Nsai ds /certified fixed orthodontic courses by Indian dental academy

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

Good
Morning

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 :
Salicylates

Aspirin, Salicylamide, Benorylate, Diflunisal

Pyrazolone derivatives

Phenylbutazone, oxyphenbutazone

Indole derivatives

Indomethacin, sulindac

Propionic acid derivatives

Ibuprofen,Naproxen, Ketoprofen, Fenoprofen,
Flurbiprofen.

Anthranilic acid derivative

Mephenamic acid

Aryl-acetic acid derivatives

Diclofenac, Tolmetin

Oxicam derivatives

Piroxicam, Tenoxicam, Meloxicam.

Pyrrolo-pyrrole derivative

Ketorolac.

Sulfonanilide derivative

NImesulide

Alkanones


Nabumetone

B. Analgesic but poor antiinflammatory:
Paraaminophenol derivative

Paracetamol (Acetaminophen)

Pyrazolone derivatives

Metamizol (Dipyrone), propiphenazone

Benzoxazocine derivative

Nefopam

Acc. to Goodman and Gillman
A. Non selective Cox inhibitor
Salicylic acid derivatives

Aspirin, sodium salicylate, choline magnesium
trisalicylate, salsalate, diflunisal, salfasalazine,
olsalazine.

Para amino derivatives

Acetaminophen

Indole & indene acetic acid

Indomethacin, sulindac

Heteroaryl acetic acid

Tolmetin, diclofenac,

ketorolac.

Aryl propionic acid

Ibuprofen, naproxen, flurbiprofen, ketoprofen,
fenoprofen, oxaproxin.

Anthranilic acid (fenamates)
Enolic acid

Mefenamic acid, meclofenamic acid
Oxicams (piroxicam, Meloxicam)

Alkanones

Nabumetone.

B. Selective cox-2 inhibitor
Diaryl substituted furanones
Diaryl substituted
Pyrazoles
Indole acetic acid
Sulfonanilides

Rofecoxib
Celecoxib
Etodolac
Nimesulide


MECHANISM OF ACTION
Odontogenic pain
Noxious stimuli
Disease process
+
Surgical intervention

Acute pain
Tissue destruction or injury
Cellular destruction
Release / synthesis of histamine /
prostaglandin / bradykinin
+
Peripheral nociceptor / free nerve
endings
PAIN

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
Anaphylactoid
reactions

Antipyresis
Antiinflammatory

Renal effects

Dysmenorrhoea

Gastric mucosal
damage
Parturition

Ductus
arteriosus
closure


Antiplatelet
aggregatory

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
 <2g/day

• Blood

 2-5 g/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.

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 :

Patent ductus
arteriosus

Analgesic

Pregnancy induced
hypertension and
preeclampsia

Antipyretic

Acute rheumatic
fever (4-6 g)

Postmyocardial
infarction &
poststroke patients

Delay labour

Rheumatoid
arthritis (3-5 g)

Osteoarthritis

* Aspirin, dispirin, colosprin

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


Interactions :
 Sulfonamides, tolbutamide,
imipramine & methotrexate

warfarin,

 Anticoagulants
 Phenytoin & tolbutamide
P L

Uses :

Rheumatic
fever

Severe
cases

Acute gout
Ankylosing
spondylitis
Zolandin


Rheumatoid
arthritis

Sioril, phenabid

 Oxyphenbutazone
 Metamizol (Dipyrone) : 0.5-1.5 g

Analgin, novalgin

 Propiphenazone : 300-600 mg TDS

Saridon, anafebrin

INDOLE DERIVATIVES
Indomethacin
Pharmacokinetics
 90% bound to plasma
proteins.
 Plasma t ½ = 2-5 hrs.
 Dose 25-50mg BD/QID

Adverse effects

Interactions :
 Furosemide
 Thiazides, furosemide, β
blockers, ACE inhibitors
 Warfarin


Uses :

P L
Psoriatic
arthritis

Rheumatoid
arthritis
Ankylosing
spondylitis

Acute gout

Malignancy
asso. fever

Acu. Exa.
destructive
arthropathies
Patent ductus arteriosus
closure (0.1/0.2 mg/kg/12 hrly
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 :
Antipyretic
Analgesic
Dysmenorrhoea

ANTHRANILIC ACID DERIVATIVE (Fenamate)
Mephenamic acid
Pharmacokinetics
 Highly bound to plasma
proteins.
 Plasma t ½ = 2-4 hrs
 250-500 mg TDS


Adverse effects

L

Uses :

Osteoarthritis

Analgesic
Rheumatoid
arthritis

Dysmenorrhoea
Medol, meftal, ponstan

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

Rheumatoid
arthritis

Bursitis

Dysmenorrhoea

Post-traumatic / post-op
inflammatory condition

Voveran, diclonac, movonac

Tolmetin : 400-600 mg TDS

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


Uses :

P L

Ankylosing
spondylitis

Osteoarthritis

Rheumatoid
arthritis

Dysmenorrhoea
Dentistry

Acute gout
Episiotomy

Musculoskeletal injuries

Dolonex, pirox, piricam, toldin
Tenoxicam : 20 mg OD
Meloxicam : 7.5-15 mg/day (rheumatoid & osteo-arthritis)

Melflam, Meloxi

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


Uses :
Renal colic

Bony
metastasis

Migraine

Post-op / acute
musculoskeletal pain
(15-30 mg i.m. / 4-6 hrs

Ketorol, torolac
SULFONANILIDE DERIVATIVE
Nimesulide :
Pharmacokinetics
 100 mg BD


Adverse effects

Uses :
Sports injuries

Dental surgery

ENT disorders
Bursitis
Low backache

Dysmenorrhoea
Post-op
pain/osteoarthritis

Nimulid, nimodol

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 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

Antipyretic

Dysmenorrhoea

Musculoskeletal
pain
Crocin, metacin, paracin

BENZOXAZOCINE DERIVATIVE
Nefopam
30-60 mg TDS oral
20 mg i.m. 6 hrly
Nefomax

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


• 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

D

3

iagnosis
efinitive Rx
rugs

Definitive treatment :

Drug :

•Pulpotomy, pulpectomy

•Pretreat with NSAIDs

•Extraction

•Prescribe by clock

•Incision & drainage

•Long acting LA
•Flexible prescription plan

Flexible analgesic prescription plan
Mild
pain

Aspirin like drugs
indicated
Ibuprofen 200 mg

Moderate
pain

NSAIDs (alone max.effective
dose) OR NSAID +
acetaminophen

Aspirin like drugs contra
indicated
Acetaminophen 600-1000mg
Acetaminophen 600-1000
mg + codine 60 mg

Ibuprofen 400 mg/4 hrly and
equivalent of acetaminophen
600 mg / codine 60 mg 4 hrly

Severe
pain

NSAID (max. dose) &
Acetaminophen 1000 mg with
acetaminophen / oxycodone
equivalent of oxycodone 10
10 mg combination
mg

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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Nsai ds /certified fixed orthodontic courses by Indian dental academy

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