Didanosine
Didanosine Uses, Dosage, Side Effects, Food Interaction and all others data.
A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by a hydrogen. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. Didanosine is a potent inhibitor of HIV replication, acting as a chain-terminator of viral DNA by binding to reverse transcriptase; ddI is then metabolized to dideoxyadenosine triphosphate, its putative active metabolite.
Didanosine is a nucleoside reverse transcriptase inhibitor (NRTI) with activity against Human Immunodeficiency Virus Type 1 (HIV-1). Didanosine is a hypoxanthine attached to the sugar ring, unlike other nucleoside analogues. Didanosine 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. Didanosine is effective against HIV, and usually used in combination with other antiviral therapy. Switching from long term AZT treatment to didanosine has been shown to be beneficial. Didanosine has weak acid stability and therefore, it is often combined with an antacid.
| Trade Name | Didanosine |
| Availability | Discontinued |
| Generic | Didanosine |
| Didanosine Other Names | 2,3-Dideoxyinosine, ddIno, Didanosina, Didanosine, Didanosinum, Dideoxyinosine |
| Related Drugs | Biktarvy, Truvada, tenofovir, ritonavir, zidovudine, abacavir, emtricitabine, Complera, Atripla, Stribild |
| Weight | 125mg, 200mg, 250mg, 400mg, 10mg/ml |
| Type | Oral delayed release capsule, oral powder for reconstitution |
| Formula | C10H12N4O3 |
| Weight | Average: 236.2273 Monoisotopic: 236.09094027 |
| Protein binding | Low (<5%) |
| Groups | Approved |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Didanosine is a reverse transcriptase inhibitor used to treat HIV.
For use, in combination with other antiretroviral agents, in the treatment of HIV-1 infection in adults.
Didanosine is also used to associated treatment for these conditions: Human Immunodeficiency Virus Type 1 (HIV-1) Infection
How Didanosine works
Didanosine (ddI) is metabolized intracellularly by a series of cellular enzymes to its active moiety, dideoxyadenosine triphosphate (ddATP), which inhibits the HIV reverse transcriptase enzyme competitively by competing with natural dATP. It also acts as a chain terminator by its incorporation into viral DNA as 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.
Toxicity
Side effects include pancreatitis, peripheral neuropathy, diarrhea, hyperuricemia and hepatic dysfunction
Food Interaction
- Avoid alcohol.
- Take on an empty stomach. Take at least 1 hour before or 2 hours after meals.
[Moderate] ADJUST DOSING INTERVAL: Didanosine bioavailability is decreased when administered with food.
Loss of efficacy may result.
MANAGEMENT: Didanosine should be administered in the fasting state, at least 30 minutes before or more than 2 hours after eating.
Didanosine 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.
Didanosine Hypertension interaction
[Moderate] Didanosine (ddI) formulations have a high sodium content.
There are 265 mg of sodium per tablet and 1380 mg per packet of powder for oral solution, which may be of concern in patients with conditions that may be adversely affected by excessive amounts of sodium, such as congestive heart failure, hypertension, and fluid retention.
Each tablet also contains 8.6 mEq of magnesium.
Patients with significant renal impairment may not tolerate these loads.
Didanosine Drug Interaction
Major: tenofovir, tenofovirModerate: efavirenz, efavirenzUnknown: raltegravir, raltegravir, valproic acid, valproic acid, multivitamin, multivitamin, cyanocobalamin, cyanocobalamin, pyridoxine, pyridoxine, ascorbic acid, ascorbic acid, phytonadione, phytonadione, zinc sulfate, zinc sulfate
Didanosine Disease Interaction
Major: renal dysfunction, bone marrow suppression, hepatotoxicity, pancreatitis, peripheral neuropathyModerate: hyperuricemia, PKU, sodium
Elimination Route
Rapidly absorbed (bioavailability 30-40%) with peak plasma concentrations appearing within 0.5 and 1.5 hrs.
Half Life
30 minutes in plasma and more than 12 hours in intracellular environment.
Elimination Route
Based on data from in vitro and animal studies, it is presumed that the metabolism of didanosine in man occurs by the same pathways responsible for the elimination of endogenous purines. Purines are eliminated by the kidneys.
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