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ADDIVET (fludrocortidone acetate)

Composition: ADDIVET: Fludrocortisone 0.2 mg. Excipient q.s.p 150 mg.

 

Indications for Use: Fludrocortisone is used in small animal medicine for the treatment of adrenocortical insufficiency (Addison's disease). It can also be used as adjunctive therapy in hyperkalaemia. Fludrocortisone acetate is a potent corticosteroid that possesses glucocorticoid and mineralocorticoid activity. It is approximately 10 to 15 times more potent as a glucocorticoid than hydrocortisone, but it is a much more potent mineralocorticoid (125 times more potent than hydrocortisone). It is only used clinically for its mineralocorticoid effects. The site of action of mineralocorticoids is the renal distal tubule where they increase sodium absorption. Mineralocorticoids also enhance the excretion of potassium and hydrogen ions.

Administration: Oral route (tablets).

 

Pharmacological properties and action: Fludrocortisone acetate is a potent corticosteroid that possesses glucocorticoid and mineralocorticoid activity. It is approximately 10 to 15 times more potent as a glucocorticoid than hydrocortisone, but it is a much more potent mineralocorticoid (125 times more potent than hydrocortisone). It is only used clinically for its mineralocorticoid effects. The site of action of mineralocorticoids is the renal distal tubule where they increase sodium absorption. Mineralocorticoids also enhance the excretion of potassium and hydrogen ions.
Fludrocortisone is a synthetic corticosteroid with anti-inflammatory and anti-allergic properties. Fludrocortisone is a mineralocorticoid and glucocorticoid receptor agonist that binds to cytoplasmic receptors, translocates to the nucleus, and subsequently initiates transcription of glucocorticoid-responsive genes, such as lipocortins, to inhibit phospholipase A2. This prevents the release of arachidonic acid, a precursor to prostaglandins and leukotrienes, both of which are important mediators in the proinflammatory response mechanism. In addition, this agent exerts its mineralocorticoid effect on the distal tubules and collecting ducts of the kidney by inducing permease, an enzyme that regulates Na + permeability in cells, thus enhancing Na + reabsorption and water retention, as well as increasing the excretion of K +, H +. Fludrocortisone is a C21 steroid, a 3-oxo-Delta(4) steroid, a 20-oxo steroid, a 21-hydroxy steroid, a fluorinated steroid, a mineralocorticoid, a 17 alpha-hydroxy steroid, and an 11 beta-hydroxy steroid. . It has a role as an adrenergic and anti-inflammatory agent. It derives from a hydride of a pregnane. Fludrocortisone is a synthetic mineralocorticoid used in conjunction with [hydrocortisone] to replace missing endogenous corticosteroids in patients with adrenal insufficiency. It is functionally similar to [aldosterone], the body's main endogenous mineralocorticoid, and is structurally analogous to [cortisol], differing only by a fluorine atom at position 9 of the steroid structure; this fluorination is believed to be crucial for the significant concentration of fludrocortisone. mineralocorticoid potency.

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