Pain lecture

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HuskerDevil
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35085
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Pain lecture
Updated:
2010-09-16 13:07:18
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DPAP2012 pharmacology pain
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Pain lecture
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  1. Pain Relief Stepladder
    Mild, Moderate, Severe
    • 1. Mild
    • Aspirin
    • Acetaminophen
    • NSAIDs
    • +/- adjuvants

    • 2. Moderate
    • APAP/Codeine
    • APAP/Hydrocodone
    • APAP/Oxycodone
    • APAP/Dihydrocodeine
    • Tramadol
    • +/- Adjuvants

    • 3. Severe
    • Morphine
    • Hydromorphone
    • Methadone
    • Levorphanol
    • Fentanyl
    • Oxycodone
    • +/- Adjuvants
  2. Non-Opioid Analgesice
    • Differ from opioids:
    • Ceiling effect applies
    • No tolerance or physical dependence
    • Not associated with abuse/addiction
    • Antipyretic
    • Most=Anti-inflammatory

    APS recommends consideration for all analgesic regimens unless high risk or ineffective.
  3. Acetaminophen
    (N-Acetyl-Para-Amino-Phenol or APAP)

    MOA: ?, central

    • Use:
    • · Analgesic and anti-pyretic
    • · No anti-inflammatory effect
    • · No anti-platelet activity
    • · No GI damage

    • Useful for mild-moderate pain
    • · Use alone or in combination
    • · Dose limit = 4000 mg/day, divided doses (ALF rec.3000 mg)

    • Safety
    • · Use with caution in pts with liver dz or alcoholism
    • · FDA – hot topic - associated with liver damage, often combined with other meds and pt is unaware

    • Drug interactions
    • · MinimalWarfarin
  4. NSAIDs
    Salicylates
    • Aspirin (Bayer, Ecotrin, Norwich)
    • Choline magnesium trisalicylate (Trilisate)
    • Diflunisal (Dolobid)
    • Magnesium salicylate (Doan’s)
    • Salsalate (Disalcid)
  5. NSAIDs
    Aspirin
    Acetylsalicylic acid or ASA

    MOA: inhibits Cox-1/Cox-2

    • Use
    • Mild to moderate pain
    • Antipyretic, anti-inflammatory
    • Low-dose: cardioprotection (only irrev. inhibition of platelet aggregation)

    • Safety
    • Upper GI disturbance and bleeding
    • Increased bleeding time
    • Hypersensitivity/bronchospasm in asthma pts (nasal polyps)
    • Tinnitus with high doses
    • Blood pressure (BP) increases
    • Avoid in children <12 with viral illness (Reyes syndrome)
    • Risk of hypersensitivity reaction (and cross-sensitivity with NSAIDs)
    • Many drug interactions
  6. NSAIDs
    Non-salicylates
    • MOA:
    • inhibit Cox-1/Cox-2
    • Ex: ibuprofen (Motrin, Advil, Caldolor), naproxen (Naprosyn), diclofenac (Voltaren, Flector patch, Pennsaid), indomethacin (Indocin)

    • Use
    • Mild to moderate pain
    • Antipyretic, anti-inflammatory

    • Safety
    • GI erosion / risk of bleeding (less than aspirin)
    • Decreased renal perfusion
    • Rashes, hypersensitivity/bronchospasm in asthma pts
    • Blood dyscrasias, liver effects, CNS effects, BP
    • Drug interactions
    • Bind to plasma proteins – many drug interactions
  7. NSAIDs
    COX-2 Inhibitors
    Celecoxib (Celebrex)

    • Use
    • Mild to moderate pain for patients at risk for GI ulcers

    • Safety
    • Increased risk of cardiovascular toxicity (Black Box)
    • Lower GI toxicity than NSAIDs
    • Relative risk 2.6 vs. 3.7
    • Use of ASA with Cox-2 eliminates advantage
    • Sulfonamide allergy
    • Renal
    • Drug interactions
  8. Opioids
    Full agonist (most common)

    • Antagonist (stop effects of opioids)
    • Naloxone, Naltrexone

    • Mixed Agonist/Antagonist
    • Buprenorphine, Butorphanol, Nalbuphine, Pentazocine, Bupenorphine/Naloxone (Suboxone)
  9. Opioid Classes
    • Morphine-like
    • Morphine (MS Contin, Kadian, avinza)
    • Hydromorphone (Dilaudid)
    • Codeine (prodrug for morphine)
    • Hydrocodone
    • Oxycodone (Oxycontin)

    • Meperidine-like
    • Meperidine (Demerol)
    • Toxic metabolites with repeated dosing
    • Esp. renal failure, elderly
    • Not recommended for chronic pain
    • Fentanyl (Duragesic)

    • Methadone-like
    • Methadone (Dolophine)
    • Propoxyphene (Darvon)
    • High adverse reaction profile
    • Not recommended for elderly or for chronic pain
    • Little evidence that it is any more effective for mild to moderate pain than less toxic non-opioid drugs
  10. Opioids
    Short vs Long Acting
    • Short:
    • Codeine
    • Hydrocodone
    • Hydromorphone
    • Morphine
    • Oxycodone
    • Tapentadol
    • Fentanyl (ultra-short)

    • Long:
    • Methadone
    • Buprenorphine
    • Sustained relase products of short acting
  11. Opiates Adverse Reactions
    Constipation: It is inevitable! Prevent it and treat it. Stool softeners, fluid, fiber, exercise

    Nausea/vomiting: Common early in therapy, ↓ with time, Codeine

    Sedation/cognitive impairment: Transitory (at initiation and dose escalation), Decrease dose?, trial of psychostimulant, rule out other causes if persistent.

    • Potential serious adverse reactions:
    • Respiratory depression
    • Apnea
    • Respiratory arrest
    • Circulatory depression
    • Hypotension
    • Shock
    • ►►naloxone (Narcan) = antagonist◄◄

    • Other common reactions:
    • Pruritus
    • Dizziness
    • Headache
    • Dry mouth
    • Urinary retention
  12. Adjuvants
    • Antidepressants
    • MOA: block reuptake of norepinephrine (NE) & serotonin, NMDA-receptor antagonism, sodium-channel blockade
    • Tricyclic antidepressants (TCAs)
    • Analgesia independent of antidepressant effect
    • Ex: amitriptyline (Elavil) – more adverse reactions, nortriptyline (Pamelor), desipramine (Norpramin)
    • Anticholinergic adverse reactions prominent: dry mouth, urinary retention, constipation, sedation, and orthostatic hypotension, cardiac arrhythmias
    • Other Antidepressants:
    • Selective Serotonin Reuptake Inhibitors (SSRIs): Fewer adverse reactions but not as effective as TCAs
    • Serotonin-NE Reuptake Inhibitors: duloxetine (Cymbalta), venlafaxine (Effexor), milnacipran (Savella)

    • Antiepileptic drugs (AEDs)
    • Another first line drug class for neuropathic pain
    • Especially lancinating
    • First generation: carbamazepine (Tegretol), phenytoin (Dilantin)
    • Second generation: gabapentin (Neurontin), pregabalin (Lyrica)

    Local anesthetics

    • Topical agents
    • lidocaine 5% patch (LidoDerm), Excellent choice for localized pain, 12 hours on – 12 hours off, Few adverse reactions; don’t use with class I antiarrhythmics
    • capsaicin (Zostrix, Qutenza), Chile pepper derivative, Causes burning and stinging sensation, Wash hands after applying

    • Miscellaneous
    • - First-Line Medications
    • - gabapentin (Neurontin)
    • - 5% Lidocaine patch (LidoDerm)
    • - Opioid analgesics
    • - tramadol (Ultram)
    • - Tricyclic antidepressants (TCAs)
    • - Non-Pharmacologic Techniques
    • - Supplement to pharmacological measures
    • o Increased pain relief
    • - Other advantages
    • o Improve mood
    • o Reduce anxiety
    • o Increase a patient’s sense of control
    • § Strengthen coping abilities
    • o Assist with sleep
    • o Relax muscles
    • - Improve quality of life
    • - Psychosocial
    • o Patient education and preparation
    • o Psychological and behavioral techniques
    • - Other physical modalities
    • o Physical rehabilitation
    • o Electrical stimulation
    • o Acupuncture
    • o Heat and cold
    • o Splinting, assistive devices, etc.
  13. Medication Schedules
    • CI
    • High potential for abuse; no accepted therapeutic use
    • Heroin, LSD

    • CII
    • High potential for abuse; accepted therapeutic use
    • Oxycodone, morphine, cocaine
    • No refills
    • Can only write for a 30 day supply

    • CIII
    • Potential for abuse less than CII
    • Ketamine, anabolic steroids
    • 5 refills
    • Prescription expires in 6 months
    • Can only write for a 30 day supply

    • CIV
    • Potential for abuse less than CIII
    • Benzodiazepines, phenobarbital, most sleep meds
    • 5 refills
    • Prescription expires in 6 months

    • CV
    • Potential for abuse less than CIV
    • OTC codeine products, cough medicines
    • 5 refills
    • Prescription expires in 6 months

    • CVI
    • Marijuana (in NC)

    • Unscheduled
    • No potential for abuse
    • Anything else: HTN meds, antibiotics, etc

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