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Fluorometholone

Fluorometholone structure

CAS No:
426-13-1
Formula:
C22H29FO4
Chemical Name:
Fluorometholone
Synonyms:
Pregna-1,4-diene-3,20-dione,9-fluoro-11,17-dihydroxy-6-methyl-,(6α,11β)-;Pregna-1,4-diene-3,20-dione,9-fluoro-11β,17-dihydroxy-6α-methyl-;(6α,11β)-9-Fluoro-11,17-dihydroxy-6-methylpregna-1,4-diene-3,20-dione;U 8614;21-Desoxy-9α-fluoro-6-methylprednisolone;9α-Fluoro-11β,17α-dihydroxy-6α-methylpregna-1,4-diene-3,20-dione;Fluorometholone;6α-Methyl-9α-fluoro-21-desoxyprednisolone;6α-Methyl-9α-fluoro-11β,17α-dihydroxypregna-1,4-diene-3,20-dione;Oxylone;Cortilet;Delmeson;NSC-33001;Flumetholone;FML;Fluormetholon;FML SOP;Fluaton;FML Forte;Loticort;FML Liquifilm;Fluor-Op;Efflumidex;Flumetholon;Ursnon;Fluaton PVA;23784-31-8
Categories:
Active Pharmaceutical Ingredients > Hormones and the Endocrine System

Description

Fluorometholone is the topical synthetic glucocorticoid. Its tropical anti-inflammatory effect is 40 times as much as hydrocortisone, but their effects of oral administration are almost equal. It is mainly used for local treatment of skin allergy, pruritus, rash and other diseases related to allergy. Oral administration is also used for the treatment of breast cancer, childhood leukemia, connective tissue disease, and so on.

Solid

Fluorometholone is a member of the class of glucocorticoids that is Delta(1)-progesterone substituted at positions 11beta and 17 by hydroxy groups, at position 6alpha by a methyl group and at position 9 by a fluoro group. Used for the treatment of corticosteroid-responsive inflammation of the palpebral and bulbar conjunctiva, cornea and anterior segment of the globe. It has a role as an anti-inflammatory drug. It is a fluorinated steroid, an 11beta-hydroxy steroid, a 20-oxo steroid, a 3-oxo-Delta(1),Delta(4)-steroid, a glucocorticoid, a 17alpha-hydroxy steroid and a tertiary alpha-hydroxy ketone. It derives from a Delta(1)-progesterone.|A glucocorticoid employed, usually as eye drops, in the treatment of allergic and inflammatory conditions of the eye. It has also been used topically in the treatment of various skin disorders. (From Martindale, The Extra Pharmacopoeia, 30th ed, p732)|Fluorometholone is a Corticosteroid. The mechanism of action of fluorometholone is as a Corticosteroid Hormone Receptor Agonist.|Fluorometholone is a synthetic glucocorticoid with anti-inflammatory and anti-allergic properties. Fluorometholone exerts its effects by interacting with cytoplasmic glucocorticoid receptors and subsequently activates glucocorticoid receptor mediated gene expression. The synthesis of certain anti-inflammatory proteins is induced while the synthesis of certain inflammatory mediators is inhibited. As a result, there is an overall reduction in chronic inflammation and autoimmune reactions.

Fluorometholone Basic Attributes

Molecular Weight：

376.46

Exact Mass：

376.46

EC Number：

207-041-5

UNII：

SV0CSG527L

NSC Number：

33001

DSSTox ID：

DTXSID7047435

NCI Thesaurus Code：

C29058

ATC Code：

S01BA07|C - Cardiovascular system|D - Dermatologicals|S - Sensory organs

HScode：

2937229000

Characteristics

PSA：

74.6

XLogP3：

Appearance：

Solid

Density：

1.3±0.1 g/cm3

Melting Point：

297 °C

Boiling Point：

527.1±50.0 °C at 760 mmHg

Flash Point：

272.6±30.1 °C

Refractive Index：

55 ° (C=1, Pyridine)

Water Solubility：

30mg/L(25 ºC)

Safety Information

Transport codes：

NONH for all modes of transport

wgk germany：

hazard class code：

20/21/22

safety instructions：

RTECS Number：

TU3834100

Marks：

Precautionary statement(s)：

P280

Hazard Statements：

H302-H312-H332

Toxicity

Toxicity Summary：

Side effects may include acute anterior uveitis and perforation of the globe. Keratitis, conjunctivitis, corneal ulcers, mydriasis, conjunctival hyperemia, loss of accommodation and ptosis have occasionally been reported following local use of corticosteroids. LD50 = 234 mg/kg (rats)

Drug Information

Drug Indication：

For the ophthalmic treatment of corticosteroid-responsive inflammation of the palpebral and bulbar conjunctiva, cornea and anterior segment of the globe.|FDA Label

Pharmacology：

Corticosteroids such as fluorometholone inhibit the inflammatory response to a variety of inciting agents and probably delay or slow healing. They inhibit the edema, fibrin deposition, capillary dilation, leukocyte migration, capillary proliferation, fibroblast proliferation, deposition of collagen, and scar formation associated with inflammation.

MeSH：

Agents that are used to treat allergic reactions. Most of these drugs act by preventing the release of inflammatory mediators or inhibiting the actions of released mediators on their target cells. (From AMA Drug Evaluations Annual, 1994, p475) (See all compounds classified as Anti-Allergic Agents.)|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.)

Mechanism of Action：

There is no generally accepted explanation for the mechanism of action of ocular corticosteroids. However, corticosteroids are thought to act by the induction of phospholipase A2 inhibitory proteins, collectively called lipocortins. It is postulated that these proteins control the biosynthesis of potent mediators of inflammation 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. Their primary target is the cytosolic 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 (GRE) in the promoter region of the target genes. The DNA bound receptor then interacts with basic transcription factors, causing the increase in expression of specific target genes.

MeSH Entry Terms：

Cortisdin

Fluorometholone Use and Manufacturing

Uses

Fluorometholone is a glucocorticoid; anti-inflammatory.

Use Classification：

Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients|Pharmaceuticals

Computed Properties

Molecular Weight:376.5
XLogP3:2
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:5
Rotatable Bond Count:1
Exact Mass:376.20498756
Monoisotopic Mass:376.20498756
Topological Polar Surface Area:74.6
Heavy Atom Count:27
Complexity:787
Defined Atom Stereocenter Count:8
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

Drug Function and Efficacy

Not yet clear

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Fluorometholone eye drops
Ingredients	Fluorometholone.
Indication	Not yet clear.
Specifications	5ml:1mg

Fluorometholone eye drops
Ingredients	Each milliliter of eye drops contains 1 mg of fluorometholone, 14 mg of liquid film component (polyethylene alcohol), 40 mg of chlorpheniramine, disodium edetate, sodium chloride, monobasic sodium phosphate, polyoxyethylene sorbitan, fatty acid esters (surfactants) and purified water.
Indication	Not yet clear.
Specifications	5 ml: 5 mg

Fluorometholone eye drops
Ingredients	The main ingredient of this product is fluorometholone.

See More Related Drugs

Registered Holders

EUROAPI FRANCE

France
Active
FARMABIOS S.P.A.

Italy
Active
Taipei (Beijing) Pharmaceutical Technology Co., Ltd.

China
Active

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