Adverse Drug Reaction Classification System

Pharmaceutical Information
Drug Name Methotrexate
Drug ID BADD_D01418
Description Methotrexate is a folate derivative that inhibits several enzymes responsible for nucleotide synthesis.[A180322] This inhibition leads to suppression of inflammation as well as prevention of cell division.[A180322] Because of these effects, methotrexate is often used to treat inflammation caused by arthritis or to control cell division in neoplastic diseases such as breast cancer and non-Hodgkin's lymphoma.[A180322,L7144,L7147,L7150,L7180] Due to the toxic effects of methotrexate, it is indicated for treatment of some forms of arthritis and severe psoriasis only if first line treatment has failed or patients are intolerant of those treatments.[L7180] Methotrexate was granted FDA approval on 7 December 1953.[L7198]
Indications and Usage Methotrexate is indicated in the treatment of gestational choriocarcinoma, chorioadenoma destruens and hydatidiform mole. In acute lymphocytic leukemia, methotrexate is indicated in the prophylaxis of meningeal leukemia and is used in maintenance therapy in combination with other chemotherapeutic agents. Methotrexate is also indicated in the treatment of meningeal leukemia. Methotrexate is used alone or in combination with other anticancer agents in the treatment of breast cancer, epidermoid cancers of the head and neck, advanced mycosis fungoides (cutaneous T cell lymphoma), and lung cancer, particularly squamous cell and small cell types. Methotrexate is also used in combination with other chemotherapeutic agents in the treatment of advanced stage non-Hodgkin’s lymphomas. Methotrexate is indicated in the symptomatic control of severe, recalcitrant, disabling psoriasis. Methotrexate is indicated in the management of selected adults with severe, active rheumatoid arthritis (ACR criteria), or children with active polyarticular-course juvenile rheumatoid arthritis.
Marketing Status Prescription; Discontinued
ATC Code L01BA01; L04AX03
DrugBank ID DB00563
KEGG ID D00142
MeSH ID D008727
PubChem ID 126941
TTD Drug ID D0SV8E
NDC Product Code 59137-530; 0703-3671; 59137-550; 0703-3678; 52652-2001; 0143-9516; 0143-9830; 61703-408; 69238-1423; 51285-367; 49452-4601; 66220-812; 66220-810; 0143-9519; 70518-1398; 0143-9517; 61703-350; 16729-277; 66220-822; 54436-012; 59137-535; 59137-540; 59137-510; 70771-1058; 54436-022; 70518-3263; 66220-817; 59137-520; 0703-3675; 54436-020; 51407-121; 51079-670; 71335-1772; 58623-0040; 0143-9367; 46014-1005; 50090-5457; 71335-0782; 42291-505; 59137-525; 0143-9518; 46014-1023; 0904-7141; 51285-369; 51927-1565; 54436-025; 0378-0014; 68382-775; 66220-815; 71335-1118; 59651-182; 66220-820; 59137-505; 59137-515; 63660-0006; 12780-0491; 51285-366; 66220-825; 54436-017; 46014-1133; 66220-807; 51285-368; 16729-486; 54436-010; 0555-0572; 54436-015; 50268-527
Synonyms Methotrexate | Amethopterin | Methotrexate, (D)-Isomer | Methotrexate, (DL)-Isomer | Mexate | Methotrexate Sodium | Sodium, Methotrexate | Methotrexate, Sodium Salt | Methotrexate, Disodium Salt | Methotrexate Hydrate | Hydrate, Methotrexate | Methotrexate, Dicesium Salt | Dicesium Salt Methotrexate
Chemical Information
Molecular Formula C20H22N8O5
CAS Registry Number 59-05-2
SMILES CN(CC1=CN=C2C(=N1)C(=NC(=N2)N)N)C3=CC=C(C=C3)C(=O)NC(CCC(=O)O)C(=O)O
Chemical Structure
ADR Related Proteins Induced by Drug
ADR Term Protein Name UniProt AC TTD Target ID PMID
ApoptosisCellular tumor antigen p53P04637T157399681674; 16445776; 9358758
ApoptosisThymidine kinase, cytosolicP04183T300813252959; 1626950
Chromosomal abnormalities and abnormal gene carriersUracil-DNA glycosylaseP13051Not Available12167490; 11425516; 10871356
DeathAlanine aminotransferase 2Q28DB5Not Available10461859; 9013204; 8742516
DeathAspartate aminotransferase, cytoplasmicP17174T3336710461859; 9013204; 8742516
EnterocolitisGlutathione peroxidase 3P23764Not Available3138440
HepatotoxicityDiazepam-binding inhibitor-like 5P56702Not Available25912852
HepatotoxicityCatalaseP04762Not Available25912852
HepatotoxicityTumor necrosis factorP16599Not Available25912852
HepatotoxicityNitric oxide synthase, inducibleQ06518Not Available25912852
HepatotoxicityGlutathione peroxidase 1P04041Not Available25912852
HepatotoxicitySuperoxide dismutase [Cu-Zn]P07632Not Available25912852
Intestinal angioedemaGlutathione peroxidase 3P23764Not Available3138440
Liver injuryLysosome-associated membrane glycoprotein 1P11279T311458915142; 15787813; 15787812; 8731673; 8864370; 7577576
Nephropathy toxicTumor necrosis factorP16599Not Available25912852
Nephropathy toxicNitric oxide synthase, inducibleQ06518Not Available25912852
Nephropathy toxicGlutathione peroxidase 1P04041Not Available25912852
Nephropathy toxicSuperoxide dismutase [Cu-Zn]P07632Not Available25912852
Nephropathy toxicDiazepam-binding inhibitor-like 5P56702Not Available25912852
Nephropathy toxicCatalaseP04762Not Available25912852
Traumatic lung injuryPulmonary surfactant-associated protein DP35247T3586212135181; 12322797; 9330247
ADRs Induced by Drug
ADR Term ADReCS ID ADR Frequency (FAERS) ADR Severity Grade (FAERS) ADR Severity Grade (CTCAE)
Dehydration14.05.05.001--
Dementia19.20.02.001; 17.03.01.001--Not Available
Demyelination17.16.02.0010.000560%Not Available
Depressed level of consciousness17.02.04.002--
Depressed mood19.15.02.001--Not Available
Depression19.15.01.001--
Dermatitis23.03.04.002--Not Available
Dermatitis allergic10.01.03.014; 23.03.04.003--Not Available
Dermatitis bullous23.03.01.002--
Dermatitis exfoliative23.03.07.001; 10.01.01.004--
Diabetes mellitus14.06.01.001; 05.06.01.001--Not Available
Diarrhoea07.02.01.001--
Diarrhoea haemorrhagic24.07.02.004; 07.02.01.002--Not Available
Diffuse large B-cell lymphoma16.28.02.001; 01.15.02.0010.003506%Not Available
Diplegia17.01.04.015--Not Available
Discomfort08.01.08.003--Not Available
Disseminated intravascular coagulation24.01.01.010; 01.01.02.002--
Disseminated tuberculosis11.04.01.0010.000146%Not Available
Disturbance in attention19.21.02.002; 17.03.03.001--
Diverticulitis11.01.07.003; 07.10.02.0010.003640%Not Available
Diverticulum07.10.01.001--Not Available
Dizziness17.02.05.003; 24.06.02.007; 02.01.02.004--
Drug abuse19.07.02.010--Not Available
Drug eruption08.01.06.015; 23.03.05.001; 10.01.01.0050.004200%Not Available
Drug hypersensitivity10.01.01.0010.617923%Not Available
Dry eye06.08.02.0010.004480%
Dry mouth07.06.01.002--
Dry skin23.03.03.001--
Dysarthria19.19.03.001; 17.02.08.001--
Dysgeusia17.02.07.003; 07.14.03.001--
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