Description
Composition
Active Ingredient
- Folinic Acid: Each vial contains 300 mg of folinic acid, equivalent to 381.195 mg of calcium folinate pentahydrate.
Inactive Ingredients
- Sodium Chloride: 255 mg per vial.
Pharmaceutical Form
The solution is a clear, colorless liquid intended for intravenous (IV) or intramuscular (IM) injection.
Therapeutic Indications
Neutralization of Toxic Effects
Calcium Folinate is utilized to counteract the acute toxic effects of high-dose methotrexate, trimethoprim, and pyrimethamine, which are folic acid antagonists.
Colorectal Cancer Treatment
It is also administered in combination with 5-fluorouracil (5-FU) to reduce cytotoxicity in the treatment of colorectal cancer.
Megaloblastic Anemia
Calcium Folinate is indicated for the treatment of megaloblastic anemia due to folic acid deficiency when oral administration of folic acid is not feasible.
Dosage and Administration
Methotrexate Therapy
The dosage and administration of calcium folinate are contingent upon the dosage and regimen of methotrexate. The initial dose is typically 15 mg (6-12 mg/m²) administered 12-24 hours after the start of methotrexate infusion, repeated every 6 hours for 72 hours.
Colorectal Cancer
For colorectal cancer, calcium folinate is administered as a 500 mg/m² IV bolus injection in combination with 5-FU.
Common Side Effects
Calcium Folinate can cause several side effects, including:
Gastrointestinal Issues
- Nausea
- Vomiting
- Severe diarrhea, which can sometimes lead to dehydration
Skin Reactions
- Redness and swelling, particularly in the palms of the hands and soles of the feet
Blood-Related Issues
- Reduction in blood cells, including a decrease in white blood cells, which can increase the risk of infections
Inflammation
- Inflammation of the lining of the mouth and intestine, which can be severe and life-threatening in some cases
Allergic Reactions
- Severe allergic reactions, including symptoms like rash, itching, swelling, severe dizziness, and trouble breathing
It is crucial to monitor for these side effects and consult a healthcare provider if any occur. They can help manage the side effects and adjust the treatment if necessary.
Drug Interactions
Folic Acid Antagonists
- Co-trimoxazole (an antibiotic) and pyrimethamine (used to treat malaria): Calcium Folinate may reduce or fully counteract the effects of these medications.
Anticancer Drugs
- Fluorouracil (5-FU): Calcium Folinate enhances the effectiveness and side effects of fluorouracil. This combination is often used in the treatment of colorectal cancer.
Epilepsy Medications
- Phenobarbital, Phenytoin, Primidone, and Ethosuximide: Calcium Folinate may reduce the effect of these medications. Blood levels should be monitored, and doses adjusted to prevent increased convulsions.
Other Considerations
Pregnancy and Breastfeeding
Calcium Folinate does not induce harmful effects if used alone during pregnancy. However, it should not be used in combination with fluorouracil during pregnancy or breastfeeding.
It is essential to inform healthcare providers about all medications being taken to avoid potential interactions and ensure safe and effective treatment.
Effect on Folic Acid Levels
Enhanced Plasma Folate Levels
Calcium Folinate, also known as folinic acid, is an activated form of folic acid. It bypasses several steps in folic acid metabolism, including the MTHFR gene, which is responsible for converting folic acid into its active form. It raises plasma folate levels more effectively than folic acid supplements because it is already in an active form, making it more readily available for the body to use.
Neutralization of Folic Acid Antagonists
Calcium Folinate is used to neutralize the effects of folic acid antagonists like methotrexate, trimethoprim, and pyrimethamine. These drugs inhibit the action of folic acid, and calcium folinate helps restore folate levels in the body.
Support in Chemotherapy
When used in combination with fluorouracil (5-FU), calcium folinate enhances the effectiveness of the chemotherapy drug while also helping to mitigate its side effects.
Treatment of Anemia
Calcium Folinate is used to treat megaloblastic anemia caused by folic acid deficiency, especially when oral administration of folic acid is not possible.
In summary, Calcium Folinate plays a crucial role in maintaining and enhancing folic acid levels in the body, especially in situations where folic acid metabolism is impaired or when folic acid antagonists are used.
Use in Colorectal Cancer Treatment
Mechanism of Action
Calcium Folinate is not a chemotherapy drug itself but enhances the effectiveness of certain chemotherapy drugs, particularly fluorouracil (5-FU). It works by stabilizing the binding of 5-FU to the enzyme thymidylate synthase, thereby increasing the cytotoxic effects of 5-FU on cancer cells.
Combination Therapy
Fluorouracil (5-FU)
- Enhanced Efficacy: When used in combination with 5-FU, calcium folinate enhances the drug’s effectiveness in treating colorectal cancer.
- Administration: It is often administered as an intravenous (IV) bolus injection or infusion alongside 5-FU.
Oxaliplatin and UFT
- Advanced Colorectal Carcinoma: Calcium folinate is also used in combination with oxaliplatin and UFT (uracil plus tegafur) for the treatment of advanced colorectal carcinoma.
- Dosage: The combination therapy typically involves oral calcium folinate given in divided doses daily for a specified period.
Treatment Regimens
De Gramont Regimen
- Metastatic Colon Rectal Cancer (mCRC): The De Gramont regimen, which includes high-dose folinic acid (HD-FUFA) and 5-FU, is a standard treatment for metastatic colorectal cancer.
- Additional Agents: This regimen may also include other agents like oxaliplatin, irinotecan, or biological agents such as anti-EGFR or antiangiogenic monoclonal antibodies.
Clinical Benefits
- Improved Survival Rates: The combination of calcium folinate with 5-FU and other agents has been shown to improve response rates and overall survival in patients with colorectal cancer.
- Palliation: It provides palliation and modest impact on overall survival in patients with metastatic colorectal cancer.
Side Effects
- Common Side Effects: Diarrhea, nausea, and vomiting are common side effects when used in combination with 5-FU.
- Hand-Foot Syndrome: This side effect is associated with protracted intravenous infusions of 5-FU but has not been observed with UFT plus oral calcium folinate.
In summary, Calcium Folinate is a crucial component in the treatment of colorectal cancer, enhancing the efficacy of chemotherapy drugs and improving patient outcomes.
Benefits of Calcium Folinate
Calcium Folinate offers several benefits, particularly in medical treatments:
Enhances Chemotherapy Effectiveness
- Combination with Fluorouracil (5-FU): Calcium folinate is often used in combination with 5-FU to treat colorectal cancer. It enhances the effectiveness of 5-FU by stabilizing its binding to the enzyme thymidylate synthase, thereby increasing its cytotoxic effects on cancer cells.
Reduces Toxicity of Chemotherapy Drugs
- Methotrexate Rescue: Calcium folinate is used to reduce the toxic effects of high-dose methotrexate therapy, known as “folinic acid rescue” or “leucovorin rescue.” It helps protect healthy cells from the harmful effects of methotrexate.
Treatment of Anemia
- Megaloblastic Anemia: Calcium folinate is used to treat megaloblastic anemia caused by folic acid deficiency, especially when oral administration of folic acid is not possible.
Prevention of Blood Cell Disorders
- Blood Cell Protection: It is used to treat or prevent serious blood cell disorders such as thrombocytopenia, neutropenia, and anemia caused by certain drugs like folic acid antagonists (e.g., methotrexate, trimethoprim, pyrimethamine).
Support in Pregnancy
- Fetal Development: Folinic acid is crucial for healthy fetal spine and brain development. It helps prevent neural tube defects such as spina bifida and anencephaly.
Improved Absorption and Utilization
- Effective Absorption: Calcium folinate is an activated form of folic acid, making it more readily available for the body to use. It bypasses several steps in folic acid metabolism, including the MTHFR gene, which is responsible for converting folic acid into its active form.
In summary, Calcium Folinate offers significant benefits in enhancing chemotherapy effectiveness, reducing toxicity, treating anemia, preventing blood cell disorders, supporting fetal development, and improving folate absorption and utilization.
| Category | Information |
|---|---|
| Composition | Active Ingredient: Folinic Acid (300 mg per vial) <br> In |
| Composition | Active Ingredient: Folinic Acid (300 mg per vial) <br> Inactive Ingredients: Sodium Chloride (255 mg per vial) |
| Pharmaceutical Form | Clear, colorless liquid intended for IV or IM injection |
| Therapeutic Indications | – Neutralizes toxic effects of methotrexate, trimethoprim, and pyrimethamine <br> – Used with 5-FU in colorectal cancer treatment <br> – Treats megaloblastic anemia due to folic acid deficiency |
| Dosage & Administration | – Methotrexate therapy: Initial dose typically 15 mg (6-12 mg/m²) 12-24 hours after methotrexate infusion, repeated every 6 hours for 72 hours <br> – Colorectal cancer: 500 mg/m² IV bolus injection with 5-FU |
| Common Side Effects | – Gastrointestinal issues: Nausea, vomiting, severe diarrhea <br> – Skin reactions: Redness, swelling <br> – Blood-related issues: Decreased white blood cells <br> – Inflammation of mouth and intestine lining <br> – Severe allergic reactions: Rash, itching, swelling, severe dizziness, trouble breathing |
| Drug Interactions | – Reduces effects of folic acid antagonists (co-trimoxazole, pyrimethamine) <br> – Enhances effectiveness and side effects of 5-FU <br> – Reduces effect of epilepsy medications (phenobarbital, phenytoin, primidone, ethosuximide) |
| Effect on Folic Acid Levels | – Enhances plasma folate levels <br> – Neutralizes effects of folic acid antagonists <br> – Supports chemotherapy <br> – Treats megaloblastic anemia |
| Use in Colorectal Cancer | – Enhances effectiveness of 5-FU by stabilizing binding to thymidylate synthase <br> – Used in combination therapy with 5-FU, oxaliplatin, UFT <br> – Included in De Gramont regimen for metastatic colorectal cancer <br> – Improves survival rates, provides palliation |
| Benefits | – Enhances chemotherapy effectiveness <br> – Reduces toxicity of methotrexate <br> – Treats megaloblastic anemia <br> – Prevents blood cell disorders <br> – Supports fetal development <br> – Improves folate absorption and utilization |
Calcium Folinate, in its multiple applications, proves to be an indispensable component in various medical treatments, particularly for those involving chemotherapy and folic acid deficiency-related conditions. Its strategic use in combination with other medications like 5-FU enhances therapeutic outcomes while mitigating adverse effects, making it a critical tool in modern oncology and hematology
Reviews
There are no reviews yet.