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INDIAN DENTAL ACADEMY
Leader in continuing dental education
www.indiandentalacademy.com

Good
Morning
www.indiandentalacad...
www.indiandentalacademy.com
CONTENTS
 Introduction
 History
 Classification
 Mechanism of action
 Beneficial action and toxicities of PG synthesi...
HISTORY
Willow Bark – Centuries ago.
1875

– Sodium salicylate

1899

– Phenacetin + antipyrine

1899

– Acetyl salicylic ...
CLASSIFICATION
(Acc. to Tripathi)
A. Analgesic and antiinflammatory :
Salicylates

Aspirin, Salicylamide, Benorylate, Difl...
B. Analgesic but poor antiinflammatory:
Paraaminophenol derivative

Paracetamol (Acetaminophen)

Pyrazolone derivatives

M...
Aryl propionic acid

Ibuprofen, naproxen, flurbiprofen, ketoprofen,
fenoprofen, oxaproxin.

Anthranilic acid (fenamates)
E...
MECHANISM OF ACTION
Odontogenic pain
Noxious stimuli
Disease process
+
Surgical intervention

Acute pain
Tissue destructio...
Beneficial actions due to PG
Synthesis inhibition
• Analgesia
• Antipyresis
• Antiinflammatory
• Antithrombotic
• Closure ...
COMMON PROPERTIES OF ALL NSAIDS

Analgesia
Anaphylactoid
reactions

Antipyresis
Antiinflammatory

Renal effects

Dysmenorr...
SALICYLATES
Aspirin (prototype)
Pharmacological actions
• Analgesic (0.3-1.5 g/day)
• Antipyretic
• Antiinflammatory (3-6 ...
Pharmacokinetics
 80% bound to plasma proteins.
 Volume distribution 0.17 L/kg.
 Plasma t ½ = 15-20 min.
 Release sali...
Adverse effects

Salicylism : dizziness, tinnitus, vertigo, reversible impairment of
hearing & vision, excitement & mental...
Contraindications :
 Sensitivity, peptic ulcers, bleeding tendency, chicken pox
or influenza.
 Chronic liver disease
 D...
Interactions :
 Warfarin, naproxen, sulfonylureas,
phenytoin and methotrexate.
 Oral anticoagulants.
 Uric acid
 Probe...
Uses :

Patent ductus
arteriosus

Analgesic

Pregnancy induced
hypertension and
preeclampsia

Antipyretic

Acute rheumatic...
PYRAZOLONES
Phenylbutazone
Pharmacokinetics
 98% bound to plasma proteins.
 Plasma t ½ = 60 hrs.
 Dose 100-200 mg BD/TD...
Interactions :
 Sulfonamides, tolbutamide,
imipramine & methotrexate

warfarin,

 Anticoagulants
 Phenytoin & tolbutami...
Sioril, phenabid

 Oxyphenbutazone
 Metamizol (Dipyrone) : 0.5-1.5 g

Analgin, novalgin

 Propiphenazone : 300-600 mg T...
Adverse effects

Interactions :
 Furosemide
 Thiazides, furosemide, β
blockers, ACE inhibitors
 Warfarin

www.indianden...
Uses :

P L
Psoriatic
arthritis

Rheumatoid
arthritis
Ankylosing
spondylitis

Acute gout

Malignancy
asso. fever

Acu. E...
PROPIONIC ACID DERIVATIVES
Pharmacokinetics
 90-99% bound to plasma proteins.

Drug

Plasma t ½

Dosage

Ibuprofen

2 hr
...
Adverse effects

Interactions :
 Anticoagulants
 Furosemide, thiazides &
β blockers

www.indiandentalacademy.com
Uses :
Antipyretic
Analgesic
Dysmenorrhoea

ANTHRANILIC ACID DERIVATIVE (Fenamate)
Mephenamic acid
Pharmacokinetics
 High...
Adverse effects

L

Uses :

Osteoarthritis

Analgesic
Rheumatoid
arthritis

Dysmenorrhoea
www.indiandentalacademy.com
Med...
ARYL-ACETIC ACID DERIVATIVES
Diclofenac sodium :
Pharmacokinetics
 99% bound to plasma proteins.
 Plasma t ½ = 2 hrs
 5...
Uses :
Ankylosing
spondylitis

Osteoarthritis

Rheumatoid
arthritis

Bursitis

Dysmenorrhoea

Post-traumatic / post-op
inf...
OXICAM DERIVATIVES
Piroxicam
Pharmacokinetics
 99% bound to plasma proteins.
 Plasma t ½ = 2 days
 20 mg BD / 20 mg OD
...
Uses :

P L

Ankylosing
spondylitis

Osteoarthritis

Rheumatoid
arthritis

Dysmenorrhoea
Dentistry

Acute gout
Episiotom...
PYRROLO-PYRROLE DERIVATIVE
Ketorolac :
Pharmacokinetics
 Highly bound to plasma proteins.
 Plasma t ½ = 5-7 hrs
 10-20 ...
Uses :
Renal colic

Bony
metastasis

Migraine

Post-op / acute
musculoskeletal pain
(15-30 mg i.m. / 4-6 hrs

Ketorol, tor...
Adverse effects

Uses :
Sports injuries

Dental surgery

ENT disorders
Bursitis
Low backache

Dysmenorrhoea
Post-op
www.in...
PARA-AMINO PHENOL DERIVATIVES
•

Phenacetin 1887

•

Paracetamol (acetaminophen) 1950

Actions
Pharmacokinetics
 1/3 boun...
Adverse effects

Analgesic nephropathy
Acute paracetamol poisoning
 150 mg/kg
 Fatality > 250 mg/kg
 Early manifestatio...
 Mechanism of toxicity
 Treatment –
• Gastric lavage
• N-acetylcysteine 150 mg/kg / i.v./ 15 min / 20 hrs
• 75 mg/kg / o...
BENZOXAZOCINE DERIVATIVE
Nefopam
30-60 mg TDS oral
20 mg i.m. 6 hrly
Nefomax

CHOICE OF NSAIDS
• Mild to moderate pain – p...
• Exacerbation

of

rheumatoid

arthritis,

ankylosing

spondylitis, acute gout, acute rheumatic fever – aspirin,
indometh...
Analgesics after certain endodontic procedures

www.indiandentalacademy.com
PAIN MANAGEMENT STRATEGY

D

3

iagnosis
efinitive Rx
rugs

Definitive treatment :

Drug :

•Pulpotomy, pulpectomy

•Pretr...
Flexible analgesic prescription plan
Mild
pain

Aspirin like drugs
indicated
Ibuprofen 200 mg

Moderate
pain

NSAIDs (alon...
ADVANCES
Selective cox-2 inhibitors :
Celecoxib, rofecoxib, valdecoxib, etoricoxib, meloxicam,
diisopropyl flurophosphate...
Valdecoxib
Dose – 10-20 mg OD
Commercial name – Valed, Valus, Vorth, Bextra
Banned –7 April 2005.
Other drugs banned by FD...
REFERENCES :
1) Effectiveness of prophylactic use of refecoxib is comparison
with ibuprofen on postendodontic pain. JOE. J...
CONCLUSION

www.indiandentalacademy.com
Thank you
For more details please visit
www.indiandentalacademy.com

www.indiandentalacademy.com
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Nsai ds /certified fixed orthodontic courses by Indian dental academy

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The Indian Dental Academy is the Leader in continuing dental education , training dentists in all aspects of dentistry and offering a wide range of dental certified courses in different formats.

Indian dental academy provides dental crown & Bridge,rotary endodontics,fixed orthodontics,
Dental implants courses.for details pls visit www.indiandentalacademy.com ,or call
0091-9248678078

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Nsai ds /certified fixed orthodontic courses by Indian dental academy

  1. 1. INDIAN DENTAL ACADEMY Leader in continuing dental education www.indiandentalacademy.com Good Morning www.indiandentalacademy.com
  2. 2. www.indiandentalacademy.com
  3. 3. CONTENTS  Introduction  History  Classification  Mechanism of action  Beneficial action and toxicities of PG synthesis inhibition  Common properties of all NSAIDs  Drugs proper  Choice of analgesic after certain endodontic procedures  Pain management strategy  Flexible prescription plan  Advances  References  Conclusion www.indiandentalacademy.com
  4. 4. HISTORY Willow Bark – Centuries ago. 1875 – Sodium salicylate 1899 – Phenacetin + antipyrine 1899 – Acetyl salicylic acid 1949 – Phenyl butazone 1963 – Indomethacin 1963 – Propionic acid derivatives (NSAIDS) 1971 – Vane and coworkers observed that NSAIDS blocked PG synthesis. www.indiandentalacademy.com
  5. 5. CLASSIFICATION (Acc. to Tripathi) A. Analgesic and antiinflammatory : Salicylates Aspirin, Salicylamide, Benorylate, Diflunisal Pyrazolone derivatives Phenylbutazone, oxyphenbutazone Indole derivatives Indomethacin, sulindac Propionic acid derivatives Ibuprofen,Naproxen, Ketoprofen, Fenoprofen, Flurbiprofen. Anthranilic acid derivative Mephenamic acid Aryl-acetic acid derivatives Diclofenac, Tolmetin Oxicam derivatives Piroxicam, Tenoxicam, Meloxicam. Pyrrolo-pyrrole derivative Ketorolac. Sulfonanilide derivative NImesulide Alkanones www.indiandentalacademy.com Nabumetone
  6. 6. B. Analgesic but poor antiinflammatory: Paraaminophenol derivative Paracetamol (Acetaminophen) Pyrazolone derivatives Metamizol (Dipyrone), propiphenazone Benzoxazocine derivative Nefopam Acc. to Goodman and Gillman A. Non selective Cox inhibitor Salicylic acid derivatives Aspirin, sodium salicylate, choline magnesium trisalicylate, salsalate, diflunisal, salfasalazine, olsalazine. Para amino derivatives Acetaminophen Indole & indene acetic acid Indomethacin, sulindac Heteroaryl acetic acid Tolmetin, diclofenac, www.indiandentalacademy.com ketorolac.
  7. 7. Aryl propionic acid Ibuprofen, naproxen, flurbiprofen, ketoprofen, fenoprofen, oxaproxin. Anthranilic acid (fenamates) Enolic acid Mefenamic acid, meclofenamic acid Oxicams (piroxicam, Meloxicam) Alkanones Nabumetone. B. Selective cox-2 inhibitor Diaryl substituted furanones Diaryl substituted Pyrazoles Indole acetic acid Sulfonanilides Rofecoxib Celecoxib Etodolac Nimesulide www.indiandentalacademy.com
  8. 8. MECHANISM OF ACTION Odontogenic pain Noxious stimuli Disease process + Surgical intervention Acute pain Tissue destruction or injury Cellular destruction Release / synthesis of histamine / prostaglandin / bradykinin + Peripheral nociceptor / free nerve endings PAIN www.indiandentalacademy.com
  9. 9. Beneficial actions due to PG Synthesis inhibition • Analgesia • Antipyresis • Antiinflammatory • Antithrombotic • Closure of ductus arteriosus • • • • • Shared toxicities due to PG synthesis inhibition Gastric mucosal damage Bleeding Limitation of renal blood flow Delay / prolongation of labour Asthma & anaphylactoid reactions www.indiandentalacademy.com
  10. 10. COMMON PROPERTIES OF ALL NSAIDS Analgesia Anaphylactoid reactions Antipyresis Antiinflammatory Renal effects Dysmenorrhoea Gastric mucosal damage Parturition Ductus arteriosus closure www.indiandentalacademy.com Antiplatelet aggregatory
  11. 11. SALICYLATES Aspirin (prototype) Pharmacological actions • Analgesic (0.3-1.5 g/day) • Antipyretic • Antiinflammatory (3-6 g/day or 100mg/kg/day) • Metabolic effects • Respiration • Acid base and electrolyte balance • CVS • GIT • Urate excretion  <2g/day • Blood  2-5 g/day  > 5g/day www.indiandentalacademy.com
  12. 12. Pharmacokinetics  80% bound to plasma proteins.  Volume distribution 0.17 L/kg.  Plasma t ½ = 15-20 min.  Release salicylic acid (t ½) = 3-5 hrs.  Antiinflammatory doses (t ½) = 8-12 hrs. (30 hrs in poisoning) www.indiandentalacademy.com
  13. 13. Adverse effects Salicylism : dizziness, tinnitus, vertigo, reversible impairment of hearing & vision, excitement & mental confusion, hyperventilation & electrolyte imbalance. www.indiandentalacademy.com Acute salicylate poisoning : fatal dose-15-30g , > 50 mg/dl.
  14. 14. Contraindications :  Sensitivity, peptic ulcers, bleeding tendency, chicken pox or influenza.  Chronic liver disease  Diabetics, low cardiac reserve or frank CHF, juvenile rheumatoid arthritis. Precautions :  Stopped 1 week before elective surgery.  During pregnancy  Avoided by breast feeding mothers.  G-6-PD deficient individuals www.indiandentalacademy.com
  15. 15. Interactions :  Warfarin, naproxen, sulfonylureas, phenytoin and methotrexate.  Oral anticoagulants.  Uric acid  Probenecid  Methotrexate.  Furosemide and thiazides  Spironolactone. www.indiandentalacademy.com  Protein bound iodine levels.
  16. 16. Uses : Patent ductus arteriosus Analgesic Pregnancy induced hypertension and preeclampsia Antipyretic Acute rheumatic fever (4-6 g) Postmyocardial infarction & poststroke patients Delay labour Rheumatoid arthritis (3-5 g) Osteoarthritis www.indiandentalacademy.com * Aspirin, dispirin, colosprin
  17. 17. PYRAZOLONES Phenylbutazone Pharmacokinetics  98% bound to plasma proteins.  Plasma t ½ = 60 hrs.  Dose 100-200 mg BD/TDS Adverse effects  Bone marrow depression  Agranulocytosis  Stevens-Johnson syndrome www.indiandentalacademy.com
  18. 18. Interactions :  Sulfonamides, tolbutamide, imipramine & methotrexate warfarin,  Anticoagulants  Phenytoin & tolbutamide P L Uses : Rheumatic fever Severe cases Acute gout Ankylosing spondylitis Zolandin www.indiandentalacademy.com Rheumatoid arthritis
  19. 19. Sioril, phenabid  Oxyphenbutazone  Metamizol (Dipyrone) : 0.5-1.5 g Analgin, novalgin  Propiphenazone : 300-600 mg TDS Saridon, anafebrin INDOLE DERIVATIVES Indomethacin Pharmacokinetics  90% bound to plasma proteins.  Plasma t ½ = 2-5 hrs.  Dose 25-50mg BD/QID www.indiandentalacademy.com
  20. 20. Adverse effects Interactions :  Furosemide  Thiazides, furosemide, β blockers, ACE inhibitors  Warfarin www.indiandentalacademy.com
  21. 21. Uses : P L Psoriatic arthritis Rheumatoid arthritis Ankylosing spondylitis Acute gout Malignancy asso. fever Acu. Exa. destructive arthropathies Patent ductus arteriosus closure (0.1/0.2 mg/kg/12 hrly Indicin, indocap www.indiandentalacademy.com
  22. 22. PROPIONIC ACID DERIVATIVES Pharmacokinetics  90-99% bound to plasma proteins. Drug Plasma t ½ Dosage Ibuprofen 2 hr 400-800 mg TDS Brufen, emflam Naproxen 12-16 hr 250 mg BD/TDS Xenobid, naxid Ketoprofen 2-3 hr 100 mg BD/TDS Ketofen Fenoprofen 2-4 hr 300-600 mg TDS Arflur Flurbiprofen 4-6 hr www.indiandentalacademy.com 50 mg BD/QID Flurofen
  23. 23. Adverse effects Interactions :  Anticoagulants  Furosemide, thiazides & β blockers www.indiandentalacademy.com
  24. 24. Uses : Antipyretic Analgesic Dysmenorrhoea ANTHRANILIC ACID DERIVATIVE (Fenamate) Mephenamic acid Pharmacokinetics  Highly bound to plasma proteins.  Plasma t ½ = 2-4 hrs  250-500 mg TDS www.indiandentalacademy.com
  25. 25. Adverse effects L Uses : Osteoarthritis Analgesic Rheumatoid arthritis Dysmenorrhoea www.indiandentalacademy.com Medol, meftal, ponstan
  26. 26. ARYL-ACETIC ACID DERIVATIVES Diclofenac sodium : Pharmacokinetics  99% bound to plasma proteins.  Plasma t ½ = 2 hrs  50 mg TDS/BD, 75 mg i.m. Adverse effects www.indiandentalacademy.com
  27. 27. Uses : Ankylosing spondylitis Osteoarthritis Rheumatoid arthritis Bursitis Dysmenorrhoea Post-traumatic / post-op inflammatory condition Voveran, diclonac, movonac Tolmetin : 400-600 mg TDS www.indiandentalacademy.com
  28. 28. OXICAM DERIVATIVES Piroxicam Pharmacokinetics  99% bound to plasma proteins.  Plasma t ½ = 2 days  20 mg BD / 20 mg OD Adverse effects www.indiandentalacademy.com
  29. 29. Uses : P L Ankylosing spondylitis Osteoarthritis Rheumatoid arthritis Dysmenorrhoea Dentistry Acute gout Episiotomy Musculoskeletal injuries Dolonex, pirox, piricam, toldin Tenoxicam : 20 mg OD Meloxicam : 7.5-15 mg/day (rheumatoid & osteo-arthritis) www.indiandentalacademy.com Melflam, Meloxi
  30. 30. PYRROLO-PYRROLE DERIVATIVE Ketorolac : Pharmacokinetics  Highly bound to plasma proteins.  Plasma t ½ = 5-7 hrs  10-20 mg / 6 hrly (orally) Adverse effects www.indiandentalacademy.com
  31. 31. Uses : Renal colic Bony metastasis Migraine Post-op / acute musculoskeletal pain (15-30 mg i.m. / 4-6 hrs Ketorol, torolac SULFONANILIDE DERIVATIVE Nimesulide : Pharmacokinetics  99% bound to plasma proteins.  Plasma t ½ = 2-5 hrs  100 mg BD www.indiandentalacademy.com
  32. 32. Adverse effects Uses : Sports injuries Dental surgery ENT disorders Bursitis Low backache Dysmenorrhoea Post-op www.indiandentalacademy.com pain/osteoarthritis Nimulid, nimodol
  33. 33. PARA-AMINO PHENOL DERIVATIVES • Phenacetin 1887 • Paracetamol (acetaminophen) 1950 Actions Pharmacokinetics  1/3 bound to plasma proteins.  Plasma t ½ = 2-3 hrs  3-5 hrs (orally)  0.5-1g TDS  Infants - 50 mg  Children 1-3 yrs- 80-160 mg 4-8 yrs 240-320 mg www.indiandentalacademy.com 9-12 yrs 300-600 mg
  34. 34. Adverse effects Analgesic nephropathy Acute paracetamol poisoning  150 mg/kg  Fatality > 250 mg/kg  Early manifestations / 12-18 hrs / 2 days www.indiandentalacademy.com
  35. 35.  Mechanism of toxicity  Treatment – • Gastric lavage • N-acetylcysteine 150 mg/kg / i.v./ 15 min / 20 hrs • 75 mg/kg / orally / 4-6 hrs / 2-3 days Uses : ‘Over the counter’ analgesic Antipyretic Dysmenorrhoea Musculoskeletal pain Crocin, metacin, paracin www.indiandentalacademy.com
  36. 36. BENZOXAZOCINE DERIVATIVE Nefopam 30-60 mg TDS oral 20 mg i.m. 6 hrly Nefomax CHOICE OF NSAIDS • Mild to moderate pain – paracetamol, ibuprofen • Acute musculoskeletal, osteoarthritic, injury associated inflammation – ibuprofen, diclofenac, piroxicam • Post-op / acute / short lasting painful condition – ketorolac, nefopam www.indiandentalacademy.com
  37. 37. • Exacerbation of rheumatoid arthritis, ankylosing spondylitis, acute gout, acute rheumatic fever – aspirin, indomethacin, naproxen, piroxicam • Asthma or anaphylactoid reactions to aspirin – nimesulide www.indiandentalacademy.com
  38. 38. Analgesics after certain endodontic procedures www.indiandentalacademy.com
  39. 39. PAIN MANAGEMENT STRATEGY D 3 iagnosis efinitive Rx rugs Definitive treatment : Drug : •Pulpotomy, pulpectomy •Pretreat with NSAIDs •Extraction •Prescribe by clock •Incision & drainage •Long acting LA •Flexible prescription plan www.indiandentalacademy.com
  40. 40. Flexible analgesic prescription plan Mild pain Aspirin like drugs indicated Ibuprofen 200 mg Moderate pain NSAIDs (alone max.effective dose) OR NSAID + acetaminophen Aspirin like drugs contra indicated Acetaminophen 600-1000mg Acetaminophen 600-1000 mg + codine 60 mg Ibuprofen 400 mg/4 hrly and equivalent of acetaminophen 600 mg / codine 60 mg 4 hrly Severe pain NSAID (max. dose) & Acetaminophen 1000 mg with acetaminophen / oxycodone equivalent of oxycodone 10 www.indiandentalacademy.com 10 mg combination mg
  41. 41. ADVANCES Selective cox-2 inhibitors : Celecoxib, rofecoxib, valdecoxib, etoricoxib, meloxicam, diisopropyl flurophosphate. Action Celecoxib P© L© Use-osteoarthritis, rheumatoid arthritis Dose – 200 mg / day OD or 100 mg BD. Commercial names – Celebrex, Celib, Celfast, Celact etc. Banned – July 2001 Rofecoxib P© L© Dose – 12.5 mg OD (max. dose 25 mg) Commercial name – Vioxx, Dolib MD, Roff, Rofaday www.indiandentalacademy.com Banned – September 2004
  42. 42. Valdecoxib Dose – 10-20 mg OD Commercial name – Valed, Valus, Vorth, Bextra Banned –7 April 2005. Other drugs banned by FDA  Benoxaprofen  Phynylbutazone  Oxyphenbutazone  Saprofen  Piroxicam www.indiandentalacademy.com
  43. 43. REFERENCES : 1) Effectiveness of prophylactic use of refecoxib is comparison with ibuprofen on postendodontic pain. JOE. Jan 2003, Vol. 29, No. 1, pg. 62-64. 2) Evaluation of meloxicam (cox-2 inhibitor) for management of post operative endodontic pain – A double blind placebo controlled study. JOE, Oct 03, Vol. 29, No. 10, Pg. 634-637. 3) The efficacy of pain control following nonsurgical root canal treatment using ibuprofen in a combination of ibuprofen and acetaminophen in a randomized, double-blind, placebo controlled study. IEJ, 2004, Vol. 37, Pg. 531-541. www.indiandentalacademy.com
  44. 44. CONCLUSION www.indiandentalacademy.com
  45. 45. Thank you For more details please visit www.indiandentalacademy.com www.indiandentalacademy.com

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