocaine
- widely used local anesthetic
- used with epinephrine
- control of dysrhythmias
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bupivicaine
- Marcaine, sensorcaine
- epidural and local
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cocaine
- ester
- used in EENT procedures
- topical only
- do not use with epinephrine
- produces euphoria
- physical dependence
- avoid with cardiac patients
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Local anesthetics: Methods of administration
- topical: mixture of locals (lidocaine/prilocaine)
- by injection: infiltration, nerve block, IV regional, epidural, spinal
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General anesthetics
- Produce unconsciousness, lack of response to all painful stimuli
- Two groups: inhalation, IV
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Stages of anesthesia
- Stage I: analgesia
- Stage II: delirium
- Stage III: surgical anesthesia
- Stage IV: medullary paralysis
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Propofol (Diprivan)
IV Anesthetic
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sumatriptan
(Imitrex)
- Seratonin agonist
- Migraine treatment
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methotrexate (Rheumatrex)
- Disease-Modifying Antirheumatic Drug (DMARD)
- Treatment of RA
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etanercept (Enbrel)
- DMARD
- Tumor necrosis factor blocker
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gout
- deposit of uric acid crystals in joint
- increased uric acid production or decreased excretion
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