Drug Guide
Delavirdine Mesylate
Classification
Therapeutic: Antiretroviral, NNRTI (Non-Nucleoside Reverse Transcriptase Inhibitor)
Pharmacological: Reverse Transcriptase Inhibitor
FDA Approved Indications
- Treatment of HIV-1 infection in combination with other antiretroviral agents
Mechanism of Action
Delavirdine binds non-competitively to reverse transcriptase enzyme of HIV-1, inhibiting its activity and thus preventing viral replication.
Dosage and Administration
Adult: 200 mg three times daily, with or without food
Pediatric: Not recommended for pediatric use due to limited data
Geriatric: No specific dosage adjustment, but caution in patients with comorbidities and concurrent medications
Renal Impairment: Use with caution, no specific adjustment recommended
Hepatic Impairment: Use with caution; dose adjustment may be needed in severe hepatic impairment
Pharmacokinetics
Absorption: Well absorbed orally, peak plasma levels in 2-4 hours
Distribution: Extensively bound to plasma proteins (~99%)
Metabolism: Metabolized mainly by CYP3A4 enzyme
Excretion: Primarily via feces, small amount via urine
Half Life: Approximately 5 hours
Contraindications
- Hypersensitivity to delavirdine or any component of the formulation
Precautions
- Use with caution in patients with hepatic impairment, adequate liver function monitoring is recommended. May cause hepatotoxicity.
- Coadministration with drugs highly dependent on CYP3A4 for clearance or that strongly induce or inhibit CYP3A4 can alter delavirdine levels.
Adverse Reactions - Common
- Rash (Common)
- Fatigue (Common)
- Nausea (Common)
- Headache (Common)
Adverse Reactions - Serious
- Hepatotoxicity including hepatic failure (Rare)
- Allergic reactions including angioedema or hypersensitivity (Rare)
Drug-Drug Interactions
- CYP3A4 inhibitors (e.g., ketoconazole, ritonavir) increase delavirdine levels
- CYP3A4 inducers (e.g., rifampin, carbamazepine) decrease delavirdine levels
- Other antiretrovirals and drugs metabolized by CYP enzymes
Drug-Food Interactions
- None specifically
Drug-Herb Interactions
- St. John’s Wort and other herbal products that induce CYP3A4 may decrease efficacy
Nursing Implications
Assessment: Monitor liver function tests regularly; observe for signs of hepatotoxicity. Assess for rash or allergic reactions.
Diagnoses:
- Risk for hepatotoxicity
- Impaired skin integrity related to rash
Implementation: Administer with or without food, encourage adherence, and educate patient on potential side effects.
Evaluation: Regularly evaluate viral load and CD4 counts to assess therapy effectiveness.
Patient/Family Teaching
- Take medication exactly as prescribed, at the same times daily.
- Report any signs of rash, jaundice, abdominal pain, or allergic reactions immediately.
- Avoid alcohol and hepatotoxic medications.
- Discuss potential drug interactions, especially with other prescribed drugs.
Special Considerations
Black Box Warnings:
- Hepatotoxicity, including rare cases of hepatic failure
Genetic Factors: None specified.
Lab Test Interference: No known interference but monitor liver functions closely.
Overdose Management
Signs/Symptoms: Nausea, vomiting, dizziness, somnolence, and abnormal liver function tests.
Treatment: Supportive care, monitor liver function, activated charcoal if ingestion was recent, no specific antidote.
Storage and Handling
Storage: Store at room temperature (20-25°C / 68-77°F), protect from moisture and light.
Stability: Stable under recommended storage conditions for at least 2 years.