Maa: Etelä-Afrikka
Kieli: englanti
Lähde: South African Health Products Regulatory Authority (SAHPRA)
Aspen-h
PREZISTA® (film-coated tablets) SCHEDULING STATUS: Schedule 4 PROPRIETARY NAME (and dosage form): PREZISTA® (film-coated tablets) COMPOSITION: Each film-coated tablet contains 300 mg of Darunavir (corresponding to 325,23 mg of Darunavir Ethanolate). The other ingredients are microcrystalline cellulose, colloidal anhydrous silica, crospovidone, magnesium stearate. The film-coating contains poly(vinyl alcohol) –partially hydrolyzed, macrogol 3350, titanium dioxide, talc. PHARMACOLOGICAL CLASSIFICATION: A.20.2.8 Antiviral agents. PHARMACOLOGICAL ACTION: Pharmacodynamic properties Mechanism of action Darunavir is an inhibitor of the HIV-1 protease. It selectively inhibits the cleavage of HIV encoded Gag-Pol polyproteins in virus infected cells, thereby preventing the formation of mature infectious virus particles. Darunavir tightly binds to the HIV-1 protease. Antiviral activity in-vitro Darunavir exhibited activity against laboratory strains and clinical isolates of HIV-1 and laboratory strains of HIV-2 in acutely infected T-cell lines, human peripheral blood mononuclear cells and human monocytes/macrophages in-vitro with median EC 50 values ranging from 1,2 to 8,5 nM (0,7 to 5,0 ng/mL). Darunavir demonstrated antiviral activity in- vitro against a broad panel of HIV-1 group M (A, B, C, D, E, F, G) and group O primary isolates with EC 50 values ranging from <0,1 to 4,3 nM. These EC 50 values are well below the 50% cellular toxicity concentration range of 87 µM to >100 µM. The EC 50 value of darunavir increases by a median factor of 5,4 in the presence of human serum. Darunavir showed synergistic antiviral activity when studied in combination with the protease inhibitors ritonavir, nelfinavir, or amprenavir and additive antiviral activity when studied in combination Lue koko asiakirja