ANALGESICS AND
ANTIINFLAMMATORY
DRUGS

INDIAN DENTAL ACADEMY
Leader in continuing dental education
www.indiandentalacademy...
PAIN (Algesia)

“Pain is an unpleasant sensory and
emotional experience associated with
actual or potential tissue damage ...
WHY FEEL PAIN?

• Gives conscious awareness of tissue
damage
• Protection:
– Removes body from danger
– Promotes healing b...
LOCALIZATION OF PAIN

• Superficial Somatic Pain arises from
skin areas

• Deep Somatic Pain arises from
muscle, joints, t...
FAST AND SLOW PAIN

• Most pain sensation is a combination of the
two types of message.
– If we prick our finger we first ...
• FAST PAIN (acute)
– Occurs rapidly after stimuli (0.1
second)
– Sharp pain like needle puncture or cut
– Not felt in dee...
• SLOW PAIN (chronic)
– Begins more slowly & increases in
intensity
– In both superficial and deeper tissues
– Smaller unm...
PAIN PATHWAY

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ANALGESIC

• It is a drug that selectively relieves pain
by acting in the CNS or on peripheral
pain mechanisms,without sig...
ANALGESICS

Analgesics can be:-

a) Opioid/Narcotic
b) Non opioid/Non narcotic
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OPIOID ANALGESICS

Derived from opium
 It has 2 types of alkaloids:-

Phenanthrene

Benzoisoquinoline

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CLASSIFICATION

1 .Natural Opium AlkaloidsMorphine,Codeine
2. Semisynthetic OpiatesDiacetylmorphine,Pholcodeine
3. Synthet...
OPIOID ANALGESICS
AND ANTAGONISTS
OPIOID DRUGS

Agonists

Mixed actions

Antagonists

Morphine

Naloxone

Heroin
Methadone...
MECHANISM OF ACTION

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RECEPTORS

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OPIOID RECEPTORS

• Mu opioid receptor-

Respiratory depression
Euphoria
Physical dependence
Pupil constriction
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• Kappa opiod receptor-

Sedation
Spinal anaesthesia
Pupil constriction
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• Sigma opioid receptor-

Hallucinations
Dysphoria
Pupil dilation
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POPPY PLANT

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MORPHINE

• Serturner,1806 morphine –Morpheus.
• Source- crude opium
• Prototype agonist

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MECHANISM OF ACTIONa) Morphine + receptors
Hyperpolarization of nerve cells
Inhibition of nerve firing
Presynaptic inhibit...
b) Morphine + k receptors

Reduces release of substance P
c) Morphine inhibits release of
excitatory transmitters from ner...
MECHANISM OF ACTION

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NOCICEPTORS

• Nociceptors are special receptors that
respond only to noxious stimuli and
generate nerve impulses which th...
ACTION

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ACTIONS

a) Analgesia: Selective
 Raises pain threshold at spinal cord level
 Alters brain perception of pain

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b) Euphoria:- stimulates ventral tegmentum
c) Respiration:d) Depression of cough reflex:e) Miosis:-

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f) Emesis:g) Cardiovascular:h) G.I. tract:i) Histamine Release:j) Hormonal actions:www.indiandentalacademy.com
USES

a. Analgesia

b. Treatment of diarrhoea
c. Relief of cough
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ADVERSE EFFECTS



Respiratory depression



Nausea and vomiting,constipation



Addiction potential
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MEPERIDINE
• It is a synthetic opioid used for acute pain.
1.MECHANISM OF ACTION:Meperidine+k receptors
2. ACTIONS: Depre...
Contracts smooth muscle
i.v.;
in peripheral resistance
It decreases gastric motility
Dilates the pupils
3. THERAPEUTIC...
5. ADVERSE EFFECTS:Large doses lead to tremors,muscle twitches
6.DRUG INTERACTIONS:It increases depression along with majo...
METHADONE
 High oral parenteral activity ratio (1:2) and firm
binding to tissue proteins.
1. MECHANISM OF ACTION:Methadon...
3.THERAPEUTIC USES:a) SUBSTITUTION THERAPY OF OPIOID
DEPENDENCE;
1 mg of oral methadone for 4 mg of opioid ,2
mg of heroin...
5.ADVERSE EFFECTS:Dependence
Mild withdrawal syndrome

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FENTANYL
It is 80-100 times more potent than morphine.
1.ACTIONS:Analgesia
Respiratory depression
2.THERAPEUTIC USES:An...
Along with Droperidol,it causes NEUROLEPT
ANAESTHESIA

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PROPOXYPHENE

It is a derivative of methadone

2.USES:d isomer leads to analgesia
l isomer leads to antitussive action
w...
3.SIDE EFFECTS: Nausea,vomiting
 Toxic doses ; respiratory depression
 Used with alcohol,sedatives ;severe CNS
depressi...
CODEINE
It is a less potent analgesic than morphine having
higher oral efficacy
ACTIONS:Analgesia
Sedation
Euphoria
D...
PENTAZOCINE

1.MECHANISM OF ACTION:It is an agonist on k receptors and weak antagonist
on mu and delta receptors.
2.USES:A...
3.ACTIONS: Analgesia by activating receptors in the spinal
cord
4.ADVERSE EFFECTS:Higher dose;respiratory depression
To...
BUPRENORPHINE

 It is a partial agonist acting at the mu
receptors metabolized in liver and excreted in
bile and urine.
...
NALOXONE
It reverses coma and respiratory depression of
opioid overdose.
It rapidly displaces all receptor bound opioid
...
NALTREXONE
 It has a longer duration of action than
naloxone and a single oral dose blocks the
effect of injected heroin ...
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ANTI INFLAMMTORY DRUGS

 INFLAMMATION:It is the body’s effort to inactivate or destroy
invading microorganisms ,remove ir...
CLASSIFICATION
DRUGS
NSAIDS GOUT ARTHRITIS ANALGESICS
(Non narcotic)

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NSAIDS
1) NONSELECTIVE COX INHIBITORS :a) Salicylates- Aspirin
b) Propionic acid derivatives- Ibuprofen
c) Anthranilic aci...
g) Indole- Indomethacin
h)Pyrazolone- Phenylbutazone

2) PREFERENTIAL COX-2 INHIBITORS :- Nimesulid
- Meloxicam
- Nabumeto...
3) SELECTIVE COX-2 INHIBITORS :- Celecoxib
- Etoricoxib
- Valdecoxib
4) ANALGESIC –ANTIPYRETIC WITH POOR
ANTIINFLAMMATORY:...
c) Benzoxacine derivative:- Nefopam

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SALICYLATES
ASPIRIN
 Weak organic acid
Irreversibly acetylates
Inactivates cyclooxygenase

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MECHANISM OF ACTION

• Blocks Prostaglandin synthesis(Peripheral targets)
• Prevents sensitization of pain receptors
• Dep...
PHARMACOLOGICAL EFFECTS

1. Antipyretic and analgesic effect:The two effects of aspirin are strong and rapid.
2. Anti infl...
3.

Inhibits platelet aggregation and prevent
thrombosis
– Inhibits TXA2 synthetase
– Aspirin administrated in low dose ca...
CLINICAL USES

1. Antipyretic and analgesic: Headache,toothache,myalgia,neuralgia , fever ,
dysmenorrhoea(decreases PGE2 ...
3. Cariovascular applications:•
•
•
•

Stable and variant angina pectoris
Progressive myocardial infarction patients
Trans...
ADVERSE REACTIONS
1.Gastrointestinal reactions:
Irritates gastric mucosa directly:
cause epigastric distress nausea and
v...
2. Blood Coagulation Disorders:-

• In usual dose:
Inhibits platelet coagulation and prolongs the
bleeding time.
• In high...
3. Allergy urticaria, allergic shock,
angioneurotic edema.

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SALICYLISM:•

≥5mg/d

•
•
•
•
•

headache, dizziness, nausea, vomiting, tin
nitus, sight and hearing failure
Severe
www.in...
Treatment:Mild;symptomatic , urinary pH
Serious; sodium bicarbonate i.v.drip
Reye’s syndrome:
Severe hepatic dysfunction ...
DRUG INTERACTIONS

•

Replaces dicoumarol (enhances its
anticoagulation effect)

•

Replaces tolbutamide and causes
hypogl...
PROPIONIC ACID DERIVATIVES
IBUPROFEN
1.ACTIONSAnalgesic
Antipyretic
Antiinflammatory
2.USES Chronic treatment of rheumato...
4. ADVERSE EFFECTS: Gastrointestinal
 Headache
 Tinnitus

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ANTHRANILIC ACID
DERIVATIVE
MEPHENAMIC ACID
1) MECHANISM OF ACTION:Inhibits COX as well as antagonises certain actions
of ...
ARYL ACETIC ACID
DERIVATIVE
DICLOFENAC SODIUM
1) MECHANISM OF ACTION:Inhibits prostaglandin synthesis and has short
lastin...
3)USES:Rheumatoid and osteoarthritis
Toothache
Bursitis
Dysmenorrhoea
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OXICAM DERIVATIVES
PIROXICAM
1)MECHANISM OF ACTION:



Reversible inhibitor of COX
Lowers PG concentration in synovial ...
3) ADVERSE EFFECTS:Heartburn
Nausea
Anorexia
Rashes
4) USES: Osteoarthritis
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 Ankylosing ...
PYRROLO PYRROLE
DERIVATIVE
KETOROLAC
1 MECHANISM OF ACTION:Inhibits prostaglandin synthesis
Relieves pain by peripheral ac...
3. ADVERSE EFFECTS:Nausea
Dyspepsia
Dizziness
Pruritus
4. USES:Postoperative dental , musculoskeletal pain
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INDOLE DERIVATIVE
INDOMETHACIN
1. MECHANISM OF ACTION:Potent inhibitor of prostaglandin synthesis
Supresses neutrophil mot...
3 ADVERSE EFFECTS:Gastric irritation
Anorexia,diarrhoea,gastric bleeding
Frontal headache, mental confusion,dizziness
4 US...
PYRAZOLONES
METAMIZOL
Derivative of amidopyrine
Potent and promptly acting analgesic
Antipyretic
Poor antiinflammatory
1.M...
3 ADVERSE EFFECTS:Gastric irritation
Agranulocytosis

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PREFERENTIAL COX 2
INHIBITORS
NIMESULIDE
1. MECHANISM OF ACTION Weak inhibitor of PG synthesis
 Inhibition of platelet a...
3. ADVERSE EFFECTS: Epigastralgia
 Pruritus
 Fulminant hepatic failure
4.USES: Sports injuries
 Dental surgery
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MELOXICAM
1. MECHANISM OF ACTION:It has a COX 2:COX 1 ratio of 10
It inhibits platelet TXA production
2.ADVERSE EFFECTS:Ga...
3. USES:• Osteoarthritis
• Rheumatoid arthritis

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SELECTIVE COX 2 INHIBITORS
They reduce prostaglandin 2 production by
vascular endothelium
CELECOXIB
Time dependent
Irrever...
2.ADVERSE EFFECTS:Abdominal pain
3. USES:Osteoarthritis
Rheumatoidarthritis
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VALDECOXIB
1.USE:Osteoarthritis
Rheumatoid arthritis
2. ADVERSE EFFECTS:In few cases severe skin reaction
Stevens-Johnson ...
PARA AMINO PHENOL
DERIVATIVE
PARACETAMOL
1. MECHANISM OF ACTION:It raises pain threshold but has weak peripheral
anti infl...
3. ADVERSE EFFECTS:Acute paracetamol poisoining
Low hepatic glucuronide conjugating ability
>10 gms in an adult; serious t...
Manifestations:Nausea,vomiting
After 2-18 hours,CENTRILOBULAR HEPATIC
NECROSIS and HYPOGLYCEMIA ,COMA
Mechanism:Paracetamo...







Very large dose is taken
Glucuronidation capacity is saturated
More of minor metabolite is formed
Hepatic glu...
TREATMENT: Patient brought early- GASTRIC LAVAGE
 Prevent further absorption- ACTIVATED
CHARCOAL
 Specific antidote-N-a...
DRUG INTERACTIONS

• NSAIDs + Hypotensive drugs ( β-blockers, ACEinhhibitors, diuretics ) = ↓ hypotensive effect
• NSAIDs ...
• NSAIDs + Oral antidiabetic drugs = ↑ risk of
hypoglycemia
• NSAIDs + Coumarines =↑ risk of bleeding
• NSAIDs + Corticost...
• NSAIDs + Lithium = ↑ lithium toxicity
• NSAIDs + Cylosporine or ACE-inhibitors or
Tacrolimus= ↑ nephrotoxicity of drugs
...
COMBINATIONS

DEXIBUPROFEN + PARACETAMOL

Inhibits COX
Inhibits COX-3
Paracetamol; central antinociceptive
action.

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 PARACETAMOL
+
DEXTROPROPOXYPHENE:greater
analgesic effect( centrally acting)

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TRAMADOL+PARACETAMOL:

o Faster onset of action compared to
Tramadol alone (17 minutes)
o Longer duration of action compa...
 DICLOFENAC + PARACETAMOL;

 Actions of Paracetamol set in
earlier and provides pain relief
before the effects of Diclof...
 ACECLOFENAC + PARACETAMOL
Inhibits synthesis
of IL-1b,PGE2 production
Positive cartilage anabolism
Modulating effect on ...
 IBUPROFEN + PARACETAMOL

Potent
Antiinflammatory,analgesic
antipyretic
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NIMESULIDE + RACEMETHIONINE

Scavenger

Precursor for
glutathione synthesis
Promotes production of
cartilage proteoglycan...
TOPICAL NSAIDS









Aceclofenac
Benzydamine
Diclofenac
Ketoprofen
Naproxen
Nimesulide
Piroxicam
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DISEASE MODIFYING ANTIRHEUMATIC AGENTS
A.




1.

GOLD SALTS:Are taken up by macrophages
Supresses phagocytosis
Lysoso...
3 .ADVERSE EFFECTS:Dermatitis of skin,mucous membranes
Proteinuria
Nephrosis
ANTIDOTE:- Dimercaprol
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•
•
•
•
•

CHLOROQUININE AND HYDROXY
CHLOROQUININE:It inhibits nucleic acid synthesis
Stabilizes lysosomal membranes
Traps...
PENICILLAMINE: It slows the progress of bone destruction and
rheumatoid arthritis.
 Prolonged treatment leads to aplasti...
DRUGS FOR GOUT
COLCHICINE:It is a plant alkaloid reserved for the treatment of
acute gouty attacks
2) USE:Alleviates the p...
ALLOPURINOL: Treats primary hyperuricemia of gout
 Hyperuricemia secondary to certain
malignancies.
1. ADVERSE EFFECTS:H...
URICOSURIC AGENTS• PROBENECID is a general inhibitor of the tubular
secretion of organic acids and SULFINPYRAZONE
is a der...
CORTICOSTEROIDS
MECHANISM OF ACTION:-(cellular level)
Corticosteroids
Bind to high affinity
Receptor protein(cytoplasmic)
...
• The most important overall mechanism appears
to be limitation of inflammatory cells at the local
site.

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IMPLICATIONS IN DENTISTRY

•
•
•
•

Recurrent oral ulceration
Severe oral lesions
TMJ pain and stiffness
In case of patien...
• For traumatic procedures and those to be performed
under general anaesthesia ,supplemental steroids
may be needed,partic...
PREEMPTIVE DIASICS

 Recommended to orthodontic
patients before separator placement
IBUPROFEN(reduces pain
at 6 hours and...
ORTHODONTICS
• Direct injection of prostaglandin into periodontal
ligament increases the rate of tooth movement.
• 2 types...
BISPHOSPHONATES:-

• Synthetic analogues of pyrophosphate
+
Hydroxyapatite in bone,acts as specific inhibitors of
osteocla...
PROSTAGLANDIN INHIBITORS:A) Corticosteroids and NSAIDS
B) Other agents
CORTICOSTEROIDS:Reduces PG synthesis
Both children ...
NSAIDS
• Potent prostaglandin inhibitors like Indomethacin
can inhibit tooth movement.
OTHER AGENTS
• Tricyclic antidepres...
• Phenytoin has been reported to decrease tooth
movement
• Some tetracycline(doxycycline) inhibits osteoclast
recruitment....
1. Acetaminophen has no effect on the rate
of tooth movement in rabbits
undergoing orthodontic tooth
movement.
2. Acetamin...
3. Some test subjects may have exhibited
deleterious effects on somatic growth
due either to acetaminophen toxicity or
to ...
REFERENCES
 Essentials of Pharmacology for Dentistry
K.D. Tripathi ;2005
Lippincott’s illustrared reviews
Clinical Phar...
• MANY OTHER WORKS IN
PROGRESS…

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•QUESTIONS?????

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THANK YOU
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Leader in continuing dental education

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Analgesics and antiinflammatory drugs /certified fixed orthodontic courses by Indian dental academy

  1. 1. ANALGESICS AND ANTIINFLAMMATORY DRUGS INDIAN DENTAL ACADEMY Leader in continuing dental education www.indiandentalacademy.com
  2. 2. PAIN (Algesia) “Pain is an unpleasant sensory and emotional experience associated with actual or potential tissue damage or described in terms of such damage” International Association for the Study of Pain www.indiandentalacademy.com
  3. 3. WHY FEEL PAIN? • Gives conscious awareness of tissue damage • Protection: – Removes body from danger – Promotes healing by preventing further damage • Elicits behavioural and emotional www.indiandentalacademy.com responses
  4. 4. LOCALIZATION OF PAIN • Superficial Somatic Pain arises from skin areas • Deep Somatic Pain arises from muscle, joints, tendons & fascia • Visceral Pain arises from receptors in visceral organs www.indiandentalacademy.com
  5. 5. FAST AND SLOW PAIN • Most pain sensation is a combination of the two types of message. – If we prick our finger we first feel a sharp pain which is conducted by the A fibres, – and this is followed by a dull pain conveyed along C fibres. www.indiandentalacademy.com
  6. 6. • FAST PAIN (acute) – Occurs rapidly after stimuli (0.1 second) – Sharp pain like needle puncture or cut – Not felt in deeper tissues – Larger myelinated A nerve fibers – Velocity of 80 m/s www.indiandentalacademy.com
  7. 7. • SLOW PAIN (chronic) – Begins more slowly & increases in intensity – In both superficial and deeper tissues – Smaller unmyelinated C nerve fibers – Velocity of 0.4 m/s www.indiandentalacademy.com
  8. 8. PAIN PATHWAY www.indiandentalacademy.com
  9. 9. ANALGESIC • It is a drug that selectively relieves pain by acting in the CNS or on peripheral pain mechanisms,without significantly altering consciousness www.indiandentalacademy.com
  10. 10. ANALGESICS Analgesics can be:- a) Opioid/Narcotic b) Non opioid/Non narcotic www.indiandentalacademy.com
  11. 11. OPIOID ANALGESICS Derived from opium  It has 2 types of alkaloids:- Phenanthrene Benzoisoquinoline www.indiandentalacademy.com
  12. 12. CLASSIFICATION 1 .Natural Opium AlkaloidsMorphine,Codeine 2. Semisynthetic OpiatesDiacetylmorphine,Pholcodeine 3. Synthetic OpioidsPethidine,Fentanyl www.indiandentalacademy.com
  13. 13. OPIOID ANALGESICS AND ANTAGONISTS OPIOID DRUGS Agonists Mixed actions Antagonists Morphine Naloxone Heroin Methadone Codeine Naltrexone Pentazocine Nalbuphine Butorphan www.indiandentalacademy.com
  14. 14. MECHANISM OF ACTION www.indiandentalacademy.com
  15. 15. RECEPTORS www.indiandentalacademy.com
  16. 16. OPIOID RECEPTORS • Mu opioid receptor- Respiratory depression Euphoria Physical dependence Pupil constriction www.indiandentalacademy.com
  17. 17. • Kappa opiod receptor- Sedation Spinal anaesthesia Pupil constriction www.indiandentalacademy.com
  18. 18. • Sigma opioid receptor- Hallucinations Dysphoria Pupil dilation www.indiandentalacademy.com
  19. 19. www.indiandentalacademy.com
  20. 20. POPPY PLANT www.indiandentalacademy.com
  21. 21. MORPHINE • Serturner,1806 morphine –Morpheus. • Source- crude opium • Prototype agonist www.indiandentalacademy.com
  22. 22. MECHANISM OF ACTIONa) Morphine + receptors Hyperpolarization of nerve cells Inhibition of nerve firing Presynaptic inhibition(transmitter) www.indiandentalacademy.com
  23. 23. b) Morphine + k receptors Reduces release of substance P c) Morphine inhibits release of excitatory transmitters from nerve terminals carrying nociceptive stimuli www.indiandentalacademy.com
  24. 24. MECHANISM OF ACTION www.indiandentalacademy.com
  25. 25. NOCICEPTORS • Nociceptors are special receptors that respond only to noxious stimuli and generate nerve impulses which the brain interprets as "pain". www.indiandentalacademy.com
  26. 26. ACTION www.indiandentalacademy.com
  27. 27. ACTIONS a) Analgesia: Selective  Raises pain threshold at spinal cord level  Alters brain perception of pain www.indiandentalacademy.com
  28. 28. b) Euphoria:- stimulates ventral tegmentum c) Respiration:d) Depression of cough reflex:e) Miosis:- www.indiandentalacademy.com
  29. 29. f) Emesis:g) Cardiovascular:h) G.I. tract:i) Histamine Release:j) Hormonal actions:www.indiandentalacademy.com
  30. 30. USES a. Analgesia b. Treatment of diarrhoea c. Relief of cough www.indiandentalacademy.com
  31. 31. ADVERSE EFFECTS  Respiratory depression  Nausea and vomiting,constipation  Addiction potential www.indiandentalacademy.com
  32. 32. MEPERIDINE • It is a synthetic opioid used for acute pain. 1.MECHANISM OF ACTION:Meperidine+k receptors 2. ACTIONS: Depression of respiration  Dilates cerebral vessels www.indiandentalacademy.com
  33. 33. Contracts smooth muscle i.v.; in peripheral resistance It decreases gastric motility Dilates the pupils 3. THERAPEUTIC USES: Analgesia www.indiandentalacademy.com Pre anaesthetic medication
  34. 34. 5. ADVERSE EFFECTS:Large doses lead to tremors,muscle twitches 6.DRUG INTERACTIONS:It increases depression along with major neuroleptics 7.TOLERANCE:It causes dependence and cross tolerance. www.indiandentalacademy.com
  35. 35. METHADONE  High oral parenteral activity ratio (1:2) and firm binding to tissue proteins. 1. MECHANISM OF ACTION:Methadone+mu receptors 2. ACTIONS:-Analgesia -Respiratory depression www.indiandentalacademy.com
  36. 36. 3.THERAPEUTIC USES:a) SUBSTITUTION THERAPY OF OPIOID DEPENDENCE; 1 mg of oral methadone for 4 mg of opioid ,2 mg of heroin,20 mg of pethidine. b) MAINTENANCEwww.indiandentalacademy.com THERAPY :-
  37. 37. 5.ADVERSE EFFECTS:Dependence Mild withdrawal syndrome www.indiandentalacademy.com
  38. 38. FENTANYL It is 80-100 times more potent than morphine. 1.ACTIONS:Analgesia Respiratory depression 2.THERAPEUTIC USES:Anaesthesia injection form exclusively Transdermal fentanyl has become available for use www.indiandentalacademy.com in cancer or chronic pain
  39. 39. Along with Droperidol,it causes NEUROLEPT ANAESTHESIA www.indiandentalacademy.com
  40. 40. PROPOXYPHENE It is a derivative of methadone 2.USES:d isomer leads to analgesia l isomer leads to antitussive action www.indiandentalacademy.com
  41. 41. 3.SIDE EFFECTS: Nausea,vomiting  Toxic doses ; respiratory depression  Used with alcohol,sedatives ;severe CNS depression and death www.indiandentalacademy.com
  42. 42. CODEINE It is a less potent analgesic than morphine having higher oral efficacy ACTIONS:Analgesia Sedation Euphoria Depresses the cough reflex. www.indiandentalacademy.com
  43. 43. PENTAZOCINE 1.MECHANISM OF ACTION:It is an agonist on k receptors and weak antagonist on mu and delta receptors. 2.USES:Analgesia Angina www.indiandentalacademy.com
  44. 44. 3.ACTIONS: Analgesia by activating receptors in the spinal cord 4.ADVERSE EFFECTS:Higher dose;respiratory depression Tolerance and dependence www.indiandentalacademy.com
  45. 45. BUPRENORPHINE  It is a partial agonist acting at the mu receptors metabolized in liver and excreted in bile and urine.  It causes nausea,dizziness,respiratory depression. www.indiandentalacademy.com
  46. 46. NALOXONE It reverses coma and respiratory depression of opioid overdose. It rapidly displaces all receptor bound opioid molecules MECHANISM OF ACTION: It is a competitive antagonist at mu,k,delta receptors with a ten fold affinity for mu . www.indiandentalacademy.com
  47. 47. NALTREXONE  It has a longer duration of action than naloxone and a single oral dose blocks the effect of injected heroin for upto 48 hours. USES: Opiate dependence maintenance programs  Chronic alcoholism www.indiandentalacademy.com
  48. 48. www.indiandentalacademy.com
  49. 49. www.indiandentalacademy.com
  50. 50. ANTI INFLAMMTORY DRUGS  INFLAMMATION:It is the body’s effort to inactivate or destroy invading microorganisms ,remove irritants and set the stage for tissue repair. www.indiandentalacademy.com
  51. 51. CLASSIFICATION DRUGS NSAIDS GOUT ARTHRITIS ANALGESICS (Non narcotic) www.indiandentalacademy.com
  52. 52. NSAIDS 1) NONSELECTIVE COX INHIBITORS :a) Salicylates- Aspirin b) Propionic acid derivatives- Ibuprofen c) Anthranilic acid- Mephenamic acid d) Aryl acetic acid - Diclofenac e) Oxicam- Piroxicam f) Pyrrolo pyrrole- Ketorolac www.indiandentalacademy.com
  53. 53. g) Indole- Indomethacin h)Pyrazolone- Phenylbutazone 2) PREFERENTIAL COX-2 INHIBITORS :- Nimesulid - Meloxicam - Nabumetone www.indiandentalacademy.com
  54. 54. 3) SELECTIVE COX-2 INHIBITORS :- Celecoxib - Etoricoxib - Valdecoxib 4) ANALGESIC –ANTIPYRETIC WITH POOR ANTIINFLAMMATORY:a) Para aminophenol derivative-Paracetamol b) Pyrazolone derivative- Metamizol www.indiandentalacademy.com
  55. 55. c) Benzoxacine derivative:- Nefopam www.indiandentalacademy.com
  56. 56. SALICYLATES ASPIRIN  Weak organic acid Irreversibly acetylates Inactivates cyclooxygenase www.indiandentalacademy.com
  57. 57. MECHANISM OF ACTION • Blocks Prostaglandin synthesis(Peripheral targets) • Prevents sensitization of pain receptors • Depresses pain stimuli at subcortical sites (Thalamus,Hypothalamus) www.indiandentalacademy.com
  58. 58. PHARMACOLOGICAL EFFECTS 1. Antipyretic and analgesic effect:The two effects of aspirin are strong and rapid. 2. Anti inflammatory and anti rheumatic effect:(1) Relatively stronger (2) Often used to the dose of tolerance www.indiandentalacademy.com
  59. 59. 3. Inhibits platelet aggregation and prevent thrombosis – Inhibits TXA2 synthetase – Aspirin administrated in low dose can reduce TXA2 remarkably – Anticoagulant effect www.indiandentalacademy.com
  60. 60. CLINICAL USES 1. Antipyretic and analgesic: Headache,toothache,myalgia,neuralgia , fever , dysmenorrhoea(decreases PGE2 synthesis) 2. Anti-inflammation and antirheumatism: Diagnosis and therapy of acute rheumatic fever www.indiandentalacademy.com
  61. 61. 3. Cariovascular applications:• • • • Stable and variant angina pectoris Progressive myocardial infarction patients Transient ischemic attack patients Angioplasty, bypass transplant operations www.indiandentalacademy.com
  62. 62. ADVERSE REACTIONS 1.Gastrointestinal reactions: Irritates gastric mucosa directly: cause epigastric distress nausea and vomiting  Irritates chemoreceptor trigger zone(CTZ): cause nausea ,vomiting  Gastric ulcer: can cause and www.indiandentalacademy.com deteriorate ulcer
  63. 63. 2. Blood Coagulation Disorders:- • In usual dose: Inhibits platelet coagulation and prolongs the bleeding time. • In high dose or in long term: Inhibits the formation of prothombin and prolongs the prothombin time www.indiandentalacademy.com
  64. 64. 3. Allergy urticaria, allergic shock, angioneurotic edema. www.indiandentalacademy.com
  65. 65. SALICYLISM:• ≥5mg/d • • • • • headache, dizziness, nausea, vomiting, tin nitus, sight and hearing failure Severe www.indiandentalacademy.com hyperventilation, acid-base in
  66. 66. Treatment:Mild;symptomatic , urinary pH Serious; sodium bicarbonate i.v.drip Reye’s syndrome: Severe hepatic dysfunction with complication of encephalopathy www.indiandentalacademy.com
  67. 67. DRUG INTERACTIONS • Replaces dicoumarol (enhances its anticoagulation effect) • Replaces tolbutamide and causes hypoglycemia www.indiandentalacademy.com
  68. 68. PROPIONIC ACID DERIVATIVES IBUPROFEN 1.ACTIONSAnalgesic Antipyretic Antiinflammatory 2.USES Chronic treatment of rheumatoid arthritis www.indiandentalacademy.com  Soft tissue injuries,tooth extractions,fractures
  69. 69. 4. ADVERSE EFFECTS: Gastrointestinal  Headache  Tinnitus www.indiandentalacademy.com
  70. 70. ANTHRANILIC ACID DERIVATIVE MEPHENAMIC ACID 1) MECHANISM OF ACTION:Inhibits COX as well as antagonises certain actions of prostaglandins 3)USES:Analgesic in muscle,joint and soft tissue pain Dysmenorrhoea www.indiandentalacademy.com
  71. 71. ARYL ACETIC ACID DERIVATIVE DICLOFENAC SODIUM 1) MECHANISM OF ACTION:Inhibits prostaglandin synthesis and has short lasting antiplatelet action. Neutrophil chemotaxis,superoxide production at the inflammatory site is reduced. www.indiandentalacademy.com
  72. 72. 3)USES:Rheumatoid and osteoarthritis Toothache Bursitis Dysmenorrhoea www.indiandentalacademy.com
  73. 73. OXICAM DERIVATIVES PIROXICAM 1)MECHANISM OF ACTION:   Reversible inhibitor of COX Lowers PG concentration in synovial fluid Inhibits platelet aggregation. www.indiandentalacademy.com
  74. 74. 3) ADVERSE EFFECTS:Heartburn Nausea Anorexia Rashes 4) USES: Osteoarthritis www.indiandentalacademy.com  Ankylosing spondylitis
  75. 75. PYRROLO PYRROLE DERIVATIVE KETOROLAC 1 MECHANISM OF ACTION:Inhibits prostaglandin synthesis Relieves pain by peripheral action www.indiandentalacademy.com
  76. 76. 3. ADVERSE EFFECTS:Nausea Dyspepsia Dizziness Pruritus 4. USES:Postoperative dental , musculoskeletal pain www.indiandentalacademy.com Migraine
  77. 77. INDOLE DERIVATIVE INDOMETHACIN 1. MECHANISM OF ACTION:Potent inhibitor of prostaglandin synthesis Supresses neutrophil motility. www.indiandentalacademy.com
  78. 78. 3 ADVERSE EFFECTS:Gastric irritation Anorexia,diarrhoea,gastric bleeding Frontal headache, mental confusion,dizziness 4 USES:Antiinflammatory agent;ankylosing spondylitis Hodgkin’s disease(antipyretic) Patent ductus arteriosus www.indiandentalacademy.com
  79. 79. PYRAZOLONES METAMIZOL Derivative of amidopyrine Potent and promptly acting analgesic Antipyretic Poor antiinflammatory 1.MECHANISM OF ACTION:Potent analgesic www.indiandentalacademy.com Antipyretic
  80. 80. 3 ADVERSE EFFECTS:Gastric irritation Agranulocytosis www.indiandentalacademy.com
  81. 81. PREFERENTIAL COX 2 INHIBITORS NIMESULIDE 1. MECHANISM OF ACTION Weak inhibitor of PG synthesis  Inhibition of platelet activating factor synthesis and tumor necrosis factor release  Inhibition of metalloproteinase activity www.indiandentalacademy.com
  82. 82. 3. ADVERSE EFFECTS: Epigastralgia  Pruritus  Fulminant hepatic failure 4.USES: Sports injuries  Dental surgery www.indiandentalacademy.com  Dysmenorrhoea
  83. 83. MELOXICAM 1. MECHANISM OF ACTION:It has a COX 2:COX 1 ratio of 10 It inhibits platelet TXA production 2.ADVERSE EFFECTS:Gastric changes Long term bleeding and perforation www.indiandentalacademy.com
  84. 84. 3. USES:• Osteoarthritis • Rheumatoid arthritis www.indiandentalacademy.com
  85. 85. SELECTIVE COX 2 INHIBITORS They reduce prostaglandin 2 production by vascular endothelium CELECOXIB Time dependent Irreversible inhibition of COX-2 www.indiandentalacademy.com
  86. 86. 2.ADVERSE EFFECTS:Abdominal pain 3. USES:Osteoarthritis Rheumatoidarthritis www.indiandentalacademy.com
  87. 87. VALDECOXIB 1.USE:Osteoarthritis Rheumatoid arthritis 2. ADVERSE EFFECTS:In few cases severe skin reaction Stevens-Johnson syndrome www.indiandentalacademy.com
  88. 88. PARA AMINO PHENOL DERIVATIVE PARACETAMOL 1. MECHANISM OF ACTION:It raises pain threshold but has weak peripheral anti inflammatory component Inhibits Prstaglandin synthesis in CNS www.indiandentalacademy.com
  89. 89. 3. ADVERSE EFFECTS:Acute paracetamol poisoining Low hepatic glucuronide conjugating ability >10 gms in an adult; serious toxicity >250 mg/kg; fatal www.indiandentalacademy.com
  90. 90. Manifestations:Nausea,vomiting After 2-18 hours,CENTRILOBULAR HEPATIC NECROSIS and HYPOGLYCEMIA ,COMA Mechanism:Paracetamol gives rise to metabolite, N-acetyl p benzoquinoneimine www.indiandentalacademy.com
  91. 91.       Very large dose is taken Glucuronidation capacity is saturated More of minor metabolite is formed Hepatic glutathione is depleted Metabolite binds covalently to proteins Necrosis www.indiandentalacademy.com
  92. 92. TREATMENT: Patient brought early- GASTRIC LAVAGE  Prevent further absorption- ACTIVATED CHARCOAL  Specific antidote-N-acetylcysteine i.v./oral 4 .USES: Best antipyretic www.indiandentalacademy.com  Headache,toothache,musculoskeletal pain
  93. 93. DRUG INTERACTIONS • NSAIDs + Hypotensive drugs ( β-blockers, ACEinhhibitors, diuretics ) = ↓ hypotensive effect • NSAIDs + Ethanol = ↑ risk of bleeding from gastrointestinal tract • NSAIDs + Ticlopidine or Clopidogrel = ↑ risk of bleeding www.indiandentalacademy.com
  94. 94. • NSAIDs + Oral antidiabetic drugs = ↑ risk of hypoglycemia • NSAIDs + Coumarines =↑ risk of bleeding • NSAIDs + Corticosteroids = ↑ risk of gastropathy and bleeding from gastrointestinal tract www.indiandentalacademy.com
  95. 95. • NSAIDs + Lithium = ↑ lithium toxicity • NSAIDs + Cylosporine or ACE-inhibitors or Tacrolimus= ↑ nephrotoxicity of drugs • NSAIDs + Fluoroquinolons = ↑ toxic action of fluoroquinolones on CNS • NSAIDs + Oral antidiabetic drugs = ↑ risk of hypoglycemia www.indiandentalacademy.com
  96. 96. COMBINATIONS DEXIBUPROFEN + PARACETAMOL Inhibits COX Inhibits COX-3 Paracetamol; central antinociceptive action. www.indiandentalacademy.com
  97. 97.  PARACETAMOL + DEXTROPROPOXYPHENE:greater analgesic effect( centrally acting) www.indiandentalacademy.com
  98. 98. TRAMADOL+PARACETAMOL: o Faster onset of action compared to Tramadol alone (17 minutes) o Longer duration of action compared to Paracetamol alone (5 hours) www.indiandentalacademy.com
  99. 99.  DICLOFENAC + PARACETAMOL;  Actions of Paracetamol set in earlier and provides pain relief before the effects of Diclofenac sets in. www.indiandentalacademy.com
  100. 100.  ACECLOFENAC + PARACETAMOL Inhibits synthesis of IL-1b,PGE2 production Positive cartilage anabolism Modulating effect on matrix catabolism( GAG ) www.indiandentalacademy.com
  101. 101.  IBUPROFEN + PARACETAMOL Potent Antiinflammatory,analgesic antipyretic www.indiandentalacademy.com
  102. 102. NIMESULIDE + RACEMETHIONINE Scavenger Precursor for glutathione synthesis Promotes production of cartilage proteoglycans www.indiandentalacademy.com antioxidant
  103. 103. TOPICAL NSAIDS        Aceclofenac Benzydamine Diclofenac Ketoprofen Naproxen Nimesulide Piroxicam www.indiandentalacademy.com
  104. 104. DISEASE MODIFYING ANTIRHEUMATIC AGENTS A.     1. GOLD SALTS:Are taken up by macrophages Supresses phagocytosis Lysosomal enzyme activity Retards bone, articular destruction THERAPEUTIC USES:Rheumatoid arthritis that does not respond www.indiandentalacademy.com to SALICYLATES or other NSAIDS.
  105. 105. 3 .ADVERSE EFFECTS:Dermatitis of skin,mucous membranes Proteinuria Nephrosis ANTIDOTE:- Dimercaprol www.indiandentalacademy.com
  106. 106. • • • • • CHLOROQUININE AND HYDROXY CHLOROQUININE:It inhibits nucleic acid synthesis Stabilizes lysosomal membranes Traps free radicals Reserved for RHEUMATOID ARTHRITIS that has been unresponsive to NSAIDS Adverse effects include headache, rashes www.indiandentalacademy.com
  107. 107. PENICILLAMINE: It slows the progress of bone destruction and rheumatoid arthritis.  Prolonged treatment leads to aplastic anemia,nephritis METHOTREXATE: It is used for patients with severe rheumatoid arthritis www.indiandentalacademy.com
  108. 108. DRUGS FOR GOUT COLCHICINE:It is a plant alkaloid reserved for the treatment of acute gouty attacks 2) USE:Alleviates the pain of acute gout within 12 hours. www.indiandentalacademy.com
  109. 109. ALLOPURINOL: Treats primary hyperuricemia of gout  Hyperuricemia secondary to certain malignancies. 1. ADVERSE EFFECTS:Hypersensitivity reactions Nausea,diarrhoea www.indiandentalacademy.com
  110. 110. URICOSURIC AGENTS• PROBENECID is a general inhibitor of the tubular secretion of organic acids and SULFINPYRAZONE is a derivative of phenylbutazone. • At therapeutic doses, they block proximal tubular absoption of uric acid. www.indiandentalacademy.com
  111. 111. CORTICOSTEROIDS MECHANISM OF ACTION:-(cellular level) Corticosteroids Bind to high affinity Receptor protein(cytoplasmic) Migrate into the nucleus Transcription of m-Rna Regulation of protein synthesis www.indiandentalacademy.com
  112. 112. • The most important overall mechanism appears to be limitation of inflammatory cells at the local site. www.indiandentalacademy.com
  113. 113. IMPLICATIONS IN DENTISTRY • • • • Recurrent oral ulceration Severe oral lesions TMJ pain and stiffness In case of patients who have been in recent past on long term corticosteroid therapy,consideration has to be given to the need for supplementary prophylactic corticoid to cover a dental procedure. www.indiandentalacademy.com
  114. 114. • For traumatic procedures and those to be performed under general anaesthesia ,supplemental steroids may be needed,particularly if the dose and duration of steroid therapy are such as to have caused significant adrenal supression . www.indiandentalacademy.com
  115. 115. PREEMPTIVE DIASICS  Recommended to orthodontic patients before separator placement IBUPROFEN(reduces pain at 6 hours and at bedtime on the night of separator placement) NAPROXEN SODIUM www.indiandentalacademy.com
  116. 116. ORTHODONTICS • Direct injection of prostaglandin into periodontal ligament increases the rate of tooth movement. • 2 types of drugs are known to depress the response to orthodontic force and may influence current treatment:  BISPHOSPHONATES  PROSTAGLANDIN INHIBITORS www.indiandentalacademy.com
  117. 117. BISPHOSPHONATES:- • Synthetic analogues of pyrophosphate + Hydroxyapatite in bone,acts as specific inhibitors of osteoclast mediated bone resorption. www.indiandentalacademy.com
  118. 118. PROSTAGLANDIN INHIBITORS:A) Corticosteroids and NSAIDS B) Other agents CORTICOSTEROIDS:Reduces PG synthesis Both children and adults on chronic steroid therapy- difficulty www.indiandentalacademy.com in tooth movement.
  119. 119. NSAIDS • Potent prostaglandin inhibitors like Indomethacin can inhibit tooth movement. OTHER AGENTS • Tricyclic antidepressants • Antimalarial drugs –can affect the response to orthodontic force www.indiandentalacademy.com
  120. 120. • Phenytoin has been reported to decrease tooth movement • Some tetracycline(doxycycline) inhibits osteoclast recruitment. www.indiandentalacademy.com
  121. 121. 1. Acetaminophen has no effect on the rate of tooth movement in rabbits undergoing orthodontic tooth movement. 2. Acetaminophen, a proven analgesic that lacks the anti-inflammatory properties of NSAIDS, appears to be the drug of choice for the relief of orthodontic pain. www.indiandentalacademy.com
  122. 122. 3. Some test subjects may have exhibited deleterious effects on somatic growth due either to acetaminophen toxicity or to orthodontically induced pain. 4. Misoprostol had an insignificant inhibitory effect on local PGE2 production; however, the degree and rate of tooth movement was enhanced www.indiandentalacademy.com
  123. 123. REFERENCES  Essentials of Pharmacology for Dentistry K.D. Tripathi ;2005 Lippincott’s illustrared reviews Clinical Pharmacology,8th edition Clinical Pharmacology,9th edition Basic and clinical Pharmaology,8th edition,Katzung Neller’s illustrated Pharmacology www.google.co.in www.indiandentalacademy.com  Articles;Angle orthodontics,AJO-DO
  124. 124. • MANY OTHER WORKS IN PROGRESS… www.indiandentalacademy.com
  125. 125. •QUESTIONS????? www.indiandentalacademy.com
  126. 126. THANK YOU www.indiandentalacademy.com Leader in continuing dental education www.indiandentalacademy.com

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