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(μg)	Medium dose(μg)	High dose(μg)
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: 

1000μg Beclomethasone dipropionate = 800μg Budesonide = 500μg 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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Have you ever used corticosteroids ointments❓❓❓

Topical glucocorticoid is a very commonly used topical drug. Some people think that it is a panacea that can cure skin diseases such as itching, redness and swelling. However, some people refuse to use it because it contains steroids. The following are some practical knowledge about topical glucocorticoids.

1. Classification and intensity.

According to the different types and concentrations of glucocorticoids, topical glucocorticoids can be divided into 4 categories: super strong, strong, medium and weak. The same glucocorticoid has different strengths at different concentrations.

Commonly used topical glucocorticoids
Super strong	Clobetasol propionate	0.02%	1.    It is suitable for severe and hypertrophic skin lesions. 2.      Not for use in children <12 years old. 3.    Do not use on soft skin area. 4.    Long-term use in a small area. 5.    Do not exceed 50g per week. 6.    Continuous medication should not exceed 2-3 weeks. 7.    * They can be used with caution in children.
	Betamethasone valerate	0.1%
	Halometasone	0.05%
	Halcinonide	0.1%
	Fluocinolone	0.2%
Strong	Beclomethasone dipropionate	0.025%
	Betamethasone valerate	0.05%
	Fluocinolone	0.025%
	*Fluticasone propionate	0.05%
	*Mometasone furoate	0.1%
Medium	Prednisolone acetate	0.5%	1.    Suitable for mild to moderate skin lesions. 2.    It should not be used for a long time in a large area. 3.    It can be applied continuously for 4-6 weeks. 4.    Children <12 years old try not to use it continuously for more than 2 weeks.
	Dexamethasone acetate	0.05%
	Clobetasone butyrate	0.05%
	Hydrocortisone butyrate	1%
	Triamcinolone acetonide	0.025%
	Fludrocortisone acetate	0.025%
	Fluocinolone acetonide	0.01%
Weak	Hydrocortisone acetate	1%	1.    Suitable for mild to moderate skin lesions. 2.    Apply to the soft skin areas. 3.    Suitable for children <12 years old. 4.    It can be used in a larger area in a short time. 5.    It can be used for a long time if necessary.
	Methylprednisolone acetate	0.025%
	Desonide	0.05%
	Fluocinolone acetonide	0.0025%

Although fluticasone propionate and mometasone furoate are both strong glucocorticoids, they are less absorbed throughout the body when used externally. They are suitable for use by the elderly, infants and in a large areas.

2. The choice of topical glucocorticoids in various populations.

Children and the elderly: It is advisable to choose weak glucocorticoids, and use strong and super strong types with caution.

Pregnant women: Glucocorticoids should be used with caution in pregnant women. Weak or medium types can be selected when they must be used.

Soft skin areas: The face, neck, armpits, groin, inner thighs, perineum and other soft skin areas have a high drug absorption rate, so strong glucocorticoids should not be used. When it must be used, desonide, mometasone furoate and hydrocortisone can be used.

Ointment: The ointment dosage form has an encapsulating effect, which enhances the drug penetration ability. Ointment is suitable for keratinized, hypertrophic and desquamative skin, especially palms and soles. It is not recommended for non-hypertrophic, keratinized skin lesions on soft skin areas such as the face. Ointment should not be used in skin areas where babies wear diapers.

Creams, gels and solutions: They are suitable for all kinds of skin lesions and are also suitable for thick hair areas.

3. Indications.

Dermatitis, eczema, papular urticaria, erythema scaly skin disease, autoimmune skin disease, etc.

4. Contraindications.

Impetigo (bacterial infection), tinea hand and foot (fungal infection), shingles (viral infection), rosacea, acne, skin ulcers, etc. It is also not suitable for acute urticaria. The redness and itching caused by acute urticaria should be relieved with appropriate antihistamines (such as cetirizine, loratadine).

5. Dosage:

The most commonly used method for estimating the amount is the "fingertip unit"(FTU).

FTU: It refers to the amount of ointment squeezed from the ointment tube (with a diameter of 5mm) to an adult's fingertip (from the end of the index finger to the horizontal line of the first knuckle joint). A fingertip unit is about 0.5g ointment.

Estimate the skin area with the palm of your hand, and then calculate the FTU based on the area. Use about 0.5 FTU per palm area.

6. Adverse reactions.

The correct use of topical glucocorticoids is relatively safe. Long-term or large amounts of topical glucocorticoids may induce or aggravate local infections, leading to skin atrophy, telangiectasia, hirsutism, pigment changes, hormone dependence and other adverse reactions.

Patients should actively monitor for adverse reactions: The strong and super strong types are once every 2 weeks, the medium types are once every 3-4 weeks, and the weak types are once every 4-6 weeks.

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Application of glucocorticoids in clinical diseases.👀

The applications of glucocorticoids are very extensive and vary with the dose.
Glucocorticoids secreted under physiological conditions mainly affect the metabolism of substances. It will cause metabolic disorders and death when lacking. When glucocorticoids are pharmacological doses, in addition to affecting substance metabolism, it also have immunosuppressive , anti-inflammatory, detoxify and anti-shock effects.

1. Classification and difference of common glucocorticoids

According to the duration of action, glucocorticoids can be divided into three categories:

Category	Drug	Dose equivalent (mg)	Effective drug duration (hours)
Short-acting	Cortisone	25	8-12
	Hydrocortisone	20
Medium-acting	Prednisone	5	12-36
	Prednisolone	5
	Methylprednisolone	4
Long-acting	Dexamethasone	0.75	36-54
	Betamethasone	0.6

2. Glucocorticoid treatment course and withdrawal

Pulse therapy: The course of treatment is usually less than 5 days. It indicated for rescue of critically ill patients. The drug can be withdrawn quickly.

Short-term treatment: The course of treatment is less than 1 month. It indicated for infection or allergic diseases. Withdraw the drug by gradually reducing.

Medium-term treatment: The course of treatment is during within 3 months. It indicated for long term and multiple organ involvement disease. Withdraw the drug by gradually reducing.

Long-term treatment: The course of treatment is more than 3 months. It indicated for chronic autoimmune diseases, such as systemic lupus erythematosus. Before stopping the drug, the drug treatment should be gradually transitioned to alternate day therapy, then reduce the dose gradually and slowly.

Alternative therapy: Lifetime use. It indicated for primary or secondary chronic adrenocortical insufficiency.

3. Application of glucocorticoids in common diseases

Hyperthyroidism crisis: The level of thyroid hormones is sudden increase in the body. It is always related to the patients with insufficient treatment in severe or chronic hyperthyroidism. 

Treatment: Inorganic iodides, antithyroid drugs, β-receptor blockers and glucocorticoids (glucocorticoids can inhibit the conversion of peripheral T4 to T3).

Graves' ophthalmopathy: It is an organ-specific autoimmune disease related to the thyroid. It mainly manifests as exophthalmos, eyelid contracture, periorbital edema, bulbar conjunctival edema and eyeball activity dysfunction.

Treatment: For mild, the main treatment is to control hyperthyroidism or hypothyroidism. For moderate to severe, intravenous or oral glucocorticoid therapy is the main treatment.

Autoimmune hemolytic anemia: It is caused by lymphocytes function abnormally. Lymphocytes produce antibodies against the red blood cells, which accelerates the destruction of red blood cells in the body.

Treatment: For acute hemolytic attacks, intravenous infusion of dexamethasone or methylprednisolone is the first choice. Oral prednisone is the first choice for milder conditions (Taken in the morning).

Idiopathic thrombocytopenic purpura: The patient produces anti-platelet autoantibodies in the body.

Treatment: Glucocorticoids are the first choice. Immunosuppressants are needed for ineffectiveness and large doses of intravenous γ-globulin are used for severe bleeding.

Aplastic anemia: Abnormal activation and hyperfunction of T lymphocytes cause bone marrow damage.

Treatment: Antithymus/lymphocyte globulin (daily simultaneous application of glucocorticoids to prevent allergic reactions) and cyclosporine are commonly used.

Graft-versus-host disease: It is the most common complication of allogeneic hematopoietic stem cell transplantation and involving a variety of immune cells and inflammatory cytokines.

Treatment: For acute, use glucocorticoids (common use methylprednisolone and prednisone) combined with calcineurin inhibitors. For chronic, use cyclosporine A combined with glucocorticoids.

Nephrotic syndrome: It is characterized by massive proteinuria and it often accompanied by hypoalbuminemia (≤30g/L), edema and hyperlipidemia.

Treatment: Glucocorticoids or combined immunosuppressive agents (cyclophosphamide, cyclosporine A, mycophenolate mofetil, etc.).

Lupus nephritis: It refers to systemic lupus erythematosus complicated by kidney damage. It has varying clinical manifestations, such as hematuria, tubular urine, persistent proteinuria or decreased renal function.

Treatment: Oral glucocorticoid therapy is the main treatment. If it is necessary, glucocorticoid pulse therapy or other immunosuppressive agents should be added.

Adrenal crisis: Acute reduction of adrenal cortex function induced by infection, trauma and other stress conditions or withdrawal of hormones. It leads to high fever, drop in blood pressure and so on. 

Treatment: Intravenous infusion of glucocorticoid (hydrocortisone), correction of dehydration and electrolyte disturbances and treatment of hypoglycemia.

Systemic lupus erythematosus: It is an autoimmune-mediated diffuse connective tissue disease characterized by immune inflammation.

Treatment: For mild, use no or small doses glucocorticoids. For medium, glucocorticoids + other immunosuppressive agents (cyclophosphamide or mycophenolate mofetil). For severe conditions, it is required large doses of glucocorticoids + other immunosuppressive agents. If it is necessary pulse treatment, methylprednisolone can be used.

Bronchial asthma: Asthma is a chronic airway inflammatory disease involving a variety of cells and cellular components.

Treatment: Inhaled glucocorticosteroids (ICS) are the first choice for long-term treatment of asthma. For chronic severe persistent asthma that cannot be controlled by high-dose ICS + LABA (Long-acting beta-agonists, such as formoterol.), low-dose oral glucocorticoid maintenance therapy can be added. Generally use a short half-life glucocorticoids (such as prednisone.), and take it in the morning. 

Idiopathic pulmonary fibrosis (IPF): It is a chronic, progressive and fibrotic interstitial pneumonia of unknown etiology. The median survival time from diagnosis is only 2 to 3 years.

Treatment: Anti-fibrosis agents pirfenidone and nintedanib can delay the decline of pulmonary function in patients with IPF. Patients with acute exacerbations should be treated with glucocorticoids as appropriate and avoiding glucocorticoids in the stable phase is beneficial to prolong the natural progress of the disease.

Ulcerative colitis (UC): Inflammatory bowel disease refers specifically to inflammatory bowel disease of unknown etiology, including ulcerative colitis and Crohn's disease. The cause is unknown and there is no cure for the time being. The lesions of UC were distributed continuously.

Treatment: For mild, use aminosalicylic acid preparations (such as mesalazine). For moderate, adequate aminosalicylic acid preparations are not well controlled and switch to glucocorticoid therapy. Thiopurine drugs can be used for glucocorticoid-ineffective or dependent patients. If the above treatments are ineffective, it should consider using infliximab.

Crohn's disease: Crohn's disease is also an inflammatory bowel disease of unknown etiology and the lesions are distributed in segments.

Treatment: For mild, use aminosalicylic acid preparations (such as mesalazine). For moderate to severe, use glucocorticoid. For those who fail to treat glucocorticoids or sulfa drugs, switch to or add azathioprine, cyclosporine and other immunosuppressive agents Agent. If the above treatments are ineffective, consider using infliximab.

Ankylosing spondylitis: It is a chronic inflammatory disease that mainly affects the sacroiliac joints, spine, paraspinal soft tissues and peripheral joints. It may be accompanied by extra-articular manifestations. In severe cases, spinal deformity and rigidity can occur.

Treatment: First using the drugs  to improve symptoms and disease progress, such as NSAIDs, sulfasalazine and anti-TNFα antagonists. Systemic corticosteroid therapy is generally not recommended. Glucocorticoids are usually used as local adjuvant drugs to improve Symptoms (such as injection into the joint cavity).

Rheumatoid arthritis: It is an autoimmune disease with erosive arthritis as the main clinical manifestation. It can occur at any age.

Treatment: The first choice is methotrexate alone. If it does not achieve treatment effect, it combined with leflunomide, sulfasalazine, and tocilizumab. Patients with moderate/high disease activity, combined with glucocorticoid therapy to quickly control symptoms.

👉When taking glucocorticoids for a long time, calcium and active vitamin D should be supplemented regularly to prevent osteoporosis and femoral head necrosis.

👉Patients with long-term use of glucocorticoids should check their weight, blood pressure, blood lipids, blood sugar, electrolytes, growth and development regularly.

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