Capecitabine

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Generic Name of Capecitabine - Learn More

Capecitabine

Capecitabine Precaution - What You Need to Know

Capecitabine is an oral chemotherapy medication commonly used to treat various types of cancer, including breast cancer and colorectal cancer. Before starting capecitabine, it is important to assess the patient's overall health and medical history, particularly for conditions like liver disease, kidney disease, or heart problems. Capecitabine is metabolized in the liver, and its effects can be altered in individuals with liver dysfunction, so close monitoring of liver enzymes is recommended. It should be used with caution in patients with a history of cardiovascular disease, as capecitabine can lead to cardiac toxicity, including chest pain, arrhythmias, and heart failure.

Pregnant women should avoid using capecitabine as it can cause fetal harm. It is classified as a category D drug by the FDA, indicating that there is evidence of harm to the fetus. Breastfeeding should also be avoided during treatment with capecitabine, as the drug can be excreted in breast milk and potentially harm the infant.

Patients receiving capecitabine should be monitored for signs of gastrointestinal toxicity, such as nausea, vomiting, diarrhea, or mucositis, which are common side effects. The drug can also cause hand-foot syndrome (palmar-plantar erythrodysesthesia), a painful skin reaction affecting the palms and soles, and it may require dose reduction or discontinuation.

Capecitabine Indication - Uses and Benefits

Capecitabine is primarily indicated for the treatment of advanced or metastatic breast cancer, colorectal cancer, and gastric cancer. It is often used as part of a combination regimen with other chemotherapy agents or targeted therapies. In breast cancer, capecitabine may be used as a second-line treatment for patients who have not responded to previous chemotherapy regimens. In colorectal cancer, it is frequently used for both adjuvant treatment after surgery to prevent recurrence and for metastatic disease. It can also be used in combination with other chemotherapy agents, such as oxaliplatin, for more aggressive cancer forms.

Capecitabine is sometimes used off-label for other types of cancer, including esophageal cancer and hepatobiliary cancers. The drug is considered a prodrug, which means it is converted into its active form, 5-fluorouracil (5-FU), once inside the body. This active form inhibits the growth of cancer cells by interfering with DNA synthesis, leading to cell death and tumor shrinkage.

Capecitabine Contraindications - Important Warnings

Capecitabine is contraindicated in patients who have a known hypersensitivity to the drug or any of its components. It should also not be used in patients who have severe renal impairment (creatinine clearance <30 mL/min) or significant liver dysfunction (e.g., cirrhosis) because these conditions can reduce the body's ability to metabolize and clear the drug, leading to toxicity.

Patients with a history of significant cardiovascular disease, such as heart failure or arrhythmias, should not use capecitabine without careful consideration and monitoring, as the drug can exacerbate cardiac issues. Additionally, capecitabine is contraindicated in pregnant women and should be avoided during breastfeeding, as it may harm the fetus or infant. It should also not be used in patients with a history of severe hand-foot syndrome resulting from chemotherapy, as capecitabine can cause this condition.

Capecitabine Side Effects - What to Expect

Capecitabine has several common side effects, many of which are related to its chemotherapy properties. These include:

- Gastrointestinal issues: Nausea, vomiting, diarrhea, and mucositis (inflammation of the mouth and digestive tract) are frequently experienced during treatment. These side effects can be severe and may require dose reduction or supportive care, such as antiemetic medications or hydration.

- Hand-foot syndrome (palmar-plantar erythrodysesthesia): A hallmark side effect of capecitabine, hand-foot syndrome presents as redness, swelling, pain, and peeling skin on the palms of the hands and soles of the feet. In severe cases, it may lead to difficulty walking or using the hands and may require discontinuation or dose adjustment.

- Fatigue: Many patients report feeling tired or weak during treatment, which can significantly affect quality of life. Fatigue may be exacerbated by other side effects such as anemia or dehydration.

- Myelosuppression: Capecitabine can cause bone marrow suppression, leading to low white blood cell counts, anemia, and thrombocytopenia (low platelet counts). This increases the risk of infections, bleeding, and anemia-related symptoms like dizziness or shortness of breath.

- Cardiac toxicity: Capecitabine can lead to cardiac complications such as chest pain, arrhythmias, and in rare cases, heart failure. Monitoring for these symptoms is essential, particularly in patients with pre-existing cardiovascular conditions.

- Liver toxicity: Liver enzyme abnormalities, including elevated levels of transaminases (AST, ALT), are common. In severe cases, this can lead to liver dysfunction or failure, necessitating dose adjustments or discontinuation of therapy.

Capecitabine Pregnancy Category ID - Safety Information

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Capecitabine Mode of Action - How It Works

Capecitabine is a prodrug that, once absorbed in the gastrointestinal tract, is converted into its active form, 5-fluorouracil (5-FU), in the liver and tumor tissues. 5-FU is a potent antimetabolite that interferes with DNA synthesis by inhibiting thymidylate synthase, an enzyme crucial for the synthesis of thymidine, a nucleotide needed for DNA replication and repair.

By blocking thymidylate synthase, 5-FU prevents the production of DNA, thereby inhibiting cancer cell proliferation and leading to cell death. The drug is more active in rapidly dividing cells, such as cancer cells, which makes it effective in treating various types of cancer.

Capecitabine is preferentially activated within tumors, allowing for a targeted therapeutic effect, which can reduce the impact on normal tissues and minimize side effects compared to older chemotherapy agents like intravenous 5-FU. This selective activation is enhanced by enzymes that are more concentrated in tumor cells, such as thymidine phosphorylase.

Capecitabine Drug Interactions - What to Avoid

Capecitabine can interact with a variety of other medications, which may affect its efficacy or safety. For instance:

- Warfarin: Capecitabine can increase the anticoagulant effect of warfarin, raising the risk of bleeding. If both drugs are used together, close monitoring of INR (International Normalized Ratio) is required, and dosage adjustments of warfarin may be necessary.

- Leucovorin: The combination of capecitabine and leucovorin (a folic acid derivative) may enhance the toxicity of capecitabine and increase the risk of side effects such as myelosuppression (bone marrow suppression) and gastrointestinal toxicity. Monitoring and dose adjustments are recommended.

- Antacids and proton pump inhibitors: These medications may affect the absorption of capecitabine, potentially reducing its effectiveness. Antacids and proton pump inhibitors should be used with caution and ideally administered several hours apart from capecitabine doses.

- Phenytoin: The use of capecitabine in combination with phenytoin, an anticonvulsant, may increase the risk of toxicity from phenytoin, as capecitabine may affect the metabolism of phenytoin in the liver.

Patients should inform their healthcare providers of all medications they are taking, including over-the-counter drugs and supplements, to avoid harmful interactions.

Capecitabine Adult Dose - Recommended Dosage

The typical adult dose of capecitabine for colorectal cancer is 1,250 mg/m², taken orally twice daily for 14 days, followed by a 7-day rest period. This cycle is repeated every 21 days. For breast cancer, the dose is generally 1,250 mg/m² twice daily for 14 days, followed by a 7-day rest period, repeated every 21 days. The exact dose may vary depending on the patient’s performance status, liver function, and tolerance to the medication.

Doses may be adjusted based on the patient's tolerance and the severity of side effects, particularly for hand-foot syndrome, gastrointestinal symptoms, or blood cell abnormalities. If significant toxicity occurs, dose reductions or interruptions are necessary.

Capecitabine Child Dose - Dosage for Children

Capecitabine is not typically used in pediatric populations due to insufficient evidence on its safety and efficacy in children. However, in certain pediatric cancer cases, particularly for advanced or relapsed cancers, capecitabine may be considered on an off-label basis. Pediatric dosages, if used, should be based on body surface area (BSA), with close monitoring for adverse effects such as myelosuppression, hand-foot syndrome, and gastrointestinal toxicity.

Since there is limited pediatric-specific data, treatment should only be initiated by a specialist familiar with chemotherapy regimens, and the child’s response and side effects should be carefully monitored.

Capecitabine Renal Dose - Dosage for Kidney Conditions

Capecitabine should be used with caution in patients with renal impairment, particularly those with creatinine clearance below 30 mL/min. In patients with moderate renal dysfunction (creatinine clearance of 30-50 mL/min), dose reductions may be necessary to avoid accumulation of the drug. For patients with severe renal impairment, capecitabine should generally be avoided, unless the benefits outweigh the risks and the patient is closely monitored.

Renal function should be monitored before each cycle, and dose adjustments should be made accordingly to minimize the risk of toxicity.