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 |
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.
Estavudox Drug Interaction
Moderate: atorvastatin, efavirenzUnknown: amoxicillin / clavulanate, sulfamethoxazole / trimethoprim, diphenhydramine, levothyroxine, cyclobenzaprine, lopinavir / ritonavir, ritonavir, acetaminophen, darunavir, atazanavir, budesonide / formoterol, emtricitabine / tenofovir, valproic acid, sildenafil, tenofovir, multivitamin, pyridoxine, ascorbic acid
Estavudox Disease Interaction
Major: bone marrow suppression, hepatotoxicity, pancreatitis, peripheral neuropathy, renal dysfunction
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
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