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The survive ratio of HIV infected patients has been increased with highly active antiretroviral therapy. However, some new questions have been raised such as drug resistance, drug toxicity and drug-drug interactions. Researchers have conducted many studies on relationship between plasma drug concentrations and efficacy and/or toxicity and they identified that therapeutic drug monitoring (TDM) of antiretroviral drugs is essential in clinical care to determine the best dosage regimen adapted to each individual to reduce the risk of virologic failure from low plasma drug concentrations and to limit the toxicity linked to high plasma drug concentrations.