The document provides information on analgesics used in dentistry, including classifications, mechanisms of action, uses, and side effects. It discusses both opioid analgesics like morphine and codeine as well as non-opioid analgesics/NSAIDs like aspirin, ibuprofen, indomethacin, piroxicam, and paracetamol. It notes that NSAIDs work by inhibiting prostaglandin synthesis and describes considerations for patients taking common analgesics like aspirin.

1. GOOD MORNING

2. Department Of Oral Medicine & Radiology PRESENTED BY: NEHA KAPOOR ROLL NO. 32 4th batch

3. SEMINAR ON ANALGESICS USED IN DENTISTRY

4. CONTENTS Introduction Classification NSAIDs References

5. INTRODUCTION ANALGESICS A drug that selectively relieves pain by acting in CNS or on peripheral pain mechanism, without significantly altering consciousness. ANAESTHESIA Anaesthesia means loss of sensation. Anaesthetic agent is one which bring about loss of all modalities of sensation, particularly pain, along with a reversible loss of consciousness. PAIN (ALGESIA) An unpleasant sensory and emotional experience associated with actual or potential tissue damage or described in terms of such damage. -IASP

6. OROFACIAL PAIN NOCICEPTIVE PAIN ( tissue injury and inflammation) Odontogenic conditions Eg. Pulpitis,apical periodontitis. Mucosal conditions Eg. Ulcers,lichen planus,herpes simplex Musculo skeletal conditions Eg. Myofacial pain,temporo mandibular joint capsulitis,arthritis. NEUROPATHIC PAIN ( primary lesion or dysfunction of nervous system) Classic cranial neuralgias Eg. Trigeminal and glossopharygeal Stomatodynia Phantom tooth pain Traumatic nerve injuries

7. CLASSIFICATION Divided into 2 groups: 1. Opioid Analgesics -Narcotics/Morphine like analgesics 2. Non Opioid Analgesics -NSAIDs/Non narcotic/aspirin like analgesics

8. OPIOID ANALGESICS Natural Opium alkaloids - Morphine & Codeine. Semi synthetic opiates Diacetylmorphine oxymorphone - Pholcodeine Synthetic opioids Pethidine Fentanyl Methadone Dextropropoxyphene Ethoheptazine Tramadol

9. NON OPIOID ANALGESICS & NSAIDs Analgesic and Anti inflammatory NON-SELECTIVE COX INHIBITORS Salicylates – Aspirin, Salicylamide, Benorylate, Diflunisal. Pyrazolone derivatives – Phenyl butazone, Oxyphenyl-butazone. Propionic acid derivatives – Ibuprofen, Naproxen, Ketoprofen, Fenoprofen, Flurbiprofen, Oxaprozin. Indole derivatives – Indomethacin, Sulindac. Anthranilic acid derivative – Mephanimic acid, Flufenamic acid. Aryl acetic acid derivative – Diclofenac, Tolmetin.. Oxicam derivative – Piroxicam, Tenoxicam. Pyrrolo pyrrole derivatives – Ketorolac, Feprazone.

10. B. Prefential COX-2 inhibitors - Nimesulide - Meloxicam - Nabumetone C. Selective COX-2 inhibitors - Valdecoxib - Celecoxib - Rofecoxib

11. D. Analgesics with poor Anti inflammatory action- Paraminophenol derivative - Paracetamol (Acetaminophen) Pyrazolone derivative - Metamizol, Propiphenazone Benzoxazocine derivative - Nefopam

12. MECHANISM OF ACTION OF NSAIDS Prostaglandins synthesis inhibiton Membrane phospholipids Phospholipase A Arachidonic acid Cyclo oxygenase PG G 2 + PG H 2 Isomerases Thromboxane sythetase Prostacyclin synthetase PG E 2 , PG D 2 , PG F TX A2 TX B 2 PG I 2 PG E 2 , PG D 2 , PG F TX A 2

13. ASPIRIN Acetylsalicylic acid Pharmacological actions Analgesic, antipyretic, antiinflammatory actions Metabolic effects: Blood sugar may decrease, plasma free fatty acid & cholesterol levels reduced Respiration: Hyperventilation in salicylate poisoning Acid base & electrolyte balance: Compensated respiratory alkalosis CVS: Vasodilation, increase in cardiac output GIT: Epigastric distress, nausea & vomiting Blood: Prolongs bleeding time

14. ADVERSE EFFECTS : Nausea, vomiting, epigastric distress, increased blood loss in stools Rashes, fixed drug eruptions, urticaria, rhinorrhea, angioedema, asthma, anaphylactoid reaction Salicylism – dizziness, tinnitus, vertigo, impairment of hearing & vision, excitement & mental confusion, hyperventilation & electrolyte imbalance Acute salicylate poisoning: Fatal dose in adults 15-30g, lower in children

15. USES : Analgesic Antipyretic Acute rheumatic fever Rheumatoid arthritis Osteoarthritis Postmyocardial infarction Patent Ductus Arteriosus Familial colonic polyposis Prevention of colon cancer Treatment of Bartter’s syndrome

16. Precautions & Contraindications : Peptic ulcer Bleeding tendencies Children with chicken pox or influenza Chronic liver disease Diabetics Pregnancy Breast feeding mothers G6 PD deficient individuals : Hemolysis Dose - 0.3-0.6 g 4-6 hrly orally

17. Commercially available as: Aspirin : 350 mg tab. Disprin: 350mg tab. Colsprin: 100, 325,650mg tab. Ecosprin: 75, 150, 325mg tab.

18. Dental consideration in a patient who is on aspirin therapy BT CT PT INR

19. INDOMETHACIN Indole derivative Potent inhibitor of PG synthesis & suppresses neutrophil motility Well absorbed orally & t ½ is 2-5 hrs Adverse effects: Gastric irritation, nausea, anorexia, gastric bleeding & diarrhoea, frontal headache, dizziness, ataxia, mental confusion, depression, psychosis, leukopenia, rashes, increased risk of bleeding Contraindicated in machinery operators, drivers, psychiatric patients, epileptics, kidney disease, pregnant women & children Dose: 25-50mg BD-QID Commercially available as- Idicin, Indocap, Indoflam : 25mg, 75mg tab

20. IBUPROFEN Propionic acid derivative Adverse effects: Gastric discomfort, nausea & vomiting Headache, dizziness, blurring of vision, tinnitus & depression Avoided in pregnancy, peptic ulcer patient & asthmatic patients

21. USES: Analgesic & Antipyretic Rheumatoid arthritis, osteoarthritis, musculoskeletal disorders Soft tissue injuries, fractures, vasectomy, tooth extraction Postpartum & postoperatively : suppress swelling & inflammation Dose: 400-800 mg TDS Comercially available as- Brufen, Emflam, Ibusynth : 200, 400, 600mg tab. Ibugesic : 100mg, 400 mg tab.

22. MEPHENAMIC ACID Anthranilic acid derivative Adverse effect: Diarrhoea, skin rashes, dizziness & other CNS manifestation Orally absorbed & t ½ is 2-4 hrs Uses: Analgesic in muscle, joint & soft tissue pain, dysmenorrhoea, rheumatoid & osteoarthritis Dose: 250-500 mg TDS Commercially available as: Medol, Meftal - 250, 500 mg tab.

23. DICLOFENAC SODIUM Aryl-acetic acid derivative Well absorbed orally Plasma t ½ - 2 hrs Adverse effects: Epigastric pain, nausea, headache, dizziness, rashes Uses: Rheumatoid arthritis, ankylosing spondylitis, dysmenorrhea, post traumatic & post inflammatory conditions Dose: 50mg TDS, then BD oral, 75mg deep i.m Commercially available as: Voveran, Diclonac, Movonac : 50 mg tab. Diclomax : 25, 50 mg tab.

24. PIROXICAM Oxicam derivative Long acting potent NSAID Good analgesic-antipyretic action Metabolised in liver ; excreted in urine & bile Plasma t ½ is 2 days Side effects : heart burn, nausea & anorexia Use as short term analgesic & long term anti inflammatory drug – rheumatoid & osteo arthritis, ankylosing spondylitis, acute gout, musculoskeletal injuries,dysmenorrhoea etc Dose: 20mg BD for 2 days followed by 20mg OD Commercially available as- Dolonex, Pirox, Piricam : 10, 20 mg cap.

25. KETOROLAC Pyrrolo-pyrrole derivative Potent analgesic & modest anti inflammatory Rapidly absorbed after oral & i.m administration Plasma t ½ is 5-7 hrs Adverse effects: Nausea, abdominal pain, dyspepsia, ulceration, loose stools, drowsiness, headache, dizziness, nervousness, pruritis, pain & fluid retention Not be given to patients on anticoagulants

26. USES: Postoperative & acute musculoskeletal pain: 15-30 mg i.m or i.v every 4-6 hrs Used for renal colic, migraine, pain due to bony metastasis Orally in a dose of 10-20 mg 6 hrly. Commercially available as – Ketorol, Zorovon, Ketanov, Torolac : 10mg tab.

27. NIMESULIDE Preferential COX-2 inhibitors Used for short lasting painful inflammatory conditions like sports injuries, sinusitis, ear nose throat disorders, dental surgery, bursitis, low backache, dysmenorrhoea, post operative pain, osteoarthritis & for fever Completely absorbed orally, excreted in urine, t ½ of 2-5 hrs

28. Adverse effects: - Epigastralgia, heart burn, nausea, loose motions, rash pruritus. - Hematuria & fulminant hepatic failure in few cases Useful in asthmatics, bronchospasm or intolerance to aspirin & other NSAIDs Dose: 100 mg BD Commercially available as- Nimulid, Nimegesic, Nise, Nobel, Nimodol : 100mg tab.

29. ROFECOXIB Selective COX-2 inhibitor. Effective in osteoarthritis, rheumatoid arthritis, dysmenorrhoea, dental, post operative & acute musculoskeletal pain at dose of 12.5-25 mg OD daily Side effects mild g.i complaints, headache & dizziness Well absorbed orally & t ½ of 17 hrs Avoided in presence of severe hepatic or renal disease Dose: 12.5-25 mg OD Commercially available as- Rofact, Rofegesic, Rofibax : 12.5, 25 mg tab.

30. PARACETAMOL Para-amino phenol derivative Actions: Good & promptly acting antipyretic Well absorbed orally Plasma t ½ is 2-3 hrs Safe & well tolerated Nausea & rashes occur occasionally Analgesic nephropathy- years of heavy ingestion

31. Acute paracetamol poisoning: - In small children with glucuronide conjugating ability Nausea, vomiting, abdominal pain, liver tenderness Centrilobular hepatic necrosis accompanied by renal tubular necrosis & hypoglycemia, may progress to coma Jaundice after 2 days Treatment: Vomiting induced, activated charcoal given, N-acetylcystein 150mg/kg infused iv over 20hrs, alternatively, 75mg/kg orally every 4-6 hrs for 2-3 days.

32. USES: First choice analgesic for osteoarthritis Best drug to be used as antipyretic Over the counter analgesic for headache, musculoskeletal pain, dysmenorrhoea, etc Much safer than aspirin Does not prolong bleeding time Used in all age groups, pregnant & lactating women, in other disease states & in patients in whom aspirin is contraindicated No significant drug interactions

33. DOSE: 0.5-1g TDS; infants 50mg; children 1-3 yrs 80-160mg 4-8 yrs 240-320mg 9-12 yrs 300-600mg Commercially available as- Crocin : 0.5, 1 gm tab. Ultragin, Pyrigesic, Calpol : 500mg. tab

34. SYNERGISTIC EFFECT When the action of one drug is facilitated or increased by the other, they are said to be synergistic. ADDITIVE SYNERGISM Combiflam : ibuprofen+ paracetamol (400 + 325mg) Dolokind plus : aceclofenac + paracetamol (100 +500 mg) Diclozee plus : diclofenac Na + acetoaminophen (50 + 500 mg) Diclomol : diclofenac Na + acetoaminophen (50 + 500 mg) Serazee plus : diclofenac K + seratiopeptidase (50 +10 mg) Ibugesic plus : ibuprofen+ paracetamol (400 + 325mg) Asonac-SR plus : aceclofenac + paracetamol + seratiopeptidase (100 + 500 + 15mg )

35. TOPICAL NSAIDs Topical formulations are available for application over painful joints and muscles. Osteoarthritis Sprains Sports injuries Backache Preparations Diclofenac 1% gel : voveron emulgel, diclonac gel. Ibuprofen 10% gel : ribufen gel. Ketoprofen 2.5% gel : rhofenid gel. Nimesulide 1% gel : nimulid trans gel. Piroxicam 0.5% gel : dolonex gel, minicam gel.

36. INDICATIONS OF NSAIDS IN DENTISTRY Irreversible pulpitis Apical periodontitis Acute alveolar abscess Infected cyst Sinusitis TMJ Arthritis MPDS After tooth extraction Dry socket Recurrent apthous ulcers Lichen planus Agranulocytosis Cyclic neutropenia

37. GENERAL CONTRAINDICATIONS Ulcer Asthma Patient with nasal polyp Diabetes Gout Influenza (Reye’s syndrome) Hypo coagulation state Chronic allergic disorders Chronic liver disease Renal failure Salicylate allergy Breast feeding mothers Pregnancy

38. CONCLUSION Nature of problem along with consideration of risk factors in an individual patient directs the initial selection Drugs differ quantitatively in producing different side effects Large inter individual differences

39. REFERENCES Essentials of Medical Pharmacology, K. D Tripathy, 5 th edition Pharmacology & Pharmacotherapeutics, R. S. Satoskar,18 th edition Textbook of oral medicine, Burkett’s, 11 th edition

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