Absorption, Distribution and Excretion
Topical corticosteroids, after absorption through the skin, follow a similar pharmacokinetic pathway to systemically administered corticosteroids. Topical corticosteroids can be absorbed from normal, intact skin. They are primarily metabolized in the liver and then excreted by the kidneys. Some topical corticosteroids and their metabolites are also excreted via bile. Topical corticosteroids can be absorbed from normal, intact skin. Skin inflammation and/or other diseases can increase percutaneous absorption. …Topical corticosteroids, after absorption through the skin, follow a similar pharmacokinetic pathway to systemically administered corticosteroids. The degree of binding of corticosteroids to plasma proteins varies. They are primarily metabolized in the liver and then excreted by the kidneys. Some topical corticosteroids and their metabolites are also excreted via bile. /Topical Corticosteroids/

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Metabolism/Metabolites
Primarily metabolized in the liver
/Topical Corticosteroids/Primarily metabolized in the liver and then excreted via the kidneys. Some topical corticosteroids and their metabolites are also excreted via bile. /Topical Corticosteroids/

Effects During Pregnancy and Lactation
◉ Overview of Medication Use During Lactation
Flurandino has not been studied during lactation. Since only large-area application of potent corticosteroids is likely to have 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 advisable 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
Topical application of a corticosteroid with high mineralocorticoid activity (isofluprednisolone acetate) to the mother's nipple resulted in QT interval prolongation, Cushing's syndrome-like symptoms, severe hypertension, growth retardation, and electrolyte disturbances in her 2-month-old breastfed infant. The mother had been using the cream to treat nipple pain since the infant's birth.
◉ Effects on Lactation and Breast Milk
No relevant published information was found as of the revision date.

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Protein Binding
The degree of binding of corticosteroids to plasma proteins varies.

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Interactions
The effect of glucocorticoids on oral anticoagulation therapy varies from person to person. It has been reported that concomitant use of glucocorticoids may enhance or diminish the efficacy of oral anticoagulants. Patients taking both glucocorticoids and oral anticoagulants should be monitored (e.g., using coagulation indicators) to maintain the desired anticoagulant effect. /Corticosteroids/
Because corticosteroids suppress antibody responses, these medications may lead to a weakened response to toxoids and live or inactivated vaccines. Furthermore, corticosteroids may enhance the replication of microorganisms contained in some live attenuated vaccines, and supraphysiological doses of corticosteroids can exacerbate neurological responses induced by certain vaccines. Routine vaccinations or toxoid administration should generally be postponed until corticosteroid treatment has been discontinued. Live virus vaccines or live attenuated vaccines, including smallpox vaccines, are contraindicated in patients receiving immunosuppressive doses of glucocorticoids. Additionally, inactivated vaccines may not elicit the expected serum antibody response in these patients. The Advisory Committee on Immunization Practice (ACIP) of the U.S. Public Health Service and the American Academy of Family Physicians (AAFP) state that live virus vaccination is generally not a contraindication for patients receiving short-term (less than 2 weeks), low- to moderate-dose corticosteroid treatment; it is also not a contraindication for patients receiving long-term every-other-day corticosteroid treatment (using short-acting formulations) or maintenance physiological doses (replacement therapy); and it is equally applicable for patients receiving topical, ocular, intra-articular, intra-bursal, or intratendinous injections of corticosteroids. If a patient receiving corticosteroid treatment must be vaccinated, serological testing may be required to ensure an adequate antibody response, and additional vaccination or toxoid administration may be necessary. Immunization may also be performed for patients receiving non-immunosuppressive doses of glucocorticoids or receiving glucocorticoid replacement therapy (e.g., for Addison's disease). /Corticosteroids/ Potassium-depleting diuretics (e.g., thiazide diuretics, furosemide, ethacrynic acid) and other potassium-depleting drugs, such as amphotericin B, may enhance the potassium-depleting effects of glucocorticoids. Patients receiving glucocorticoids and potassium-depleting drugs should have their serum potassium levels closely monitored. /Corticosteroids/
Concomitant use of ulcer-inducing drugs such as indomethacin during corticosteroid treatment may increase the risk of gastrointestinal ulcers. Aspirin should be used with caution in patients with hypoprothrombinemia when combined with glucocorticoids. Although combined treatment with salicylates and corticosteroids does not appear to increase the incidence or severity of gastrointestinal ulcers, this possibility should still be considered. /Corticosteroids/

: Setaluri V, Clark AR, Feldman SR. Transmittance properties of flurandrenolide tape for psoriasis: helpful adjunct to phototherapy. J Cutan Med Surg. 2000 Oct;4(4):196-8. PubMed PMID: 11231197.

Therapeutic Uses
Synthetic corticosteroids; Topical corticosteroids. Low to moderate potency topical corticosteroids are indicated for the treatment of skin conditions that respond to corticosteroids, such as: mild to moderate atopic dermatitis; contact dermatitis; mild nummular dermatitis; seborrheic dermatitis (face and skin folds); other mild to moderate dermatitis; other mild to moderate inflammatory skin conditions; chafing; lichen planus (face and skin folds); discoid lupus erythematosus (face and skin folds); polymorphic light eruption; anogenital pruritus; senile pruritus; psoriasis (face and skin folds); xerosis (inflammatory phase). Occlusive dressings may also be necessary for chronic or severe lichen simplex, psoriasis, eczema, atopic dermatitis, or chronic hand eczema. For conditions such as discoid lupus erythematosus, lichen planus, annular granuloma, psoriatic plaques, and psoriasis affecting the palms, soles, elbows, or knees, more potent topical corticosteroids and/or occlusive dressings may be required. /Corticosteroids (Topical); Included in the US product label/
Fluranolol acts similarly to other topical corticosteroids to relieve the inflammatory presentation of corticosteroid-responsive skin diseases.
Medications (Veterinary): Glucocorticoids have significant effects on almost all cell types and organ systems, particularly immune and inflammatory activity. Depending on the selected dose, glucocorticoids can be used for anti-inflammatory or immunosuppressive therapy. Glucocorticoids are used to treat allergic dermatitis, contact dermatitis, immune-mediated diseases (e.g., pemphigus, bullous pemphigoid, lupus erythematosus), and tumors (e.g., mast cell tumor, lymphoma). …They can be administered orally, intravenously, intramuscularly, or subcutaneously. /Glucocorticoids/

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Drug Warnings
Veterinarians: Avoid covering more than 5-10% of the body surface area, especially in pregnant animals.
The following adverse reactions may be more common when using occlusive dressings: maceration, secondary infection, skin atrophy, cyanosis. /Topical Corticosteroids/
The following local adverse reactions are uncommon when using topical corticosteroids, but may be more common when using other medications. The following reactions may occur when using occlusive dressings. These reactions are listed in roughly decreasing order of frequency: burning, itching, irritation, dryness, folliculitis, hirsutism, acneiform rash, hypopigmentation, perioral dermatitis, allergic contact dermatitis. /Topical Corticosteroids/
Because children have a larger body surface area to body weight ratio, they may be more prone to hypothalamic-pituitary-adrenal (HPA) axis suppression and Cushing's syndrome caused by topical corticosteroids than adult patients. Reports have indicated that pediatric patients receiving topical corticosteroids may experience hypothalamic-pituitary-adrenal (HPA) axis suppression, Cushing's syndrome, and intracranial hypertension. Manifestations of adrenal suppression in children include linear growth retardation, delayed weight gain, low plasma cortisol levels, and unresponsiveness to adrenocorticotropic hormone (ACTH) stimulation. Manifestations of intracranial hypertension include intracranial bulging, fontanelle, headache, and bilateral papilledema. The use of topical corticosteroids in pediatric patients should be limited to the minimum dose compatible with an effective treatment regimen. Prolonged use of corticosteroids may interfere with growth and development in pediatric patients. /Topical Corticosteroids/
For more complete data on drug warnings for fluraninolide (36 total), please visit the HSDB record page.

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Pharmacodynamics
Fluraninolide exerts its therapeutic effect primarily through its anti-inflammatory, antipruritic, and vasoconstrictive effects.

C24H33FO6

436.52

436.226

1524-88-5

1524-88-5 (free);2802-11-1 (acetate);

15209

Crystals from acetone + hexane
WHITE TO OFF-WHITE, FLUFFY CRYSTALLINE POWDER

1.31g/cm3

578.7ºC at 760mmHg

209 - 219ºC

303.8ºC

8.35E-16mmHg at 25°C

1.572

2.498

2

7

2

31

868

9

C[C@@]12[C@@]3(C(CO)=O)[C@@](OC(C)(O3)C)([H])C[C@@]1([H])[C@]4([H])C[C@H](F)C5=CC(CC[C@]5(C)[C@@]4([H])[C@@H](O)C2)=O

POPFMWWJOGLOIF-XWCQMRHXSA-N

InChI=1S/C24H33FO6/c1-21(2)30-19-9-14-13-8-16(25)15-7-12(27)5-6-22(15,3)20(13)17(28)10-23(14,4)24(19,31-21)18(29)11-26/h7,13-14,16-17,19-20,26,28H,5-6,8-11H2,1-4H3/t13-,14-,16-,17-,19+,20+,22-,23-,24+/m0/s1

(1S,2S,4R,8S,9S,11S,12S,13R,19S)-19-fluoro-11-hydroxy-8-(2-hydroxyacetyl)-6,6,9,13-tetramethyl-5,7-dioxapentacyclo[10.8.0.02,9.04,8.013,18]icos-17-en-16-one

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 (~229.09 mM)

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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