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Analgesics

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  • 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
  • 40.
    • THANK YOU
    THANK YOU

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