Non opiods Flashcards
Endorphins, enkephalins
provide a natural amount of pain relief
Norepinephrine, serotonin
play an inhibitory role in the descending tract, explains why antidepressants can be used for pain control
glutamate, GABA
several receptor provide many targets for combo therapy for pain control
Somatic pain
constant, well localized, aching, throbbing; analgesic, nerve block
Visceral pain
diffuse, deep, dull, cramping, squeezing, referred, analgesic, neurological procedures
neuropathic pain
altered sensations, stabbing, burned, constant or intermittent, sharp, shooting, antidepressant, anticonvulsants, neurological procedures, not opioids
types of chronic pain
pain that persists beyond expected healing time, related to chronic disease, w/out an identifiable cause, , chronic+acute associated with CA
Tolerance
reduced effect w/ same dose, need to increase dose to get same effect, not addiction
Pseudotolerance
a need to increase the dose, but only because of disease progression, new source of pain, drug interaction
Physical dependance
described as the occurence of withdrawal symptoms when the opioid is stopped all at once or without proper tapering
Addiction
a psychologically dependent state, they exhibit drug seeking behavior, compulsive use for their psychic effects
Pseudoaddiction
can present as addiction, but is a function of poorly controlled pain, once adequately controlled, their drug seeding tendencies disappear
Non-pharmacological approaches to pain pain control
remove source, psychotherapy, weight reduction, surgery, behavioral modification, rest/exercise, nerve block, massage therapy, acupuncture, hypnosis, heat, ice, pt
NSAIDs MOA
inhibition of the enzyme COX which prevents prostaglandin synthesis
Do NSAIDs produce tolerance
they do not tolerance, physical dependence, or psychological dependence
Ceiling effects of NSAIDs
analgesia has ceiling effect, less of ceiling effect to anti-inflammatory response, increased doses will still provide additional results
Popular NSAIDs
Diclofenac ER (Voltaren), Ibuprofen (Motrin, Advil), Naproxin (Naprosyn), Noproxen Sodium (Aleve, Anaprox), Meloxicam (Mobic), Indomethacin (Indocin), Ketorolac (Toradol)
Less popular NSAIDs
Etodolac (Lodine), Sulindac (Clinoril), Tometin (Tolectin), Oxaprozin (Daypro), Ketoprofen (Orudis), Piroxicam (Feldene), Nabumetone (Relafen)
NSAID characteristics that distinguish them from narcotics
antipyretic, anti-inflammatory, ceiling effect to analgesia, do NOT cause tolerance, do NOT cause physical or psychological dependence, potentcy, time of onset, duration of action
NSAID clinical uses
acute pain of skeletal muscle or dental pain, pain and inflammation associated with osteoarthritis and RA, chronic malignaant pain as an addititve affect to narcotic analgestics, pain related to bone metastases
ADRs of NSAIDs
Renal dysfunction (can be reversed), fluid retention, increase BP, avoid in CHF, GI are most concerning, bleeding risk
Ibuprofen (Motrin, Advil)
initial choice by many for acute pain due to cost and safety, available OTC, prescription and IV, safe in peds as suspension
IV ibuprofen
used for infants with patent ductus arteriosis, Caldolar is new product used for management of acute pain and fever
Ketorolac (Toradol)
First parenteral available in US, quick onset, use limited to
IV Ketorolac (Toradol)
considered by many to be equally efficacious to opiods for severe acute piain, due to GI adrs cannot get that level of relief with oral ketorolac, caution with post op
Naproxen (Aleve, Anaprox, Naprosyn)
BID dosing, OTC, PO, inc GI bleed?
Meloxicam (Mobic)
daily dosing, more selective for COX, better for long term, prescription only, $$
COX 2 inhibitors MOA
selectively inhibit COX2, no more efficacious, less GI irritation, less anti-platelt effects, all other ADRs similar to NSAIDs, well tolerated
2 drugs pulled from the market
Valdecoxib (Bextra), Rofecoxib (Vioxx) pulled for cardiovascular disease
Celecoxib (Celebrex)
the only one left, used for low cardio risk who require long term NSAIDs and at risk for GI toxicity, not for acute pain, not PRN
Acetaminophen
APAP, no one really knows for sure how it works, analgesic and antipyretic effects, no anti-inflammatory effects, max dose 3 grams, combo
APAP uses and ADRs
recommended as 1st line therapy for ostoeoarthritis, fever, mild pain, aches; hepatic necrosis at high doses for prolonged periods of time or with a toxic doses, decreases opioid requirements
Apap available as
tablets, caplet, liquid, suppository, and IV, safe in peds
APAP IV
Ofirmev, very controversial
APAP overdoses
caused by exhaustion of glutathione stores which function to neurtralize toxic metabolites for removal, monitor w/ APAP levels in relation to time of ingestion, can be a medical ER in most severe cases
Treatment of APAP overdose
fluids, gastric lavage, activated charcoal, acetylcysteine (Mucomyst) given IV to replenish glutathione, need to treat within 8 hours
APAP physical findings
usually asymptomatic for first 24 hours, then nausea, vomiting, jaundice, abd pain, renal injury, coagulopathy, hepatic encephalopathy, cerebral edema, hypotension
Acetylcysteine indications
meets criteria on the Rumack-Matthew nomogram, single ingestion of >150 mg, unknown time of ingestion and a serum aceta > 10 mcg, history of ingestion and any evidence of liver injury, Pt with delayed presentation have less success
Aspirin
oldest analgesics and prototype of non-opioids, not used for pain but antiplatelet
Aspirin mechanism
irreversibly inhibits COX which dec prostaglandin synthesis, inhibits COX prevents formation of thromboxane A2
ADRs of aspirin
gastric disturbances and bleeding, tinnitus, rhinitis, asthma, nasal polyps, edema, hypotension, shock, Reye’s syndrome
Aspirin clearance
contingent on urine pH, pH becomes more acidic, renal excretion increases because aspirin is in ionized form
Other non-opioid approaches to pain
muscle relaxants, bisphosphonates, steroids, Clonidine, ketamine
Conditions associated with neuropathic pain
diabetic neuropathies, post herpetic neuralgia, back pain, trigeminal neuralgia, HIV, CA, HA, spinal cord injury, phantom limb
General approach to neuropathic pain
initiate one drug at a time, use more favorable ADR profiles, start dosing low, slowly increase, always investigate alternative agents in setting of therapeutic failures, drugs have a longer onset
Antidepressant options
specifically focusing on agent that have activity with regards to norepinephrine and serotonin, TCAs, SSRIs, Duloxetine (Cymbalta)
Anticonvulsant options
Gabapentin (Neurontin) never used as anticonvulsant anymore, for chronic use, should titrate up, very sedating, Pregabalin (Lyrica), Carbamazepine, topiramate
Capsaicin Cream
substance P inhibitor, available OTC for chronic management, not PRN, not as monotherapy
Lidocaine options
patches-DOC for post herpetic neuralgia, apply x12 hours, then remove 12 hours, can be cut!, apply up to 3 patches, injections also but rare
Treatment of Fibromyalgia
antidepressants, cyclobenzaprine (Fleceril), Duloxetine (Cymbalta), venlafaxine (Effexor), Tramadol (Ultram), exercise, cognitive behavioral therapy
