Rimexolone

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Rimexolone
Names
Trade namesVexol
Other namesTrimexolone; Org 6216; 11β-Hydroxy-16α,17α,21-trimethylpregna-1,4-dien-3,20-dione
  • (8S,9S,10R,11S,13S,14S,16R,17S)-11-Hydroxy-10,13,16,17-tetramethyl-17-propanoyl-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-3-one
Clinical data
Drug classCorticosteroid
Main usesInflammation of the eye[1]
Side effectsIncreased intraocular pressure, blurry vision, eye pain, redness, runny nose[1]
Pregnancy
category
  • US: C (Risk not ruled out)
Routes of
use		Eye drops
External links
AHFS/Drugs.comMonograph
MedlinePlusa606003
Pharmacokinetics
Elimination half-lifeestimated 1–2 hours
Excretion>80% faeces
Chemical and physical data
FormulaC24H34O3
Molar mass370.533 g·mol−1
3D model (JSmol)
  • CCC(=O)[C@]1([C@@H](C[C@@H]2[C@@]1(C[C@@H]([C@H]3[C@H]2CCC4=CC(=O)C=C[C@]34C)O)C)C)C
  • InChI=1S/C24H34O3/c1-6-20(27)24(5)14(2)11-18-17-8-7-15-12-16(25)9-10-22(15,3)21(17)19(26)13-23(18,24)4/h9-10,12,14,17-19,21,26H,6-8,11,13H2,1-5H3/t14-,17+,18+,19+,21-,22+,23+,24-/m1/s1 ☒N
  • Key:QTTRZHGPGKRAFB-OOKHYKNYSA-N ☒N

Rimexolone, sold under the brand name Vexol, is a steroid medication used to treat inflammation of the eye.[1] This includes anterior uveitis and following surgery of the eye.[1] It is used as an eye drop.[1]

Common side effects include increased intraocular pressure, blurry vision, eye pain, redness, and a runny nose.[1] Other complications can include fungal infection of the cornea.[1]

Rimexolone was approved for medical use in the United States in 1994.[1] In the United States a 5 ml bottle costs about 100 USD as of 2021.[2] It is no longer available in the United Kingdom as of 2019.[3]

Medical uses

Rimexolone is used to treat inflammation after eye surgery, to treat anterior uveitis, conjunctivitis and keratitis.[4][5]

Dosage

It is used as 1 to 2 drops four times per day.[1]

Contraindications

The substance is contraindicated in herpes simplex and most other viral eye infections, as well as mycobacterial, fungal and amoebal eye infections[4][5] 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.[4][5]

Pharmacology

Pharmacodynamics

Further information: Glucocorticoid § Mechanism of action

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.[4][5]

References

  1. ↑ 1.0 1.1 1.2 1.3 1.4 1.5 1.6 1.7 1.8 "Rimexolone Monograph for Professionals". Drugs.com. Archived from the original on 20 January 2021. Retrieved 17 October 2021.
  2. ↑ "Vexol Prices, Coupons & Patient Assistance Programs". Drugs.com. Retrieved 17 October 2021.
  3. ↑ "Rimexolone eye drops. Rimexolone antibiotic eye drops - Patient". patient.info. Archived from the original on 13 August 2021. Retrieved 17 October 2021.
  4. ↑ 4.0 4.1 4.2 4.3 Haberfeld, H, ed. (2015). Austria-Codex (in German). Vienna: Österreichischer Apothekerverlag. Vexol 1% (10 mg/ml)-Augentropfensuspension.{{cite book}}: CS1 maint: unrecognized language (link)
  5. ↑ 5.0 5.1 5.2 5.3 Drugs.com: Monograph.

External links

Identifiers:
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