Prednisone

see also: Etymology of Prednisone

The prednisone is a Corticostéroïde.

In Belgium, it is available in the form of masterly preparations and in particular under trade name Pred Forte.

PREDNISOLONE ACETATE

Identification of the substance: 11 beta, 17 alpha, 21-trihydroxyprégna-1,4-diene-3,20-dione 21-acetate

Pharmacological Properties

ANTIINFLAMMATOIRE (principal some)

ANTIINFLAMMATOIRE STEROIDIEN (principal some)

IMMUNOSUPPRESSEUR (principal some)

GLUCOCORTICOIDE (principal some)

Mechanisms of action

The MAIN THING

The hormone: - diffuses through the cellular membrane. - binds to a receiver cytosolic forming a complex with proteins of thermal shocks (HSP 90 and 70) and a immunophiline p59. After dimerisation, the complex receiving steroid binds to specific sequences of DNA (brief replies to corticoids or LIKING). - module the transcription of genes sensitive to corticoids by an interaction with factors of transcription (cytoplasmic or nuclear proteins). - increases the transcription and/or the stability of coding ARNm of proteins responsible for the action of the glucocorticoïdes. - represses certain genes on the level transcriptionnel while interacting with the nuclear factors necessary to the activation of these genes. - the degradation of ARNm increases or inhibits the synthesis or the secretion of proteins or the cytokines.

The effects bilogic of the action anti-inflammatory drug result in: - inhibition of the vascular permeability which allows the recruitment of the white globules towards the site of the ignition. - inhibition of the molecular events dependant on the activation of the white globules and their adhesion with the cells endothéliales:

expression of the major complex of standard histocompatibility II,
expression of the molecules of cellular adhesion (ELAM 1, ICAM 1),
the secretion of proteins of the C3 complement and the factor B,
the activity of the IL1,
the expression of the cycloexogénases of the type 2 (cox2) thus preventing the production of prostaglandins,
production of the metabolites of the pro-inflammatory acid arachidonic (the activity of the phospholipase A2 inhibits by stimulating the synthesis of lipocortine or annexine I).

- blocking of the secretion of IT 1, IT 6, TNF alpha. - reduction in the production and the dropping of leucotrienes. - depression of the tumoricide activity and bactéride of the macrophages and their differentiation. - immunosuppressor effect on the lymphocytes T and inhibition of secretion of the cytokines by these lymphocytes T. - inhibition of the proliferation of the lymphocytes B and the cytokines implied in the synthesis of the immunoglobulins (IT 1 with IT 6). Bibliographical references: - J Neuroimmunol 1992; 40: 281-286. - Am Rev Respir Say 1990; 141, Suppl: 18-21. - Proc Natl Acad Sci the USA 1992; 89: 3917-3921. - Science 1992; 258: 1598-1604. - Med Sci 1990,10:1003 - 1006. - Ann Intern Med 1993; 119: 1198-1208. - Immunol Rev 1980; 51: 337-357. - J Immunol 1980; 124: 2828-2833. - Eur J Immunol 1990; 20: 2439-2443. - Prog Biochem Pharmacol 1985; 20: 55-62.

SECONDARY

activity granylate cyclase of the receiver which deteriorates the electric potential of the cells.
stimulation of the reproduction of the alveolar cells of type II increasing the production of surfactant pulmonary:

- J Covering joint Invest 1980; 66: 504-510. - Radiat LMBO 1988; 115: 543-549. - Radiat LMBO 1988; 113: 112-119. Double connection 1-2 increases the antiinflammatoire activity. Esterification in the form of acetate gives an insoluble derivative: prolonged action.

Required Effects

ANTIINFLAMMATOIRE (principal)

ANTIALLERGIQUE (principal)

ANTIPRURIGINEUX (principal)

Therapeutic Indications

INFLAMMATORY RHEUMATISM (principal) Local treatment.

OSTEOARTHRITIS (principal)

RHEUMATISM ABARTICULAIRE (principal)

SCIATIC NERVE (principal)

Chéloïde (principal)

NEVRODERMITE (principal)

INFLAMMATORY EPANCHEMENT OF the SEREUSES (principal)

MYASTHENIE (to be confirmed)

Side effects

1. ULCERATE GASTRODUODENAL (SOME VERY RARE) Condition (S) Supporting (S): ANTIINFLAMMATOIRE NOT STEROIDIEN ASSOCIATES HIGH POSOLOGY TREATMENT PROLONGS ULCERATE OLD GASTRO-DUODENAL ULCERATE RECENT GASTRO-DUODENAL GENERAL WAY

2. GASTRODUODENITE (CERTAIN FREQUENT)

3. INSUFFICIENCY HYPOPHYSOSURRENALE (CERTAIN FREQUENT) Condition (S) Supporting (S): BRUTAL STOP OF THE TREATMENT HIGH POSOLOGY CONTINUOUS TREATMENT TREATMENT PROLONGS GENERAL WAY

4. KALIEMIE (REDUCTION) (CERTAIN RARE) Condition (S) Supporting (S): HIGH POSOLOGY CONTINUOUS TREATMENT TREATMENT PROLONGS GENERAL WAY

5. RETENTION HYDROSODEE (CERTAIN RARE) Condition (S) Supporting (S): HIGH POSOLOGY CONTINUOUS TREATMENT TREATMENT PROLONGS GENERAL WAY

6. MUSCULAR ATROPHY (CERTAIN RARE) Condition (S) Supporting (S): HIGH POSOLOGY CONTINUOUS TREATMENT TREATMENT PROLONGS GENERAL WAY

7. DELAY OF GROWTH (CERTAIN FREQUENT) Condition (S) Supporting (S): HIGH POSOLOGY CONTINUOUS TREATMENT TREATMENT PROLONGS GENERAL WAY

8. RESISTANCE TO THE INFECTIONS (REDUCTION) (CERTAIN FREQUENT) Condition (S) Supporting (S): GENERAL WAY HIGH POSOLOGY CONTINUOUS TREATMENT TREATMENT PROLONGS SEPTIC LOCAL INFILTRATIONS

Effect related to the properties glucocorticoïdes. Two cases of pneumonia to pneumocystis carinii during a treatment by the prednisolone (salt not specified) of a systemic érythémateux lupus: - Br J Rheumatol 1992; 31: 643-644.

9. SEPTIC ARTHRITIS (SOME VERY RARE) Intra-articular way

10. MICROCRYSTALLINE ARTHRITIS (CERTAIN RARE) Intra-articular way

11. ARTERIAL HYPERTENSION (SOME VERY RARE) Condition (S) Supporting (S): GENERAL WAY HIGH POSOLOGY CONTINUOUS TREATMENT TREATMENT PROLONGS

Several cases during the progressive reduction of posology, following a long-term treatment in asthmatic children: - J Allerg Covering joint Immunol 1992; 89: 816-821.

12. GLYCEMIA (INCREASE) (CERTAIN RARE) Condition (S) Supporting (S): DIABETES SWEETENS LATENT HIGH POSOLOGY CONTINUOUS TREATMENT TREATMENT PROLONGS GENERAL WAY

13. SYNDROME CUSHINGOIDE (CERTAIN FREQUENT) Condition (S) Supporting (S): HIGH POSOLOGY CONTINUOUS TREATMENT TREATMENT PROLONGS GENERAL WAY

14. CATABOLISM NITROGENIZES (INCREASE) (CERTAIN FREQUENT) Condition (S) Supporting (S): HIGH POSOLOGY GENERAL WAY

15. MENTAL HEALTH DISORDER (SOME VERY RARE) Condition (S) Supporting (S): PSYCHIATRIC ANTECEDENTS GENERAL WAY

16. PSYCHOMOTOR EXCITATION (SOME VERY RARE) Condition (S) Supporting (S): PSYCHIATRIC ANTECEDENTS GENERAL WAY

17. ACUTE PSYCHOSIS (SOME VERY RARE) Condition (S) Supporting (S): PSYCHIATRIC ANTECEDENTS GENERAL WAY

18. INTRACRANIAL HYPERTENSION (SOME VERY RARE)

19. CUTANEOUS ATROPHY (CERTAIN RARE) Condition (S) Exclusive (S): REPEATED HYPODERMIC INJECTIONS

Dependant on the properties glucocorticoïdes.

20. ULCERATE GASTRODUODENAL (AGGRAVATION) (CERTAIN RARE)

21. HYPERCORTICISME (CERTAIN FREQUENT)

22. OSTEOPOROSIS (SOME VERY RARE) Condition (S) Supporting (S): HIGH POSOLOGY CONTINUOUS TREATMENT TREATMENT PROLONGS GENERAL WAY

23. CHRONIC GLAUCOME (CERTAIN RARE) Condition (S) Supporting (S): LOCAL WAY TREATMENT PROLONGS

In ocular instillation and ophthalmic pomade. Approximately one year prolonged treatment. Usually disappears with the stop from the treatment.

24. CATARACT (TO BE CONFIRMED)

25. DIPLOPIA (TO BE CONFIRMED) Two cases after an administration péridurale or intrathécale (salt of prednisolone not specified): - Press Med 1997; 26: 271.

26. DISEASE THROMBOEMBOLIQUE (TO BE CONFIRMED)

27. MYOPATHY (TO BE CONFIRMED) A case under prednisolone (salt not specified), with ventilatory repercussion: - Am Rev Resp Say 1992; 146: 800-802.

28. POLYMORPHIC ERYTHEMA (TO BE CONFIRMED) A case of erythema generalized after injection intra-durale: - Br J Theumatol 1992; 31: 717-718.

Counter-indications

ULCERATE RECENT GASTRODUODENAL

KERATITIS HERPETIQUE

AMYLOSE

LOCAL INFECTION Condition (S) Exclusive (S): LOCAL

Routes of administration

- 1 - EYEPIECE - 2 - AURICULAR - 3 - NASAL - 4 - INTRALESIONNELLE - 5 - INTRAARTICULAIRE - 6 - EPIDURAL

Posology and mode of administration Crystalline suspension in injection will intra or periarticular, subcutaneous or intradermal, intra-tympanic, intraspinal. Proportion according to the ignition. Eye lotion, nasal drops. Rigorous asepsis in the event of application or of local infiltration. Administration by possible but nonusual general way in France. In the event of prolonged treatment, regular ophthalmologic monitoring.

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