Analgesic Used in Oral Surgery

ANALGESICS
Assistant Professor. Akram Thabet Nasher

B.D.S., M. Sc. ,Ph.D
Analgesic drugs
An analgesic (known as painkiller) drugs: is a drug

or preparation that will reduce or eliminate pain
without loss of consciousness.
Patients should be encouraged to use analgesics

before pain becomes severe and difficult to
control.
Dr. Akram Nasher Analgesic Drugs

Pain
It is an unpleasant sensory and emotional experience
arising from actual or potential tissue damage .
Most dental procedures produce tissue trauma and
release potent mediators of inflammation and pain.

Classification of Pain By Onset and Duration
Acute pain
 Sudden in onset
 Usually subsides once treated
Chronic pain
 Persistent or recurring
 Often difficult to treat

Odontogenic pain
The most common types of odontogenic pain are characterized as

acute pain.
• Acute pain is accompanied by some recognizable evidence of
tissue injury or inflammation, and it resolves spontaneously once
the underlying cause is definitively treated.
• Example of causes of acute pain:
– Inflamed pulp,
– Abscessed tooth,
– Carious lesion
 Objective autonomic phenomenon
Responds to treatment – NSAIDs , opioids , corticosteroids,

benzodiazepines
Chronic pain
• Chronic pain often lasts months or years

beyond the precipitating event, and there is rarely a
readily identifiable source, that is, an area of tissue
destruction or inflammation. ( no insult is identified)
• Vague descriptions of pain, difficulty in describing

timing and localization.

PAIN MANAGEMENT
 Pharmacological therapy
 Injection therapy (Local anesthesia, steroids)
 Exercise therapy
 Physical medicine
 Behavioral medicine
 Complementary & alternative medicine
 Intravenous therapy
 Surgical therapy

Classification of analgesic drugs
 Analgesic drugs can be classified into:

A- Nonopioid, nonnarcotic
1. Nonsteroidal anti-inflammatory drugs(NSAIDs)
a. Non-selective (aspirin, ibuprofen)
b. Selective (COX-2) NSAIDs (Rofecoxib)
2. Antipyretic analgesics (acetominophen)
B- Opioid narcotic (morphine)
C- Substances with mixed mechanism of action

(opioid and non-opioid components) such as: tramadol.
Classification of Analgesics
Analgesics
Mild Strong
Analgesics Analgesics
Aspirin Ibuprofen Opium Heroin
Codeine
Acetaminophen
I-Nonsteroidal anti inflammatory
drugs (NSAIDs)

Mechanism of action :
• NSAIDs work by inhibiting cyclooxygenase

(COX), an enzyme which catalyzes conversion
of arachidonic acid to prostanoids ( pain
mediators ) .
NSAIDs are reversible inhibitors of

cyclooxygenase (COX) enzyme except
aspirin is irreversibly inactivate COX.

Cyclooxygenase enzyme (COX)
 Two different COX enzymes existed, known as

COX-1 and COX-2.
 Cyclooxygenase-1 (COX-1) is known to be present
in most tissues (constitutive).
- In the gastrointestinal tract, COX-1 maintains
the normal lining of the stomach.
- The enzyme is also involved in kidney and
platelet function.
 Cyclooxygenase-2 (COX-2) is primarily present at
sites of inflammation (inducible).

COX Enzyme: Prostaglandin Effects
COX-1: beneficial COX-2: harmful

Peripheral injury Inflammation
site
Brain Modulate pain
perception
Promote fever
(hypothalamus)
Stomach protect mucosa
Platelets aggregation
Kidney vasodilation
Mechanism of action of (NSAIDs) analgesics
1- Depression of cyclooxygenases activity
2-Decreasing of prostaglandins synthesis in peripheral

tissues and in central nervous system
3-Decreasing of sensitivity of nervous endings and

depression of transmission of nociceptive impulses on
the level of CNS structures
4- Pain-relieving action of non-opioid analgesics is

partly connected with their anti-inflammatory activity
NSAIDs: Therapeutic Effects
1. Analgesic (mild to moderate)

2. Anti-inflammatory
3. Antipyretic
4. Relief of vascular headaches
5. Platelet inhibition (Aspirin)

Applications in Dentistry
• Toothache
• Post extraction pain
• Periodontitis
• Neuritis
• Stomatitis
• Arthritis
• Local usage as keratoplatic
agents for hyperkeratosis,
hyperesthesia

A- Selective Cox-2 Inhibitors
• Greater affinity for cyclooxygenase-2
• Decreased incidence of negative effects associated

with non-selective COX-inhibitors
Ex. Celecoxib

Celecoxib
General Info:
◦ Cox-2 specific inhibitor
◦ Usually used for arthritis pain
 Dental Use:
◦ Recently approved for acute pain
Formulation:
◦“Celebrex”
Dose:
◦ 100-200mg BID
 Side Effects: Renal/Hepatotoxicity
 Contraindications: ◦ Sulfa Allergy

◦ Asthma
◦ Hepatic/Renal impairment

Other COX 2 inhibtors
Etoricoxib “Arcoxia”,
Parecoxib
Lumiracoxib

b- Non-Selective Cox Inhibitors NSAIDs
1- Carboxylic Acids : Acetylated - aspirin (ASA)
2- Acetic Acid:
Diclofenac sodium (Voltaren)
Diclofenac potassium (Cataflam)
Etodolac
Indomethacin
3- Propionic Acids
Ibuprofen
ketoprofen
ketorolac
Naproxen

1- Aspirin (acetylsalicylic acid)
 Mechanism of action:
It can cause irreversible
inactivation of
cyclooxygenase, acting on
both COX-1 and COX-2.

Aspirin :Pharmacologic effects
In the addition of the analgesic effect of the aspirin it has other

effects:
1- Gastrointestinal effects:
(a) It can cause epigastric pain, nausea, and vomiting by :
1- irritating the gastric mucosal lining.
2- stimulating the chemoreceptor trigger zone (vomiting center) in
the CNS.
(b) It may cause a dose-related gastric ulceration, bleeding, and
erosive gastritis because of inhibiting the formation of PGE2, which
inhibits gastric acid secretion and has a cytoprotective effect.
• Salicylate-induced gastric bleeding is painless and may lead to an
iron deficiency anemia.

2- Hepatic effects:
• Dose-dependent hepatic damage.
• Usually, asymptomatic
• Elevated plasma transaminase levels (liver enzyme)
are the key indication of hepatic injury.
• More severe and associated with encephalopathy

seen in Reye’s syndrome.
 Use of salicylates in children with chickenpox or

influenza is contraindicated to avoid Reye’s
syndrome.

Reye's syndrome is a potentially fatal disease that
has numerous detrimental effects to many organs,
especially the brain and liver, as well as causing a
lower than usual level of blood sugar (hypoglycemia).
The classic features are a rash, vomiting, and liver
damage. The exact cause is unknown and, while it
has been associated with aspirin consumption by
children with viral illness, it also occurs in the
absence of aspirin use.

3- Hematologic effects:
• It inhibits the platelet aggregation by decreasing
the production of TXA2 causing prolongation of
bleeding time or decrease prothrombin level.
4-- Salicylism: usually occurs with repeated

administration of large doses.
Characteristic findings include:
headache, tinnitus and difficulty in hearing.

Aspirin : Contraindication
1- Salicylates are NOT to be given to children under

age 12 with fever due to viral infection because of the
risk of Reye’s syndrome.
2- Peptic ulcer
3- Bronchial asthma
4- Blood disease (hemophilia)

 Formulation:
◦ “Aspirin” et al.
 Dose:
◦ 650-1000 mg q4h

2- Propionic Acids (Ibuprofen)
• Ibuprofen, has demonstrated analgesic activity over a

dose range from 200 to 800 mg, with a duration of
activity from 4 to 6 hrs.
• When given prior to pain onset, it suppresses the

onset of pain and lessens its severity.
• lbuprofen suppresses swelling over the initial two- to

three-day post-operative course, when edema formation
associated with the inflammatory process is most
prominent.
General Info of Ibuprofen
 Cyclooxygenase inhibitor of PGs

 Inhibits WBC migration
 Serum half life 2h
 Heavily plasma protein bound
 Dose:
◦ 400 – 600 mg q4-6h
x (RARELY 800 mg)
◦ Max 3200 mg per day
 Notes:
◦ Analgesic ceiling at 400 mg
◦ Anti-inflammatory effects 600 & 800mg

 Side Effects:
GI upset
 Platelet aggregation
 Nephrotoxicity
 Contraindications:
 Pregnancy: Commonly used but consult MD
 Renal disease – Kidney Killer

Other PPA Derivatives
 Used more for chronic arthritis pain

◦ Ketoprofen
x 25, 50, 75 mg q6-8h
◦ Fenoprofen
x 200 mg q4-6h
◦ Flurbiprofen
x 50 mg q6h

3- Acetic Acid (Etodolac)
• Etodolac is indicated as an analgesic based on its

efficacy in the oral surgery model and a more
favorable profile of GI safety. In a dose range study
(50, 100, and 200 mg).
• Etodolac is reported to be 10-fold more selective for

COX-2 in comparison with its effect on COX-1. This
sparing of COX-1 activity gives rise to greater gastric
tolerance.

Recommendations for Safe Use of NSAIDs
• For safe use of NSAIDs, the medication should be

taken:
1. only as prescribed
2. at the lowest possible dose that is still effective
3. for the shortest time needed

Before taking NSAIDs, the doctor should inform the
patient if he/she have certain medical conditions:
1. Decreased kidney or liver function
2. Recent peptic ulcer, stomach bleeding, gastritis
3. Take anticoagulant or antiplatelet
4. Take prednisone or other steroids
5. Low platelet count
6. History of stroke or other heart issues
7. History of asthma or chronic lung conditions
8. Allergy to NSAIDs or aspirin
9. Pregnant or breastfeeding
10. Older than 65

Antipyretic analgesics
Acetaminophen (Paracetamol)
 Acetaminophen is not related to salicylates or NSAIDs.

 Pharmacologic effects:
• Paracetamol has analgesic and antipyretic actions but
only weak anti-inflammatory effects. Why?
• It appears to be an inhibitor of PG synthesis in the
brain, thus accounting for its analgesic and antipyretic
activity.
• It is much less effective than aspirin as an inhibitor
of the peripherally located PG biosynthetic enzyme
system that plays such an important role in
inflammation.
Pharmacologic effects:
• It exerts little or no pharmacologic effect on:

– the cardiovascular,
– respiratory,
– gastrointestinal systems,
– acid-base regulation,
– platelet function.

Therapeutic uses
• Paracetamol provides an effective alternative to aspirin;
1. When aspirin is contraindicated (e.g., in patients with

peptic ulcer or hemophilia)
2. When the anti-inflammtory action of aspirin is not

required.
 Dose :
0.5-1 gm every 4-6 hrs
Maximum dose 4g/day

Side effects
• When taken according to directions, side effects from

acetaminophen are rare
• Certain side effects can be signs of an allergic reaction
or a situation which requires immediate medical
attention, such as:
1. Rash
2. Itching
3. Swelling
4. Difficulty in breathing

• The most serious side effect is liver damage. Kidney
toxicity is also a possibility.
• The risk of liver damage increases with:

1. Large doses of acetaminophen
2. Chronic use of acetaminophen
3. Concomitant use of acetaminophen with other drugs
that can also potentially cause liver damage

Opioid narcotic(‫) ا ألفيون‬

II - OPIOIDS (NARCOTICS)
Only Available by prescription.
Used to relieve severe pain associated with injuries,

heart attacks, or chronic diseases such as cancer.
Most strong analgesics are derived from the opium

poppy‫ ( ) خشاشا ألفيون‬or synthetically produced.
Basically three types:

Natural, semi-synthetic, and synthetic
Mechanism of OPIOIDS (NARCOTICS)
 The human body contains “natural opiates” in the brain

called endorphins and enkephalins.
 They are circulating throughout the body on an “as-needed”

basis during extreme conditions such as “running high” and
extreme injuries.
 The endorphins are naturally occurring morphine-like

substances and are thought to bind to receptor sites on the
pain mediating pathways.
 The enkephalins have a similar function to the endorphins;

they bind to different receptor sites but provide the same
type of pain mediation.
 When these are absorbed by receptors in the brain the body
feels analgesia and the pain is reduced.
 Opiates derived from the poppy act in the same way as

endorphins but are not natural to the human body.
 The “high” is produced because of the absorption of opiates

is quicker than endorphins.
 Drugs such as naloxone act to fill the receptors in the brain

but are not analgesics and thus are used to prevent
overdoses on analgesics.
 Endorphins are not used as analgesics because the cannot

be stored and are unstable.

Mechanism of Action
Identified in the peripheral nerves.

 Opioids bind and decrease the excitability of the
peripheral sensory neurons = analgesia.
Receptors of opioids are classified into three

categories which differ in their response :
 Mu (µ)
 Kappa ()
 Delta ()

Opiod Receptor Activation
Response Mu-1 Mu-2 Kappa Delta Sigma
Analgesia
Respiratory
depression
Euphoria
Dysphoria
Decrease GI
motility
Physical
Dependence
Mania,
hallucination
Applications in Dentistry
 Narcotic (opioid) analgesics are extremely effective in reducing

acute dental and postoperative pain.
 They Can be used for postsurgical pain control in maxillofacial

operations and trauma. They relive the pain of end stage cancer-
patients.
 The narcotic analgesics have established a niche for the treatment

of pain in those situations where the NSAIDs are less effective
especially in cancer patient.
 Hydrocodone, oxycodone, codeine, and occasionally meperidine

are the narcotics used to treat sever dental pain.
Side Effects of Strong Analgesics
 Short term  Long Term
Dulling of Pain Addiction and very strong
Euphoria withdrawal effects
Slow Nervous system Constipation
Slowed heart rate Loss of libido
Loss of cough reflex Disruptions in menstruation
Nausea “Cross-tolerance”
Overdoses can lead to death Loss of appetite
Possibility of stroke Problems associated with
Overall slowdown of buying street drugs i.e.
biological systems sharing needles AIDS and
prostitution.
Withdrawal Reactions
Acute Action Withdrawl Sign

 Analgesia  Pain and irritability
 Respiratory Depression  Hyperventilation
 Euphoria  Dysphoria and depression
 Relaxation and sleep  Restlessness and insomnia

 Tranquilization  Fearfulness and hostility
 Decreased blood pressure  Increased blood pressure
 Constipation  Diarrhea
 Pupillary constriction  Pupillary dilation
 Hypothermia  Hyperthermia
 Drying of secretions  Lacrimation, runny nose
 Reduced sex drive  Spontaneous ejaculation
 Flushed and warm skin  Chilliness and “gooseflesh”

A-Natural Strong Analgesics
(Opioids)

1- Morphine
Naturally occurring in the
poppy- needs to be isolated
Very strong pain reliever but

also very addictive (2nd to
Heroin)
Usually injected but can be

smoked, sniffed or swallowed
Commonly used in hospitals
Large illegal street culture

2- Heroin
 Originally sold as cough suppressant and pain killer 10 times
stronger than Morphine
 Incredibly addictive (many times, other strong analgesics are
needed for withdrawal)

Heroin
 Synthesized from morphine
in a esterification reaction
with acetyl chloride.
 It is absorbed by the brain

very quickly resulting in a
potent high Effect.
 Many other problems are

associated with heroin
addiction including as
prostitution and AIDS.

3- Codeine
 Most commonly used strong
analgesic
 Similar to Morphine except

for the replacement of a (OH-)
group for (OCH3) group
 Commonly used with Tylenol

as a more mild analgesic
 1/6 as strong as Morphine and

less addictive

B-Synthetic Strong Analgesics (Opioids)
The active area of

morphine has been
identified and can be
synthesized.
This has produced many

synthetic analgesics and
has allowed scientists to
eliminate some of the
harmful side effects of
more natural analgesics.

1- Demerol (Meperidine)
Used for moderate to

severe pain and to stop
muscle spasms.
Usually injected or taken

orally.

2- Methadone
Compared to most strong
analgesics it is weaker.
Has been synthesized to not

have euphoric properties
and mild withdrawal effects
but is still addictive.
Used as an analgesic but

most commonly to help in
the withdrawal for Heroin
addicts.

3- Hydrocodone
It is a semi-synthetic opioid
derived from codine
It is used to treat moderate to
severe pain .
It is approximately 1.5 times less

potent opioid than oxycodone.
Analgesic action of hydrocodone

begins 20–30 minutes after taking
it and lasts 4–8 hours, often in
combination with paracetamol
(acetaminophen) or ibuprofen.

4- Oxycodone
Oxycodone is a semi-
synthetic opioid synthesized
from poppy-derived thebanie.
It is a narcotic analgesic

generally indicated for relief
of moderate to severe pain.
It is used for managing

moderate to moderately
severe acute or chronic pain.

5- Vicodin
Is solution of
acetaminophen and
hydrocodone (the latter
being the stronger)
Hydrocodone is addictive
and can cause highs.
Usually taken orally
Stronger than codeine but

not as strong than Morphine

III- Substances with mixed
mechanism of action

TRAMADOL
 Tramadol hydrochloride is a
novel, centrally acting
analgesic with two
complementary mechanisms
of action: opioid and
aminergic.
 Analgesic activity is similar
to the activity of morphine .
 Abuse potential is low.
 Less respiratory depression.
 Hemodynamic effects are
minimal

Tramadol has limited indication for management of
acute pain in dentistry, possibly as an alternative

analgesic when gastrointestinal side effects
contraindicate the use of non-steroidal anti-
inflammatory drugs and when
codeine/acetaminophen combination analgesics are
not well-tolerated or are contraindicated.

The End

Analgesic Used in Oral Surgery

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ANALGESICS

Assistant Professor. Akram Thabet Nasher

An analgesic (known as painkiller) drugs: is a drug

Patients should be encouraged to use analgesics

Dr. Akram Nasher Analgesic Drugs

It is an unpleasant sensory and emotional experience

arising from actual or potential tissue damage .

Most dental procedures produce tissue trauma and

release potent mediators of inflammation and pain.

Dr. Akram Nasher Analgesic Drugs

Dr. Akram Nasher Analgesic Drugs

The most common types of odontogenic pain are characterized as

Responds to treatment – NSAIDs , opioids , corticosteroids,

• Chronic pain often lasts months or years

• Vague descriptions of pain, difficulty in describing

Dr. Akram Nasher Analgesic Drugs

Dr. Akram Nasher Analgesic Drugs

 Analgesic drugs can be classified into:

B- Opioid narcotic (morphine)

C- Substances with mixed mechanism of action

Aspirin Ibuprofen Opium Heroin

Dr. Akram Nasher Analgesic Drugs

• NSAIDs work by inhibiting cyclooxygenase

NSAIDs are reversible inhibitors of

Dr. Akram Nasher Analgesic Drugs

 Two different COX enzymes existed, known as

Dr. Akram Nasher Analgesic Drugs

COX-1: beneficial COX-2: harmful

1- Depression of cyclooxygenases activity

2-Decreasing of prostaglandins synthesis in peripheral

3-Decreasing of sensitivity of nervous endings and

4- Pain-relieving action of non-opioid analgesics is

1. Analgesic (mild to moderate)

Dr. Akram Nasher Analgesic Drugs

Dr. Akram Nasher Analgesic Drugs

• Greater affinity for cyclooxygenase-2

• Decreased incidence of negative effects associated

Dr. Akram Nasher Analgesic Drugs

 Contraindications: ◦ Sulfa Allergy

Dr. Akram Nasher Analgesic Drugs

Dr. Akram Nasher Analgesic Drugs

1- Carboxylic Acids : Acetylated - aspirin (ASA)

Dr. Akram Nasher Analgesic Drugs

Dr. Akram Nasher Analgesic Drugs

In the addition of the analgesic effect of the aspirin it has other

Dr. Akram Nasher Analgesic Drugs

• More severe and associated with encephalopathy

 Use of salicylates in children with chickenpox or

Dr. Akram Nasher Analgesic Drugs

Dr. Akram Nasher Analgesic Drugs

4-- Salicylism: usually occurs with repeated

Dr. Akram Nasher Analgesic Drugs

1- Salicylates are NOT to be given to children under

Dr. Akram Nasher Analgesic Drugs

Dr. Akram Nasher Analgesic Drugs

• Ibuprofen, has demonstrated analgesic activity over a

• When given prior to pain onset, it suppresses the

• lbuprofen suppresses swelling over the initial two- to

 Cyclooxygenase inhibitor of PGs

Dr. Akram Nasher Analgesic Drugs

Dr. Akram Nasher Analgesic Drugs

 Used more for chronic arthritis pain

Dr. Akram Nasher Analgesic Drugs