Glucocorticoid

Anggelia Puspasari
Pharmacology and Theraupetic Departement
Medical and Health Sciences Faculty
University Jambi

Regulasi Glukokortikoid Endogen

Biosintesis Corticosteroid

Mekanisme kerja

Biologic effect of
glucocorticoid:
1.
2.
3.
4.
5.

Protein breakdown
Glucose formation
Lypolisis
Resistent to stress
Immunosuppressant

Table 59-3. Effects of Glucocorticoids on Components of Inflammatory/Immune Responses

CELL TYPE
FACTOR
COMMENTS
Macrophages and Arachidonic acid and its metabolites
Mediated by glucocorticoid inhibition of
monocytes
(prostaglandins and leukotrienes)
cyclooxygenase-2 and phospholipase A2.
Cytokines, including: interleukin (IL)-1, IL-6, Production and release are blocked. The cytokines
and tumor necrosis factor- (TNF-)
exert multiple effects on inflammation (e.g., activation
of T cells, stimulation of fibroblast proliferation).
Acute phase reactants
Endothelial cells

These include the third component of complement.

Endothelial leukocyte adhesion molecule-1 ELAM-1 and ICAM-1 are intracellular adhesion
(ELAM-1) and intracellular adhesion
molecules that are critical for leukocyte localization.
molecule-1 (ICAM-1)
Acute phase reactants

Same as above, for macrophages and monocytes.

Cytokines (e.g., IL-1)

Same as above, for macrophages and monocytes.

Arachidonic acid derivatives

Same as above, for macrophages and monocytes.

Basophils

Histamine, leukotriene C4

IgE-dependent release inhibited by glucocorticoids.

Fibroblasts

Arachidonic acid metabolites

Same as above for macrophages and monocytes.

Glucocorticoids also suppress growth factor-induced
DNA synthesis and fibroblast proliferation.

Lymphocytes

Cytokines (IL-1, IL-2, IL-3, IL-6, TNF-, GMCSF, interferon-)

Same as above for macrophages and monocytes.

Drug overview

Rute pemberian dan penggunaan klinis

Pharmakokinetik

Relative Potencies and Equivalent Doses of Representative Corticosteroids

COMPOUND

ANTIINFLAMMATORY Na+-RETAINING
POTENCY
POTENCY
1
1
0.8
0.8
125
10
0.8
4
0.8
4
0.5
5

DURATION OF EQUIVALENT
ACTION*
DOSE,a MG

S
20
Cortisol
S
25
Cortisone
b
I
Fludrocortisone
I
5
Prednisone
I
5
Prednisolone
I
4
6Methylprednisolone
0
I
4
Triamcinolone
5
0
L
0.75
Betamethasone
25
0
L
0.75
Dexamethasone
25
*S, short (i.e., 8-12 hour biological half-life); I, intermediate (i.e., 12-36 hour biological
half-life); L, long (i.e., 36-72 hour biological half-life).
aThese dose relationships apply only to oral or intravenous administration, as
glucocorticoid potencies may differ greatly following intramuscular or intraarticular
administration.
bThis agent is not used for glucocorticoid effects.

Efek samping

Interaksi obat

Table 59-4. Available Preparations of Adrenocortical Steroids and Their Synthetic Analogs
NONPROPRIETARY NAME (TRADE NAME)
TYPES OF PREPARATIONS
NONPROPRIETARY NAME (TRADE NAME)
Alclometasone dipropionate (ACLOVATE)
Topical
Cortisol (hydrocortisone) valerate (WESTCORT)

TYPES OF PREPARATIONS
Topical

Amcinonide (CYCLOCORT)
Beclomethasone dipropionate (BECLOVENT,
VANCERIL, others)
Betamethasone (CELESTONE)
Betamethasone dipropionate (DIPROSONE, others)

Topical
Inhalation

Cortisone acetate (CORTONE ACETATE)

Desonide (DESOWEN, TRIDESILON)

Oral, injectable
Topical

Oral
Topical

Desoximetasone (TOPICORT)
Dexamethasone (DECADRON, others)

Topical
Oral, topical

Betamethasonesodium phosphate (CELESTONE

PHOSPHATE, others)
Betamethasonesodium phosphate and acetate
(CELESTONE SOLUSPAN)

Injectable

Dexamethasone acetate (DECADRON-LA, others)

Injectable

Injectable

Dexamethasonesodium phosphate (DECADRON

PHOSPHATE, HEXADROL PHOSPHATE, others)

Topical, ophthalmic, otic,

injectable

Betamethasone valerate (BETA-VAL, VALISONE,

others)
Budesonide (PULMICORT, RHINOCORT)
Clobetasol propionate (TEMOVATE)
Clocortolone pivalate (CLODERM)

Topical

Diflorasone diacetate (FLORONE, MAXIFLOR)

Topical

Inhalation
Topical
Topical

Fludrocortisone acetate* (FLORINEF)

Flunisolide (AEROBID, NASALIDE)
Fluocinolone acetonide (FLUONID, SYNALAR,
others)
Cortisol (hydrocortisone) (CORTEF, HYDROCORTONE, Topical, enema, otic solutions, Fluocinonide (LIDEX)
others)
oral, injectable
Fluorometholone (FLUOR-OP, FML, LIQUIFILM)
Cortisol (hydrocortisone) acetate (HYDROCORTONE Topical, suppositories, rectal Fluorometholone acetate (FLAREX)
ACETATE others)
foam, injectable
Cortisol (hydrocortisone) butyrate (LOCOID)
Topical
Flurandrenolide (CORDRAN)
Halcinonide (HALOG)
Cortisol (hydrocortisone) cypionate (CORTEF)
Oral
Medrysone (HMS LIQUIFILM)
Methylprednisolone (MEDROL)
Cortisol (hydrocortisone) sodium phosphate
Injectable
Methylprednisolone acetate (DEPO-MEDROL,
(HYDROCORTONE PHOSPHATE)
MEDROL ACETATE, others)
Cortisol (hydrocortisone) sodium succinate (AInjectable
Methylprednisolone sodium succinate (AHYDROCORT, SOLU-CORTEF)
METHAPRED, SOLU-MEDROL)
Mometasone furoate (ELOCON)
Topical
Prednisone (DELTASONE, others)
Prednisolone (DELTA-CORTEF)
Oral
Triamcinolone (ARISTOCORT, KENACORT)
Prednisolone acetate (ECONOPRED, others)
Ophthalmic, injectable
Triamcinolone acetonide (KENALOG, others)
Prednisolone sodium phosphate (PEDIAPRED, others) Oral, ophthalmic, injectable
Prednisolone tebutate (HYDELTRA-T.B.A., others)
*

Injectable

Oral
Inhalation
Topical
Topical
Ophthalmic
Ophthalmic
Topical
Topical
Ophthalmic
Oral
Topical, injectable

Injectable
Oral
Oral
Topical, inhalation, injectable

Triamcinolone diacetate (ARISTOCORT, KENACORT Oral, injectable

DIACETATE, others)
Triamcinolone hexacetonide (ARISTOSPAN)
Injectable

Fludrocortisone acetate is intended for use as a mineralocorticoid.

Note: Topical preparations include agents for application to skin or mucous membranes in creams, solutions, ointments, gels, pastes (for oral lesions), and aerosols; ophthalmic preparations include solutions, suspensions, and ointments; inhalation preparations include agents for nasal or oral inhalation.

Used in allergic diseases

The onset of action of glucocorticoids in allergic diseases is delayed,
and patients with severe allergic reactions such as anaphylaxis
require immediate therapy with epinephrine
The manifestations of allergic diseases of limited duration such as
hay fever, serum sickness, urticaria, contact dermatitis, drug
reactions, bee stings, and angioneurotic edema can be suppressed
by adequate doses of glucocorticoids given as supplements to the
primary therapy.
In severe disease, intravenous glucocorticoids (methylprednisolone
125 mg intravenously every 6 hours, or equivalent) are appropriate.
In less severe disease, antihistamines are the drugs of first choice.
In allergic rhinitis, intranasal steroids are now viewed as the drug of
choice by many experts.

Bronchial Asthma and Other

Pulmonary Conditions
Data supporting the efficacy of corticosteroids are much
more convincing for bronchial asthma than for COPD.
In severe asthma attacks requiring hospitalization,
aggressive treatment with parenteral glucocorticoids is
considered essential, even though their onset of action is
delayed for 6 to 12 hours.
Intravenous administration of 60 to 120 mg of
methylprednisolone (or equivalent) every 6 hours is used
initially, followed by daily oral doses of prednisone (30 to
60 mg) as the acute attack resolves. The dose then is
tapered gradually, with withdrawal planned for 10 days to 2
weeks after initiation of steroid therapy.

Bronchial Asthma and Other

Pulmonary Conditions
In many patients, inhaled steroids (e.g.,
beclomethasone
dipropionate [VANCERIL], triamcinolone
acetonide [AZMACORT],
fluticasone [FLOVENT], flunisolide [AEROBID],
or budesonide [PULMICORT]) can either
reduce the need for oral corticosteroids or
replace them entirely.