On the issue of the effectiveness and bioequivalence of isotretinoin Lidose
- Authors: Olisova O.Y.1, Kukes I.V.2
-
Affiliations:
- I.M. Sechenov First Moscow State Medical University
- International Association of Clinical Pharmacologists and Pharmacists
- Issue: Vol 27, No 2 (2024)
- Pages: 179-187
- Section: DERMATOLOGY
- URL: https://journals.rcsi.science/1560-9588/article/view/262157
- DOI: https://doi.org/10.17816/dv629705
- ID: 262157
Cite item
Abstract
BACKGROUND: Acne is one of the most common types of dermatoses. Systemic isotretinoin treatment, which affects all mechanisms of acne pathogenesis, is the most effective drug for severe acne treatment. This study presents scientific data on the innovative formulation of isotretinoin for acne treatment using the patented Lidose technology. The use of lidose isotretinoin allows for the reduction of the amount of isotretinoin used by the patient by 20% without losing its therapeutic effectiveness.
AIM: This study aimed to analyze comparative studies of bioavailability and relevant pharmacokinetic parameters, which made it possible to prove that initial dosages of 8 and 16 mg of lidose isotretinoin (Aknecutan) are bioequivalent to 10 and 20 mg of the usual isotretinoin preparations. The study also aimed to evaluate the efficacy and safety of the drug.
MATERIALS AND METHODS: Over the past 7 years, 1044 patients (women, n = 651, 62.4%; men, n = 393, 37.6%) have received acne treatment using new formulations of isotretinoin (lidose isotretinoin, Aknecutan) for moderate to severe acne at a daily dose of 0.4–0.8 per 1 kg of body weight with a total drug dose of 100–120 mg/kg per course of therapy.
RESULTS: The study demonstrated the bioequivalence of 8 and 10 mg lidose isotretinoin (Aknecutan) to the usual preparations of 10 and 20 mg isotretinoin, respectively. After therapy, clinical remission was achieved in all patients, which required 7–12 months of treatment, depending on the daily drug dose. Among the side effects, cheilitis and retinoic dermatitis of the face was observed, which were completely resolved by use of moisturizing creams and moisturizing sticks. An increase in the levels of liver enzymes, triglycerides, and lipoproteins was observed in 5–10% of patients, which did not exceed 20–30% of the norm and did not require discontinuation of therapy. After the treatment, these indicators returned to normal levels. Other side effects were extremely rare. Notably, disease relapses are most often caused by a low total dose of the drug or the presence of endocrinological and gynecological diseases.
CONCLUSION: The innovative lidose isotretinoin is one of the most highly effective and safe systemic retinoids for the treatment of moderate to severe acne. Comparative studies of bioavailability and corresponding pharmacokinetic parameters have demonstrated the bioequivalence of the new formulation of isotretinoin (Aknecutan) for acne treatment, which fully corresponds to that of the original preparation.
Keywords
Full Text
##article.viewOnOriginalSite##About the authors
Olga Yu. Olisova
I.M. Sechenov First Moscow State Medical University
Author for correspondence.
Email: olisovaolga@mail.ru
ORCID iD: 0000-0003-2482-1754
SPIN-code: 2500-7989
MD, Dr. Sci. (Med.), Professor, Corresponding member of the Russian Academy of Sciences
Russian Federation, MoscowIlya V. Kukes
International Association of Clinical Pharmacologists and Pharmacists
Email: ilyakukes@gmail.com
ORCID iD: 0000-0003-1449-8711
SPIN-code: 1166-3569
MD, Cand. Sci. (Med.)
Russian Federation, MoscowReferences
- Federal clinical guidelines for the management of acne patients. Russian Society of Dermatovenerologists and Cosmetologists; 2020. 20 p. (In Russ).
- Reed ML, Stanley J, Stengel F, et al. Mal de meleda treated with 13-cis retinoic acid. Arch Dermatol. 1979;115(5):605–608.
- Nast A, Dreno B, Bettoli V, et al. European evidence-based (S3) guideline for the treatment of acne--update 2016, short version. J Eur Acad Dermatol Venenreol. 2016;30(8):1261–1268. doi: 10.1111/jdv.13776
- Norris DA, Osborn R, Robinson W, Tonnesen MG. Isotretinoin produces significant inhibition of monocyte and neutrophil chemotaxis in vivo in patients with cystic acne. J Invest Dermatol. 1987;89(1):38–43. doi: 10.1111/1523-1747.ep12580370
- Sakania LR, Plieva KT, Korsunskaya IM. Using algorithm of descending doses of retinoids in treatment of acne resistant to standard therapies. Russ J Clin Dermatol Venereol. 2016;15(2):72–76. EDN: VZLKED doi: 10.17116/klinderma201615272-76
- Dispenza M, Wolpert EB, Gilliland KL, et al. Systemic isotretinoin therapy normalizes exaggerated TLR-2-mediated innate immune responses in acne patients. J Invest Dermatol. 2012;132(9):2198–2205. doi: 10.1038/jid.2012.111
- Aravijskaja ER. Severe acne: analysis of some modern methods of treatment. Pharmateca. 2017;(S1):38–43. EDN: YIATLR
- Colburn WA, Vane FM, Shorter HJ. Pharmacokinetics of isotretinoin and its major blood metabolite following a single oral dose to man. Eur J Clin Pharmacol. 1983;24(5):689–694. doi: 10.1007/BF00542224
- Costa CS, Bagatin E, Martimbianco AL, et al. Oral isotretinoin for acne. Cochrane Database Syst Rev. 2018;11(11):CD009435. doi: 10.1002/14651858.CD009435.pub2
- Oon HH, Wong SN, Aw DC, et al. Acne management guidelines by the dermatological society of Singapore. J Clin Aesthet Dermatol. 2019;12(7):34–50. EDN: RYLJUF
- Thiboutot D, Dreno B, Araviiskaia E, et al. Practical management of acne for clinicians: An international consensus from Global Alliance to improve outcome sinacne. J Am Acad Dermatol. 2018;78(2, Suppl 1):S1–S23.e1. EDN: XXFYMP doi: 10.1016/j.jaad.2017.09.078
- Kubanova AA, Araviyskaya ER, Sokolovsky EV, et al. Systemic treatment of severe forms of acne: Experience of using isotretinoin in the Russian Federation. Vestnik dermatologii i venerologii. 2013;(5):102–114. EDN: RGTAXT
- Tlish MM, Sрavilova ME. Isotrethinoine in acne therapy. Vestnik dermatologii i venerologii. 2017;(4):90–96 EDN: YUVEEY
- Drozdina MB. The usage of Aknekutan for the treatment of fulminant acne. Remedium Privolzhye. 2019;(2):25. EDN: GIPCSM
- Samtsov AV, Statsenko AV, Volkova SV, et al. Questions of the effectiveness and safety of the use of acnecutan in acne therapy. Vestnik dermatologii i venerologii. 2012;(3):053–056. EDN: RCFWAD
- Batkaev EA, Molodova YS. Aknekutan in acne therapy: A new low-dose scheme. Russ J Clin Dermatol Venereol. 2014;12(2):84–90. EDN: SDKGYX
- Danilova AA, Kosorukova IM. On the results of an open-label single-arm study to evaluate the efficacy, safety and tolerability of acnecutan in patients suffering from severe forms of acne as well as acne resistant to other therapies. Vestnik dermatologii i venerologii. 2012;(2):60–63. EDN: PAGKVR
- Ustinov MV, Sirmais NS. Aknekutan--interesting cases in everyday practice. Russkii meditsinskii zhurnal. 2013;(22):1100–1104. EDN: RDYVRH
- Olisova OY, Ma T. Effectiveness vs inefficiency of systemic retinoids in acne. Effective Pharmacotherapy. 2020;16(9):18–24. EDN: BIUECI doi: 10.33978/2307-3586-2020-16-9-18-22
- Liu A, Yang DJ, Gerhardstein PC, Hsu S. Relapse of acne following isotretinoin treatment: A retrospective study of 405 patients. J Drugs Dermatol. 2008;(7):963–966.