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Therapeutics In Dentistry


        Analgesics



          Iyad Abou-Rabii
          DDS, OMFS, Mres, PhD
misconceptions about the pain
1. The Dentist is the best judge of pain.
2. A person with pain will always have
obvious signs such as moaning, abnormal
vital signs, or not eating.
3. Pain is a normal part of aging.
4. Addiction is common when opioid
medications are prescribed.
misconceptions about the pain
5. Morphine and other strong pain
relievers should be reserved for the late
stages of dying.
6. Morphine and other opioids can easily
cause lethal respiratory depression.
7. Pain medication should be given only
after the resident develops pain.
8. Anxiety always makes pain worse.
Ceiling effect

• The term ceiling effect has two distinct meanings,
  referring to the level at which an independent
  variable no longer has an effect on a dependent
  variable,
• In case of Analgesics, a ceiling effect in treatment, is
  pain relief by some kinds of Analgesics drugs,
  which have no further effect on pain above a
  particular dosage level
Most Important Analgesics in
        Dentistry
Acetaminophen
Opoid non-opoid?
– Nonopioid analgesic generally used for
  mild to moderate pain.
Dose
– Adults: 0.5–1 g every 4–6 hours.
– 6–12 years, 250–500 mg every 4–6 hours.
– 1–5 years, 120–250 mg every 4–6 hours.
Acetaminophen
Indication
  – Acetaminophen appears to be a
    good analgesic for mild pain, but its
    relatively short-acting
    analgesia limits its usefulness as a
    monotherapy for the treatment
    of moderate to severe postoperative
    pain
Acetaminophen
Contarindication
  – Renal failure, papillary and tubular
    necrosis.
  – Asthma,
  – Liver failure
NSAIDs
• Examples
  – COX1 and COX-2 :
     Ibuprofen, ketorolac,
     flurbiprofen, ketoprofen, diclofenac,
     aspirin and
  – COX-2 :
     celecoxib ,rofecoxib, and Nimesulide
Nimesulide
     Indication
  – Acute pain
     Dose
  – 100 mg Twice a day
Contraindication
  – Renal failure, papillary and tubular
    necrosis.
  – Asthma,
  – Liver failure
Opioids
• Opioids act on the central nervous
  system
• Side effects
  – nausea, constipation, dizziness,
    sedation and respiratory depression
Opioids
• Although opioids as a class are
  effective analgesics, some
  commonly used formulations show
  poor analgesic efficacy for dental
  pain, and similar results can be
  achieved with other drugs with
  less severe side effects
Other Opioids
• Codeine alone has not been found as
  effective as other common analgesics
  for relief of post extraction pain.
• Oxycodone, hydrocodone and
  propoxyphene are about as effective as
  codeine, and dihydrocodeine,
Tramadol
• Tramadol is a synthetic, centrally
  acting analgesic indicated for moderate
  to moderately severe pain.
• Dose
  50 -100 mg then 50 -100 mg every 4-6 h
  (400 mg/day maximum)
Tramadol
• The serious side effects typically
  associated with opioids—such as
  dependence,sedation, respiratory
  depressionand constipation—occur less
  frequently with it.
• The side effects commonly seen with
  tramadol include
  nausea, dizziness, drowsiness and
What about Combination?
Why Combination
• Analgesic monotherapy has shown
  equivocal success in treating dental
  pain.
Why Combination
• The goal of combining analgesics with different
  mechanisms of action is to use lower doses of the
  component drugs.
• Increasing range of action by combining a fast-
  onset, short-acting analgesic (such as
  acetaminophen) for milder pain with a slower-
  onset, longer-duration analgesic (such as codeine
  or tramadol)
• Targeting different pain pathways simultaneously
Acetaminophen
          combinations
• Acetaminophen is an effective
  analgesic for mild pain, but to manage
  more severe pain it typically is
  combined with codeine or one of its
  derivatives.
Acetaminophen
          combinations
• Analgesic advantages for oral surgery
  are optimal with acetaminophen 1,000
  mg combined with codeine 60 mgor a
  codeine derivative such as oxycodone
  10 mg with acetaminophen 1,000.
Acetaminophen
          combinations
• a higher dose of hydrocodone, such as
  7.5 mg, combined with acetaminophen
  500 mg had slightly more analgesic
  efficacy than did codeine 30 mg plus
  acetaminophen 300 mg
• Both treatments resulted in analgesia
  that began 30 minutes after
  administration of the drug and
  continued for five hours
Acetaminophen
          combinations
• tramadol 150 mg alone has been shown
  to have better efficacy overall than the
  combination of propoxyphene 65 mg
  and acetaminophen 650 mg
• the combination of tramadol 75 mg
  with acetaminophen 650 mgprovided
  more effective, rapid and long-acting
  pain relief than did tramadol or
  acetaminophen alone
NSAID combinations
• Similar to acetaminophen, NSAIDs
  have a ceiling effect and
  therefore should be combined with
  other analgesics for total pain
  relief after major surgery.
• NSAIDs also allow for a
  significant dose reduction of opioids
  and hence can be useful in
  minimizing opioid side effects
NSAID combinations
• The combination of ibuprofen 400 mg
  and codeine 60 mg is superior to
  ibuprofen 400 mg alone
• Ibuprofen 400 mg and oxycodone 10
  mg provided a faster onset of relief
  from dental pain than did ibuprofen 400
  mg alone
NSAID combinations
• The combination of ibuprofen 400 mg
  with hydrocodone 15 mg was superior
  to the combination of acetaminophen
  600 mg with codeine 60 mg in
  providing analgesia after third-molar
  extraction
• Tramadol plus ibuprofen increased the
  efficacy of pain relief in patients with
  various types of dental pain
Reference
•   Bjorkman R, Hallman KM, Hedner J, Hedner T, Henning M. Acetaminophen
    blocks spinal hyperalgesia induced by NMDA and
•   Moore PA, Crout RJ, Jackson DL, Schneider LG, Graves RW, Bakos L.
    Tramadol hydrochloride: analgesic efficacy compared with codeine, aspirin with
    codeine, and placebo after dental extraction. J Clin Pharmacol 1998;38:554–60.[
•   Merskey H, Bogduk N. Classification of chronic pain: Descriptions of chronic
    pain syndromes and definitions of pain terms. 2nd ed. Seattle: IASP Press; 1994.

•   Niv D, Devor M. Transition from acute to chronic pain. In: Aronoff GM, ed.
    Evaluation and treatment of chronic pain. 3rd ed. Baltimore: Williams & Wilkins;
    1998:27–45.

•   Urquhart E. Analgesic agents and strategies in the dental pain model. J Dent
    1994;22:336–41.
•   Woolf CJ. Recent advances in the pathophysiology of acute pain. Br J Anaesth
    1989;63(2):139–46.
•   Dworkin RH. Which individuals with acute pain are most likely to develop a
    chronic pain syndrome? Pain Forum 1997;6:127–36.
    .
•   Mok MS, Lee CC, Perng JS. Analgesic effect of tramadol and diclofenac in
    combined use (abstract). Clin Pharmacol Ther 1996;59:132.

•   Broome IJ, Robb HM, Raj N, Girgis Y, Wardall GJ. The use of tramadol following
    day: case oral surgery. Anaesthesia 1999;54:289–92

•   Sunshine A. New clinical experience with tramadol. Drugs 1994;47(supplement
    1):8–18.

•   Szmyd L, Shannon IL, Mohnac AM. Control of postoperative sequelae in impacted
    third molar surgery. J Oral Ther Pharmacol 1965;1:491–6

•   Medve R, Wang J, Karim R. Tramadol and acetaminophen tablets for dental pain.
    Anesth Prog 2001;48(3):79–81
•   Cooper SA, Beaver WT. A model to evaluate mild analgesics in oral surgery
    outpatients. Clin Pharmacol Ther 1976;20:241–50.
•   Gardner GC, Simkin PA. Adverse effects of NSAIDs. Pharm Ther 2000;16:750–5.

•   Singh G, Ramey DR. NSAID-induced gastrointestinal complications: the ARAMIS
    perspective—1997. J Rheumatol 1998;51(supplement):8–16

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Therapeutics In Dentistry: Analgesics Ceiling Effects

  • 1. Therapeutics In Dentistry Analgesics Iyad Abou-Rabii DDS, OMFS, Mres, PhD
  • 2. misconceptions about the pain 1. The Dentist is the best judge of pain. 2. A person with pain will always have obvious signs such as moaning, abnormal vital signs, or not eating. 3. Pain is a normal part of aging. 4. Addiction is common when opioid medications are prescribed.
  • 3. misconceptions about the pain 5. Morphine and other strong pain relievers should be reserved for the late stages of dying. 6. Morphine and other opioids can easily cause lethal respiratory depression. 7. Pain medication should be given only after the resident develops pain. 8. Anxiety always makes pain worse.
  • 4. Ceiling effect • The term ceiling effect has two distinct meanings, referring to the level at which an independent variable no longer has an effect on a dependent variable, • In case of Analgesics, a ceiling effect in treatment, is pain relief by some kinds of Analgesics drugs, which have no further effect on pain above a particular dosage level
  • 6. Acetaminophen Opoid non-opoid? – Nonopioid analgesic generally used for mild to moderate pain. Dose – Adults: 0.5–1 g every 4–6 hours. – 6–12 years, 250–500 mg every 4–6 hours. – 1–5 years, 120–250 mg every 4–6 hours.
  • 7. Acetaminophen Indication – Acetaminophen appears to be a good analgesic for mild pain, but its relatively short-acting analgesia limits its usefulness as a monotherapy for the treatment of moderate to severe postoperative pain
  • 8. Acetaminophen Contarindication – Renal failure, papillary and tubular necrosis. – Asthma, – Liver failure
  • 9. NSAIDs • Examples – COX1 and COX-2 : Ibuprofen, ketorolac, flurbiprofen, ketoprofen, diclofenac, aspirin and – COX-2 : celecoxib ,rofecoxib, and Nimesulide
  • 10. Nimesulide Indication – Acute pain Dose – 100 mg Twice a day Contraindication – Renal failure, papillary and tubular necrosis. – Asthma, – Liver failure
  • 11. Opioids • Opioids act on the central nervous system • Side effects – nausea, constipation, dizziness, sedation and respiratory depression
  • 12. Opioids • Although opioids as a class are effective analgesics, some commonly used formulations show poor analgesic efficacy for dental pain, and similar results can be achieved with other drugs with less severe side effects
  • 13. Other Opioids • Codeine alone has not been found as effective as other common analgesics for relief of post extraction pain. • Oxycodone, hydrocodone and propoxyphene are about as effective as codeine, and dihydrocodeine,
  • 14. Tramadol • Tramadol is a synthetic, centrally acting analgesic indicated for moderate to moderately severe pain. • Dose 50 -100 mg then 50 -100 mg every 4-6 h (400 mg/day maximum)
  • 15. Tramadol • The serious side effects typically associated with opioids—such as dependence,sedation, respiratory depressionand constipation—occur less frequently with it. • The side effects commonly seen with tramadol include nausea, dizziness, drowsiness and
  • 16.
  • 18. Why Combination • Analgesic monotherapy has shown equivocal success in treating dental pain.
  • 19. Why Combination • The goal of combining analgesics with different mechanisms of action is to use lower doses of the component drugs. • Increasing range of action by combining a fast- onset, short-acting analgesic (such as acetaminophen) for milder pain with a slower- onset, longer-duration analgesic (such as codeine or tramadol) • Targeting different pain pathways simultaneously
  • 20. Acetaminophen combinations • Acetaminophen is an effective analgesic for mild pain, but to manage more severe pain it typically is combined with codeine or one of its derivatives.
  • 21. Acetaminophen combinations • Analgesic advantages for oral surgery are optimal with acetaminophen 1,000 mg combined with codeine 60 mgor a codeine derivative such as oxycodone 10 mg with acetaminophen 1,000.
  • 22. Acetaminophen combinations • a higher dose of hydrocodone, such as 7.5 mg, combined with acetaminophen 500 mg had slightly more analgesic efficacy than did codeine 30 mg plus acetaminophen 300 mg • Both treatments resulted in analgesia that began 30 minutes after administration of the drug and continued for five hours
  • 23. Acetaminophen combinations • tramadol 150 mg alone has been shown to have better efficacy overall than the combination of propoxyphene 65 mg and acetaminophen 650 mg • the combination of tramadol 75 mg with acetaminophen 650 mgprovided more effective, rapid and long-acting pain relief than did tramadol or acetaminophen alone
  • 24. NSAID combinations • Similar to acetaminophen, NSAIDs have a ceiling effect and therefore should be combined with other analgesics for total pain relief after major surgery. • NSAIDs also allow for a significant dose reduction of opioids and hence can be useful in minimizing opioid side effects
  • 25. NSAID combinations • The combination of ibuprofen 400 mg and codeine 60 mg is superior to ibuprofen 400 mg alone • Ibuprofen 400 mg and oxycodone 10 mg provided a faster onset of relief from dental pain than did ibuprofen 400 mg alone
  • 26. NSAID combinations • The combination of ibuprofen 400 mg with hydrocodone 15 mg was superior to the combination of acetaminophen 600 mg with codeine 60 mg in providing analgesia after third-molar extraction • Tramadol plus ibuprofen increased the efficacy of pain relief in patients with various types of dental pain
  • 27.
  • 28. Reference • Bjorkman R, Hallman KM, Hedner J, Hedner T, Henning M. Acetaminophen blocks spinal hyperalgesia induced by NMDA and • Moore PA, Crout RJ, Jackson DL, Schneider LG, Graves RW, Bakos L. Tramadol hydrochloride: analgesic efficacy compared with codeine, aspirin with codeine, and placebo after dental extraction. J Clin Pharmacol 1998;38:554–60.[ • Merskey H, Bogduk N. Classification of chronic pain: Descriptions of chronic pain syndromes and definitions of pain terms. 2nd ed. Seattle: IASP Press; 1994. • Niv D, Devor M. Transition from acute to chronic pain. In: Aronoff GM, ed. Evaluation and treatment of chronic pain. 3rd ed. Baltimore: Williams & Wilkins; 1998:27–45. • Urquhart E. Analgesic agents and strategies in the dental pain model. J Dent 1994;22:336–41. • Woolf CJ. Recent advances in the pathophysiology of acute pain. Br J Anaesth 1989;63(2):139–46. • Dworkin RH. Which individuals with acute pain are most likely to develop a chronic pain syndrome? Pain Forum 1997;6:127–36. .
  • 29. Mok MS, Lee CC, Perng JS. Analgesic effect of tramadol and diclofenac in combined use (abstract). Clin Pharmacol Ther 1996;59:132. • Broome IJ, Robb HM, Raj N, Girgis Y, Wardall GJ. The use of tramadol following day: case oral surgery. Anaesthesia 1999;54:289–92 • Sunshine A. New clinical experience with tramadol. Drugs 1994;47(supplement 1):8–18. • Szmyd L, Shannon IL, Mohnac AM. Control of postoperative sequelae in impacted third molar surgery. J Oral Ther Pharmacol 1965;1:491–6 • Medve R, Wang J, Karim R. Tramadol and acetaminophen tablets for dental pain. Anesth Prog 2001;48(3):79–81 • Cooper SA, Beaver WT. A model to evaluate mild analgesics in oral surgery outpatients. Clin Pharmacol Ther 1976;20:241–50. • Gardner GC, Simkin PA. Adverse effects of NSAIDs. Pharm Ther 2000;16:750–5. • Singh G, Ramey DR. NSAID-induced gastrointestinal complications: the ARAMIS perspective—1997. J Rheumatol 1998;51(supplement):8–16