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Tenofovir Disoproxil Fumarate
Before starting Tenofovir Disoproxil Fumarate, it is essential to consult with a healthcare provider due to potential risks. Key precautions include:
- Renal Function: Tenofovir Disoproxil Fumarate can cause renal impairment and may lead to acute renal failure or tubulopathy. Renal function should be assessed before initiating therapy and monitored regularly during treatment. Dose adjustments may be required for patients with renal dysfunction.
- Lactic Acidosis and Hepatomegaly: There is a risk of developing lactic acidosis and hepatomegaly (enlarged liver) associated with Tenofovir, especially in combination with other antiretroviral agents. These conditions can be fatal if not addressed promptly.
- Osteoporosis and Bone Mineral Density Loss: Tenofovir may lead to decreased bone mineral density and increase the risk of osteoporosis. Bone health should be monitored, particularly in long-term therapy.
- Pregnancy and Breastfeeding: Tenofovir Disoproxil Fumarate is classified as a Category B drug during pregnancy, indicating that it is generally considered safe to use during pregnancy, but should only be prescribed if the potential benefits outweigh the risks. It is excreted in breast milk, and its use during breastfeeding is usually not recommended unless necessary.
- Hepatitis B Reactivation: In patients with chronic hepatitis B who are co-infected with HIV, Tenofovir should be used cautiously, as the abrupt discontinuation of therapy may lead to hepatitis B reactivation.
Tenofovir Disoproxil Fumarate is primarily indicated for:
- HIV Infection: It is used in combination with other antiretroviral agents for the treatment of HIV-1 infection in both adults and children. It helps reduce the amount of virus in the blood, enhancing immune function.
- Chronic Hepatitis B: It is also approved for the treatment of chronic hepatitis B infection in adults. Tenofovir works by inhibiting the replication of the hepatitis B virus (HBV) and reducing liver inflammation.
- Pre-Exposure Prophylaxis (PrEP): Tenofovir Disoproxil Fumarate is part of a PrEP regimen to prevent HIV-1 infection in high-risk individuals, including people with HIV-positive partners or those at risk due to sexual behaviors.
Tenofovir Disoproxil Fumarate should be avoided in the following situations:
- Hypersensitivity: It is contraindicated in patients with known hypersensitivity to Tenofovir or any of its components, as it can cause severe allergic reactions.
- Severe Renal Impairment: Tenofovir Disoproxil Fumarate is contraindicated in patients with severe renal impairment (creatinine clearance < 30 mL/min) or those on hemodialysis, as the drug may further impair kidney function.
- Hepatitis B Mono-Therapy: It is not recommended as a monotherapy for hepatitis B in patients who are not co-infected with HIV, as resistance to Tenofovir may develop.
Tenofovir Disoproxil Fumarate can cause both common and serious side effects:
- Common Side Effects:
- Nausea and diarrhea: Gastrointestinal issues are commonly reported by patients on Tenofovir therapy.
- Headache: A mild to moderate headache is a frequent side effect.
- Fatigue: Many patients report feeling tired or weak while on treatment.
- Abdominal pain: Some patients may experience discomfort in the abdomen.
- Rash: A mild skin rash can occur in some patients.
- Serious Side Effects:
- Renal Impairment: Tenofovir can lead to acute renal failure or chronic kidney disease, so renal function should be closely monitored.
- Lactic Acidosis: A rare but serious condition that can be fatal if not treated immediately. Symptoms include deep, rapid breathing, muscle pain, weakness, and abdominal discomfort.
- Hepatic Steatosis: Severe liver problems, including fatty liver and hepatomegaly, may occur.
- Osteomalacia: Long-term use of Tenofovir has been associated with bone mineral density loss, which increases the risk of fractures.
- Hepatitis B Flare: Discontinuing Tenofovir in patients with chronic hepatitis B could lead to a hepatitis B flare, which may be life-threatening.
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Tenofovir Disoproxil Fumarate is an antiviral drug and works by inhibiting the replication of viruses. Its mechanism of action includes:
- Inhibition of Reverse Transcriptase: Tenofovir is a nucleotide reverse transcriptase inhibitor (NRTI). It works by inhibiting HIV reverse transcriptase, the enzyme responsible for converting HIV RNA into DNA. By doing this, Tenofovir prevents the replication of the virus in infected cells.
- Inhibition of HBV Replication: In hepatitis B, Tenofovir inhibits the replication of the HBV DNA polymerase, which is necessary for the virus to multiply within liver cells. By preventing HBV replication, Tenofovir helps reduce viral load and liver inflammation.
Tenofovir Disoproxil Fumarate can interact with several medications, which can affect its effectiveness and safety:
- Nephrotoxic Drugs: Combining Tenofovir with other nephrotoxic agents, such as NSAIDs, aminoglycosides, and radiocontrast agents, may increase the risk of kidney damage. Close monitoring of renal function is essential.
- Atazanavir and Ritonavir: Co-administration with Atazanavir or Ritonavir (protease inhibitors) may reduce Tenofovir plasma levels, so Tenofovir dose adjustments are recommended in such combinations.
- Didanosine: Co-administration of Tenofovir with Didanosine (another antiretroviral agent) may increase the risk of lactic acidosis and pancreatitis, so caution is advised.
- Other Antiretrovirals: Combining Tenofovir with other antiretroviral drugs should be done under medical supervision to avoid overlapping toxicities or reduced efficacy.
- Renal Function Altering Drugs: Drugs that affect kidney function, such as angiotensin-converting enzyme inhibitors (ACE inhibitors) or diuretics, may require dose adjustments or more frequent monitoring of renal function when used with Tenofovir.
The recommended dosing regimen for Tenofovir Disoproxil Fumarate in adults is:
- For HIV-1 Infection: The usual dose is 300 mg once daily, in combination with other antiretroviral agents.
- For Chronic Hepatitis B: The standard dose is 300 mg once daily for adult patients with HBV infection.
- For Pre-Exposure Prophylaxis (PrEP): Tenofovir Disoproxil Fumarate is prescribed at a dose of 300 mg once daily to individuals at high risk of contracting HIV.
Tenofovir Disoproxil Fumarate is generally approved for use in children aged 2 years and older for the treatment of HIV-1 infection and hepatitis B. The dosing for pediatric patients is based on weight:
- For HIV-1: The dose is usually 8 mg/kg once daily, not exceeding the adult dose of 300 mg per day.
- For Chronic Hepatitis B: The dose is generally the same as for HIV, 8 mg/kg once daily, up to a maximum of 300 mg/day.
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Tenofovir Disoproxil Fumarate is an important medication for the management of HIV-1 and chronic hepatitis B. Due to its potential side effects on the kidneys and bones, it is critical to monitor these aspects regularly during treatment. Always consult with a healthcare provider before starting or adjusting the dosage of Tenofovir, as appropriate guidance is necessary to avoid serious complications.
In patients with renal impairment, dose adjustments for Tenofovir Disoproxil Fumarate may be necessary:
- Moderate Renal Impairment (CrCl 30-49 mL/min): The standard dose may need to be reduced, and renal function should be closely monitored.
- Severe Renal Impairment (CrCl <30 mL/min) or Hemodialysis: Tenofovir is contraindicated in patients with severe renal impairment. If it is used, it should be done with caution, and kidney function should be monitored frequently.
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