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Active substance(s): METHOTREXATE

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Patient Information Leaflet


Methotrexate 100 mg/ml solution for injection

Read all of this leaflet carefully before this medicine is administered to you because it contains important
information for you.
• Keep this leaflet. You may need to read it again.
• If you have further questions, ask your doctor, pharmacist or nurse.
• This medicine has been prescribed for you only. Do not pass it on to others. It may harm them,
even if their signs of illness are the same as yours.
• If you get any side effects talk to your doctor, pharmacist or nurse.This includes any possible side
effects not listed in this leaflet. See section 4.
• Disease-modifying antirheumatic drugs (DMARD;
What is in
drugs that are used to treat rheumatoid arthritis)
this leaflet:
• probenecid (uricosuric agent used in the
1. What Methotrexate 100 mg/ml solution for
prophylaxis of gout)
injection is and what it is used for
• p-aminobenzoic acid (used in sun creams)
2. What you need to know before
• non-steroidal anti-inflammatory drugs (NSAIDs
Methotrexate 100 mg/ml solution for injection
3. How Methotrexate 100 mg/ml solution for
indomethacin, ibuprofen)
injection is administered
• anti-folate drugs (e.g. nitrous oxide or co4. Possible side effects
5. How to store Methotrexate 100 mg/ml solution
• p-aminohippuric acid (substance to check kidney
for injection
6. Contents of the
• pyrimethamine (medication against malaria)
1. What Methotrexate 100 mg/ml solution for
injection is and what it is used for
Methotrexate is one of a group of medicines known
as antimetabolites. It is used in the treatment of
cancer, as well as psoriasis. It stops a substance
called dihydrofolate reductase from working. This
substance is an enzyme, which is important in “cell
growth (replication)”. By inhibiting the enzyme,
cancer cells will eventually “die”.
Methotrexate helps patients with psoriasis by killing
the cells in the skin that are growing too fast. It is
these rapidly growing cells that cause the raised
patches of skin in psoriasis.
2. What you need to know before receiving
Methotrexate 100 mg/ml solution for
Do NOT use Methotrexate
100 mg/ml solution for injection
• if you have ever had any allergic reaction to
methotrexate or any of the ingredients of this
• if you have severe problems with your
• if you have severe problems with your liver
including alcoholic liver disease, abnormal
blood counts, fibrosis, cirrhosis or recent active
• if you suffer from alcoholism
• if you have any serious blood disorders (anaemia,
a reduction in white cell number (leucopenia) or
platelet number (thrombocytopenia))
• if you have an active infection
• if you have a medical condition or are receiving
medication, which lowers your resistance to
• if you are pregnant or intend to become
pregnant, or are breast-feeding, as the drug
can harm unborn and breast-fed infants.
Warnings and precautions
Talk to your doctor, pharmacist or nurse before using
100 mg/ml solution for injection
• if you have impaired respiratory function
• if you have mild to moderate kidney or liver
problems, or a mild to moderate blood disorder
• if you have diarrhoea
• if you have ulcers in your mouth, stomach or
intestine (large bowel)
• if you have ascites (collection of liquid in the
free abdominal cavity) and/or pleural effusions
(collection of liquid in the pleural cavity)
• if you are receiving or intend to receive any
vaccine, as methotrexate can reduce their effect
• if you have had radio- or chemotherapy before
(especially of the pelvis), or are receiving
radiotherapy concurrently
• if you have an impaired general condition (if you
feel weak or infirm)
• if you are of advanced age
• if Methotrexate 100 mg/ml solution for injection is
given to very young children.
This medicinal product contains 0.45 mmol (or
10.4 mg) sodium per ml. To be taken into
consideration by patients on a controlled sodium
Please consult your doctor, even if these
statements were applicable to you at any time
in the past.
Other medicines and
Methtrexate 100 mg/ml
solution for injection
Tell your doctor, pharmacist or nurse, if you are
taking, have recently taken, or might take any
other medicines, including medicines obtained
without a prescription.
Medications which can be influenced by or can
influence the effect of methotrexate negatively
• pain-killers such as salicylates (e.g. aspirin),
amidopyrine derivatives, phenylbutazone and
• diphenylhydantoins
antiepileptic agent)
• barbiturates and tranquillisers (sedative agents)
• antibiotics (medication against bacteria), e.g.
cotrimoxazole and sulphonamides
• cytostatics (medication against cancer), e.g.
cytarabine, doxorubicin, mercaptopurine,
procarbazine, cisplatin, L-asparaginase and 5fluorouracil
2005_043_03_PB_Methotrexate 100 mgml.indd


• cholestyramine (lipid-lowering agent)
• acitretin or other retinoids (for psoriasis or skin
• theophylline (used mainly in bronchial asthma)
• erythrocyte concentrates (for blood transfusion)
• nitrous oxide-based anaesthetics
• Proton pump inhibitors (used in the therapy of
gastric ulcers) e.g. omeprazole, esomeprazole,
lansoprazole, pantoprazole and rabeprazole
• sulphasalazine (for ulcerative colitis)
• tetrahydrofolic acid preparations
• oral antidiabetics (medications to treat diabetes)
and diuretics (increase urine output)
• hypoglycaemics (lower blood sugar levels)
• other medicinal products with nephrotoxic and
hepatotoxic potential (incl. alcohol)
• vaccinations
• azathioprine (an immunosuppressive drug)
• vitamin preparations containing folic acid or its
Please note that these statements may also apply
to products used some time ago or at some time
in the future.
Pregnancy and breast-feeding
Do not take Methotrexate 100 mg/ml solution for
injection if you are pregnant because it causes
a variety of malformations or even the death of
the foetus. Women must not get pregnant during
treatment with Methotrexate 100 mg/ml solution
for injection. If you get pregnant during treatment
with Methotrexate 100 mg/ml solution for injection,
please inform your doctor immediately!
Special indications for contraception:
Methotrexate temporarily influences sperm and
egg production. During treatment and up to
6 months after treatment is stopped, you must
practice effective contraception. In this respect, it
is of no importance whether the male or the female
partner takes Methotrexate 100 mg/ml solution for
Do not take Methotrexate 100 mg/ml solution for
injection during breast-feeding, since methotrexate
is excreted into the breast milk. Methotrexate can
seriously harm breast-fed infants.
3. How Methotrexate 100 mg/ml solution for
injection is administered
Your doctor will decide on a suitable dose for you.
Doses vary considerably and will depend on the
underlying disease.
Your doctor may instruct you to take sodium
bicarbonate or acetazolamide tablets while
receiving your injections to help make sure that
methotrexate is not concentrated in the kidneys.
If you receive methotrexate in high doses, you will
receive calcium folinate as well to lessen the side
effects of methotrexate.
It is possible that you will only get methotrexate.
In the case of cancer, it is also possible that you
will receive so-called combination therapy in which
you must take several medications.
Your body weight, age, general condition of health,
your response to the drug and whether other
medicines are required at the same time will also
influence the dose you receive.
Method of Administration
Your doctor or nurse will give you Methotrexate
100 mg/ml solution for injection injecting it either
into one of your veins (e.g. as bolus or infusion),
arteries, or a muscle.
Tests during treatment with Methotrexate
During your treatment, you will have a number
of tests, such as regular blood tests to check
that appropriate blood levels of methotrexate are
attained and that your kidneys are eliminating
excess drug properly.
Other tests are performed routinely at the start and
during the course of therapy (e.g. chest X-ray, liver
function test, full blood count and urinalysis).
4. Possible Side Effects
Like all medicines Methotrexate 100 mg/ml solution
for injection can cause side effects although not
everybody gets them.
The frequency of side effects is classified into the
following categories:

in more than 1 in 10 patients

in more than 1 in 100 patients, but
less than 1 in 10 patients
Uncommon in more than 1 in 1,000 patients,
but less than 1 in 100 patients
in more than 1 in 10,000 patients,
but less than 1 in 1,000 patients
Very rare
in less than 1 in 10,000 patients,
including isolated reports
Not known cannot be estimated from the
available data
Methotrexate has the potential for serious,
sometimes fatal toxicity. Because the toxic reactions
can occur at any time during therapy, your doctor
should observe you closely and must inform you of
early signs and symptoms of toxicity.
If you think you have an infection, a sore throat,
fever or chills during treatment, you should tell
your doctor immediately.

2005_043_03_PB_Methotrexate 100 mgml.indd


redness and inflammation
The most common undesirable effects are
ulcerative stomatitis, leucopenia, nausea, and Uncommon: Loss
abdominal discomfort.
photosensitivity, pigmentary changes
(discolouration of the skin), loss of
Undesirable effects of Methotrexate 100 mg/ml
skin tissue
solution for injection are
Acne, an increase in rheumatic
nodules, increased colouration or
Uncommon: Lymphoma
inflammation or detachment of the
Very rare: Tumour lysis syndrome (renal failure
nails, nodulosis (formation of nodules
due to massive destruction of rapidly
under the skin)
growing tumour cells)
Very rare: Telangiectasia (expansion of small
Blood disorders
superficial blood vessels in the
Common: Blood picture changes - e.g. your
skin), worsening of psoriasis (with
vulnerability for infections may
concomitant UV therapy), formation
increase, you may suffer from unusual
of boils, a „recall“ of radiation
bleeding or bruising and you may
dermatitis (inflammation of the skin)
observe signs of anaemia (weakness,
and sunburn
tiredness, difficulties in breathing)
Musculoskeletal disorders
Immune system disorder
Uncommon: Osteoporosis, pain in the joints,
Uncommon: Allergic
muscle pain
resistance to infection
Very rare: Aseptic necrosis of the femoral head
Metabolism and endocrine disorders
(loss of bone tissue in the hip joint)
Uncommon: Diabetes
Renal and urinary disorders
Hyperuricaemia (increased blood Common: Impairment of renal function
levels of uric acid, possibly leading to Uncommon: Renal failure, inflammation of the
urinary bladder, pain or difficulty in
Psychiatric disorders
passing urine
Mood swings, irritability
Very rare: Blood in the urine
Nervous system disorders
Pregnancy and lactation
Common: Headache, drowsiness, sleepiness
Uncommon: Malformations of the foetus
Uncommon: Seizures,
leucoencephalopathy Rare:
(inflammation of the brain), manifested Reproductive and breast disorders
by ventricular enlargement (expansion
Uncommon: Vaginal discomfort
of the fluid spaces inside the brain),
Menstrual dysfunction (periods may
incomplete palsy affecting one or
become less frequent or even stop
both sides of the body, confusion,
Very rare: Reduced or faulty formation of sperm
Speech disorder, subtle cognitive
and egg cells, infertility, loss of interest
in sex / impotence, development of
attention), mental disturbance
the breast gland in males
Very Rare: Unusual sensations in the head,
pain, paraesthesia (pins-and-needles General disorders
weakness, Uncommon: Fever without any detectable cause
Chills, malaise and undue fatigue,
deficit, Rare:
dementia, cerebral oedema (swelling
of the brain) after administration into Very rare: Sudden death
the central nervous system possibly In cases of acute lymphocytic leukaemia,
leading to vomiting, fits, coma and methotrexate can cause pain in the left epigastric
even death
region (the area overlying the stomach, below the
left lower border of the rib cage; inflammation of
Eye disorders
the space above the spleen due to destruction of
Impairment of vision
Very rare: Swelling, inflammation of the eyelid the leukaemic cells).
edges, conjunctivitis (inflammation There have been reports on the manifestation of
of the eye conjunctiva), unusual lymphomas which were, in some cases, reversible
after discontinuing methotrexate therapy. The
formation of tears, photophobia
potential of methotrexate to produce other cancers
Ear disorders
in humans has been evaluated in several studies,
Ringing in the ears
but the results do not confirm a cancerogenic risk.
Cardiac disorders
Low blood pressure, pericarditis
(inflammation of the outer lining of
Reporting of side effects
the heart), pericardial effusion and
tamponing (collection of fluid and
blood, respectively, in the space If you get any side effects, talk to your doctor, pharmacist or
between the outer lining of the heart nurse: This includes any possible side effects not listed in this
leaflet. You can also report side effects directly via the Yellow
and the heart muscle)
Card Scheme – website:
Vascular disorders
Uncommon: Vasculitis (inflammation of blood Alternatively you can call Freephone 0808 100 3352 (available
from 10 a.m. to 2 p.m. Mondays to Fridays) or fill in a paper
Haematoma, point-like or small flat form available from your local pharmacy. By reporting side
bleeding, complications
resulting effects you can help provide more information on the safety of
from the formation of blood clots in this medicine.
veins and arteries
Lung disorders
Common: Inflammation and fibrosis (increase in 5. How to store Methotrexate 100 mg/ml
the connective tissue); the pulmonary
solution for injection
toxicity may manifest as fever, cough • Keep the medicine out of the reach and sight of
(especially dry and nonproductive), children.
difficulties or increase in the • Keep the vial in the outer carton in order to
frequency of breathing, chest pain, protect from light.
hypoxaemia (lack of oxygen in the • Do not store above 25°C.
blood), and/or abnormal findings on
• For single dose use only. Discard any unused
chest radiography and/or tests of solution immediately and safely after initial use.
respiratory function
• This medicine should only be administered by a
Upper respiratory tract infection
medically qualified person, e.g. a doctor.
Gastro-intestinal disorders
• Methotrexate 100 mg/ml solution for injection
should not be used after the expiry date printed
common: Disorders of the mouth, stomach on the label.
and intestines like mucositis (mucus • Any unused product or waste should be disposed
e.g. of in accordance with local requirements for
inflammation of the gums, tongue, example by incineration.
throat, mouth, intestines), lack of
appetite, feeling sick
Common: Diarrhoea
Uncommon: Vomiting, gastrointestinal ulcerations,
inflammation of the pancreas
uptake of nutrition with consequences
such as body weight loss), melaena
(red to black stools)
Very rare: Unusual bleeding from the mouth,
stomach and intestines, increased risk
of perforation and toxic megacolon
(severe complication with massive
dilatation of the colon and severe
Liver and gall bladder disorders
Uncommon: Fibrosis (increase in the connective
tissue), cirrhosis
of the tissue with hardening and
abolition of the normal structure of the
organ), fatty degeneration of the liver
or other histologic (tissue) changes in
the liver
Hepatitis (inflammation of the liver)
Very rare: Acute liver cell death
Skin disorders
Common: Rash, itching, formation of blisters,

2005_043_03_PB_Methotrexate 100 mgml.indd


Contents of the
What Methotrexate 100 mg/ml solution for
injection contains
The active substance is methotrexate.
Each 1 ml of this sterile solution for injection
contains 100 milligrams methotrexate.
The other ingredients are sodium hydroxide, water
for injections and nitrogen.
What Methotrexate 100 mg/ml solution for
injection looks like and contents of the pack
Methotrexate 100 mg/ml solution for injection is an
orange-yellow and sterile solution in clear glass
The solution for injection is available in packs of
1 vial containing 50 ml solution.
Not all pack sizes may be marketed.
Marketing Authorisation Holder
hameln pharmaceuticals ltd
Gloucester, United Kingdom
Haupt Pharma Wolfratshausen GmbH
Pfaffenrieder Str. 5
82515 Wolfratshausen
This leaflet was last approved in August
2012December 2014

2005_043_03_PB_Methotrexate 100 mgml.indd


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