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Pharm Ch 16
Analgesia
| Question | Answer |
|---|---|
| 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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