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Terms in this set (65)
Nociceptive Pain pathway
stimulate peripheral nociceptive receptors which release substances--> afferent nerve fibers pick up message--> spinal cord (dorsal horn)-->cerebrum, thalamus other supra spinal structures in the brain where info is registered about the nature of pain
poor response to analgesics, nerve damage or persistent stimulation, abnormal processing by peripheral and CNS
Acute pain signs
HTN, tachycardia, sweating, facial pain expressions, organic cause, more responsive to meds, goal is to cure the cause of the pain
chronic pain signs
depression, insomnia, dependence and tolerance to meds, psych component is strong, difficult to treat, goal is pain relief and rehab
Acetaminophen (tylenol) pharmacology
Metabolized in the liver by glucuronidation, small amounts--> N hydroxylation to reactive metabolite which is conjugated by glutathione and may cause deplete hepatic glutathione and cause liver necrosis in high doses
analgesic, antipyretic, not anti inflammatory
Max dose of tylenol
650-1000 mg/dose for analgesia, max chronic daily dose is 4 grams
rarely a rash, acute overdose hepatotoxicity may occur after single dose of 10-15g
N acetylcysteine (mucomyst)
for tylenol OD, Replaces depleted glutathione ASAP mucomyst is more effective if given within 10 hours after ingestion but can be given up to 36 hours post ingestion
decrease prostaglandin synthesis by inhibiting COX enzymes (cycloxygenase)
Uses of NSAIDS
treats multiple types of pain, analgesic, antipyretic and anti inflammatory, ceiling effect may occur
AE of NSAIDs
gastritis with nausea, dyspepsia, ulceration, GI bleed, blockade of platelet aggregation, hypersensitivity reactions, decreased GFR and renal blood flow in certain patients some have more renal effects some have more GI effects
What do you treat a patient with that has a Hx of GI bleed or serious risk factors with NSAIDs?
Misoprostol, COX 2 inhibitor, lowest dose NSAID with least GI toxicity plus PPI such as omeprazole
NSAID drug interactions
anti hypertensives, blunted antihypertensive effects with ACEI, diuretics, antihypertensives, may potentiate anticoagulant effects, some decrease lithium clearance
What are the three major precursor proteins to make beta- endorphins and enkephalins?
Prepro-opiomelanocortin, Preproenkephalin, preprodynorphin
General opioid receptor characteristics
G protein coupled receptor family, Mu1, Mu2, delta 1, delta 2, Kappa 1, kappa 2
Receptor types and effects
Mu (M): analgesia, euphoria, respiratory depression, physiological dependence- most opioid analgesics act at the mu receptor, Delta and Kappa: spinal analgesia and other effects
Opioid effects on neurotransmitters
binding causes decrease release of neurotransmitters such as Ach, NE, glutamate, substance P and serotonin, hyper polarizes post synaptic membranes to prevent response to painful NTs
Where are Mu receptors found?
Int he spinal cord, thalamus, brainstem, descending pathways
why does tolerance to opioids happen?
receptors are internalized, activation of adenylyl cyclase to counteract the decrease associated with opiates binding to receptors
what are opiates?
any drug derived from or containing opium, opioids are synthetic narcotics not derived from opium, they are the strongest analgesic, no ceiling effects
Uses of opiates
analgesia, acute pulmonary edema (MI), cough (codeine, hydrocodone and dextromethoephan OTC, diarrhea
What is the active component of morphine and where is it activated?
morphine 6- glucuronide, the liver
where is morphine excreted?
How is the onset peak and duration effected by administration?
PO 1 hour, 1-2 hours and 4-12 hours vs epidural 15-60 mins, 30-60 mins, 24 hours
what happens when a patient is overdosing on morphine?
respiratory depression, miosis, hypotentionm bradycardia
Treatment of an overdose on morphine
airway and ventilation as needed and cardiac monitoring, Naloxone with repeated dosing
Morphine like agents
Dilaudid, oxymorphone, levophanol, codeine, hydrocodone, oxycodone, oxycontin
Effects of opiates
analgesia, euphoria, tranquility, muscle rigidity, miosis, resp depression, cough suppresant, N/V, slows GI tract, urinary retention, cardiovascular, itching, tolerance and dependence
In what cases do you have to use precaution when administering opiates
respiratory disease, asthma, previous addictions, renal and hepatic disease, tolerance, dependence, drug seeking behavior, when converting one opiod to another
what do you use to convert on opioid to another
What can breakthrough pain during around the clock dosing be treated with?
end of dose pain can be managed by increasing the dose or decreasing the interval of scheduled pain medicine, predictable incident pain can be managed with a short acting opioid given 30 to 45 minutes prior to activity, unpredictable or idiopathic pain requires an opiate with a fast onset, consider non opioid analgesics for neuropathic pain
Meperidine (Demerol) compared to morphine
shorter duration and less potent than morphine
what is Meperidine (Demerol) converted to and where?
metabolized in the liver to normeperidine which cause near excitation and seizures
what are the eyes like in a patient on Meperidine (Demerol)
DILATED pupils unlike morphine and heroin
what are SE of Meperidine (Demerol)
severe reactions with MAO inhibitors- serotonin syndrome- delirium, hyperthermia, rigidity, convulsions and death
Diphenoxylate (Lomitil) use and SE
antidiarrheal, high doses can cause euphoria, and physical dependence
why is lomitil dosed with atropine sulfate
to reduce likelihood of abuse
Loperamide (Imodium) use
antidiarrheal agent by slowing GI motility, low solubility--> low potential for abuse
Fentanyl and Sufentanil uses
relief od SEVERE cancer pain as an adjunct to general anesthesia, fentanyl is 100x more potent than morphine, Sulfenanil is 1000x more potent, quick in quick out, causes muscle rigidity
what do you treat cancer patients patients with severe pain with?
fentanyl preps- transdermal patch (Duragesic) an provide pain support for 48-72 hours
What are Actiq and Fentora?
a fentanyl lozenge and a buccal tablet
What is Onsolis?
a buccal film, start with lowest dose 200 mug and only use for opioid tolerant pts, high risk for respiratory depression
what is methadone (Dolophine) used for?
helps maintain abstinence in herion or opiate users, it reduces cravings and staves off withdrawal w/o causing high
how is Butophanol (stadol) used for and how is it administered?
nasal formulation for acute pain
what patients do you have to be careful giving Butophanol (stadol) to ?
CHF patients, it increases cardiac work
what is Buprenorphine (Buprenex) used for?
Reversal for fentanyl, used alone or in combination with naltrexone for opiate dependence, given sublingually
Kappa agonist/ partial agonist at the mu receptor--> psychomoromimetric effects such as weird thoughts, anxiety, hallucinations and nightmares
what happens if opiate antagonists are dosed without the patient being under the influence of opioids?
used to reverse narcotic induced respiratory depression, post-op narcotic reversal
orally active with longer duration of action
extended release morphine pellets that surround a core of a small dose of naltrexone to reduce potential for abuse
cough suppressant, no analgesic or addictive properties and minimal side effects, overdose and abuse issure, hydrocodone and codeine are also used to suppress cough
codeine analog for moderate pain, potent metabolite, duration of analgesia is 6 hours with a peak in 2 DO NOT GIVE WITH SSRIs
Can you give opiates in pregnancy?
parenteral administration of opioids within 2-4 hours of delivery may lead to transient respiratory depression of the neonate
Definition of physical dependence
anstinence syndrome induced by withdrawal of medication, does not independently cause addition
definition of addiction
fundamental features, loss of control, compulsive use, use despite harm, diagnosed by observation of aberrant drug related behavior
definition of tolerance
diminished drug effect from drug exposure, tolerance rarely "drives" dose escalation
definition of pseudo addiction
aberrant drug related behaviors driven by uncontrolled pain
what causes Neuropathic pain?
nerve damage or persistent stimulation may cause pain circuits to rewire themselves causing spontaneous stimulation, diabetes cancer and metabolic disturbances
what are symptoms of neuropathic pain
burning, tingling, shock like shooting pains, hyperalgesia, allodynia
Meds for neuropathic pain
gabapentin, pregabalin, carbamazepine, valproate, baclofen, amitriptyline, fluoxetine, sertraline, duloxetine (cymbalta)
Tier One for DM neuropathic pain
cymbalta, controlled release oxycodone, pregabalin, Amitriptyline
second tier for treatment of DM neuropathic pain
Carbamazepine, gabapentin, lamictal, ultram, effexor
Ca channel blockers and pain
Ziconotidine (Prialt) for intractable chronic neuropathic pain, dosed intrathecally
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