Corticosteroid Drugs: - Darmawan, dr.,M.Kes

CORTICOSTEROID DRUGS
• Darmawan,dr.,M.Kes
Introduction
Inflammation?
Trauma, microba, Ag, cold
cell
inflammation anti-inflammatory drugs
+ - (stricture, fibrosis)
Adrenal cortex
 Glucocorticoids ~ CS (CORTISOL)
* antiinflammatory – immunosuppressive
* metabolic potency
 Mineralocorticoids (Aldosteron)
* Sod water retention edema
BP
 androgen
INTRODUCTION
1. Cs hormone
That effects almost every organ/systems
S.E . . . . . . . (1)
2. Therapeutic uses
* endocrine substitution th/.
* non endocrine
AI & IMMUNOSUPPRESIVE
OBAT DEWA . . . . . . .(2) masking effect
3. (1) & (2) PEDANG BERMATA DUA

REGULATION
 Synthesis & secretion
regulation FBM
CS level FBM (+)
CS level FBM (-)
What happens to the patient who
chronically consume CS exogen in large
dosage ?
CS level FBH (-)
adrenal gland suppresion
ATROPHY
DIURNAL CYCLE
Concentration in plasma
8 am : 16 mg/100 ml
4 pm : 4 mg/100 ml
What does this clinically

mean ?
CORTISOL
Natural glucocorticoid
Potency :
* antiinflammation : 1
* Na+ retention :1
* metabolic : 20
PHARMACOKINETICS
A : CS is a lipophylic drug
* Good : intestinal (p.o)
Conjunctival space (topical)
Synovial (p.e)
Nasal (spray)

* Slowly : skin
Good penetration : mucosa,
conjunctiva, scrotum - face

D : 80 – 90% is bound to globulin
5 – 10% albumin
The free fraction is 3 – 10%
CS is widely distribution
M : liver
: Rifampicin
Phenobarbital CS Met
Phenytoin

E : Kidney

MECHANISM OF ACTION
1. AFFECTS THE RNA TRANSCRIPTION RNA
2. INHIBITION OF PHOSPHOLIPID ENZYM
3. STABILITIZING MEMBRAN (?)

CS EFFECTS
I. METABOLIC EFFECTS
Cs dose related effect on CM, protein
and fat metabolism
1. Carbohydrate
gluconeogenesis HYPERGLYCAEMIA
or GLUCOCA
2. Proteins
Catabolic effect
in lymphoid
connective tissue
muscle ATROPHY
fat
skin
3. Fat
Redistribution of fat
moon face
buffalo hump
supraclav deposit
atrophy
II. ANTIIMFLAMMATORY AND
IMMUNOSUPRESION
1. On vascular events
Reduced vasodilatation
Decreased fluid exudation
2. On cellular events
Indication
* in area of acute inflammation :
decreased ( ) number and activity of leucosit
* in area of chronic inflammation :
decreased activity of mononuclear cells.
Decreased fibroblast function
* in lymphoid areas :
decreased clonal expansion of T and B cells.
decreased action of cytokine – secreting T cells.

3. On inflammatory and immune mediators
decreased : cytokines (IL)
eicosanoid
PAF
complement
histamin
4. Histamin release from basophil

III. BONE
Long term CS treatment OSTEOPOROSIS
High risk : children
post menopausal
IV. CNS
euphoria withdrawl effect
treatment depression, sleep
disturbances, psychotic
V. STOMATCH
 gastric acid
 protective (mucopolysaccharidas)
VI. ELECTROLYTE AND WATER

BALANCE
 Retention : sodium & water edema
BP
VII. SCELETAL MUSCLE
steroid myopathy weakness & fatigue
VIII. EYE
Long term therapy intraocular pressure
glaucoma
blind ?
IX. GROWTH
Long term therapy growth retardation
X. REPRODUCTIVE
synthesis & secretion of gonadotropins
♂ : hypogonadism
♀ : anovulation, oligomenorrhea, uterine
bleeding
ADVERSE EFFECT
I. LARGE DOSE – LONG TERM CS
THERAPI
II. REBOUND PHENOMENE (WITH DRAWL
EFFECT)
 >= 7 days
 Abrupt stopped
 Reactivation (exacerbation) of the disease
 Anorexia, nausea, vomiting, weigh loss,
lethargy, headache, fever, joint-muscle
pain, postural hipotension
 Tapering off or alternate day
INDICATION
1. Allergic drug reaction
2. Allergic rhinitis
3. Atopic dermatitis, exzema
4. Rheumatoid arthritis
5. Bronchial asthma
6. LLA
7. Organ transplants
8. Cerebral edem
9. Septicemia
10. Nephrotic syndrome
11. Lupus erythematic
CS SYNTHESIS
Compound Anti Na+ retaining Metabolic DOA Equivalent
Inflammatory Pot Pot Dose
Potency

Cortisol 1 1 20 S 20
Cortone 0,8 0,8 S
Prednisone 4 0,8 5 I 5
Prednisolone 4 0,8 5 I 5
Methylprednisolone 5 minimal I 4
Triamcinolone 5 0 4 I 4
Betamethasone 25 0 1 L 0,75
Dexamethasone 25 0 1-1,5 L 0,6

S : 8-12 h I : 12-36 h L : 36-72 h
DEXAMETHASONE
 Synthetic CS
 AI :
 Na – water retaining potency :
 Metabolic potency :
 DOA : 36-72 h :
 Indication : * patient with HT, DM
* acute therapy (septic shock-
brain edema)
SELECTION OF DRUG
1. REPLACEMENT THERAPY
2. LONG TERM ANTIINFLAMMATORY
3. THERAPY ACUTELY
P drugs Efficacy Safety Suitability Cost Notes
(%) (%) (%) (%)
Cortisol
Prednisone
Metilprednisolone
Dexamethasone
Triamcinolone
TOPICAL CORTICOSTEROID
Classification
Potency Drugs Preparation

1 Hidrokortison krim 0,25 – 2,5%
+ m-prednisolon krim 0,25 & 1,0%
Deksametason krim 0,1%

2 ++ Aklometason dipropionat krim 0,05%
Betametason valerat krim 0,01%
Triamsinolon asetonid krim 0,025%

3 +++ Hidrokortison butirat krim 0,1%
Flutikason propionat krim 0,05%
Desoksimetason krim 0,05%

Flusinolon asetonid krim 0,25%
Hidrokortison valerat krim 0,2%
Mometason fluroat krim 0,1%
Flusinolon asetonid salep 0,02%
4 ++++ Betamethason dipropionat krim 0,05%
Flutikason propionat salep 0,005%
Flusinolon asetonid salep 0,2%

Desoksimetason krim 0,05%
Mometason fluroat salep 0,1%

5 +++++ Batametason dipropinat dalam vehikulum yang
dioptimalkan 0,05%
Klobetasol propionat krim 0,05%
Diflorasone diacetat krim 0,05%
EFEK KS TOPIKAL

1. Vasoconstriction
Sunburn

2. Antiproliferation
Psoriasis

3. Antiinflammation
Eczema, sunburn.

Soal
1. Seorang anak umur 12 thn, mengeluh mata bengkak
pada pagi hari, yang menghilang pada siang hari. Sejak
2 minggu bengkak pada mata menetap dan disertai
bengkak pada mata kaki, badan terasa lemah.
Pemeriksaan:
Fisik: TD: 160/80 mmHg
Palpebra: edem (+)/(+)
Pretibial: edem (+)/(+)
Laboratorium: Esbach: (+++)
Pekerjaan orang tua: ?
Buatlah obat terpilih (P drug) berdasarkan ESSC?
2. Seorang laki-laki umur 32 thn, mengeluh
nyeri tenggorokan sejak 2 hari yang lalu,
demam, nyeri otot.
Pemeriksaan:
Pharing: hiperemis, detritus (+)
Diagosis: Pharingitis e.c bakteri
Pekerjaan: ?
Sebutkan obat terpilih ?

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CORTICOSTEROID DRUGS

inflammation anti-inflammatory drugs

That effects almost every organ/systems

OBAT DEWA . . . . . . .(2) masking effect

3. (1) & (2) PEDANG BERMATA DUA

adrenal gland suppresion

What does this clinically

3. STABILITIZING MEMBRAN (?)

4. Histamin release from basophil

VI. ELECTROLYTE AND WATER

steroid myopathy weakness & fatigue

Long term therapy growth retardation

2. LONG TERM ANTIINFLAMMATORY

Potency Drugs Preparation

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