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analgesics and dentistry

This document provides an overview of analgesics, including opioids and NSAIDs. It discusses the classification, mechanisms of action, uses, and side effects of various opioid analgesics like morphine, codeine, fentanyl, tramadol, pethidine, and methadone. It also summarizes the classification of NSAIDs, how they work by inhibiting prostaglandin synthesis, and examples like aspirin. The document defines pain and the management of pain using topical, systemic and other analgesic medications.

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ANALGESICS
• Introduction • Opioid analgesics –Classification - Mechanism of action -Morphine -Other opioids -Uses • Prostaglandin synthesis & inhibition • NSAIDS - Classification - Mechanism of action -Aspirin -Other NSAIDS Contents
• Topical analgesics • Enzyme derived analgesics • NSAIDS as host modulating agent in periodontal disease • References
PAIN An unpleasant sensory & emotional experience associated with actual or potential tissue damage, or described in terms of such damage -IASP
Management of pain TOPICAL MEDICATIONS SYSTEMIC MEDICATIONS
Analgesic A drug that selectively relieves pain by acting in the CNS or on peripheral pain mechanisms, without significantly altering consciousness
Classesof analgesicdrugs • Opioid analgesics • Nonsteroidal anti-inflammatory drugs (NSAIDS) • Enzyme derived analgesics
OPIOIDS ANALGESICS • OPIUM: A dark brown, resinous material obtained from Papaver somniferum capsule • OPIOID: Drugs in a generic sense, natural or synthetic, with morphine- like actions
CLASSIFICATION OF OPIOIDS • NATURAL - Morphine - Codeine - Thebaine • SEMISYNTHETIC – Heroin – Oxymorphone – Hydromorphone • SYNTHETIC – Meperidine – Methadone – Fentanyl – Tramadol
OPIOIDRECEPTORS - MU – P hysical dependence – E uphoria – A nalgesia (supraspinal) – R espiratory depression - KAPPA – S edation – A nalgesia (spinal) – M iosis - DELTA • Analgesia (spinal & supraspinal) • Respirstory depression • Reduced GI motility
MECHANISMOF ACTION 1) Inhibit the transmission of nociceptive input from the periphery to the spinal cord 2) Activate descending inhibitory pathways that modulate transmission in the spinal cord 3) Alters limbic system activity
Action Of Morphine • Analgesia • Sedation • Euphoria • Mood change • Mental cloudiness MORHINE
MORPHINE ANALGESIA • Relieves all types of pain, but most effective against continuous dull aching pain • Sharp, stabbing, shooting pain also relieved by morphine • Sedation effect, but no loss of consciousness, drowsiness & without motor in-coordination • Morphine euphoria ,sense of well being (Drug abuse)
Analgesia • Strong analgesic- most effective in most kind of acute & chronic pain • Suppression of pain perception is selective ,without affecting other sensation or producing proportionate generalized CNS depression ( contrast GA _) Sedation • drowsiness • Higher doses causes sleep…coma • No anticonvulsant effects Mood & subjective effects • It has calming effect ,loss of apprehension ,feeling of detachment ,inability to concentrate • Pt in pain or anxiety & addict s specially perceive it pleasurable  euphoric effect 1) CNS EFFECTS OF MORPHINE
D) Respiratory Centre • Depresses in dose dependent manner • Rate & tidal volume both decreases • Death in poisoning due to respiratory failure E) Cough centre • depressed F) Temperature regulatory centre • Depressed ,hypothermia in cold surrounding
Morphine stimulates CTZ • Nausea ,vomiting …specia lly if stomach is full Edinger westpal nucleus • Edinger westpal nucleus of third nerve stimulated to produce miosis • Pin point pupil – diagnostic vagal centre • Stimulat ed  causes bradicar dia
• CVS Causes Vasodilatation due to - Decreasing tone of blood vessels - Histamine release • GIT - Constipation • NEUROENDOCRINE EFFECTS - Hypothalmic influence on pituitary is reduced - Decreases levels of LH, FSH, ACTH whereas PROLACTIN & GH levels are increased
Effects on smooth muscles • BILIARY TRACT Marked increase in the pressure in the biliary tract • URINARY BLADDER Have urinary retention difficulty in micturation • BRONCHIAL MUSCLE Bronchoconstriction can result. (Asthmatics)
Pharmacokinetics • Oral absorption-Unreliable (High First pass Metabolism) • Primarily metabolised in liver • Freely crosses the placenta & can effect the foetus
Adverse effects • Side effects • Idiosyncrasy and allergy • Apnoea • Acute morhine poisoning ( LD- 250mg ) • Tolerance and dependence
Therapeutic uses of morphine • As Analgesic (Severe Pain) • Preanesthetic medications • Relief of anxiety & apprehension • Acute pulmonary edema • Diarrhoea • Cough • Obstetrical analgesia • DOSE: 10-15 mg i.m/ s.c MORPHINE SULPHATE 10, 15 mg inj
Contraindications • Bronchial Asthma • Infants & Elderly • Head Injury • Undiagnosed Acute Abdominal pain. • Respiratory diseases (Emphysema, COPD)
CODEINE • One tenth the potency (analgesic) of morphine • More selective COUGH SUPPRESSANT • Good activity by oral route • Abuse Liability is low AVAILABLE : COREX , COMTUS syp. (10 mg / 5 ml)
FENTANYL • 80 to 100 times more potent than morphine • Rapidly Onset of action (5 min) • Used exclusively in Anaesthesia alone as well in combination with Droperidol • Transdermal fentanyl, is used in the management of persistent chronic pain DOSE: 100-200 µg i.v (FENT, FENDROP 50µg/ml)
TRAMADOL • Recently introduced Centrally Acting Analgesic • Has dual Norepinephrine & Serotonin reuptake inhibitory effects • 10 times potent than morphine & produces less adverse effects • Used to treat osteoarthritis, low back pain, diabetic neuropathy & cancer pain DOSE: 50-100 mg oral/ i.v. 4-6 hrly (CONTRAMAL, DOMADOL)
PETHIDINE (MEPERIDINE) • Equal analgesic efficacy to morphine & some properties like Atropine • Unlike morphine: - More respiratory depression - Less histamine release (Safer in ASTHMATICS) - Less constipation • Used primarily ANALGESIC (substitute of morphine) • DOSE : 50-100 mg i.m, s.c/ orally (PETHIDINE HCL 100mg/ 2ml inj.;50-100mg Tab
• Synthetic opioid with pharmacological activity & potency same as morphine • Long duration of activity( PPB >90%) • Powerful pain reliever • Used as SUBSTITUTION Therapy of opioid dependence DOSE: 10 mg inj. PHYSEPTONE METHADONE
PENTAZOCINE • Mixed opioid agonist-antagonist action • Efficacy lower than morphine • Useful in Mild-Moderate pain conditions • Causes Tachycardia & rise in BP (C/I- MI) • Should not be used in opioid dependent subjects DOSE: 50-100 mg oral , 30-60 mg i.m /s.c (FORTWIN, FORTSTAR)
Strategies to minimize opioid side effects • Slow titration of doses • Changing the dosing regimen or route of administration • Using a Nonopioid Or Adjuvant Analgesic for an opioid sparing effect • Adding a drug to counteract the side effect • Constipation prophylaxis
Pure opioid antagonist Naloxone • Competitive antagonist of all type of opioid receptors • No physical or psychological dependence • 0.4 -0.8 mg : all action of morphine • 4-10 mg : action of nalorphine & pentazocine • Blocks action of endogenous opioid peptides • Inactive orally , • i.v. : 2-3 mins Uses • Morphine poisoning , Neonatal asphyxia
Endogenous opioid peptide • There are 3 distinct families of opioid peptides, derived from specific polypeptide 1. Endorphins : • β-END having 31 amino acids, derived from POMC ( Pro-opio-melanocortin) • Primarily μ agonist but also has δ action
2. Enkephalins: • met-ENK and leu-ENK are the most important • Both are Pentapeptides • met-ENK has equal affinity for μ and δ, leu-ENK prefers δ receptors 3. Dynorphins: • DYN-A and DYN-B are 8-17 amino acid peptide • Are more potent on κ receptors
Prostaglandin synthesis and inhibition Cell membrane phospholipids Phospholipase A2 Arachidonic acid Cyclooxygenase (COX-1; COX-2) Endoperoxide (PGG, PGH) TXAPGI PGE PGF NSAIDs Steroid’s
NON-STEROIDAL ANTI-INFLAMMATORY DRUGS (NSAIDS)
- Analgesic, Antipyretic & Anti-inflammatory actions. - Act primarily on Peripheral Pain Receptors & CNS to raise the pain threshold - Compared to Morphine - Weaker analgesics - Do not depress CNS - Do not produce physical dependence & have no abuse liability INTRODUCTION
CLASSIFICATION A) NONSELECTIVE COX INHIBITORS (CONVENTIONAL NSAIDS) 1. Salicylates: Aspirin, Diflunisal 2. Pyrazolone derivatives: Phenylbutazone, Oxyphenbutazone 3. Indole derivatives: Indomethacin, Sulindac 4. Propionic acid derivatives: Ibuprofen, Naproxen, Ketoprofen
5.Anthranilic acid derivative: Mephenamic acid 6.Aryl-acetic acid derivatives: Diclofenac, Tolmetin 7.Oxicam derivatives: Piroxicam, Tenoxicam 8. Pyrrolo-pyrrole derivative: Ketorolac B) PREFERENTIAL COX-2 INHIBITORS – Nimesulide, Meloxicam, Nabumetone C) SELECTIVE COX-2 INHIBITORS - Celecoxib
@drashishagg D) ANALGESIC-ANTIPYRETICS WITH POOR ANTI-INFLAMMATORY ACTION - 1. Paraaminophenol derivative: Paracetamol (Acetaminophen) 2. Pyrazolone derivatives: Metamizol, Propiphenazone 3. Benzoxazocine derivatives: Nefopam
- Act as Non-selective Inhibitors of the enzyme cyclooxygenase, inhibiting both, COX-1 & COX-2 isoenzymes - Cyclooxygenase catalyses the formation of PGs & TBX 2 from arachidonic acid Mechanism of action
COX-1 - Present as part of everyday physiological function. - Protects the stomach by limiting acid secretion - Helps platelets limit bleeding by increasing their adhesiveness COX-2 - Its expression is induced by various stimuli such as the inflammation or at the site of the injury
Pharmcological actions ANALGESIA ANTIPYRESIS ANTI-INFLAMMATORY
GASTRIC MUCOSAL DAMAGE ANTIPLATELET AGGREGATION DUCTUS ARTERIOSUS CLOSURE
PARTURITION AND IN DYSMENORRHOEA RENAL EFFECTS ANAPHYLACTIC REACTIONS
@drashishagg ASPIRIN • Analgesic, Antipyretic & Anti-inflammatory Effects. • RESPIRATORY SYSTEM -Increases rate & depth. • GIT - Irritates the gastric mucosa  causes epigastric distress, nausea & vomiting - Promotes the local back diffusion of the acid  acute ulcers, erosive gastritis, microscopic haemorrhages SALICYLATES
@drashishagg • CVS - No direct effect - Larger doses increase cardiac output to meet increased peripheral O2 demand caused by direct vasodilation • BLOOD - Inhibits TXA2 synthesis by platelets - Interferes with Platelet aggregation (BT) • METABOLIC EFFECTS - Increased utilization of Glucose, blood sugar may decrease specially in diabetics
@drashishagg Pharmacokinetics - Poor Absorption- Stomach & Small Intestine - Metabolism- Gut wall, Liver, Plasma & other tissues to release salicylic acid. Excretion- Urine Adverse effects - Nausea,Vomiting, Epigastric distress & occult blood in stools, rashes, urticaria, asthma, angioedema - Anti-inflammatory doses – syndrome Salicylism – dizziness, tinitus, reversible impairment of hearing & vision, excitement
use analgesic antipyretic Acute rheumatic fever Rheumatoid arthritis Osteoarthri tis Post MI & post stroke patients pregnancy induced hypertension & preeclampsia to delay labour patent ductus arteriosus DOSE: 300-900 mg every 4 hrs (Max 3.6 gm) ( ASA, ASCAD, ECOSPRIN 50mg,75mg Tab.)
@drashishagg PHENYLBUTAZONE - Potent anti-inflammatory drug. - Poor analgesic & antipyretic activity Adverse effects: - More toxic than Aspirin - Bone marrow depression, Agranulocytosis - Banned in some countries DOSE: 100-200 mg BD or TDS after meals (ZOLANDIN 100,200 mg Tab) PYRAZOLONE DERIVATIVES
@drashishagg INDOMETHACIN - Potent anti-inflammatory, antipyretic & good analgesic - Analgesic action better than PBZ Adverse effects: - High incidence of GI & CNS side effects - C/I in drivers, epileptics, pregnancy & children Uses: - Rheumatoid Arthritis not controlled by aspirin - Acts rapidly in Acute Gout DOSE: 25-50 mg BD /TDS (INDOCAP, IDICIN) INDOLE DERIVATIVES
IBUPROFEN - Analgesic, Antipyretic & Anti-inflammatory activity is lower than aspirin - Inhibit platelet aggregation & prolong bleeding time Adverse effects: - Better tolerated than aspirin (Incidence is lower) - Gastric discomfort, nausea & vomiting are most  common side effects - Headache, dizziness, blurring of vision, tinnitus PROPIONIC ACID DERIVATIVES
Pharmacokinetics:  - Absorbed orally, highly bound to plasma proteins  (90-99%)  - Metabolized in liver & excreted in urine & bile - Enter brain, synovial fluid & cross placenta Interactions: - As they inhibit platelet function, use with  anticoagulants should be avoided  - Likely to decrease diuretic & antihypertensive action  of thiazides, furosemide and -blockers
- As Analgesic & Antipyretic - In Rheumatoid Arthritis, Osteoarthritis & other Musculoskeletal Disorders, specially where pain is more prominent than inflammation - Indicated in soft tissue injuries, fractures, tooth extraction, supppress swelling & inflammation DOSE: 400-800 mg TDS (BRUFEN, EMFLAM, IBUGESIC 200, 400, 600 mg Tab) Uses
MEPHENAMIC ACID - An Analgesic, Antipyretic & Anti-inflammatory drug, - Exerts Peripheral as well as Central Analgesic Action Adverse effects : - Diarrhoea - Epigastric distress is complained, but gut bleeding is  not significant ANTHRANILIC ACID DERIVATIVE
@drashishagg Pharmacokinetics: - Oral absorption is slow but almost complete - Partly metabolized & excreted in urine & in bile Uses:  - Analgesic in muscle, joint & soft tissue pain where  strong anti-inflammatory action is not needed (MPDS) - Useful in rheumatoid & osteoarthritis DOSE: 250-500 mg TDS (MEFTAL, PONSTAN, MEDOL 250, 500 mg cap)
• Introduction • Opioid analgesics –Classification - Mechanism of action -Morphine -Other opioids -Uses • Prostaglandin synthesis & inhibition • NSAIDS - Classification - Mechanism of action -Aspirin -Other NSAIDS Contents
CLASSIFICATION A) NONSELECTIVE COX INHIBITORS (CONVENTIONAL NSAIDS) 1. Salicylates: Aspirin, Diflunisal 2. Pyrazolone derivatives: Phenylbutazone, Oxyphenbutazone 3. Indole derivatives: Indomethacin, Sulindac 4. Propionic acid derivatives: Ibuprofen, Naproxen, Ketoprofen
5.Anthranilic acid derivative: Mephenamic acid 6.Aryl-acetic acid derivatives: Diclofenac, Tolmetin 7.Oxicam derivatives: Piroxicam, Tenoxicam 8. Pyrrolo-pyrrole derivative: Ketorolac B) PREFERENTIAL COX-2 INHIBITORS – Nimesulide, Meloxicam, Nabumetone C) SELECTIVE COX-2 INHIBITORS - Celecoxib
@drashishagg DICLOFENAC SODIUM - Analgesic, Antipyretic, Anti-inflammatory action - Inhibits PG synthesis & has short lasting antiplatelet  action  Pharmacokinetics: - Well absorbed orally, metabolized & excreted both  in urine & bile - Has good tissue penetrability & conc. in synovial  fluid is maintained longer period, exerting extended  therapeutic action in joints ARYL-ACETICACID DERIVATIVE
@drashishagg Adverse effects - Are generally mild: Epigastric pain, nausea, headache, dizziness, rashes - Gastric ulceration & bleeding -less common Uses: - Most extensively used NSAID - Rheumatoid & Osteoarthris, post-traumatic inflammatory conditions - affords quick relief of pain & wound edema (Dental Extractions) DOSE: 50 mg TDS, 75 mg i.m (VOVERAN, DICLONAC, DICLOMAX (25, 50 mg Tab., 75 mg /3ml inj)
PIROXICAM  - Long acting potent NSAID with good anti-  inflammatory, analgesic & antiplatelet action   - Reversible inhibitor of COX; lowers PG conc. in  synovial fluid & inhibits platelet aggregation-  prolonging bleeding time  - In addition, it decreases the production of IgM  rheumatoid factor OXICAM DERIVATIVES
@drashishagg Pharmacokinetics: - Rapidly & completed absorbed - Metabolized in liver & excreted in urine - Plasma t1/2 is 2 days. So, single daily administration  is sufficient Adverse effects: - Heart burn, nausea & anorexia, but it is tolerated & less ulcerogenic than PBZ; causes less faecal blood loss than aspirin
Uses: - Suitable for use as short term analgesic as well as long term anti-inflammatory action in – Rheumatoid & Osteo-arthritis, Ankylosing spondylitis, acute gout, musculoskeletal injuries, dental pain DOSE: 20 mg BD for 2 days followed by 20 mg OD (DOLONEX, PIROX) 10, 20 mg cap)
KETOROLAC - Potent analgesic & modest anti-inflammatory activity. - In postoperative pain it has equalled the efficacy of morphine - Inhibits PG synthesis & is believed to relieve pain by a peripheral mechanism - Rapidly absorbed after oral & i.m. administration & excreted unchanged in urine PYRROLO-PYRROLE DERIVATIVE
Adverse effects: - Nausea, abdominal pain, dyspepsia, ulceration, loose stools, drowsiness, headache, dizziness, nervousness, pruritus, pain at injection site - Rise in serum transaminases & fluid retention have been noted Contra-indications: - Should not be given to patients on the anti-coagulants
Uses: - In post-operative & acute musculoskeletal pain:  15-30 mg every 4-6 hours (max. 90 mg/ day)  - Also for renal colic, migraine & pain due to  due to bony metastasis  - Used in a dose of 10-20 mg 6 hourly short term  management of moderate pain AVAILABLE : KETOROL, KETANOV (10 mg Tab)
@drashishagg NIMESULIDE - Sulfonamide derivative - Selective inhibitor of PG synthesis & there is some relative COX-2 selectivity Uses  - Short lasting painful inflammatory conditions like  sports injuries, sinusitis & other ENT disorders,  dental surgery, bursitis, low backache, Postop pain,  osteoarthritis & for fever Preferential COX-2 inhibitors
@drashishagg Pharmacokinetics:  - Completely absorbed orally  - Metabolism-Liver & Excretion- Urine Adverse effects - Epigastralgia, heart burn, loose motions - Dermatological rash, pruritus - Hepatic failure & Renal failure in neonate (BANNED) DOSE- 100mg BD ( NIMULID, NIMEGESIC, NIMODOL 100 mg Tab)
- Recently developed preferential COX-2 inhibitor - Has less analgesic, antipyretic activities, effective in the treatment of rheumatoid & osteoarthritis as well as soft tissue injury - Lower incidence of gastric erosions, ulcers & bleeding DOSE: 500 mg OD (NABUFLAM, NILTIS 500 mg Tab) NABUMETONE
@drashishagg • Directly targets COX-2 which is produced at the site of inflammation • Selectivity for COX-2 can half the risk of peptic ulceration • Cox-2-selectivity might be an increase in the risk for heart attack, thrombosis & stroke by a relative increase in thromboxane Selective COX-2 inhibitors CELECOXIB, ETORICOXIB,PARECOXIB
Uses- - Osteoarthritis  - Rheumatoid arthritis  - Ankylosing spondylitis  - For the management of acute pain in adults Pharmacokinetics: - Slow absorption  - Metabolism-Liver & Excretion- Urine
Dose : - Celecoxib- 100-200 mg BD (CELACT,ZYCEL) - Etoricoxib- 60-120 mg OD (ETODY,ETOXIB) - Parecoxib- 40 mg 6-12 hrs (REVALDO,PAROXIB) Precautions: - In patient who has clinical signs of liver toxicity or if systemic manifestations arise, valdecoxib should be discontinued - Should be used with caution in patients with CHF or hypertension since fluid retention & edema can occur
PARACETAMOL (ACETAMINOPHEN) -- Central Analgesic action is like aspirin, i.e. it raises - pain threshold, but has weak Anti-inflammatory - action - Paracetamol is a good & promptly acting Antipyretic Para-amino phenol derivatives
Uses:  -Most commonly used analgesic for Headache,  Musculoskeletal pain  - Best drug to be used as Antipyretic  - Can be used in All Age groups(infants to elderly),  pregnant/lactating women, & in patients in whom  aspirin is contraindicated Adverse effects:  Safe & Well tolerated, Nausea occur occasionally,  High doses-Hepatic necrosis
Pharmacokinetics: Well absorbed orally. Metabolism-Liver  Excretion in Urine DOSE- 0.5-1gm TDS 500mg Tab (CROCIN, PARACIN, METACIN, PYRIGESIC)
@drashishagg Diuretics : ↓ Diuresis -blockers : ↓ Anti-hypertensive effect ACE inhibitors : ↓ Anti-hypertensive effect Anticoagulants :↑ risk of G.I. Bleed Sulfonylureas : ↑ Hypoglycaemia Alcohol : ↑ risk of G.I. Bleed Cyclosporine : ↑ Nephrotoxicity Drug interactions with NSAIDs
 Allergy to Asprin or any NSAID  Peptic Ulcers  During Pregnancy / Breast feeding  Anticoagulant Therapy  Suffering from blood clotting system disorders  Chronic liver diseases Contraindications
- Mild To Moderate Pain With Little Inflammation – PARACETAMOL or low dose IBUPROFEN - Acute Musculoskeletal Pain, Osteoarthritic, Injury Associated Inflammation - IBUPROFEN, DICLOFENAC - Postoperative or other acute but Short Lasting Painful Conditions With Minimal Inflammation - KETEROLAC, NEFOPAM
- Patients with history of asthma/ anaphylactoid reaction - NIMESULIDE - Gastric intolerance to conventional NSAID -CELECOXIB, ETORICOXIB,PARECOXIB
@drashishagg TOPICAL PREPARATIONS
Advantages of topical medications • Greater safety • Rapid onset of action • High concentrations can be attained at desired site without exposing the rest of the body • Fewer chances of drug interactions • Non-invasive • Better acceptability
TOPICAL PREPARATIONS MEDICATIONS EXAMPLE Topical anesthetics •Benzocaine in orabase (20%) •Lidocaine gel •Eutectic mixture of local anesthetic (EMLA cream) Neuropeptides •Capsaicin cream (0.025% & 0.075%) NSAIDs •Ketoprofen (10-20%) •Diclofenac (10-20%) Sympathomimetic agents •Clonidine (0.01%)
MEDICATIONS EXAMPLE NMDA blocking agents •Ketamine (0.5% in orabase) Anti-convulsants •Carbamazapine (2% in PLO base) Tricyclic medications •Amitriptyline (2% in PLO base) Anti-spasmodics •Baclofen (2% in PLO base)
NEUROPEPTIDES (CAPSAICIN) Available as:  Cream Indications:  Post herpetic neuralgia  Diabetic Neuropathy  Postmastectomy pain syndrome  Trigeminal neuralgia
TOPICAL ANESTHETICS (BENZOCAINE,LIDOCAINE) Available as - Gels - Ointments - Sprays - Adhesive patches Indications: • Post Herpetic Neuralgia • Oral ulcers • Burning mouth syndrome
NSAIDs (KETOPROFEN,DICLOFENAC) Available as:  Cream  Patch Indications:  Localized treatment of acute pain associated with soft tissue injury e.g. Musculoskeletal pain
Local drug delivery systems • Mucoadhesive creams • Transdermal creams • Medicated chewing gums • Dissolving tablets & lozenges • Adhesive patches & powders • Mouthwashes
- NSAIDs - Acetaminophen - Opioids - Antidepressants - Anticonvulsants - Neuroleptics - Corticosteroids - Systemic L. A.’s - Alpha adrenergic agonists - Botulinum toxin Drugs used in management of chronic pain
Analgesics in pregnancy • Acetaminophen -Most Useful -Any Stage • Morphine • Meperidine • Aspirin (Not in 3rd trim.) • Ibuprofen (Not in 3rd trim.) • Pentazocine (With Caution)
NSAIDS as host modulating agent in periodontal disease In vitro model The first evidence that NSAIDs block PG production in gingival tissue ( Gomes & co workers in 1976 ) He demonstrated that inflamed gingival fragment taken from monkey, release PG in culture medium ,& indomethacin reduced the PG production by 90 %
• NSAIDS block PGE2 production , thereby reducing inflammation & inhibiting osteoclast activity in periodontal tissue • Studies have shown that systemic NSAIDS such as indomethacin, flurbiprofen & naproxen administered daily for upto 3 yrs significantly slowed the rate of alveolar bone loss compared with placebo • However daily administration for extended period is necessary for periodontal benefits
• NSAIDS are associated with severe side effects • Research shows that periodontal benefits of taking long term NSAIDS are lost when patient stops taking drug
Trombelli et al 1996 Parallel double blind RCT ,pt undergoing periodontal surgery Pre op ketarolac 20 mg vs placebo Hourly VAS scores for 10 hrs ,time & dose of rescue analgesics Pre op ketarolac reduced pain scores & delayed the onset of post op pain compared to placebo
• Sakuma et al+ and Miyaura et al* - IL-1α, TNF- α, lipopolysaccharide, and basic fibroblast growth factor failed to induce osteoclast formation in EP4- deficient mice cultures • Suggesting that osteoclast formation is mediated by EP4 receptors by PGE2, which was produced through COX-2 + J Bone Miner Res 2000:15:218-227 *J Biol Chem 2000:275: 19819-19823
CONCLUSION • Analgesics are definitely useful in reducing pain & improving the quality of life but have their own spectrum of adverse effects. • No single drug is superior to all others for every patient. Choice of drug is inescapably empirical.
• Essentials of Medical Pharmacology - K.D.TRIPATHI (6th Ed.) • Drugs, Diseases and the Periodontium -Robin A. Seymour and Peter A. Heasman • Pharmacology - DALE,RANG AND RITTER (4th Ed.) • The role of COX-2 and prostaglandin E2 in periodontal diseases periodontology 2000,vol.40,2006,144-163 • Dental Therapeutic Update October 2002
THANK YOU
analgesics and dentistry

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analgesics and dentistry

  • 2.
  • 3.
    • Introduction • Opioidanalgesics –Classification - Mechanism of action -Morphine -Other opioids -Uses • Prostaglandin synthesis & inhibition • NSAIDS - Classification - Mechanism of action -Aspirin -Other NSAIDS Contents
  • 4.
    • Topical analgesics •Enzyme derived analgesics • NSAIDS as host modulating agent in periodontal disease • References
  • 5.
    PAIN An unpleasant sensory& emotional experience associated with actual or potential tissue damage, or described in terms of such damage -IASP
  • 6.
  • 7.
    Analgesic A drug thatselectively relieves pain by acting in the CNS or on peripheral pain mechanisms, without significantly altering consciousness
  • 8.
    Classesof analgesicdrugs • Opioidanalgesics • Nonsteroidal anti-inflammatory drugs (NSAIDS) • Enzyme derived analgesics
  • 9.
    OPIOIDS ANALGESICS • OPIUM:A dark brown, resinous material obtained from Papaver somniferum capsule • OPIOID: Drugs in a generic sense, natural or synthetic, with morphine- like actions
  • 10.
    CLASSIFICATION OF OPIOIDS •NATURAL - Morphine - Codeine - Thebaine • SEMISYNTHETIC – Heroin – Oxymorphone – Hydromorphone • SYNTHETIC – Meperidine – Methadone – Fentanyl – Tramadol
  • 11.
    OPIOIDRECEPTORS - MU – Physical dependence – E uphoria – A nalgesia (supraspinal) – R espiratory depression - KAPPA – S edation – A nalgesia (spinal) – M iosis - DELTA • Analgesia (spinal & supraspinal) • Respirstory depression • Reduced GI motility
  • 12.
    MECHANISMOF ACTION 1) Inhibitthe transmission of nociceptive input from the periphery to the spinal cord 2) Activate descending inhibitory pathways that modulate transmission in the spinal cord 3) Alters limbic system activity
  • 13.
    Action Of Morphine •Analgesia • Sedation • Euphoria • Mood change • Mental cloudiness MORHINE
  • 14.
    MORPHINE ANALGESIA • Relievesall types of pain, but most effective against continuous dull aching pain • Sharp, stabbing, shooting pain also relieved by morphine • Sedation effect, but no loss of consciousness, drowsiness & without motor in-coordination • Morphine euphoria ,sense of well being (Drug abuse)
  • 15.
    Analgesia • Strong analgesic-most effective in most kind of acute & chronic pain • Suppression of pain perception is selective ,without affecting other sensation or producing proportionate generalized CNS depression ( contrast GA _) Sedation • drowsiness • Higher doses causes sleep…coma • No anticonvulsant effects Mood & subjective effects • It has calming effect ,loss of apprehension ,feeling of detachment ,inability to concentrate • Pt in pain or anxiety & addict s specially perceive it pleasurable  euphoric effect 1) CNS EFFECTS OF MORPHINE
  • 16.
    D) Respiratory Centre •Depresses in dose dependent manner • Rate & tidal volume both decreases • Death in poisoning due to respiratory failure E) Cough centre • depressed F) Temperature regulatory centre • Depressed ,hypothermia in cold surrounding
  • 17.
    Morphine stimulates CTZ • Nausea ,vomiting …specia llyif stomach is full Edinger westpal nucleus • Edinger westpal nucleus of third nerve stimulated to produce miosis • Pin point pupil – diagnostic vagal centre • Stimulat ed  causes bradicar dia
  • 18.
    • CVS Causes Vasodilatationdue to - Decreasing tone of blood vessels - Histamine release • GIT - Constipation • NEUROENDOCRINE EFFECTS - Hypothalmic influence on pituitary is reduced - Decreases levels of LH, FSH, ACTH whereas PROLACTIN & GH levels are increased
  • 19.
    Effects on smoothmuscles • BILIARY TRACT Marked increase in the pressure in the biliary tract • URINARY BLADDER Have urinary retention difficulty in micturation • BRONCHIAL MUSCLE Bronchoconstriction can result. (Asthmatics)
  • 20.
    Pharmacokinetics • Oral absorption-Unreliable (HighFirst pass Metabolism) • Primarily metabolised in liver • Freely crosses the placenta & can effect the foetus
  • 21.
    Adverse effects • Sideeffects • Idiosyncrasy and allergy • Apnoea • Acute morhine poisoning ( LD- 250mg ) • Tolerance and dependence
  • 22.
    Therapeutic uses ofmorphine • As Analgesic (Severe Pain) • Preanesthetic medications • Relief of anxiety & apprehension • Acute pulmonary edema • Diarrhoea • Cough • Obstetrical analgesia • DOSE: 10-15 mg i.m/ s.c MORPHINE SULPHATE 10, 15 mg inj
  • 23.
    Contraindications • Bronchial Asthma •Infants & Elderly • Head Injury • Undiagnosed Acute Abdominal pain. • Respiratory diseases (Emphysema, COPD)
  • 24.
    CODEINE • One tenththe potency (analgesic) of morphine • More selective COUGH SUPPRESSANT • Good activity by oral route • Abuse Liability is low AVAILABLE : COREX , COMTUS syp. (10 mg / 5 ml)
  • 25.
    FENTANYL • 80 to100 times more potent than morphine • Rapidly Onset of action (5 min) • Used exclusively in Anaesthesia alone as well in combination with Droperidol • Transdermal fentanyl, is used in the management of persistent chronic pain DOSE: 100-200 µg i.v (FENT, FENDROP 50µg/ml)
  • 26.
    TRAMADOL • Recently introducedCentrally Acting Analgesic • Has dual Norepinephrine & Serotonin reuptake inhibitory effects • 10 times potent than morphine & produces less adverse effects • Used to treat osteoarthritis, low back pain, diabetic neuropathy & cancer pain DOSE: 50-100 mg oral/ i.v. 4-6 hrly (CONTRAMAL, DOMADOL)
  • 27.
    PETHIDINE (MEPERIDINE) • Equalanalgesic efficacy to morphine & some properties like Atropine • Unlike morphine: - More respiratory depression - Less histamine release (Safer in ASTHMATICS) - Less constipation • Used primarily ANALGESIC (substitute of morphine) • DOSE : 50-100 mg i.m, s.c/ orally (PETHIDINE HCL 100mg/ 2ml inj.;50-100mg Tab
  • 28.
    • Synthetic opioidwith pharmacological activity & potency same as morphine • Long duration of activity( PPB >90%) • Powerful pain reliever • Used as SUBSTITUTION Therapy of opioid dependence DOSE: 10 mg inj. PHYSEPTONE METHADONE
  • 29.
    PENTAZOCINE • Mixed opioidagonist-antagonist action • Efficacy lower than morphine • Useful in Mild-Moderate pain conditions • Causes Tachycardia & rise in BP (C/I- MI) • Should not be used in opioid dependent subjects DOSE: 50-100 mg oral , 30-60 mg i.m /s.c (FORTWIN, FORTSTAR)
  • 30.
    Strategies to minimizeopioid side effects • Slow titration of doses • Changing the dosing regimen or route of administration • Using a Nonopioid Or Adjuvant Analgesic for an opioid sparing effect • Adding a drug to counteract the side effect • Constipation prophylaxis
  • 31.
    Pure opioid antagonist Naloxone •Competitive antagonist of all type of opioid receptors • No physical or psychological dependence • 0.4 -0.8 mg : all action of morphine • 4-10 mg : action of nalorphine & pentazocine • Blocks action of endogenous opioid peptides • Inactive orally , • i.v. : 2-3 mins Uses • Morphine poisoning , Neonatal asphyxia
  • 32.
    Endogenous opioid peptide •There are 3 distinct families of opioid peptides, derived from specific polypeptide 1. Endorphins : • β-END having 31 amino acids, derived from POMC ( Pro-opio-melanocortin) • Primarily μ agonist but also has δ action
  • 33.
    2. Enkephalins: • met-ENKand leu-ENK are the most important • Both are Pentapeptides • met-ENK has equal affinity for μ and δ, leu-ENK prefers δ receptors 3. Dynorphins: • DYN-A and DYN-B are 8-17 amino acid peptide • Are more potent on κ receptors
  • 34.
    Prostaglandin synthesis and inhibition Cellmembrane phospholipids Phospholipase A2 Arachidonic acid Cyclooxygenase (COX-1; COX-2) Endoperoxide (PGG, PGH) TXAPGI PGE PGF NSAIDs Steroid’s
  • 36.
  • 37.
    - Analgesic, Antipyretic& Anti-inflammatory actions. - Act primarily on Peripheral Pain Receptors & CNS to raise the pain threshold - Compared to Morphine - Weaker analgesics - Do not depress CNS - Do not produce physical dependence & have no abuse liability INTRODUCTION
  • 38.
    CLASSIFICATION A) NONSELECTIVE COXINHIBITORS (CONVENTIONAL NSAIDS) 1. Salicylates: Aspirin, Diflunisal 2. Pyrazolone derivatives: Phenylbutazone, Oxyphenbutazone 3. Indole derivatives: Indomethacin, Sulindac 4. Propionic acid derivatives: Ibuprofen, Naproxen, Ketoprofen
  • 39.
    5.Anthranilic acid derivative:Mephenamic acid 6.Aryl-acetic acid derivatives: Diclofenac, Tolmetin 7.Oxicam derivatives: Piroxicam, Tenoxicam 8. Pyrrolo-pyrrole derivative: Ketorolac B) PREFERENTIAL COX-2 INHIBITORS – Nimesulide, Meloxicam, Nabumetone C) SELECTIVE COX-2 INHIBITORS - Celecoxib
  • 40.
    @drashishagg D) ANALGESIC-ANTIPYRETICS WITH POORANTI-INFLAMMATORY ACTION - 1. Paraaminophenol derivative: Paracetamol (Acetaminophen) 2. Pyrazolone derivatives: Metamizol, Propiphenazone 3. Benzoxazocine derivatives: Nefopam
  • 41.
    - Act asNon-selective Inhibitors of the enzyme cyclooxygenase, inhibiting both, COX-1 & COX-2 isoenzymes - Cyclooxygenase catalyses the formation of PGs & TBX 2 from arachidonic acid Mechanism of action
  • 42.
    COX-1 - Present aspart of everyday physiological function. - Protects the stomach by limiting acid secretion - Helps platelets limit bleeding by increasing their adhesiveness COX-2 - Its expression is induced by various stimuli such as the inflammation or at the site of the injury
  • 43.
  • 44.
    GASTRIC MUCOSAL DAMAGE ANTIPLATELETAGGREGATION DUCTUS ARTERIOSUS CLOSURE
  • 45.
    PARTURITION AND IN DYSMENORRHOEA RENALEFFECTS ANAPHYLACTIC REACTIONS
  • 46.
    @drashishagg ASPIRIN • Analgesic, Antipyretic& Anti-inflammatory Effects. • RESPIRATORY SYSTEM -Increases rate & depth. • GIT - Irritates the gastric mucosa  causes epigastric distress, nausea & vomiting - Promotes the local back diffusion of the acid  acute ulcers, erosive gastritis, microscopic haemorrhages SALICYLATES
  • 47.
    @drashishagg • CVS - Nodirect effect - Larger doses increase cardiac output to meet increased peripheral O2 demand caused by direct vasodilation • BLOOD - Inhibits TXA2 synthesis by platelets - Interferes with Platelet aggregation (BT) • METABOLIC EFFECTS - Increased utilization of Glucose, blood sugar may decrease specially in diabetics
  • 48.
    @drashishagg Pharmacokinetics - Poor Absorption-Stomach & Small Intestine - Metabolism- Gut wall, Liver, Plasma & other tissues to release salicylic acid. Excretion- Urine Adverse effects - Nausea,Vomiting, Epigastric distress & occult blood in stools, rashes, urticaria, asthma, angioedema - Anti-inflammatory doses – syndrome Salicylism – dizziness, tinitus, reversible impairment of hearing & vision, excitement
  • 49.
    use analgesic antipyretic Acute rheumatic fever Rheumatoid arthritis Osteoarthri tis Post MI & poststroke patients pregnancy induced hypertension & preeclampsia to delay labour patent ductus arteriosus DOSE: 300-900 mg every 4 hrs (Max 3.6 gm) ( ASA, ASCAD, ECOSPRIN 50mg,75mg Tab.)
  • 50.
    @drashishagg PHENYLBUTAZONE - Potent anti-inflammatorydrug. - Poor analgesic & antipyretic activity Adverse effects: - More toxic than Aspirin - Bone marrow depression, Agranulocytosis - Banned in some countries DOSE: 100-200 mg BD or TDS after meals (ZOLANDIN 100,200 mg Tab) PYRAZOLONE DERIVATIVES
  • 51.
    @drashishagg INDOMETHACIN - Potent anti-inflammatory,antipyretic & good analgesic - Analgesic action better than PBZ Adverse effects: - High incidence of GI & CNS side effects - C/I in drivers, epileptics, pregnancy & children Uses: - Rheumatoid Arthritis not controlled by aspirin - Acts rapidly in Acute Gout DOSE: 25-50 mg BD /TDS (INDOCAP, IDICIN) INDOLE DERIVATIVES
  • 52.
    IBUPROFEN - Analgesic, Antipyretic& Anti-inflammatory activity is lower than aspirin - Inhibit platelet aggregation & prolong bleeding time Adverse effects: - Better tolerated than aspirin (Incidence is lower) - Gastric discomfort, nausea & vomiting are most  common side effects - Headache, dizziness, blurring of vision, tinnitus PROPIONIC ACID DERIVATIVES
  • 53.
    Pharmacokinetics:  - Absorbedorally, highly bound to plasma proteins  (90-99%)  - Metabolized in liver & excreted in urine & bile - Enter brain, synovial fluid & cross placenta Interactions: - As they inhibit platelet function, use with  anticoagulants should be avoided  - Likely to decrease diuretic & antihypertensive action  of thiazides, furosemide and -blockers
  • 54.
    - As Analgesic& Antipyretic - In Rheumatoid Arthritis, Osteoarthritis & other Musculoskeletal Disorders, specially where pain is more prominent than inflammation - Indicated in soft tissue injuries, fractures, tooth extraction, supppress swelling & inflammation DOSE: 400-800 mg TDS (BRUFEN, EMFLAM, IBUGESIC 200, 400, 600 mg Tab) Uses
  • 55.
    MEPHENAMIC ACID - AnAnalgesic, Antipyretic & Anti-inflammatory drug, - Exerts Peripheral as well as Central Analgesic Action Adverse effects : - Diarrhoea - Epigastric distress is complained, but gut bleeding is  not significant ANTHRANILIC ACID DERIVATIVE
  • 56.
    @drashishagg Pharmacokinetics: - Oral absorptionis slow but almost complete - Partly metabolized & excreted in urine & in bile Uses:  - Analgesic in muscle, joint & soft tissue pain where  strong anti-inflammatory action is not needed (MPDS) - Useful in rheumatoid & osteoarthritis DOSE: 250-500 mg TDS (MEFTAL, PONSTAN, MEDOL 250, 500 mg cap)
  • 58.
    • Introduction • Opioidanalgesics –Classification - Mechanism of action -Morphine -Other opioids -Uses • Prostaglandin synthesis & inhibition • NSAIDS - Classification - Mechanism of action -Aspirin -Other NSAIDS Contents
  • 59.
    CLASSIFICATION A) NONSELECTIVE COXINHIBITORS (CONVENTIONAL NSAIDS) 1. Salicylates: Aspirin, Diflunisal 2. Pyrazolone derivatives: Phenylbutazone, Oxyphenbutazone 3. Indole derivatives: Indomethacin, Sulindac 4. Propionic acid derivatives: Ibuprofen, Naproxen, Ketoprofen
  • 60.
    5.Anthranilic acid derivative:Mephenamic acid 6.Aryl-acetic acid derivatives: Diclofenac, Tolmetin 7.Oxicam derivatives: Piroxicam, Tenoxicam 8. Pyrrolo-pyrrole derivative: Ketorolac B) PREFERENTIAL COX-2 INHIBITORS – Nimesulide, Meloxicam, Nabumetone C) SELECTIVE COX-2 INHIBITORS - Celecoxib
  • 61.
    @drashishagg DICLOFENAC SODIUM - Analgesic,Antipyretic, Anti-inflammatory action - Inhibits PG synthesis & has short lasting antiplatelet  action  Pharmacokinetics: - Well absorbed orally, metabolized & excreted both  in urine & bile - Has good tissue penetrability & conc. in synovial  fluid is maintained longer period, exerting extended  therapeutic action in joints ARYL-ACETICACID DERIVATIVE
  • 62.
    @drashishagg Adverse effects - Aregenerally mild: Epigastric pain, nausea, headache, dizziness, rashes - Gastric ulceration & bleeding -less common Uses: - Most extensively used NSAID - Rheumatoid & Osteoarthris, post-traumatic inflammatory conditions - affords quick relief of pain & wound edema (Dental Extractions) DOSE: 50 mg TDS, 75 mg i.m (VOVERAN, DICLONAC, DICLOMAX (25, 50 mg Tab., 75 mg /3ml inj)
  • 63.
    PIROXICAM  - Longacting potent NSAID with good anti-  inflammatory, analgesic & antiplatelet action   - Reversible inhibitor of COX; lowers PG conc. in  synovial fluid & inhibits platelet aggregation-  prolonging bleeding time  - In addition, it decreases the production of IgM  rheumatoid factor OXICAM DERIVATIVES
  • 64.
    @drashishagg Pharmacokinetics: - Rapidly &completed absorbed - Metabolized in liver & excreted in urine - Plasma t1/2 is 2 days. So, single daily administration  is sufficient Adverse effects: - Heart burn, nausea & anorexia, but it is tolerated & less ulcerogenic than PBZ; causes less faecal blood loss than aspirin
  • 65.
    Uses: - Suitable foruse as short term analgesic as well as long term anti-inflammatory action in – Rheumatoid & Osteo-arthritis, Ankylosing spondylitis, acute gout, musculoskeletal injuries, dental pain DOSE: 20 mg BD for 2 days followed by 20 mg OD (DOLONEX, PIROX) 10, 20 mg cap)
  • 66.
    KETOROLAC - Potent analgesic& modest anti-inflammatory activity. - In postoperative pain it has equalled the efficacy of morphine - Inhibits PG synthesis & is believed to relieve pain by a peripheral mechanism - Rapidly absorbed after oral & i.m. administration & excreted unchanged in urine PYRROLO-PYRROLE DERIVATIVE
  • 67.
    Adverse effects: - Nausea,abdominal pain, dyspepsia, ulceration, loose stools, drowsiness, headache, dizziness, nervousness, pruritus, pain at injection site - Rise in serum transaminases & fluid retention have been noted Contra-indications: - Should not be given to patients on the anti-coagulants
  • 68.
    Uses: - In post-operative& acute musculoskeletal pain:  15-30 mg every 4-6 hours (max. 90 mg/ day)  - Also for renal colic, migraine & pain due to  due to bony metastasis  - Used in a dose of 10-20 mg 6 hourly short term  management of moderate pain AVAILABLE : KETOROL, KETANOV (10 mg Tab)
  • 69.
    @drashishagg NIMESULIDE - Sulfonamide derivative -Selective inhibitor of PG synthesis & there is some relative COX-2 selectivity Uses  - Short lasting painful inflammatory conditions like  sports injuries, sinusitis & other ENT disorders,  dental surgery, bursitis, low backache, Postop pain,  osteoarthritis & for fever Preferential COX-2 inhibitors
  • 70.
    @drashishagg Pharmacokinetics:  - Completelyabsorbed orally  - Metabolism-Liver & Excretion- Urine Adverse effects - Epigastralgia, heart burn, loose motions - Dermatological rash, pruritus - Hepatic failure & Renal failure in neonate (BANNED) DOSE- 100mg BD ( NIMULID, NIMEGESIC, NIMODOL 100 mg Tab)
  • 71.
    - Recently developedpreferential COX-2 inhibitor - Has less analgesic, antipyretic activities, effective in the treatment of rheumatoid & osteoarthritis as well as soft tissue injury - Lower incidence of gastric erosions, ulcers & bleeding DOSE: 500 mg OD (NABUFLAM, NILTIS 500 mg Tab) NABUMETONE
  • 72.
    @drashishagg • Directly targetsCOX-2 which is produced at the site of inflammation • Selectivity for COX-2 can half the risk of peptic ulceration • Cox-2-selectivity might be an increase in the risk for heart attack, thrombosis & stroke by a relative increase in thromboxane Selective COX-2 inhibitors CELECOXIB, ETORICOXIB,PARECOXIB
  • 73.
    Uses- - Osteoarthritis  -Rheumatoid arthritis  - Ankylosing spondylitis  - For the management of acute pain in adults Pharmacokinetics: - Slow absorption  - Metabolism-Liver & Excretion- Urine
  • 74.
    Dose : - Celecoxib-100-200 mg BD (CELACT,ZYCEL) - Etoricoxib- 60-120 mg OD (ETODY,ETOXIB) - Parecoxib- 40 mg 6-12 hrs (REVALDO,PAROXIB) Precautions: - In patient who has clinical signs of liver toxicity or if systemic manifestations arise, valdecoxib should be discontinued - Should be used with caution in patients with CHF or hypertension since fluid retention & edema can occur
  • 76.
    PARACETAMOL (ACETAMINOPHEN) -- CentralAnalgesic action is like aspirin, i.e. it raises - pain threshold, but has weak Anti-inflammatory - action - Paracetamol is a good & promptly acting Antipyretic Para-amino phenol derivatives
  • 77.
    Uses:  -Most commonlyused analgesic for Headache,  Musculoskeletal pain  - Best drug to be used as Antipyretic  - Can be used in All Age groups(infants to elderly),  pregnant/lactating women, & in patients in whom  aspirin is contraindicated Adverse effects:  Safe & Well tolerated, Nausea occur occasionally,  High doses-Hepatic necrosis
  • 78.
    Pharmacokinetics: Well absorbed orally.Metabolism-Liver  Excretion in Urine DOSE- 0.5-1gm TDS 500mg Tab (CROCIN, PARACIN, METACIN, PYRIGESIC)
  • 79.
    @drashishagg Diuretics : ↓Diuresis -blockers : ↓ Anti-hypertensive effect ACE inhibitors : ↓ Anti-hypertensive effect Anticoagulants :↑ risk of G.I. Bleed Sulfonylureas : ↑ Hypoglycaemia Alcohol : ↑ risk of G.I. Bleed Cyclosporine : ↑ Nephrotoxicity Drug interactions with NSAIDs
  • 80.
     Allergy toAsprin or any NSAID  Peptic Ulcers  During Pregnancy / Breast feeding  Anticoagulant Therapy  Suffering from blood clotting system disorders  Chronic liver diseases Contraindications
  • 81.
    - Mild ToModerate Pain With Little Inflammation – PARACETAMOL or low dose IBUPROFEN - Acute Musculoskeletal Pain, Osteoarthritic, Injury Associated Inflammation - IBUPROFEN, DICLOFENAC - Postoperative or other acute but Short Lasting Painful Conditions With Minimal Inflammation - KETEROLAC, NEFOPAM
  • 82.
    - Patients withhistory of asthma/ anaphylactoid reaction - NIMESULIDE - Gastric intolerance to conventional NSAID -CELECOXIB, ETORICOXIB,PARECOXIB
  • 83.
  • 84.
    Advantages of topicalmedications • Greater safety • Rapid onset of action • High concentrations can be attained at desired site without exposing the rest of the body • Fewer chances of drug interactions • Non-invasive • Better acceptability
  • 85.
    TOPICAL PREPARATIONS MEDICATIONS EXAMPLE Topicalanesthetics •Benzocaine in orabase (20%) •Lidocaine gel •Eutectic mixture of local anesthetic (EMLA cream) Neuropeptides •Capsaicin cream (0.025% & 0.075%) NSAIDs •Ketoprofen (10-20%) •Diclofenac (10-20%) Sympathomimetic agents •Clonidine (0.01%)
  • 86.
    MEDICATIONS EXAMPLE NMDA blocking agents •Ketamine(0.5% in orabase) Anti-convulsants •Carbamazapine (2% in PLO base) Tricyclic medications •Amitriptyline (2% in PLO base) Anti-spasmodics •Baclofen (2% in PLO base)
  • 87.
    NEUROPEPTIDES (CAPSAICIN) Available as:  Cream Indications: Post herpetic neuralgia  Diabetic Neuropathy  Postmastectomy pain syndrome  Trigeminal neuralgia
  • 88.
    TOPICAL ANESTHETICS (BENZOCAINE,LIDOCAINE) Available as- Gels - Ointments - Sprays - Adhesive patches Indications: • Post Herpetic Neuralgia • Oral ulcers • Burning mouth syndrome
  • 89.
    NSAIDs (KETOPROFEN,DICLOFENAC) Available as:  Cream Patch Indications:  Localized treatment of acute pain associated with soft tissue injury e.g. Musculoskeletal pain
  • 90.
    Local drug deliverysystems • Mucoadhesive creams • Transdermal creams • Medicated chewing gums • Dissolving tablets & lozenges • Adhesive patches & powders • Mouthwashes
  • 91.
    - NSAIDs - Acetaminophen -Opioids - Antidepressants - Anticonvulsants - Neuroleptics - Corticosteroids - Systemic L. A.’s - Alpha adrenergic agonists - Botulinum toxin Drugs used in management of chronic pain
  • 92.
    Analgesics in pregnancy •Acetaminophen -Most Useful -Any Stage • Morphine • Meperidine • Aspirin (Not in 3rd trim.) • Ibuprofen (Not in 3rd trim.) • Pentazocine (With Caution)
  • 93.
    NSAIDS as hostmodulating agent in periodontal disease In vitro model The first evidence that NSAIDs block PG production in gingival tissue ( Gomes & co workers in 1976 ) He demonstrated that inflamed gingival fragment taken from monkey, release PG in culture medium ,& indomethacin reduced the PG production by 90 %
  • 94.
    • NSAIDS blockPGE2 production , thereby reducing inflammation & inhibiting osteoclast activity in periodontal tissue • Studies have shown that systemic NSAIDS such as indomethacin, flurbiprofen & naproxen administered daily for upto 3 yrs significantly slowed the rate of alveolar bone loss compared with placebo • However daily administration for extended period is necessary for periodontal benefits
  • 95.
    • NSAIDS areassociated with severe side effects • Research shows that periodontal benefits of taking long term NSAIDS are lost when patient stops taking drug
  • 96.
    Trombelli et al1996 Parallel double blind RCT ,pt undergoing periodontal surgery Pre op ketarolac 20 mg vs placebo Hourly VAS scores for 10 hrs ,time & dose of rescue analgesics Pre op ketarolac reduced pain scores & delayed the onset of post op pain compared to placebo
  • 97.
    • Sakuma etal+ and Miyaura et al* - IL-1α, TNF- α, lipopolysaccharide, and basic fibroblast growth factor failed to induce osteoclast formation in EP4- deficient mice cultures • Suggesting that osteoclast formation is mediated by EP4 receptors by PGE2, which was produced through COX-2 + J Bone Miner Res 2000:15:218-227 *J Biol Chem 2000:275: 19819-19823
  • 98.
    CONCLUSION • Analgesics aredefinitely useful in reducing pain & improving the quality of life but have their own spectrum of adverse effects. • No single drug is superior to all others for every patient. Choice of drug is inescapably empirical.
  • 99.
    • Essentials ofMedical Pharmacology - K.D.TRIPATHI (6th Ed.) • Drugs, Diseases and the Periodontium -Robin A. Seymour and Peter A. Heasman • Pharmacology - DALE,RANG AND RITTER (4th Ed.) • The role of COX-2 and prostaglandin E2 in periodontal diseases periodontology 2000,vol.40,2006,144-163 • Dental Therapeutic Update October 2002
  • 100.