Buy Methotrexate
Methotrexate

0.73
A powerful medication used once weekly for various autoimmune conditions and certain types of cancer.


Ingredient
Availability
In Stock
Delivery
Airmail (14-21 days) | EMS trackable (5-9 days)
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Product Sheet

Alternative/Local Brand
Maxtrex
Active Ingredient(s)
Methotrexate
Primary Category
Immunosuppressant, Chemotherapy
Therapeutic Class
Antineoplastic and immunomodulating agents, Antimetabolites, Folic acid analogues
Pharmacological Class
Folic Acid Antagonists
Indications
Rheumatoid arthritis, Psoriasis, Crohn's disease, Leukaemia
Contraindications
Pregnancy, Severely impaired liver function, Severely impaired kidney function, Current infections
Minor Side Effects
Nausea, Stomach upset, Fatigue, Mild hair thinning
Moderate Side Effects
Mouth ulcers, Changes in liver enzymes, Diarrhoea, Skin sensitivity to light
Serious Side Effects
Low white blood cell count, Liver damage, Lung inflammation, Severe skin reactions
Dosage Forms
Tablet, Injection
Administration Route
Oral
Mechanism of Action
Methotrexate slows down the body's immune system and reduces inflammation. In higher doses, it stops the growth of cancer cells by interfering with their DNA production.
Prescription Status
Rx
Manufacturer
Pfizer
Patient Summary
A powerful medication used once weekly for various autoimmune conditions and certain types of cancer.
Onset Time
3-6 weeks for arthritis symptoms
Duration
Weekly dosing
Storage Instructions
Store below 25°C in a dry place.
Drug Interactions
NSAIDs, Penicillin, Trimethoprim, Protopn pump inhibitors
Age Restrictions
Dose must be carefully calculated by a specialist for children
Pregnancy Use
Strictly contraindicated; highly teratogenic.
Alternative Drugs
Leflunomide, Sulfasalazine, Azathioprine

Methotrexate: Generic Medication Overview

Methotrexate is a prescription-only medication used in Hong Kong for both autoimmune disorders and certain cancers. It belongs to the therapeutic categories of Autoimmune Support and Oncology Support. The medication is available as a pill (tablet) containing 2.5 mg of the active ingredient methotrexate. In Hong Kong, methotrexate is regulated under the Pharmacy and Poisons Ordinance and may be dispensed only with a qualified healthcare-provider’s prescription.

How Methotrexate Works in the Body

Methotrexate is a folate antagonist. It blocks the enzyme dihydrofolate reductase, which is essential for converting folic acid into tetrahydrofolate-a co-factor required for the synthesis of purines and thymidylate. By limiting these building blocks, methotrexate interferes with DNA, RNA, and protein synthesis, a mechanism that is especially effective against rapidly dividing cancer cells.

At lower weekly doses used for autoimmune conditions, methotrexate also increases extracellular adenosine levels. Adenosine acts as an anti-inflammatory mediator, dampening the activity of immune cells such as T-lymphocytes and neutrophils. This dual action-antiproliferative and anti-inflammatory-explains methotrexate’s efficacy in both oncology and immune-mediated diseases.

Conditions Treated by Methotrexate

Autoimmune Indications

  • Rheumatoid arthritis (RA): Reduces joint inflammation, pain, and structural damage.
  • Severe plaque psoriasis: Controls skin lesions when topical therapies are insufficient.

Oncology Indications

  • Acute lymphoblastic leukaemia (ALL): Part of multi-agent chemotherapy protocols.
  • Non-Hodgkin lymphoma: Used in combination regimens.
  • Breast cancer, osteosarcoma, and choriocarcinoma: Administered at higher doses under specialist supervision.

These indications are approved by the Hong Kong Department of Health and reflect the drug’s dual role in modulating the immune system and inhibiting malignant cell growth.

Evidence-Based Off-Label Uses

Research has investigated methotrexate for several conditions that are not formally approved in Hong Kong:

  • Juvenile idiopathic arthritis (JIA): Randomised trials demonstrate improvement in joint counts and functional scores.
  • Inflammatory bowel disease (IBD) - Crohn’s disease: Small-scale studies suggest benefit as a steroid-sparing agent.

Because these uses are off-label, they require careful clinical judgment and close monitoring. Off-label use must be overseen by a qualified healthcare provider and patients should be informed of the experimental nature of the therapy.

Who Should (and Should Not) Use Methotrexate?

Absolute Contra-Indications

  • Known hypersensitivity to methotrexate or any tablet excipients.
  • Pregnancy (any trimester) and lactation - methotrexate is teratogenic and can be excreted in breast milk.
  • Severe liver disease (e.g., cirrhosis, persistent transaminase elevation >3 × upper limit).
  • Uncontrolled active infection (including tuberculosis).

Relative Contra-Indications

  • Moderate renal impairment (creatinine clearance <30 mL/min).
  • Chronic alcohol use (increases risk of hepatotoxicity).
  • Pre-existing pulmonary disease (methotrexate-induced pneumonitis risk).
  • Concomitant use of other cytotoxic agents or strong folate antagonists.

Special Populations

  • Children: Low-dose oral methotrexate is approved for specific paediatric cancers and JIA under specialist care.
  • Elderly: Dose adjustments may be required due to reduced renal and hepatic reserve.
  • Patients of reproductive age: Effective contraception is mandatory during treatment and for at least three months after the last dose.

Safety Profile: Side Effects and Interactions

Common Side Effects

  • Nausea or mild vomiting.
  • Stomatitis (mouth sores) and sore throat.
  • Transient elevation of liver enzymes.
  • Fatigue or mild headache.

These effects are usually dose-related and may diminish with folic acid supplementation (commonly 1 mg daily, taken on non-methotrexate days).

Serious Adverse Events

  • Hepatotoxicity: Persistent or severe liver enzyme elevation, potentially progressing to fibrosis or cirrhosis.
  • Bone-marrow suppression: Pancytopenia, leading to infection risk, anemia, or bleeding.
  • Pulmonary toxicity: Acute interstitial pneumonitis that can present with dyspnea, cough, or fever.
  • Renal toxicity: Crystalluria and acute kidney injury, especially with high-dose intravenous regimens.

Any signs of severe toxicity warrant immediate medical evaluation.

Drug Interactions

  • Non-steroidal anti-inflammatory drugs (NSAIDs): May increase methotrexate serum levels by reducing renal clearance.
  • Sulfonamides and trimethoprim-sulfamethoxazole: Heighten risk of bone-marrow suppression.
  • Penicillins (e.g., ampicillin) and tetracyclines: Can interfere with renal excretion.
  • Warfarin: Methotrexate may potentiate anticoagulant effect; INR monitoring is advisable.
  • Live vaccines: Immunosuppression can reduce vaccine efficacy and increase infection risk; avoid during therapy.

Food and Lifestyle Interactions

  • Alcohol: Even modest intake can amplify liver toxicity; limiting alcohol consumption is recommended.
  • Folate-rich foods: Do not replace prescribed folic acid supplementation, but a balanced diet is encouraged.
  • Driving or operating machinery: Methotrexate does not usually impair cognition, but severe fatigue or dizziness should be reported.

If patients are uncertain about any medication, supplement, or herbal product, they should disclose all items to their prescribing clinician.

How to Take Methotrexate

Standard Dosing (Low-Dose, Autoimmune Use)

  • Typical starting dose: 7.5 mg orally once weekly (often three 2.5 mg tablets).
  • Titration: Incremental increases of 2.5 mg every 2-4 weeks may be made up to a maximum of 25 mg per week, guided by clinical response and laboratory monitoring.

Special Populations

  • Renal impairment: Dose reduction is advised; for creatinine clearance <30 mL/min, many clinicians avoid oral methotrexate altogether.
  • Hepatic disease: Initiate at the lowest possible weekly dose and monitor liver enzymes closely.

Administration of the 2.5 mg Pill

  • Swallow the tablet whole with a full glass of water.
  • It may be taken with or without food; some patients prefer taking it with food to lessen gastrointestinal upset.
  • Do not split, crush, or chew the tablet unless specifically instructed.

Missed Dose

  • If a weekly dose is missed, skip the missed dose and resume the regular schedule the following week. Do not take a double dose to “make up” for the missed one.

Overdose Management

  • Symptoms may include severe nausea, vomiting, abdominal pain, and myelosuppression.
  • Immediate emergency care is essential. Administration of leucovorin (folinic acid) rescue can mitigate toxicity, especially after high-dose exposure.

Discontinuation

  • Low-dose weekly methotrexate does not usually require tapering; however, abrupt cessation may lead to disease flare-ups in rheumatoid arthritis. Gradual dose reduction can be considered under professional guidance.

Monitoring and Follow-Up

  • Baseline labs before initiation:

  • Complete blood count (CBC) with differential.

  • Liver function tests (ALT, AST, bilirubin).

  • Serum creatinine and calculated creatinine clearance.

  • Pregnancy test for women of child-bearing potential.

  • Routine monitoring:

  • CBC and liver enzymes every 4-8 weeks for the first three months, then every 8-12 weeks thereafter.

  • Renal function every 8-12 weeks.

  • Pulmonary assessment (history, physical exam, chest X-ray if indicated) at baseline and periodically.

  • Clinical follow-up: Patients should report new respiratory symptoms, persistent fatigue, unexplained bruising, or signs of infection promptly.

Storage and Handling

  • Keep tablets in the original container, tightly closed, at room temperature (15-30 °C).
  • Protect from moisture, heat, and direct sunlight.
  • Keep out of reach of children and pets.
  • Do not use tablets after the expiration date printed on the package.

Medication-Specific Glossary

Folate antagonist
A compound that blocks the utilization of folic acid, thereby impairing DNA and RNA synthesis. Methotrexate belongs to this class.
Polyglutamation
The process by which intracellular methotrexate molecules acquire multiple glutamate residues, prolonging their retention and activity within cells.
Leucovorin rescue
Administration of folinic acid (leucovorin) to bypass the blocked dihydrofolate reductase pathway, used to reduce toxicity after high-dose methotrexate.
Hepatotoxicity
Liver injury caused by a drug, manifesting as elevated enzymes, fibrosis, or cirrhosis.

Medical Disclaimer

This article provides educational information about methotrexate and is not a substitute for professional medical advice. Treatment decisions, including use for unapproved indications, must be made under the guidance of a qualified healthcare provider. The content is intended for informational purposes and does not constitute medical recommendations. Always consult a physician before starting, stopping, or changing any medication regimen.

Methotrexate FAQ

Can I travel with methotrexate and pass airport security?

Methotrexate tablets are permitted in both carry-on and checked luggage. It is advisable to keep the medication in its original pharmacy-labelled container, carry a copy of the prescription, and have a brief physician letter if you are traveling internationally, as some countries require documentation for controlled medications.

Does methotrexate show up on standard drug tests for employment or sports?

Routine workplace drug screens (e.g., urine immunoassays for cannabinoids, opiates, cocaine) do not detect methotrexate. However, targeted testing for chemotherapeutic agents can identify it, and certain sports anti-doping programs may consider it a prohibited substance if used without a therapeutic use exemption.

What does a 2.5 mg methotrexate tablet look like, and how can I identify it?

The 2.5 mg tablets are typically round, white or off-white, and may bear a numeric imprint such as “2.5” or a manufacturer’s logo. Verify the imprint, shape, and packaging against the pharmacy label each time you receive a refill.

Why is methotrexate taken once weekly instead of daily?

Weekly dosing allows sufficient drug exposure to achieve anti-inflammatory effects while minimizing cumulative toxicity, especially bone-marrow suppression. Daily dosing would lead to higher steady-state levels and a markedly increased risk of severe adverse events.

Can I take methotrexate with over-the-counter NSAIDs for pain?

Concurrent NSAIDs can reduce renal clearance of methotrexate, potentially raising blood levels and toxicity risk. Short-term, low-dose NSAID use is sometimes permitted under close monitoring, but patients should discuss any NSAID use with their prescriber before combining the drugs.

How does alcohol consumption affect methotrexate therapy?

Alcohol is metabolised by the liver and can synergistically increase the risk of methotrexate-induced hepatotoxicity. Limiting or avoiding alcohol while on methotrexate is recommended, especially for patients with existing liver enzyme elevations.

Is methotrexate safe to use while breastfeeding?

Methotrexate is excreted in breast milk and can cause fetal toxicity. Health authorities advise against breastfeeding during treatment and for at least three months after the last dose to avoid infant exposure.

What are the differences between oral methotrexate and injectable forms?

Injectable methotrexate (intramuscular or subcutaneous) bypasses gastrointestinal absorption, leading to more predictable serum concentrations, especially at higher doses. Oral forms are convenient for low-dose weekly regimens but may have variable bioavailability in some patients.

How long does it typically take to see improvement in rheumatoid arthritis symptoms?

Clinical improvement often begins within 4-6 weeks of initiating low-dose weekly methotrexate, but maximal benefit may require 3-6 months of steady therapy and dose optimisation. Ongoing monitoring helps assess response and guide adjustments.

Are there any special considerations for methotrexate use in people with chronic kidney disease?

Reduced renal clearance can lead to higher systemic methotrexate levels, increasing the risk of bone-marrow and mucosal toxicity. Dose reduction, extended dosing intervals, or choosing an alternative therapy may be necessary for patients with moderate to severe renal impairment.

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