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NSAIDS

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  • 1. Good Morning INDIAN DENTAL ACADEMY Leader in continuing dental education www.indiandentalacademy.com www.indiandentalacademy.com
  • 2. www.indiandentalacademy.com
  • 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. 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. CLASSIFICATION (Acc. to Tripathi) A. Analgesic and antiinflammatory : Aspirin, Salicylamide, Benorylate, Diflunisal Salicylates Phenylbutazone, oxyphenbutazonePyrazolone derivatives Indomethacin, sulindacIndole derivatives Ibuprofen,Naproxen, Ketoprofen, Fenoprofen, Flurbiprofen. Propionic acid derivatives Mephenamic acidAnthranilic acid derivative Diclofenac, TolmetinAryl-acetic acid derivatives Piroxicam, Tenoxicam, Meloxicam.Oxicam derivatives Ketorolac.Pyrrolo-pyrrole derivative NImesulideSulfonanilide derivative NabumetoneAlkanones www.indiandentalacademy.com
  • 6. B. Analgesic but poor antiinflammatory: Paracetamol (Acetaminophen)Paraaminophenol derivative Metamizol (Dipyrone), propiphenazonePyrazolone derivatives Nefopam Benzoxazocine derivative Acc. to Goodman and Gillman A. Non selective Cox inhibitor Aspirin, sodium salicylate, choline magnesium trisalicylate, salsalate, diflunisal, salfasalazine, olsalazine. Salicylic acid derivatives AcetaminophenPara amino derivatives Indomethacin, sulindacIndole & indene acetic acid Tolmetin, diclofenac, ketorolac.Heteroaryl acetic acid www.indiandentalacademy.com
  • 7. Ibuprofen, naproxen, flurbiprofen, ketoprofen, fenoprofen, oxaproxin. Aryl propionic acid Mefenamic acid, meclofenamic acid Anthranilic acid (fenamates) Oxicams (piroxicam, Meloxicam) Enolic acid Nabumetone. Alkanones Rofecoxib Diaryl substituted furanones B. Selective cox-2 inhibitor Celecoxib Diaryl substituted Pyrazoles Etodolac Indole acetic acid Nimesulide Sulfonanilides www.indiandentalacademy.com
  • 8. MECHANISM OF ACTION Odontogenic pain Acute pain Noxious stimuli Tissue destruction or injury Cellular destruction Release / synthesis of histamine / prostaglandin / bradykinin Peripheral nociceptor / free nerve endings PAIN + Disease process + Surgical intervention www.indiandentalacademy.com
  • 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. COMMON PROPERTIES OF ALL NSAIDS Analgesia Antipyresis Anti- inflammatory Dysmenorrhoea Antiplatelet aggregatory Ductus arteriosus closure Parturition Gastric mucosal damage Renal effects Anaphylactoid reactions www.indiandentalacademy.com
  • 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 • Blood  2-5 g/day <2g/day  > 5g/day www.indiandentalacademy.com
  • 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. Adverse effects Salicylism : dizziness, tinnitus, vertigo, reversible impairment of hearing & vision, excitement & mental confusion, hyperventilation & electrolyte imbalance. Acute salicylate poisoning : fatal dose-15-30g , > 50 mg/dl.www.indiandentalacademy.com
  • 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 individualswww.indiandentalacademy.com
  • 15. Interactions :  Warfarin, naproxen, sulfonylureas, phenytoin and methotrexate.  Oral anticoagulants.  Uric acid  Probenecid  Methotrexate.  Furosemide and thiazides  Spironolactone.  Protein bound iodine levels. www.indiandentalacademy.com
  • 16. Uses : Analgesic Antipyretic Acute rheumatic fever (4-6 g) Rheumatoid arthritis (3-5 g) Osteoarthritis Postmyocardial infarction & poststroke patients Pregnancy induced hypertension and preeclampsia Delay labour Patent ductus arteriosus * Aspirin, dispirin, colosprinwww.indiandentalacademy.com
  • 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. Interactions :  Sulfonamides, tolbutamide, warfarin, imipramine & methotrexate  Anticoagulants  Phenytoin & tolbutamide Uses : Rheumatoid arthritis Ankylosing spondylitis Rheumatic fever Acute gout Severe cases Zolandin P  L  www.indiandentalacademy.com
  • 19.  Oxyphenbutazone  Metamizol (Dipyrone) : 0.5-1.5 g  Propiphenazone : 300-600 mg TDS INDOLE DERIVATIVES Indomethacin Pharmacokinetics  90% bound to plasma proteins.  Plasma t ½ = 2-5 hrs.  Dose 25-50mg BD/QID Sioril, phenabid Analgin, novalgin Saridon, anafebrin www.indiandentalacademy.com
  • 20. Adverse effects Interactions :  Furosemide  Thiazides, furosemide, β blockers, ACE inhibitors  Warfarin www.indiandentalacademy.com
  • 21. Uses : Rheumatoid arthritis Ankylosing spondylitis Psoriatic arthritis Acute gout Acu. Exa. destructive arthropathies Malignancy asso. fever Patent ductus arteriosus closure (0.1/0.2 mg/kg/12 hrly P  L  Indicin, indocap www.indiandentalacademy.com
  • 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 50 mg BD/QID Flurofen www.indiandentalacademy.com
  • 23. Adverse effects Interactions :  Anticoagulants  Furosemide, thiazides & β blockers www.indiandentalacademy.com
  • 24. Uses : Analgesic Antipyretic 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. Adverse effects Uses : Analgesic Osteoarthritis DysmenorrhoeaRheumatoid arthritis Medol, meftal, ponstan L  www.indiandentalacademy.com
  • 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. Uses : Ankylosing spondylitis Osteoarthritis Dysmenorrhoea Rheumatoid arthritis Bursitis Post-traumatic / post-op inflammatory condition Tolmetin : 400-600 mg TDS Voveran, diclonac, movonac www.indiandentalacademy.com
  • 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. Uses : Ankylosing spondylitis Osteoarthritis Dysmenorrhoea Rheumatoid arthritis Acute gout Musculoskeletal injuries Dentistry Episiotomy Tenoxicam : 20 mg OD Meloxicam : 7.5-15 mg/day (rheumatoid & osteo-arthritis) Dolonex, pirox, piricam, toldin P  L  Melflam, Meloxi www.indiandentalacademy.com
  • 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. Uses : Post-op / acute musculoskeletal pain (15-30 mg i.m. / 4-6 hrs Renal colic Bony metastasis Migraine SULFONANILIDE DERIVATIVE Nimesulide : Pharmacokinetics  99% bound to plasma proteins.  Plasma t ½ = 2-5 hrs  100 mg BD Ketorol, torolac www.indiandentalacademy.com
  • 32. Adverse effects Uses : Bursitis Sports injuries Dental surgery ENT disorders Low backacheDysmenorrhoea Post-op pain/osteoarthritis Nimulid, nimodolwww.indiandentalacademy.com
  • 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 9-12 yrs 300-600 mg www.indiandentalacademy.com
  • 34. Adverse effects Analgesic nephropathy Acute paracetamol poisoning  150 mg/kg  Fatality > 250 mg/kg  Early manifestations / 12-18 hrs / 2 dayswww.indiandentalacademy.com
  • 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 Musculoskeletal pain Dysmenorrhoea Antipyretic Crocin, metacin, paracinwww.indiandentalacademy.com
  • 36. BENZOXAZOCINE DERIVATIVE Nefopam 30-60 mg TDS oral 20 mg i.m. 6 hrly 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 Nefomax www.indiandentalacademy.com
  • 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. Analgesics after certain endodontic procedures www.indiandentalacademy.com
  • 39. PAIN MANAGEMENT STRATEGY 3D iagnosis efinitive Rx rugs Definitive treatment : •Pulpotomy, pulpectomy •Extraction •Incision & drainage Drug : •Pretreat with NSAIDs •Prescribe by clock •Long acting LA •Flexible prescription plan www.indiandentalacademy.com
  • 40. Flexible analgesic prescription plan Aspirin like drugs indicated Aspirin like drugs contra indicated Ibuprofen 200 mg Acetaminophen 600-1000mg NSAIDs (alone max.effective dose) OR NSAID + acetaminophen Acetaminophen 600-1000 mg + codine 60 mg Ibuprofen 400 mg/4 hrly and equivalent of acetaminophen 600 mg / codine 60 mg 4 hrly Acetaminophen 1000 mg with equivalent of oxycodone 10 mg NSAID (max. dose) & acetaminophen / oxycodone 10 mg combination Mild pain Moderate pain Severe pain www.indiandentalacademy.com
  • 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 Banned – September 2004 www.indiandentalacademy.com
  • 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. 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. CONCLUSION www.indiandentalacademy.com
  • 45. Thank you For more details please visit www.indiandentalacademy.com www.indiandentalacademy.com