Polycystic Ovary Syndrome (PCOS) is a complex disease characterised by hyperandrogenism, menstrual irregularities, and the presence of cysts on one or both ovaries, posing not only immediate hormonal and metabolic effects but also long-term effects, including infertility and an increased risk of endometrial cancer. The use of Combined Oral Contraceptives (COCs) has been a breakthrough in the treatment of PCOS. The pharmacology of COCs is a key aspect of a proper management of PCOS, and for predicting and preventing side effects that follow these drugs. This work comprehensively examines the pharmacological aspects of hormonal and metabolic outcomes of the COCs, especially focusing on the later generations of COCs that are commonly used clinically today. Also included are some recommended clinical uses of each generation as the progestin component and dose of the COCs greatly influence the effect of the COCs. While COCs play a vital role in controlling PCOS, challenges persist, including the limited research on the hormonal and metabolic outcomes, as well as the complexity of the disease itself, especially when exploring the metabolic outcomes of the COCs. A foundational understanding of both PCOS and COCs is essential for medical students, healthcare workers and physicians to effectively approach this complex disease and to manage its complicated symptoms.