Rimexolone

Rimexolone
Clinical data
Trade names Vexol
Synonyms Trimexolone; Org 6216; 11β-Hydroxy-16α,17α,21-trimethylpregna-1,4-dien-3,20-dione
AHFS/Drugs.com Monograph
MedlinePlus a606003
Pregnancy
category
  • US: C (Risk not ruled out)
    Routes of
    administration
    Eye drops
    ATC code
    Pharmacokinetic data
    Elimination half-life estimated 1–2 hours
    Excretion >80% faeces
    Identifiers
    CAS Number
    PubChem CID
    IUPHAR/BPS
    DrugBank
    ChemSpider
    UNII
    KEGG
    ChEMBL
    ECHA InfoCard 100.211.227
    Chemical and physical data
    Formula C24H34O3
    Molar mass 370.525 g/mol
    3D model (JSmol)
     NY (what is this?)  (verify)

    Rimexolone is a glucocorticoid steroid used to treat inflammation in the eye.[1] It is marketed as a 1% eye drop suspension under the trade name Vexol by Alcon Laboratories, but was discontinued in the US and other countries.[2][3]

    Medical uses

    Rimexolone is used to treat inflammation after eye surgery, to treat anterior uveitis, conjunctivitis and keratitis.[2][3]

    Contraindications

    The substance is contraindicated in herpes simplex and most other viral eye infections, as well as mycobacterial, fungal and amoebal eye infections[2][3] because it only reduces the inflammation but does not act against such microorganisms.

    Side effects

    The most common adverse effects are blurred vision, tearing and other kinds of eye discomfort. Eye pain, eye oedema, headache, increased intraocular pressure and other side effects are seen in less than 1% of patients.[2][3]

    Pharmacology

    Pharmacodynamics

    As a glucocorticoid, rimexolone acts as an agonist of the glucocorticoid receptor.

    Pharmacokinetics

    A small amount of rimexolone is absorbed into the systemic circulation. On hourly treatment with the eye drops for a week, blood serum concentrations peaked at 150 pg/ml on average, with many patients remaining below the detection threshold of 80 pg/ml. The elimination half-life from the circulation is estimated at one to two hours; the substance is mainly (over 80%) excreted via the faeces.[2][3]

    References

    1. Kavuncu S, Horoz H, Ardagil A, Erbil HH (August 2008). "Rimexolone 1% versus prednisolone acetate in preventing early postoperative inflammation after cataract surgery". Int Ophthalmol. 28 (4): 281–5. doi:10.1007/s10792-007-9131-0. PMID 17762913.
    2. 1 2 3 4 5 Haberfeld, H, ed. (2015). Austria-Codex (in German). Vienna: Österreichischer Apothekerverlag. Vexol 1% (10 mg/ml)-Augentropfensuspension.
    3. 1 2 3 4 5 Drugs.com: Monograph.


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