Source: Medicines Authority (MT) Revision Year: 2021 Publisher: URSAPHARM Arzneimittel GmbH, Industriestraße, 66129 Saarbrücken, Germany Tel.: +49 (0)6805/92 92-0 Fax: +49 (0)6805/92 92-88 e-mail: info@ursapharm.de
Pharmacotherapeutic group: Ophthalmologicals/other Anti-infectives
ATC code: S01AX05
Bibrocathol is a bismuth-containing substance which acts as antiseptic, adstringent and secretion inhibitng agent on mucous membranes and wounds. The mechanism of action is explained by its phenolic molecular structure consisting of tetrabromopyrocatechol and bismuth hydroxide that causes the precipitation of proteins and the shrinking of superficial layers of tissue. These activities result in the formation of a protective membrane against pathogenic invasion and non-specifically inhibit inflammation and secretion.
The efficacy and safety of the bibrocathol 2% eye ointment in the treatment of blepahritis was investigated in two double-blind, placebo-controlled, randomised studies in patients with moderately severe blepharitis/blepharoconjunctivitis which did not require antibiotic therapy. 200 patients were treated for 2 weeks three times daily, respectively 196 patients were treated three times a day for an average of 10 days. In Study 1, the primary endpoint was the mean change from baseline after two weeks, of a composite endpoint of five signs of the disease (eye lid oedema, lid erythema, debris, hyperemia and pouting of Meibomian glands) as assessed by the investigator. The maximum score was 20. The primary endpoint of Study 2 was similar, but it consisted of 4 components instead of five (minus the hyperemia), with maximal score of 16. Both studies met their primary endpoints. In Study 1, the Least Square mean change from baseline (Baseline score about 14) to Day 15 was -8.621 in the bibrocathol group and -5.996 in the placebo group (LS means difference 2.625 [95%CI: -3.360, -1.890], p<0.0001). In Study 2, the mean baseline values were 10.5 points, and the primary outcome difference was -2.32 points [95%-CI: -2.84; -1.80], p<0.0001. In both studies, the primary endpoints were supported by a secondary Patient Reported Outcome regarding ocular symptoms relief. Both studies confirmed the efficacy and safety of bibrocathol 2%-eye ointment.
Bibrocathol is almost insoluble in water and therefore does not penetrate into aqueous humour of the eye. Therefore, its ophthalmologic use is limited to the topical treatment of chronic inflammation of the lid margin (Blepharitis chronica).
There is no remarkable systemic absorption after topical application.
The systemic administration of single intragastric bibrocathol doses vastly exceeding the therapeutic dose temporarily accelerated respiration and decreased activity of mice, but not in rats. No mortality was observed.
Multiple ophthalmologic bibrocathol doses up to 2-fold of the therapeutic dose in rats and up to 150-fold of the therapeutic dose in rabbits for 30 days did not result in appreciable adverse effects. The elevated levels of triglycerides or cholesterol determined in the blood of rabbits and rats, respectively, did not correlate with histological changes.
Bibrocathol did not show any genotoxic potential in bacteria and bone marrow cells of mice. Carcinogenicity studies were not performed.
In limited investigations of the reproductive toxicity in rats, ophthalmic administration of up to 2-fold of the therapeutic dose did not affect male and female fertility, embryogenesis or foetal and postnatal development.
No ocular intolerabilities of bibrocathol were observed up to maximum dosages in repeated-dose toxicity studies in rats and rabbits. Single ophthalmic administration of up to 20% bibrocathol also did not induce hypersensitivities or effects on humoral, cell-mediated or non-specific immunity of guinea pigs and mice, respectively.
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