Pivalone Compositum
Pivalone Compositum Uses, Dosage, Side Effects, Food Interaction and all others data.
Pivalone Compositum is a 21-thiol derivative of hydrocortisone classified as a class A corticosteroid. It is a synthetic steroid with topical anti-inflammatory properties without the systemic glucocorticoid and mineralocorticoid activities and toxicity.
Pivalone Compositum presents the characteristic of local action which reduces significantly the side effects of systemic glucocorticoids. Reports have demonstrated that gastrointestinal administration of tixocortol generates a decrease in abdominal pain, bleeding, and frequency of stools which resulted in an amelioration in the malabsorption laboratory tests. All the effects were independent of suppression of the pituitary-adrenal axis, which was shown by the absence of significant depression of cortisol. Administration of tixocortol as a nasal spray has been shown to respect nasal drainage by the ciliary beats of the pituitary mucosa. The actions of tixocortol have no effect on leukocyte count, blood glucose level, sodium urinary excretion, and immunosupressive activity on lymphocytes.
| Trade Name | Pivalone Compositum |
| Generic | Tixocortol |
| Tixocortol Other Names | Tixocortol |
| Type | |
| Formula | C21H30O4S |
| Weight | Average: 378.53 Monoisotopic: 378.18648062 |
| Protein binding | The presence of the C-17 in the corticosteroids is a protein binding site. |
| Groups | Approved, Withdrawn |
| Therapeutic Class | |
| Manufacturer | F UHLMANN-EYRAUD |
| Available Country | Switzerland |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Pivalone Compositum is a corticosteroid used for the symptomatic treatment of rhinitis, pharyngitis, and ulcerative colitis.
Pivalone Compositum is indicated for the treatment of rhinitis as a nasal suspension or aerosol. It is also used in the form of lozenges for the treatment of pharyngitis and in the form of enemas or rectal solution for the treatment of ulcerative colitis. Pivalone Compositum can be used orally in a suspension or powder for the treatment of inflammatory conditions. It is also the substance used for the screening of contact allergies to class A steroids.
How Pivalone Compositum works
The mechanism of action of tixocortol is similar to other corticosteroids regarding the binding sites and prostaglandin synthesis but the local properties of tixocortol are given by the immediate liver metabolism and transformation withing red blood cells. All the immediate transformations of tixocortol classified it as part of the nonsystemic steroids.
Toxicity
Diverse studies performed on tixocortol proved that this drug is non-toxic and non-immunosupressive. This low toxicity and abscence of immuno supression gave tixocortol the potential to be a lead for topical or local anti-inflammatory treatments. Nevertheless, toxicortol is a potent cutaneous sensitizer, causing a local allergy.
Food Interaction
No interactions found.Volume of Distribution
Studies have shown that oral or intravenous administration of tixocortol presents a significantly larger volume of distribution compared to cortisol of 21.7 L/kg.
Elimination Route
The absorption of tixocortol is the same as in other steroids including hydrocortisone. Oral administration of tixocortol presents a 10-20% bioavailability with a significantly lower plasma Cmax than cortisol. The fast metabolism, larger volume of distribution and low bioavailability donates tixocortol with the absence of systemic activity.
Half Life
Pivalone Compositum presents a shorter half-life than cortisol.
Clearance
Studies have shown that oral or intravenous administration of tixocortol presents a significantly larger clearance rate compared to cortisol of 33.3 L h/kg.
Elimination Route
Pivalone Compositum has a rapid elimination after continuous metabolism. Urine analysis of oral administration of tixocortol demonstrate a complete lack of unchanged drug.
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