Malaria remains one of the most significant infectious diseases worldwide, with a devastating impact on public health, particularly in regions with limited resources. The pharmacology of antimalarial drugs is a crucial aspect of malaria control strategies, encompassing the understanding of drug mechanisms, pharmacokinetics, pharmacodynamics, resistance patterns, and adverse effects. This work comprehensively examines the pharmacological aspects of antimalarial drugs, covering some of the major drugs belonging to the classes such as quinolines, artemisinin derivatives, antifolates, and antimicrobials. Also included are the most notable combinations in the treatment of malaria. Additionally exploration of the complex mechanisms of action employed by these drugs to combat the Plasmodium parasites is covered. While antimalarial drugs play a vital role in malaria control and elimination efforts, challenges persist, including the spread of drug-resistant parasites, limited access to treatment in endemic regions, and gaps in healthcare infrastructure. A foundational understanding of the pharmacology of antimalarial drugs is essential for medical students, healthcare workers and physicians to effectively manage malaria cases, advocate for public health interventions, and contribute to malaria eradication efforts worldwide.