ESBRIET 801 mg Price

Overview

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

Name

Abacavir + Lamivudine + Zidovudine

Precaution

- **Pregnancy and Breastfeeding**: Abacavir, **lamivudine**, and **zidovudine** are all classified as **Category C** for pregnancy. This means that the potential risk to the fetus cannot be ruled out, but the drugs may be used if the benefits outweigh the risks, particularly in pregnant women with **HIV**. In general, these drugs are commonly used during pregnancy, especially in combination regimens for maternal HIV management, to reduce the risk of **vertical transmission** of HIV to the infant. During breastfeeding, the components of this combination may pass into breast milk, and caution is advised. Some guidelines suggest avoiding breastfeeding while using antiretroviral therapy to prevent transmission of HIV through milk. - **Hepatic Impairment**: The combination of **abacavir**, **lamivudine**, and **zidovudine** requires caution in patients with **hepatic disease**, particularly those with **severe hepatic impairment**. **Zidovudine** and **lamivudine** are both processed through the liver, and liver dysfunction can affect their metabolism. Abacavir is contraindicated in patients with **hepatic impairment** (Child-Pugh Class C) and should be used cautiously in those with moderate liver dysfunction (Child-Pugh Class B). - **Renal Impairment**: **Lamivudine** and **zidovudine** are excreted by the kidneys, and dose adjustment may be necessary for patients with **renal impairment** (e.g., **creatinine clearance** below 50 mL/min). Abacavir is not primarily eliminated by the kidneys, so it does not require dose modification in renal impairment, but regular monitoring is advised. - **Hypersensitivity Reactions**: **Abacavir** has been associated with **serious hypersensitivity reactions** in some patients, which can include symptoms like **fever**, **rash**, **gastrointestinal distress**, and **respiratory symptoms**. **HLA-B*5701** testing should be performed prior to starting abacavir therapy to identify those at increased risk of hypersensitivity. If a hypersensitivity reaction occurs, **abacavir should be immediately discontinued**, and it should not be reintroduced, as doing so could lead to life-threatening consequences. - **Monitoring Parameters**: Regular monitoring should include complete blood counts, liver function tests (ALT, AST), renal function tests (creatinine), and HIV RNA load to assess the efficacy of therapy and monitor for any adverse effects or complications.

Indication

- **HIV Treatment**: The combination of **abacavir**, **lamivudine**, and **zidovudine** is primarily used as part of **highly active antiretroviral therapy (HAART)** for the **treatment of HIV-1 infection**. This combination provides an effective regimen for **antiviral therapy**, aiming to reduce the viral load to **undetectable levels** and improve immune function by increasing **CD4 cell counts**. - **Postexposure Prophylaxis (PEP)**: In certain situations, this combination may also be used for **postexposure prophylaxis (PEP)** to reduce the likelihood of HIV transmission following potential exposure. However, this use is more commonly restricted to **zidovudine** and **lamivudine** as part of a PEP regimen, rather than the combination with **abacavir**. - **Off-label Uses**: While the primary indication is for HIV, **zidovudine** may also be used in the prevention of **mother-to-child transmission of HIV** during labor and delivery. The combination is not typically indicated for other viral infections or conditions outside of **HIV** management. - This combination therapy is recommended as a first-line regimen by several treatment guidelines, including the **Department of Health and Human Services (DHHS)** guidelines for the treatment of HIV.

Contra indication

- **Hypersensitivity to Abacavir**: **Abacavir** should not be used in individuals who test positive for the **HLA-B*5701 allele**, as they are at an increased risk of a **serious hypersensitivity reaction**. This is a critical contraindication and requires prior genetic testing before initiating therapy. - **Severe Hepatic Impairment**: As mentioned, **abacavir** is contraindicated in patients with **severe hepatic impairment** (Child-Pugh Class C). Caution is also needed in those with **mild to moderate hepatic impairment**, as these patients may have altered drug metabolism. - **Severe Renal Impairment**: While **zidovudine** and **lamivudine** can be used in patients with renal dysfunction, the dosage should be adjusted for **creatinine clearance** less than 50 mL/min. Severe renal impairment may warrant close monitoring and possible adjustment or discontinuation of therapy. - **Active, Severe Anemia**: **Zidovudine** can cause **bone marrow suppression**, including **anemia**, so this combination is contraindicated in patients with severe **anemia** (hemoglobin less than 7.5 g/dL) or a history of **bone marrow suppression**. - **Pregnancy**: Though the combination may be used in **pregnant women** with HIV, there are **alternative regimens** for certain circumstances. The regimen should be selected based on pregnancy-specific considerations, including the stage of pregnancy and the mother's HIV resistance profile.

Side Effect

- **Common Side Effects**: - **Gastrointestinal**: The most common side effects include **nausea**, **vomiting**, **diarrhea**, and **loss of appetite**, which are usually transient but can be bothersome, especially early in treatment. - **Fatigue**: Many patients report feeling **tired** or **weak**, which may persist during the early phases of therapy but tends to resolve with continued treatment. - **Serious Side Effects**: - **Abacavir Hypersensitivity**: As previously noted, a severe **hypersensitivity reaction** can occur in patients who are positive for **HLA-B*5701**. Symptoms of this reaction include **fever**, **rash**, **gastrointestinal distress**, and **respiratory symptoms**. This is a medical emergency, and the drug must be discontinued immediately. - **Bone Marrow Suppression**: Both **zidovudine** and **lamivudine** are associated with **bone marrow suppression**, leading to **anemia**, **leukopenia**, and **thrombocytopenia**. Regular monitoring of complete blood counts is essential during treatment. - **Liver Toxicity**: Rare but severe cases of **liver toxicity**, including **hepatitis** and **hepatic failure**, may occur. Signs of liver dysfunction (e.g., **jaundice**, **dark urine**, **abdominal pain**) should be promptly evaluated. - **Lactic Acidosis**: Like other NRTIs, this combination has been linked to the rare but serious complication of **lactic acidosis**, particularly in patients with long-term therapy or those with **hepatic dysfunction**. - **Lipodystrophy**: Long-term use of zidovudine has been associated with **lipodystrophy**, a condition characterized by changes in fat distribution, including **lipohypertrophy** and **lipoatrophy**.

Pregnancy Category ID

3

Mode of Action

This combination therapy includes three **nucleoside reverse transcriptase inhibitors (NRTIs)**, which block the reverse transcription of HIV RNA into DNA, an essential step in the HIV life cycle. - **Abacavir**: Abacavir is an NRTI that is incorporated into the growing DNA chain during reverse transcription. It acts as a **chain terminator**, preventing further DNA synthesis and inhibiting viral replication. - **Lamivudine**: Lamivudine also functions as a chain terminator when incorporated into the HIV DNA by reverse transcriptase. It is highly effective against **HIV-1** and **HIV-2** and inhibits both **viral replication** and the **spread** of the virus. - **Zidovudine**: Zidovudine also acts as a **reverse transcriptase inhibitor**, and like other NRTIs, it incorporates into the viral DNA, causing premature chain termination. It is effective in reducing viral load and increasing **CD4 cell counts**. Together, these agents work synergistically to inhibit **HIV replication** at multiple stages, significantly improving the prognosis for individuals with HIV.

Interaction

- **Abacavir**: Abacavir has few significant **drug-drug interactions**. However, it should be avoided in combination with other **HIV nucleoside reverse transcriptase inhibitors (NRTIs)**, as they may have overlapping toxicities. Caution is also advised when used with drugs that affect **hepatic metabolism** (e.g., **ritonavir**, **atazanavir**, or **efavirenz**), as these may alter the pharmacokinetics of abacavir. - **Lamivudine**: **Lamivudine** is primarily metabolized by the **kidneys**, and it may interact with other drugs that affect renal function or renal clearance (e.g., **trimethoprim-sulfamethoxazole**, **ganciclovir**). Patients using these drugs together should be monitored for signs of **renal toxicity** or impaired renal function. - **Zidovudine**: Zidovudine has several known interactions, particularly with drugs that impact **bone marrow** (e.g., **ganciclovir**, **dapsone**) or **liver metabolism**. Co-administration with **doxorubicin** or other **cytotoxic drugs** can enhance the bone marrow suppression risk. Zidovudine should also be used cautiously with **rifampin**, as this antibiotic induces liver enzymes that can reduce zidovudine concentrations. - **Food and Alcohol**: Alcohol consumption should be minimized or avoided, as it can exacerbate the side effects of **zidovudine**, including liver toxicity and **anemia**. Taking the combination with food may reduce gastrointestinal side effects but does not significantly affect absorption.

Pregnancy Category Note

Information not available

Adult Dose

The typical dosage for this combination therapy is: - **Abacavir**: **300 mg twice daily** or **600 mg once daily**. - **Lamivudine**: **150 mg twice daily** or **300 mg once daily**. - **Zidovudine**: **300 mg twice daily**.

Child Dose

The pediatric dosage for this combination is weight-based, and specific formulations are available for **children**. The dose should be tailored for **children aged 3 months to 18 years** based on the child’s weight, with adjustments for renal or hepatic dysfunction. Regular blood tests are required for **pediatric patients** to monitor for potential side effects.

Renal Dose

- **Lamivudine** and **zidovudine** require **dose adjustments** in patients with **renal impairment** (e.g., creatinine clearance < 50 mL/min). **Abacavir** does not require adjustments based on renal function.

Administration

Information not available