Raltitrexed is a chemotherapy drug that is given as a treatment for some types of cancer. It is also known as Tomudex®. It is most commonly used to treat bowel cancer or advanced rectal cancer. It is often used as a substitute for 5-Fluorouracil in situations where there has been an adverse effect to 5FU or where 5FU could be dangerous (for example in a patient with a serious heart condition). This information describes raltitrexed, how it is given and some of its possible side effects.
What raltitrexed looks like
Raltitrexed is a colourless fluid.
How it is given
Raltitrexed may be given:
- As a drip (infusion) through a fine tube (cannula) inserted into a vein. It is given over a short period of time.
- Through a central line, which is inserted under the skin into a vein near the collarbone, or into a PICC line, which is inserted into a vein in the crook of the arm.
- Chemotherapy is usually given as a course of several sessions (or cycles) of treatment over a few months. The length of your treatment and the number of cycles you have will depend on the type of cancer for which you are being treated. Your nurse or doctor will discuss your treatment plan with you.
Possible side effects
Each person’s reaction to chemotherapy is different. Some people have very few side effects, while others may experience more. The side effects described in this information will not affect everyone who is given raltitrexed and may be different if you are having more than one chemotherapy drug.
We have outlined the most common side effects as well as rarer ones, so that you can be aware of them if they occur. However, we have not included those that are very rare and therefore extremely unlikely to affect you. If you notice any effects which you think may be due to the drug, but which are not listed in this information, please discuss them with your doctor or chemotherapy nurse.
Feeling sick (nausea) and being sick (vomiting)
If you do feel sick this may begin a few hours after the treatment is given and last for up to a day. Your doctor can prescribe very effective anti-sickness (anti-emetic) drugs to prevent, or greatly reduce, nausea. If the sickness is not controlled, or continues, tell your doctor; they can prescribe other anti-sickness drugs which may be more effective.
Loss of appetite
This is usually mild and may last a day or so.
This can usually be easily controlled with medicines such as imodium (loperamide) or codeine, but tell your doctor if it is severe or if it continues. It is important to drink plenty of fluids if you have diarrhoea.
Lowered resistance to infection
Raltitrexed can reduce the production of white blood cells by the bone marrow, making you more prone to infection. This effect can begin seven days after treatment has been given and your resistance to infection usually reaches its lowest point 10–14 days after chemotherapy. Your blood cells will then increase steadily and will usually have returned to normal levels before your next cycle of chemotherapy is due.
Contact your doctor or the hospital straightaway if:
- your temperature goes above 38ºC (100.5ºF)
- you suddenly feel unwell (even with a normal temperature).
- You will have a blood test before having more chemotherapy to make sure that your cells have recovered. Occasionally it may be necessary to delay your treatment if the number of blood cells (the blood count) is still low.
Bruising or bleeding
Raltitrexed can reduce the production of platelets (which help the blood to clot). Let your doctor know if you have any unexplained bruising or bleeding, such as nosebleeds, blood spots or rashes on the skin, and bleeding gums.
Anaemia (low number of red blood cells)
While having treatment with raltitrexed you may become anaemic. This may make you feel tired and breathless on exertion. Let your doctor or nurse know if these symptoms are a problem.
Temporary effect on liver function
Raltitrexed may cause changes in the way that your liver works, though your liver will return to normal when the treatment is finished. You are very unlikely to notice any problems but your doctor will check your liver is working properly with a blood test before each treatment.
Raltitrexed can cause a rash, which may be itchy. Your doctor can prescribe medication to relieve the symptoms.
Tiredness and weakness
Some people feel tired when having raltitrexed and occasionally a flu-like illness may occur. You may have headaches, aching joints and muscles and a high temperature. It is important to let your doctor know immediately if you get a high temperature.
Less common side effects
Less commonly, raltitrexed can cause constipation, which is usually relieved by a high fibre diet or simple laxatives. Let your doctor know if you become constipated.
Sore mouth and ulcers
Your mouth may become sore, or you may notice small ulcers during this treatment. Drinking plenty of fluids, and cleaning your teeth regularly and gently with a soft toothbrush, can help to reduce the risk of this happening. Tell your nurse or doctor if you have any of these problems, as special mouthwashes and medicines to prevent or clear any mouth infection can be prescribed.
You may notice that your food tastes different. Normal taste will usually come back after the treatment finishes
This is rare with raltitrexed, but may occasionally happen. More commonly your hair may just thin. Hair loss is temporary and your hair will regrow once the treatment has finished.
ADDITIONAL INFORMATION FOR HEALTHCARE PROFESSIONALS
ADVERSE REACTIONS SIGNIFICANT
- Central nervous system: Fever (2% to 23%), may be delayed until several days after administration
- Dermatologic: Rashes (14%), usually pruritic papular lesions on head and thorax
- Gastrointestinal: Nausea (58%; grade 3 or 4 in 12%), mucositis/stomatitis (12% to 48%; grade 3 or 4 in 2%), diarrhea (38%; grade 3 or 4 in 11%), vomiting (37%), anorexia (27%), abdominal pain (18%), constipation (13% to 15%; grade 3 or 4 in 2%)
- Hematologic: Myelosuppression; leukopenia occurs in about 21% of patients (grade 3 or 4 in 12%), nadirs occur in ~8 days, but may be delayed to day 21, with recovery in ~10 days; thrombocytopenia (5% to 6%; grade 3 or 4 in 4%), anemia (15% to 18%; grade 3 or 4 in 7%)
- Hepatic: Transaminases increased (14% to 18%; grade 3 or 4 in 10%)
- Neuromuscular & skeletal: Weakness (46% to 48%; grade 3 or 4 in 9%)
1% to 10%:
- Cardiovascular: Arrhythmias (3%), edema (9% to 10%), CHF (2%)
- Central nervous system: Malaise, headache, pain, chills, insomnia, depression, paresthesia
- Dermatologic: Alopecia, cellulitis, exfoliative eruptions
- Endocrine & metabolic: Dehydration, hypokalemia
- Gastrointestinal: Dyspepsia, flatulence, xerostomia, weight loss, taste perversion
- Genitourinary: Urinary tract infection
- Hepatic: Bilirubin increased, alkaline phosphatase increased
- Neuromuscular & skeletal: Arthralgia, myalgia, hypotonia
- Ocular: Conjunctivitis
- Renal: Serum creatinine increased
- Respiratory: Cough (increased), dyspnea, pharyngitis
- Miscellaneous: Flu-like syndrome (6% to 8%), diaphoresis, infection, sepsis
<1% (Limited to important or life-threatening):
- Hypersensitivity/allergic reaction (including stridor and wheezing following the first dose), desquamation
PHARMACODYNAMICS / KINETICS
Distribution: Vss: 548 L
Protein binding: 93%
Metabolism: Undergoes extensive intracellular metabolism to active polyglutamate forms; appears to be little or no systemic metabolism of the drug
Half-life elimination: Triphasic; Beta: 2 hours; Terminal: Up to 198 hours
Excretion: Urine (50% as unchanged drug); fAeces (15%)