 | |
 | |
| Clinical data | |
|---|---|
| Pronunciation | /ˌmɛθəˈtrɛkˌseɪt, ˌmiː-, -θoʊ-/ [1] [2] [3] |
| Trade names | Trexall, Rheumatrex, Otrexup, others [4] |
| Other names | MTX, amethopterin |
| AHFS/ Drugs.com | Monograph |
| MedlinePlus | a682019 |
| License data |
|
|
Pregnancy category |
|
|
Routes of administration | By mouth, intravenous (IV), intramuscular (IM), subcutaneous injection (SC), intrathecal |
| Legal status | |
| Legal status | |
| Pharmacokinetic data | |
| Bioavailability | 60% at lower doses, less at higher doses. [5] |
| Protein binding | 35–50% (parent drug), [5] 91–93% (7-hydroxymethotrexate) [6] |
| Metabolism | Liver and intracellular [5] |
| Elimination half-life | 3–10 hours (lower doses), 8–15 hours (higher doses) [5] |
| Excretion | Urine (80–100%), faeces (small amounts) [5] [6] |
| Identifiers | |
| |
| Chemical and physical data | |
| Formula | C20H22N8O5 |
| Molar mass | 454.447 g·mol−1 |
| 3D model ( JSmol) | |
| |
| |
| (verify) | |
Methotrexate (MTX), formerly known as amethopterin, is a chemotherapy agent and immune system suppressant. [4] It is used to treat cancer, autoimmune diseases, ectopic pregnancy, and for medical abortions. [4] Types of cancers it is used for include breast cancer, leukemia, lung cancer, lymphoma, gestational trophoblastic disease, and osteosarcoma. [4] Types of autoimmune diseases it is used for include psoriasis, rheumatoid arthritis, and Crohn's disease. [4] It can be given by mouth or by injection. [4]
Common side effects include nausea, feeling tired, fever, increased risk of infection, low white blood cell counts, and breakdown of the skin inside the mouth. [4] Other side effects may include liver disease, lung disease, lymphoma, and severe skin rashes. [4] People on long-term treatment should be regularly checked for side effects. [4] It is not safe during breastfeeding. [4] In those with kidney problems, lower doses may be needed. [4] It acts by blocking the body's use of folic acid. [4]
Methotrexate was made in 1947, and initially came into medical use to treat cancer, as it was less toxic than the then-current treatments. [8] In 1956 it provided the first cures of a metastatic cancer. [9] It is on the World Health Organization's List of Essential Medicines. [10] Methotrexate is available as a generic medication. [4] It is not expensive. [11] The wholesale cost as of 2014 in the developing world is between US$0.06 and US$0.36 per day for the form taken by mouth. [12] In the United States, a typical month of treatment costs $25 to $50. [13] In 2017, it was the 117th most commonly prescribed medication in the United States, with more than six million prescriptions. [14] [15]
- ^ "methotrexate – definition of methotrexate in English from the Oxford dictionary". OxfordDictionaries.com. Archived from the original on 2015-12-04. Retrieved 2016-01-20.
- ^ "methotrexate". Merriam-Webster.com Dictionary.
- ^ "methotrexate". Dictionary.com Unabridged (Online). n.d.
- ^ a b c d e f g h i j k l m n o "Methotrexate". The American Society of Health-System Pharmacists. Archived from the original on 2016-10-08. Retrieved 22 Aug 2016.
- ^ a b c d e "Trexall, Rheumatrex (methotrexate) dosing, indications, interactions, adverse effects, and more". Medscape Reference. WebMD. Archived from the original on 8 February 2014. Retrieved 12 April 2014.
- ^ a b Bannwarth B, Labat L, Moride Y, Schaeverbeke T (January 1994). "Methotrexate in rheumatoid arthritis. An update". Drugs. 47 (1): 25–50. doi: 10.2165/00003495-199447010-00003. PMID 7510620.
- ^ "WHOCC - ATC/DDD Index". www.whocc.no. Archived from the original on 6 November 2020. Retrieved 21 September 2020.
- ^ Sneader, Walter (2005). Drug Discovery: A History. John Wiley & Sons. p. 251. ISBN 9780470015520. Archived from the original on 2017-02-16.
- ^ "Today's anti-cancer tools are ever better wielded". The Economist. 14 September 2017. Archived from the original on 15 May 2018. Retrieved 16 September 2017.
-
^
World Health Organization (2019). World Health Organization model list of essential medicines: 21st list 2019. Geneva.
hdl:
10665/325771. WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO.
{{ cite book}}: CS1 maint: location missing publisher ( link) - ^ Hitchings, Andrew; Lonsdale, Dagan; Burrage, Daniel; Baker, Emma (2019). The Top 100 Drugs: Clinical Pharmacology and Practical Prescribing (2nd ed.). Elsevier. pp. 156–157. ISBN 978-0-7020-7442-4. Archived from the original on 2021-05-22. Retrieved 2021-11-09.
- ^ "Methotrexate Sodium". International Drug Price Indicator Guide. Archived from the original on 11 June 2019. Retrieved 23 August 2016.
- ^ Hamilton, Richart (2015). Tarascon Pocket Pharmacopoeia 2015 Deluxe Lab-Coat Edition. Jones & Bartlett Learning. p. 464. ISBN 9781284057560.
- ^ "The Top 300 of 2020". ClinCalc. Archived from the original on 12 February 2021. Retrieved 11 April 2020.
- ^ "Methotrexate - Drug Usage Statistics". ClinCalc. Archived from the original on 8 July 2020. Retrieved 11 April 2020.
|
| |
|
| |
| Clinical data | |
|---|---|
| Pronunciation | /ˌmɛθəˈtrɛkˌseɪt, ˌmiː-, -θoʊ-/ [1] [2] [3] |
| Trade names | Trexall, Rheumatrex, Otrexup, others [4] |
| Other names | MTX, amethopterin |
| AHFS/ Drugs.com | Monograph |
| MedlinePlus | a682019 |
| License data |
|
|
Pregnancy category |
|
|
Routes of administration | By mouth, intravenous (IV), intramuscular (IM), subcutaneous injection (SC), intrathecal |
| Legal status | |
| Legal status | |
| Pharmacokinetic data | |
| Bioavailability | 60% at lower doses, less at higher doses. [5] |
| Protein binding | 35–50% (parent drug), [5] 91–93% (7-hydroxymethotrexate) [6] |
| Metabolism | Liver and intracellular [5] |
| Elimination half-life | 3–10 hours (lower doses), 8–15 hours (higher doses) [5] |
| Excretion | Urine (80–100%), faeces (small amounts) [5] [6] |
| Identifiers | |
| |
| Chemical and physical data | |
| Formula | C20H22N8O5 |
| Molar mass | 454.447 g·mol−1 |
| 3D model ( JSmol) | |
| |
| |
| (verify) | |
Methotrexate (MTX), formerly known as amethopterin, is a chemotherapy agent and immune system suppressant. [4] It is used to treat cancer, autoimmune diseases, ectopic pregnancy, and for medical abortions. [4] Types of cancers it is used for include breast cancer, leukemia, lung cancer, lymphoma, gestational trophoblastic disease, and osteosarcoma. [4] Types of autoimmune diseases it is used for include psoriasis, rheumatoid arthritis, and Crohn's disease. [4] It can be given by mouth or by injection. [4]
Common side effects include nausea, feeling tired, fever, increased risk of infection, low white blood cell counts, and breakdown of the skin inside the mouth. [4] Other side effects may include liver disease, lung disease, lymphoma, and severe skin rashes. [4] People on long-term treatment should be regularly checked for side effects. [4] It is not safe during breastfeeding. [4] In those with kidney problems, lower doses may be needed. [4] It acts by blocking the body's use of folic acid. [4]
Methotrexate was made in 1947, and initially came into medical use to treat cancer, as it was less toxic than the then-current treatments. [8] In 1956 it provided the first cures of a metastatic cancer. [9] It is on the World Health Organization's List of Essential Medicines. [10] Methotrexate is available as a generic medication. [4] It is not expensive. [11] The wholesale cost as of 2014 in the developing world is between US$0.06 and US$0.36 per day for the form taken by mouth. [12] In the United States, a typical month of treatment costs $25 to $50. [13] In 2017, it was the 117th most commonly prescribed medication in the United States, with more than six million prescriptions. [14] [15]
- ^ "methotrexate – definition of methotrexate in English from the Oxford dictionary". OxfordDictionaries.com. Archived from the original on 2015-12-04. Retrieved 2016-01-20.
- ^ "methotrexate". Merriam-Webster.com Dictionary.
- ^ "methotrexate". Dictionary.com Unabridged (Online). n.d.
- ^ a b c d e f g h i j k l m n o "Methotrexate". The American Society of Health-System Pharmacists. Archived from the original on 2016-10-08. Retrieved 22 Aug 2016.
- ^ a b c d e "Trexall, Rheumatrex (methotrexate) dosing, indications, interactions, adverse effects, and more". Medscape Reference. WebMD. Archived from the original on 8 February 2014. Retrieved 12 April 2014.
- ^ a b Bannwarth B, Labat L, Moride Y, Schaeverbeke T (January 1994). "Methotrexate in rheumatoid arthritis. An update". Drugs. 47 (1): 25–50. doi: 10.2165/00003495-199447010-00003. PMID 7510620.
- ^ "WHOCC - ATC/DDD Index". www.whocc.no. Archived from the original on 6 November 2020. Retrieved 21 September 2020.
- ^ Sneader, Walter (2005). Drug Discovery: A History. John Wiley & Sons. p. 251. ISBN 9780470015520. Archived from the original on 2017-02-16.
- ^ "Today's anti-cancer tools are ever better wielded". The Economist. 14 September 2017. Archived from the original on 15 May 2018. Retrieved 16 September 2017.
-
^
World Health Organization (2019). World Health Organization model list of essential medicines: 21st list 2019. Geneva.
hdl:
10665/325771. WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO.
{{ cite book}}: CS1 maint: location missing publisher ( link) - ^ Hitchings, Andrew; Lonsdale, Dagan; Burrage, Daniel; Baker, Emma (2019). The Top 100 Drugs: Clinical Pharmacology and Practical Prescribing (2nd ed.). Elsevier. pp. 156–157. ISBN 978-0-7020-7442-4. Archived from the original on 2021-05-22. Retrieved 2021-11-09.
- ^ "Methotrexate Sodium". International Drug Price Indicator Guide. Archived from the original on 11 June 2019. Retrieved 23 August 2016.
- ^ Hamilton, Richart (2015). Tarascon Pocket Pharmacopoeia 2015 Deluxe Lab-Coat Edition. Jones & Bartlett Learning. p. 464. ISBN 9781284057560.
- ^ "The Top 300 of 2020". ClinCalc. Archived from the original on 12 February 2021. Retrieved 11 April 2020.
- ^ "Methotrexate - Drug Usage Statistics". ClinCalc. Archived from the original on 8 July 2020. Retrieved 11 April 2020.