Lopinavir
Mechanism :
Lopinavir, an inhibitor of the HIV protease, prevents cleavage of the Gag-Pol polyprotein, resulting in the production of immature, non-infectious viral particles.
Indication :
- Combination with other antiretroviral agents for the treatment of HIV-infection along with ritonavir
Contraindications :
Contraindicated in patients with known hypersensitivity to any of its ingredients, including ritonavir.
Dosing :
2 weeks to 6 months:
300 mg/75 mg (LPV/r)/m², or 16 mg/4 mg (LPV/r)/kg orally, every 12 hours.
6 months-18 years:
450 mg/m²/day along with
ritonavir 108 mg/m²/day PO divided in 12 hours.
Adverse Effect :
Increased spontaneous bleeding in patients with haemophilia, liver function abnormalities, pancreatitis; dyspepsia, arthralgia, new onset diabetes mellitus, exacerbation of pre-existing diabetes mellitus, hyperglycemia, anaphylactoid reactions, urticaria, vasculitis, depression, oral paraesthesia, rash including erythema multiforme and Stevens-Johnson syndrome, hyperpigmentation, alopecia, paronychia, ingrown toenails, pruritus, redistribution/accumulation of body fat, urolithiasis, nephrolithiasis, increased serum cholesterol, increased serum triglycerides, myocardial infarction.
Interaction :
CYP3A Drugs: Lopinavir is an inhibitor of CYP3A (cytochrome P450 3A) both in vitro and in vivo. Co-administration of drugs primarily metabolized by CYP3A (e.g., dihydropyridine calcium channel blockers, HMG-CoA reductase inhibitors, immunosuppressants and sildenafil) may result in increased plasma concentrations of the other drugs that could increase or prolong their therapeutic and adverse effects.
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. Monitor closely |
Dose in Patients undergoing Renal Replacement Therapies
| CAPD | Unlikely to be dialysed. Dose as in GFR<10 mL/min |
| HD | Unlikely to be dialysed. Dose as in GFR<10 mL/min |
| HDF/High flux | Unlikely to be dialysed. Dose as in GFR<10 mL/min |
| CAV/VVHD | Unknown dialysability. Dose as in normal renal function |
Hepatic Dose :
Use with caution in hepatic impairment. Mild to moderate impairment: There are no dosage adjustments recommended; however, lopinavir AUC may be increased ~30% in patients with mild to moderate hepatic impairment; use with caution.
Severe impairment: No data is available. It should not be given in patients with severe impairment.