presentation opioids
TRANSCRIPT
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OPIOIDS AND ANALGESIA
Alberto Rivera Sanchez MD FAAPMR, ABPM, ABDAPain Management Sub SpecialistAmerican Board of Pain Medicine
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DISCLOSURES: I HAVE RECEIVED EDUCATIONAL GRANTS FROM SEVERAL IMPLANT COMPANIES BUT NONE HAVE FUNDED OR INFLUENCED THE CONTENT OF THIS EDUCATIONAL MATERIAL
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PHYSIOLOGIC & PHARMACOLOGIC EFFECTS
Nausea and VomitingSedation, sense of tranquility
ConstipationAnxiolysis, lethargyCough suppression
MiosisConstipation, pruritus, respiratory depression, delayed gastric emptying, sexual dysfunction,
muscle rigidity and myoclonus
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MECHANISM OF ACTIONPresynaptic inhibition of of substance P releaseIncrease K+ conductance (hyperpolarization)
Inactivation of calcium channels
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OPIOID RECEPTORS
Delta Receptors- its agonists produce analgesia on inflammatory mediated and malignant bone painAmoxapine, Ketamine, Norbuprenorphine
Kappa receptors- agonists are being developed to target inflammatory, visceral and chronic neuropathic pain Terpenoids in Cannabis Nalbuphine Pentazocine
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MU RECEPTORS
μ1,μ2,μ3 subtypesPresent in the Brain, Spinal Cord, Peripheral sensory neurons and GI tract
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OPIOID AGONISTSMorphine
HydromorphoneCodeineFentanylHeroin
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MORPHINE
Agonist for all 3 MOR, KOR and DORCan be administered orally (IR & ER)IV, IM, Epidural, IntrathecalApproved by FDA for use in IT PumpsDuration of action in orally administered is longer than IV
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HYDROMORPHONE1mg Hydromorphone = 5mg of MorphineIV, Rectal, SQ, Oral, Epidural, ITIV ½ life is 2.3 hrsHigh abuse potentialExcellent in cancer pain, fractures, burn unit, renal colicOral onset is 15 minutes
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FENTANYLIV, IT, Oral, Transdermal (most popular for administration)Patch onset of action is 17 hours Oral onset of action is 7 minutes60-134mg Morphine equivalent to 25mcg Fentanyl patch10 times more potent than hydromorphoneAction is mostly mu1 receptor
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TRAMADOL
Synthetic mu receptor agonistSerotonin-NE reuptake inhibitor1mg Morphine po = 10mg TramadolCardiac effects are rare: low BP, HBP, Inc. HR
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OXYCODONE15mg Morphine po = 10mg Oxycodone poAbsorption is increased by fatty meals and ibuprophenGabapentin potentiates its analgesic effectsHas a IR and CR presentationIR ½ life is 3.2 hrs, onset 10-30 minCR onset of action 46 min, duration 10-12 hrs (Clin Pharm 1996)
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ULTRA RAPID METABOLIZER
1-2% populationIncreased enzyme activity.
Increased formation of morphine following codeine administration, leading to higher risk of toxicity.Use Morphine or non opioids
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NON-NARCOTICS FOR PAINAnti-depressants
Gabapentin/PregabalinBDZs
Muscle relaxantsNSAID’s
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CHALLENGER IN THE HORIZONCannabis derived products with the correct
THC/CBD/terpenoid concentration