Category:Corticosteroids

From Ganfyd

(Redirected from Corticosteroid)
Jump to: navigation, search

Used primarily for their glucocorticoid (anti-inflammatory) activity, when significant mineralocorticoid is disadvantageous.

This subgroup are used often in supraphysiological doses for their immunodulating or immunosuppressant properties. This runs of risk of fairly predictable side effects which are a classic situation of trading off benefits to these risks.

Steroids used therapeutically will have differential properties to each other that can be very important to understand. Some of these differences may have minimal clinical impact but others such as the relative potency and insolubility designed into some esters are very important. Most steroids used at long term therapeutic dosage (not replacement physiological dosage which in adults is about 30mg of hydrocortisone a day) have predictable side effects that do not vary much.

Comparative properties steroids (based on 20mg adult dose hydrocortisone)
Steroid Comparative glucocorticoid activity Comparative mineralocorticoid activity Comment
Prednisolone 5mg 16mg The active drug that prednisone is metabolised to
Prednisone 5mg 16mg Prodrug with ketone radical on C-11 which is hydrolysed to prednisolone.
Dexamethasone 750 µg none Usual to use to treat CNS oedema and if heart failure. The doses of the various salts cause confusion and be careful of the preparation used if given into an sensory organ or CSF as it must be preservative free
Hydrocortisone (cortisol) 20mg 20mg Corticosteroid of choice for physiological replacement as fair mineralocorticoid activity
Betamethasone 750 µg none
Methylprednisolone 4mg 10mg Prodrug with ketone radical on C-11 which is hydrolysed.
Cortisone acetate 25mg 25mg Prodrug with ketone radical on C-11 which is hydrolysed. As acetate will be insoluble. Fair mineralocorticoid activity.
Deflazacort 6mg No affinity for corticosteroid binding globulin (transcortin) and has markedly less crossing of the blood-brain barrier
Triamcinolone 4mg none
Fludrocortisonealdosterone 2mg 160µg Additional fluorination at the C-9 position enhances both glucocorticoid and mineralocorticoid activity
Aldosterone Prototype mineralocorticoid

The introduction to the hydrocortisone basic structure of a double bond between C-1 and C-2 increases glucocorticoid and anti-inflammatory activity. Many steroids are administered as esters. Esterification of the alcohol at C-21 determines the extent of water/lipid solubility. Esterification with acetic acid, yields water-insoluble drugs used for long acting IM or IA formulations (eg, methylprednisolone acetate). Esterification by succinic acid or a phosphate can yield a hydrosoluble ester useful for iv preparations. Esterification at C-17 (valerate) produces a lipophilic compound with an enhanced topical:systemic potency ratio. Similarly fluticasone propionate is designed to be rapidly metabolised to reduce systematic side effects and is used in respiratory inhalers.

Subcategories

This category has only the following subcategory.

G

Pages in category "Corticosteroids"

The following 14 pages are in this category, out of 14 total.

B

C

C cont.

D

F

H

M

P

T

Personal tools