Interchangeability of levothyroxine sodium tablets
Abstract
The article reviews scientific literature and regulatory documents on safe and efficacious use of levothyroxine medicines. Levothyroxine has less than a twofold difference between the minimal toxic concentration and minimal effective concentration. The article discusses the issue of switching between levothyroxine medicines that can be therapeutically nonequivalent while having proven bioequivalence. The article reviews results of levothyroxine medicines interchangeability studies in different countries. The authors assert the need for improving the coordination of manufacturing and the clinical use of levothyroxine medicines, which will help achieve the equivalence of generic and innovator medicines in the future.
About the Authors
G. I. Gorodetskaya
Scientific Centre for Expert Evaluation of Medicinal Products
Russian Federation
Russian Federation
E. A. Sokova
Scientific Centre for Expert Evaluation of Medicinal Products
Russian Federation
Russian Federation
O. V. Muslimova
Scientific Centre for Expert Evaluation of Medicinal Products
Russian Federation
Russian Federation
T. V. Aleksandrova
Scientific Centre for Expert Evaluation of Medicinal Products
Russian Federation
Russian Federation
I. A. Mazerkina
Scientific Centre for Expert Evaluation of Medicinal Products
Russian Federation
Russian Federation
S. G. Rudnev
Scientific Centre for Expert Evaluation of Medicinal Products
Russian Federation
Russian Federation
References
1. Eskandari S, Loo DD, Dai G, Levy O, Wright EM, Carrasco N. Thyroid Na+/I– symporter. Mechanism, stoichiometry, and specificity. J Biol Chem.1997; 272: 27230–8.
2. De la Vieja A, Dohan O, Levy O, Carrasco N. Molecular analysis of the sodium/iodide symporter: impact on thyroid and extrathyroid pathophysiology. Physiological Reviews 2000; 80(3): 1083–105.
3. Boron WF. Medical Physiology: A Cellular And Molecular Approach. Elsevier/Saunders; 2003.
4. Dunn JT, Ray SC. Changes in the structure of thyroglobulin following the administration of thyroid-stimulating hormone. J Biol Chem. 1975; 250: 5801–7.
5. Greer MA, Grimm Y, Studer H. Qualitative changes in the secretion of thyroid hormones induced by iodine deficiency. Endocrinology 1968; 83: 1193–8.
6. Laurberg P. Mechanisms governing the relative proportions of thyroxine and 3,5,3- triiodothyronine in thyroid secretion. Metab Clin Exp. 1984; 33: 379–92.
7. Leonard JL, Kohrle J. Intracellular pathways of iodothyronine metabolism. In: Braverman LE, Utiger RD, eds. The Thyroid. 8th ed. Lippincott, Philadelphia; 2000.
8. Panicker V, Saravanan P, Vaidya B, Evans J, Hattersley AT, Frayling TM, et al. Common variation in the DIO2 gene predicts baseline psychological well-being and response to combination thyroxine plus triiodothyronine therapy in hypothyroid patients. J Clin Endocrinol Metab. 2009; 94(5): 1623–9.
9. Panicker V, Cluett C, Shields B, Murray A, Parnell KS, Perry JR, et al. A common variation in deiodinase 1 gene DIO1 is associated with the relative levels of free thyroxine and triiodothyronine. J Clin Endocrinol Metab. 2008; 93(8): 3075–81.
10. Mendel CM. The Free Hormone Hypothesis: A Physiologically Based Mathematical Model. Endocrine reviews 1989; 10(3): 232–74.
11. Wilber JF, Xu AH. The thyrotropin-releasing hormone gene: cloning, characterization, and transcriptional regulation in the central nervous system, heart, and testis. Thyroid 1998; (8): 897–901.
12. Zakharenko RV. Clinical aspects of thyroid disease in patients with cardiac pathology. Dalnevostochny meditsinskiy zhurnal 2010; (3): 18–22 (in Russian).
13. Veintraub BV, ed. Molecular endocrinology. Fundamental study and it’s reflection in the clinic. Moscow: Meditsina; 2003 (in Russian).
14. Pearce SHS, Brabant G, Duntas L, Monzani F, Peeters R, Razvi S, Wemeau JL. 2013 ETA Guideline: Management of Subclinical Hypothyroidism. Eur Thyroid J 2013; 2(4): 215–28.
15. Selmer C, Olesen JB, Hansen ML, Lindhardsen J, Olsen AM, Madsen JC, et al. The spectrum of thyroid disease and risk of new onset atrial fibrillation: a large population cohort study. BMJ 2012; 345.
16. Tsareva YuO. Features of daily fluctuations of thyroid hormones in patients with cardiovascular disease. Bulleten meditsinskih Internetkonferentsiy 2014; 4(3): 232. Available from: https://goo.gl/783enU (in Russian).
17. Nekrasova TA, Strongin LG, Ledentsova OV, Kazakova LV. The relationship between TTG levels and some of the factors of cardiovascular risk in patients with autoimmune thyroiditis and subclinical hypothyroidism. Klinicheskaya i eksperimentalnaya tireoidologiya 2014; (2): 16–22 (in Russian).
18. Bartáková J, Potlukova E, Rogalewicz V, Fait T, Schöndorfova D, Telivcka Z, et al. Screening for autoimmune thyroid disorders after spontaneous abortion is cost- saving and it improves the subsequent pregnancy rate. BMC Pregnancy Childbirth 2013; 13: 217.
19. Peroni E, Vigone MC, Mora S, Bassi LA, Pozzi C, Passoni A, Weber G. Congenital hypothyroidism treatment in infants: a comparative study between liquid and tablet formulations of levothyroxine. Hormone Research in Paediatrics 2013; 81(1): 50–4.
20. Garber JR, Cobin RH, Gharib H, Hennessey JV, Klein I, Mechanick JI, et al. Clinical Practice Guidelines for Hypothyroidism in Adults: Cosponsored by the American Association of Clinical Endocrinologists and the American Thyroid Association. Endocr Pract. 2012; 18(6): 988–1028.
21. Gkotsina M, Michalaki M, Mamali I, Markantes G, Sakellaropoulos GC, Kalfarentzos F, et al. Improved levothyroxine pharmacokinetics after bariatric surgery. Thyroid 2013; 23: 414–9.
22. Wenzel KW, Kirschsieper HE. Aspects of the absorption of oral L-thyroxine in normal man. Metabolism 1977; 26: 1–8.
23. Centanni M, Gargano L, Canettieri G, Viceconti N, Franchi A, Delle Fave G, et al. Thyroxine in goiter, Helicobacter pilori infection, and chronic gastritis. N Engl J Med 2006; 354: 1787–95.
24. Hadithi M, de Boer H, Meijer JW, Willekens F, Kerckhaert JA, Heijmans R, et al. Coeliac disease in Dutch patients with Hashimoto’s thyroditis and vice versa. World J Gastroenterol. 2007; 13: 1715–22.
25. Muñoz-Torres M, Varsavsky M, Alonso G. Lactose intolerance revealed by severe resistance to treatment with levothyroxine. Thyroid 2006; 16: 1171–3.
26. Ladas S, Papanikos J, Arapakis G. Lactose malabsorption in Greek adults: correlation of small bowel transit time with the severity of lactose intolerance. Gut 1982; 23: 968–73.
27. Belmer SV, Mukhina YuG, Chubarova AI, et al. Lactose intolerance in children and adults. Voprosy detskoy dietologii 2004; 2(1): 101–3 (in Russian).
28. Eadala P, Waud JP, Matthews SB, Green JT, Campell AK, Quantifying the «hidden» lactose in drugs used for the treatment of gastrointestinal conditions. Aliment Pharmacol Ther. 2009; 29: 677–87.
29. United States Pharmacopoeia. Available from: http://www.usp.org.
30. Patel H, Stalcup A, Dansereau R, Sakr A. The effect of excipients on the stability of levothyroxine sodium pentahydrate tablets. Int J Pharm. 2003; 264(1–2): 35–43.
31. Emshanova SV, Sadchikova NP, Zuev AP. Drug particle shape and size control: A necessary factor for high-quality drug production. Pharmaceutical Chemistry Journal 2007; 41(1): 40–9.
32. Emshanova SV. Ensuring the quality of domestic medical products (technology optimization and improvement of tablet dosage forms standardization). Dr. Pharm. Sci [thesis]. Moscow; 2007 (in Russian).
33. State Register of medicines. Available from: http://grls.rosminzdrav.ru/grls.aspx.
34. Fadeev VV, Morgunova TB. Topical issues of substitution treatment of hypothyroidism. Farmateka 2007; (11): 36–40 (in Russian).
35. Approved Drug Products with Therapeutic Equivalence Evaluations. 37th ed. 2017. Available from: https://goo.gl/YDrmMM.
36. American Thyroid Association, Endocrine Society, American Association of Clinical Endocrinologists. Joint statement on the U. S. Food and Drug Administration’s decision regarding bioequivalence of levothyroxine sodium. Thyroid 2004; 14: 486.
37. Wiersinga WM. Adult hypothyroidism. In: Endotext. 2014.
38. State Register of medicines. Available from: http://grls.rosminzdrav.ru/grls.aspx.
39. Demidova MA. The problem of interchangeability of L-thyroxine medicines. Effektivnaya farmakoterapiya 2013; 2(22): 8–12 (in Russian). Available from: https://goo.gl/B1gJxy.
40. Madiyarova MSh, Morgunova TB, Fadeyev VV. Treatment of primary hypothyroidism: unresolved issues. Klinicheskaya i eksperimentalnaya tireoidologiya 2015; 11(1): 22–34 (in Russian).
41. Melnichenko GA, Fadeev VV, Proskurina IA, Bogdanov AN, Gorodetsky VV, Gorodetskaya GI. Guidelines for conducting clinical trials of medicinal products used in the thyroid gland pathology. In: Mironov AN, ed. Guide for conducting clinical trials of medicinal products. Moscow: Grif i K; 2012. P. 163–76 (in Russian).
Review
For citations:
Gorodetskaya G.I., Sokova E.A., Muslimova O.V., Aleksandrova T.V., Mazerkina I.A., Rudnev S.G. Interchangeability of levothyroxine sodium tablets. The Bulletin of the Scientific Centre for Expert Evaluation of Medicinal Products. 2017;7(1):33-40. (In Russ.)
Views:
770
Email this article 