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METHOTREXATE 2.5MG/ML SOLUTION FOR INJECTION

Active substance(s): METHOTREXATE

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Patient Information Leaflet

hameln

Methotrexate 2.5 mg/ml solution for injection
methotrexate

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.
drugs that are used to treat rheumatoid arthritis)
What is in
• probenecid (uricosuric agent used in the
this
this
prophylaxis of gout)
leaflet:
• p-aminobenzoic acid (used in sun creams)
1. What Methotrexate 2.5 mg/ml solution for
• non-steroidal anti-inflammatory drugs (NSAIDs
injection is and what it is used for
medications
against
"rheumatism",
e.g
2. What you need to know before
receiving
indomethacin, ibuprofen)
Methotrexate 2.5 mg/ml solution for injection
• anti-folate drugs (e.g. nitrous oxide or co3. How Methotrexate 2.5 mg/ml solution for
trimoxazole)
injection is administered
• p-aminohippuric acid (substance to check kidney
4. Possible side effects
function)
5. How to store Methotrexate 2.5 mg/ml solution
for injection
6. Contents of the
pack
and
other
information
1. What Methotrexate 2.5 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 including psoriatic
arthritis. 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 2.5 mg/ml solution for
injection
Do NOT use Methotrexate
2.5 mg/ml solution for injection
• if you have ever had any allergic reaction to
methotrexate or any of the ingredients of this
product
• if you have severe problems with your
kidneys
• if you have severe problems with your liver,
including alcoholic liver disease, abnormal
blood counts, fibrosis, cirrhosis or recent active
hepatitis
• 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
infection
• 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
Methotrexate 2.5 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 2.5 mg/ml solution for injection is
given to very young children.
This medicinal product contains 0.16 mmol (or
3.7 mg) sodium per ml. To be taken into
consideration by patients on a controlled sodium
diet.
Please consult your doctor, even if these
statements were applicable to you at any time
in the past.
Other medicines and
Methotrexate 2.5 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
leflunomide
• diphenylhydantoins
(e.g.
phenytoin,
an
antiepileptic agent)
• barbiturates and tranquillisers (sedative agents)
• antibiotics (medication against bacteria), e.g.
tetracyclines,
penicillins,
chloramphenicol,
cotrimoxazole and sulphonamides
• cytostatics (medication against cancer), e.g.
cytarabine, doxorubicin, mercaptopurine,
procarbazine, cisplatin, L-asparaginase and 5fluorouracil
• Disease-modifying antirheumatic drugs (DMARD;
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• pyrimethamine (medication against malaria)
• cholestyramine (lipid-lowering agent)
• acitretin or other retinoids (for psoriasis or skin
disorders)
• 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
derivates
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 2.5 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 2.5 mg/ml solution for injection. If you
get pregnant during treatment with Methotrexate
2.5 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 2.5 mg/ml solution for
injection!
Do not take Methotrexate 2.5 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 2.5 mg/ml solution for
injection is administered
Dosage
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
2.5 mg/ml solution for injection injecting it either
into the central nervous system (intraventricular or
intrathecal administration), 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 2.5 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:
Very
common
Common

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
Rare
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.

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If you think you have an infection, a sore throat,
fever or chills during treatment, you should tell
your doctor immediately.
The most common undesirable effects are
ulcerative stomatitis, leucopenia, nausea, and
abdominal discomfort.
Undesirable effects of Methotrexate 2.5 mg/ml
solution for injection are
Neoplasms
Uncommon: Lymphoma
Very rare: Tumour lysis syndrome (renal failure
due to massive destruction of rapidly
growing tumour cells)
Blood disorders
Common: Blood picture changes - e.g. your
vulnerability for infections may
increase, you may suffer from unusual
bleeding or bruising and you may
observe signs of anaemia (weakness,
tiredness, difficulties in breathing)
Immune system disorder
Uncommon: Allergic
reactions,
decreased
resistance to infection
Metabolism and endocrine disorders
Uncommon: Diabetes
Rare:
Hyperuricaemia (increased blood
levels of uric acid, possibly leading to
gout)
Psychiatric disorders
Rare:
Mood swings, irritability
Nervous system disorders
Common: Headache, drowsiness, sleepiness
Uncommon: Seizures,
leucoencephalopathy
(inflammation of the brain), manifested
by ventricular enlargement (expansion
of the fluid spaces inside the brain),
incomplete palsy affecting one or
both sides of the body, confusion,
dizziness
Rare:
Speech disorder, subtle cognitive
dysfunction
(easily
disturbed
attention), mental disturbance
Very Rare: Unusual sensations in the head,
pain, paraesthesia (pins-and-needles
sensation),
muscle
weakness,
significant
intellectual
deficit,
dementia, cerebral oedema (swelling
of the brain) after administration into
the central nervous system possibly
leading to vomiting, fits, coma and
even death
Eye disorders
Rare:
Impairment of vision
Very rare: Swelling, inflammation of the eyelid
edges, conjunctivitis (inflammation
of the eye conjunctiva), unusual
formation of tears, photophobia
Ear disorders
Rare:
Ringing in the ears
Cardiac disorders
Rare:
Low blood pressure, pericarditis
(inflammation of the outer lining of
the heart), pericardial effusion and
tamponing (collection of fluid and
blood, respectively, in the space
between the outer lining of the heart
and the heart muscle)
Vascular disorders
Uncommon: Vasculitis (inflammation of blood
vessels)
Rare:
Haematoma, point-like or small flat
bleeding, complications
resulting
from the formation of blood clots in
veins and arteries
Lung disorders
Common: Inflammation and fibrosis (increase in
the connective tissue); the pulmonary
toxicity may manifest as fever, cough
(especially dry and nonproductive),
difficulties or increase in the
frequency of breathing, chest pain,
hypoxaemia (lack of oxygen in the
blood), and/or abnormal findings on
chest radiography and/or tests of
respiratory function
Rare:
Upper respiratory tract infection
Gastro-intestinal disorders
Very
common: Disorders of the mouth, stomach
and intestines like mucositis (mucus
membrane
inflammation,
e.g.
inflammation of the gums, tongue,
throat, mouth, intestines), lack of
appetite, feeling sick
Common: Diarrhoea
Uncommon: Vomiting, gastrointestinal ulcerations,
inflammation of the pancreas
Rare:
Malabsorption
(disturbances
of
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
pain
Liver and gall bladder disorders
Uncommon: Fibrosis (increase in the connective
tissue), cirrhosis
(transformation
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
Rare:
Hepatitis (inflammation of the liver)
Very rare: Acute liver cell death

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Skin disorders
Common: Rash, itching, formation of blisters,
redness and inflammation
Uncommon: Loss
of
hair,
nettle
rash,
photosensitivity, pigmentary changes
(discolouration of the skin), loss of
skin tissue
Rare:
Acne, an increase in rheumatic
nodules, increased colouration or
inflammation or detachment of the
nails, nodulosis (formation of nodules
under the skin)
Very rare: Telangiectasia (expansion of small
superficial blood vessels in the
skin), worsening of psoriasis (with
concomitant UV therapy), formation
of boils, a „recall“ of radiation
dermatitis (inflammation of the skin)
and sunburn
Musculoskeletal disorders
Uncommon: Osteoporosis, pain in the joints,
muscle pain
Very rare: Aseptic necrosis of the femoral head
(loss of bone tissue in the hip joint)
Renal and urinary disorders
Common: Impairment of renal function
Uncommon: Renal failure, inflammation of the
urinary bladder, pain or difficulty in
passing urine
Very rare: Blood in the urine
Pregnancy and lactation
Uncommon: Malformations of the foetus
Rare:
Abortion
Reproductive and breast disorders
Uncommon: Vaginal discomfort
Rare:
Menstrual dysfunction (periods may
become less frequent or even stop
completely)
Very rare: Reduced or faulty formation of sperm
and egg cells, infertility, loss of interest
in sex / impotence, development of
the breast gland in males
General disorders
Uncommon: Fever without any detectable cause
Rare:
Chills, malaise and undue fatigue,
sweating
Very rare: Sudden death
In cases of acute lymphocytic leukaemia,
methotrexate can cause pain in the left epigastric
region (the area overlying the stomach, below the
left lower border of the rib cage; inflammation of
the space above the spleen due to destruction of
the leukaemic cells).
Other possible complications from administration
into the central nervous system include GuillainBarré syndrome (inflammation of the central
nervous system), nerve palsies, and cerebellar
dysfunction like ataxia (disturbance of balance
and coordination), arachnoiditis (inflammation
of one of the membranes surrounding the spinal
cord) manifested as headache, back pain, neck
stiffness, and/or fever, subacute myelopathy
(disorder affecting the spinal cord) manifested as
complete or incomplete palsy of the lower limbs
(paraparesis or paraplegia).
There have been reports on the manifestation of
lymphomas which were, in some cases, reversible
after discontinuing methotrexate therapy. The
potential of methotrexate to produce other cancers
in humans has been evaluated in several studies,
but the results do not confirm a cancerogenic risk.

Reporting of side effects
If you get any side effects, talk to your doctor, pharmacist or
nurse: This includes any possible side effects not listed in this
leaflet. You can also report side effects directly via the Yellow
Card Scheme – website: www.mhra.gov.uk/yellowcard.
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
form available from your local pharmacy. By reporting side
effects you can help provide more information on the safety of
this medicine.

5. How to store Methotrexate 2.5 mg/ml
solution for injection
• Keep the medicine out of the reach and sight of
children.
• Keep the vial in the outer carton in order to
protect from light.
• Do not store above 25°C.
• For single dose use only. Discard any unused
solution immediately and safely after initial use.
• This medicine should only be administered by a
medically qualified person, e.g. a doctor.
• Methotrexate 2.5 mg/ml solution for injection
should not be used after the expiry date printed
on the label.
• Any unused product or waste should be disposed
of in accordance with local requirements for
example by incineration.

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6.
Contents of the
pack
and
other
information
What Methotrexate 2.5 mg/ml solution for
injection contains
The active substance is methotrexate.
Each 1 ml of this sterile solution for injection
contains 2.5 milligrams methotrexate.
The other ingredients are sodium hydroxide, sodium
chloride, water for injections, and nitrogen.
What Methotrexate 2.5 mg/ml solution for
injection looks like and contents of the pack
Methotrexate 2.5 mg/ml solution for injection is a
yellowish and sterile solution in clear glass vials.
The solution for injection is available in packs of 1,
5 or 10 vials containing 2 ml solution.
Not all pack sizes may be marketed.
Marketing Authorisation Holder
hameln pharmaceuticals ltd
Gloucester, United Kingdom
Manufacturer
Haupt Pharma Wolfratshausen GmbH
Pfaffenrieder Str. 5, 82515 Wolfratshausen,
Germany
This leaflet was last approved in December
2014

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Source: Medicines and Healthcare Products Regulatory Agency

Disclaimer: Every effort has been made to ensure that the information provided here is accurate, up-to-date and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. This information has been compiled for use by healthcare practitioners and consumers in the United States. The absence of a warning for a given drug or combination thereof in no way should be construed to indicate that the drug or combination is safe, effective or appropriate for any given patient. If you have questions about the substances you are taking, check with your doctor, nurse or pharmacist.

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