Estavudox

Estavudox Uses, Dosage, Side Effects, Food Interaction and all others data.

A dideoxynucleoside analog that inhibits reverse transcriptase and has in vitro activity against HIV.

Estavudox is a nucleoside reverse transcriptase inhibitor (NRTI) with activity against Human Immunodeficiency Virus Type 1 (HIV-1). Estavudox is phosphorylated to active metabolites that compete for incorporation into viral DNA. They inhibit the HIV reverse transcriptase enzyme competitively and act as a chain terminator of DNA synthesis. The lack of a 3'-OH group in the incorporated nucleoside analogue prevents the formation of the 5' to 3' phosphodiester linkage essential for DNA chain elongation, and therefore, the viral DNA growth is terminated.

Trade Name Estavudox
Availability Discontinued
Generic Stavudine
Stavudine Other Names Estavudina, Sanilvudine, Stavudin, Stavudine, Stavudinum
Related Drugs Biktarvy, Truvada, tenofovir, ritonavir, zidovudine, abacavir, emtricitabine, Complera, Atripla, Stribild
Type
Formula C10H12N2O4
Weight Average: 224.2133
Monoisotopic: 224.079706882
Protein binding

Negligible

Groups Approved, Investigational
Therapeutic Class
Manufacturer
Available Country
Last Updated: September 19, 2023 at 7:00 am
Estavudox
Estavudox

Uses

Estavudox is a dideoxynucleoside used in the treatment of HIV infection.

For the treatment of human immunovirus (HIV) infections.

Estavudox is also used to associated treatment for these conditions: Human Immunodeficiency Virus (HIV) Infections

How Estavudox works

Estavudox inhibits the activity of HIV-1 reverse transcriptase (RT) both by competing with the natural substrate dGTP and by its incorporation into viral DNA.

Toxicity

Side effects include peripheral neuropathy tingling, burning, numbness, or pain in the hands or feet), fatal lactic acidosis has been reported in patients treated with stavudine (ZERIT) in combination with other antiretroviral agents, severe liver enlargement, inflammation (pain and swelling) of the liver, and liver failure.

Food Interaction

  • Avoid alcohol. Ingesting alcohol while taking stavudine may increase the risk of liver damage and pancreatitis.
  • Take with or without food.

Estavudox Cholesterol interaction

[Major] The reverse transcriptase inhibitors, didanosine (ddI), zalcitabine (ddC), stavudine (d4T) and lamivudine (3TC), may cause pancreatitis.

The incidence is generally low but is approximately 7% with ddI, and up to 15% in pediatric patients given 3TC.

Patients with a history of or known risk factors for pancreatitis, such as alcohol abuse or hypertriglyceridemia, should be monitored closely during therapy with these agents.

Therapy should be discontinued at the first signs or symptoms suggestive of pancreatitis (e.g., nausea, vomiting, abdominal pain, hyperamylasemia with dysglycemia, rising triglycerides, decreasing serum calcium), and preferably permanently discontinued if clinical pancreatitis develops.

Volume of Distribution

  • 46 ± 21 L

Elimination Route

Following oral administration, stavudine is rapidly absorbed (bioavailability is 68-104%).

Half Life

0.8-1.5 hours (in adults)

Clearance

  • Renal cl=272 mL/min [Healthy subjects receiving 80 mg PO]
  • 594 +/- 164 mL/min [HIV-infected adult and pediatric patients following 1-hour IV infusion]
  • 9.75 +/- 3.76 mL/min/kg [HIV- Exposed or -Infected Pediatric Patients(Age 5 weeks – 15 years) following 1-hour IV infusion]

Innovators Monograph

You find simplified version here Estavudox

*** Taking medicines without doctor's advice can cause long-term problems.
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