Tuberculosis is the most common opportunistic infection associated with HIV/AIDS, and remains a disease of global significance. Co-infection with HIV complicates proper TB diagnosis and therapeutic outcomes. Profound immunosuppression characterizes HIV/TB co-infection prompting early initiation of HAART during TB treatment. Effective management of the co-infection requires concomitant administration of ART and anti-tuberculosis drugs; however, this therapeutic approach has had its fair share of challenges including: overlapping drug toxicities, drugdrug interactions and immune reconstitution reactions. For instance, combination of nevirapine-based ART and rifampicin-based TB treatment is reported to cause hepatotoxicity in healthy volunteers. As such, this review compiles information from multiple studies describing drug interactions associated with co-treatments, with a view to improving management of these co-morbidities.