Antiinflamasi Steroid Glucocorticoid

7/25/2019 Antiinflamasi Steroid Glucocorticoid

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Glucocorticoid

Anggelia Puspasari

Pharmacology and Theraupetic Departement

Medical and Health Sciences FacultyUniversity Jambi


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Regulasi Glukokortikoid Endogen


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Biosintesis Corticosteroid


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Mekanisme kerja


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Biologic effect of

glucocorticoid:

1. Protein breakdown2. Glucose formation

3. Lypolisis

4. Resistent to stress

5. Immunosuppressant


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

CELL TYPE FACTOR COMMENTS

Macrophages and

monocytes

Arachidonic acid and its metabolites

(prostaglandins and leukotrienes)

Mediated by glucocorticoid inhibition of

cyclooxygenase-2 and phospholipase A2.

Cytokines, including: interleukin (IL)-1, IL-6,

and tumor necrosis factor- (TNF-)

Production and release are blocked. The cytokines

exert multiple effects on inflammation (e.g., activation

of T cells, stimulation of fibroblast proliferation).

Acute phase reactants These include the third component of complement.

Endothelial cells Endothelial leukocyte adhesion molecule-1

(ELAM-1) and intracellular adhesion

molecule-1 (ICAM-1)

ELAM-1 and ICAM-1 are intracellular adhesion

molecules that are critical for leukocyte localization.

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-, GM-CSF, interferon-) Same as above for macrophages and monocytes.


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Drug overview


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Rute pemberian dan penggunaan klinis


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Pharmakokinetik


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Relative Potencies and Equivalent Doses of Representative Corticosteroids

COMPOUND ANTIINFLAMMATORY

POTENCY

Na+-RETAINING

POTENCY

DURATION OF

ACTION*

EQUIVALENT

DOSE,aMG

Cortisol 1 1 S 20

Cortisone 0.8 0.8 S 25

Fludrocortisone 10 125 I b

Prednisone 4 0.8 I 5

Prednisolone 4 0.8 I 56-

Methylprednisolone

5 0.5 I 4

Triamcinolone 5 0 I 4

Betamethasone 25 0 L 0.75

Dexamethasone 25 0 L 0.75

*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.b

This agent is not used for glucocorticoid effects.


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Efek samping


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Interaksi obat


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Table 59-4.Available Preparations of Adrenocortical Steroids and Their Synthetic Analogs

NONPROPRIETARY NAME (TRADE NAME) TYPES OF PREPARATIONS NONPROPRIETARY NAME (TRADE NAME) TYPES OF PREPARATIONS

Alclometasone dipropionate (ACLOVATE) Topical Cortisol (hydrocortisone) valerate (WESTCORT) Topical

Amcinonide (CYCLOCORT) Topical Cortisone acetate (CORTONE ACETATE) Oral, injectable

Beclomethasone dipropionate (BECLOVENT,

VANCERIL, others)

Inhalation Desonide (DESOWEN, TRIDESILON) Topical

Betamethasone (CELESTONE) Oral Desoximetasone (TOPICORT) Topical

Betamethasone dipropionate (DIPROSONE, others) Topical Dexamethasone (DECADRON, others) Oral, topical

Betamethasonesodium phosphate (CELESTONE

PHOSPHATE, others)

Injectable Dexamethasone acetate (DECADRON-LA, others) Injectable

Betamethasonesodium phosphate and acetate

(CELESTONE SOLUSPAN)

Injectable Dexamethasonesodium phosphate (DECADRON

PHOSPHATE, HEXADROL PHOSPHATE, others)

Topical, ophthalmic, otic,

injectable

Betamethasone valerate (BETA-VAL, VALISONE,

others)

Topical Diflorasone diacetate (FLORONE, MAXIFLOR) Topical

Budesonide (PULMICORT, RHINOCORT) Inhalation Fludrocortisone acetate* (FLORINEF) Oral

Clobetasol propionate (TEMOVATE) Topical Flunisolide (AEROBID, NASALIDE) Inhalation

Clocortolone pivalate (CLODERM) Topical Fluocinolone acetonide (FLUONID, SYNALAR,

others)

Topical

Cortisol (hydrocortisone) (CORTEF, HYDROCORTONE,

others)

Topical, enema, otic solutions,

oral, injectable

Fluocinonide (LIDEX) Topical

Fluorometholone (FLUOR-OP, FML, LIQUIFILM) Ophthalmic

Cortisol (hydrocortisone) acetate (HYDROCORTONE

ACETATE others)

Topical, suppositories, rectal

foam, injectable

Fluorometholone acetate (FLAREX) Ophthalmic

Cortisol (hydrocortisone) butyrate (LOCOID) Topical Flurandrenolide (CORDRAN) Topical

Halcinonide (HALOG) Topical

Cortisol (hydrocortisone) cypionate (CORTEF) Oral Medrysone (HMS LIQUIFILM) Ophthalmic

Methylprednisolone (MEDROL) Oral

Cortisol (hydrocortisone) sodium phosphate

(HYDROCORTONE PHOSPHATE)

Injectable Methylprednisolone acetate (DEPO-MEDROL,

MEDROL ACETATE, others)

Topical, injectable

Cortisol (hydrocortisone) sodium succinate (A-

HYDROCORT, SOLU-CORTEF)

Injectable Methylprednisolone sodium succinate (A-

METHAPRED, SOLU-MEDROL)

Injectable

Mometasone furoate (ELOCON) Topical Prednisone (DELTASONE, others) Oral

Prednisolone (DELTA-CORTEF) Oral Triamcinolone (ARISTOCORT, KENACORT) Oral

Prednisolone acetate (ECONOPRED, others) Ophthalmic, injectable Triamcinolone acetonide (KENALOG, others) Topical, inhalation, injectable

Prednisolone sodium phosphate (PEDIAPRED, others) Oral, ophthalmic, injectable Triamcinolone diacetate (ARISTOCORT, KENACORT

DIACETATE, others)

Oral, injectable

Prednisolone tebutate (HYDELTRA-T.B.A., others) Injectable Triamcinolone hexacetonide (ARISTOSPAN) Injectable* Fludrocortisoneacetateis intendedfor useas amineralocorticoid.

Note: Topicalpreparations includeagents for application toskin or mucous membranes increams, solutions,ointments, gels,pastes (for oral lesions),andaerosols; ophthalmicpreparations include solutions,s uspensions,and ointments; inhalationpreparations includeagents for nasal or oral inhalation.


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Used in allergic diseases

The onset of action of glucocorticoids in allergic diseases is delayed,and patients with severe allergic reactions such as anaphylaxisrequire immediate therapy with epinephrine

The manifestations of allergic diseases of limited duration such ashay fever, serum sickness, urticaria, contact dermatitis, drug

reactions, bee stings, and angioneurotic edema can be suppressedby adequate doses of glucocorticoids given as supplements to theprimary therapy.

In severe disease, intravenous glucocorticoids (methylprednisolone125 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 ofchoice by many experts.


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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 isconsidered essential, even though their onset of action isdelayed for 6 to 12 hours.

Intravenous administration of 60 to 120 mg ofmethylprednisolone (or equivalent) every 6 hours is usedinitially, followed by daily oral doses of prednisone (30 to60 mg) as the acute attack resolves. The dose then istapered gradually, with withdrawal planned for 10 days to 2weeks after initiation of steroid therapy.


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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 orreplace them entirely.

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Antiinflamasi Steroid Glucocorticoid