pharmacology

1. 1
PRESENTED BY
Dr. E. RAMNATH
DEPARTMENT OF PERIODONTOLOGY

2. History
 By the middle of 19th century it was demonstrated
that adrenal glands were essential for life
 Later, it was appreciated that the cortex was more
important than the medulla
 A number of steroidal active principles were
isolated and their structures were elucidated by
kendall and his coworkers in the 1930s.
2

3.  However, the gate to their
great therapeutic potential was
opened by Hench (1949) who
obtained striking improvement
in rheumatoid arthritis by using
cortisone.
 The nobel prize was awarded
the very next year to kendall
and Hench.
 Currently, corticosteroids are
drugs with one of the broadest
spectrum of clinical utility.
3

4. Functional anatomy and histology of
adrenal glands

4

5. 5

6. 6

7. 7
Zones of adrenal cortex Hormones
Zona glomerulosa Aldosterone
Desoxycorticosterone
Zona fasciculata
Cortisone
Cortisol
Zona reticularis
Dehydroepiandrosterone
Androstenidione
Traces of estrogens
Essentials Of Medical Physiology 3rd Edition,
K Sembulingam

8. 8
MECHANISM OF ACTION
plasma memb
Corticosteroids
CYTOPLASMIC
RECEPTOR
PROTEIN
GLUCOCORTICOID
RESPONSE
ELEMENT
Nucleus
Transcription of
m - RNA
New protein
synthesis
TOTAL
TIME
30 – 60 mins

9. On resistance to stress 9
Physical or mental stress
Increases ACTH
Increase in glucocorticoid secretion
High resistance to body against stress
GOODMAN & GILMAN'S THE PHARMACOLOGICAL BASIS OF
THERAPEUTICS - 11th Ed. (2006)

10. Steroids in Dentistry
 Used primarily to decrease postoperative edema and
manage oral inflammatory diseases
10

11. Classification of steroids based on their
relative activity
11
Mineralocorticoids
• Desoxycorticosterone acetate(DOCA)
• Fludrocortisone
• Aldosterone

12. Classification of steroids based on their
relative activity
12
Short acting
(t1/2 < 12 hr)
• Hydrocortisone
• Cortisone
Intermediate
acting:
(t1/2 12 – 36)
• Prednisole
• Methyl prednisole
• Triamcinolone
Long acting:
(t1/2 > 36 hrs)
• Paramethasone
• Dexamethasone
• Betamethasone

13. 13
Cortisone
Oral: 5, 10, 25 mg tablets
Parentral:22,25 mg of
solution

14. 14
Hydrocortisone
Oral:5mg,10mg,20mgtab
Topical:
1%eye drops
0.025%nasal drops
0.25-2.5%skin cream
Parenteral:25, 50 mg for IV,IM,SC Injections

15. 15
Prednisolone
Oral:5,10, 20 mg tablets,
15mg/5 ml syrup, 5mg
suspension as pediatric drops
Parenteral:25,50 mg
IM,IV,Intralesional

16. Triamcinolone
Oral:1,4,8mg syrup
Topical:0.1% eye drops, ointment
Parentral: 3,10,40 mg for I.M,
intraarticular, intralesional
injections
16

17. 17
Dexamethasone
Oral:0.25,0.5,0.75,1,2,4,6mg tablets
Topical:0.1% eye drops, ear drops,
skin ointment
Parenteral: 4,8,10,20 mg for IV, IM,
intralesional and intraarticular.

18. 18
Betamethasone
Oral: oral drops – 0.5 mg/ ml, tablets –
0.5 to 1 mg.
Topical – 0.1% eye drops, ointment,0.05%
nasal drops, 0.12% skin creams
Parenteral:4 mg/ml for IM, IV,
intralesional, intraarticular

19. ADMINISTRATION OF
STEROIDS
 TOPICAL
 SYSTEMIC
 INTRA - LESIONAL
19

20. Protocols for use -(TC)
 POTENCY
 RELIEF
20
JDR April 2005 vol. 84 no. 4 294-301

21. 21
short course of
TCs
Accelerate
remission without
adverse effects
Recurrent aphthous
stomatitis (RAS), some
cases of erythema
multiforme (EM), and
Drug-induced
ulceration.
TCs must be used
for longer, less
predictable periods
Severe RAS, Erosive oral
lichen planus (OLP),
specific forms of EM,
and mucous membrane
pemphigoid (MMP)
Scully et al., 1999; Chan et al., 2002
Criteria for use topical and systemic

22. 22
very severe cases
of ulceration
Short course of systemic
corticosteroids followed
by maintenance regimen
of TCs and or can also be
started simultaneously
with the systemic therapy
Pemphigus
vulgaris ,10-30%
of Pemphigoid
patients, Erosive
lichen planus
Inevitably be treated with
systemic corticosteroids
and/or other
immunosuppressant
therapies
Laskaris and Angelopoulos, 1981;
Nisengard and Neiders, 1981; Fine et al., 1984;
Domloge-Hultsch et al., 1994; Dayan et al., 1999

23. The key factors 23
JDR April 2005 vol. 84 no. 4 294-301
The specific diagnosis
The severity of the oral disease
The presence or absence of extra-oral lesions
The medical history of the patient

24. Factors that influence the
effectiveness of TCs:
24
JDR April 2005 vol. 84 no. 4 294-301
The intrinsic potency of the drug

25. Factors that influence the
effectiveness of TCs:
25
JDR April 2005 vol. 84 no. 4 294-301
The contact time between the
drug and lesion and the vehicle
used to apply it;

26. Factors that influence the
effectiveness of TCs:
26
JDR April 2005 vol. 84 no. 4 294-301
Concentration

27. Success of a topical medicine
27
Two main factors
Number of applications per day
High-potency
(2-3 times)
Low potency
(5-10 times)
The vehicle
used
Various vehicles
JDR April 2005 vol. 84 no. 4 294-301

28. Various vehicles. 28
JDR April 2005 vol. 84 no. 4 294-301
Orabase (Stoy, 1966),
Cyanoacrylate (Jasmin et al., 1993),
Bioadhesive patches made of cellulose derivatives (Mahdi et al., 1996),
Gels (Regezi and Sciubba, 1999), and
Denture adhesive paste (Lo Muzio et al., 2001).

29. Steroids as anti- inflammatory 29
Prevention of postoperative pain,
edema, trismus after 3rd molar surgery
Prevention of postoperative edema
after orthognathic surgery
TREATING alveolar osteitis

30. 30
Phospholipids
Arachidonic acids
lipoxygenase Cylo - oxygenase
Leukotriene
Prostaglandins,
Thromboxane
Prostacyclins
Phospholipase A2
Lipocortin
Corticosteroids

31. Steroids as intra-canal
medicaments
 Ledermix
 triamcinolone acetonide + demeclocycline.
31
Journal of Interdisciplinary Dentistry / May-Aug 2014 / Vol-4
/ Issue-2

32. Corticosteroids in auto immune disorders and other aids
32
• Eg: Erosive LP
• RAS
Ulcerative, Vesiculoerosive
diseases
• Eg: CGCG
• HemangiomaBenign lesions
• Eg: Mucocele
Salivary gland disorders
• Eg: Osteoarthritis
• Rheumatiid arthritisTMJ Disorders
• Eg. Post herpatic neuralgia
Neuralgia Treatment
• OSMF
Miscellanous

33. Systemic steroids for ulcerative
vesiculobullous diseases
33

34. major aphthae or severe multiple
minor aphthae
 Prednisone therapy should be started at 1.0 mg/kg/day
in patients with severe RAU and should be tapered after
1 to 2 weeks.
34

35. 35
Minor EM 20 – 40 mg/day for 4 – 6
days / PREDNISOLONE
Severe or rapidly
progressing
lesions
60 mg/day slowly
tapered by 10 mg/day
over 6 weeks
Erythema multiforme

36. Pemphigus Vulgaris
 Mainstay 1-2mg/kg/d.
 Initial dose of treatment – 0.5 mg/kg/day to 3 mg/kg/d
 Dose that achieves clinical control is maintained for 2-
3 weeks and then gradually tapered.
36
Burkit’s Oral Medicine, 11th edition

37. Pulse therapy
 Also called short term therapy
 High dose therapy involves a 48-72 hrs course of
intensive steroid administration
 Single i.v injection of a supra-physiological dose of
steroid
 Dose of 0.5-2g of prednisolone or equivalent
37

38. 39Cicatricial pemphigoid
Predisolone – 30
to 60 mg/day
2-3 weeks to
stop new bullae
formation
Tapered by 20%
every 2-3 weeks
until the dose of
10 mg is reached
Dose maintained on
alternate days and
reduced by 5 mg
every 2 weeks, then
stopped

39. 40Bullous pemphigoid
Clobetasol propionate
20 -40 mg/day is more
effective for the treatment.
JIAOMR, April-June 2011;23(2):128-131

40. 41Lichen planus
Prednisolone
1mg/kg/d for <7
days
Tapered to
10-20mg per day
for 2 weeks
Burkit’s Oral Medicine, 11th edition
JIAOMR, April-June 2011;23(2):128-131

41. 42Lupus erythematosus
Predisolone – 20
- 30 mg/day for
2- 6 weeks
Tapered
gradually

42. Steroids in the treatment of benign
lesions
43
CENTRAL GIANT CELL GRANULOMA
HEMANGIOMA

43. 44CGCG
Intralesional injection of triamcinolone
can be given in a dose of 1 to 2 mg/kg/d
(maximum of 60 mg).
The treatment interval at 4 to 6 weeks.

44. Hemangioma 46
Prednisone at a dose of 20-30
mg/d can be given for 2 weeks
to 4 months
( Fost and Esterly)
Intralesional triamcinolone
acetonide (4 mg/mL)
(Hawkins et al)

45. 47
Steroids in salivary gland disorders
MUCOCELE

46. 48Mucocele
 0.05% clobetasol
propionate 3 times a
day for 4 weeks in a
mucosal adhesive base.
 Intralesional injections

47. 51
Steroids in neuralgia
POST HERPETIC
NEURALGIA

48. 52Post herpetic neuralgia
To reduce incidence of post herpetic neuralgia:
 Prednisolone 20 to 30 mg/day for 7 – 10 days
tapered to 10 mg/day for 1 week
(Treatment of oral diseases, George Lascaris)

49. 54
Steroids for TMJ disorders
OSTEOARTHRITIS
RHEUMATOID ARTHRITIS

50. 55
Rheumatoid
arthritis
Intraarticular injection –
10 to 40 mg/ml
osteoarthritis
Intraarticular injection –
20 mg/ml(2 injections 14
days apart)
Arthritis

51. 56
Miscellaneous
OSMF

52. 57OSMF
Predisolone – 20
- 30 mg/day for
2 – 4 weeks
Gradually taper
Discontinue in 1-
2 months

53. 58
Injections of triamcinolone 10mg/ml diluted
in 1 ml of 2% lidocaine with hyaluronidase 1500
IU, biweekly for 4 weeks.
(Borle et al)
dexamethasone (4mg/ml) and
two parts of hyaluronidase,
diluted in 1.0 ml of 2%
xylocaine.

54. 59Adverse effects
Due to extention of pharmacological action occuring
with prolonged therapy
Mineralocorticoids:
 Sodium and water retention
 Edema
 Hypokalemic alkalosis
 Progressive rise in B.P
 Fluid and electrolyte disturbance

55. 60Glucocorticoid:
Metabolic effects:
 Hyperglycemia
 Ketoacidosis
 Hyperosmolar coma
 Hypophosphatemia

56. 61
Cushing’s Habitus:
Prolonged therapy causes
 Central obesity with moon face
 Buffalo hump
 Pink florid striae are liable to appear on the
abdomen, hips and pectoral region and skin may
become friable

57. 62
CVS and renal system:
 Hypertension
 Salt and water retention
 Hypokalemic alkalosis
CNS:
 Influence mood, sleep pattern
 Insomnia
 Acute psychotic reactions
 Benign intracranial hypertension
 Epilepsy

58. 63
Suppression of inflammation and immune response:
 Latent infection may flare
 Oppurtunistic infection with low grade pathogens
Retardation of linear growth:
 Occurs in children who receive more than 50 mg
of cortisone per day.

59. Relative Contraindications: 64
 Peptic ulcer
 Diabetes mellitus
 Hypertension
 Pregnancy
 Herpes simplex
keratitis
 Tuberculosis
 Osteoporosis
 Psycosis
 Epilepsy
 Renal failure

60. 65Adrenal crisis
Causes
Sudden withdrawal of
glucocorticoid treatment

61. Rule of 2
Adrenocortical suppression should be suspected if a patient
has received Glucocoticoid therapy through two of the
following methods
 In a dose of 20 mg or more of cortisone or its equivalent
 Via oral or parenteral route or a continuous period of 2
weeks or longer
 Within 6 months -2 years of therapy
66
Medical emergencies in dental office, Stanley F.Malamed
Complications in Anesthesia - John L. Atlee; Page-132

62. Drug interactions 67
Glucocorticoid dosage decreased:
 Antibiotics (Erythromycin)
 Cyclosporine
 Isoniazid
 Ketakonazole
 Estrogen
Reduce metabolic
clearance

63. THANK YOU
68