Distinctive Features of Corticosteroids

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Chapter: Essential pharmacology : Corticosteroids

Hydrocortisone (Cortisol) acts rapidly but has short duration of action. In addition to primary glucocorticoid, it has significant mineralocorticoid activity as well.


DISTINCTIVE FEATURES

 

The relative potency and activity of different natural and synthetic corticosteroids employed systemically is compared in Table 20.1.

 

 

1. Hydrocortisone (Cortisol)

 

Acts rapidly but has short duration of action. In addition to primary glucocorticoid, it has significant mineralocorticoid activity as well. Used for:

 

Replacement therapy—20 mg morning + 10 mg afternoon orally.

 

Shock, status asthmaticus, acute adrenal insufficiency—100 mg i.v. bolus + 100 mg 8 hourly i.v. infusion.

 

Topically (see Ch. No. 64) and as suspension for enema in ulcerative colitis (see Ch. No. 48).

 

LYCORTINS, EFCORLIN SOLUBLE 100 mg/2 ml inj. (as hemisuccinate for i.v. inj.) WYCORT, EFCORLIN 25 mg/ml inj (as acetate for i.m./intraarticular inj.). PRIMACORT 100, 200, 400 mg/vial inj.

 

2. Prednisolone

 

It is 4 times more potent than hydrocortisone, also more selective glucocorticoid, but fluid retention does occur with high doses. Has intermediate duration of action: causes less pituitaryadrenal suppression when a single morning dose or alternate day treatment is given. Used for allergic, inflammatory, autoimmune diseases and in malignancies: 5–60 mg/day oral, 10–40 mg i.m., intraarticular; also topically.

 

DELTACORTRIL, HOSTACORTINH, 5, 10 mg tab, 20 mg/ml (as acetate) for i.m., intraarticular inj., WYSOLONE, NUCORT, 5, 10, 20, 30, 40 mg tabs.

 

3. Methylprednisolone

 

Slightly more potent and more selective than prednisolone: 4–32 mg/ day oral. Methylprednisolone acetate has been used as a retention enema in ulcerative colitis.

 

Pulse therapy with high dose methylprednisolone (1 g infused i.v. every 6–8 weeks) has been tried in nonresponsive active rheumatoid arthritis, renal transplant, pemphigus, etc. with good results and minimal suppression of pituitaryadrenal axis.

SOLUMEDROL Methylprednisolone (as sod. succinate) 40 mg, 125 mg, 0.5 g (8 ml) and 1.0 g (16 ml) inj, for i.m. or slow i.v. inj.

 

The initial effect of methylprednisolone pulse therapy (MPPT) is probably due to its anti-inflammatory action, while long term benefit may be due to temporary switching off of the immunodamaging processes as a consequence of lymphopenia and decreased Ig synthesis.

 

4. Triamcinolone

 

Slightly more potent than prednisolone but highly selective glucocorticoid: 4–32 mg/day oral, 5–40 mg i.m., intraarticular injection. Also used topically.

 

KENACORT, TRICORT 1, 4, 8 mg tab., 10 mg/ml, 40 mg/ml (as acetonide) for i.m., intraarticular inj., LEDERCORT 4 mg tab.

 

5. Dexamethasone

 

Very potent and highly selective glucocorticoid. Long acting, causes marked pituitaryadrenal suppression, but fluid retention and hypertension are not a problem.

 

It is used for inflammatory and allergic conditions 0.5–5 mg/day oral. Shock, cerebral edema, etc. 4–20 mg/day i.v. infusion or i.m. injection. Also used topically.

 

DECADRON, DEXONA 0.5 mg tab, 4 mg/ml (as sod. phosphate) for i.v., i.m. inj., 0.5 mg/ml oral drops; WYMESONE, DECDAN 0.5 mg tab, 4 mg/ml inj.

 

6. Betamethasone

 

Similar to dexamethasone, 0.5–5 mg/ day oral, 4–20 mg i.m., i.v. injection or infusion, also topical.

 

BETNESOL, BETACORTRIL, CELESTONE 0.5 mg, 1 mg tab, 4 mg/ml (as sod. phosphate) for i.v., i.m. inj., 0.5 mg/ml oral drops. BETNELAN 0.5 mg, 1 mg tabs.

 

Dexamethasone or betamethasone are preferred in cerebral edema and other states in which fluid retention must be avoided.

 

7. Desoxycorticosterone acetate (DOCA) 


It has only mineralocorticoid activity. Used occasionally for replacement therapy in Addison’s disease: 2–5 mg sublingual, 10–20 mg i.m. once or twice weekly.

 

In DOCABOLIN 10 mg/ml inj (along with nandrolone).

 

In addition a number of topically active glucocorticoids have been developed.

 

Beclomethasone dipropionate budesonide, etc. are used by inhalation in asthma, as spray in nasal allergy, as well as for skin and mucous membrane lesions (see Ch. No. 16).

 

Fluocinolone acetonide, fluocortolone, clobetasol propionate and esters of betamethasone, dexamethasone, triamcinolone are described in Ch. No. 64.

 

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