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OPIOIDS AND ANALGESIA
Alberto Rivera Sanchez MD FAAPMR, ABPM, ABDAPain Management Sub SpecialistAmerican Board of Pain Medicine
DISCLOSURES: I HAVE RECEIVED EDUCATIONAL GRANTS FROM SEVERAL IMPLANT COMPANIES BUT NONE HAVE FUNDED OR INFLUENCED THE CONTENT OF THIS EDUCATIONAL MATERIAL
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
MECHANISM OF ACTIONPresynaptic inhibition of of substance P releaseIncrease K+ conductance (hyperpolarization)
Inactivation of calcium channels
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
MU RECEPTORS
μ1,μ2,μ3 subtypesPresent in the Brain, Spinal Cord, Peripheral sensory neurons and GI tract
OPIOID AGONISTSMorphine
HydromorphoneCodeineFentanylHeroin
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
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
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
TRAMADOL
Synthetic mu receptor agonistSerotonin-NE reuptake inhibitor1mg Morphine po = 10mg TramadolCardiac effects are rare: low BP, HBP, Inc. HR
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)
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
NON-NARCOTICS FOR PAINAnti-depressants
Gabapentin/PregabalinBDZs
Muscle relaxantsNSAID’s
CHALLENGER IN THE HORIZONCannabis derived products with the correct
THC/CBD/terpenoid concentration
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