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Pharm Ch 16

Analgesia

QuestionAnswer
Natural μ-agonist, first-pass M6G in liver Tx: Pain (cancer, trauma, burn, surgery, sickle cell crisis) ADRs: high abuse potential, epidural lasts longer Morphine
Natural μ-agonist, higher oral bioavailability Tx: Antitussive (cough-suppressive), antidiarrhea Metabolized by liver cytP450 Codeine (Methylmorphine)
Semisynthetic μ-agonist More effective analogues of codeine Often combined w/ acetaminophen Oxycodone Hydrocodone
Synthetic μ-agonist Tx: drug addiction, pain management, terminal cancer (long-lasting relief of chronic pain) Methadone
Synthetic μ-agonist, short-acting 100X more potent than morphine Lozenge for buccal transmuccosal admin (pediatric patients), transdermal patch (long-acting) Fentanyl, Alfentanil (more potent), Sufentanil (less potent)
Synthetic μ-agonist rapid metabolism and elimination, rapid offset requires admin of longer-acting drug to maintain analgesia postop Remifentanil
Synthetic μ-agonist ADRs: dysphoria, increased CNS excitability & seizures, causes mydriasis Meperidine
partial μ-agonist produces morphine-like anagesia, but without euphoria Butorphanol Buprenorphine
k-agonist, μ-antagonist ADRs: dysphoria Nalbuphine
Opioid Receptor Antagonists: Reverse opioid OD addiction (IV) Naloxone
Opioid Receptor Antagonists: Reverse opioid OD addiction (PO) Naltrexone
Opioid Receptor Antagonists: restricted to periphery, Tx: postop ileus, GI effects chronic opioids Alvimopan
Covalently acetylates COX-1 & COX-2, Tx: mild or moderate pain ADRs: GI irritation & erosion, hemorrhage, vomiting, renal ATN Aspirin (ASA)
Pyrrole acetic acid, PO, Tx: moderate to severe pain ADRs: anaphylaxis, renal failure, SJS, GI bleed Diclofenac
Pyrrole acetic acid, IV or PO Ketorolac
Propionic acid, Analgesia, Antipyretic, less ADRs vs ASA, ADRs: GI (dyspepsia, gastric bleeding) Ibuprofen
Propionic acid, more potent, longer half-life, ADRs: GI (dyspepsia, gastric bleeding) Naproxen
Benzothiazines Piroxicam
para-aminophenol, analgesic, antipyretic (only acts centrally) Tx: moderate pain, combined w/ others Acetaminophen (Tylenol)
Inhibits COX-2 only; given to patients who require NSAIDs and are at high risk of GI, renal bleeds Celecoxib
minimal abuse central-acting ADRs: nausea, dizziness, constipation Tramadol
least selective antidepressants; most effective in pain management Amitriptyline Nortriptyline Imipramine
SNRIs Desipramine Maprotiline
SSRIs, least effective in pain management Paroxetine Fluoxetine Citalopram
dual NE/5HT reuptake inhibitors used to treat neuropathic pain & fibromyalgia Venlafaxine Duloxetine
reduces chronic pain, ADRs: dizziness, somnolence, confusion, ataxia Oral bioavailability not predictable or linear Gabapentin
more potent, faster onset, more predictable bioavailability, less side effects than gabapentin Pregabalin
block Na+ channels Tx: neuropathy, stroke, MS, phantom limb ADRs: skin reactions Lamotrigine
block Na+ channels Tx: trigeminal neuralgia ADRs: aplastic anemia Carbamazepine Oxcarbazepine (less side effects)
antiarrhythmic, ADRs: paralysis of GI tract Mexiletine
use dependent Na+ channel blocker Tx: local anesthetic, skin pain, post-herpetic neuralgia, regional pain management (IV) Lidocaine
General category of Gabapentin, Pregabalin, Lamotrigine, Carbamazepine, Oxcarbazepine, Mexiletine, Lidocaine Anticonvulsants & Antiarrhythmics
anesthetic used to treat chronic pain, postop pain, acute severe pain such as in battlefield, ADR: psychomimetic Ketamine
antitussive, ADR: dizziness, fatigue, confusion, psychomimetic Dextromethorphan
MOA of ketamine & dextromethorphan NMDA Receptor Antagonists
α2-agonist, Tx: acute & chronic pain, ADR: postural hypotension Clonidine
diminish central sensitization, cause vasoconstriction, used to treat migraines; CI: CHD Sumatriptan, Zolmitriptan, Naratriptan, Rizatriptan
vasoconstrictor, replaced by triptans for migraines Ergotamine tartrate
MOA of "triptans" Serotonin 1B/1D receptor agonist
Created by: fmuralid
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