meds

• AD of NSAIDs/APAP


  • GI (low cox-1→inc gastric secretion, dec mucus production)
  • inc bleed risk
  • retention of water/na in kidneys→edema
  • lessens anti-HTN med effects
  • CV thrombotic event inc risk
  • inc leukotriene production (exacerbate asthma)
  • HA
  • tinnitus
  • dizzy
  • renal/hepatic toxicity
  • hypersensitivity
  • preg
• Acetaminophen (Tylenol) aka APAP


  Centrally acting analgesic and antipyretic with weak anti-inflammatory properties
• MOA of Acetaminophen


  Uncertain; possible inhibition of COX-3
• Clinical uses of Acetaminophen

  • HA
  • myalgia
  • dysmenorrhea
  • OA
  • RA
  • gout
  • combo w opioids allows lower opioid dosage
• Acetaminophen is safe in pregnancy
• Acetaminophen is a substitute for NSAIDs when analgesic/antipyretic effects are needed without risk of adverse effects associated with NSAIDs
• Acetaminophen is used in peds who cannot take aspirin
• AD of Acetaminophen includes good but hepatic necrosis
• Aspirin


  Irreversible inhib of COX-1 mediated TXA2 formation
• Clinical uses of Aspirin

  • Fever
• Ibuprofen (Advil, Motrin)


  Oral, IM; 2hr half life (dose 2-4x daily)
• Clinical uses of Ibuprofen

  • Fever
• Naproxen (Aleve)


  14hr half life (2x daily dose)
• Clinical uses of Naproxen

  • Fever
• Indomethacin (Indocin)


  Potent COX-1 inhib but lots of AD
• Clinical uses of Indomethacin

  • Mod/severe acute inflam not controlled by other NSAIDs
  • Used to accelerate closure of patent ductus arteriosus in premature infants
• Sulindac


  Renal sparing effect; mod doses alter renal prostaglandin production LESS than other NSAIDs
• Ketorolac


  Oral, parenteral, intranasal; limit to <5 days bc there's a hematologic toxicity/other AD
• Clinical uses of Ketorolac

  • Potent analgesic activity (comparable to morphine but less n/v, drowsy)
• Meloxicam


  More selective for COX-2 than most NSAIDs
• Diclofenac


  Oral, transdermal patch, topical
• Celecoxib (Celebrex)


  Selective COX-2 inhib; potent analgesic, antipyretic, and anti-inflammatory agent
• 1. acetylcysteine


  Used as an antidote for acetaminophen overdose
• Opioid Agonists


  Mediated by three G protein-coupled receptor families: m (mu), k (kappa), and d (delta)
• Analgesic properties of opioids are primarily mediated by m receptors
• k receptors also contribute to analgesia
• Opioids interact with opioid receptors on the membranes of certain cells in the CNS and other anatomic structures, such as the GI tract and urinary bladder
• Binding effects of opioids

  • Presynaptic neurons (decrease influx of Ca2+ and decreased release of excitatory neurotransmitters)
  • Postsynaptic neurons (increases in K+ efflux and decreased response to excitatory neurotransmitters)
• Morphine (MS Contin, Roxanol)


  Least lipophilic of opioids so very little crosses BBB; crosses placenta so NO preg
• Clinical uses of Morphine

  • Analgesia
  • Euphoria
  • Depression of cough reflex
  • Depressed Respiration
  • Miosis
  • Emesis
  • GI
  • CV
• AD of Morphine


  • Respiratory depression (fatal)
  • inc intracranial pressure (NO if head injury)
  • Hypotension
  • bradycardia
  • N/V
  • Constipation
  • Sedation
  • Pruritus
  • Addictive potential
  • Opioid-induced neurotoxicity
  • Allergy
• Codeine


  Can be used in lower conc than opium; only useful in mild/mod pain; antitussive at low doses
• Oxycodone (Oxycontin)


  2x morphine; used in combo w ASA/acetaminophen
• Hydrocodone


  Weaker analgesic than hydromorphone; used w acetaminophen/ibuprofen in mod/severe pain; use as antitussive
• Hydromorphone (Dilauded)


  Use over morphine in renal dysfunction
• Fentanyl


  Very lipophilic and has a rapid onset of action and shorter duration (10-30mins)
• Methadone


  Acts as agonist on m opioid receptors and as antagonist on NMDA receptor; inhib norepinephrine/serotonin reuptake
• Clinical uses of Methadone

  • Effective for nociceptive/neuropathic pain
  • Used in controlled withdrawal of opioids and heroin; used by experienced clinicians only due to long half-life
• Meperidine (Demerol)


  Acts as k agonist w some u agonist activity; also does anticholinergic effects (delirium incidence inc)
• Clinical uses of Meperidine

  • Acute pain so do not use for over 48hrs