The document provides a comprehensive overview of analgesics and antibiotics used in dentistry, focusing on various classifications and types of analgesics, including NSAIDs and their mechanisms of action. It highlights the pharmacokinetics, adverse effects, and typical uses of these medications, including both topical and systemic applications. Additionally, it addresses the management of chronic pain and treatment considerations for analgesics during pregnancy.

1. ©M. S. Ramaiah University of Applied Sciences
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Course Code: BDSDEN106
Course Title: Oral Medicine and Radiology
Antibiotics and Analgesics – Part II
Dr. N Rakesh
rakesh.or.ds@msruas.ac.in

2. Lecture No. 23
Antibiotics and Analgesics – Part II
At the end of this lecture, student will be able to
• Classify analgesics
• Describe the commonly used analgesics in dentistry
• Enlist the different modes of local drug delivery systems

3. ©M. S. Ramaiah University of Applied Sciences
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Content
• Commonly used analgesics
• Non-steroidal anti-inflammatory drugs (NSAIDs)
– Nonselective cox inhibitors
– Preferential cox-2 inhibitors
– Selective cox-2 inhibitors
– Analgesic-antipyretics with poor anti-inflammatory action
• Topical preparations
• Neuropeptides
• Local drug delivery systems
• Adjuvent drugs
• Drugs used in management of Chronic pain
• Summary

4. Non-steroidal
anti-inflammatory
drugs (NSAIDS)
Commonly used analgesics

5. - Analgesic, Antipyretic & Anti-inflammatory actions.
- Act primarily on Peripheral Pain Receptors
& CNS to raise the pain threshold.
- Compared to Morphine
- Weaker analgesics
- Do not depress CNS
-Do not produce physical dependence
& have no abuse liability.
Introduction

6. Classification
A) NONSELECTIVE COX INHIBITORS
(CONVENTIONAL NSAIDS)
1. Salicylates: Aspirin, Diflunisal.
2. Pyrazolone derivatives: Phenylbutazone,
Oxyphenbutazone
3. Indole derivatives: Indomethacin, Sulindac.
4. Propionic acid derivatives: Ibuprofen, Naproxen, Ketoprofen.

7. 5.Anthranilic acid derivative: Mephenamic acid.
6.Aryl-acetic acid derivatives: Diclofenac, Tolmetin.
7.Oxicam derivatives: Piroxicam, Tenoxicam.
8. Pyrrolo-pyrrole derivative: Ketorolac.
B) PREFERENTIAL COX-2 INHIBITORS –
Nimesulide, Meloxicam, Nabumetone
C) SELECTIVE COX-2 INHIBITORS -
Celecoxib, Rofecoxib, Valdecoxib

8. D)ANALGESIC-ANTIPYRETICS WITH
POOR ANTI-INFLAMMATORY ACTION -
1. Paraaminophenol derivative: Paracetamol
(Acetaminophen).
2. Pyrazolone derivatives: Metamizol, Propiphenazone.
3. Benzoxazocine derivatives: Nefopam

9. - Act as Non-selective
Inhibitors of the enzyme
cyclooxygenase, inhibiting
both, COX-1 & COX-2
isoenzymes.
- Cyclooxygenase catalyses
the formation of PGs &
TBX 2 from arachidonic
acid (itself derived from the
cellular phospholipid bilayer
by phospholipase A2)
Mechanism of action

10. COX-1
- Present as part of everyday physiological function.
- Protects the stomach by limiting acid secretion.
- Helps platelets limit bleeding by increasing their
adhesiveness.
COX-2
- Its expression is induced by various stimuli such as
the inflammation or at the site of the injury.

11. Aspirin
• Analgesic, Antipyretic & Anti-inflammatory Effects.
• Respiratory system
-Increases rate & depth.
• GIT
- Irritates the gastric mucosa  causes epigastric distress,
nausea & vomiting.
- Promotes the local back diffusion of the acid  acute
ulcers, erosive gastritis, microscopic haemorrhages.
Salicylates

12. • CVS
- No direct effect.
- Larger doses increase cardiac output to meet increased
peripheral O2 demand caused by direct vasodilation.
• Blood
- Inhibits TXA2 synthesis by platelets
- Interferes with Platelet aggregation (BT)
• Metabolic effects
-Increased utilization of Glucose, blood sugar may
decrease specially in diabetics.

13. Pharmacokinetics
- Poor Absorption- Stomach & Small Intestine.
- Metabolism- Gut wall, Liver, Plasma & other tissues
to release salicylic acid. Excretion- Urine.
Adverse effects
- Nausea,Vomiting, Epigastric distress & occult
blood in stools, rashes, urticaria, asthma, angioedema
- Anti-inflammatory doses – syndrome Salicylism –
dizziness, tinitus, reversible impairment
of hearing & vision, excitement.

14. Uses
- As analgesic – headache, backache, myalgia, joint pain,
toothache, neuralgias.
- As antipyretic
- Acute rheumatic fever, Rheumatoid arthritis, Osteoarthrtis
- Postmyocardial infarction & post-stroke patients.
DOSE: 300-900 mg every 4 hrs (Max 3.6 gm)
( ASA, ASCAD, ECOSPRIN 50mg,75mg Tab.)

15. Phenylbutazone
- Potent anti-inflammatory drug.
- Poor analgesic & antipyretic activity.
Adverse effects:
- More toxic than Aspirin
- Bone marrow depression, Agranulocytosis
- Banned in some countries.
Dose: 100-200 mg BD or TDS after meals
(ZOLANDIN 100,200 mg Tab.)
Pyrazolone derivatives

16. Indomethacin
- Potent anti-inflammatory, antipyretic & good
analgesic.
- Analgesic action better than PBZ.
Adverse effects:
- High incidence of GI & CNS side effects.
- C/I in drivers, epileptics, pregnancy & children.
Uses:
- Rheumatoid Arthritis not controlled by aspirin.
- Acts rapidly in Acute Gout.
Dose: 25-50 mg BD /TDS (INDOCAP, IDICIN)
Indole derivatives

17. Ibuprofen
- Analgesic, Antipyretic & Anti-inflammatory activity
is lower than aspirin.
- Inhibit platelet aggregation & prolong bleeding time.
Adverse effects:
- Better tolerated than aspirin (Incidence is lower).
- Gastric discomfort, nausea & vomiting are most
 common side effects.
Propionic acid derivatives

18. Pharmacokinetics:
 - Absorbed orally, highly bound to plasma proteins
 (90-99%)
 - Metabolized in liver & excreted in urine & bile.
- Enter brain, synovial fluid & cross placenta.
Interactions:
- As they inhibit platelet function, use with
 anticoagulants should be avoided.
 - Likely to decrease diuretic & antihypertensive action
 of thiazides, furosemide and -blockers.

19. - As Analgesic & Antipyretic.
- In Rheumatoid Arthritis, Osteoarthritis & other
Musculoskeletal Disorders, specially where pain is more
prominent than inflammation.
- Indicated in soft tissue injuries, fractures, tooth extraction,
supppress swelling & inflammation.
DOSE: 400-800 mg TDS
(BRUFEN, EMFLAM, IBUGESIC
200, 400, 600 mg Tab.)
Uses

20. Mephenamic acid
- An Analgesic, Antipyretic & Anti-inflammatory drug,
which inhibits COX as well as antagonises certain
actions of PGs.
- Exerts Peripheral as well as Central Analgesic Action.
ADVERSE EFFECTS :
- Diarrhoea is the important dose related side effect.
- Epigastric distress is complained, but gut bleeding is
 not significant.
Anthranilic acid derivative

21. Pharmacokinetics:
- Oral absorption is slow but almost complete.
- Partly metabolized & excreted in urine & as bile.
Uses:
 - Analgesic in muscle, joint & soft tissue pain where
 strong anti-inflammatory action is not needed (MPDS).
- Useful in rheumatoid & osteoarthritis.
Dose: 250-500 mg TDS
(MEFTAL, PONSTAN, MEDOL
250, 500 mg cap.)

22. Diclofenac sodium
- Analgesic, Antipyretic, Anti-inflammatory action.
- Inhibits PG synthesis & has short lasting antiplatelet
action.
Pharmacokinetics:
- Well absorbed orally, metabolized & excreted both
 in urine & bile.
- Has good tissue penetrability & conc. in synovial
 fluid is maintained longer period, exerting extended
 therapeutic action in joints.
Aryl-aceticacid derivative

23. Adverse effects
- Are generally mild: Epigastric pain, nausea,
headache, dizziness, rashes.
- Gastric ulceration & bleeding -less common.
Uses:
- Most extensively used NSAID.
- Rheumatoid & Osteoarthris, post-traumatic
inflammatory conditions - affords quick relief of
pain & wound edema (Dental Extractions).
Dose: 50 mg TDS, 75 mg i.m
(VOVERAN, DICLONAC, DICLOMAX
25, 50 mg Tab., 75 mg /3ml inj.)

24. Piroxicam
 - Long acting potent NSAID with good anti-
 inflammatory, analgesic & antiplatelet action.
 - Reversible inhibitor of COX; lowers PG conc. in
 synovial fluid & inhibits platelet aggregation-
 prolonging bleeding time.
 - In addition, it decreases the production of IgM
 rheumatoid factor.
Oxicam derivatives

25. Pharmacokinetics:
- Rapidly & completed absorbed.
- Metabolized in liver & excreted in urine.
- Plasma t1/2 is 2 days. So, single daily administration
 is sufficient.
Adverse effects:
- Heart burn, nausea & anorexia, but it is tolerated &
less ulcerogenic than PBZ; causes less faecal blood
loss than aspirin.

26. Uses:
- Suitable for use as short term analgesic as well as long term anti-
inflammatory action in –
Rheumatoid & Osteo-arthritis, Ankylosing spondylitis,
acute gout, musculoskeletal injuries, dental pain.
Dose: 20 mg BD for 2 days followed by 20 mg OD
(DOLONEX, PIROX
10, 20 mg cap.)

27. Ketorolac
- Potent analgesic & modest anti-inflammatory activity.
- In postoperative pain it has equalled the efficacy of
morphine.
- Inhibits PG synthesis & is believed to relieve pain by
a peripheral mechanism.
- Rapidly absorbed after oral & i.m. administration
& excreted unchanged in urine.
Pyrrolo-pyrrole derivative

28. Adverse effects:
- Nausea, abdominal pain, dyspepsia, ulceration,
loose stools, drowsiness, headache, dizziness,
nervousness, pruritus, pain at injection site.
- Rise in serum transaminases & fluid retention
have been noted.
Contra-indications:
- Should not be given to patients on the anti-coagulants

29. Uses:
 - In post-operative & acute musculoskeletal pain:
 15-30 mg every 4-6 hours (max. 90 mg/ day).
 - Also for renal colic, migraine & pain due to
 due to bony metastasis.
 - Used in a dose of 10-20 mg 6 hourly short term
management of moderate pain. AVAILABLE
: KETOROL, KETANOV (10 mg Tab.)

30. Nimesulide
- Sulfonamide derivative
- Selective inhibitor of PG synthesis & there
is some relative COX-2 selectivity.
Uses
 - Short lasting painful inflammatory conditions like
 sports injuries, sinusitis & other ENT disorders,
 dental surgery, bursitis, low backache, Postop pain,
 osteoarthritis & for fever.
Preferential cox-2 inhibitors

31. Pharmacokinetics:
 - Completely absorbed orally
 - Metabolism-Liver & Excretion- Urine
Dose- 100mg BD
( Nimulid, Nimegesic, Nimodol 100 mg Tab.)
Adverse effects
- Epigastralgia, heart burn, loose motions
- Dermatological rash, pruritus
- Hepatic failure & Renal failure in neonate.
(BANNED)

32. - Recently developed preferential COX-2 inhibitor.
- Has less analgesic, antipyretic activities, effective
in the treatment of rheumatoid & osteoarthritis as
well as soft tissue injury.
- Lower incidence of gastric erosions, ulcers &
bleeding.
Dose: 500 mg OD
(NABUFLAM, NILTIS 500 mg Tab.)
Nabumetone

33. Selective cox-2 inhibitors
Celecoxib, Rofecoxib, Valdecoxib
• NSAIDS that directly targets COX-2 which is produced at the
site of inflammation.
• Selectivity for COX-2 can half the risk of peptic ulceration.
• Cox-2-selectivity does not seem to affect other side-effects
of NSAIDs & there might be an increase in the risk for heart
attack, thrombosis & stroke by a relative increase in
thromboxane.

34. Uses-
 - Osteoarthritis.
 - Rheumatoid arthritis.
 - Ankylosing spondylitis.
 - For the management of acute pain in adults.
Pharmacokinetics:
 - Slow absorption
 - Metabolism-Liver & Excretion- Urine

35. Dose :
- Celecoxib- 100-200 mg BD (CELACT,ZYCEL)
- Rofecoxib- 12.5-50 mg OD
- Valdecoxib- 10 mg OD (VALOXIB, VALK)
Precautions:
- In patient who has clinical signs of liver toxicity or if systemic
manifestations arise, valdecoxib should be discontinued.
 - Should be used with caution in patients with CHF or
hypertension since fluid retention & edema can occur.

36. Paracetamol (Acetaminophen)
-- Central Analgesic action is like aspirin,
- i.e. it raises pain threshold, but has weak
- Anti-inflammatory action.
- Paracetamol is a good & promptly acting
Antipyretic Action.
Para-amino phenol derivatives

37. Uses:
 -Most commonly use analgesic for Headache,
 Musculoskeletal pain
 - Best drug to be used as Antipyretic.
 - Can be used in All Age groups(infants to elderly),
 pregnant/lactating women, & in patients in whom
 aspirin is contraindicated.
Adverse effects:
 Safe & Well tolerated, Nausea occur occasionally,
 High doses-Hepatic necrosis

38. Pharmacokinetics:
Well absorbed orally. Metabolism-Liver
 Excretion in Urine.
Dose- 0.5-1gm TDS 500mg Tab.
(Crocin, Paracin, Metacin, Pyrigesic)

39. Diuretics : ↓ Diuresis
-blockers : ↓ Anti-hypertensive effect
ACE inhibitors : ↓ Anti-hypertensive effect
Anticoagulants :↑ risk of G.I. Bleed
Sulfonylureas : ↑ Hypoglycaemia
Alcohol : ↑ risk of G.I. Bleed
Cyclosporine : ↑ Nephrotoxicity
Drug interactions with NSAIDS

40. Allergy to Asprin or any NSAID.
 Peptic Ulcers
 Should not be used < 16 years.
 During Pregnancy / Breast feeding.
 Anticoagulant Therapy.
 Suffering from blood clotting system disorders.
 Chronic liver diseases.
Contraindications

41. - Mild To Moderate Pain With Little Inflammation
– PARACETAMOL or low dose IBUPROFEN.
- Acute Musculoskeletal Pain, Osteoarthritic,
Injury Associated Inflammation
- IBUPROFEN ,DICLOFENAC
- Postoperative or other acute but Short Lasting Painful
Conditions With Minimal Inflammation
- KETEROLAC, NEFOPAM
Clinical notes

42. - Patients with history of asthma/ anaphylactoid reaction
- NIMESULIDE
- Gastric intolerance to conventional NSAID
- - ROFECOXIB, CELECOXIB

43. Advantages of topical medications
• Greater safety
• Rapid onset of action
• High concentrations can be attained at desired site without
exposing the rest of the body
• Fewer chances of drug interactions
• Non-invasive
• Better acceptability

44. Topical preparations
MEDICATIONS EXAMPLE
Topical anesthetics •Benzocaine in orabase (20%)
•Lidocaine gel
•Eutectic mixture of local anesthetic
(EMLA cream)
Neuropeptides •Capsaicin cream (0.025% & 0.075%)
NSAIDs •Ketoprofen (10-20%)
•Diclofenac (10-20%)
Sympathomimetic
agents
•Clonidine (0.01%)

45. ©M. S. Ramaiah University of Applied Sciences
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MEDICATIONS EXAMPLE
NMDA blocking
agents
•Ketamine (0.5% in orabase)
Anti-convulsants •Carbamazapine (2% in PLO base)
Tricyclic medications •Amitriptyline (2% in PLO base)
Anti-spasmodics •Baclofen (2% in PLO base)

46. Neuropeptides
(capsaicin)
Available as:
 Cream
Indications:
 Post herpetic neuralgia
 Diabetic Neuropathy
 Postmastectomy pain syndrome
 Trigeminal neuralgia

47. Topical anesthetics
(benzocaine, lidocaine)
Available as:
 Gels
 Ointments
 Sprays
 Adhesive patches
Indications:
 Post Herpetic Neuralgia
 Oral ulcers
 Burning mouth syndrome

48. NSAIDs
(Ketoprofen,diclofenac)
Available as:
 Cream
 Patch
Indications:
 Localized treatment of acute
pain associated with soft tissue
injury e.g. Musculoskeletal pain

49. Local drug delivery systems
• Mucoadhesive creams
• Transdermal creams
• Toothpastes
• Medicated chewing gums
• Dissolving tablets & lozenges
• Adhesive patches & powders
• Mouthwashes
• Medicated lipsticks

50. ©M. S. Ramaiah University of Applied Sciences
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Adjuvent drugs
- Antidepressants
- Anticonvulsants
- Neuroleptics
- Corticosteroids
- Systemic L.A.
- Alpha adrenergic agonists
- Botulinum toxins

51. ©M. S. Ramaiah University of Applied Sciences
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WHO ladder for treatment
Of chronic cancer pain

52. ©M. S. Ramaiah University of Applied Sciences
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- NSAIDs
- Acetaminophen
- Opioids
- Antidepressants
- Anticonvulsants
- Neuroleptics
- Corticosteroids
- Systemic L. A.’s
- Alpha adrenergic
agonists
- Botulinum toxin
Drugs used in management of
Chronic pain

53. Analgesics in pregnancy
• Acetaminophen
-Most Useful
-Any Stage
• Morphine
• Meperidine
• Aspirin (Not in 3rd trim.)
• Ibuprofen (Not in 3rd trim.)
• Pentazocine (With Caution)

54. Conclusion
• Analgesics are definitely useful in reducing
pain & improving the quality of life but have
their own spectrum of adverse effects.
• No single drug is superior to all others for
every patient. Choice of drug is inescapably
empirical.

56. Summary
• Analgesics are commonly used to dentistry to control pain due
to dental infections, post extraction etc.
• A good understanding of the various class of analgesics their
indications and adverse effects helps us in selecting the
appropriate analgesic.

57. Reference
• K D Tripathi, (2013), Textbook of Pharmacology. 7th Edition,
Jaypee Brothers Medical Publishers.
• Richard G Topazian, Goldberg, Hupp, (2002), Oral and
maxillofacial Infections. 4th Edition, Elsevier.
• Malcolm A Lynch, Martin S Greenberg, (2008), Burket’s Oral
Medicine. 11th Edition, BC Decker.

58. Disclaimer
• All data and content provided in this presentation are
taken from the reference books, internet – websites
and links, for informational purposes only.