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-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
REFERENCE: Tripathi K, Essentials of medical pharmacology ,6 th edition,2007
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
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 8
REF:aspirin inhibition of COX 1 decreases TXA2 production
source:gasparyan yet al.j am coll,cardiol 2008;51:1829-1843 9
 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
10
 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
Tripathi K, Essentials of medical pharmacology ,6 th edition,2007 11
 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.
Tripathi K, Essentials of medical pharmacology ,6 th
edition,2007 12
 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.
 Adverse effects:
 Epigastria pain
 Nausea vomiting
 Dizziness, headache
 Rash and purities
REF:Tripathi K, Essentials of medical pharmacology ,6 th edition,2007
13
 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.
Tripathi K, Essentials of medical pharmacology ,6 th
edition,2007 14
 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
Wilson S,Ganzberg S in Casamassimo P,Fields H,Mctigue D.,Nowak A, pediatric dentistry
infancy through adolescence,2013,chapter :pain perception control
15
Blocks COX 3 AND COX 2
ANALGESIC ACTION
16
 Indications:
 Useful as pre emptive analgesic
 Fever due to infection or inflammation
 Pain due to trauma or odontogenic infections
 Headache, musculoskeletal pain
Tripathi K, Essentials of medical pharmacology ,6 th
edition,2007 17
 Adverse effect:
 Hypersensitivity
 Renal or hepatic impairment
 Nausea and rashes occur occasionally,
leucopenia is rare
Tripathi K, Essentials of medical pharmacology ,6 th
edition,2007
18
 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 19
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 20
 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.
Tripathi K, Essentials of medical pharmacology ,6 th edition,2007 21
 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
Tripathi K, Essentials of medical pharmacology ,6 th
edition,2007 22
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
Tripathi K, Essentials of medical pharmacology ,6 th edition,2007 23
 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
Jaske A.in mosby’s dental drug reference book ,2011,10th edition
24
 CLASSIFICATIONS OF OPIOIDS :
 Natural opium alkaloids: morphine, codeine
 Semisynthetic opiates: diacetylmorphine,
pholcodiene
 Synthetic
opioids:pethidiene,fentanyl,methadone,
 dextropropoxyphene,tramadol
Tripathi K, Essentials of medical pharmacology ,6 th
edition,2007
25
NATURAL OPIUM
ALKALOIDS:MORPHINE,CODIENE
SYNTHETIC
OPIOIDS:PETHIDINE(MEPERIDIENE),FENATNYL,
TRAMADOL
26
 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
Tripathi K, Essentials of medical pharmacology ,6 th
edition,2007
27
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
28
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 29
 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.
Tripathi K, Essentials of medical pharmacology ,6 th
edition,2007,
30
 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 .
Tripathi K, Essentials of medical pharmacology ,6 th
edition,2007,
31
 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

Tripathi K, Essentials of medical pharmacology ,6 th
edition,2007
32
 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 .
33
 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 34
 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.
Jaske A.in mosby’s dental drug reference book ,2011,10th edition
35
 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.
Jaske A.in mosby’s dental drug reference book ,2011,10th edition
36
 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
Tripathi K, Essentials of medical pharmacology ,6 th
edition,2007
37
ACTS ON MU OPIOID RECEPTOR
MORPHINE
CODIENE
EMETHYLATION BY CP2D6
Tripathi K, Essentials of medical pharmacology ,6 th 38
 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
 Adverse effects:
 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 39
 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
Wilson S,Ganzberg S in Casamassimo P,Fields H,Mctigue D.,Nowak A, pediatric dentistry
infancy through adolescence,2013,chapter :pain perception control
40
 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
 Assess salivary flow as a factor in
caries,periodontal status,candidiasis.
 Psychologic and physical dependence may
occur with chronic administration
Jaske A.in mosby’s dental drug reference book
,2011,10th edition 41
 TEACH patient/relative:
 When chronic dry mouth occurs,advise
patient to:
 Avoid mouth rinses with alcohol content
because of drying effects
 Use daily home flourides
 Use sugarless gum,frequently sips of water or
salivary substitute.
Jaske A.in mosby’s dental drug reference book ,2011,10th
edition 42
 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
Tripathi K, Essentials of medical pharmacology ,6 th edition,2007 43
 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 44
 Adverse effects:
 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 45
 Dosage: oral, sc, im 1.0 to 2.2 mg/kg not to
exceed 100mg
Tripathi K, Essentials of medical pharmacology ,6 th edition,2007
46
 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
occur with chronic administration
 TEACH patient/relative:
 Avoid mouth rinses with high alcohol content
because of drying effects.
Jaske A.in mosby’s dental drug reference book ,2011,10th edition
47
 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
48
 Adverse effects:
 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 49
 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 50
 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.
Jaske A.in mosby’s dental drug reference book ,2011,10th
edition 51
 CONSULTATION:
 Medical consultation for disease control may
be required.
 TEACH:
 Effective oral hygiene to prevent gingival
inflammation
 Avoid mouth rinses with high alcohol content
because of drying effects.
Jaske A.in mosby’s dental drug reference book ,2011,10th edition
52
 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.
Tripathi K, Essentials of medical pharmacology ,6 th edition,2007 53
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
Tripathi K, Essentials of medical pharmacology ,6 th edition,2007 54
 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.
Tripathi K, Essentials of medical pharmacology ,6 th
edition,2007 55
 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
 Assess salivary flow as a factor in
caries,periodontal status,candidiasis
 Take precautions if dental surgery is antcipated
and general anesthesia is required
 Risk of cross hypersensitivity to other analgesics
Jaske A.in mosby’s dental drug reference book ,2011,10th
edition
56
 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:
 Avoid mouth rinses with high alcohol content
because of drying effects
 Use sugarless gums,frequent sips of water or
saliva substitutes
 Daily home flouride products for anticaries
effects
Jaske A.in mosby’s dental drug reference book ,2011,10th edition
57
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
Tripathi K, Essentials of medical pharmacology ,6 th
edition,2007
58
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%
Tripathi K, Essentials of medical pharmacology ,6 th
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
59
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 60
 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
Tripathi K, Essentials of medical pharmacology ,6 th edition,2007
61
 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
Tripathi K, Essentials of medical pharmacology ,6 th edition,2007
62
Ibuprofen- 100mg and
Paracetamol- 125mg
Syrup: Ibuprofen-100mg
and Paracetamol-162.5mg
Diclofenac- 50mg and
Paracetamol- 500mg
Aceclofenac 100mg and
Paracetamol 500mg
63
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 64
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 65
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
66
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 67
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 68
 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
69
 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 70
 Enkephalins inhibitors:
 Methionine –enkephalins(met ENK) and
leucine –enkephalin (leu-ENK)are the most
important.
 pentapeptides
Tripathi K, Essentials of medical pharmacology ,6 th
edition,2007,chapter:Introduction,routes of drug administration
71
PRECURSOR
PRO
ENKEPHALINS
MET ENK
MU
RECEPTOR
DELTA
RECEPTOR
LEU ENK
DELTA
RECEPTOR
Tripathi K, Essentials of medical pharmacology ,6 th
edition,2007,chapter:Introduction,routes of drug administration 72
 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.
Tripathi K, Essentials of medical pharmacology ,6 th
edition,2007,chapter:Introduction,routes of drug administration
73
 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. 74
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.
75
 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
76
 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
77
 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
78
 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
79
80

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Pedodontic Fear mamngement.pptx

  • 3.  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
  • 4.  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
  • 5.  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
  • 6.  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 REFERENCE: Tripathi K, Essentials of medical pharmacology ,6 th edition,2007 6
  • 7.  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
  • 8. 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 8
  • 9. REF:aspirin inhibition of COX 1 decreases TXA2 production source:gasparyan yet al.j am coll,cardiol 2008;51:1829-1843 9
  • 10.  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 10
  • 11.  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 Tripathi K, Essentials of medical pharmacology ,6 th edition,2007 11
  • 12.  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. Tripathi K, Essentials of medical pharmacology ,6 th edition,2007 12
  • 13.  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.  Adverse effects:  Epigastria pain  Nausea vomiting  Dizziness, headache  Rash and purities REF:Tripathi K, Essentials of medical pharmacology ,6 th edition,2007 13
  • 14.  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. Tripathi K, Essentials of medical pharmacology ,6 th edition,2007 14
  • 15.  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 Wilson S,Ganzberg S in Casamassimo P,Fields H,Mctigue D.,Nowak A, pediatric dentistry infancy through adolescence,2013,chapter :pain perception control 15
  • 16. Blocks COX 3 AND COX 2 ANALGESIC ACTION 16
  • 17.  Indications:  Useful as pre emptive analgesic  Fever due to infection or inflammation  Pain due to trauma or odontogenic infections  Headache, musculoskeletal pain Tripathi K, Essentials of medical pharmacology ,6 th edition,2007 17
  • 18.  Adverse effect:  Hypersensitivity  Renal or hepatic impairment  Nausea and rashes occur occasionally, leucopenia is rare Tripathi K, Essentials of medical pharmacology ,6 th edition,2007 18
  • 19.  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 19
  • 20. 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 20
  • 21.  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. Tripathi K, Essentials of medical pharmacology ,6 th edition,2007 21
  • 22.  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 Tripathi K, Essentials of medical pharmacology ,6 th edition,2007 22
  • 23. 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 Tripathi K, Essentials of medical pharmacology ,6 th edition,2007 23
  • 24.  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 Jaske A.in mosby’s dental drug reference book ,2011,10th edition 24
  • 25.  CLASSIFICATIONS OF OPIOIDS :  Natural opium alkaloids: morphine, codeine  Semisynthetic opiates: diacetylmorphine, pholcodiene  Synthetic opioids:pethidiene,fentanyl,methadone,  dextropropoxyphene,tramadol Tripathi K, Essentials of medical pharmacology ,6 th edition,2007 25
  • 27.  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 Tripathi K, Essentials of medical pharmacology ,6 th edition,2007 27
  • 28. 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 28
  • 29. 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 29
  • 30.  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. Tripathi K, Essentials of medical pharmacology ,6 th edition,2007, 30
  • 31.  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 . Tripathi K, Essentials of medical pharmacology ,6 th edition,2007, 31
  • 32.  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  Tripathi K, Essentials of medical pharmacology ,6 th edition,2007 32
  • 33.  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 . 33
  • 34.  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 34
  • 35.  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. Jaske A.in mosby’s dental drug reference book ,2011,10th edition 35
  • 36.  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. Jaske A.in mosby’s dental drug reference book ,2011,10th edition 36
  • 37.  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 Tripathi K, Essentials of medical pharmacology ,6 th edition,2007 37
  • 38. ACTS ON MU OPIOID RECEPTOR MORPHINE CODIENE EMETHYLATION BY CP2D6 Tripathi K, Essentials of medical pharmacology ,6 th 38
  • 39.  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  Adverse effects:  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 39
  • 40.  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 Wilson S,Ganzberg S in Casamassimo P,Fields H,Mctigue D.,Nowak A, pediatric dentistry infancy through adolescence,2013,chapter :pain perception control 40
  • 41.  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  Assess salivary flow as a factor in caries,periodontal status,candidiasis.  Psychologic and physical dependence may occur with chronic administration Jaske A.in mosby’s dental drug reference book ,2011,10th edition 41
  • 42.  TEACH patient/relative:  When chronic dry mouth occurs,advise patient to:  Avoid mouth rinses with alcohol content because of drying effects  Use daily home flourides  Use sugarless gum,frequently sips of water or salivary substitute. Jaske A.in mosby’s dental drug reference book ,2011,10th edition 42
  • 43.  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 Tripathi K, Essentials of medical pharmacology ,6 th edition,2007 43
  • 44.  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 44
  • 45.  Adverse effects:  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 45
  • 46.  Dosage: oral, sc, im 1.0 to 2.2 mg/kg not to exceed 100mg Tripathi K, Essentials of medical pharmacology ,6 th edition,2007 46
  • 47.  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 occur with chronic administration  TEACH patient/relative:  Avoid mouth rinses with high alcohol content because of drying effects. Jaske A.in mosby’s dental drug reference book ,2011,10th edition 47
  • 48.  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 48
  • 49.  Adverse effects:  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 49
  • 50.  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 50
  • 51.  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. Jaske A.in mosby’s dental drug reference book ,2011,10th edition 51
  • 52.  CONSULTATION:  Medical consultation for disease control may be required.  TEACH:  Effective oral hygiene to prevent gingival inflammation  Avoid mouth rinses with high alcohol content because of drying effects. Jaske A.in mosby’s dental drug reference book ,2011,10th edition 52
  • 53.  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. Tripathi K, Essentials of medical pharmacology ,6 th edition,2007 53
  • 54. 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 Tripathi K, Essentials of medical pharmacology ,6 th edition,2007 54
  • 55.  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. Tripathi K, Essentials of medical pharmacology ,6 th edition,2007 55
  • 56.  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  Assess salivary flow as a factor in caries,periodontal status,candidiasis  Take precautions if dental surgery is antcipated and general anesthesia is required  Risk of cross hypersensitivity to other analgesics Jaske A.in mosby’s dental drug reference book ,2011,10th edition 56
  • 57.  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:  Avoid mouth rinses with high alcohol content because of drying effects  Use sugarless gums,frequent sips of water or saliva substitutes  Daily home flouride products for anticaries effects Jaske A.in mosby’s dental drug reference book ,2011,10th edition 57
  • 58. 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 Tripathi K, Essentials of medical pharmacology ,6 th edition,2007 58
  • 59. 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% Tripathi K, Essentials of medical pharmacology ,6 th 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 59
  • 60. 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 60
  • 61.  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 Tripathi K, Essentials of medical pharmacology ,6 th edition,2007 61
  • 62.  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 Tripathi K, Essentials of medical pharmacology ,6 th edition,2007 62
  • 63. Ibuprofen- 100mg and Paracetamol- 125mg Syrup: Ibuprofen-100mg and Paracetamol-162.5mg Diclofenac- 50mg and Paracetamol- 500mg Aceclofenac 100mg and Paracetamol 500mg 63
  • 64. 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 64
  • 65. 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 65
  • 66. 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 66
  • 67. 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 67
  • 68. 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 68
  • 69.  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 69
  • 70.  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 70
  • 71.  Enkephalins inhibitors:  Methionine –enkephalins(met ENK) and leucine –enkephalin (leu-ENK)are the most important.  pentapeptides Tripathi K, Essentials of medical pharmacology ,6 th edition,2007,chapter:Introduction,routes of drug administration 71
  • 72. PRECURSOR PRO ENKEPHALINS MET ENK MU RECEPTOR DELTA RECEPTOR LEU ENK DELTA RECEPTOR Tripathi K, Essentials of medical pharmacology ,6 th edition,2007,chapter:Introduction,routes of drug administration 72
  • 73.  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. Tripathi K, Essentials of medical pharmacology ,6 th edition,2007,chapter:Introduction,routes of drug administration 73
  • 74.  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. 74
  • 75. 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. 75
  • 76.  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 76
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