Delavirdine Mesylate
Name: Delavirdine Mesylate
- Delavirdine Mesylate 600 mg
- Delavirdine Mesylate dosage
- Delavirdine Mesylate drug
- Delavirdine Mesylate adverse effects
Interactions for Delavirdine Mesylate
Metabolized by CYP3A and CYP2D6.1
Inhibits CYP3A and, to a lesser extent, 2C9, 2D6, and 2C19.1
Drugs Affecting or Metabolized by Hepatic Microsomal Enzymes
Pharmacokinetic interactions likely with drugs that are inhibitors, inducers, or substrates of CYP3A;1 possible alteration in metabolism of delavirdine and/or other drug.1
Specific Drugs
| Drug | Interaction | Comments |
|---|---|---|
| Amphetamines | Possible increased amphetamine concentrations1 | Use with caution1 |
| Antacids, aluminum- or magnesium-containing | Decreased delavirdine concentrations1 | Take delavirdine at least 1 hour before or after antacids1 |
| Antiarrhythmic agents (amiodarone, flecainide, systemic lidocaine, propafenone, quinidine) | Possible increased concentrations of antiarrhythmic agent; potential for serious or life-threatening effects (e.g., cardiac arrhythmias) with certain agents1 | Use concomitantly with caution; monitor plasma concentrations of antiarrhythmic agent1 |
| Anticoagulants, oral | Possible increased warfarin concentrations 1 | Monitor INR; adjust warfarin dosage accordingly1 |
| Anticonvulsants (carbamazepine, phenytoin, phenobarbital) | Decreased delavirdine concentrations; possible loss of virologic response and development of resistance to the antiretroviral and other NNRTIs1 | Do not use concomitantly with delavirdine1 |
| Antifungals, azoles (fluconazole, ketoconazole, voriconazole) | Fluconazole: Pharmacokinetic interaction not clinically important1 | |
|
| Ketoconazole: Increased delavirdine concentrations1 | |
|
| Voriconazole: Increased voriconazole concentrations53 | Voriconazole: Monitor frequently for voriconazole adverse effects53 |
| Antimycobacterials (rifabutin, rifampin, rifapentine) | Rifabutin: Decreased delavirdine AUC; increased rifabutin AUC1 Rifampin: Decreased delavirdine AUC 1 Possible loss of virologic response and increased risk of delavirdine or NNRTI resistance1 | Concomitant use with rifabutin, rifampin, or rifapentine not recommended1 34 35 200 |
| Atazanavir | No in vitro evidence of antagonistic antiretroviral effects203 |
|
| Benzodiazepines (alprazolam, midazolam, triazolam) | Potential for serious and/or life-threatening adverse effects such as prolonged or increased sedation or respiratory depression1 | Concomitant use contraindicated1 |
| Calcium-channel blocking agents (amlodipine, diltiazem, felodipine, isradipine, nifedipine, nimodipine, nisoldipine, verapamil) | Possible increased concentrations of calcium-channel blocking agent1 | Use concomitantly with caution; clinical monitoring recommended1 |
| Cisapride | Potential for serious or life-threatening reactions (e.g., cardiac arrhythmias)1 | Concomitant use contraindicated1 |
| Co-trimoxazole | Interaction unlikely1 |
|
| Corticosteroids (dexamethasone, fluticasone) | Dexamethasone: Possible decreased delavirdine concentrations 1 | Dexamethasone: Use with caution; delavirdine may be less effective1 |
|
| Fluticasone (orally inhaled, intranasal): Possible increased fluticasone concentrations1 | Fluticasone (orally inhaled, intranasal): Use concomitantly with caution; consider alternative to fluticasone, especially when long-term corticosteroid therapy is anticipated1 |
| Darunavir | No in vitro evidence of antagonistic antiretroviral effects204 |
|
| Didanosine | Decreased delavirdine concentrations if given at same time as buffered didanosine preparations;1 clinically important pharmacokinetic interaction not observed when buffered didanosine administered 1 hour after delavirdine1 In vitro evidence of additive to synergistic antiretroviral effects1 | Administer buffered didanosine (pediatric oral solution admixed with antacid) at least 1 hour before or after delavirdine1 |
| Efavirenz |
| Do not use concomitantly1 200 |
| Emtricitabine | In vitro evidence of additive or synergistic antiretroviral effects218 | |
| Ergot alkaloids (dihydroergotamine, ergonovine, ergotamine, methylergonovine) | Concomitant use contraindicated1 | |
| Estrogens/Progestins | Hormonal contraceptives: Possible increased concentrations of ethinyl estradiol1 | Clinical importance unknown1 |
| Etravirine | Possible increased etravirine concentrations214 | Do not use concomitantly1 200 214 |
| Fluoxetine | Increased delavirdine trough concentrations1 |
|
| Fosamprenavir | Studies using amprenavir (active metabolite of fosamprenavir) indicate increased amprenavir concentrations and AUC and possible decreased delavirdine concentrations and AUC;205 possible decreased antiretroviral efficacy and increased risk of antiretroviral resistance205 In vitro evidence of synergistic antiretroviral effects205 | Fosamprenavir (with or without low-dose ritonavir): Concomitant use contraindicated205 |
| Histamine H2-receptor antagonists (cimetidine, famotidine, nizatidine, ranitidine) | Possible decreased GI absorption of delavirdine1 | Long-term concomitant use not recommended1 |
| HMG-CoA reductase inhibitors (statins) | Atorvastatin, fluvastatin, lovastatin, simvastatin: Possible increased concentrations of the antilipemic agents; increased risk of myopathy and/or rhabdomyolysis1 | Atorvastatin: Use lowest possible atorvastatin dosage;1 consider using pravastatin instead1 Fluvastatin: Use lowest possible fluvastatin dosage;1 consider using pravastatin instead1 Lovastatin: Do not use concomitantly1 Simvastatin: Do not use concomitantly1 |
| Immunosuppressive agents (cyclosporine, sirolimus, tacrolimus) | Potential for increased concentrations of cyclosporine, sirolimus, or tacrolimus1 | Monitor plasma concentrations of immunosuppressive agent1 |
| Indinavir | Delavirdine inhibits indinavir metabolism and may increase indinavir concentrations and AUC; no effect on delavirdine pharmacokinetics1 206 | Use reduced indinavir dosage of 600 mg every 8 hours with usual delavirdine dosage (400 mg 3 times daily)1 206 |
| Lamivudine | In vitro evidence of additive or synergistic antiretroviral effects1 |
|
| Lopinavir/ritonavir | Possible increased lopinavir concentrations1 | Appropriate dosages for concomitant use with respect to safety and efficacy not established1 |
| Macrolides (clarithromycin) | No change in delavirdine pharmacokinetic; increased clarithromycin AUC1 | Dosage adjustments not needed in patients with normal renal function; reduce clarithromycin dosage by 50% in patients with Clcr 30–60 mL/minute and by 75% in patients with Clcr <30 mL/minute1 |
| Maraviroc | Possible increased maraviroc concentrations1 No in vitro evidence of antagonistic antiretroviral effects224 | Recommended maraviroc dosage is 150 mg twice daily in patients receiving delavirdine224 |
| Methadone | Possible increased methadone concentrations1 | Methadone dosage may need to be reduced1 |
| Nelfinavir | Decreased delavirdine concentrations and AUC; increased nelfinavir concentrations and AUC1 208 In vitro evidence of synergistic antiretroviral effects208 | Appropriate dosages for concomitant use with respect to safety and efficacy not established1 208 |
| Nevirapine | Do not use concomitantly1 200 | |
| Pimozide | Potential for serious or life-threatening reactions (e.g., cardiac arrhythmias)1 | Concomitant use contraindicated1 |
| Proton-pump inhibitors (omeprazole, lansoprazole) | Possible decreased GI absorption of delavirdine1 | Long-term concomitant use not recommended1 |
| Quinupristin and dalfopristin | Possible increased delavirdine concentrations39 |
|
| Raltegravir | In vitro evidence of additive to synergistic antiretroviral effects225 | |
| Rilpivirine | Possible increased rilpivirine concentrations226 | Do not use concomitantly1 200 226 |
| Ritonavir | Increased ritonavir concentrations1 | Appropriate dosages for concomitant use with respect to safety, efficacy, and pharmacokinetics not established1 |
| Saquinavir | Increased saquinavir concentrations and AUC;1 210 no clinically important effect on delavirdine concentrations1 Ritonavir-boosted saquinavir: Concomitant use not evaluated210 | Appropriate dosages for concomitant use with respect to safety, efficacy, and pharmacokinetics not established1 210 |
| Simeprevir | Possible increased simeprevir concentrations187 | Concomitant use not recommended187 |
| St. John’s wort (Hypericum perforatum) | Possible loss of virologic response and increased risk of delavirdine or NNRTI resistance1 | Do not use concomitantly1 |
| Sildenafil | Possible increased sildenafil concentrations and increased risk of sildenafil-associated adverse effects (e.g., hypotension, visual changes, prolonged erection)1 | Use caution; do not exceed 25 mg once every 48 hours1 |
| Tenofovir | No in vitro evidence of antagonistic antiretroviral effects221 |
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| Tipranavir | In vitro evidence of additive antiretroviral effects211 |
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| Trazodone | Possible increased trazodone concentrations1 Adverse effects (nausea, dizziness, hypotension, syncope) reported with concomitant use of trazodone and other CYP3A inhibitors (e.g., ritonavir)1 | Use with caution; consider using decreased trazodone dosage1 |
| Zidovudine | No pharmacokinetic interaction1 6 In vitro evidence of additive or synergistic antiretroviral effects1 |
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