Absorption, Distribution and Excretion
Topical corticosteroids can be absorbed through intact, healthy skin. The extent of transdermal absorption of topical corticosteroids depends on a variety of factors, including excipients and the integrity of the epidermal barrier. Skin occlusion, inflammation, and/or other disease processes may also increase transdermal absorption. The degree of binding of corticosteroids to plasma proteins varies. They are primarily metabolized in the liver and excreted via the kidneys. A portion of topical corticosteroids and their metabolites are also excreted via bile. Pharmacokinetic studies in men using 0.25% Desmetryn cream (USP) showed a total excretion of 5.2% ± 2.9% in urine (4.1% ± 2.3%) and feces (1.1% ± 0.6%). Metabolism/Metabolites Primarily metabolized in the liver and then excreted via the kidneys.

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Biological half-life
Between the third and fifth days of the experiment, the half-life of the substance was 15 ± 2 hours (urine) and 17 ± 2 hours (feces).

Effects During Pregnancy and Lactation
◉ Overview of Medication Use During Lactation
No studies have been conducted on Desmetryn during lactation. Since only large-area application of potent corticosteroids has systemic effects on the mother, short-term topical application of corticosteroids is unlikely to pose a risk to the nursing infant through breast milk. However, it is a precautionary practice to use the least potent medication on the smallest possible area of skin. It is especially important to ensure that the infant's skin does not come into direct contact with the treated area. Only low-potency corticosteroids should be used on the nipple or areola, where the infant may ingest the medication directly through the skin. Only water-soluble creams or gels should be applied to the breast, as ointments may expose the infant to high concentrations of mineral oil through licking. If any topical corticosteroids are applied to the breast or nipple area, they should be thoroughly wiped off before breastfeeding.
◉ Effects on breastfed infants
A mother applied a topical corticosteroid (isofluprednisolone acetate) with high mineralocorticoid activity to her nipples, resulting in QT interval prolongation, Cushing's syndrome-like symptoms, severe hypertension, growth retardation, and electrolyte imbalance in her 2-month-old breastfed infant. The mother had been using the cream due to nipple pain since birth.
◉ Effects on lactation and breast milk
As of the revision date, no relevant published information was found.

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Protein binding
The degree of binding to plasma proteins varies.

[1]. Desoximetasone, From Wikipedia.

Desmetryn is a derivative of Desmetryn, with its 17α-hydroxyl group replaced by a hydrogen atom. It is a synthetic glucocorticoid with glucocorticoid activity, used to treat various skin conditions, including skin allergies and psoriasis, and has anti-inflammatory and antipruritic effects. It is an 11β-hydroxysteroid, 21-hydroxysteroid, glucocorticoid, 20-oxosteroid, fluorinated steroid, 3-oxo-Δ1,Δ4-steroid, and primary α-hydroxyketone. It is a topical anti-inflammatory glucocorticoid used to treat skin diseases, skin allergies, psoriasis, etc. Desmetryn is a glucocorticoid. The mechanism of action of Desmetryn is as a corticosteroid receptor agonist. Desmetryn is a synthetic glucocorticoid receptor agonist with metabolic, anti-inflammatory, and immunosuppressive activities. Desmetryn activates specific intracellular receptors that bind to specific sites on DNA, thereby altering gene transcription. This leads to the induction of anti-inflammatory protein synthesis and the inhibition of inflammatory mediator synthesis. Ultimately, this leads to an overall reduction in chronic inflammation and autoimmune responses. Desmetryn is indicated for the relief of inflammatory and pruritus symptoms in corticosteroid-sensitive dermatitis. A topical anti-inflammatory glucocorticoid used to treat skin diseases, skin allergies, psoriasis, etc. See also: Desmetryn; Nicotinamide (ingredient); Desmetryn; Hydroquinone; Retinoic acid (ingredient).

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Drug Indications
For the relief of inflammatory and pruritus symptoms in corticosteroid-sensitive dermatitis.
FDA Label

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Mechanism of Action
The anti-inflammatory mechanism of topical steroids in the treatment of corticosteroid-sensitive dermatitis is not fully understood. However, it is believed that the mechanism of action of corticosteroids is through inducing phospholipase A2 inhibitory proteins (collectively known as lipocortin). First, the drug binds to glucocorticoid receptors, then translocates to the cell nucleus and binds to DNA, leading to various gene activations and repressions. It is speculated that these proteins control the biosynthesis of potent inflammatory mediators such as prostaglandins and leukotrienes by inhibiting the release of their common precursor, arachidonic acid. Arachidonic acid is released from membrane phospholipids by phospholipase A2.

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Pharmacodynamics
Like other topical corticosteroids, Desmetryn has anti-inflammatory, antipruritic, and vasoconstrictive effects. The pharmacokinetic pathway of topical corticosteroids after absorption through the skin is similar to that of systemically administered corticosteroids. Desmetryn is a potent topical corticosteroid and should not be used with occlusive dressings. It is recommended that the course of treatment not exceed two consecutive weeks and that treatment be discontinued after achieving the desired therapeutic effect.

C22H29FO4

376.46

376.204

382-67-2

5311067

White to off-white solid powder

1.3±0.1 g/cm3

532.3±50.0 °C at 760 mmHg

217ºC

275.7±30.1 °C

0.0±3.2 mmHg at 25°C

1.574

2.2

2

5

2

27

757

8

C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@@]4([C@]3([C@H](C[C@@]2([C@H]1C(=O)CO)C)O)F)C

VWVSBHGCDBMOOT-IIEHVVJPSA-N

InChI=1S/C22H29FO4/c1-12-8-16-15-5-4-13-9-14(25)6-7-21(13,3)22(15,23)18(27)10-20(16,2)19(12)17(26)11-24/h6-7,9,12,15-16,18-19,24,27H,4-5,8,10-11H2,1-3H3/t12-,15+,16+,18+,19-,20+,21+,22+/m1/s1

(8S,9R,10S,11S,13S,14S,16R,17S)-9-fluoro-11-hydroxy-17-(2-hydroxyacetyl)-10,13,16-trimethyl-7,8,11,12,14,15,16,17-octahydro-6H-cyclopenta[a]phenanthren-3-one

A-41-304; A 41304; A 41-304

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ≥ 100 mg/mL (~265.63 mM)
H2O : ~0.14 mg/mL (~0.37 mM)

Solubility in Formulation 1: ≥ 2.5 mg/mL (6.64 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

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Solubility in Formulation 2: ≥ 2.5 mg/mL (6.64 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (6.64 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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 (Please use freshly prepared in vivo formulations for optimal results.)