CONTRAVE 8mg/90mg Price

Overview

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This medicine contains an important and useful components, as it consists of
Bupropion HCl, Naltrexone HClis available in the market in concentration

Name

5-Fluorouracil (5-FU)

Precaution

Before administering **5-Fluorouracil (5-FU)**, it is essential to consider the following precautions: - **Bone Marrow Suppression**: **5-FU** can cause significant **bone marrow suppression**, leading to **neutropenia**, **thrombocytopenia**, and **anemia**. Blood counts should be closely monitored, especially during therapy. - **Hepatic Impairment**: In patients with liver disease, including **cirrhosis** or **hepatic dysfunction**, **5-FU** metabolism can be impaired, increasing the risk of toxicity. Dose adjustments and frequent liver function tests are recommended for these patients. - **Renal Impairment**: **Renal insufficiency** can affect the elimination of 5-FU and increase the likelihood of toxic effects. Renal function should be monitored closely. - **Pregnancy and Breastfeeding**: **5-FU** is a **category D drug** (based on FDA pregnancy classification) due to its teratogenic effects. It should not be used during pregnancy unless the benefits outweigh the risks. **Breastfeeding** is also not recommended during therapy as **5-FU** can pass into breast milk. - **Cardiac Conditions**: Patients with a history of **cardiac disease** should be monitored closely as **5-FU** has been associated with **cardiotoxicity**, including **chest pain**, **arrhythmias**, and **heart failure**. - **Gastrointestinal (GI) Toxicity**: **5-FU** can cause **severe gastrointestinal toxicity**, including **nausea**, **vomiting**, **diarrhea**, and **stomatitis**. Pre-medications to manage these side effects may be required.

Indication

**5-Fluorouracil (5-FU)** is primarily used to treat various cancers, including: - **Colon and Rectal Cancer**: As part of combination chemotherapy regimens, it is commonly used in both adjuvant (post-surgery) and metastatic settings. - **Breast Cancer**: It is used for the treatment of metastatic **breast cancer**, especially when other therapies are not effective. - **Gastric Cancer**: It is also indicated in the treatment of **gastric cancer** either alone or as part of combination therapy. - **Pancreatic Cancer**: **5-FU** is used in the treatment of **pancreatic cancer** and is often combined with other chemotherapeutic agents. - **Skin Cancer**: It is used topically in the treatment of **actinic keratosis** and superficial **basal cell carcinoma**. - **Head and Neck Cancer**: It is sometimes used in combination with other drugs for the treatment of **head and neck squamous cell carcinoma**.

Contra indication

**5-Fluorouracil (5-FU)** should be contraindicated in the following conditions: - **Severe Bone Marrow Suppression**: Patients with existing **severe neutropenia**, **thrombocytopenia**, or **anemia** should avoid **5-FU**, as it can further suppress bone marrow activity. - **Severe Liver Dysfunction**: Patients with **severe liver disease**, including cirrhosis or liver failure, should not receive **5-FU** or should receive it only after careful consideration and dose adjustment due to impaired drug metabolism. - **Hypersensitivity**: If a patient has a known allergy to **5-FU** or any of its components, it should be avoided. - **Severe Renal Impairment**: As **5-FU** is eliminated through the kidneys, severe renal impairment is a contraindication.

Side Effect

The side effects of **5-Fluorouracil** can be mild to severe, including: - **Common Side Effects**: - **Gastrointestinal**: **Nausea**, **vomiting**, **diarrhea**, **stomatitis** (inflammation of the mouth), and **mucositis** (inflammation of mucous membranes). - **Bone Marrow Suppression**: Leading to **neutropenia**, **anemia**, and **thrombocytopenia**, which can increase the risk of **infection** and **bleeding**. - **Fatigue**: Often caused by **anemia** or overall treatment burden. - **Hair loss** (alopecia), which is common in chemotherapy. - **Skin Changes**: Rash, redness, and **photosensitivity** (increased sensitivity to sunlight). - **Serious Side Effects**: - **Cardiotoxicity**: Includes **chest pain**, **arrhythmias**, and **heart failure**. Patients receiving **5-FU** should be monitored for cardiovascular signs. - **Hepatotoxicity**: Liver damage, including **elevated liver enzymes**, jaundice, and even **liver failure** in extreme cases. - **Severe Mucositis**: **5-FU** can cause painful inflammation of the mucous membranes, leading to difficulty eating, swallowing, and speaking. - **Severe Diarrhea**: Profuse diarrhea can lead to **dehydration**, **electrolyte imbalances**, and potentially **life-threatening complications**. - **Hand-Foot Syndrome**: This condition is marked by **redness**, **swelling**, and **pain** in the hands and feet, sometimes leading to peeling and **skin ulcers**.

Pregnancy Category ID

4

Mode of Action

**5-Fluorouracil (5-FU)** is a **pyrimidine analog** that interferes with **DNA** and **RNA synthesis** by inhibiting the enzyme **thymidylate synthase**, which is crucial for **DNA replication**. This inhibition prevents the formation of **thymidine**, a necessary building block for DNA synthesis, leading to **cell death**, particularly in rapidly dividing cancer cells. **5-FU** is considered an **antimetabolite** and primarily exerts its action during the **S-phase** of the cell cycle. By disrupting normal cell division, **5-FU** inhibits the growth of tumors.

Interaction

Several drug interactions can affect the efficacy and safety of **5-Fluorouracil**: - **Leucovorin**: Leucovorin enhances the activity of **5-FU** by stabilizing the binding between **5-FU** and the enzyme **thymidylate synthase**, leading to an increased effect. **Leucovorin** is often used in combination with **5-FU** in chemotherapy regimens. - **Phenytoin**: **5-FU** can increase the serum levels of **phenytoin**, leading to a potential risk of **phenytoin toxicity**. Monitoring serum levels of **phenytoin** is advised. - **Warfarin**: **5-FU** may alter the metabolism of **warfarin**, potentially increasing the risk of **bleeding**. Regular monitoring of the **INR** (International Normalized Ratio) is necessary. - **Other Chemotherapy Drugs**: Combination with other chemotherapy agents, such as **cyclophosphamide**, **doxorubicin**, or **cisplatin**, can result in enhanced **myelosuppression**, **gastrointestinal toxicity**, or **renal toxicity**. - **Antacids**: Antacids or **H2 antagonists** may alter the absorption of **5-FU**, though this interaction is not well-established. Caution should be exercised when co-administering these medications.

Pregnancy Category Note

Information not available

Adult Dose

The dosage of **5-Fluorouracil (5-FU)** varies based on the type of cancer and the treatment regimen: - **For Colon Cancer (Adjuvant)**: The typical dose is **425 mg/m²** administered as an intravenous infusion over a period of **46 hours**, often in combination with **leucovorin**. - **For Metastatic Breast Cancer**: **5-FU** is used as part of combination chemotherapy, usually given as **500-750 mg/m²** intravenously every **2-3 weeks**. - **For Topical Use (Skin Cancer)**: **5-FU** cream is applied directly to the affected skin, usually twice daily for up to **4 weeks**. Doses may be adjusted based on **toxicity**, **blood counts**, and **liver function**.

Child Dose

In pediatric patients, the use of **5-Fluorouracil (5-FU)** is typically reserved for certain cancers, such as **neuroblastoma** or **brain tumors**, and is often used within a chemotherapy regimen. Dosing is usually based on body surface area (**mg/m²**) and can vary according to the specific protocol being followed. Pediatric dosing should always be determined by an oncologist experienced in pediatric chemotherapy. --- **Important Note**: It is crucial that patients receive **5-Fluorouracil** under the supervision of an oncologist or a healthcare provider with experience in cancer treatment. Regular monitoring of blood counts, liver function, and renal function is necessary during therapy to mitigate potential adverse effects and ensure the best outcome. Always consult with a healthcare provider before starting any treatment regimen.

Renal Dose

In patients with **renal impairment**, dose adjustments may not be necessary for **5-FU** in standard regimens; however, patients with **severe renal impairment** (creatinine clearance < 30 mL/min) should be closely monitored for **toxicity**, as the drug may accumulate. Dosage reductions or delays may be required based on the patient's clinical condition.

Administration

Information not available