drugs

Cortisonici

What are Cortisonics

Cortisonics are anti-inflammatory and immunosuppressive drugs, with a structure similar to endogenous corticosteroids. The latter are synthesized in the adrenal glands starting from cholesterol and are divided into two categories: that of mineralocorticoids and that of glucocorticoids (depending on whether the action mainly involves the glucidic or hydrosaline balance).

Synthetic corticosteroids have a structure similar to endogenous ones and as such are characterized by the presence of the cyclopentanoperidrofenantrene ring typical of cholesterol and steroid hormones; on the basic structure substitutions are carried out at the level of the carbon atoms to enhance their anti-inflammatory power and reduce the side effects on the intermediate metabolism.

Among the synthetic cortisones we mention prednisone, prednisolone, metasone, dexamethasone and fluocortisol.

For what they use

Cortisonics are found in preparations intended for topical use (to be applied to the skin or mucous membranes), inhalation, oral (it is the case of prednisone and prednisolone) and systemic (soluble esters and as such injectables). The therapeutic indications of these drugs are quite numerous; just to mention a few examples, cortisones are classically used in the presence of arthritis, joint pains and inflammations, dermatitis, allergic reactions, asthma, rhinitis, systemic lupus erythematosus, chronic autoimmune hepatitis and inflammatory bowel diseases. However, their use remains palliative, that is destined to mitigate the symptoms of a disease without removing the cause.

Effects

Effects → SIDE EFFECTS

  • They determine sodium retention (aldosterone) by increasing the excretion of potassium → HYPERTENSION, EDEMI, WATER RETENTION, IPOKALIEMIA
  • They reduce intestinal calcium absorption by antagonizing vitamin D-mediated transport. At the same time, they increase excretion → OSTEOPENIA
  • Gluconeogenesis increases from amino acids and decreases peripheral utilization of glucose → HYPERGLYCEMIA, INSULIN RESISTANCE, DIABETES MELLITUS.
  • Protein catabolism increases except in the heart and central nervous system → MUSCULAR ATROPHY, CAPILLARY FRAGILITY, DELAYED HEALING HEALING
  • Increases the catabolism of lipids, for which free fatty acids and ketone bodies rise in the blood → REDISTRIBUTION OF BODY FAT, WHICH IS ACCUMULATED AT THE LEVEL OF THE FACE, THE NECK AND THE ABDOMEN, WHILE IT REDUCES AT THE LEVEL OF ARTS, WHO COEISTS MUSCULAR HYPOTROPHY.
  • They can give psychotic phenomena due to elevation of mood, morning insomnia → DEPRESSIVE SYMPTOMS OF SUSPENSION.
  • At the blood level they cause an increase in red blood cells and hemoglobin, increase neutrophils and reduce the number of lymphocytes (antilinfoblastic action).

Anti-inflammatory action

  • Reduce redness, swelling and edema

  • Inhibit monocyte migration

  • Reduce circulating lymphocytes

  • Block MIF (factor inhibiting macrophage migration)

  • By means of lipocortin, they block the initial stage of release of arachidonic acid which gives rise to the inflammatory cascade.
  • The anti-inflammatory action of corticosteroids is related to the block of the synthesis of pro-inflammatory prostaglandins (responsible for edema, hyperalgesia, erythema and regulation of body temperature) and pro-inflammatory leukotrienes (which act as chemotactic factors, stimulate the production of free radicals and determine bronchoconstriction).
  • The immunosuppressive action of corticosteroids is inseparable from the anti-inflammatory one, which in turn is parallel to the effects on carbohydrate and anti-inflammatory metabolism; all these effects are not directly related to those on sodium retention.
Relative powers and equivalent doses of the main cortisone drugs

Composed

Anti-inflammatory powerPower of sodium retentionDuration of action. Biological half-life

Equivalent dose

mg os-ev

Cortisol11Short 8 -12 h20
Cortisone0.80.8Short 8 -12 h25
Fludrocortisone10125Short 8 -12 h0.1
Prednisone40.8Intermediate 12-35 h5
Prednisolone40.8Intermediate 12-35 h5
Metiprednisolone50.5Intermediate 12-35 h4
Triamcinolone50Intermediate 12-35 h4
Betamethasone250Long 36 - 72 h0.75
Desametason250Long 36 - 72 h0.75

Side effects

OF LIEVE ENTITIES (due to single administrations; generally a single dose is free of side effects and - for a short period, up to a week - even of harmful effects)

  • Increased appetite, weight gain also due to water retention
  • Hypertrichosis and pupure striae
  • Lunar facies and petechiae
  • Increased endocular pressure

OF MEDIUM ENTITIES (due to prolonged use of cortisone drugs)

  • Steroid Diabetes
  • Potassium loss
  • Growth delay
  • Aggravation of ulcers
  • Infection aggravation
  • dysproteinemia

SERIOUS (due to prolonged use and high doses of cortisone)

  • hemorrhage
  • edema
  • Osteoporosis and fractures
  • polyneuritis
  • dysproteinemia