Fludrocortisone

Fludrocortisone

Fludrocortisone
Systematic (IUPAC) name
9-fluoro-11,17-dihydroxy-17- (2-hydroxyacetyl)- 10,13-dimethyl- 1,2,6,7,8,9,10,11,12, 13,14,15,16,17- tetradecahydrocyclopenta[a]phenanthren-3-one
Clinical data
AHFS/Drugs.com
Pregnancy
category
  • C
Legal status
Routes of
administration
Oral
Pharmacokinetic data
Protein binding High
Metabolism Hepatic
Biological half-life 3.5 hours
Identifiers
CAS Registry Number  Y
ATC code H02
PubChem CID:
IUPHAR/BPS
DrugBank  Y
ChemSpider  Y
UNII  Y
KEGG  Y
ChEBI  Y
ChEMBL  N
Chemical data
Formula C21H29FO5
Molecular mass 380.45 g/mol
 N   

Fludrocortisone (also called 9α-fluorocortisol or 9α-fluorohydrocortisone) is a synthetic health system.[1]

Contents

  • Medical uses 1
  • Side effects 2
  • Dosing 3
  • Chemical properties 4
  • References 5

Medical uses

Fludrocortisone has been used in the treatment of cerebral salt wasting syndrome.[2] It is used primarily to replace the missing hormone aldosterone in various forms of adrenal insufficiency such as Addison's disease and the classic salt wasting (21-hydroxylase deficiency) form of congenital adrenal hyperplasia. Due to its effects on increasing Na+ levels, and therefore blood volume, fludrocortisone is the first line of treatment for orthostatic intolerance and Postural Orthostatic Tachycardia Syndrome (POTS).[3] It can be used to treat low blood pressure.

Fludrocortisone is also a confirmation test for diagnosing Conn's 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.

Side effects

  • Sodium and water retention
  • Swelling due to fluid retention (edema)
  • High blood pressure (hypertension)
  • Headache
  • Low blood potassium level (hypokalemia)
  • Muscle weakness
  • Fatigue
  • Increased susceptibility to infection
  • Impaired wound healing
  • Increased sweating
  • Increased hair growth (hirsutism)
  • Thinning of skin and stretch marks
  • Disturbances of the gut such as indigestion (dyspepsia), distention of the abdomen and ulceration (peptic ulcer)
  • Decreased bone density and increased risk of fractures of the bones
  • Difficulty in sleeping (insomnia)
  • 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)
  • Increased pressure in the skull (intracranial pressure)

Dosing

Renin plasma, sodium, and potassium is checked through blood tests in order to verify that the correct dosage is reached.

Chemical properties

Chemically, fludrocortisone is identical to cortisol except for the substitution of fluorine in place of one hydrogen. Fluorine is a good bioisostere for hydrogen because it is similar in size. The major difference is in its electronegativity.

References

  1. ^ "WHO Model List of EssentialMedicines" (PDF). World Health Organization. October 2013. Retrieved 22 April 2014. 
  2. ^ Taplin CE, Cowell CT, Silink M, Ambler GR (December 2006). "Fludrocortisone therapy in cerebral salt wasting". Pediatrics 118 (6): e1904–8.  
  3. ^ Freitas J, Santos R, Azevedo E, Costa O, Carvalho M and Falcão de Freitas A (2000). "Clinical improvement in patients with orthostatic intolerance after treatment with bisoprolol and fludrocortisone". Clinical Autonomic Research 10 (5): 293–299.