NSAIDs / Orthodontic Courses by Indian Dental Academy

INDIAN DENTAL ACADEMY
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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
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.
CLASSIFICATION
(Acc. to Tripathi)
A. Analgesic and antiinflammatory :
Aspirin, Salicylamide, Benorylate, Diflunisal
Salicylates
Phenylbutazone, oxyphenbutazone
Pyrazolone derivatives
Indomethacin, sulindac
Indole derivatives
Ibuprofen,Naproxen, Ketoprofen, Fenoprofen,
Flurbiprofen.
Propionic acid derivatives
Mephenamic acid
Anthranilic acid derivative
Diclofenac, Tolmetin
Aryl-acetic acid derivatives
Piroxicam, Tenoxicam, Meloxicam.
Oxicam derivatives
Ketorolac.
Pyrrolo-pyrrole derivative
NImesulide
Sulfonanilide derivative
Nabumetone
Alkanones
B. Analgesic but poor antiinflammatory:
Paracetamol (Acetaminophen)
Paraaminophenol derivative
Metamizol (Dipyrone), propiphenazone
Pyrazolone 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
Acetaminophen
Para amino derivatives
Indomethacin, sulindac
Indole & 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 = 15-20 min.
Release salicylic acid (t ) = 3-5
hrs.
Antiinflammatory doses (t ) =
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.
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 individuals
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, colosprin
PYRAZOLONES
Phenylbutazone
Pharmacokinetics
Plasma t = 60 hrs.
Dose 100-200 mg BD/TDS
Adverse effects
Bone marrow
depression
Agranulocytosis
Stevens-Johnson
syndrome
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 = 2-5 hrs.
Dose 25-50mg BD/QID
Sioril, phenabid
Analgin, novalgin
Saridon, anafebrin
Adverse effects
Interactions :
Furosemide
Thiazides, furosemide,
blockers, ACE inhibitors
Warfarin
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 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 &
blockers
Uses :
Analgesic
Antipyretic
Dysmenorrhoea
ANTHRANILIC ACID DERIVATIVE (Fenamate)
Mephenamic acid
Pharmacokinetics
Highly bound to plasma
proteins.
Plasma t = 2-4 hrs
250-500 mg TDS
Adverse effects
Uses :
Analgesic
Osteoarthritis
Dysmenorrhoea
Rheumatoid
arthritis
Medol, meftal, ponstan
L
ARYL-ACETIC ACID DERIVATIVES
Diclofenac sodium :
Pharmacokinetics
Plasma t = 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 = 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.
Plasma t = 5-7 hrs
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
Plasma t = 2-5 hrs
100 mg BD
Ketorol, torolac
Adverse effects
Uses :
Bursitis
Sports injuries
Dental surgery
ENT disorders
Low backache Dysmenorrhoea
Post-op
pain/osteoarthritis
Nimulid, nimodol www.indiandentalacademy.com
PARA-AMINO PHENOL DERIVATIVES
Phenacetin 1887
Paracetamol (acetaminophen) 1950
Actions
Pharmacokinetics
1/3 bound to plasma proteins.
Plasma t = 2-3 hrs
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 days
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, paracin
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
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
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.
CONCLUSION

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