Nelfinavir
Mechanism :
Nelfinavir inhibits the HIV viral proteinase enzyme which prevents cleavage of the gag-pol polyprotein, resulting in non-infectious, immature viral particles.
Indication :
Contraindications :
Hepatic impairment, Child-Pugh Class B or C
Hypersensitivity
Dosing :
2 to <13 years:
45 to 55 mg/kg orally 2 times a day or 25 to 35 mg/kg orally thrice a day. Maximum dose: 2500 mg/day.
>13 years:
1250 mg orally twice a day (preferred regimen) or 750 mg orally 3 times a day.
Adverse Effect :
Serious Reactions: Hyperglycemia, diabetes mellitus, hypercholesterolemia, hypertriglyceridemia, pancreatitis, hepatotoxicity, leukopenia, thrombocytopenia, anemia, hypersensitivity reaction.
Common Reactions: Diarrhea, nausea, anorexia, abdominal pain, flatulence, rash, neutropenia, leukopenia, hyperglycemia, lipodystrophy, elevated ALT/AST.
Interaction :
Abacavir: The serum concentration of Abacavir may be decreased.
Abiraterone: Strong CYP3A4 inhibitors may increase levels of abiraterone.
Acenocoumarol, Anisindione: Nelfinavir may increase the anticoagulant effect of acenocoumarol.
Alprazolam: Nelfinavir may increase the effect of the alprazolam.
Amiodarone: Nelfinavir may increase the effect and toxicity of amiodarone.
Aprepitant: This CYP3A4 inhibitor increases the effect and toxicity of Aprepitant.
Astemizole: Increased risk of cardiotoxicity and arrhythmias.
Atorvastatin, Bromazepam: Nelfinavir, a strong CYP3A4 inhibitor, may increase the serum concentration of atorvastatin by decreasing its metabolism.
Cabazitaxel: Concomitant therapy with a strong CYP3A4 inhibitor may increase concentrations of cabazitaxel.
Chlordiazepoxide: Nelfinavir may increase the effect of the benzodiazepine, chlordiazepoxide.
Cisapride: Increased risk of cardiotoxicity and arrhythmias.
Clorazepate, Clonazepam: The protease inhibitor, nelfinavir, may increase the effect of the benzodiazepines.
Midazolam: The protease inhibitor, nelfinavir, may increase the effect of the benzodiazepine, midazolam.
Pimozide: Nelfinavir increases the effect and toxicity of pimozide.
Ponatinib: Strong CYP3A4 inhibitors may increase levels of ponatinib.
Quazepam: The protease inhibitor, nelfinavir, may increase the effect of the benzodiazepine, quazepam.
Solifenacin: This potent CYP3A4 inhibitor slows darifenacin/solifenacin metabolism.
Tamoxifen: Nelfinavir may increase the serum concentration of Tamoxifen by decreasing its metabolism.
Tamsulosin: Nelfinavir, a CYP3A4 inhibitor, may decrease the metabolism and clearance of Tamsulosin, a CYP3A4 substrate.
Telaprevir: Telaprevir increases levels by affecting CYP3A4 metabolism.
Telithromycin: Nelfinavir may increase the plasma concentration of Telithromycin.
Temsirolimus: Nelfinavir may inhibit the metabolism and clearance of Temsirolimus.
Teniposide: The strong CYP3A4 inhibitor, Nelfinavir, may decrease the metabolism and clearance of Teniposide, a CYP3A4 substrate.
Terfenadine: Increased risk of cardiotoxicity and arrhythmias
Tiagabine: The strong CYP3A4 inhibitor, Nelfinavir, may decrease the metabolism and clearance of Tiagabine, a CYP3A4 substrate.
Tolterodine: Nelfinavir may decrease the metabolism and clearance of Tolterodine.
Topotecan: The p-glycoprotein inhibitor, Nelfinavir, may increase the bioavailability of oral Topotecan. A clinically significant effect is also expected with IV Topotecan.
Tramadol: Nelfinavir may increase Tramadol toxicity by decreasing Tramadol metabolism and clearance.
Triazolam, Trazodone: The protease inhibitor, nelfinavir, may increase the effect of the benzodiazepine, triazolam.
Trimipramine: The strong CYP3A4 inhibitor, Nelfinavir, may decrease the metabolism and clearance of Trimipramine, a CYP3A4 substrate.
Vardenafil: Nelfinavir, a strong CYP3A4 inhibitor, may reduce the metabolism and clearance of Vardenafil.
Vemurafenib: Strong CYP3A4 inhibitors may increase levels of vemurafenib. Monitor concomitant therapy closely.
Verapamil, Venlafaxine: Nelfinavir, a strong CYP3A4 inhibitor, may increase the serum concentration of Verapamil, a CYP3A4 substrate, by decreasing its metabolism and clearance.
Vinblastine, Vinorelbine, Vincristine: Nelfinavir, a strong CYP3A4 inhibitor, may increase the serum concentration of Vinorelbine by decreasing its metabolism.
Voriconazole: Nelfinavir may decrease the serum concentration of voriconazole likely by increasing its metabolism. Voriconazole may increase the serum concentration of nelfinavir by decreasing its metabolism.
Warfarin: The protease inhibitor, nelfinavir, may increase the anticoagulant effect of warfarin.
Zopiclone, Zonisamide, Zolpidem: Nelfinavir, a strong CYP3A4 inhibitor, may increase the serum concentration of zopiclone by decreasing its metabolism.
Renal Dose :
Dose in Renal Impairment GFR (mL/min)
| 20-50 | Dose as in normal renal function |
| 10-20 | Dose as in normal renal function |
| <10 | Dose as in normal renal function. |
Dose in Patients undergoing Renal Replacement Therapies
| CAPD | Not dialysed. Dose as in GFR<10 mL/min |
| HD | Not dialysed. Dose as in GFR<10 mL/min |
| HDF/High flux | Not dialysed. Dose as in GFR<10 mL/min |
| CAV/VVHD | Unlikely to be dialysed. Dose as in normal renal function |
Hepatic Dose :
Children =2 years and adolescents:
Mild hepatic impairment (Child-Pugh Class A): Use with caution; no dosage adjustment is necessary.
Moderate to severe hepatic impairment (Child-Pugh Class B or C): Use not recommended.