Darunavir Tablets and Halcion

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 triazolam together with darunavir is not recommended. Combining these medications may significantly increase the blood levels and effects of triazolam, which can lead to increased or prolonged drowsiness and breathing difficulties. Death may occur as a result of excessive triazolam levels. 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.

CONTRAINDICATED: Coadministration with protease inhibitors (PIs) may significantly increase the plasma concentrations and pharmacologic effects of orally administered midazolam and triazolam. The mechanism is PI inhibition of intestinal and hepatic CYP450 3A4, the isoenzyme primarily responsible for the metabolic clearance of these benzodiazepines. Within the class, ritonavir is the most potent CYP450 3A4 inhibitor, while saquinavir is considered one of the weaker ones. In six healthy volunteers, ritonavir (200 mg twice a day for 2 days) nearly doubled the peak plasma concentration (Cmax) of triazolam (0.125 mg single dose) and increased its systemic exposure (AUC) and elimination half-life by 20- and 14-fold, respectively, compared to placebo. Ritonavir also decreased triazolam clearance to less than 4% of control values. In 12 healthy volunteers, the Cmax and AUC of oral midazolam (7.5 mg single dose) increased by more than 2- and 5-fold, respectively, during coadministration with saquinavir (soft gelatin capsule 1200 mg three times a day for 5 days) relative to placebo, while oral bioavailability increased from 41% to 90%. The AUC of intravenous midazolam (0.05 mg/kg single dose) increased 2.4-fold, and mean plasma clearance decreased by 56%. In both studies, the pharmacokinetic changes were accompanied by increased sedation and impairment of psychomotor performance.

MANAGEMENT: Given the potential for prolonged and/or increased sedation and respiratory depression associated with excessive benzodiazepine blood levels, concomitant use of oral midazolam or triazolam with protease inhibitors is considered contraindicated. Caution and close clinical monitoring are recommended when administering parenteral midazolam in combination with protease inhibitors. Appropriate medical management should be readily available in case of respiratory depression and/or prolonged sedation. Dosage adjustment for midazolam may be appropriate, especially if more than a single dose of midazolam is administered.

Darunavir Tablets

Generic Name: darunavir

Brand name: Prezista

Synonyms: Darunavir

What is Darunavir Tablets?

Halcion

Generic Name: triazolam

Brand name: Halcion

Synonyms: n.a.

What is Halcion?