Analgesic in Pediatric Dentistry

-DrKOMAL GHIYA
PEDIATRIC DENTIST
1

ANALGESICS IN PEDIATRIC DENTISTRY
2

 DEFINITIONS:
 Pharmacology
 Pain
 Analgesia
 Analgesics
 AAPD policy on pediatric pain management
 TYPES OF ANALGESICS
 NON OPIOID ANALGESICS
 CLASSIFICATION OF NON OPOIDS
 TYPES OF NON OPOIDS USED IN PEDIATRIC DENTISTRY
 NSAIDS:ASPIRIN
 IBUPROFEN
 DICLOFENAC
 KETOROLAC
 PREFERENTIAL COX INHIBITOR:NIMESULIDE
 PARACETAMOL
3

 OPIOID ANALGESICS
 CLASSIFICATION
 TYPES USED IN PEDIATRIC DENTISTRY
 NATURALLY OCCURING OPIOID:MORPHINE
 CODIENE
 SYNTHETIC OPIOIDS:MEPERIDINE
 FENATNYL
 TRAMADOL
 PHARMACOKINETICS
 WHO three step ladder
 COMBINATION OF ANALGESICS
 RECENT ADVANCES IN ANALGESICS
 CONCLUSION
 BIBLIOGRAPHY
4

 Pharmacology is the science of drugs (greek
Pharmacon-drug;logos-discourse in).In a
broad sense deals with interaction of
exogenously administered chemical molecules
(drugs)with living systems.
 Pain an unpleasant emotional experience
usually initiated by a noxious stimulus and
transmitted over a specialized neural network
to the central nervous system where it is
interpreted as such
REFERENCE: Tripathi K, Essentials of medical pharmacology ,6 th edition,2007
Bennet C,bonani S,Cassidy M, neston A,phero J,monhiem’s local anesthesia and pain control in
dental practice,7th edition,1990
5

 Analgesia: a deadening or absence of the sense
of pain without loss of consciousness.
 Analgesics: A drug that selectively relieves pain
by acting in the CNS or on peripheral pain
mechanism, without significantly altering
consciousness
6

 Recognize and assess pain,documenting in the
patient’s chart
 Use non pharmacologic strategies to reduce pain
experience pre operatively
 Be familiar with the patient’s medical history to
avoid prescribing a drug that would be otherwise
be contraindicated
 Comprehend the consequences,morbidities and
toxicities associated with the use of specific
therapeutics
 Consider non opioid analgesics as first line
agents for post operative pain mangement
AMERICAN ACADEMY OF PEDIATRIC DENTISTRY- POLICY ON
PEDIATRIC PAIN MANGEMENT2012
7

 Utilize drug formularies in order to accurately
prescribe medications for the mangement of
postoperative pain
 Consider combining NSAIDs with
acetaminophen to provide a greater analgesic
effect than the single agent alone
 Combine opioid analgesics with NSAIDs for
post operative treatment of moderate to
severe pain in children and adolescents
AMERICAN ACADEMY OF PEDIATRIC DENTISTRY :POLICY ON PEDIATRIC
PAIN MANGEMENT-2012 8

 Analgesics are divided mainly into two
groups:
 Opioid/narcotic /morphine like analgesics
 Nonopioid/non narcotic/aspirin like/anti-
inflammatory or antipyretic analgesics
9

A] Nonselective COX inhibitors (traditional NSAIDs)
Salicylates: Aspirin
Propionic acid derivatives: Ibuprofen, Naproxen, Ketoprofen, flurbiprofen
Anthranilic acid derivative: Mephenamic Acid
Aryl acetic acid derivative: Diclofenac, Aceclofenac
Oxicam derivatives: Piroxicam, Tenoxicam
Pyrrolo –pyrrole derivative: Ketorolac
Indole derivative: Indomethacin
Pyrazolone derivatives: Phenylbutazone,
Oxyphenbutazone
REFERENCE: Tripathi K, Essentials of medical pharmacology ,6 th edition,2007 10

B] Preferential COX -2
inhibitors
Nimesulide, Meloxicam,
Namebumetone
C] Selective COX2 inhibitors
Calecoxib, Etoricoxib,
Parecoxib
D] Analgesic –antipyretics with
poor anti-inflammatory action
Paraaminophenol derivative:
Paracetamol (Acetaminophen)
Pyrazole derivatives:
Metamizol, Propiphenazone
Benzoxazocine derivative:
Nefopam

NON SELECTIVE COX INHIBITORS(TRADIONALLY
NSAIDS)
SALICYLATES:ASPIRIN
PROPIONIC ACID DERIVATIVE:IBUPROFEN
ARYL ACETIC ACID DERIVATIVE:DICLOFENAC
PYRROLO PYRROLE DERIVATIVE:KETOROLAC
PREFERENTIAL COX-2
INHIBITORS:
NIMESULIDE
ANTIPYRETICS WITH POOR ANTI
INFLAMMATORY ACTION:
PARACETAMOL
12

 Derivative : phenylalkanoic acid.
 analgesic
 anti inflammatory
 effective for management of acute pain following
minor surgery or trauma.
 produce fewer bleeding problems
 platelet aggregation is reversible
 Metabolized in liver
 excreted in the urine.
 Effective alone after oral and dental procedures.
 Have an opioid sparing effect
reference:Casamassimo P,Fields H,Mctigue D.,Nowak A, pediatric dentistry
infancy through adolescence,2013,page no 102 13

ANTI INFLAMMATORY ACTION
14

ELEVATED BODY
TEMPERATURE
HYPOTHALAMIC
REGULATION CENTER
SETS AT HIGHER
TEMPERATURE
PERIPHERAL
VASOCONSTRICTION
DECREASE IN HEAT
LOSS
RESET
HYPOTHALAMIC
CENTER AT LOWER
TEMPERATURE
CAUSES SWEATING
REDUCES BODY
TEMPERATURE
NSAIDS

 Contraindications
 Bleeding or coagulopathies
 Renal disease
 Hematological malignancies, in children who
may have or develop thrombocytopenia.
 Severe asthma, especially if child is sensitive
to aspirin, steroid dependent or have co
existing nasal polyps.
REFERENCE: Tripathi K, Essentials of medical pharmacology ,6 th
edition,2007 16

 Side effects
 Gastrointestinal upset: gastric irritation, erosions,
ulcerations, gastric bleeding/perforations, esophagitis.
 Rash
 CNS: Headache, mental confusion, behavioural
disturbances, seizure precipitation.
 Dizziness
 Eye problem
 Hepatic dysfunction: raised transaminases, hepatic failure
(rare).
 Renal dysfunction: Na+ and water retention, chronic renal
failure, interstitial nephritis, papillary necrosis (rare).
 Hematological: bleeding, thrombocytopenia, hemolytic
anemia, agranulocytosis.
 Others: asthma, exacerbation, nasal polyposis ,
angioedema
17

 Analgesic
 antipyretic
 anti inflammatory properties
 a standard drug of choice for management of
mild pain.
 weaker analgesic than morphine type drugs
 used in management of juvenile rheumatoid.
 ROUTE:oral
Wilson S,Ganzberg S in Casamassimo P,Fields H,Mctigue D.,Nowak A, pediatric dentistry
infancy through adolescence,2013
18

Analgesic action of
aspirin
Obtunding of
peripheral pain
receptors
Prevention of PG
mediated sensitization
of nerve endings
Subcortical action of
raising threshold to
pain persists
REFERENCE: Tripathi K, Essentials of medical pharmacology ,6 th
edition,2007 19

REF:aspirin inhibition of COX 1 decreases TXA2 production
source:gasparyan yet al.j am coll,cardiol 2008;51:1829-1843 20

 alteration of coagulation
 gastric distress
 dyspepsia
 occult blood loss
REF:Wilson S,Ganzberg S in Casamassimo P,Fields H,Mctigue
D.,Nowak A, pediatric dentistry infancy through adolescence
21

 The anticoagulant properties of aspirin are
rarely a problem in children however a single
dose of aspirin can increase bleeding time.
 Aspirin therapy in children with rheumatoid
arthritis has been found to raise serum
transaminases, indicating liver damage. Most
cases are asymptomatic but potentially
dangerous
 Rarely used in children for mild pain due to
risk of Reye syndrome
REF:Wilson S,Ganzberg S in Casamassimo P,Fields H,Mctigue
D.,Nowak A, pediatric dentistry infancy through adolescence
22

 common in children.
 seen at serum salicylate levels>50mg/dl.
Manifestations : vomiting, diarrhea,
 electrolyte imbalance,
 acidoitic breathing,
 hyper/hypoglycemia,
 petechial haemmorhage,
 restlessness,
 delirium,
 hallucinations,
 hyperpyrexia,
 convulsions,
 coma
 death due to respiratory failure+cardiovascular
collapse
REF:Tripathi K, Essentials of medical pharmacology ,6 th edition,2007 23

Treatment: is symptomatic, supportive External
cooling
 i.v fluid with Na+,K+,HCO3
- and glucose
 Gastric lavage to remove unabsorbed drug
 forced alkaline diuresis
 hemodialysis to remove absorbed drug is
indicated in severe cases.
 Blood transfusion and vitK should be given if
bleeding occurs.
24

 Contraindications
 sensitive patient
 have peptic ulcer, bleeding tendencies,
 children suffering from chicken pox or
influenza.
 avoided in diabetes, in those with low
cardiac reserve or frank congestive heart
failure
 stopped 1 week before elective surgery.
 Given during pregnancy it may be
responsible for low birth weight babies.
 G6PD deficient individual-hemolysis can
occur.
REFE:Wilson S,Ganzberg S in Casamassimo P,Fields H,Mctigue D.,Nowak A, pediatric dentistry infancy through
adolescence
Tripathi K, Essentials of medical pharmacology ,6 th edition,2007 25

 Dosages:
 Recommended dosage for analgesia and
antipyretic purposes in children in 10-15 mg
given at 4 hour intervals up to a total of 60-
80 mg/kg per day, with maximal limit of 3.6
g/day
REFE:Wilson S,Ganzberg S in Casamassimo P,Fields H,Mctigue D.,Nowak A, pediatric
dentistry infancy through adolescence

 Consider semisupine chair position for
patient comfort of GI effect
 Question patient about tolerance of aspirin
related to GI effects
 Patient with GERD may have oral symptoms of
acid reflux ,increase dental erosion or TMJ
dysfunction that may require appropriate
dental treatment.
Jaske A in mosby’s dental drug reference ,10 th edition,2011
27

 TEACH PATIENT /FAMILY TO:
 Seek medical care for worsening or unrelieved
GI symptoms.
 Use flouridated toothpaste and effective oral
hygiene measures to minimize sensitivity and
caries associated with dental erosion.
28

 anti-inflammatory, analgesic and anti pyretic
effects,
 The analgesic effect has both central and
peripheral effects.
 It has been rated as the safest conventional
NSAIDS by the spontaneous adverse drug
reaction reporting system in U.K. ibuprofen
(400mg) has been found equally or more
efficacious than a combination of
aspirin(650mg)+codeine(60mg)in relieving
dental surgery pain.
 Route: orally
M S Muthu,N Sivakumar ,Pediatric dentistry :principles and practice-,2nd edition
Tripathi K, Essentials of medical pharmacology ,6 th edition,2007
29

 Indications:
 Commonly used in febrile patients
 Commonly used in children for mild pain with
less gastrointestinal side effects compared
with aspirin
 Musculoskeletal pain
 Inflammatory and degenerative arthritis
 Dental pain
 Contraindications:
 with renal impairment
REF:Tripathi K, Essentials of medical pharmacology ,6 th edition,2007 30

 Adverse effects
 Hematemesis,
 Agranulocytosis
 Gastrointestinal disturbances
 Thrombocytopenia
 CNS effect: Dizziness, headache, blurring of
vision, tinnitus, depression, rashes, and
itching, other hypersensitivity phenomena are
infrequent.
 However these drugs precipitate aspirin
induced asthma.
REF:Tripathi K, Essentials of medical pharmacology ,6 th edition,2007
31

 Dosages:
 The recommended dose for analgesic
/antipyretic effects is 10-15mg/kg to be
given every 4-6 hours .It should not to be
given to children less than 7kgs
12Tate A R, ACSG: Dental clinic of north America 46:707-712,2002
32

Patients on chronic drug therapy may rarely
have symptoms of blood dyscrasias,which
can increase infection,bleeding and poor
healing.
Assess salivary flow
Avoid aspirin containing products
Consider semisupine position for patient with
arthritic disease.
Jaske A.in mosby’s dental drug reference book ,2011,10th edition
33

 Severe stomach bleeding may occur:
 Regualar use of NSAIDs.
 In geraitric patients
 Nsaids+anticoagulant/antiplatelet
 Peptic ulcer disease
 Warn patient of potential for severe stomach
bleeding
 CONSULT:
 Blood dyscrasias:medical consultation for blood
studies
 Postpone dental treatment untill normal values
are restored
 Medical consulation to assess disease control
Jaske A.in mosby’s dental drug reference book ,2011,10th
edition 34

 TEACH patient/relative:
 Encourage oral hygiene to prevent soft tissue
inflammation
 Caution to prevent injury when using oral
hygiene aids
 When chronic dry mouth occurs:
• Avoid mouth rinses with high alcohol content
because of drying effects
• Daily home flouride product for anticaries effect
• Use sugarless gum,frequently sips of water or
saliva substitue
35

 Has potent anti inflammatory ,analgesic and
antipyretic actions
 Diclofenac is available as sodium or
potassium salt .The sodium salt is enteric
coated to ensure optimum bioavailability .this
leads to some delay in onset of action.
 Route: orally and i.v
REF:M S Muthu,N Sivakumar ,Pediatric dentistry :principles and practice-,2nd
edition
36

DICLOFENAC
MECHANISM
INHIBITS COX 2
NEUTROPHIL
CHEMOTAXIS AND
SUPEROXIDE
PRODUCTION IS
REDUCED
REF:Tripathi K, Essentials of medical pharmacology ,6 th
edition,2007 37

 Adverse effects:
 Mild epigastric pain
 Perforation of gastric ulcer
 Gastrointestinal hemorrhage
 Blood dyscrasias
 Nausea
 Headache, dizziness
 Rashes
 Gastric ulceration
 Bleeding is less common.
 Reverse elevation of serum aminotransferases
38

 Dosages:
AGE WEIGHT DOSAGE(mg)
lbs Kg
6-11 months 12-17 5.1-
7.7
50
12-23 months 18-23 7.8-
10.5
75
2-3years 24-35 10.6-
15.9
100
4-5 years 36-47 16-
21.4
150
6-8 years 48-59 21.4-
26.8
200
9-10 years 60-71 26.8-
32.2
250
11 years 72-95 32.2-
43.2
300
AMERICAN ASSOCIATION OF PEDIATRIC DENTISTRY
reference manual V36/no 6 14/15 39

 The dose for children over 1 year is 1-3
mg/kg/day in divided doses or maximum
3mg/kg/day upto 150 mg/kg/day.
12Tate A R, ACSG: Dental clinic of north America 46:707-
712,2002
40

 Use with caution in patient with
cardiovascular diseses at risk of
thromboembolism
 Prolonged use causes nepherotoxicity
 Risk of decreased renal function
 Increases effect:oral anticoagulant
 Antidiabetics
 Lithium
 Methotrexate
41

 Decreases effect: diuretics
 Beta adrenergic blocker
 ACE inhibitors
 First time users of SSRIs taking NSAIDs may
have higher risk of GI side effects
British clincal pharmacology 55:591-595,2003 42

 Potent analgesic
 modest anti inflammatory activity.
 Route: i.v or i.m , oral administration in
children is not recommended in children.
 CAUTION: maximum duration of therapy-5
days.
 MECHANISM OF ACTION: blocks pg
synthesis,thus analgesic action is due to
peripheral actions
Tripathi K, Essentials of medical pharmacology ,6 th
edition,2007 43

 Nausea, abdominal pain, loose stools,
dyspepsia, ulceration,
 Drowsiness ,headache, dizziness,
nervousness,
 Pruritis pain at injection site
 Rise in serum transaminase
 Fluid retention

 Orally used in a dose of 10-20 mg 6 hourly
for short term management of moderate pain
45

 Assess salivary flow
 Avoid in pregnancy
 Do not use along with aspirin or NSAIDs
 Do not use for long term for management of
chronic pain syndromes,Combined use of I.V
or I.M and oral dose must not exceed 5 days.
 CONSULTATION:Medical consultation may be
required to assess disease control.
 TEACH:
Avoid mouthrinses with high alcohol content
because of drying effects.
edition 46

 used for short lasting painful inflammatory
conditions.
 The chances of development of gastric ulcers
and inhibition of platelet aggregation is less
as compared to the other NSAIDS .
 It is a stomach friendly drug.
 Route: orally
REF:M S Muthu,N Sivakumar ,Pediatric dentistry :principles and practice-,2nd
edition

 Mechanism of action
 It selectively inhibits the COX-2 enzymes and
decreases prostaglandin synthesis.
 It is relatively weak inhibitor of prostaglandin
synthesis but has potent anti inflammatory
action.
edition,2007 48

 Indications:
 Most asthmatics and those who develop
bronchospasm or intolerance to aspirin and
other NSAIDs do not cross react with
Nimesulide .Its specific usefulness appears to
be only in such patients.
 Epigastria pain
 Nausea vomiting
 Dizziness, headache
 Rash and purities
49

 Dosages:
 The recommended pediatric dose is 5 mg/kg
/day in 2 or 3 divided doses.
 WARNING: this drug has been banned
recently in many countries due to reported
instances of hepatic failure .Thus safety of
the drug is subject to controversy. It is left to
the decision of the clinician to carefully
exercise his/her own judgement in this
regard.
edition,2007 50

 Paraamino phenol derivatives.
 It has an analgesic/antipyretic of choice when
salicylates or NSAIDS are contraindicated eg
asthmatic patients, peptic ulcer patients and
children.
 does not inhibit platelet function.
 It also causes less gastric upset and has not
been implicated in Reye syndrome.
 Route: orally
REF:Satoskar R,Bhandarkar S,Rege N,pharmacology and pharmacotherapeutics,21 st edition
infancy through adolescence,2013,chapter :pain perception control
51

Blocks COX 3 AND COX 2
ANALGESIC ACTION
52

 Indications:
 Useful as pre emptive analgesic
 Fever due to infection or inflammation
 Pain due to trauma or odontogenic infections
 Headache, musculoskeletal pain
edition,2007 53

 Adverse effect:
 Hypersensitivity
 Renal or hepatic impairment
 Nausea and rashes occur occasionally,
leucopenia is rare
edition,2007
54

 20mg/kg orally ,then 15mg/kg every 4 hour
 30mg/kg rectally as a single dose.
 Maximum 24 hour dosage of 90 mg/kg for 2
days, then 60 mg/kg per day by any route of
administration.
 Maximum: 5 doses/day
 Intravenous paracetamol is available .the
same dose is used and administered over 15
min.
Alcaino E,Mcdonald J,cooper M,malhi S in Cameron A,Widmer
R,Hall R,Handbook of pediatric dentistry,4 th edition,2003 55

age Weight(kg) Weight(pound) Dose/(mg)
0-3 months
6-11 2.7-5 40
4-11 months 12-17 5.1-7.7 80
1-2 years 18-23 7.8-10.5 120
2-3 years 24-35 10.6-15.9 160
4-5 years 36-47 16-21.4 240
6-8 years 48-59 21.5-26.8 320
9-10 years 60-71 26.9-32.3 400
11 years 72-95 32.4-43.2 480
American academy of pediatric dentistry refernce manual V36/no
6,14/15 56

 occurs in small children who have low
hepatic glucuronide conjugation ability.
 If a large dose(>150mg/kg or >10 g in
adult) is taken serious toxicity can occur.
 Fatality is common with >250 mg/kg.

 Manifestations : nausea, vomiting,
abdominal pain and liver tenderness.
 After 12-18 hours :centrilobular hepatic
necrosis + renal tubular necrosis
+hypoglycemia coma.
 Jaundice starts after 2 days.
 Fulminating hepatic failure and death are
likely if the plasma levels are above the line
joining 200microgram/ml at 4 hours and
30 micrograms/ml at 15 hours
edition,2007 58

Treatment:
Induce vomiting
gastric lavage done.
Activated charcoal is given orally or through the tube
 Other supportive measures as needed should be taken.
N-acetylcystiene 150 mg/kg should be infused i.v over
15 min, followed by the same dose i.v over the next 20
hours. Alternatively 75 mg/kg may be given orally every 4-
6 hours for 2-3 days .It replenishes the glutathione stores
of liver and prevents binding of the toxic metabolite to
other cellular constituents.
Ingestion treatment interval is critical; earlier the better .
It is practically ineffective if started 16 hours or more after
paracetamol ingestion

 For a patient with symptoms of blood
dyscrasias ,require a medical consult for
blood studies and postpone dental treatment
until normal values are restored.
 TEACH patient /family:
 Question patient concerning other drugs
being taken including acetaminophen
 Caution patient to be aware of products that
might include acetaminophen
 Emphasize the potential risk to liver when
consuming alcohol and taking acetaminophen
60

 CLASSIFICATIONS OF OPIOIDS :
 Natural opium alkaloids: morphine, codeine
 Semisynthetic opiates: diacetylmorphine,
pholcodiene
 Synthetic
opioids:pethidiene,fentanyl,methadone,
 dextropropoxyphene,tramadol
edition,2007
61

NATURAL OPIUM
ALKALOIDS:MORPHINE,CODIENE
SYNTHETIC
OPIOIDS:PETHIDINE(MEPERIDIENE),FENATNYL,
TRAMADOL
62

 principal alkaloid in opium
 Therefore, it is described as prototype
 No risk of addiction for supervised analgesic
use in children.
 EFFECTS:
 dull, poorly, localized visceral pain >sharply
defined somatic pain
 peripheral pain >neurotic pain
edition,2007
63

Perception of pain and
its emotional or
suffering component
are both altered so that
pain is no longer as
unpleasant or
distressing i.e. the
patient tolerates pain
better.
reference:White P F :the changing role of non opioid analgesic techniques in the
management of post operative pain.anesthesia ans analgesia 2005;101 :S5
64

MECHANISM OF ACTION OF
MORPHINE
SPINAL SITES
In substantia gelatinosa of dorsal
horn to inhibit release of excitatory
transmitters from primary afferents
carrying pain impulse. The action
appears to be exerted through
interneurones which are involved in
gating of pain impulse .
Release of glutamate from primary
pain afferents in the spinal cord and
its postsynaptic action on dorsal horn
neurons is inhibited by morphine .
SUPRA SPINAL SITES
medulla ,midbrain,
limbic, cortical,
areas alter processing
and interpretation of
pain impulses
send inhibitory
impulses through the
descending pathways to
the spinal cord
Several
aminergic
and other
neuronal
systems
appear to be
involved in
the action of
morphine.
SIMULTANEOUS ACTION AT SPINAL AND SUPRASPINAL AMPLIFY THE
EFFECT 65

 Sedation , mental clouding, lethargy,
vomiting is occasional in recumbent patient,
constipation . Respiratory depression,
blurring of vision, urinary retention.
 Allergy and anaphylactoid reaction is rare.
 Urticaria, itch, swelling of lips, a local reaction
may occur at injection site due to histamine
release.
edition,2007,
66

 Apnoea may occur in the newborn when
morphine is given to mothers during labour.
The blood brain barrier of fetus is
undeveloped, Morphine attains higher
concentration in fetal brain than in that of
mother.
 Treatment of choice :Naloxone 10
micrograms/kg is injected in the umbilical
cord .
edition,2007,
67

 It is accidental and suicidal or seen in drug abusers.
 In the non tolerant adult; 50 mg of morphine i.m
produces serious toxicity .
 human lethal dose:250 mg.
 Manifestations :
 Stupor ,
 coma,
 flaccidity,
 occasional breathing cyanosis,
 pinpoint pupil,
 fall in b.p.
 shock
 convulsion
 pulmonary edema

edition,2007
68

 Treatment:
 respiratory support ,
 maintenance of BP .
 Gastric lavage with potassium
permanganate to remove unabsorbed drug
 Specific antidote:
 Naloxone 0.4-0.8 mg i.v repeated every 2-3
minute till respiration picks up
 Injection should be repeated every 1-4 hours
later on according to response .
69

 Infants are more susceptible to the respiratory
depressant action of morphine
 respiratory insufficiency
 Bronchial asthma(Histamine releasing action)
 Head injury
 Undiagnosed acute abdominal pain
 Elderly male : urinary retention
 Hypothyroidism ,liver and kidney disease patients
are more sensitive to morphine.
 Unstable personalities
 Dosage:
 in children 0.1-0.2mg/kg
Tripathi K, Essentials of medical pharmacology ,6 th 70

 Monitor vital signs at every appointment
because of cardiovascular and respiratory
side effects.
 Assess salivary flow as a factor in
caries,periodontal status,candidiasis
 After supine positioning ,have patient sit
upright for atleast minute before standing to
avoid orthostatic hypotension
 Psychologic and physical dependance may
occur with chronic administration
 Determine why the patient is taking the drug.
71

 Consider use of NSAIDs when additional
analgesia is required
 TEACH:
 When chronic dry mouth occurs,advise
patient to
 Use daily home flouride products for
anticaries effect
 Avoid mouth rinses with high alcohol content
because of drying effect
 Use sugarless gum,frequent sips of water or
salivary substitutes.
72

 used to an extent in dentistry for children is
codeine phosphate
 standard of comparison for oral narcotics
 most commonly prescribed for moderate to
severe pain.
 abuse liability is low
 its antitussive effect
 If given in high doses or over prolonged
periods, codiene may produce more serious side
effects of respiratory depression and
dependence seen with other more potent
narcotics.
 used to control diarrheas
edition,2007
73

ACTS ON MU OPIOID RECEPTOR
MORPHINE
CODIENE
EMETHYLATION BY CP2D6
Tripathi K, Essentials of medical pharmacology ,6 th 74

 Route:
 Codeine has good activity by the oral route
(oral : parenteral ratio 1;2)
 Though codeine phosphate is water soluble
and can be injected, parenteral preparation is
not available. Intravenous use may cause
profound hypotension
 nausea, sedation, dizziness and cramps.
 Constipation is a prominent side effect when
it is used as analgesic
Wilson S,Ganzberg S in Casamassimo P,Fields H,Mctigue D.,Nowak A, pediatric
dentistry infancy through adolescence,2013,chapter :pain perception control 75

 Dosage:
 It is recommended that codeine be given in
combination with acetaminophen when it is
given orally for pediatric analgesia. The
recommended dosage in children is 0.5 to
1.0mg/kg every 4-6 hours as needed.
 Adults: 30 to 60mg/kg given every 4 to 6
hours as needed
infancy through adolescence,2013,chapter :pain perception control
76

 Vital signs at every appointment because of
cardiovascular and respiratory side effects
 After supine positioning,have patient sit
upright at least 2 minute to avoid othostatic
hypotension
caries,periodontal status,candidiasis.
 Psychologic and physical dependence may
Jaske A.in mosby’s dental drug reference book
,2011,10th edition 77

 When chronic dry mouth occurs,advise
patient to:
 Avoid mouth rinses with alcohol content
 Use daily home flourides
 Use sugarless gum,frequently sips of water or
salivary substitute.
edition 78

 a premedication for operative dentistry alone
 CNS depressant
 Important differences in comparison to
morphine are:
 1/10 th in analgesic potency
 onset of action is more rapid
 duration is shorter(2-3)hours
 Spasmodic action on smooth muscle is less
marked
 Equally sedative
 similar abuse potential
 the degree of respiratory depression:same.
 less histamine release
 safer in asthmatic
 It has local anesthetic action

 ROUTE:
 Meperidine may be administered orally or by
subcutaneous ,intramuscular or intravenous
injection.
 least effective by mouth.
 very bitter and requires masking by a
flavouring agent.
 By the oral route, peak effect occurs in 1 hour
and lasts about 4 hours.
 Parentral administration shortens the time of
onset and duration
Alcaino E,Mcdonald J,cooper M,malhi S in Cameron A,Widmer R,Hall R,Handbook of
pediatric dentistry,4 th edition,2003 80

 Similar to morphine .
 atropinic effects .
 Overdose produces many excitatory effects-
tremors
mydriasis
hyperreflexia
delirium
myoclonus
convulsions.
This is due to accumulation of norpethidine
which has exctant effect.Renal failure patients
given repeated doses of pethidine may also
experience similar effects.
Dock M,creedon R in Ralph E,Mc Donald,Avery D,Dean J,Dentistry for the child and
adolescent , 9 th edition 2007, pharmacological management of patient behavior 81

 Dosage: oral, sc, im 1.0 to 2.2 mg/kg not to
exceed 100mg
82

 Avoid prescribing for dental use in pregnancy
 After supine positioning ,have patient sit
upright for atleast 2minute before standing
to avoid orthostatic hypotension
 Psychologic and physical dependance may
83

 It is a very potent narcotic analgesic.
 a rapid action and after a submucosal or
intramuscular injection onset will occur in 7
to 15 minutes,
 Because of high lipid solubility it enters brain
rapidly and produces peak analgesia 5 min
after i.v. injection.
Dock M,creedon R in Ralph E,Mc Donald,Avery D,Dean J,Dentistry for the child and
adolescent , 9 th edition 2007, pharmacological management of patient behavior
84

 Respiratory depression. When fenatnyl is used
, one should be attentive to and competent in
airway management.
 With higher doses administered rapidly by
vein ,rigidity of skeletal muscle relaxant and
/or managed by assisted or controlled
ventilation.
 Bradycardia has been reported. Atropine can
be used to normalize heart rate
Dock M,creedon R in Ralph E,Mc Donald,Avery D,Dean J,Dentistry for
the child and adolescent , 9 th edition 2007, pharmacological
management of patient behavior 85

 Route: intramuscular, intravenous, or
submucosal route. When it is used with other
CNS depressants, the dose should be
reduced. The drug works well with orally
administered diazepam and nitrous oxide-
oxygen. It is not recommended for use in
children under 2 years of age.
 Transdermal fentanyl has become available
for use in cancer or other types of chronic
pain for patients requiring opioid analgesia
 Dosage: 0.002 to 0.004 mg/kg
Dock M,creedon R in Ralph E,Mc Donald,Avery D,Dean J,Dentistry for the
child and adolescent , 9 th edition 2007, pharmacological management of 86

 Monitor vital signs at every appointment because
of cardiovascular and respiratory side effects
 After supine positioning,have patient sit upright
for atleast 2 minute before standing to avoid
orthostatic hypotension
 Assess salivary flow as a factor in caries
,periodontal status,candidiasis.
 Psychologic and physical dependence may occur
with chronic administration
 Consider alternative use of NSAIDs to opioids for
treatment of dental pain.
edition 87

 CONSULTATION:
 Medical consultation for disease control may
be required.
 TEACH:
 Effective oral hygiene to prevent gingival
inflammation
88

 Can be used for moderate pain in children
over 12 years of age.
 Injected i.v . 100mg tramadol is
equianalgesic to 10 mg i.m morphine
 Its analgesic action is only partially reversed
by opioid antagonist Naloxone.
 Little tendency to dose escalation is seen and
abuse potential is low.

TRAMADOL
OTHER
MECHANISMS
PREVENTS
REUPTAKE OF
NOR ADRENALINE
INCREASE
NEURONAL
SYNAPTIC 5 HT
OPIOID ACTION
MU,DELTA,KAPPA
RECEPTORS
Activates monoaminergic
spinal inhibition of pain

 Side effects :
 dizziness ,
 nausea,
 sleepiness,
 dry mouth,
 sweating ,
 lowering of seizure threshold.
 Contraindications:
 Avoid use in children with seizure disorders
and those taking tricyclic or selective
serotonin reuptake (ssri) antidepressants.
edition,2007 91

 Determine why the patient is taking the drug
 Patient taking opioids for acute or chronic pain
should be given alternative analgesics for dental
 Geriatric patients are more susceptible to drug
effects;use lower doses in such patients
caries,periodontal status,candidiasis
 Take precautions if dental surgery is antcipated
and general anesthesia is required
 Risk of cross hypersensitivity to other analgesics
edition
92

 TEACH patient/family:
 Use caution to prevent trauma using oral
hygiene aids
 Caution when driving or operating complex
equipments
 When chronic dry mouth occurs advise
patient to:
 Use sugarless gums,frequent sips of water or
saliva substitutes
 Daily home flouride products for anticaries
effects
93

DRUG ABSORBED EXCRETED Plasma t1/2 Bound to
plasma
aspirin orally urine 15-50 min 80%
Ibuprofen Orally Urine and bile 90-99%
diclofenac orally Urine and bile 2 hours 99%
ketorolac orally urine 5-7 hours 40%
nimesulide orally urine 2-5 hours 99%
paracetamol orally urine 2-3 hours 1/4th
edition,2007
94

Drug Absorbed Excreted Plasma
t1/2
Bound to
plasma
Meperidi
ne
Oral Urine 2- 3
hours
70%
Fenatnyl Parentera
lly
Urine,fec
es,human
milk
4 hours 99%
Tramadol Orally Urine 5 hours
Morphine Parentera
lly
Orally:un
reliable
Urine,bile 2-3
hours
30%
Codiene Oral Urine 3-4
hours
7-25%
edition,2007
Ronald miller,jeanine P,lars I,erikson ,lee Afleisher,jeanine
P,wiener kronish,william young in miller ‘s anesthesia 7 h
edition,2010
95

WHO 1996.Cancer pain relief with a guide to opioid availability.cancer
pain relief and palliative care in children
Schug SA ,auret k clinical pharmacology,principes of analgesics of
drug management.2 nd edition 96

 Combination of aspirin and paracetamol is
additive and a ceiling analgesic effect is
obtained when the total amount of
aspirin+paracetamol is 100 mg .
 The same is true for combination of
paracetamol with the other NSAIDs like
ibuprofen,diclofenac etc
 There is no convincing evidence that such
combination are superior to single
agents,either in efficacy or in safety.
 If at all used such combinations should be
limited to short period
97

 Codeine may be given alone or in
combination with another analgesic. Because
the narcotics act at a central site and the non
narcotic analgesics act at a separate site, it is
prudent to combine the two types of
analgesics for enhanced activity. An example
is acetaminophen with codeine.
 Combination of codiene with aspirin or
paracetamol is also additional,Analgesia
beyond the ceiling effects of aspirin
/paracetamol can be obtained
 Such combinations can be used rational
98

Ibuprofen- 100mg and
Paracetamol- 125mg
Syrup: Ibuprofen-100mg
and Paracetamol-162.5mg
Diclofenac- 50mg and
Paracetamol- 500mg
Aceclofenac 100mg and
Paracetamol 500mg
99

1 20 mg
acetaminophen
and 12 mg
codeine/5 mL
Usual oral dosage:
Children 12 years:
15 mL elixir every
4 hours as needed
Liquids 300 mg acetaminophen and 15
mg codeine
300 mg acetaminophen and 30
mg codeine
300 mg acetaminophen and 60
mg codeine
Adults: Based on codeine
30-60 mg dose every 4-6
hours as needed
(maximum 4 g
acetaminophen/24 hours)
OR 1-2 tablets every 4
hours as needed
(maximum of 12 tablets/24
hours)
Tablet
AMERICAN ACADEMY OF PEDIATRIC DENTISTRY
10
0

Liquids:
•300 mg acetaminophen and
10 mg hydrocodone/15 mL
325 mg acetaminophen and
7.5 mg hydrocodone /15 mL
325 mg acetaminophen and
10 mg hydrocodone /15 mL
Higher strengths of
acetaminophen are available
but are not recommended for
children
Tablets
•300 mg acetaminophen in
combination with 5 mg, 7.5
mg,
• 10 mg hydrocodone 325 mg
acetaminophen in combination
with 5 mg, 7.5 mg,
•10 mg hydrocodone
•Higher strengths of
acetaminophen are available
but are not recommended for
children
AMERICAN ACADEMY OF PEDIATRIC DENTISTRY REFERENCE MANUAL V36
NO 614/15
10
1

BASED ON AGE WEIGHT(kg
)
DOSAGE MAXIMUM
CHILD 2-13 YEARS <50 0.135 mg
hydrocodone/kg
every 4-6 hours as
needed
6 doses
hydrocodone/da
y OR maximum
recommended
acetaminophen
dosage
CHILD >13 YEARS >50 2.5-10 mg
hydrocodone every 4-
6 hours as needed
60 mg
hydrocodone/da
y OR 4 g
acetaminophen/
24 hours
ADULT >50 5-10 mg
hydrocodone every 4-
6 hours as needed
60 mg
hydrocodone/da
y OR 4 g
acetaminophen/
24 hours
10
2

Solution
• 325 mg acetaminophen and
5 mg oxycodone/5 mL
(Note: the solution contains
alcohol)
tablets
•300 mg acetaminophen in
combination with 5 mg, 7.5
mg, or 10 mg oxycodone
325 mg acetaminophen in
combination with 2.5 mg, 5
mg, 7.5 mg, or 10 mg
oxycodone Higher strengths
of acetaminophen are
available but are not
recommended for children
AMERICAN ACADEMY OF PEDIATRIC DENTISTRY REFERENCE MANUAL V36 NO
614/15
10
3

CHILDREN
• Children: 0.05-0.15 mg
oxycodone/kg every 4-6
hours as needed. May
titrate up to 5 mg/dose
oxycodone every 4-6
hours
• (maximum 90 mg/kg
acetaminophen/24 hours)
ADULTS
• :2.5-10 mg oxycodone
every 4-6 hours as needed
(maximum 4 g
acetaminophen/24 hours
AMERICAN ACADEMY OF PEDIATRIC DENTISTRY MANUAL V36 NO 614/15 10
4

 Alfenatinil and Ramifenatinil:
 Rapid onset of action
 Metabolized in liver
 Half life is 1-2 hours
 Short,painful procedures requiring intense analgesia
and blunting of stress response.
 Ramifenatanil for longer neurosurgical procedures
wher rapid emergence from anaesthesia is
important.
 Rofecoxib:
 It is NSAID which acts by inhibiting COX 2 .
 It is a potent analgesic .
 However its use has been banned due to an increase
in the risk of cardiovascular episodes like myocardial
infarction and stroke.
Alcaino E,Mcdonald J,cooper M,malhi S in Cameron A,Widmer R,Hall R,Handbook
of pediatric dentistry,4 th edition,2003
10
5

 Valdecoxib:
 Selective COX 2 inhbitor.
 a newer congener of rafecoxib. Even this
drug has been withdrawn from the market
due to increase risk of myocardial infarction,
skin reactions like Steven Johnson‘s
syndrome, toxic epidermal necrolysis etc.
Alcaino E,Mcdonald J,cooper M,malhi S in Cameron A,Widmer R,Hall
R,Handbook of pediatric dentistry,4 th edition,2003
10
6

 Enkephalins inhibitors:
 Methionine –enkephalins(met ENK) and
leucine –enkephalin (leu-ENK)are the most
important.
 pentapeptides
edition,2007,chapter:Introduction,routes of drug administration 10
7

PRECURSOR
PRO
ENKEPHALINS
MET ENK
MU
RECEPTOR
DELTA
RECEPTOR
LEU ENK
DELTA
RECEPTOR
edition,2007,chapter:Introduction,routes of drug administration
10
8

 Enkephalins inhibitor as thiorphan and
experimental drug RB 120 act by inhibiting
metabolic degradation of endogenous opioid
peptides.
 It has morphine like effects without causing
dependence.
 Transplantation of enkephalin-secreting
adrenal medulla cells into spinal canal.
edition,2007,chapter:Introduction,routes of drug administration
10
9

 Non peptide antagonist of substance –P ,
have recently been developed and may prove
to be useful analgesic drugs.
 Adenosine analogues and adenosine kinase
inhibitors.
 Agonist at nicotinic acetylcholine based at
epibatidine
J. R. Sneyd,J. A. Langton, L. G. Allan, J. E. Peacock D. J. Rowbotham, multicentre evaluation of the
adenosine agonist GR79236X in patients with dental pain after third molar extractionBr. J.
Anaesth. (2007) 98 (5):672-676.doi: 10.1093/bja/aem075First published online: April 7, 2007
Cucchiaro G, Xiao Y, Gonzalez-Sulser A, Kellar KJ,Analgesic effects of Sazetidine-A, a new nicotinic
cholinergic drug, 08 Sep;109(3):512-9. doi: 10.1097/ALN.0b013e3181834490.
11
0

Most pediataric patients undergoing dental
treatment do experience pain sometimes pre
operatively or post operatively.
So as pedodontists it is important to
understand completely analgesics and
prescribe accordingly to reduce pain and
thus increase patient comfort.
11
1

 1Tripathi K, Essentials of medical pharmacology ,6 th
edition,2007,chapter:Introduction,routes of drug administration,page
no:3-10
 2 Hawes R in Finn .S, Clinical pedodontics- 4th edition,
2004,chapter:The problem of pain and sedation ,page no:114-134
 3 Alcaino E,Mcdonald J,cooper M,malhi S in Cameron A,Widmer R,Hall
R,Handbook of pediatric dentistry,4 th edition,2003,chapter
:pharmacological behavior management
 4 Leach R.H,Wood BSB drug dosage for children Laneet 2:1350-
1351,1967
 5 Picker G, Dosage calculation,7 th edition,2004,body surface area and
advanced pediatric calculations,p373-393
 6 Bennet C,bonani S,Cassidy M, neston A,phero J,monhiem’s local
anesthesia and pain control in dental practice,7th edition,1990
 7 Tripathi K, Essentials of medical pharmacology ,6 th
edition,2007,chapter:opioid analgesics and antagonists,page no:453-
468
11
2

 8 Tripathi K, Essentials of medical pharmacology ,6 th
edition,2007,chapter:Non steroidal anti inflammatory
drugs and anti pyretic –analgesics, page no:184-201
 9 Wilson S,Ganzberg S in Casamassimo P,Fields H,Mctigue
D.,Nowak A, pediatric dentistry infancy through
adolescence,2013,chapter :pain perception control
 10 Dock M,creedon R in Ralph E,Mc Donald,Avery D,Dean
J,Dentistry for the child and adolescent , 9 th edition 2007,
pharmacological management of patient behavior ,p:285-
311
 11Tate A R, ACSG: Dental clinic of north America 46:707-
712,2002
 12Satoskar R,Bhandarkar S,Rege N,pharmacology and
pharmacotherapeutics,21 st edition,2009,4275,p-159-
180
 13Wilson S,conscious sedation and pulse oximetry,false
alarms,pediatric dentistry 12(4)-232,1990
11
3

 14 R s sneyd,I a langton L.G allan,J.E peacock,D J rowbottham,
multicentre evaluation of the adenosine agonist GR79236X in
patients with dental pain after third molar extractionBr. J.
Anaesth. (2007)
 15 Cacchiario G,Xiao Y,Gonzalez susler A,kellar K.J.,Analgesic effects
of Sazetidine-A, a new nicotinic cholinergic drug, 08 Sep.
 16Figure denoting mechanism of action of
morphine:reference:White P F :the changing role of non
opioid analgesic techniques in the management of post
operative pain.anesthesia ans analgesia 2005;101 :S5
 17aspirin inhibition of COX 1 decreases TXA2 production
source:gasparyan yet al.j am coll,cardiol 2008;51:1829-1843
 18American academy of pediatric dentistry :useful drugs for oral
useREFERENCE MANUAL V36 NO 614/15
 19WHO 1996.Cancer pain relief with a guide to opioid
availability.cancer pain relief and palliative care in children
 20Schug SA ,auret k clinical pharmacology,principes of
analgesics of drug management.2 nd edition
11
4

 21 Ronald miller,jeanine P,lars I,erikson ,lee
Afleisher,jeanine P,wiener kronish,william
young in miller ‘s anesthesia 7 th
edition,2010
 22 American academy of pediatric dentistry
:policy on pain pediatric pain mangement 2012
11
5

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