GOOD MORNING

PRESENTED BY:NEHA KAPOORROLL NO. 324th batch

SEMINAR ON

ANALGESICS USED IN

DENTISTRY

CONTENTS

IntroductionClassificationNSAIDsReferences

INTRODUCTIONANALGESICS

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

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

CLASSIFICATION

Divided into 2 groups:1. Opioid Analgesics -

Narcotics/Morphine like analgesics

2. Non Opioid Analgesics -NSAIDs/Non narcotic/aspirin like analgesics

OPIOID ANALGESICS

Natural Opium alkaloids

- Morphine & Codeine.

Semi synthetic opiates - Diacetylmorphine- oxymorphone- Pholcodeine

Synthetic opioids- Pethidine- Fentanyl- Methadone- Dextropropoxyphene- Ethoheptazine- Tramadol

NON OPIOID ANALGESICS& NSAIDs

Analgesic and Anti inflammatory

A. NON-SELECTIVE COX INHIBITORS

1. Salicylates – Aspirin, Salicylamide, Benorylate, Diflunisal.

2. Pyrazolone derivatives – Phenyl butazone, Oxyphenyl-butazone.

3. Propionic acid derivatives – Ibuprofen, Naproxen, Ketoprofen, Fenoprofen, Flurbiprofen, Oxaprozin.

4. Indole derivatives – Indomethacin, Sulindac.5. Anthranilic acid derivative – Mephanimic

acid, Flufenamic acid.6. Aryl acetic acid derivative – Diclofenac,

Tolmetin..7. Oxicam derivative – Piroxicam, Tenoxicam.8. Pyrrolo pyrrole derivatives – Ketorolac,

Feprazone.

B. Prefential COX-2 inhibitors- Nimesulide- Meloxicam- Nabumetone

C. Selective COX-2 inhibitors- Valdecoxib- Celecoxib- Rofecoxib

D. Analgesics with poor Anti inflammatory action-

1. Paraminophenol derivative - Paracetamol (Acetaminophen)

2. Pyrazolone derivative- Metamizol, Propiphenazone

3. Benzoxazocine derivative- Nefopam

MECHANISM OF ACTION OF NSAIDS

Prostaglandins synthesis inhibitonMembrane phospholipids

Phospholipase A

Arachidonic acidCyclo oxygenase

PG G2 + PG H2

Isomerases Thromboxane sythetase

Prostacyclin synthetase

PG E2, PG D2, PG F TX A2

TX B2

PG I2PG E2, PG D2, PG F TX A2

ASPIRINAcetylsalicylic 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

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

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

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

Commercially available as:• Aspirin: 350 mg tab.

• Disprin: 350mg tab.• Colsprin: 100, 325,650mg tab.• Ecosprin: 75, 150, 325mg tab.

Dental consideration in a patient who is on aspirin therapy

BTCTPTINR

INDOMETHACIN

Indole derivativePotent inhibitor of PG synthesis & suppresses neutrophil motilityWell absorbed orally & t ½ is 2-5 hrsAdverse effects: Gastric irritation, nausea, anorexia, gastric bleeding & diarrhoea, frontal headache, dizziness, ataxia, mental confusion, depression, psychosis, leukopenia, rashes, increased risk of bleedingContraindicated in machinery operators, drivers, psychiatric patients, epileptics, kidney disease, pregnant women & childrenDose: 25-50mg BD-QIDCommercially available as-

Idicin, Indocap, Indoflam : 25mg, 75mg tab

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

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.

MEPHENAMIC ACID

Anthranilic acid derivative

Adverse effect: Diarrhoea, skin rashes, dizziness & other CNS manifestationOrally absorbed & t ½ is 2-4 hrs

Uses: Analgesic in muscle, joint & soft tissue pain, dysmenorrhoea, rheumatoid & osteoarthritisDose: 250-500 mg TDSCommercially available as:

Medol, Meftal - 250, 500 mg tab.

DICLOFENAC SODIUM

Aryl-acetic acid derivativeWell absorbed orallyPlasma t ½ - 2 hrs

Adverse effects: Epigastric pain, nausea, headache, dizziness, rashes

Uses: Rheumatoid arthritis, ankylosing spondylitis, dysmenorrhea, post traumatic & post inflammatory conditionsDose: 50mg TDS, then BD oral, 75mg deep i.mCommercially available as:

Voveran, Diclonac, Movonac : 50 mg tab. Diclomax : 25, 50 mg tab.

PIROXICAM

Oxicam derivativeLong acting potent NSAIDGood analgesic-antipyretic actionMetabolised in liver ; excreted in urine & bilePlasma t ½ is 2 daysSide effects : heart burn, nausea & anorexiaUse as short term analgesic & long term anti inflammatory drug – rheumatoid & osteo arthritis, ankylosing spondylitis, acute gout, musculoskeletal injuries,dysmenorrhoea etcDose: 20mg BD for 2 days followed by 20mg ODCommercially available as-

Dolonex, Pirox, Piricam : 10, 20 mg cap.

KETOROLAC

Pyrrolo-pyrrole derivativePotent analgesic & modest anti inflammatoryRapidly absorbed after oral & i.m administrationPlasma t ½ is 5-7 hrsAdverse effects: Nausea, abdominal pain, dyspepsia, ulceration, loose stools, drowsiness, headache, dizziness, nervousness, pruritis, pain & fluid retentionNot be given to patients on anticoagulants

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.

NIMESULIDE

Preferential COX-2 inhibitorsUsed 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 feverCompletely absorbed orally, excreted in urine, t ½ of 2-5 hrs

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 NSAIDsDose: 100 mg BDCommercially available as-

Nimulid, Nimegesic, Nise, Nobel, Nimodol : 100mg tab.

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 & dizzinessWell absorbed orally & t ½ of 17 hrsAvoided in presence of severe hepatic or renal diseaseDose: 12.5-25 mg ODCommercially available as-

Rofact, Rofegesic, Rofibax : 12.5, 25 mg tab.

PARACETAMOL

Para-amino phenol derivative

Actions: Good & promptly acting antipyreticWell absorbed orallyPlasma t ½ is 2-3 hrsSafe & well toleratedNausea & rashes occur occasionallyAnalgesic nephropathy- years of heavy ingestion

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.

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

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

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 )

TOPICAL NSAIDsTopical 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.

INDICATIONS OF NSAIDS IN DENTISTRY

Irreversible pulpitisApical periodontitisAcute alveolar abscessInfected cystSinusitisTMJ ArthritisMPDSAfter tooth extractionDry socketRecurrent apthous ulcersLichen planusAgranulocytosisCyclic neutropenia

GENERAL CONTRAINDICATIONSUlcerAsthmaPatient with nasal polypDiabetesGoutInfluenza (Reye’s syndrome)Hypo coagulation stateChronic allergic disordersChronic liver diseaseRenal failureSalicylate allergyBreast feeding mothersPregnancy

CONCLUSION

Nature of problem along with consideration of risk factors in an individual patient directs the initial selectionDrugs differ quantitatively in producing different side effectsLarge inter individual differences

REFERENCES

Essentials of Medical Pharmacology, K. D Tripathy, 5th editionPharmacology & Pharmacotherapeutics,

R. S. Satoskar,18th edition Textbook of oral medicine,

Burkett’s, 11th edition

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