Nsaid Tanveer-Final (NXPowerLite) / Orthodontic Courses by Indian Dental Academy

INDIAN DENTAL ACADEMY
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USE OF STEROIDAL & NON-
STEROIDAL ANTI-INFLAMMATORY
DRUGS IN ORAL AND MAXILLOFACIAL
SURGERY PATIENTS

MODERATOR: Dr.Preetham Shetty
PRESENTER: Dr.Tanveer.Ahmed
CONTENTS
1. INTRODUCTION
2. IMPORTANCE OF INFLAMMATION
3. DEFINITION
4. MEDIATORS OF INFLAMMATORY
PROCESS
5. CLASSIFICATION OF NSAIDS
6. INDIVIDUAL DRUGS
7. SELECTIVE COX-2 INHIBITORS
8. CONCLUSION
9. REFRENCES
IMPORTANCE OF INFLAMMATION
DEFINITION OF INFLAMMATION
As per Ebert & Grant Inflammation is a
process that begins following sub lethal
injury to tissue and ends with permanent
destruction of tissue or with complete
healing.
FUNDAMENTAL EVENTS IN
INFLAMMATION
1. Increased permeability of the micro
vasculature.
2. Accumulation and activation of
Leucocytes.

MEDIATORS OF
INFLAMMATORY PROCESS
MAJOR GROUPS
TISSUE
Lymphocyte products

Macrophage products

Mast Cell products

MAJOR MEDIATORS

Interferon
Interleukins
Skin reactive factor

TNF-
PAF

Histamine
Cytokines
Prostaglandin D
2
Eosinophil Products

PLASMA
Kinin System
Complement System

Clotting System

Lysosomal Enzymes
Major Basic proteins
Leukotrienes

Bradykinin
C
3
fragments
C
5
fragments
Fibrinopeptides
Fibrin Degradation
products
HOW NSAIDS WORKS
Interfering with cycloxygenase pathway
Process begins with AA-a dietary 20 carbon poly
unsaturated fatty acid obtained from animal fat
AA is liberated from membrane phospholipids by the
action of phospholipase A2.
Free AA is metabolically transformed through either
cycloxygenase or lipoxygenase pathway
When AA is enzymatically oxidized by cycloxygenase it
forms unstable intermediates(PGG2 and PGH2) leading to
prostanoid synthesis
By the action of lipoxygenase,AA forms leukotrienes
This process is referred to as arachidonic acid cascade

ARACHIDONIC ACID
Lipooxygenase COX-1
COX-2
Prostaglandin Throboxanes
Gastric
protection
uterine
contraction,
renal function
Platelet
Aggregation
Leukotrienes
Bronchospasm
Inflammation
prostaglandins
Pain inflammation, renal
function
Tissue damage
Cox-1 And Cox-2
Cox-1(constitutive)
-House keeping function
- For blood clotting
- For kidney function
- For stomach protection
Cox-2 (induced) contributes:
- Pain
- Heat
- Swelling www.indiandentalacademy.com
CLASSIFICATION OF NSAIDS
A. ANALGESIC AND ANTI INFLAMMATORY
1. Salicylates : Aspirin, Salicylamide, Diflunisal.
2. Pyrazolone : Phenylbutazone, Oxyphenbutazone.
3. Indole Derivatives : Indomethacin,Sulindac.
4. Propionic acid derivatives : Ibuprofen,Naproxen,
Ketoprofen, Fenoprofen.
5. Anthranilic Acid derivative : Mephenamic acid.
6. Aryl acetic acid derivative : Diclofenac,Tolmetin.
7. Oxicam derivative : Piroxicam, Tenoxicam, Meloxicam.
8. Pyrrolo Pyrrole derivative : Ketorolac.
9. Sulfonanilide derivative : Nimesulide.
10. Alkanones : Nabumetone.
B. ANALGESIC BUT POOR ANTI-
INFLAMMATORY
1. Para- aminophenol derivative : Paracetamol
(Acetaminophen).
2. Pyrazolone derivative : Metamizol (Dipyrone)
propiphenazone.
3. Benzoxazocine derivative : Nefopam.

SALICYLATES
ASPIRIN
ACTIONS:- 1
i. Analgesic, Anti- pyretic and Anti-inflammatory.
ii. Weaker analgesic than morphine type drugs.
iii. Analgesic action is mainly due to obtunding of
peripheral pain receptors and prevention of PG
mediated sensitization of nerve endings.
iv. It resets the hypothalamic thermostat and rapidly
reduces fever by promoting heat loss but does not
decrease heat production.
2. Aspirin and released Salicylic acid irritates
gastric mucosa causes epigastric distress,
nausea, vomiting.
3. It interferes with platelet aggregation and
bleeding time is prolonged to nearly twice the
normal.
- Absorbed from stomach and small intestine.
- Slowly enters brain and freely crosses placenta.

Effects of NSAIDS on upper GIT
Contraindications to the use of
Aspirin and other salicylates:

Disease state Possible adverse effect
1 Ulcer Internal Bleeding,possible
hemorrhage
2 Asthama Asthmatic attack
resembling allergic
reaction.
3 Diabetes low doses may cause
hyperglycemia .
high doses may cause
hypoglycemia.

Adverse effects:

1. Analgesic dose nausea, vomiting, epigastric
distress and increased blood loss in stools.
2. Hypersensitivity and Idiosyncrasy.
3. Inflammatory doses- produce syndrome called
Salicylism .
4. Acute Salicylate poisoning more common in
children causes vomiting, dehydration ,
electrolyte imbalance, delirium,
hallucinations,convulsions, and death.
USES
1. Analgesic- for headache, backache, myalgia,
joint pain, neuralgias,etc.low dose .3 to .6 gm
sixth hourly.
2. Antipyretic- effective in fever of any origin.
3. Acute rheumatic fever- It is the first drug to be
used in all cases.
4. Rheumatoid arthritis- It is the first drug to be
tried.Produces relief of pain, swelling, and
morning stiffness.
5. Other conditions: Osteoarthritis, post myocardial
infarction and post stroke patients.
Precautions:

Should be stopped a week before elective
surgery.
Should be avoided during pregnancy,
lactation.
Should be avoided in chronic liver diseases
and in patients with bleeding tendencies.
Pyrazolones:

Phenylbutazones:
1. Inhibits Cox and is more potent Anti
inflammatory.
2. Analgesic and anti-pyretic effect ois poor and
slower in onset.
3. Causes definite retention of Na and water by
direct action on renal tubules-edema,which
occurs after 1-2weeks of use.
4. Completely absorbed orally and completely
metabolised in liver.
Adverse effects;
More toxic than Aspirin

Nausea,vomitting,epigastric distress, and
epigastric ulceration are common.
edema is a major limitation for use for more than
1-2 weeks.
Hypersensitivity reactions like rashes,serum
sickness and stomatitis.
Bone marrow depression, agranulocytosis and
Steven-Johnsons syndrome are more serious.
Indole derivatives:
Indomethacin:
Water insoluble , and soluble in common organic slovents.
Actions:
Analgesic and potent anti-inflamatory and anti pyretic
action.
inhibits PG synthesis as well as phospho- diesterase thus
increasing cyclic AMP intracellularly.
Also interferes with migration of leukocytes to inflammatory
cells
Absorbed orally reaching peak plasma levels in one and half
hours.
Clinical use:
Rheumatoid Arthritis and associated disorders.
Ankylosing spondylitis.
Gout.
Neurovascular headache.
Malignancy associated fever refractory to other
anti-pyretic.
Most commonly used drug for closure for closure
of PDA.
Propionic Acid Derivatives:
Ibuprofen:
Actions similar to Aspirin but are better
tolerated orally although they may produce
gastric irritation and ulceration.
Highly bound to plasma protiens- 90 99%
Metabolised in liver.
Interactions/Contraindications
1 should be avoided with anti-coagulants as
they inhibit platelet funtions
2 Not to be prescribed during pregnancy and
peptic ulcer patients.
3 Contra indicated in indivisuals with nasal
polyps, angioedema and bronchospasmic
activity to aspirin.
Anthranilic Acid derivative:
Mefenamic acid
Actions: weaker analgesic than aspirin.
Inhibits PG synthesis.
Exerts peripheral as well as central
analgesic activity.

Clinical use:
Dull aching pain.
Indicated primarily as an analgesic in
muscle,joint and soft tissue pain-where
strong anti-inflammatory action is not
needed.

Adverse effects

Nausea,vomitting,epigastric distress, and
epigastric ulceration are common.
Dizziness,headache,skin rashes,heamolytic
anemia and blood dyscrasias.

ArylAcetic acid derivatives:
Diclofenac,Tolmetin
Actions:
Newer analgesics and antipyretic and anti-
inflammatory drug.
Inhibits PG synthesis and short lasting antiplatelet
action.
Concentration in synovial fluid is three times more
than in plasma.
Well absorbed orally.
Plasma t1/2-2hrs

Clinical use:
Osteoarthritis,Rheumatoid
arthritis,ankylosing spondylitis,bursitis.
Post traumatic and post-op inflammatory
conditions-affords quick relief of pain and
wound edema.

Oxicam derivatives
piroxicam
Actions:
lowers PG concentrations in synovial fluid.
Produces ratio of T-helper to T-supressor
lymphocytes.
Inhibits platelet aggregation thus prolongs
bleeding time.
Half life-28-45hrs.
Pyrolo-pyrrole derivatives
ketorolac:
Actions;
Highly potent member of a new class of analgesic
compound.
Has both anti-inflammatory and anlgesic property but is
more systemic analgesic then anti-inflammatory.
More potent than indomethacin andphenylbutazone.
Inhibits PG synthesis and is believed to relieve pain by
peripheral mechanism.
In post-op pain it has equal efficacy of morphine.
Excreted in urine-90% unchanged.

Uses:
Frequently used in post op and acute
musculo-skeletal pain
May also be used for renal colic, migraine
and pain due to bone metastasis.
Should not be given in patients on anti-
coagulants.
Sulfonanilide derivatives:
nimesulide:

Selective for Cox-2.
Can be given for asthamatics.
Newer NSAID and is a relatively weaker
inhibitor of PG synthesis.
Completely absorbed orally and is excreted
in urine.

Uses:
Primarily in short lasting painful
inflammatory conditions like sport
injuries,sinusitis,other ENT disorders,dental
surgeries,bursitis,low back ache and post op
pain.
Nimesulide is safe (Hindustan Times-13
th

Jan 2003)
ParaAminoPhenol derivatives
paracetamol(acetaminophen)
Action:
Central analgesic action is similar to Aspirin but
negligible anti-inflammatory action.
Good and promptly acting anti-pyretic.
Doest not affect platelet function.
No effect on CVS,and rare gastric irritation.
Well absorbed orally,uniformly distributed in
body and excreted rapidly in urine.
Plasma t1/2- 2-3hrs.
Adverse effects:
In isolated anti-pyretic doses , it is safe and
well tolerated.
Nausea and rashes occur rarely.
Analgesic nephopathy occurs after years of
heavy ingestion of the drug.
Acute paracetamol can occur specially in
small children who have low hepatic
glucoronide conjugating ability.
Acute Paracetamol poisoning
Occurs if a large dose of more than 150mg/kg is
taken.
Fatality is common with more than 250mg/kg.
Early manifestations are nausea,vommiting,
abdominal pain and liver tenderness with no
impairment of conciousness.
After 12-18hrs centri-lobular hepatic necrosis
occurs.
Hypoglycemia may progress to coma.]
Jaundice occurs after 2 days.

Treatment:

If patient is brought early, vomiting should
be induced or gastric lavage done.
Activated charcoal is given orally or
through tube to prevent further absorption.
Specific:
N-Acetyl Cysteine 150mg/kg should be
infused iv over 15mins followed by the
same dose iv over the next 20hrs.
SELECTIVE COX2 INHIBITORS
First generation
- Celecoxib and rofecoxib
Second generation
- Valdecoxib
CELECOXIB
First selective cox2 inhibitor to be approved by
FDA
Launched in 1999
Exerts potent anti inflammatory analgesic and
anti-pyretic action with low ulcerogenic potential
Time action and peak analgesic effort is approx.
half than that of ibuprofen 600mg.

ADVERSE EFFECTS
Mild diarrhoea
Abdominal pain
Dyspepsia
DOSAGE
100-200mg BD
Celecoxib is effective for cancer prevention in
people with familial adenomatous polyposis
Celecoxib is the only drug that is approved
by USA-FDA for the treatment of familial
adenomatous polyposis
Rofecoxib-selective cox2 inhibitor
Reported to be more selective cox2 inhibitor than
celecoxib using in-vitro assays
Greater analgesic effect than celecoxib
800 times more selective for cox2 than cox1
Half life 17 hr
DOSAGE
50 mg OD
VALDECOXIB
Has quicker action than rofecoxib
Administration of valdecoxib resulted in better
pain relief and lower pain intensity as compared to
rofecoxib
DOSAGE
20mg BD
DRUGS IN THE PIPELINE
PARECOXIB
- An injectable product of valdecoxib used for
managing severe acute pain including post op pain
-Parecoxib 40mg and 80 mg is effective and safe
for treating post op pain
ETORICOXIB
- Currently being reviewed by FDA
- Highly selective for cox2
REFERENCES
Essentials of medical pharmacology fourth edition
K.D.TRIPATHI
Principles of medical pharmacology fifth edition
KALANT
Pharmacology-fourth edition
DALE,RANG AND RITTER
Basic and clinical pharmacology
BERTRAN AND KATZUNG
Dental therapeutic update october 2002


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