CAPEGARD 500MG

Description

Capegard 500mg is an orally-administered chemotherapeutic agent used in the treatment of metastatic breast and colorectal cancers.

Capegard 500mg belongs to prodrug, which is enzymatically changes to fluorouracil (antimetabolite) in the tumor, where it prohibits DNA synthesis and reduces growth of tumor tissue.

Capegard 500mg indication

Capegard 500mg is indicated for the treatment of Colorectal cancer

• Adjuvant treatment in Duke’s colon cancer
• First line therapy in colon-rectal cancer metastasis

Breast cancer

Capegard 500mg is indicated for the treatment in metastatic breast cancer: used in combination with docetaxel after failure of anthracycline containing chemotherapy

Capegard pharmacology

Capecitabine is a prodrug and belongs to type of chemotherapy called an anti-metabolite. The body converted capecitabine into a common chemotherapy drug called fluorouracil. It blocks cells making and repairing DNA. Cancer cells require to make and repair DNA, so they can grow and replicate.

Pharmacokinetic

Absorption

The peak plasma level at about 1.5 hours

Distribution

The human plasma protein bound to Capecitabine is occurred in less than 60%

Bio-activation and metabolism

Capecitabine is largely metabolized to 5-FU enzymatically. In liver, 60 kDa carboxylesterase hydrolyses to 5’-deoxy-5-fluorocytidine.

Excretion

The route of elimination of Capecitabine is occurred through urine 95.5%

The mean terminal half-life period of Capecitabine is 0.75 hour 

Dosage and administration

Monotherapy

First line therapy of patients with advanced colorectal cancer

The prescribed dose of Capegard is 1250mg/m² should be administer orally as twice daily (morning and evening dose 2500mg/m²); treatment follow for 2 weeks followed by 1-week rest period given as 3 weeks cycle

Adjuvant therapy for Duke’s colon cancer

The prescribed dose of Capegard is 1250mg/m² orally as twice daily (morning and evening dose 2500mg/m²); for 2 weeks followed by 1 week given as 3 weeks for total 8 cycles (24 weeks)

Breast cancer

Monotherapy:

Prescribed dose is 1250mg/m² should be administer as orally for twice daily

In combination with docetaxel the recommended dose is 1250mg/m² of Capegard with 75mg/m² of docetaxel for 3 weeks

Capegard should be administered within 30 minutes after a meal

In pediatric

The safety and efficacy of the Capegard tablets in pediatric patients has not been established

Side effects

Common side effects of Capegard 500mg

• Decreased appetite
• Decreased low bloodplatelet count
• Decreased white blood cells
• dehydration
• Difficult or labored breathing
• eyeirritation
• fever
• flusymptoms
• hair loss
• headache
• Inflamed and soremouth
• Anemia
• Bloody, black, or tarry stools
• Chest pain
• Coughing up blood
• lightheadedness
• Loss of appetite
• Mild skinrash
• Nausea
• Pale skin
• Rapid heart rate
• Severe diarrhea
• dyspnea
• stomachpain or upset
• Swelling, rapid weight gain
• tastedisturbance
• tiredfeeling
• Trouble concentrating
• vomitthat looks like coffee grounds
• Vomiting
• Weakness
• Yellowing of the skin or eyes (jaundice)

Post marketing effects of Capegard 500mg includes

• skin lesions
• failure in liver
• tear duct obstruction
• acute kidney failure secondary to dehydration
• eye inflammation  with severe pain
• damage in white matter brain 

Contraindication

Capegard 500mg is contraindicated to renal impairment patients

Capegard 500mg is contraindicated in patients with hypersensitivity to Capegard 500mg or other components

Drug interaction

Capegard 500mg combination with warfarin and phenprocoumon, bleeding occurs. These events occurred within several days and even a month also

when combination of phenytoin and Capegard 500mg, toxicity related to elevation of phenytoin levels

The toxicity and concentration of 5-FU increased by Leucovorin. In elderly patients, phenytoin and Leucovorin is administered weekly which may cause; diarrhea, dehydration, enterocolitis which may causes death.

Other than warfarin, there is no drug interaction occurs while concomitant with CYP2C9 substrates

Care should be taken while combination of Capegard 500mg with CYP2C9 substrates

Precaution and warning

Coagulopathy: concomitant with warfarin, anti-coagulant response should be monitored

While using drug may results in bleeding, death; monitor anticoagulant response

When administrating the drug may cause cardiomyopathy and acute decreases in LVEF

Diarrhea: patients with severe diarrhea should be monitored

Cardio toxicity: while taking Capegard 500mg, cardio toxicity occurs like; myocardial infarction, angina, dyshythmias, cardiac arrest sudden death, Cardiomyopathy

Dihydropyrimidine dehydrogenase deficiency

Embryo fetal toxicity: occurs fetal harm; discuss with women of the potential risk to the foetus

On basis of animal studies regarding fetal risk, therapy may impair fertility in females and males of reproductive potential

Hyperbilirubinemia: If hyperbilirubinemia occurs, break off therapy immediately until it resolves or reduces in intensity

Mucocutaneous and dermatologic toxicity

Hematological problems

Care should be taken while using in geriatric patients

Hepatic insufficiency

Pregnancy and lactation

Pregnancy category: D

Capegard 500mg may cause harm to the fetus

Generally, Capegard 500mg should not be recommended in pregnancy or women who are become pregnant

Breast feeding is not recommended

Storage

Capegard 500mg should be stored at 20^oC to 25^oC (68^oF to 77^oF)

Missed dose

If dose is forgetting to take then have the dose immediately before next dose arrives or the missed dose should be skipped and follow the regular dosing schedule

Do not double the dose

Must consult with medical oncologist and follow the suggestions