Invirase and Ketoconazole (Systemic)

In the database of official manuals used in the service creation an interaction registered by statistical results of studies was found, which can either lead to negative consequences for the patient health or strengthen a mutual positive effect. A doctor should be consulted to address the issue of joint drug administration.

Using saquinavir together with ketoconazole may increase the effects of saquinavir. Contact your doctor if you experience diarrhea, nausea, abdominal discomfort, increase in cholesterol, or changes in the shape or location of body fat. If your doctor does prescribe these medications together, you may need a dose adjustment or special test to safely use both medications. It is important to tell your doctor about all other medications you use, including vitamins and herbs. Do not stop using any medications without first talking to your doctor.

MONITOR: According to the manufacturer, ketoconazole (200 mg/day) increased the steady-state area under the plasma concentration-time curve (AUC) of saquinavir (administered as saquinavir mesylate 600 mg orally three times a day) by nearly 1.5-fold in 12 healthy volunteers, presumably due to its inhibition of saquinavir metabolism via CYP450 3A4. In a published study involving 12 HIV-infected subjects receiving both ritonavir and saquinavir mesylate (400 mg each orally twice a day), ketoconazole (200 mg or 400 mg once a day for 10 days) led to increases in the AUC and half-life of saquinavir by nearly 40%. However, a study consisting of seven HIV-infected male subjects found no significant differences in the median peak and trough levels of saquinavir following the addition of ketoconazole 200 mg/day for 7 days or 400 mg/day for another 7 days. Thus, the effect of ketoconazole on saquinavir pharmacokinetics may be inconsistent, unpredictable, and subject to substantial interpatient variability. The interaction has not been studied using the saquinavir soft gel capsule (SGC) formulation.

MANAGEMENT: When saquinavir mesylate or SGC is administered in combination with ketoconazole, patients should be monitored for potentially excessive plasma levels and increased adverse effects of saquinavir such as diarrhea, nausea, abdominal discomfort, dyspepsia, dyslipidemia, and lipodystrophy. However, ketoconazole should not be expected to reliably enhance the systemic exposure of saquinavir mesylate.

Invirase

Generic Name: saquinavir

Brand name: Invirase, Fortovase

Synonyms: n.a.

What is Invirase?

Ketoconazole (Systemic)

Generic Name: ketoconazole

Brand name: Nizoral

Synonyms: Ketoconazole

What is Ketoconazole (Systemic)?