Mechanism of effect
Fludrocortisone binds the mineralocorticoid receptor (aldosterone receptor). It is a potent mineralocorticoid with high glucocorticoid activity; promotes increased reabsorption of sodium and excretion of potassium from renal distal tubules
Pharmacodynamic
Fludrocortisone is a synthetic adrenocortical steroid possessing very potent mineralocorticoid properties and high glucocorticoid activity. It is indicated as partial replacement therapy for primary and secondary adrenocortical insufficiency in Addison’s disease and for the treatment of salt-losing adrenogenital syndrome
The physiologic action of fludrocortisone acetate is similar to that of hydrocortisone. However, the effects of fludrocortisone acetate, particularly on electrolyte balance, but also on carbohydrate metabolism, are considerably heightened and prolonged.
Mineralocorticoids act on the distal tubules of the kidney to enhance the reabsorption of sodium ions from the tubular fluid into the plasma; they increase the urinary excretion of both potassium and hydrogen ions.
Pharmacokinetics
Bioavailability: 100%
Peak plasma time: ≤1.7 hr
Distribution
Protein bound: 42%
Metabolism
Metabolized in liver
Elimination
Half-life: Plasma, 3.5 hr; biologic, 18-36 hr
Drug indications
Partial replacement therapy for primary and secondary adrenocortical insufficiency in Addison disease , congenital adrenal hyperplasia , Idiopathic orthostatic hypotensionDosage
• Addison's Disease
0.05 to 0.1 mg orally/24 hours (range 0.1 mg 3 times a week to 0.2 mg/day)
• Adrenogenital Syndrome
0.1 to 0.2 mg orally/24 hours
Drug contraindications
Systemic fungal infection , Documented hypersensitivity , Receipt of live or attenuated live vaccineSide effects
Headache , insomnia , vertigo , Depression , asthenia , Hypertension , Hyperglycemia , itching , diabetes mellitus , osteoporosis , cardiac failure , swelling , redness or flaking of treated skin , Irregular periods , nervousnessInteractions
Ergotamine-C , Rifampin , Phenytoin , Rifabutin , Ranolazine , Aldesleukin , Dofetilide , Hib vaccine , Grepafloxacin , Tisagenlecleucel , Axicabtagene ciloleucel , Hepatitis B Vaccine , Lorlatinib , Glycerol Phenylbutyrate , Meningococcal conjugate vaccine , Rabies Vaccine , sirukumabAlerts
1. Use with caution in diabetes mellitus, hypertension, hypothyroidism, electrolyte abnormalities, sodium and water retention, infections, immunizations, ocular herpes simplex, myasthenia gravis, peptic ulcer disease, psychosis, renal insufficiency
2. Thromboembolic disorders and myopathy may occur
3. Delayed wound healing is possible
4. Patients receiving corticosteroids should avoid chickenpox or measles-infected persons if unvaccinated
5. Latent tuberculosis may be reactivated (patients with positive tuberculin test should be monitored)
6. Some suggestion (not fully substantiated) of slightly increased cleft palate risk if corticosteroids are used in pregnancy
7. Prolonged corticosteroid use may result in elevated intraocular pressure, glaucoma, or cataracts and has been associated with development of Kaposi sarcoma
8. Use with caution If you have any of these health problems: A fungal infection or malaria infection in the brain, or If you have a herpes infection of the eye or nerve problems in the eye.
9. This medicine may lower how much natural steroid is in your body. If you have a fever, an infection, surgery, or you are hurt, talk with your doctor. You may need extra doses of oral steroids. These extra steroids will help your body deal with these stresses.
10. If you are 65 or older, use fludrocortisone with care. You could have more side effects.
11. This medicine may affect growth in children and teens in some cases. They may need regular growth checks
Points of recommendation
1. Take in the morning if taking once a day.
2. Take with or without food.
3. This medicine may cause weak bones (osteoporosis) with long-term use. Have blood work checked , a bone density test as you have been told by the doctor.
4. Have your eye pressure checked if you are on fludrocortisone for a long time.
5. If you have been taking this medicine for many weeks, talk with your doctor before stopping. You may want to slowly stop fludrocortisones .
6. This medicine may affect certain lab tests.
7. You may have more chance of getting an infection. Wash hands often. Stay away from people with infections, colds, or flu, chickenpox and measles.
8. Talk with your doctor before getting any vaccines. Use with this medicine may either raise the chance of an infection or make the vaccine not work as well.
9. If you have high blood sugar (diabetes), you will need to watch your blood sugar closely.
10. Talk with your doctor before you drink alcohol.
11. You may need to lower how much salt is in your diet and take extra potassium. Talk with your doctor.
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