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A comprehensive review of opioid receptors, their ligands, and the mechanisms of action of various drugs used in pain management. It covers topics such as opioid effects, overdose management, local anesthetics, and conditions affecting their toxicity. It also includes information on neuromuscular blockers and their side effects, making it a valuable resource for medical students and practitioners in anesthesiology. Useful for exam preparation and quick reference.
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Opioid receptors & their ligands? Where do opioids work? Mu --> endorphins delta --> enk kappa --> Dyn PNS & CNS (brain, spinal cord) what drugs work on each step of pain nociception? transduction - NSAIDs, LA, opioids, antihistamines, steroids transmission - LA modulation - nmda, ssri, snri, nxl opioids, alpha 2 agonists, ache inhibitors perception: alpha 2 agonists, GA, opioids
explain 1st, 2nd, 3rd order neurons in transmission. What spinal tract is transmission in? 1st: site --> dorsal horn 2nd: DH --> thalamus (cell body in DH) 3rd: thalamus --> cortex (cell body in thalamus) Spinothalamic Where is the most important site of modulation? Substantia gelatinosa in DH rex lam 2 & 3 Which 2 effects of opioids are NOT impacted by tolerance? Miosis & constipation MoA of opioids? -bind to g protein
*can do infusion which drugs release histamine? opioids: morphine, meperidine, codeine NMB: succs, atra, miva, (NOT PANC) barbs: thiopental (reflex tachy) which opioid increase sphincter of oddi pressure the least? meperidine which opioids have metabolites? How are opioid metabolites excreted? morphine, meperidine, TRAMADOL & maybe hydromorphone (CODEINE??) morphine - m6g, m3g *CI in renal pt, elderly mep - normep *can cause myoclonus, seizures
renally how are all opioids metabolized? liver which opioid contraindicated for nxl use? remi *has glycine in constitution, causes skeletal muscle weakness which opioids are likely to cause chest wall rigidity? tx? does chest wall rigidity increase icp? FRC? more potent ones (suf, alf, remi, fent) paralyze & intubate ↑ICP, ↓FRC how do opioids affect immune function? how do they affect SSEPs?
which opioid is the most ionized/least unionized at phys pH? mep list opioids by potency meperidine 100mg morphine 10mg hydromorphone 1.4mg (7x as strong) alfentanil 1000mcg fentanyl 100mcg remi 100mcg sufentanil 10mcg draw context sensitive half time graph of opioids list opioid antagonists Naloxone Naltrexone - can also use for alcohol abuse, long acting
Nalmefene - longer acting narcan Methylnaltrexone - doesnt cross cns, good for bowel obs list partial agonists drawbacks Buprenorphine - analgesia stronger than morphine butorphanol - analgesia stronger than morphine nalbuphine - good for heart disease a local anesthetic with a pka (further, closer) to physiological pH will have a faster onset. closer to. 3 components of local anesthetic molecule and what they determine?
**except w/ benzocaine Order pkas locals amides have lower pka *bupi, levobupi, ropi: 8. *lido, prilo: 7. *mepi: 7. esters higher *procaine 8. *chloro 8. *tetra 8. what is the highest pka of the amides? what is the highest pka of the esters?
max doses amides
levobupi, bupi, bupi + epi, ropi, lido, mepi etc levobupi 150mg (2mg/kg) bupi 175 (2.5) bupi + epi 200 (3) ropi 200 (3) lido 300 (4.5) mepi 400 (7) lido + epi 500 (7) prilo <70kg: 500/>70kg: 600 (8) max doses esters procaine 350-600mg (7mg/kg) chloroprocaine 800 (11) chloroprocaine + epi 1000 (14) Max dose of Exparel (liposomal bupi) Exparel rules: CI & when can give lido 266 mg *can give exparel 20min after lido inf
unless which drug is used? seizures **unless bupi is used: cardiac arrest Difficulty of cardiac resuscitation from LAST Bupi tox risk is increased in.. Bupivacaine > Levobupivacaine> Ropivacaine > Lidocaine pregnancy, dig, ccb, bb LAST >70kg lipid guidelines max recc dose? drugs to avoid? drug of choice arrythmia 100ml over 2-3min 250ml over 15-20min
12ml/kg epi (<1mcg/kg), vaso, ccb, bb, prop amio vascular uptake of locals by locations fastest to slowest IV Tracheal Intrapleural Intercostal Caudal Epidural Brachial plexus Femoral Sciatic Subq protein binding locals ranked Levo-bupivacaine = 98% Bupivacaine = 96%
bicarb hyaluronidase Hyaluronidase as an additive for block? Often used in ophthalmic blocks to lower risk of strabismus postop, shrink hematoma size, increase speed of onset, and improve quality of block, and mitigate rise of IOP. -has allergic potential Dose of cocaine 1.5mg/kg to 200mg max *available topically only Cocaine OD: how to manage SNS DO not give beta 1 specific blocker *best choice is vasodilator like ntg
*if must pick BB, pick nonselective like labetalol What is unique about benzocaine? Pka 3. *is IONIZED at phys pH, not unionized like other locals. *does not req charged part of molecule to exert action risk of methgb at high doses (>200-300mg) Max dose tumescent anesthesia? 55mg/kg mix of lido, epi, bicarb & NS What is EMLA 5%? What drug can be applied to hasten the onset of emla cream? How long does emla cream take to produce analgesia? Do infants & children have a higher risk of tox with emla cream? -2.5% lido, 2.5% prilo (2 amides)
-EMLA (contains prilo) -NTG -NTP -Phenytoin -Sulfonamides -inhaled nitric oxide Which local anesth reduces the effect of nxl opioids? chloroprocaine Methgb: tx, s/s, what is needed for accurate dx? -methylene blue 1-2mg/kg /5min *may need to redose *max 7-8mg/kg -exchange transfusion *in pt w/ glucose 6 phosphate reductase def s/s: tachycardia, mental status changes, slate grey pseudo cyanosis, choc colored blood, tachypnea, coma, dysrhythmias
accurate dx req co ox. What is Hgb pathology in methgb? what SpO2 expected with methgb? Ferrous state hgb --> ferric state "methheads ruin the ferris wheel" *unable to bind O2, ↓CaO2, acidosis, L shift, tissue hypoxia 85% *absorbs both wavelengths equally When is GETA preferred in tumescent anesthesia? -when >2-3L tumescent being used *otherwise MAC ok which LA is not used in nxl anesthesia? chloroprocaine **associated w/ neurotoxicity in subarachnoid blocks
