Fludrocortisone (also called
9α-Flouocortisol) is a synthetic
corticosteroidCorticosteroids are a class of steroid hormones that are produced in the adrenal cortex. Corticosteroids are involved in a wide range of physiologic systems such as stress response, immune response and regulation of inflammation, carbohydrate metabolism, protein catabolism, blood electrolyte...
with moderate
glucocorticoidGlucocorticoids are a class of steroid hormones that bind to the glucocorticoid receptor , which is present in almost every vertebrate animal cell...
potency and much greater
mineralocorticoidMineralocorticoids are a class of steroid hormones characterised by their similarity to aldosterone and their influence on salt and water balance.-Physiology:...
potency.
The brand name in the U.S. is
Florinef.
It has been used in the treatment of cerebral salt wasting.
It is used primarily to replace the missing hormone
aldosteroneAldosterone is a hormone that increases the reabsorption of sodium and water and the release of potassium in the kidneys. This increases blood volume and, therefore, increases blood pressure. Many drugs, such as spironolactone, lower blood pressure by blocking the aldosterone receptor...
in various forms of
adrenal insufficiencyAdrenal insufficiency is a condition in which the adrenal glands, located above the kidneys, do not produce adequate amounts of steroid hormones , primarily cortisol, but may also include impaired aldosterone production which regulates sodium, potassium and water retention...
such as
Addison's diseaseAddison's disease is a rare endocrine disorder in which the adrenal glands do not produce enough steroid hormones...
and the classic salt wasting (21-hydroxylase deficiency) form of
congenital adrenal hyperplasiaCongenital adrenal hyperplasia refers to any of several autosomal recessive diseases resulting from mutations of genes for enzymes mediating the biochemical steps of production of cortisol from cholesterol by the adrenal glands ....
.
It is the first line of treatment for
orthostatic intoleranceOrthostatic intolerance is a subcategory of dysautonomia, a disorder of the autonomic nervous system occurring when an individual stands up....
as well.
It is also a confirmation test for diagnosing Conns Syndrome (Aldosterone producing-Adrenal adenoma), the fludrocortisone suppression test.
Fludrocortisone (also called
9α-Flouocortisol) is a synthetic
corticosteroidCorticosteroids are a class of steroid hormones that are produced in the adrenal cortex. Corticosteroids are involved in a wide range of physiologic systems such as stress response, immune response and regulation of inflammation, carbohydrate metabolism, protein catabolism, blood electrolyte...
with moderate
glucocorticoidGlucocorticoids are a class of steroid hormones that bind to the glucocorticoid receptor , which is present in almost every vertebrate animal cell...
potency and much greater
mineralocorticoidMineralocorticoids are a class of steroid hormones characterised by their similarity to aldosterone and their influence on salt and water balance.-Physiology:...
potency.
The brand name in the U.S. is
Florinef.
Uses
It has been used in the treatment of cerebral salt wasting.
It is used primarily to replace the missing hormone
aldosteroneAldosterone is a hormone that increases the reabsorption of sodium and water and the release of potassium in the kidneys. This increases blood volume and, therefore, increases blood pressure. Many drugs, such as spironolactone, lower blood pressure by blocking the aldosterone receptor...
in various forms of
adrenal insufficiencyAdrenal insufficiency is a condition in which the adrenal glands, located above the kidneys, do not produce adequate amounts of steroid hormones , primarily cortisol, but may also include impaired aldosterone production which regulates sodium, potassium and water retention...
such as
Addison's diseaseAddison's disease is a rare endocrine disorder in which the adrenal glands do not produce enough steroid hormones...
and the classic salt wasting (21-hydroxylase deficiency) form of
congenital adrenal hyperplasiaCongenital adrenal hyperplasia refers to any of several autosomal recessive diseases resulting from mutations of genes for enzymes mediating the biochemical steps of production of cortisol from cholesterol by the adrenal glands ....
.
It is the first line of treatment for
orthostatic intoleranceOrthostatic intolerance is a subcategory of dysautonomia, a disorder of the autonomic nervous system occurring when an individual stands up....
as well.
It is also a confirmation test for diagnosing Conns Syndrome (Aldosterone producing-Adrenal adenoma), the fludrocortisone suppression test. Loading the patient with fludrocortisone would suppress serum aldosterone level in a normal patient, whereas the level will not be altered in a Conns patient.
Dosing
It is available in 0.1 mg tablets. Typical daily doses for mineralocorticoid replacement are between 0.05 mg - 0.2 mg. Renin plasma, sodium, and potassium is checked through blood tests in order to verify that the correct dosage is reached.
Chemical properties
Chemically, its structure is identical to cortisone except for the substitution of fluorine in place of one hydrogen. Fluorine is a good
bioisostereIn medicinal chemistry, bioisosteres are substituents or groups with similar physical or chemical properties that impart similar biological properties to a chemical compound. In drug design, the purpose of exchanging one bioisostere for another is to enhance the desired biological or physical...
for hydrogen because it is similar in size. The major difference is in its
electronegativityElectronegativity, symbol χ, is a chemical property that describes the ability of an atom to attract electrons towards itself in a covalent bond. An atom's electronegativity is affected by both its atomic weight and the distance that its valence electrons reside from the charged nucleus...
.
Side Effects
- Sodium and water retention
- Swelling due to fluid retention (edema
Edema or oedema , formerly known as dropsy or hydropsy, is an abnormal accumulation of fluid beneath the skin, or in one or more cavities of the body...
)
- High blood pressure (hypertension
Hypertension is a chronic medical condition in which the blood pressure is elevated. It is also referred to as high blood pressure or shortened to HT, HTN or HPN. The word "hypertension", by itself, normally refers to systemic, arterial hypertension.Hypertension can be classified as either...
)
- Headache
- Low blood potassium level (hypokalemia
Hypokalemia Hypokalaemia refers to the condition in which the concentration of potassium in the blood is low. The prefix hypo- means low...
)
- Muscle weakness
- Fatigue
- Increased susceptibility to infection
- Impaired wound healing
- Increased sweating
- Increased hair growth (hirsutism
Hirsutism is excessive and increased hair growth on female humans in locations where the occurrence of terminal hair normally is minimal or absent. For example, a beard, or chest hair. It refers to a male pattern of body hair and it is therefore primarily of cosmetic and psychological concern...
)
- Thinning of skin and stretch marks
- Disturbances of the gut such as indigestion (dyspepsia
Dyspepsia , popularly known as indigestion, meaning hard or difficult digestion, is a medical condition characterized by chronic or recurrent pain in the upper abdomen, upper abdominal fullness and feeling full earlier than expected when eating. It can be accompanied by bloating, belching, nausea...
), distention of the abdomen and ulceration (peptic ulcerA peptic ulcer, also known as ulcus pepticum, PUD or peptic ulcer disease, is an ulcer of an area of the gastrointestinal tract that is usually acidic and thus extremely painful...
)
- Decreased bone density and increased risk of fractures of the bones
- Difficulty in sleeping (insomnia
Insomnia is a symptom of any of several sleep disorders, characterized by persistent difficulty falling asleep or staying asleep despite the opportunity. Insomnia is a symptom, not a stand-alone diagnosis or a disease. By definition, insomnia is "difficulty initiating or maintaining sleep, or both"...
)
- Depression
- Weight gain
- Raised blood sugar level
- Changes to the menstrual cycle
- Partial loss of vision due to opacity in the lens of the eye (cataracts)
- Raised pressure in the eye (glaucoma
Glaucoma is a group of diseases that affect the optic nerve and involves a loss of retinal ganglion cells in a characteristic pattern. It is a type of optic neuropathy. Raised intraocular pressure is a significant risk factor for developing glaucoma...
)
- Increased pressure in the skull (intracranial pressure
Intracranial pressure is the pressure in the cranium and thus in the brain tissue and cerebrospinal fluid ; this pressure is exerted on the brain's intracranial blood circulation vessels. ICP is maintained in a tight normal range dynamically, through the production and absorption of CSF and...
)