Delavirdina Uses, Dosage, Side Effects and more
A potent, non-nucleoside reverse transcriptase inhibitor with activity specific for HIV-1.
Delavirdina is a non-nucleoside reverse transcriptase inhibitor (nNRTI) with activity against Human Immunodeficiency Virus Type 1 (HIV-1). Delavirdina binds directly to reverse transcriptase (RT) and blocks the RNA-dependent and DNA-dependent DNA polymerase activities by causing a disruption of the enzyme's catalytic site. The activity of Delavirdina does not compete with template or nucleoside triphosphates. HIV-2 RT and eukaryotic DNA polymerases (such as human DNA polymerases alpha, beta, or sigma) are not inhibited by Delavirdina.
| Attribute | Details |
|---|---|
| Trade Name | Delavirdina |
| Availability | Discontinued |
| Generic | Delavirdine |
| Delavirdine Other Names | Delavirdin, Delavirdina, Delavirdine, Delavirdinum |
| Related Drugs | Biktarvy, Truvada, tenofovir, ritonavir, Complera, Atripla, Stribild |
| Type | |
| Formula | C22H28N6O3S |
| Weight | Average: 456.561 Monoisotopic: 456.194359482 |
| Protein binding | 98% |
| Groups | Approved |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | January 7, 2025 at 1:49 am |
Uses
Delavirdina is a non-nucleoside reverse transcriptase inhibitor used to treat HIV infection.
For the treatment of HIV-1 infection in combination with appropriate antiretroviral agents when therapy is warranted
Delavirdina is also used to associated treatment for these conditions: Human Immunodeficiency Virus Type 1 (HIV-1) Infection
How Delavirdina works
Delavirdina binds directly to viral reverse transcriptase (RT) and blocks the RNA-dependent and DNA-dependent DNA polymerase activities by disrupting the enzyme's catalytic site.
Toxicity
Major toxicity of delavirdine is rash and should be advised to promptly notify their physician should rash occur. The majority of rashes associated with delavirdine occur within 1 to 3 weeks after initiating treatment with delavirdine. The rash normally resolves in 3 to 14 days and may be treated symptomatically while therapy with delavirdine is continued. Any patient experiencing severe rash or rash accompanied by symptoms such as fever, blistering, oral lesions, conjunctivitis, swelling, muscle or joint aches should discontinue medication and consult a physician.
Food Interaction
- Take with or without food. The absorption is unaffected by food.
Drug Interaction
Moderate: esomeprazole, esomeprazole, ritonavir, ritonavirUnknown: lactobacillus acidophilus, lactobacillus acidophilus, nitazoxanide, nitazoxanide, dicyclomine, dicyclomine, lamivudine, lamivudine, crofelemer, crofelemer, enfuvirtide, enfuvirtide, raltegravir, raltegravir, atropine / diphenoxylate, atropine / diphenoxylate
Disease Interaction
Moderate: achlorhydria, liver disease
Elimination Route
Rapidly absorbed
Half Life
5.8 hours
Elimination Route
Delavirdina is extensively converted to several inactive metabolites by cytochrome P450 3A (CYP3A). Delavirdina was excreted in the milk of lactating rats at a concentration three to five times that of rat plasma.
