What Is Fludrocortisone?

Fludrocortisone can inhibit the proliferation of connective tissue, reduce the permeability of capillaries and cell membranes, reduce inflammatory exudation, inhibit the formation and release of histamine and other inflammatory transmitters, and its anti-inflammatory effect is stronger than that of hydrocortisone 15 times or so. It is mainly mineralocorticoid. Although it has a certain glucocorticoid activity, there is no obvious glucocorticoid effect at the usual dose.

Chinese name: Fludrocortisone
Alias: Fludrocortisone acetate

Character: Tablets, ointments
Specifications: 0.1mg per tablet

Basic information of fludrocortisone

Chinese name: fluhydrocortisone

English name: fludrocortisone

English alias: Fludrocortone; Astonin-H; Alflorone; Fluorocortisone; Fluohydrocortisone;

CAS number: 127-31-1

Molecular formula: C ₂₁ H ₂₉ FO ₅

Molecular weight: 380.45000

Hydrocortisone (5 photos)

Exact mass: 380.20000

PSA: 94.83000

LogP: 1.87370

Physicochemical properties of hydrocortisone

Appearance and properties: white solid

Density: 1.3g / cm ³

Melting point: 208-212ºC

Boiling point: 575.1ºC at 760 mmHg Flash point: 301.6ºC

Refractive index: 1.563

Vapor pressure: 1.27E-15mmHg at 25 ° C ^[1]

Molecular structure data of fludrocortisone

1. Molar refractive index: 95.72

2. Molar volume (cm ³ / mol): 286.1

3. Isotonic specific volume (90.2K): 786.7

4. Surface tension (dyne / cm): 57.1

5. Polarizability (10-24cm ³ ): 37.94

Calculated Chemical Data for Fludrocortisone

1. Hydrophobic parameter calculation reference value (XlogP): None

2.Number of hydrogen bond donors: 33. Number of hydrogen bond acceptors: 6

4.Number of rotatable chemical bonds: 2

5.Number of tautomers: 15

6. Topological molecular polar surface area 94.8

7.Number of heavy atoms: 27

8.Surface charge: 0

9.Complexity: 734

10.Number of isotope atoms: 0

11. Determine the number of atomic stereocenters: 712. Uncertain number of atomic stereocenters: 0

13. Determine the number of chemical bond stereocenters: 0

14. Uncertain number of chemical bond stereocenters: 0

15. Number of covalent bond units: 1 ^[2]

Indications of fludrocortisone function

In the treatment of primary adrenal insufficiency, it can be used as an alternative treatment with glucocorticosteroids. For low renin low aldosterone syndrome and orthostatic hypotension caused by autonomic neuropathy. Because this product is easy to cause edema when taken internally, it is mostly used for external application (local application) to treat skin seborrheic eczema, contact dermatitis, and anal and vulvar itching.

Usage and dosage: 1. Alternative treatment: Adults take orally, 0.1 0.2mg per day, divided into 2 times. 2. Local skin application: 2 to 4 times a day. Adverse reactions and attention: In pregnancy, liver disease, myxedema, due to the long half-life of this product and prolonged action time, the dose can be appropriately reduced to prevent excessive sodium retention, edema, hypertension and hypokalemia. 2. Hydrocortisone acetate ointment: 2.5mg (10g) each.

Pharmacokinetics of Fludrocortisone

It has anti-inflammatory and anti-allergic effects. Can inhibit the proliferation of connective tissue, reduce the permeability of capillaries and cell membranes, reduce inflammatory exudation, inhibit the formation and release of histamine and other inflammatory transmitters, and its anti-inflammatory effect is about 15 times stronger than hydrocortisone. It is mainly mineralocorticoid. Although it has a certain glucocorticoid activity, there is no obvious glucocorticoid effect at the usual dose.

Fludrocortisone precautions

In pregnancy, liver disease, myxedema, due to the long half-life of this product and prolonged action time, the dose can be appropriately reduced to prevent excessive sodium retention, edema, hypertension and hypokalemia. During the medication can be given a low sodium and potassium diet. Specifications: 1. Tablets: 0.1mg per tablet, 2. Hydrocortisone acetate ointment: 2.5mg (10g) each.

Adaptation symptoms: In the treatment of primary adrenal insufficiency, it can be used together with glucocorticosteroids as an alternative treatment. For low renin low aldosterone syndrome and orthostatic hypotension caused by autonomic neuropathy. Because this product is easy to cause edema when taken internally, it is mostly used for external application (local application) to treat skin seborrheic eczema, contact dermatitis, and anal and vulvar itching.

Fludrocortisone dosage

Apply to affected area 2 to 4 times a day. Preparation and specifications: 10 g of hydrocortisone acetate ointment: 2.5 mg. Commonly used amount for adults: Addison syndrome, 0.1mg daily, combined with cortisone or hydrocortisone, if hypertension occurs, reduce to 0.05mg daily; congenital adrenal syndrome with loss of salt , 0.1 0.2mg daily, combined with cortisone or hydrocortisone. Apply ointment topically, 2 to 3 times a day. Preparations and specifications: Flucortisone acetate tablets 0.1mg. Hydrocortisone acetate ointment 10g: 2.5mg. Adults take orally, 0.1-0.2mg a day, divided into two doses. For topical skin application, 2-4 times a day. For allergic dermatitis, contact dermatitis, seborrheic dermatitis, eczema, neurodermatitis and other skin diseases.

Allergic dermatitis of fludrocortisone

Allergic dermatitis is an inflammation of the skin caused by many factors. There are many common causes of this disease, and the names of allergic reactions caused by different causative factors are different. Now we introduce two types of common allergic dermatitis. Cosmetic dermatitis The skin inflammation caused by cosmetics is called cosmetic dermatitis. Cosmetics have become indispensable in people's daily life. Some people often use some kind of cosmetics, and allergic reactions will occur once they are discontinued or re-used; others will have an allergic reaction after the first use; and others will react after exposure to sunlight. Contact dermatitis is an acute inflammation of the skin caused by contact of the skin or mucosal site with an external stimulating substance.

The reasons can be divided into two major categories: 1. Primary irritation: mainly caused by strong acids, strong bases, cantharidium and certain strong irritating or concentrated chemicals. This type is non-individually selective and has no incubation period. Anyone's contact can immediately cause acute skin inflammation. 2. Allergies (allergic reactions): This type is mainly delayed allergies (type vI allergies). It is caused by contact with a certain stimulating factor (allergen) on the skin and mucous membranes, and only a few people with specific allergies have the disease. The disease does not occur immediately after the first contact, and often the incubation period of 4-20 days (average 7 8 days) The body is first sensitized. If it is contacted again, dermatitis can occur in about 12 hours (generally no more than 72 hours). This type of allergic reaction is the most common in contact dermatitis.

Hydrocortisone contact dermatitis

Contact dermatitis is an inflammatory reaction of the skin and mucous membranes due to contact with external substances, such as chemical fiber clothing, cosmetics, drugs, and so on. Clinical features

Fludrocortisone In order to cause sharp edge damage at the contact site, the lighter is edema erythema, the heavier has pimples, leeches, or even large scars, and the more severe can have epidermal lysis and even necrosis. If the cause can be removed early and treated appropriately, it can be cured quickly, otherwise it may be transformed into eczema-like dermatitis.

Contact dermatitis is generally caused by allergies to external contact objects, so you should actively find the source of allergies and eliminate the allergic factors. Can take oral anti-histamine drugs such as ceritantin, cetirizine, diphenhydramine, cyproheptadin, etc., of which fludrocortisone is more effective. For external use Lanke skinning, citrus stone lotion. Do not scratch the affected area or wash it with hot water! Take care of yourself.

Clinical application of fludrocortisone

1. Replacement therapy: Complementary replacement therapy for acute and chronic adrenal insufficiency, anterior pituitary hypofunction, and subtotal adrenalectomy. Severe acute infection or inflammation. Severe acute infections. For bacterial severe acute infections, a sufficient amount of effective antibacterial drugs are applied. Compatible with GCS, using its anti-inflammatory and anti-toxic effects, can alleviate symptoms and help patients through the dangerous period. For viral infections, GCS is generally not used, and patients with chickenpox and shingles can exacerbate after use.

2, but for patients with severe hepatitis, mumps, measles and JE can relieve symptoms. Prevent sequelae of inflammation, meningitis, pericarditis, arthritis and burns. GCS can reduce scars and adhesions, and reduce inflammation sequelae. For iritis, keratitis, retinitis, in addition to the above-mentioned effects, it can still produce anti-inflammatory and analgesic effects.

3. Autoimmune and allergic diseases, autoimmune diseases: GCS can relieve symptoms of rheumatic fever, rheumatoid arthritis, systemic lupus erythematosus and other autoimmune diseases. Application to organ transplantation can suppress rejection. Allergic diseases: GCS can relieve symptoms of allergic diseases such as urticaria, hay fever, and allergic rhinitis. But it cannot be cured.

4. Treatment of shock: It has the best effect on toxic shock of infection. The second is anaphylactic shock, which is also effective for cardiogenic shock and hypovolemic shock. Hematological diseases: better effect on acute lymphocytic leukemia. Aplastic anemia, granulocytopenia, thrombocytopenia, allergic purpura can also be significantly relieved, but long-term high-dose medication is required.

5, skin diseases: for psoriasis, eczema, contact dermatitis, topical application, but for severe skin diseases such as pemphigus and exfoliative dermatitis need systemic administration. Malignant tumors: Malignant lymphoma, advanced breast cancer, and prostatic cancer are all effective.