Delavirdine uses and side effects
Table of Contents
Introduction
- Delavirdine is an antiretroviral drug.
- It belongs to the class of NNRTIs (Non-Nucleoside Reverse Transcriptase Inhibitors).
- It works by binding directly to the reverse transcriptase enzyme of HIV-1 and blocking viral replication.
- It was one of the earlier NNRTIs developed for HIV/AIDS treatment, but its use has declined due to better alternatives.
Uses
- Used in combination with other antiretroviral drugs for the treatment of HIV-1 infection.
- It helps reduce viral load and increase CD4+ cell counts, thereby improving immune function.
- Not a cure, but part of ART (Antiretroviral Therapy) to prolong life and reduce HIV transmission.
Side Effects
Common side effects:
- Rash (very frequent, sometimes severe)
- Headache
- Nausea, vomiting, diarrhea
- Fatigue
- Abdominal pain
Serious side effects (less common):
- Severe skin reactions (Stevens–Johnson syndrome, erythema multiforme)
- Liver toxicity (elevated liver enzymes, hepatitis, rarely liver failure)
- Drug interactions (it inhibits CYP3A4, so it interacts with many medications)
Popular Brand Names
- Rescriptor® (Pfizer – U.S., discontinued in 2015 due to low demand and availability of better HIV drugs).
✅ Summary:
Delavirdine (brand Rescriptor®) is an NNRTI antiretroviral used for HIV-1 treatment in combination therapy. Its use is now limited because of drug resistance, interactions, frequent rashes, and better alternatives (like efavirenz, nevirapine, rilpivirine, etravirine).
| Feature | Delavirdine | Efavirenz | Nevirapine | Rilpivirine | Etravirine |
|---|---|---|---|---|---|
| Brand Name | Rescriptor® (discontinued) | Sustiva®, also in Atripla® | Viramune® | Edurant®, also in Complera®/Odefsey® | Intelence® |
| Approval (U.S.) | 1997 | 1998 | 1996 | 2011 | 2008 |
| Generation | 1st-gen NNRTI | 1st-gen NNRTI | 1st-gen NNRTI | 2nd-gen NNRTI | 2nd-gen NNRTI |
| Dosing | 3× daily (high pill burden) | 1× daily | 2× daily (can be QD with XR) | 1× daily (with food) | 2× daily (with food) |
| Potency | Weaker vs others | Strong, widely used | Moderate | Stronger, good tolerability | Strong, used in resistant HIV |
| Common Side Effects | Rash, headache, nausea | CNS effects (vivid dreams, dizziness, mood changes), rash | Rash, hepatotoxicity (esp. women, higher CD4 count) | Depression, insomnia, headache | Rash, nausea, mild GI upset |
| Serious Risks | Severe rash, liver toxicity, major drug interactions | Suicidality risk, teratogenic (avoid in pregnancy) | Severe rash (SJS/TEN), liver failure | Not effective if viral load >100,000 or CD4 <200 | Rash, hypersensitivity, resistance mutations |
| Drug Interactions | Strong CYP3A4 inhibitor → many interactions | CYP3A4 inducer | CYP3A4 inducer | Fewer interactions | Fewer interactions |
| Current Use | Obsolete (discontinued) | Still used, but declining | Limited use (esp. resource-limited settings) | Preferred in some modern regimens | Used for resistant HIV strains |
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