INN monograph
Methotrexate
Therapeutic agent (verify pharmacological class) · POM
Source-linked · Updated 03 Aug 2026 · Source: Local active-ingredient clinical extract; RxNorm (NLM RxNav); PubChem; Professional class pharmacology (Therapeutic agent (verify pharmacological class))
Kenya market
Wholesale / list prices where loaded
Risk first
Contraindications
- Hypersensitivity to the active substance or excipients.
- Additional absolute contraindications are indication- and product-specific — consult SmPC.
Precautions
- Should be used in the treatment of neoplastic diseases in pregnancy only when the potential benefit outweighs the risk to the fetus
- pregnancy should be avoided if either partner is on the drug.
- 8, 10a, 20
Point of care
Dosing
Adult
Orally or IM, 15-30 mg daily x 5/7. This is repeated for 3-5 times with rest periods of at least one week interjected between courses, until any manifesting toxic symptoms subside. Consult specialist literature for further information.
Paediatric
See label paediatric section if present; otherwise use paediatric formulary — do not extrapolate adult doses.
Renal
Review renal impairment dosing; many agents need CrCl/eGFR adjustment.
- CrCl 0–120: Confirm renal dosing in product SmPC / primary label.
Hepatic
Review hepatic impairment dosing; monitor LFTs if agent is hepatically cleared or hepatotoxic.
Safety
Drug interactions
- Professional use: confirm indication, dose, duration, monitoring and patient counselling points against current Kenya STG / EML and the product SmPC.
- Document allergy status and key interactions.
Safety
Adverse effects
- Ulcerative stomatitis
- leukopenia
- anorexia
- vomiting
- abdominal distress
- asthenia
- chills and fever
- dizziness
- decreased resistance to infection
- gingivitis
- pharyngitis
- diarrhoea
- hematemesis
- GI ulceration and bleeding
Use
Indications
- Gestational choriocarcinoma, chorioadenoma destruens
- hydatidiform mole
- acute lymphocytic leukemia
- meningeal leukemia
- breast cancer
- epidermoid cancers of the head and neck
- advanced mycosis fungoides
- lung cancer, particularly squamous cell and small cell types
- non-Hodgkin's lymphomas
- non-metastatic osteosarcoma
- severe, recalcitrant, disabling psoriasis
- severe, active, classical or definite rheumatoid arthritis unresponsive to conventional therapy.
Pharmacology
Mode of action
It reversibly inhibits dihydro-folate reductase an enzyme that reduces folic acid to tetrahydrofolic acid.
Full mechanism text
It reversibly inhibits dihydro-folate reductase an enzyme that reduces folic acid to tetrahydrofolic acid. Inhibition of tetrahy-drofolate formation limits the accessibility of one-carbon fragments necessary for synthesis of purines and the conversion of deoxyuridylate to thymidylate in the synthesis of DNA and cell reproduction
ADME
Pharmacokinetics & PD
| Onset | Product-specific |
|---|---|
| Duration | Product-specific |
| Route | See product SmPC |
| Elimination | are product-specific. Consider food effects, protein binding, hepatic CYP/UGT |
| Half-life | when adjusting for organ impairment, age and drug interactions. Verify parameters in the current SmPC. |
Full PK/PD text
Absorption, distribution, metabolism and excretion are product-specific. Consider food effects, protein binding, hepatic CYP/UGT metabolism, renal clearance and half-life when adjusting for organ impairment, age and drug interactions. Verify parameters in the current SmPC.
Kenya
Brands & prices
| Brand | Company | Pack | KES |
|---|---|---|---|
| METHOTREXATE | DAIMA BIASHARA / Wholesale Import | 2.5MG 30*S (TREXGLO) | 432.15 |
Special populations
Pregnancy & lactation
Pregnancy
Use only if potential benefit justifies potential risk; prefer agents with better reproductive data when alternatives exist.
Lactation
Assess infant risk vs benefit of maternal therapy; prefer agents with lactation data.
Diet
Food & alcohol
- Food
- Food
Trust
Sources & disclaimer
Source: Local active-ingredient clinical extract; RxNorm (NLM RxNav); PubChem; Professional class pharmacology (Therapeutic agent (verify pharmacological class))
Clinical review date not recorded.
Decision support only — not a substitute for clinical judgment, product SmPC, or Kenya STG/EML.