How does this medication work? What will it do for me?

Raltitrexed belongs to the group of cancer-fighting medications known as antineoplastics, and specifically to the group of antineoplastics known as antimetabolites. Raltitrexed fights cancer by preventing the growth of cancer cells, which eventually results in their destruction. Raltitrexed is used to treat colorectal cancer (cancer of the colon and rectum).

This medication may be available under multiple brand names and/or in several different forms. Any specific brand name of this medication may not be available in all of the forms or approved for all of the conditions discussed here. As well, some forms of this medication may not be used for all of the conditions discussed here.

Your doctor may have suggested this medication for conditions other than those listed in these drug information articles. If you have not discussed this with your doctor or are not sure why you are taking this medication, speak to your doctor. Do not stop taking this medication without consulting your doctor.

Do not give this medication to anyone else, even if they have the same symptoms as you do. It can be harmful for people to take this medication if their doctor has not prescribed it.

What form(s) does this medication come in?

Each vial of sterile, lyophilized powder without preservative or bacteriostatic agent contains raltitrexed 2 mg (as the disodium salt). Nonmedicinal ingredients: dibasic sodium phosphate, mannitol, nitrogen, and sodium hydroxide. Single dose vials of 2 mg.

How should I use this medication?

The recommended dose of raltitrexed varies according to body size; many things can affect the schedule and dose of medication that a person needs, such as other medical conditions and other medications.

Raltitrexed is available as an intravenous (into the vein) injection. The medication is usually injected through a specially prepared site on the skin. Raltitrexed is usually given once every 3 weeks by an intravenous infusion, which usually takes about 15 minutes. If extreme side effects or toxicity occur, the next dose is usually not given until all ill effects from the medication have gone away.

Very careful handling of this medication is required. It is always administered in a hospital or similar setting with access to sterile equipment for preparation.

Your doctor may want you to drink extra fluids while taking this medication in order to help you pass more fluid and protect your kidneys.

As well as interfering with the genetic material DNA of cancer cells, raltitrexed can interfere with some of your normal cells. This may cause a number of side effects such as mouth sores. Keep track of any side effects and report them to your doctor as suggested in the section, "What side effects are possible with this medication?"

It is important this medication be given exactly as recommended by your doctor. If you miss an appointment to receive raltitrexed, contact your doctor as soon as possible to reschedule your appointment.

Do not dispose of medications in wastewater (e.g. down the sink or in the toilet) or in household garbage. Ask your pharmacist how to dispose of medications that are no longer needed or have expired.

Who should NOT take this medication?

Raltitrexed should not be used by or given to anyone who:

  • is sensitive or allergic to raltitrexed or any ingredients of the medication
  • is a child
  • is breast-feeding
  • is pregnant
  • has severe kidney or liver problems

Do not give this medication to anyone under the age of 18 years.

What side effects are possible with this medication?

Many medications can cause side effects. A side effect is an unwanted response to a medication when it is taken in normal doses. Side effects can be mild or severe, temporary or permanent.

The side effects listed below are not experienced by everyone who takes this medication. If you are concerned about side effects, discuss the risks and benefits of this medication with your doctor.

The following side effects have been reported by at least 1% of people taking this medication. Many of these side effects can be managed, and some may go away on their own over time.

Contact your doctor if you experience these side effects and they are severe or bothersome. Your pharmacist may be able to advise you on managing side effects.

  • constipation
  • diarrhea
  • difficulty swallowing
  • feeling of tiredness or weakness
  • general flu-like symptoms
  • headache
  • heartburn
  • increased sweating
  • loss of appetite
  • muscle pain or cramps
  • nausea and vomiting
  • painful joints
  • red or itchy eyes
  • sore throat
  • stomach pain
  • swelling inside the mouth
  • taste sensation changes
  • temporary loss of hair
  • trouble sleeping
  • ulcers or sores on mouth and lips
  • weight loss

Although most of the side effects listed below don't happen very often, they could lead to serious problems if you do not seek medical attention.

Check with your doctor as soon as possible if any of the following side effects occur:

  • cough that doesn't go away
  • fever
  • pinpoint red spots on skin
  • red or peeling skin
  • skin infection
  • skin rash
  • severe feeling of tiredness or weakness
  • swelling of fingers, feet, or lower legs
  • unusual bleeding or bruising

Stop taking the medication and seek immediate medical attention if any of the following occur:

  • black, tarry stools, or blood in stools or urine
  • breathing troubles, tightness in chest, or wheezing
  • cough or hoarseness with fever or chills
  • fast or irregular heartbeat
  • fever or chills
  • lower back or side pain with fever or chills
  • painful or difficult urination with fever or chills
  • swelling of the mouth or face

Some people may experience side effects other than those listed. Check with your doctor if you notice any symptom that worries you while you are taking this medication.

Are there any other precautions or warnings for this medication?

Before you begin using a medication, be sure to inform your doctor of any medical conditions or allergies you may have, any medications you are taking, whether you are pregnant or breast-feeding, and any other significant facts about your health. These factors may affect how you should use this medication.

Blood clotting: This medication can reduce the number of platelet cells in the blood. Platelets help the blood to clot, and a shortage could make you bleed more easily. Tell your doctor of any signs that your blood is not clotting as quickly. Such symptoms may include black and tarry stools, blood in the urine, easy bruising, or cuts that won't stop bleeding.

Drowsiness/reduced alertness: Raltitrexed can make you feel unwell or weak after you receive a dose, affecting the mental or physical abilities needed to drive or operate machinery. Avoid driving, operating machinery, or performing other potentially hazardous tasks until you have determined how this medication affects you.

Infection: As well as killing cancer cells, this medication can reduce the number of cells that fight infection in the body (white blood cells). Avoid contact with people with contagious infections and tell your doctor if you notice signs of an infection, such as fever or chills.

Kidney function: Kidney disease or reduced kidney function may cause this medication to build up in the body, causing side effects. If you have kidney problems, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Liver function: If you have liver problems, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Pregnancy: Raltitrexed may harm the baby if used during pregnancy. It should not be used during pregnancy, and pregnancy should be avoided (by using effective birth control) during treatment and for at least 6 months after treatment of either parent. If you become pregnant while taking this medication, contact your doctor immediately.

Breast-feeding: Because of the risks associated with raltitrexed, a decision should be made to cease breast-feeding or to discontinue the medication, taking into account the importance of the medication to the mother.

Children: The safety and effectiveness of using this medication have not been established for children. This medication should not be given to children and adolescents.

Seniors: Seniors may be more at risk of side effects from this medication.

What other drugs could interact with this medication?

There may be an interaction between raltitrexed and any of the following:

  • 5-aminosalicylic acid medications (e.g., mesalamine, olsalazine, sulfasalazine)
  • acetylsalicylic acid (ASA)
  • anticoagulants (e.g., apixaban, dabigatran, dalteparin, enoxaparin, rivaroxaban, warfarin)
  • BCG
  • cladribine
  • clopidogrel
  • clozapine
  • folic acid
  • leucovorin
  • multivitamin and mineral supplements
  • non-steroidal anti-inflammatory medications (NSAIDs; e.g., diclofenac, ibuprofen, ketorolac, naproxen)

If you are taking any of these medications, speak with your doctor or pharmacist. Depending on your specific circumstances, your doctor may want you to:

  • stop taking one of the medications,
  • change one of the medications to another,
  • change how you are taking one or both of the medications, or
  • leave everything as is.

An interaction between two medications does not always mean that you must stop taking one of them. Speak to your doctor about how any drug interactions are being managed or should be managed.

Medications other than those listed above may interact with this medication. Tell your doctor or prescriber about all prescription, over-the-counter (non-prescription), and herbal medications you are taking. Also tell them about any supplements you take. Since caffeine, alcohol, the nicotine from cigarettes, or street drugs can affect the action of many medications, you should let your prescriber know if you use them.

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