GOOD AFTERNOON

Analgesics

Presented byDr Guru Ram Tej. KI yr Post Graduate

Dept Of Periodontics

Introduction Pain/ Algesia Analgesics Classification Opoid analgesics Non opoid analgesics NSAIDs Contra indications Analgesics used in periodontics

Contents

Introduction

The Sumerians wrote of demons and tooth worms causing tooth decay. People would pray to gods such as Shamash, Anu or Ea to cure them of their painful oral afflictions

“An unpleasant sensory and emotional experience associated with actual or potential tissue damage, or described in terms of such damage.”

Pain

1. Pain perception2. Reception to pain

Two components of pain

SUBSTANCES RELEASED SUBSTANCE-P SERATONIN HISTAMIINE BRADYKININ-prostaglandins to act

PAIN PERCEPTION

PAIN RECEPTORS SOMATIC NOCIRECEPTORS

VISCERAL NOCICEPTORS

PAIN PATHWAYS Trigeminal nerve

Semilunar ganglion (g.g)

Pons

Sensory root

Ascending fibres Descending fibres

Tactile sensibility Pain and Temperature

Sensory root

PAIN PATHWAYS

Each end organ has its pathway into CNS

The pain pathway consists of

First order neurons

Second order neurons

Third order neurons

First order neurons

Cells of posterior nerve root ganglia

A- delta fibres- marginal cells in posterior

gray horn

C- fibres- Substantia gelatinosa in posterior

gray horn

Second order neurons

The marginal cells and the cells of Substantia gelatinosa form the second order neurons

Third order neurons

Neurons of Thalamic nucleus, reticular

formation, tectum and grey matter around

aqueduct of sylvius

These neuron axons reach sensory area of

cerebral cortex

SPECIFICITY THEORY Descartes-1644 Muller-19th century Von frey-1895

PATTERN THEORY Gold Scheider-1894

INTENSITY THEORY GATE CONTROL THEORY

THEORIES TO EXPLAIN PAIN

GATE CONTROL THEORY

• GATE input

• GATE output

Physical (injury)

Emotional (depression)

Behavioural (focusing on pain)

Factors that OPEN the gate

Physical (medication)

Emotional (happiness, relaxation)

Behavioural (distraction)

Factors that CLOSE the gate

No one has located the actual gate mechanism

Still assumes the organic basis

LIMITATIONS

International Association Of Somatic Pain(IASP) REGION

SYSTEM

TEMPERATURE CHANGE

PATIENT STATEMENT

ETIOLOGY

CLASSIFICATION OF PAIN

CLASSIFICATION

Based on duration

Acute and chronic

Based on etiology

Inflammatory, Nociceptive and

Neuropathic pain

Atypical facial pain

Refered pain

Types of DENTAL pain Arising from

Pulp

Peri radicular region

Exposed dentin

Cracked tooth syndrome

LOCAL ANESTHETICS

ANALGESICS

NSAIDS

OPOIDS

CONSCIOUS SEDATION

MANAGEMENT OF PAIN

“Analgesics are a class of drugs which obtunds the perception of pain without producing unconsciousness”

These act on CNS or the peripheral pain mechanisms

ANALGESICS

Oral Intramuscular Injection Intravenous Injection PCA: patient controlled analgesia Other routes

Transdermal Sublingual

ROUTES OF ADMINISTRATION

Narcotic (opioid / morphine like analgesics)

Non-narcotic (Non opioid / antipyretic /

aspirin like analgesics or NSAIDs)

CLASSIFICATION OF ANALGESICS

Opium: oldest types of drugs

Opium is extracted from poppy seeds

(Papaver somniferum)

16th century - Analgesic qualities

By the 19th century considered “as

legitimate as tobacco or tea”

Narcotic analgesics

  Agonists: Morphine Pethidine, methadone

and propoxyphene. Antagonists: Naloxone Mixed: Butorphanol, nalbuphine, &

buprenorphine.

OPIOID ANALGESICS:

SYNTHETIC DERIVATIVES WITH STRUCTURE UNRELATED TO MORPHINE:

(a)Phenyl piperidine series- pethidine & fentanyl

(b)Methadone series- methadone & dextropropoxyphene

(c )Benzomorphan series- Pentazocine & cyclazocine

(d)Semisynthetic thebaine derivatives:etorphine & buprenorphine

Mu Kappa Delta

OPOID RECEPTORS

Non-Steroidal Anti Inflammatory Drugs(NSAIDs)

CHEMICAL NATURE

MECHANISM OF ACTION

MODE OF ACTION

THERAPEUTIC CLASSIFICATION

CLASSIFICATION

CHEMICAL CLASSIFICATION SALICYLATES - Acetyl salicylic acid (aspirin),

sodium salicylate, Mg salicylate, choline salicylate, Na thio salicylate.

PROPIONIC ACID DERIVATIVES -Ibuprofen, ketoprofen, naproxen, oxaprozin, flurbiprofen

INDOLE ACETIC ACID -Indomethacin, sulindac, SUBSTITUTED ANTHRANILIC ACIDS -

Mefenamic acid, meclofenamate Na PYRROLE ALKANOIC ACID ketorolac OXICAMS Piroxicam, meloxicam DIFLUOROPHENYL DERIVATIVES Diflunisal

ARYL ACETIC ACID Diclofenac ACETIC ACID DERIVATIVES Etodolac NAPHTHYL ACETIC ACID PRODRUGS

Nabumetrone PARA-AMINO PHENOL DERIVATIVES

Acetaminophen

ACCORDING TO MECHANISM OF ACTION

NON-SELECTIVE COX INHIBITORS Diclofenac,

etodolac, indomethacin, ketoprofen, ketorolac,

nabumetone, naproxen, oxaprozin, ibuprofen,

flurbiprofen, diflunisol, sulindac, tenoxicam,

tolmetin

COX-1 INHIBITORS Aspirin, indomethacin,

piroxicam, sulindac

COX-2 SELECTIVE INHIBITORS Celecoxib,

etoricoxib, meloxicam

THERAPEUTIC CLASSIFICATION

ANALGESICS Aspirin, paracetamol

ANTI-INFLAMMATORY Indomethacin, naproxen,

ibuorofen

ANTI-COAGULANTS Aspirin

ANTI-PYRETICS Aspirin, paracetamol,

indomethacin, celecoxib, ibuprofen

W.H.O CLASSIFICATION in 2001 A: DRUGS WITH WEAK ANTI-INFLAMMATORY

EFFECT Acetaminophen

B: DRUGS WITH MILD TO MODERATE ANTI-INFLAMMATORY EFFECT Propionic acid derivatives, anthranilic acid derivatives

C: DRUGS WITH MARKED ANTI-INFLAMMATORY EFFECTS Salicylates, acetic acid derivatives, oxicams, diclofenac.

PROSTAGLANDINS Prostaglandins were first discovered

in1930s by Ulf von Euler During inflammation, pain, fever,

Arachidonic acid is liberated from phospholipids fraction of the cell membrane, Arachidonic acid is then enzymatically converted to prostaglandin (pgi2) and thromboxane a2 in presence of enzyme cycloxygenase

Cycloxygenase exists in: Cox-1 (constitutive) Cox-2 isoforms (inducible)

%

SALICYLATES

Gastric mucosal damage – peptic ulcer Nausea, vomiting, blood loss in stools

(haemotochesia) Epigastric distress Hypersentivity

Salicylism

ADVERSE EFFECTS

Diclofenac sodium

Newer analgesic, anti-inflammatory.

Antipyretic

Inhibits prostaglandin synthesis,

short lasting antiplatelet action

Neutrophil – production of superoxide

dismutase inhibits chemotaxis

ARYL ACETIC ACID DERIVATIVES

Piroxicam

Meloxicam

Tenoxicam

OXICAM DERIVATIVES

Ibuprofen Prostaglandin synthesis inhibition Anti inflammatory Anti pyretic

Dosage – 400mg every 6th hourly

PROPIONIC ACID DERIVATIVES

Nausea, dyspepsia, heartburn, vomiting and abdominal pain

Gastric ulceration and bleeding can occur in patients using Ibuprofen for prolonged period of up to one year

Drug interactions- thiazides and lithium

Side Effects

Ketorolac COX 2 inhibition Free radical scavenging property Inhibition of TNF- alpha

Contra-indications: Patients on anticoagulants

Uses: Post –operative pain, acute musculoskeletal

disorders.

PYRROLE ALKANOIC ACID DERIVATIVES

Indomethacin prostaglandin synthetase epileptics and pregnant women

Sulindac

INDOLE ACETIC ACID DERIVATIVES

MEFANAMIC ACIDLow efficacy

Plasma half life 2-4 hrs

ANTHRANILIC ACID DERIVATIVES

Paracetamol: (acetaminophen)

PARA-AMINO PHENOL DERIVATIVES

Drug Preparations Route Usual Adult Dose (Mg)

Pentazocine Lactate (Talwin)

30 mg/ml Intramuscular, Subcutaneous, Intravenous

30

Pentazocine Hcl 50 mg tablets Oral 50 to 100

Meperidine Hcl 25, 50, 75 and 100 mg / ml

Intramuscular, Subcutaneous

50 to 100

50 and 100 mg tablets Oral 50 to 100

Morphine Sulfate 8, 10, 15 and 30 mg / ml

Subcutaneous 10 to 15

Control Of Pain And Infection, Dent. Clin. North Am. 17 : 417-427, 1973.

Pearlman et al in 1997- IBUPROFEN

D W Paquette et al in 1997- KETOPROFEN

J M Thomason et al in 1997- ASPIRIN

A B Pablos et al in 2008- MELOXICAM & DS

C Alen Yen et al in 2008-CELECOXIB

Khalid Al-Hezaimi et al in 2011- KETOROLAC

TROMETHACINE

USE IN PERIODONTICS

Eli E Machtei et al in 2011

AS A LDD AND HOST MODULATION

Essentials of medical pharmacology- KD Tripathi Lippincots illustrated rewiew pharmacology Pharmacology – padmaja uday Kumar JSSN U30S-6979 Enantiospecific inhibition of ligature-induced periodontitis in beagles with

topical (S)-ketoprofen: D.W.Paquette J,P.Fioretlini, C Martusceili R,J. Oringer, T H. Howell, J R. McCullough,D.S.Reasner and R. C williams: J Clin periodontol 1997: 24: 521-528.

The analgesic efficacy of ibuprofen in periodontal surgery: A multicentre study: B. Pearlman, S. Boyatzis, C. Daly, R. Evans, J. Gouvoussis, J. Highfield, S. Kitchings, V. Liew, S. Parsons, P. Serb, P. Tseng, C. Wallis: Australian Dental Journal 1997;42:5.

Aspirin-induced post-gingivectomy haemorrhage: a timely reminder, Thoniason JM, Seymour RA, Murphy P, Brigkam KM, Jones P: Aspirin-induced post-gingivectomv haetnorrhage: a timely reminder, J Clin Periodontol 1997; 24: 136-138

REFERENCES

Effect of Meloxicam and diclofenac sodium on peri implant bone healing in rats: AB Pablos, satunino AR, B Konig, Cristiane F, Vera C de Arujo and Patricia R Cury: J periodontol 2008; 79; 300-306.

The effect of a selective cycloxygenase-2 inhibitor (Celecoxib) on chronic periodontitis: C Alen Yen, Petros D Damoulis, Paul C Stark, Patricia L Hibberd, Medha Singh and Anthena S Papas. J Periodontol 2008; 79: 104-113.

Evaluation of novel adhesive film containing ketorolac for post surgery and pain control: a safety and efficacy study: Khalid Al-Hezaimi, Mansour Al-Askar, Zuied Selamhe, Jia- Hui Fu, Ibrahim A. Alsarra, and Hom Lay Wang: J periodontol 2011; 82: 963-968

Multiple applications of Flurbiprofen and chlorhexidine chips in patients with chronic periodontitis: a randomized, double blind, parallel, 2- arms clinical trial: Eli E Machtei, Ilan Hirsh, Maher Falah, Eyal Shoshani, Avi Avramoff and Adel Penhasi. J Clin Periodontol 2011; 38: 1037-1043.

REFERENCES

Thank You….