Thursday, February 17, 2022

How to choose which glucocorticoid to use?😡😡😡

There are many clinical situations where glucocorticoids are needed. But
which one should be used among so many glucocorticoids? How should glucocorticoids be interchanged?

Effect period of glucocorticoids.

Glucocorticoids can be divided into short-acting, medium-acting and long-acting according to their effect period.

  1. Short-acting glucocorticoids: Commonly used are cortisone and hydrocortisone. They are natural and endogenous hormones. They have a short duration of action and weak anti-inflammatory effects. Therefore, they should not be used to treat rheumatism. It is generally used for replacement therapy of adrenal insufficiency.
  2. Medium-acting glucocorticoids: Commonly used intermediate-acting glucocorticoids are prednisone, prednisolone, triamcinolone, and methylprednisolone. They are often used to treat rheumatism.
  3. Long-acting glucocorticoids: Commonly used long-acting hormones are betamethasone and dexamethasone. They are long-acting and have strong anti-inflammatory properties. However, they significantly inhibit the hypothalamic-pituitary-adrenal axis and should not be used long-term. They should only be used as a temporary medication such as for treating allergies. Intermediate-acting and long-acting glucocorticoids are both exogenous and synthetic hormones.

Efficacy of different dosage forms of glucocorticoids.

Oral corticosteroids:

Equivalent dose: 

25mg cortisone = 20mg hydrocortisone = 5mg prednisone = 5mg prednisolone = 4mg triamcinolone = 4mg methylprednisolone = 0.6mg betamethasone = 0.75 dexamethasone.

Anti-inflammatory potency: 

  • Cortisone = 0.8
  • Hydrocortisone = 1
  • Prednisone = 3.5 to 4
  • Prednisolone = 4
  • Triamcinolone = 5
  • Methylprednisolone = 5
  • Betamethasone = 25 to 35
  • Dexamethasone = 30

Potency of mineralocorticoids:

  • Cortisone = 0.8
  • Hydrocortisone = 1
  • Prednisone = 0.8
  • Prednisolone = 0.8
  • Triamcinolone = 0
  • Methylprednisolone = 0.5
  • Betamethasone = 0
  • Dexamethasone = 0

Duration of action:

  • Short-acting glucocorticoids: 8 to 12 hours.
  • Medium-acting glucocorticoids: 12 to 36 hours.
  • Long-acting glucocorticoids: 36 to 54 hours.

Inhaled corticosteroids:

Drug

Low dose(ΞΌg)

Medium dose(ΞΌg)

High dose(ΞΌg)

Beclomethasone dipropionate

200 – 500

500 – 1000

1000 - 2000

Budesonide

200 – 400

400 – 800

800 – 1600

Fluticasone propionate

100 – 250

250 - 500

500 - 1000

Ciclesonide

80 – 160

160 – 320

320 - 1280

Equivalent dose: 

1000ΞΌg Beclomethasone dipropionate = 800ΞΌg Budesonide = 500ΞΌg Fluticasone propionate.

Topical corticosteroids:

Topical corticosteroids are frequently used in dermatology.

Weak glucocorticoids: 1% hydrocortisone acetate, 0.25% methylprednisolone.

Moderate glucocorticoids: 0.5% prednisolone acetate, 0.05% dexamethasone acetate, 0.05% clobetasone butyrate, 0.025%-0.1% triamcinolone acetonide, 1% hydrocortisone butyrate, 0.025% fludrocortisone acetate , 0.01% fluocinolone.

Potent glucocorticoids: 0.025% beclomethasone propionate, 0.1% mometasone furoate, 0.025% fluocinolone, 0.025% cloflusolone, 0.05% betamethasone valerate.

Super potent glucocorticoids: 0.02%-0.05% clobetasol propionate, 0.1% cloflubutasone, 0.1% betamethasone valerate, 0.05% halometasone, 0.05% diacetate difluorosone.

Therapeutic use.

  1. Alternative therapy for primary adrenal insufficiency: Adrenal insufficiency causes Addison disease. Hydrocortisone is effective in improving cortisol deficiency. Deficiencies in insufficient cortisol can lead to death.
  2. Alternative treatment for secondary adrenal insufficiency: Deficiency of adrenocorticotropic hormone synthesized by the pituitary gland or corticotropin-releasing hormone synthesized by the hypothalamus can cause this disorder. It can be treated with hydrocortisone.
  3. Diagnosis of Cushing syndrome: Excessive release of adrenocorticotropic hormone from the pituitary gland or tumor of the adrenal gland. This can cause too much cortisol and cause Cushing syndrome. In addition, long-term use of high-dose glucocorticoids can also cause iatrogenic Cushing syndrome. The release of cortisol is suppressed with dexamethasone under normal conditions, but not in patients with Cushing syndrome. Therefore, a test for the inhibition of cortisol by dexamethasone can be used to diagnose Cushing syndrome.
  4. Alternative Treatment for Congenital Adrenal Hyperplasia: It is a group of disorders caused by a deficiency in one or more of the enzymes that synthesize adrenal steroids. It causes the body to overproduce adrenaline androgen. Adrenocorticotropic hormone and corticotropin-releasing hormone release can be suppressed with adequate corticosteroids, thereby maintaining normal hormone levels in the body.
  5. Relieve inflammatory symptoms: Glucocorticoids can significantly reduce inflammation-related symptoms such as redness, swelling, heat, and pain in inflamed areas of rheumatoid arthritis or the skin. It can be used to treat asthma attacks and control persistent asthma symptoms. It is also used to treat inflammatory bowel disease. In addition, for some non-inflammatory diseases such as osteoarthritis, it can be administered intra-articularly to treat the onset of osteoarthritis.
  6. Treating Allergic Reactions: Glucocorticoids are used to treat a variety of allergic reactions such as drug-induced allergy and allergic rhinitis. In addition, when used for allergic rhinitis and asthma, topical administration is generally used to reduce the occurrence of systemic adverse reactions.
  7. Promoting fetal lung maturation: Premature infants may develop respiratory distress syndrome. Fetal lung maturation is regulated by fetal cortisol. Inject dexamethasone or betamethasone subcutaneously to the mother within 48 hours before delivery. It promotes fetal lung maturation.

Glucocorticoids have a wide range of clinical uses, and they are also used to treat other diseases such as cancer.

Side effect.

Although glucocorticoids are widely used and effective, their side effects are numerous and related to the timing and dosage of use. Side effects of long-term use of glucocorticoids include osteoporosis, increased appetite, hypertension, glaucoma, increased risk of infection, mood disorders, peripheral edema, central obesity, increased risk of diabetes, and hypokalemia.

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