Reasons to use methotrexate in the form of a subcutaneous injection in the treatment of rheumatoid arthritis Review article
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Published:
Jun 30, 2023
Keywords:
methotrexate, rheumatoid arthritis, bioavailability
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Abstract
Methotrexate is the main drug used in the treatment of rheumatoid arthritis. Currently, the doctor can choose between the form administered orally and subcutaneously.
The article highlights the features that positively distinguish the subcutaneous form of the drug. In particular, attention was paid to the bioavailability of the drug.
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How to Cite
Ligocki, P. (2023). Reasons to use methotrexate in the form of a subcutaneous injection in the treatment of rheumatoid arthritis. Medycyna Faktow (J EBM), 16(2(59), 165-169. https://doi.org/10.24292/01.MF.0223.06
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References
1. Smolen JS, Landewé RBM, Bergstra SA et al. EULAR recommendations for the management of rheumatoid arthritis with synthetic and biological disease-modifying antirheumatic drugs: 2022 update. Ann Rheum Dis. 2023; 82(1): 3-18. http://doi.org/10.1136/ard-2022-223356.
2. PWX/Rynek Zdrowia: Co lepsze – zastrzyk czy tabletka? 26.08.2014 .
3. Ligocki P, Orlik G, Vekariya V. THU0179 Patient and their illness – atypical sources of therapy risks. Characteristics of the use of MTX and FA supplementation in therapy lasting minimum 8 weeks in adult patients with RA. Ann Rheum Dis. 2019; 78: 364-5.
4. Pichlmeier U, Heuer KU. Subcutaneous administration of methotrexate with a prefilled autoinjector pen results in a higher relative bioavailability compared with oral administration of methotrexate. Clin Exp Rheumatol. 2014; 32(4): 563-71.
5. Dhaon P, Das SK, Srivastava R et al. Oral Methotrexate in split dose weekly versus oral or parenteral Methotrexate once weekly in Rheumatoid Arthritis: a short-term study. Int J Rheum Dis. 2018; 21(5): 1010-17. http://doi.org/10.1111/1756-185X.12910.
6. Zhao R, Goldman ID. The proton-coupled folate transporter: physiological and pharmacological roles. Curr Opin Pharmacol. 2013;13(6): 875-80. http://doi.org/10.1016/j.coph.2013.09.011.
7. Zhang Y, Sun L, Chen X et al. A Systematic Review of Population Pharmacokinetic Models of Methotrexate. Eur J Drug Metab Pharmacokinet. 2022; 47; 143-164. https://doi.org/10.1007/s13318-021-00737-6.
8. Urquhart BL, Gregor JC, Chande N et al. The human proton-coupled folate transporter (hPCFT): modulation of intestinal expression and function by drugs. Am J Physiol Gastrointest Liver Physiol. 2010; 298(2): G248-54. http://doi.org/10.1152/ajpgi.00224.2009.
9. Artacho A, Isaac S, Nayak R et al. The Pretreatment Gut Microbiome Is Associated With Lack of Response to Methotrexate in New-Onset Rheumatoid Arthritis. Arthritis Rheumatol. 2021; 73(6): 931-42. http://doi.org/10.1002/art.41622.
10. Charakterystyka Produktu Leczniczego. Metotreksat.
11. Maksimovic V, Pavlovic-Popovic Z, Vukmirovic S et al. Molecular mechanism of action and pharmacokinetic properties of methotrexate. Mol Biol Rep. 2020; 47(6): 4699-708.
12. Koźmiński P, Halik PK, Chesori R et al. Overview of Dual-Acting Drug Methotrexate in Different Neurological Diseases, Autoimmune Pathologies and Cancers. Int J Mol Sci. 2020; 21(10): 3483. http://doi.org/10.3390/ijms21103483.
13. Kabisch S, Weigand T, Plischke H et al. Bioavailability of methotrexate (MTX) following different routes of application. Akt Rheumatol. 2004; 29: 197-200.
14. Bedoui Y, Guillot X, Sélambarom J et al. Methotrexate an old drug with new tricks. Int J Mol Sci. 2019; 20(20): 5023.
15. Schiff MH, Jaffe JS, Freundlich B. Head-to-head, randomised, crossover study of oral versus subcutaneous methotrexate in patients with rheumatoid arthritis: drug-exposure limitations of oral methotrexate at doses ≥15 mg may be overcome with subcutaneous administration. Ann Rheum Dis. 2014; 73(8): 1549-51. http://doi.org/10.1136/annrheumdis-2014-205228.
16. Godfrey C, Sweeney K, Miller K et al. The population pharmacokinetics of long-term methotrexate in rheumatoid arthritis. Br J Clin Pharmacol. 1998; 46(4): 369-76. http://doi.org/10.1046/j.1365-2125.1998.t01-1-00790.x.
17. Pasma A, den Boer E, van’t Spijker A et al. Nonadherence to disease modifying antirheumatic drugs in the first year after diagnosis: comparing three adherence measures in early arthritis patients. Rheumatology (Oxford). 2016; 55(10): 1812-9. http://doi.org/10.1093/rheumatology/kew247.
18. Hoekstra M, Haagsma C, Neef C et al. Bioavailability of higher dose methotrexate comparing oral and subcutaneous administration in patients with rheumatoid arthritis. J Rheumatol. 2004; 31(4): 645-8.
19. Dervieux T, Furst D, Lein DO et al. Polyglutamation of methotrexate with common polymorphisms in reduced folate carrier, aminoimidazole carboxamide ribonucleotide transformylase, and thymidylate synthase are associated with methotrexate effects in rheumatoid arthritis. Arthritis Rheum. 2004; 50(9): 2766-74. http://doi.org/10.1002/art.20460.
20. Stamp LK, Barclay ML, O’Donnell JL et al. Effects of changing from oral to subcutaneous methotrexate on red blood cell methotrexate polyglutamate concentrations and disease activity in patients with rheumatoid arthritis. J Rheumatol. 2011; 38(12): 2540-7. http://doi.org/10.3899/jrheum.110481.
21. Becker ML, van Haandel L, Gaedigk R et al. Analysis of intracellular methotrexate polyglutamates in patients with juvenile idiopathic arthritis: effect of route of administration on variability in intracellular methotrexate polyglutamate concentrations. Arthritis Rheum. 2010; 62(6): 1803-12. http://doi.org/10.1002/art.27434.
22. Tanaka Y. Subcutaneous injection of methotrexate: advantages in the treatment of rheumatoid arthritis. Mod Rheumatol. 2022: roac156. http://doi.org/10.1093/mr/roac156.
2. PWX/Rynek Zdrowia: Co lepsze – zastrzyk czy tabletka? 26.08.2014 .
3. Ligocki P, Orlik G, Vekariya V. THU0179 Patient and their illness – atypical sources of therapy risks. Characteristics of the use of MTX and FA supplementation in therapy lasting minimum 8 weeks in adult patients with RA. Ann Rheum Dis. 2019; 78: 364-5.
4. Pichlmeier U, Heuer KU. Subcutaneous administration of methotrexate with a prefilled autoinjector pen results in a higher relative bioavailability compared with oral administration of methotrexate. Clin Exp Rheumatol. 2014; 32(4): 563-71.
5. Dhaon P, Das SK, Srivastava R et al. Oral Methotrexate in split dose weekly versus oral or parenteral Methotrexate once weekly in Rheumatoid Arthritis: a short-term study. Int J Rheum Dis. 2018; 21(5): 1010-17. http://doi.org/10.1111/1756-185X.12910.
6. Zhao R, Goldman ID. The proton-coupled folate transporter: physiological and pharmacological roles. Curr Opin Pharmacol. 2013;13(6): 875-80. http://doi.org/10.1016/j.coph.2013.09.011.
7. Zhang Y, Sun L, Chen X et al. A Systematic Review of Population Pharmacokinetic Models of Methotrexate. Eur J Drug Metab Pharmacokinet. 2022; 47; 143-164. https://doi.org/10.1007/s13318-021-00737-6.
8. Urquhart BL, Gregor JC, Chande N et al. The human proton-coupled folate transporter (hPCFT): modulation of intestinal expression and function by drugs. Am J Physiol Gastrointest Liver Physiol. 2010; 298(2): G248-54. http://doi.org/10.1152/ajpgi.00224.2009.
9. Artacho A, Isaac S, Nayak R et al. The Pretreatment Gut Microbiome Is Associated With Lack of Response to Methotrexate in New-Onset Rheumatoid Arthritis. Arthritis Rheumatol. 2021; 73(6): 931-42. http://doi.org/10.1002/art.41622.
10. Charakterystyka Produktu Leczniczego. Metotreksat.
11. Maksimovic V, Pavlovic-Popovic Z, Vukmirovic S et al. Molecular mechanism of action and pharmacokinetic properties of methotrexate. Mol Biol Rep. 2020; 47(6): 4699-708.
12. Koźmiński P, Halik PK, Chesori R et al. Overview of Dual-Acting Drug Methotrexate in Different Neurological Diseases, Autoimmune Pathologies and Cancers. Int J Mol Sci. 2020; 21(10): 3483. http://doi.org/10.3390/ijms21103483.
13. Kabisch S, Weigand T, Plischke H et al. Bioavailability of methotrexate (MTX) following different routes of application. Akt Rheumatol. 2004; 29: 197-200.
14. Bedoui Y, Guillot X, Sélambarom J et al. Methotrexate an old drug with new tricks. Int J Mol Sci. 2019; 20(20): 5023.
15. Schiff MH, Jaffe JS, Freundlich B. Head-to-head, randomised, crossover study of oral versus subcutaneous methotrexate in patients with rheumatoid arthritis: drug-exposure limitations of oral methotrexate at doses ≥15 mg may be overcome with subcutaneous administration. Ann Rheum Dis. 2014; 73(8): 1549-51. http://doi.org/10.1136/annrheumdis-2014-205228.
16. Godfrey C, Sweeney K, Miller K et al. The population pharmacokinetics of long-term methotrexate in rheumatoid arthritis. Br J Clin Pharmacol. 1998; 46(4): 369-76. http://doi.org/10.1046/j.1365-2125.1998.t01-1-00790.x.
17. Pasma A, den Boer E, van’t Spijker A et al. Nonadherence to disease modifying antirheumatic drugs in the first year after diagnosis: comparing three adherence measures in early arthritis patients. Rheumatology (Oxford). 2016; 55(10): 1812-9. http://doi.org/10.1093/rheumatology/kew247.
18. Hoekstra M, Haagsma C, Neef C et al. Bioavailability of higher dose methotrexate comparing oral and subcutaneous administration in patients with rheumatoid arthritis. J Rheumatol. 2004; 31(4): 645-8.
19. Dervieux T, Furst D, Lein DO et al. Polyglutamation of methotrexate with common polymorphisms in reduced folate carrier, aminoimidazole carboxamide ribonucleotide transformylase, and thymidylate synthase are associated with methotrexate effects in rheumatoid arthritis. Arthritis Rheum. 2004; 50(9): 2766-74. http://doi.org/10.1002/art.20460.
20. Stamp LK, Barclay ML, O’Donnell JL et al. Effects of changing from oral to subcutaneous methotrexate on red blood cell methotrexate polyglutamate concentrations and disease activity in patients with rheumatoid arthritis. J Rheumatol. 2011; 38(12): 2540-7. http://doi.org/10.3899/jrheum.110481.
21. Becker ML, van Haandel L, Gaedigk R et al. Analysis of intracellular methotrexate polyglutamates in patients with juvenile idiopathic arthritis: effect of route of administration on variability in intracellular methotrexate polyglutamate concentrations. Arthritis Rheum. 2010; 62(6): 1803-12. http://doi.org/10.1002/art.27434.
22. Tanaka Y. Subcutaneous injection of methotrexate: advantages in the treatment of rheumatoid arthritis. Mod Rheumatol. 2022: roac156. http://doi.org/10.1093/mr/roac156.