Fluocinolone 16,17-acetonide

452.49

452.49

200-668-5

0CD5FD6S2M

92339

DTXSID0040674

C29055

CRYSTALS FROM ACETONE & HEXANE|WHITE, CRYSTALLINE POWDER

C - Cardiovascular system|D - Dermatologicals|S - Sensory organs

2937210000

93.1

2.48

Solid

1.4±0.1 g/cm3

266 °C

578.5±50.0 °C at 760 mmHg

303.7±30.1 °C

1.577

soluble in water (partly), DMSO, alcohol, chloroform and methanol.

Refrigerator

LD50 oral in rat: > 4gm/kg

D +95° (chloroform)

ODORLESS

13.9None

13.9

199.7 Ų [M+H]+ [CCS Type: TW, Method: calibrated with polyalanine and drug standards]

DECOMP IN HEAT

NONH for all modes of transport

3

36/37/38-40-20/21/22

26-36-22

TU3830000

Xi,Xn

STABLE IN LIGHT

P261-P305 + P351 + P338

H315-H319-H335

|Warning|H315 (40.21%): Causes skin irritation [Warning Skin corrosion/irritation]|P201, P202, P261, P264, P271, P280, P281, P302+P352, P304+P340, P305+P351+P338, P308+P313, P312, P321, P332+P313, P337+P313, P362, P403+P233, P405, and P501|Aggregated GHS information provided by 97 companies from 7 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Studies to determine the carcinogenic and its effect in fertility have not been performed. It is important to consider that several corticosteroids have been shown to present genotoxic potential but fluocinolone acetonide was shown to not be genotoxic in the Ames test and mouse lymphoma TK assay.

REVERSAL OF CORTICOSTEROID-INDUCED IMPAIRMENT OF WOUND HEALING HAS BEEN REPORTED AFTER TOPICAL APPLICATION OF VITAMIN /VITAMIN A/. /CORTICOSTEROIDS/

This pharmacokinetic parameter is not relevant as the systemic absorption of fluocinolone acetonide is very minimal.

Fluocinolone acetonide has been used extensively in different medical areas. -In dermatology, it is extensively used for the relief of inflammatory dermatosis, dermatitis, psoriasis, hypertrophic tissues, keloid tissues and atopic dermatitis. -It has been used in shampoo products as a low to medium potency corticosteroid for the treatment of seborrheic dermatitis of the scalp. -In ear drops, it is used as a low to medium potency corticosteroid for the treatment of chronic eczematous external otitis in adults and pediatric patients 2 years and older. -As an intravitreal implant, it is indicated for the treatment of diabetic macular edema with patients that have been previously treated with a course of corticosteroids and no clinically significant rise in intraocular pressure. -Fluocinolone acetonide was announced on October 15, 2018 to be FDA approved for the treatment of chronic non-infectious uveitis affecting the posterior segment of the eye. -Some reports have indicated the use of fluocinolone acetonide as a vasoprotective agent and for its use in the treatment of first-degree hemorrhoids.|FDA Label|Treatment of dermatitis and eczema|Treatment of diabetic macular oedema|Treatment of chronic non-infectious uveitis

Glucocorticoids, Synthetic; Glucocorticoids, Topical|WITH EXCEPTION OF SUBSTITUTION THERAPY, USE OF CORTICOSTEROIDS & THEIR CONGENERS IN DISEASE IS EMPIRICAL. ...FOR ANY DISEASE, IN ANY PT, APPROPRIATE DOSE TO ACHIEVE GIVEN THERAPEUTIC EFFECT MUST BE DETERMINED BY TRIAL & ERROR & MUST BE REEVALUATED FROM TIME TO TIME AS STAGE & ACTIVITY OF DISEASE ALTER... /CORTICOSTEROID/|GLUCOCORTICOID WITH POTENT ANTI-INFLAMMATORY & METABOLIC ACTIONS & NEGLIGIBLE MINERALOCORTICOID ACTIONS.|IT IS EMPLOYED TOPICALLY IN TREATMENT OF VARIOUS DERMATOSES. IN RESISTANT NUMMULAR DERMATITIS, PSORIASIS, OR CHRONIC NEURODERMATITIS USUALLY USED UNDER OCCLUSIVE DRESSINGS.|For more Therapeutic Uses (Complete) data for FLUOCINOLONE ACETONIDE (7 total), please visit the HSDB record page.

...AS CORTICOSTEROID THERAPY IS PROLONGED OVER PERIODS OF MO, & TO EXTENT THAT DOSE EXCEEDS EQUIV OF SUBSTITUTION THERAPY, INCIDENCE OF DISABLING & POTENTIALLY LETHAL EFFECTS INCR; EXCEPT IN ADRENAL INSUFFICIENCY, ADMIN...IS NEITHER ETIOLOGICAL OR CURATIVE THERAPY BUT ONLY PALLIATIVE...ANTI-INFLAMMATORY... /CORTICOSTEROIDS/|EVEN IN INSTANCES IN WHICH NEARLY WHOLE BODY HAS BEEN COVERED BY CREAM CONTAINING CORTICOID, EVIDENCES OR SYSTEMIC SIDE EFFECTS ARE RARE. ... TOPICAL FLUOCINOLONE IS CONTRAINDICATED IN PRESENCE OF TUBERCULOSIS, FUNGAL INFECTIONS, & MOST VIRAL LESIONS OF SKIN (VACCINIA, VARICELLA, HERPES SIMPLEX, ETC).|...CAUTION SHOULD BE EXERCISED IF FLUORINATED PREPN ARE USED ON FACE OR OTHER COSMETICALLY IMPORTANT AREAS, SINCE PARADOXICAL SKIN ERUPTIONS MAY OCCUR WITH LONG-TERM USE.|VET: SOLN IN PROPYLENE GLYCOL USUALLY PRODUCES FAR MORE THAN "TRANSIENT STINGING SENSATION" DESCRIBED BY MFR & SHOULD BE AVOIDED ESP ON RAW OR DENUDED AREAS.|For more Drug Warnings (Complete) data for FLUOCINOLONE ACETONIDE (7 total), please visit the HSDB record page.

Fluocinolone acetonide is a synthetic anti-inflammatory corticosteroid and thus, the effect of its interaction with the body produces vasoconstriction and suppression of membrane permeability, mitotic activity, immune response and release of inflammatory mediators. For its ophthalmic indications, fluocinolone acetonide is administered as intravitreal micro-insert. This preparation was observed in clinical trials to reduce the recurrence of uveitis flares by 2 fold when compared with the non treated patients even after six months after initial administration. As well the intraocular pressure seemed to increase slightly with the presence of the fluocinolone implant but it is important to monitor intraocular pressure.

Substances that reduce or suppress INFLAMMATION. (See all compounds classified as Anti-Inflammatory Agents.)|A group of CORTICOSTEROIDS that affect carbohydrate metabolism (GLUCONEOGENESIS, liver glycogen deposition, elevation of BLOOD SUGAR), inhibit ADRENOCORTICOTROPIC HORMONE secretion, and possess pronounced anti-inflammatory activity. They also play a role in fat and protein metabolism, maintenance of arterial blood pressure, alteration of the connective tissue response to injury, reduction in the number of circulating lymphocytes, and functioning of the central nervous system. (See all compounds classified as Glucocorticoids.)

When administered as an eye implant, fluocinolone acetonide presents a sustained delivery for even 12 months in which there can be observed a sustained release. The concentration of fluocinolone acetonide are generally higher in the vitreous and retina with a little dispersion to the aqueous humor. There are reports indicating that topical administration of fluocinolone acetonide produces a percutaneous absorption which is determined by the vehicle, integrity of the epidermal barrier and the use of occlusive dressing. Independently of the route of administration, the systemic absorption of fluocinolone acetonide is below 0.1 ng/ml which indicates that the systemic distribution is very minimal and the effect of fluocinolone is mainly local.|Fluocinolone acetonide is mainly excreted by the kidneys. It is important to mention that the systemically absorbed dose is very minimal.|This pharmacokinetic parameter is not relevant as the systemic absorption of fluocinolone acetonide is very minimal.|This pharmacokinetic parameter is not relevant as the systemic absorption of fluocinolone acetonide is very minimal and the concentration in urine is lower than the minimum quantitation limit.|METABOLISM OF CORTICOSTEROIDS IS GREATLY SLOWED BY INTRODUCTION OF THE 1,2 DOUBLE BOND OR A FLUORINE ATOM INTO MOLECULE, & HALF-LIFE IS CORRESPONDINGLY PROLONGED. /CORTICOSTEROIDS/|(14)C WAS RAPIDLY & MAINLY EXCRETED IN 48-HR FECES (90%), VIA BILE (70% IN 24 HR), & IN URINE (8%). AFTER DERMAL APPLICATION OF CREAM CONTAINING [(14)C]FLUOCINOLONE ACETONIDE TO MICE, GREATER THAN 7% OF (14)C WAS ABSORBED.|...WITHIN 1 HR OF SC DOSE OF [(14)C]FLUOCINOLONE ACETONIDE TO MICE, LARGE AMT...PRESENT IN LIVER & INJECTION SITE, LOWER AMT IN PANCREAS, KIDNEYS, SALIVARY GLANDS, MYOCARDIUM, PITUITARY, & LACRIMAL GLANDS. TISSUE (14)C DECR FAIRLY RAPIDLY DURING 24 HR, EXCEPT IN LIVER & INTESTINES, BECAUSE OF BILIARY SECRETION...|PENETRATION OF...FLUOCINOLONE ACETONIDE...TOPICALLY APPLIED, THROUGH HUMAN ABDOMINAL SKIN WAS OPTIMAL WHEN CONCN OF DRUGS WAS MAXIMAL WHILE MAINTAINING FAVORABLE PARTITION COEFFICIENT BETWEEN SKIN BARRIER & VEHICLE.|For more Absorption, Distribution and Excretion (Complete) data for FLUOCINOLONE ACETONIDE (6 total), please visit the HSDB record page.

Following absorption, fluocinolone acetonide metabolism is primarily hepatic. It is important to mention that the systemically absorbed dose is very minimal.|...IT IS GENERALLY ASSUMED THAT METAB OF /CORTISOL &/ ITS CONGENERS & SYNTH DERIV IS QUALITATIVELY SIMILAR. ...METABOLIZED PRINCIPALLY BY REDN OF RING A, REDN OF KETONE AT C 20, & CLEAVAGE OF SIDE CHAIN. METABOLITES ARE EXCRETED...AS GLUCURONIDES, SULFATES, & UNCONJUGATED COMPOUNDS. /CORTICOSTEROIDS/

The reported half-life of fluocinolone acetonide ranges between 1.3-1.7 hours.

Fluocinolone acetonide is a corticosteroid and thus, it can be inferred that it acts by inhibiting the edema, fibrin deposition, capillary dilation, leukocyte migration, capillary proliferation, fibroblast proliferation, collagen deposition, and scar formation. Some reports have indicated that fluocinolone acetonide presents a high binding affinity for the glucocorticoid receptor. After binding the receptor, the newly formed receptor-ligand complex translocates itself into the cell nucleus, where it binds to many glucocorticoid response elements in the promoter region of the target genes. This effect promotes the induction of phospholipase A2 inhibitory proteins (lipocortins). Through this mechanism of action, it is thought that fluocinolone induces mainly one of the lipocortins, annexin 1, which will later mediate the synthesis of inflammatory mediators such as prostaglandins and leukotrienes by inhibiting the release of arachidonic acid which is the precursor of all these inflammatory mediators. Hence, the induction of these proteins will prevent the release of arachidonic acid by phospholipase A2.|CORTICOSTEROIDS...ARE THOUGHT TO ACT BY CONTROLLING RATE OF SYNTH OF PROTEINS. ...CORTICOSTEROIDS REACT WITH RECEPTOR PROTEINS IN CYTOPLASM OF SENSITIVE CELLS TO FORM STEROID-RECEPTOR COMPLEX. ... STEROID HORMONES APPEAR TO STIMULATE TRANSCRIPTION & ULTIMATELY SYNTH OF SPECIFIC PROTEINS. /CORTICOSTEROIDS/|...CORTICOSTEROIDS...INFLUENCE CARBOHYDRATE, PROTEIN, FAT, & PURINE METABOLISM; ELECTROLYTE & WATER BALANCE; & FUNCTIONS OF CVS, KIDNEY, SKELETAL MUSCLE, NERVOUS SYSTEM, & OTHER ORGANS & TISSUES. ...CORTICOSTEROIDS ENDOW ORGANISM WITH CAPACITY TO RESIST MANY TYPES OF NOXIOUS STIMULI & ENVIRONMENTAL CHANGE. /CORTICOSTEROIDS/

...FOLLICULITIS OR STRIAE IS FREQUENT COMPLICATION, ESP IF OCCLUSIVE DRESSINGS ARE USED.|PHARMACOLOGICAL DOSES OF GLUCOCORTICOIDS RETARD OR INTERRUPT GROWTH OF CHILDREN, INDICATING ADVERSE EFFECT ON EPIPHYSEAL CARTILAGE. INHIBITION OF GROWTH IS RATHER WIDESPREAD EFFECT... /GLUCOCORTICOIDS/|PROLONGED THERAPY WITH CORTICOSTEROIDS MAY RESULT IN SUPPRESSION OF PITUITARY-ADRENAL FUNCTION THAT CAN BE SLOW IN RETURNING TO NORMAL. /CORTICOSTEROIDS/|...PRINCIPAL COMPLICATIONS RESULTING FROM PROLONGED THERAPY...ARE FLUID & ELECTROLYTE DISTURBANCES; HYPERGLYCEMIA & GLYCOSURIA; INCR SUSCEPTIBILITY TO INFECTIONS, INCL TUBERCULOSIS; PEPTIC ULCERS, WHICH MAY BLEED OR PERFORATE; OSTEOPOROSIS; CHARACTERISTIC MYOPATHY; BEHAVIORAL DISTURBANCES... /CORTICOSTEROIDS/|...PRINCIPAL COMPLICATIONS...POSTERIOR SUBCAPSULAR CATARACTS; & CUSHING'S HABITUS, CONSISTING OF "MOON FACE," "BUFFALO HUMP," SUPRACLAVICULAR FAT PADS, "CENTRAL OBESITY," STRIAE, ECCHYMOSES, ACNE, & HIRSUTISM. /CORTICOSTEROIDS/

Acetonide, Fluocinolone

FLUOCINOLONE ACETONIDE, USP (FLUONID, SYNALAR); TOPICAL FORMS: 0.01, 0.025, 0.2% CREAM; 0.025% OINTMENT; 0.01% TOPICAL SOLN. /FROM TABLE/|NEOMYCIN IS OFTEN INCL IN TOPICAL PREPN OF FLUOCINOLONE ACETONIDE TO SUPPRESS INFECTIONS SECONDARY TO INFLAMMATORY PROCESS OR WHICH RESULT FROM USE OF THE GLUCOCORTICOID.

CHROMATOGRAPHY PROCEDURE FOR STEROID IDENTIFICATION INVOLVED SPOTTING STEROID ON FLUORESCENT SILICA GEL PLATE WITHOUT BINDER, HEATING PLATE FOR 18 HR @ 110 DEG, DEVELOPING RESULTANT DECOMP PRODUCTS TO FORM PATTERN CHARACTERISTIC OF STEROID.

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