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TINDEN 1 mg/ml Price

Active Substance: Dimetindene maleate .

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Overview

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This medicine contains an important and useful components, as it consists of
Dimetindene maleate is available in the market in concentration

Name

Lapatinib

Precaution

Before starting **Lapatinib**, it is essential for patients to consult with their healthcare provider due to the following precautions: - **Cardiotoxicity**: **Lapatinib** has been associated with **cardiac events**, including **heart failure** and **decreased left ventricular ejection fraction**. Patients with pre-existing heart conditions, especially those with a history of **heart disease**, should be closely monitored for signs of heart-related symptoms, such as **shortness of breath**, **swelling in the legs**, or **fatigue**. - **Liver Function**: **Lapatinib** can cause **hepatic toxicity**, including **hepatitis** or **elevated liver enzymes**. Liver function tests should be conducted regularly, particularly in patients with pre-existing liver conditions such as **hepatitis B** or **cirrhosis**. - **Diarrhea**: One of the most common side effects of **Lapatinib** is **diarrhea**. It can be severe, and patients should be instructed to manage this symptom immediately, especially in cases of dehydration. **Oral rehydration** and **anti-diarrheal medications** may be recommended. - **Pregnancy and Breastfeeding**: **Lapatinib** is classified as a **Category D** drug, which means it can cause harm to the fetus. It should not be used during **pregnancy**, and women of childbearing potential should use **effective contraception** while on treatment. The drug is also excreted in **breast milk**, so breastfeeding is not recommended during therapy. - **Drug Interactions**: **Lapatinib** can interact with other drugs, potentially affecting its effectiveness or leading to increased toxicity. For example, **antacids**, **H2 blockers**, or **proton pump inhibitors** can reduce its absorption. It is important to inform healthcare providers about all medications being taken.

Indication

**Lapatinib** is an **oral targeted therapy** used in the treatment of certain types of **breast cancer**, specifically: - **HER2-positive Breast Cancer**: **Lapatinib** is primarily used to treat **HER2-positive** metastatic or advanced **breast cancer** in combination with other medications such as **capecitabine** or **letrozole**. - **HER2 (Human Epidermal Growth Factor Receptor 2)** is a protein that promotes the growth of cancer cells. In **HER2-positive** cancers, this receptor is overexpressed, making the cancer cells more aggressive. **Lapatinib** works by inhibiting both **HER2** and **EGFR (Epidermal Growth Factor Receptor)**, which are involved in cancer cell proliferation. - **Treatment of Advanced or Metastatic Breast Cancer**: **Lapatinib** is specifically indicated in patients whose disease has **progressed after previous chemotherapy** regimens or **trastuzumab** treatment, and those with **resistant cancer** that requires another line of therapy. - **Combination Therapy**: It is often used in combination with **capecitabine** for patients with **HER2-positive** metastatic breast cancer, especially when **trastuzumab** has not been effective.

Contra indication

**Lapatinib** should not be used in the following situations: - **Hypersensitivity**: **Lapatinib** is contraindicated in patients who have a known **hypersensitivity** or **allergy** to **Lapatinib** or any of its components. Severe **allergic reactions** such as **rash**, **itching**, and **difficulty breathing** may occur. - **Severe Liver Disease**: The drug should not be used in patients with **severe hepatic impairment** due to the increased risk of **liver toxicity**. Liver function should be assessed prior to starting treatment. - **Pregnancy**: **Lapatinib** is contraindicated in pregnancy due to its potential to cause **fetal harm**. It is classified as a **Category D** drug, and women of childbearing potential should use effective contraception. - **Severe Heart Disease**: **Lapatinib** should be avoided in patients with severe **cardiac conditions**, particularly those with **heart failure** or **significant arrhythmias**, due to its potential effects on **cardiac function**.

Side Effect

**Lapatinib** can cause several side effects, ranging from mild to severe: - **Common Side Effects**: - **Diarrhea**: This is the most frequent side effect and can sometimes be severe. It may lead to dehydration, requiring the use of **anti-diarrheal medications**. - **Skin Rash**: A rash, particularly on the **face** or **upper torso**, is common, and it may sometimes lead to **itching** or **skin irritation**. - **Nausea** and **vomiting**. - **Fatigue** or **malaise**. - **Loss of appetite** and **weight loss**. - **Mouth sores** or **stomatitis**. - **Severe Side Effects**: - **Cardiotoxicity**: The risk of **heart failure** and other **cardiac issues**, including **arrhythmias**, can be significant, particularly in patients with pre-existing heart conditions. - **Liver Toxicity**: Elevated **liver enzymes** (ALT, AST) and **hepatitis** have been reported. Symptoms of liver dysfunction include **yellowing of the skin or eyes** (jaundice), **dark urine**, or **persistent abdominal pain**. - **Severe Diarrhea**: In rare cases, **Lapatinib**-induced diarrhea can be severe enough to lead to **dehydration**, requiring hospitalization. - **Interstitial Lung Disease (ILD)**: A rare but severe lung condition characterized by **cough**, **shortness of breath**, and **fever**.

Pregnancy Category ID

4

Mode of Action

**Lapatinib** is a **small molecule tyrosine kinase inhibitor** that targets **HER2 (Human Epidermal Growth Factor Receptor 2)** and **EGFR (Epidermal Growth Factor Receptor)**. It works by blocking the signaling pathways that promote the growth of **cancer cells**, specifically in **HER2-positive** breast cancer cells. - **HER2 Inhibition**: **HER2** is a receptor protein overexpressed in some cancers, leading to uncontrolled cell division. **Lapatinib** binds to and inhibits this receptor, preventing the cancer cells from proliferating. - **EGFR Inhibition**: In addition to HER2, **Lapatinib** also targets **EGFR**, a receptor involved in cellular growth and survival. By inhibiting both **HER2** and **EGFR**, **Lapatinib** blocks key growth signals in cancer cells. - **Cancer Cell Growth Inhibition**: This inhibition leads to the **reduced growth** and **death** of **HER2-positive cancer cells**, making it effective in treating **HER2-positive breast cancer**.

Interaction

**Lapatinib** can interact with several drugs, potentially altering its effectiveness or leading to serious side effects: - **Antacids and Proton Pump Inhibitors (PPIs)**: These drugs can reduce the absorption of **Lapatinib** by altering stomach pH. Therefore, **Lapatinib** should be taken at least **1 hour before or 2 hours after** antacids, **H2 blockers**, or **PPIs**. - **CYP3A4 Inhibitors**: **CYP3A4** is a liver enzyme involved in the metabolism of **Lapatinib**. Drugs that inhibit **CYP3A4**, such as **ketoconazole**, **ritonavir**, and some **antibiotics**, may increase the levels of **Lapatinib**, leading to an increased risk of side effects. - **CYP3A4 Inducers**: Conversely, **CYP3A4 inducers**, such as **rifampin**, can lower the concentration of **Lapatinib**, reducing its effectiveness. - **Digoxin**: **Lapatinib** can interact with **digoxin**, a drug used for heart conditions, by increasing its levels and potentially leading to **digoxin toxicity**. - **St. John’s Wort**: This herbal supplement is a known **CYP3A4 inducer**, and its use can decrease the effectiveness of **Lapatinib**. - **Warfarin**: Caution should be used when administering **Lapatinib** with **warfarin**, as **Lapatinib** can affect **blood clotting** and alter **warfarin**’s effectiveness.

Pregnancy Category Note

Information not available

Adult Dose

The typical adult dosing for **Lapatinib** in the treatment of **HER2-positive breast cancer** is: - **Initial Dose**: **1250 mg** orally once daily. - **In combination with Capecitabine**: Often given in combination with **capecitabine** (1250 mg/m2 twice daily). - **Dosage Adjustments**: Dose modifications may be necessary based on **side effects** such as **diarrhea**, **liver toxicity**, or **cardiotoxicity**.

Child Dose

**Lapatinib** is generally not recommended for use in **pediatric** patients due to a lack of established safety and efficacy in children. The drug is used predominantly in **adults** with **HER2-positive** breast cancer. As always, patients should consult their healthcare provider to determine appropriate dosing and to address any concerns regarding potential side effects or interactions.

Renal Dose

No specific **renal dosing** adjustments are required for **Lapatinib** in patients with **mild to moderate renal impairment**. However, **liver function** should be monitored, as **Lapatinib** is primarily metabolized by the liver.

Administration

Information not available

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