Voriconazole is an antifungal triazole, approved for management of invasive fungal diseases in patients. It is absorbed during two hours and its serum levels will be above 90%, based on the underlying factors, when the drug is administered orally. Voriconazole shows a propotional increase in an area under the plasma concentration-time curve (AUC), with increasing dose. Plasma protein binding of voriconazole is approximately 60%. Standard doses of the drug and optimal concentration are not predictable due to voriconazole’s nonlinear pharmacokinetics, drug-drug interactions, age, and genetic polymorphisms of the cytochrome CYP2C19. Therefore, in order to prevent adverse effects and optimize outcomes, therapeutic drug monitoring is highly suggested. The application of linking pharmacokinetic and pharmacodynamics characteristics provides information about the relationships between antimicrobial in vitro susceptibility, dosage, drug concentrations and antimicrobial or toxicological effects. The current review paper presents a comprehensive overview of the relation between pharmacokinetic and pharmacodynamics parameters for voriconazole treatment efficacy.