NSAIDS

Good
Morning
INDIAN DENTAL ACADEMY
Leader in continuing dental education
www.indiandentalacademy.com

CONTENTS
 Introduction
 History
 Classification
 Mechanism of action
 Beneficial action and toxicities of PG synthesis inhibition
 Common properties of all NSAIDs
 Drugs proper
 Choice of analgesic after certain endodontic procedures
 Pain management strategy
 Flexible prescription plan
 Advances
 References
 Conclusion www.indiandentalacademy.com

HISTORY
Willow Bark – Centuries ago.
1875 – Sodium salicylate
1899 – Phenacetin + antipyrine
1899 – Acetyl salicylic acid
1949 – Phenyl butazone
1963 – Indomethacin
1963 – Propionic acid derivatives (NSAIDS)
1971 – Vane and coworkers observed that NSAIDS
blocked PG synthesis.www.indiandentalacademy.com

CLASSIFICATION
(Acc. to Tripathi)
A. Analgesic and antiinflammatory :
Aspirin, Salicylamide, Benorylate, Diflunisal
Salicylates
Phenylbutazone, oxyphenbutazonePyrazolone derivatives
Indomethacin, sulindacIndole derivatives
Ibuprofen,Naproxen, Ketoprofen, Fenoprofen,
Flurbiprofen.
Propionic acid derivatives
Mephenamic acidAnthranilic acid derivative
Diclofenac, TolmetinAryl-acetic acid derivatives
Piroxicam, Tenoxicam, Meloxicam.Oxicam derivatives
Ketorolac.Pyrrolo-pyrrole derivative
NImesulideSulfonanilide derivative
NabumetoneAlkanones www.indiandentalacademy.com

B. Analgesic but poor antiinflammatory:
Paracetamol (Acetaminophen)Paraaminophenol derivative
Metamizol (Dipyrone), propiphenazonePyrazolone derivatives
Nefopam
Benzoxazocine derivative
Acc. to Goodman and Gillman
A. Non selective Cox inhibitor
Aspirin, sodium salicylate, choline magnesium
trisalicylate, salsalate, diflunisal, salfasalazine,
olsalazine.
Salicylic acid derivatives
AcetaminophenPara amino derivatives
Indomethacin, sulindacIndole & indene acetic acid
Tolmetin, diclofenac, ketorolac.Heteroaryl acetic acid

Ibuprofen, naproxen, flurbiprofen, ketoprofen,
fenoprofen, oxaproxin.
Aryl propionic acid
Mefenamic acid, meclofenamic acid
Anthranilic acid (fenamates)
Oxicams (piroxicam, Meloxicam)
Enolic acid
Nabumetone.
Alkanones
Rofecoxib
Diaryl substituted furanones
B. Selective cox-2 inhibitor
Celecoxib
Diaryl substituted
Pyrazoles
Etodolac
Indole acetic acid
Nimesulide
Sulfonanilides

MECHANISM OF ACTION
Odontogenic pain Acute pain
Noxious stimuli Tissue destruction or injury
Cellular destruction
Release / synthesis of histamine /
prostaglandin / bradykinin
Peripheral nociceptor / free nerve
endings
PAIN
+
Disease process
+
Surgical intervention

Beneficial actions due to PG
Synthesis inhibition
• Analgesia
• Antipyresis
• Antiinflammatory
• Antithrombotic
• Closure of ductus arteriosus
Shared toxicities due to PG
synthesis inhibition
• Gastric mucosal damage
• Bleeding
• Limitation of renal blood flow
• Delay / prolongation of labour
• Asthma & anaphylactoid
reactions

COMMON PROPERTIES OF ALL NSAIDS
Analgesia Antipyresis
Anti-
inflammatory
Dysmenorrhoea
Antiplatelet
aggregatory
Ductus
arteriosus
closure
Parturition
Gastric mucosal
damage
Renal effects
Anaphylactoid
reactions

SALICYLATES
Aspirin (prototype)
Pharmacological actions
• Analgesic (0.3-1.5 g/day)
• Antipyretic
• Antiinflammatory (3-6 g/day or 100mg/kg/day)
• Metabolic effects
• Respiration
• Acid base and electrolyte balance
• CVS
• GIT
• Urate excretion
• Blood
 2-5 g/day <2g/day  > 5g/day

Pharmacokinetics
 80% bound to plasma proteins.
 Volume distribution 0.17 L/kg.
 Plasma t ½ = 15-20 min.
 Release salicylic acid (t ½) = 3-5
hrs.
 Antiinflammatory doses (t ½) =
8-12 hrs. (30 hrs in poisoning)

Adverse effects
Salicylism : dizziness, tinnitus, vertigo, reversible impairment of
hearing & vision, excitement & mental confusion,
hyperventilation & electrolyte imbalance.
Acute salicylate poisoning : fatal dose-15-30g , > 50 mg/dl.www.indiandentalacademy.com

Contraindications :
Sensitivity, peptic ulcers, bleeding tendency, chicken pox
or influenza.
Chronic liver disease
Diabetics, low cardiac reserve or frank CHF, juvenile
rheumatoid arthritis.
Precautions :
Stopped 1 week before elective surgery.
During pregnancy
Avoided by breast feeding mothers.
G-6-PD deficient individualswww.indiandentalacademy.com

Interactions :
 Warfarin, naproxen, sulfonylureas,
phenytoin and methotrexate.
 Oral anticoagulants.
 Uric acid
 Probenecid
 Methotrexate.
 Furosemide and thiazides
 Spironolactone.
 Protein bound iodine levels.

Uses :
Analgesic
Antipyretic
Acute rheumatic
fever (4-6 g)
Rheumatoid
arthritis (3-5 g)
Osteoarthritis
Postmyocardial
infarction &
poststroke patients
Pregnancy induced
hypertension and
preeclampsia
Delay labour
Patent ductus
arteriosus
* Aspirin, dispirin, colosprinwww.indiandentalacademy.com

PYRAZOLONES
Phenylbutazone
Pharmacokinetics
 Plasma t ½ = 60 hrs.
 Dose 100-200 mg BD/TDS
Adverse effects
 Bone marrow
depression
 Agranulocytosis
 Stevens-Johnson
syndrome www.indiandentalacademy.com

Interactions :
 Sulfonamides, tolbutamide, warfarin,
imipramine & methotrexate
 Anticoagulants
 Phenytoin & tolbutamide
Uses :
Rheumatoid
arthritis
Ankylosing
spondylitis
Rheumatic
fever
Acute gout
Severe
cases
Zolandin
P  L 

 Oxyphenbutazone
 Metamizol (Dipyrone) : 0.5-1.5 g
 Propiphenazone : 300-600 mg TDS
INDOLE DERIVATIVES
Indomethacin
Pharmacokinetics
 90% bound to plasma
proteins.
 Plasma t ½ = 2-5 hrs.
 Dose 25-50mg BD/QID
Sioril, phenabid
Analgin, novalgin
Saridon, anafebrin

Adverse effects
Interactions :
 Furosemide
 Thiazides, furosemide, β
blockers, ACE inhibitors
 Warfarin www.indiandentalacademy.com

Uses :
Rheumatoid
arthritis
Ankylosing
spondylitis
Psoriatic
arthritis
Acute gout
Acu. Exa.
destructive
arthropathies
Malignancy
asso. fever
Patent ductus arteriosus
closure (0.1/0.2 mg/kg/12 hrly
P  L 
Indicin, indocap

PROPIONIC ACID DERIVATIVES
Pharmacokinetics
 90-99% bound to plasma proteins.
Drug Plasma t ½ Dosage
Ibuprofen 2 hr 400-800 mg TDS Brufen, emflam
Naproxen 12-16 hr 250 mg BD/TDS Xenobid, naxid
Ketoprofen 2-3 hr 100 mg BD/TDS Ketofen
Fenoprofen 2-4 hr 300-600 mg TDS Arflur
Flurbiprofen 4-6 hr 50 mg BD/QID Flurofen

Adverse effects
Interactions :
 Anticoagulants
 Furosemide, thiazides &
β blockers

Uses :
Analgesic
Antipyretic
Dysmenorrhoea
ANTHRANILIC ACID DERIVATIVE (Fenamate)
Mephenamic acid
Pharmacokinetics
 Highly bound to plasma
proteins.
 Plasma t ½ = 2-4 hrs
 250-500 mg TDS www.indiandentalacademy.com

Adverse effects
Uses :
Analgesic Osteoarthritis
DysmenorrhoeaRheumatoid
arthritis
Medol, meftal, ponstan
L 

ARYL-ACETIC ACID DERIVATIVES
Diclofenac sodium :
Pharmacokinetics
 Plasma t ½ = 2 hrs
 50 mg TDS/BD, 75 mg i.m.
Adverse effects

Uses :
Ankylosing
spondylitis Osteoarthritis
Dysmenorrhoea
Rheumatoid
arthritis
Bursitis Post-traumatic / post-op
inflammatory condition
Tolmetin : 400-600 mg TDS
Voveran, diclonac, movonac

OXICAM DERIVATIVES
Piroxicam
Pharmacokinetics
 Plasma t ½ = 2 days
 20 mg BD / 20 mg OD
Adverse effects

Uses :
Ankylosing
spondylitis
Osteoarthritis
Dysmenorrhoea
Rheumatoid
arthritis
Acute gout
Musculoskeletal injuries
Dentistry
Episiotomy
Tenoxicam : 20 mg OD
Meloxicam : 7.5-15 mg/day (rheumatoid & osteo-arthritis)
Dolonex, pirox, piricam, toldin
P  L 
Melflam, Meloxi

PYRROLO-PYRROLE DERIVATIVE
Ketorolac :
Pharmacokinetics
 Highly bound to plasma proteins.
 10-20 mg / 6 hrly (orally)
Adverse effects

Uses :
Post-op / acute
musculoskeletal pain
(15-30 mg i.m. / 4-6 hrs
Renal colic
Bony
metastasis
Migraine
SULFONANILIDE DERIVATIVE
Nimesulide :
Pharmacokinetics
 100 mg BD
Ketorol, torolac

Adverse effects
Uses :
Bursitis
Sports injuries
Dental surgery
ENT disorders
Low backacheDysmenorrhoea
Post-op
pain/osteoarthritis
Nimulid, nimodolwww.indiandentalacademy.com

PARA-AMINO PHENOL DERIVATIVES
• Phenacetin 1887
• Paracetamol (acetaminophen) 1950
Actions
Pharmacokinetics
 1/3 bound to plasma proteins.
 3-5 hrs (orally)
 0.5-1g TDS
 Infants - 50 mg
 Children 1-3 yrs- 80-160 mg
4-8 yrs 240-320 mg
9-12 yrs 300-600 mg

Adverse effects
Analgesic nephropathy
Acute paracetamol poisoning
 150 mg/kg
 Fatality > 250 mg/kg
 Early manifestations / 12-18 hrs / 2 dayswww.indiandentalacademy.com

 Mechanism of toxicity
 Treatment –
• Gastric lavage
• N-acetylcysteine 150 mg/kg / i.v./ 15 min / 20 hrs
• 75 mg/kg / orally / 4-6 hrs / 2-3 days
Uses :
‘Over the
counter’ analgesic
Musculoskeletal
pain
Dysmenorrhoea
Antipyretic
Crocin, metacin, paracinwww.indiandentalacademy.com

BENZOXAZOCINE DERIVATIVE
Nefopam
30-60 mg TDS oral
20 mg i.m. 6 hrly
CHOICE OF NSAIDS
• Mild to moderate pain – paracetamol, ibuprofen
• Acute musculoskeletal, osteoarthritic, injury associated
inflammation – ibuprofen, diclofenac, piroxicam
• Post-op / acute / short lasting painful condition – ketorolac,
nefopam
Nefomax

• Exacerbation of rheumatoid arthritis, ankylosing
spondylitis, acute gout, acute rheumatic fever – aspirin,
indomethacin, naproxen, piroxicam
• Asthma or anaphylactoid reactions to aspirin – nimesulide

Analgesics after certain endodontic procedures

PAIN MANAGEMENT STRATEGY
3D
iagnosis
efinitive Rx
rugs
Definitive treatment :
•Pulpotomy, pulpectomy
•Extraction
•Incision & drainage
Drug :
•Pretreat with NSAIDs
•Prescribe by clock
•Long acting LA
•Flexible prescription plan

Flexible analgesic prescription plan
Aspirin like drugs
indicated
Aspirin like drugs contra
indicated
Ibuprofen 200 mg
Acetaminophen 600-1000mg
NSAIDs (alone max.effective
dose) OR NSAID +
acetaminophen
Acetaminophen 600-1000
mg + codine 60 mg
Ibuprofen 400 mg/4 hrly and
equivalent of acetaminophen
600 mg / codine 60 mg 4 hrly
Acetaminophen 1000 mg with
equivalent of oxycodone 10
mg
NSAID (max. dose) &
acetaminophen / oxycodone
10 mg combination
Mild
pain
Moderate
pain
Severe
pain www.indiandentalacademy.com

ADVANCES
Selective cox-2 inhibitors :
Celecoxib, rofecoxib, valdecoxib, etoricoxib, meloxicam,
diisopropyl flurophosphate.
Action
Celecoxib P© L©
Use-osteoarthritis, rheumatoid arthritis
Dose – 200 mg / day OD or 100 mg BD.
Commercial names – Celebrex, Celib, Celfast, Celact etc.
Banned – July 2001
Rofecoxib P© L©
Dose – 12.5 mg OD (max. dose 25 mg)
Commercial name – Vioxx, Dolib MD, Roff, Rofaday
Banned – September 2004

Valdecoxib
Dose – 10-20 mg OD
Commercial name – Valed, Valus, Vorth, Bextra
Banned –7 April 2005.
Other drugs banned by FDA
 Benoxaprofen
 Phynylbutazone
 Oxyphenbutazone
 Saprofen
 Piroxicam www.indiandentalacademy.com

REFERENCES :
1) Effectiveness of prophylactic use of refecoxib is comparison
with ibuprofen on postendodontic pain. JOE. Jan 2003, Vol.
29, No. 1, pg. 62-64.
2) Evaluation of meloxicam (cox-2 inhibitor) for management
of post operative endodontic pain – A double blind placebo
controlled study. JOE, Oct 03, Vol. 29, No. 10, Pg. 634-637.
3) The efficacy of pain control following nonsurgical root canal
treatment using ibuprofen in a combination of ibuprofen
and acetaminophen in a randomized, double-blind, placebo
controlled study. IEJ, 2004, Vol. 37, Pg. 531-541.www.indiandentalacademy.com

CONCLUSION

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NSAIDS

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