Background/Purpose: Aminaphtone has been used for many years to treat microvascular disorders. In vitro Aminaphtone counteracts vasoconstriction downregulating endothelin-1 production and interferes with adhesion molecules and cadherin degradation thus defending vessels permeability (1-3). In vivo aminaphtone ameliorates clinical symptoms of several clinical conditions, including Raynaud’s phenomenon (RP) (4).

The aim of the study was to evaluate long-term tolerability of standard dosage of Aminaphtone in a cohort of systemic sclerosis (SSc) patients with secondary RP.

Methods: Seventy-eight SSc patients (mean age 65±13 years; mean disease duration 9±7 years) treated with Aminaphtone due to active RP were enrolled (ACR/EULAR 2013 criteria). They were taking various concomitant treatments, including aspirin, calcium-channel blockers, cyclic intravenous iloprost, immunomodulators, endothelin receptor antagonists. SSc patients performed periodic clinical assessments and blood tests on average every four months per clinical practice. Duration of Aminaphtone administration, side effects, and self-assessment of Raynaud Condition Score (RCS) in a scale from 0 (absence of pain) to 10 (intolerable pain) were retrospectively taken into account.

Results: Duration of Aminaphtone administration (75 mg bis in die dosage, as standard initial posology ) was between six and sixty-seven months (mean 31±20 months). During the follow-up, five patients (6.4%) referred headache as side effect: three of them had to reduce Aminaphtone posology to 75 mg per day, while maintaining clinical benefits. Periodic blood tests did not reveal any significant alteration attributable to Aminaphtone. No other side effects related to the drug appeared during the treatment period.

At baseline, mean RCS was 7.3±0.8. After 3 months of treatment sixty-four patients (82%) yet referred a subjective improvement of RCS (3.5±0.8, p=0.03), whereas 14 patients (18%) were clinically unsatisfied (RCS 6.1±0.4, p=0.12). In this last group, posology was increased to 75 mg tris in die, with a satisfactory amelioration in further nine patients (93.6%) (RCS 4.0±0.6 p=0.04), while five patients (6.4%) definitively discontinued therapy for subjective ineffectiveness within six months. Patients referred a sustained improvement of RCS along the observational period (31±20 months) (last RCS 3.7±0.7, p=0.03 vs baseline).

Conclusion: Aminaphtone shows an acceptable long-term tolerability along with sustained efficacy in the management of SSc-related RP, without disabling side effects. A randomized controlled trial for Aminaphtone use in the management of SSc-related RP is desirable.

References. 1. Scorza R et al. 2008. Drugs R D 9(4):251-7. 2. Scorza R et al. 2008. Clin Ther 30(5):924-9. 3. Felice F et al. 2018. Phlebology 33(9):592-599. 4. Ruaro B et al. 2019. Front Pharmacol 10:293.

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ACR Meeting Abstracts - https://acrabstracts.org/abstract/long-term-tolerability-of-aminaphtone-in-raynauds-phenomenon-secondary-to-systemic-sclerosis/