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Hi. This is Dr. Amit T. Suryawanshi. Oral & Maxillofacial surgeon from Pune, India. I am here on slideshare.com to share some of my own presentations presented at various levels in the field of OMFS. Hope this would somehow be helpful to you making your presentations. All the best & your replies are welcomed!
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Analgesics in maxillofacial surgery by Dr. Amit Suryawanshi .Oral & Maxillofacial Surgeon, Pune , India
1. AAnnaallggeessiiccss
Dr. Amit T. Suryawanshi
Oral and Maxillofacial Surgeon
Pune, India
Contact details :
Email ID - amitsuryawanshi999@gmail.com
Mobile No - 9405622455
2. CCoonntteennttss
Introduction
– Pain
– Analgesia
Analgesics
Classification of analgesics
NSAID’s
– History
– Classification of NSAID’s
– Mechanism of action
– Adverse effects
– Individual drugs
3. CCoonntteennttss
Opioids
– Classification of opioids
– Individual drugs
– Opioid receptors
– Complex action opioids and opioid antagonists
- Opioids in dental pain
Analgesics and Medical conditions
Adjuvant drugs
Future of Analgesics
References
4. IInnttrroodduuccttiioonn
PPaaiinn --
“ 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 ”
- Monheim’s
“Pain is whatever the experiencing person says it is
and exists whenever he says it does.”
5. GGooaallss ooff ppaaiinn mmaannaaggeemmeenntt
To relieve suffering
To increase functional capacity
To improve quality of life
6. MMeetthhooddss ooff ppaaiinn ccoonnttrrooll
1. Removing the cause
2. Blocking the pathway of painful impulses
3. Raising the pain threshold
4. Preventing pain reaction by cortical depression
5. Using psychosomatic methods
7. WWhhaatt iiss AAnnaallggeessiiaa??
The word analgesia is derived from Greek word
analgetos (an – without ; algesia – pain )
‘Analgesia simply means the absence of pain without
losing consciousness’
“The analgesia system is mediated by 3 major
components :
1. Periaquaductal grey matter
2. Nucleus raphe magnus
3. Pain inhibitory neurons
8. Analgesics
Definition -
“Analgesics are drugs that selectively relieve
pain by acting in the CNS or on the peripheral
pain mechanisms, without altering
consciousness”
9. HHiissttoorryy ooff AAnnaallggeessiiccss
BBCC:: Ancient Greeks and Romans used salicylate
extracts derived from willow leaves as analgesics
and antipyretics
Middle Ages: Medicinal herb gardens featured
salicylate containing wintergreen and meadowsweet
plants
1763: Edward Stone reported on use of willow bark
powder as an anti-inflammatory agent.
1853: Von Gerhardt synthesized a crude form of
aspirin (acetylsalicylic acid)
1860: Felix Hoffman synthesized pure aspirin
10. continued
Opiates are one of the oldest types of drugs in history
Opium is extracted from poppy seeds (Paper
somniforum)
Undisputed reference to opium found in writings from
the third century BC
Use of Opium was first recorded in China over 2000
years ago
Greeks dedicated the Opium poppy to the Gods of Death
(Thanatos), Sleep (Hypnos), and Dreams (Morpheus)
Sixteenth Century is the first reported use of Opium for
its Analgesic qualities
11. Contnd…
1949: The NSAID Phenylbutazone was introduced
1963: Indomethacin was introduced
1971: Vane and Piper demonstrated that NSAIDs inhibit
prostaglandin production
1974: Ibuprofen was introduced
1976: Miyamoto et al identified the COX-1 enzyme
1989: Simmons et al identified the COX-2 enzyme
1999: The COXIBs celecoxib and rofecoxib were introduced
2004: Rofecoxib was banned in india due to its cardiotoxic effect .
14. NSAIDs aanndd pprroossttaaggllaannddiinn ((PPGG))
ssyynntthheessiiss iinnhhiibbiittiioonn
Prostaglandins, prostacyclin (PGI2) and thromboxane
A2(TXA2) are produced from arachidonic acid by the
enzyme cyclo oxygenase which exists in 2 forms
– (COX-1) - Cyclo oxygenase -1
– (COX-2) - Cyclo oxygenase -2
• Most NSAID’s inhibit COX-1 and COX-2
non selectively
• Some selective COX-2 inhibitors have now been
produced
18. TTooxxiicciittiieess dduuee ttoo PPGG ssyynntthheessiiss
iinnhhiibbiittiioonn
Gastric mucosal damage
Bleeding: inhibition of platelet function
Limitation of renal blood flow: sodium and water
retention
Delay / prolongation of labour
Asthma and anaphylactic reactions in susceptible
individuals
23. SSaalliiccyyllaatteess --AAsspprriinn
Is acetylsalicylic acid
Pharmacological actions
– Analgesic, antipyretic, anti inflammatory actions
• Analgesic action is due to prevention of PG mediated
sensitization of nerve endings
• Resets the hypothalamic thermoregulatory centre
• Anti inflammatory at high doses
– Blood
• Irreversibly inhibits TXA2 synthesis thus interferes
with platelet aggregation and BT is prolonged
• Long term use of large doses decreases synthesis of
clotting factors in liver
24. AAssppiirriinn
– Respiration
• Anti inflammatory doses – stimulates respiration
• Hyperventilation in salicylate poisoning, in doses
higher than this there is respiratory depression
– Acid-base electrolyte balance
• Adults treated with aspirin 4-6g/day stay in a state of
compensated respiratory alkalosis
• Still higher doses can cause respiratory acidosis
• Dehydration occurs in poisoning due to increased
urine output, sweating and hyperventilation
– CVS
• No direct effect in therapeutic doses
25. AAssppiirriinn
– GIT
• Aspirin irritates gastric mucosa & causes epigastric
pain, nausea and vomiting
• ‘Ion trapping’ in gastric mucosa increases gastric
toxicity
• Acute ulcers, erosive gastritis, congestion and
microscopic hemorrhages
– Metabolic effects
• Chronic use can cause negative nitrogen balance by
increased conversion of protein to carbohydrate.
26. AAssppiirriinn
Pharmacokinetics
– Absorbed from stomach and small intestine
Precautions and contraindications
– Contraindicated in patients sensitive to it and in
peptic ulcer, bleeding tendencies, & in children
suffering from chicken pox or influenza. (due to
risk of Reye’s syndrome)
– In chronic liver disease
– Asprin should be stopped 5 days before elective
surgery, dental extraction
– Pregnancy and lactating mothers
27. AAsspprriinn
Adverse effects
– Most important – gastric mucosal damage and
peptic ulceration
– Acute salicylate poisoning
– Assosiated with Reye’s syndrome
Uses
– As analgesic
– As antipyretic
– Acute rheumatic fever
– Rheumatoid arthritis
– Osteoarthritis
28. PPrrooppiioonniicc aacciidd ddeerriivvaattiivveess
Ibuprofen –
first introduced member of this class
Anti inflammatory efficacy is lower than asprin
Inhibit Prostaglandin synthesis
Adverse effects
– Milder and better tolerated than asprin
– GI disturbances are present
– Precipitate asprin-induced asthma
29. PPrrooppiioonniicc aacciidd ddeerriivvaattiivveess
Pharmacokinetics
– Well absorbed orally
Uses
– Analgesic and Antipyretic and anti-inflammatory
– Soft tissue injuries, tooth extraction, fractures, post
operative pain.
– Rheumatoid arthritis, osteoarthritis and
musculoskeletal disorders… where pain is more
prominent than inflammation
30. AAnntthhrraanniilliicc aacciidd ddeerrvvaattiivvee
Mephenamic acid-
– Inhibits COX & antagonises certain actions of PG’s
– Exerts peripheral as well as central analgesic action
Pharmacokinetics
– Oral absorption is slow but complete
Adverse effects - Diarrhoea
Uses
– Muscle, joint and soft tissue pain
– Effective in dysmenorrhoea
31. AArryyll--aacceettiicc aacciidd ddeerriivvaattiivvee
Diclofenac sodium
– Inhibits PG synthesis
– Has short lasting anti platelet action
– Adverse effects are mild
Pharmacokinetics
– Well absorbed orally
– Excreted both in urine and bile
Uses
– Toothache
– Post operative and post traumatic inflammatory conditions
– Rheumatoid arthritis and osteoarthritis
32. OOxxiiccaamm ddeerriivvaattiivveess
Piroxicam -
– Long acting NSAID
– Reversible inhibitor of COX
Pyrrolo-pyrrole derivative
Ketorolac
– Potent analgesic and moderate anti inflammatory
activity
– Used in post operative pain after surgery and acute
dental pain
33. IInnddoollee ddeerriivvaattiivvee
Indomethacin
– Potent antiinflammatory and antipyretic action
– High incidence of GI and CNS side effects.
Pyrazolones derivative
Metamizol and propiphenazone are used as analgesic
and antipyretics
34. PPrreeffeerreennttiiaall CCOOXX--22 iinnhhiibbiittoorrss
Nimesulide
– Newer NSAID
– Completely absorbed orally
– Used in patient with history of asthma and
anaphylactic reactions to other NSAIDs.
– Used for short-lasting painful inflammatory
conditions like -
- sports injuries,
- sinusitis and other ENT disorders
- fever and low back pain
Adverse effect – Hepatotoxic in pediatric patients .
35. PPaarraa--aammiinnoo pphheennooll ddeerriivvaattiivveess
Paracetamol (Acetaminophen) -
– Central analgesic action similar to asprin, i.e it raises
pain threshold
– Has weak peripheral anti inflammatory component
– Promptly acting antipyretic
Pharmacokinetics
– Well absorbed orally
– Effects after oral dose last for 3-5 hours
Adverse effects
– Acute paracetamol poisoning – children
36. PPaarraacceettaammooll ((AAcceettaammiinnoopphheenn))
Uses –
– Most commonly used drug & One of the best
antipyretic drugs
– Can be used in all age groups, also in pregnant
and lactating women
Clinical studies have found paracetamol and
asprin to be equally effective in relieving pain
after 3rd molar extraction
And it is more safer than asprin – lesser GI
disturbances and bleeding tendencies
39. MMoorrpphhiinnee
– Alkaloid of opium
– Widely used
Pharmacological actions
CNS
– Analgesia
• Strong analgesic
• Nociceptive pain arising from peripheral pain
receptors is better relieved than neuritic pain
• Reactions associated with intense pain –
apprehension, fear are also depressed
40. MMoorrpphhiinnee
– CNS
– Sedation
• Drowsiness and indifference to surroundings as well
as to own body , ataxia and apparent excitement also
occur
• Higher doses produce sleep and coma
– Mood and subjective changes
• Calming effect
• Loss of apprehension, feeling of detachment,mental
clouding and inability to concentrate
41. MMoorrpphhiinnee
– Respiratory and cough centres
• Depresses Repiration and Cough centre
– Temperature regulating and vasomotor centre
• Depressed
– CTZ, vagal centre & certain cortical areas are
stimulated
– GIT
• Constipation is a prominent feature
42. MMoorrpphhiinnee
Neuro-endocrine
– Enhances ADH release and so urine volume is reduced
– Causes sympathetic stimulation – mild hypoglycemia
CVS
– Causes vasodilation
– Cardiac work is consistently reduced due to decrease in
peripheral resistance
43. MMoorrpphhiinnee
Pharmacokinetics
– Oral absorption is unreliable – high and variable first
pass metabolism
– Freely crosses placenta, affects foetus more than the
mother
Adverse effects
– Mental clouding, sedation and lethargy
– constipation
– Acute morphine poisoning
• Human lethal dose is 250mg .
• Death is due to respiratory failure
44. MMoorrpphhiinnee
Tolerance and dependence
– Partly pharmacokinetic (enhanced rate of metabolism)
but mainly pharmacodynamic (cellular tolerance)
– Treated by substitution with oral methadone
Precautions and contraindications
– Infants and elderly
– Bronchial asthma
– Head injury
45. CCooddeeiinnee
Is methyl morphine
Less potent than morphine (1/10th as analgesic)
Is more selective cough suppressant
46. PPeetthhiiddiinnee
Synthesized as an atropine substitute
Interacts with opioid receptors (mu)
Similar to morphine in most of its properties
– Uses
• As analgesic (substitute to morphine)
• In pre anaesthetic medication
47. MMeetthhaaddoonnee
Chemically dissimilar but pharmacologically
similar to morphine
Used
– primarily as substitution therapy for opioid
dependence
– Also in methadone maintenance therapy
48. TTrraammaaddooll
Centrally acting analgesic
It is believed to work through modulation of serotonin
and norepinephrine in addition to its relatively-weak μ-
opioid receptor agonism
100mg tramadol IV is equally analgesic to 10mg
morphine IM
Uses
– Mild to moderate intensity short lasting pain due to
surgery, dental procedures, injury etc
49. OOppiiooiidd rreecceeppttoorrss
Opioids interact with specific receptors present on neurons
in the CNS and peripheral tissues
Radioligand binding studies divide receptors into
– mu, kappa and delta
Pattern of effect of particular agent depends on the nature
of its interaction with different opioid receptors and also
its relative affinity to these receptors
51. PPeennttaazzooccaaiinnee
Indicated in post operative and moderately severe
pain in trauma, cancer and burns,
Naloxone
Competitive antagonist for all opioid receptors
Injected i.v (0.4- 0.8mg) it antagonizes all actions
of morphine
Drug of choice in morphine poisoning
52. OOppiiooiiddss iinn ddeennttaall ppaaiinn
Opioids are less effective and suitable than NSAID’s for
dental pain
Mostly used as additional drugs with NSAID’s to boost
their analgesic effect
Among opioids oral codeine is most suitable
Oral tramadol and pentazocine are alternatives
Injectable opioids like morphine, pethidine are limited
to intra-operative use to supplement anaesthesia and to
allay apprehension
53. AAnnaallggeessiiccss && MMeeddiiccaall ccoonnddiittiioonnss
NSAIDs should be given in 2nd triemister of
pregnancy and opioids should be avoided .
Paracetamol is the safest drug to use in pregnancy
Aspirin & Ibuprofen should not be given in
asthmatic patients
Aspirin & Paracetamol should not be given in
nephropathy.
Codein should not be used in renal dysfunction
while fentanyl & methadone are safe .
54. AAddjjuuvvaanntt ddrruuggss
To supplement the action of analgesics
To limit the side effects of analgesics
Adjuvants
– Steroids
– Anti arrythmics
– Anti depressants
– Anti epileptics
– Serotonin reuptake inhibitors
– Muscle relaxants
Adjuvant medications are mostly used for chronic pain
Cox 1 – kidney, stomach, blooad vessels .
Cox 2 – activated leucocytes and lymphocytes in the region of inflammation.
Whenever there is inflammatory simulus like tooth ache, dental extraction , maxilla or mandible fracture …
Phospholipase A2 is secreted from cells in the region of inflammation (mainly present in kidney and pancreas) and acts on phospholipid component of cell to release arachidonic acid.
Arachidonic acid is a polyunsaturated fatty acid , and is abundant in the brain, muscles, liver.
Cyclooxygenase is an enzyme present in different cells of the body
COX 1 is present in Kidney, stomach and blood vessels
COX 2 is present in activated leucocytes , macrophages in the region of inflammation
These 2 enzymes act on arachidonic acid to produce its active metabolites called as eicosanoids
Eicosanoids include prostaglandins and leukotrienes which are inflammatory mediators which sensitize pain receptors to histamine , serotonin and bradykinin to cause pain & inflammation.. Pg disturbs fucnction of hypothalamic thermoregulatory centre in brain and causes elevated body temprature,..
COX 1 enzyme converts arachidonic acid to prostaglandins which do housekeeping functions
Blood clotting , kidney function and stomach protection …so when we prescribe non selective cox inhibitors and preferential cox 2 inhibitors , they inhibit these prostglandins also and affect blood clotting ( aspirin ) , gastric mucosa damage ( ibuprofen , aspirin )
COX 2 enzyme converts arachidonic acid to inflammatory prostglandins which contribute to pain inflammation and elevate body temp. so when we prescribe selective cox 2 inhibitors … then they produce analgesic , antipyretic and intiinflammatory effect only ..rather than affecting blood clotting , kidney function and irritating gastric mucosa…
Local - When NSAids enter stomach (Unionised ) then they enter gastric mucosal cells and become ionised at PH of cell.then they Accumulate there and cause damage to mucosa .
Systemic – they inhibit PG synthesis which are protectors of gastric mucosa.
ORAL 10-50 mg tabs ( Morcontin ) QID
IM or SC 10-15 mg/ml (Morphine sulphate)
IV 2-6 mg
ORAL 10-50 mg tabs ( Morcontin )
IM or SC 10-15 mg (Morphine sulphate)
IV 2-6 mg
ORAL 10-50 mg tabs ( Morcontin )
IM or SC 10-15 mg (Morphine sulphate)
IV 2-6 mg
ORAL 10-50 mg tabs ( Morcontin )
IM or SC 10-15 mg (Morphine sulphate)
IV 2-6 mg
ORAL 10-50 mg tabs ( Morcontin )
IM or SC 10-15 mg (Morphine sulphate)
IV 2-6 mg
Morphin poisoning – shallow breathing , cynosis , fall in BP , shock,convulsions, coma , death .
Treatment of poisoning-
Respiratory suppor with the help of ventilator , maintain BP with fluids and vasoconstrictors , gastric lavage with pot. Permangnate,
Naloxone 0.4-0.8 mg IV repeated every 2-3 mins till resp picks up
Nalorphine 3-5 mg IV
ORAL 10-50 mg tabs ( Morcontin ) QID
IM or SC 10-15 mg (Morphine sulphate)
IV 2-6 mg
Its shouldn’t be given in head injusry cause it increases intracranial pressure
Morphine causes respiratory depression hence not being used as a preanasthetic medication
ORAL 100mg tab every 4 hourly
IM 100mg/ 2ml injection every 4 hourly
Analgesia , sedation and reduced GI mobility are common actions of all receptors
Pentazocin
ORAL 30-60mg every 4 hrly
Opioids cause drug dependence , cns depression along with analgesic effect .
Codein---
ORAL - 30-60mg tab Codein QID
Combination with aspirin
ORAL Codopyrin, Apidin -- aspirin 325 mg + codein 30 mg
Pentazocin --ORAL 30-60mg every 4 hrly
Tramadol ---ORAL 100mg tab ( cotramol , domadol)
IV 50mg / ml in 2 ml ampules
IV morphine
IM or SC 10-15 mg (Morphine sulphate)
IV 2-6 mg
pethidine IM 100mg/ 2ml injection every 4 hourly
Miscarriage risk in first trimester
Premature Ductus Arteriosus closure in third trimester
Safe in preg
Ibuprofen (Motrin)
Indomethacin (Indocin)
Ketoprofen (Orudis)
Naproxen (Naprosyn)
Piroxicam (Feldene)
Sulindac (Clinoril)
Aspirin is contraindicated coz there r chances of perinatal death , neonatal hemorg
Asthma –
nimesulide is preferential cox 2 and can be used