Pain/Inflammation Meds

  1. Fxn of COX-1:
    "TGPS" (travel w/your GPS)
    • "Good COX"
    • T: Tissues: housekeeping
    • G: GI: protects GI mucosa
    • P: Platelets: promotes platelet aggregation
    • S: Supports Renal Fxn
  2. Fxn of COX-2:
    • "Bad COX"
    • T: Tissue: inflammation, pain
    • B: Brain: pain perception, fever
    • B: Blood Vessels: vasodilation
    • C: Kidney: supports renal fxn
    • C: Colon: causes colon cancer (CA)
  3. Aspirin [ASA]
    • COX-1 Inhibitor
    • use: RA/OA, ↓Pain, ↓Fever, prevent Clotting, prevent MI/CVA
    • ae: GI Bleeding, Bleeding, ↓Renal Fxn, Reye's Syndrome
    • intrxn: warfarin(↑anticoag.), glucocorticoid (↑GI ulcer), Alcohol (↑GI bleed), IbuProfen (↓antiplt), ACE/ARB (↓renal fxn)
  4. Celecoxib [Celebrex]
    • COX-2 Inhibitor
    • use: RA/OA, ↓Fever, prevent CA
    • ae: MI/CVA, GI Ulcer, Renal Impairment
    • intrxn: warfarin (↑anticoag), Sulfonamide Allergy
    • No cardiovascular Benefit.
    • No Risk of Bleeding (like cox-1).
    • Don't take with existing MI/CVA, ↓Renal Fxn, Diabetes.
  5. Acetaminophen [Tylenol]
    • COX Inhibitor
    • only works in CNS, not peripherally, so it only works for pain/fever
    • use: Analgesia, Antipyretic
    • ae: minimal, OD=Liver Injury
    • intrxn: Alcohol (↑liver injury), Warfarin (↑risk bleeding)
    • Cannot take with Liver Impairment.
    • Max Dose 4000 mg/day.
    • Antidote: Acetylcysteine [Mucomyst]
  6. Hydrocortisone and Prednisone
    • Glucocorticoids
    • Works with cortisol in the body to ↓immune response and ↓inflammation
    • use: prevent rejection of organ transplants, RA, asthma (hydrocortisone only)
    • ae: ↑Glucose, Fluid Retention, Risk for Infxn (↓immune response), ↓K+, Osteoporosis
    • intrxn: Aspirin (↑risk GI ulcer), K+wasting Diuretics (↑risk hypokalemia)
    • DO NOT GIVE if pt has a systemic fungal infxn.
    • Discontinue slowly.
    • GIVE DOSE IN AM (cortisol is highest in AM).
  7. Mu Receptor Activation:
    • M: Misosis: pupils contrict
    • U: Urinary Retention + ICP

    • A: Analgesia: pain relief
    • B: Breathing: respiratory depression
    • ---Blood Pressure: orthostatic hypotension
    • C: Constipation (+emesis, biliary colic)
    • ---Cough Suppression
    • D: Dependecy + Tolerance
    • E: Euphoria + Dysphoria
    • S: Sedation: drowsiness or clouding
  8. Kappa Receptor Activation:
    • G: GI: contipation
    • r: respiratory depression (little)
    • A: Analgesia
    • S: Sedation
  9. Morphine
    • Strong/Pure Opiod Analgesic
    • Activate Mu Receptors
    • Uses and A/E are relative to indication
    • use: Moderate to Severe Pain Relief (modifies pain perception, mimic endogenous opoid peptides)
    • intrxn: Alcohol (CNS depr), CNS Depressants, Anti-Cholinergic, Agon-Antag Opoid, Hypotensive, Opoid Antag, MAO Inhbitor, Benzodiazepines (↑sedation)
    • Onset of Respiratory Depression:
    • IV: 7 min
    • IM: 30 min
    • SubQ: 90 min
    • Need Baseline BP, Pulse, RR
    • Antidote: Nalaxone [Narcan]
  10. Pentazocine
    • Agonist-Antagonist Opoid
    • Activates Kappa Receptors, Blocks Mu Receptors
    • use: Mild to Moderate Pain Relief (less powerful analgesic effect)
    • ae: usually like Morphine, ↑Cardiac Work (don't take w/MI pain), mild dependence
    • intrxn: precipitates withdrawal from Pure Agonist
    • Low Abuse Potential, Less Respiratory Depression
    • Antidote: Nalaxone [Narcan]
  11. Nalaxone [Narcan]
    • Pure Opoid Antagonist
    • competitive antagonist at opoid receptors, blocks effects of opoid agonist
    • use: Reversal Agent/Antidote (blocks analgesia, euphoria, sedation, resp depr)
    • ae: Immediate Withdrawal (Abstinence Syndrome)
    • *Titrate*series of small dose to prevent withdrawal
  12. Diazepam [Valium]
    • Benzodiazepine
    • Enhances GABA at receptro sites to depress CBS (insomnia) or limbic system (anxiety)
    • use: choice for Insomnia and Anxiety (also seizure, muscle spasms, alcohol withdrawal, induce anesthesia)
    • ae: CNS Depression (drowsiness, unable to concentrate), Anterograde Amnesia
    • Some Dependence/Withdrawal (discontinue gradually).
    • Safer: ↓abuse, ↓tol/dep, ↓drug intrxn
  13. Zolpidem [Ambien]
    Zoleplon [Sonata]
    • Benzodiazepine-Like Drugs
    • agonist at Benzodiazepine receptors
    • use: Insomnia (not anxiety), SHORT TERM USE ONLY
    • ae: drowzy, dizzy, sleep-driving
    • Ambien: most widely used
    • Sonata: new drug, "Pyrazolopyrimidines"
    • Highly effective Hypnotics, Low Abuse Potential
  14. Flumazenil [Romazicon]
    • Competitive Benzodiazepine Receptor Antagonist
    • reverses sedative effects of benzo, but maybe not respiratory depression
    • use: Antidote for Benzo Overdose
    • ae: Convulsions (can produce the same effects you're trying to stop)
    • Effects begin Rapidly and All at Once
Card Set
Pain/Inflammation Meds