Herbal medicines have been integral to human healthcare for centuries, providing a rich source of therapeutic agents derived from plants. This comprehensive review explores the multifaceted aspects of herbal medicines, encompassing their phytochemistry, pharmacology, efficacy, safety, regulation, and integration into modern healthcare. Herbal medicines contain a diverse array of bioactive compounds, such as alkaloids, flavonoids, terpenoids, glycosides, and phenolic acids, which contribute to their therapeutic effects. Clinical studies and meta-analyses have demonstrated the efficacy of certain herbal medicines, including Ginkgo biloba for cognitive decline, St. John’s Wort for depression, and turmeric for osteoarthritis. However, the variability in product composition and study quality highlights the need for more rigorous and standardized research. Safety concerns, including adverse effects and herb-drug interactions, are significant considerations. Regulatory frameworks and pharmacovigilance systems are essential to monitor and mitigate these risks, ensuring the safe use of herbal medicines. The regulation and standardization of herbal products vary globally, with different countries adopting diverse approaches. Advances in analytical techniques, such as high-performance liquid chromatography (HPLC) and mass spectrometry (MS), play a crucial role in ensuring the quality and consistency of herbal medicines. Ethnopharmacology and traditional knowledge are invaluable in the discovery of new herbal medicines. Ethical considerations, such as benefit-sharing and informed consent, are critical in respecting the contributions of indigenous communities. Current challenges in the field include variability in product quality, lack of robust clinical evidence, and potential herb-drug interactions. Future research should focus on large-scale clinical trials, mechanistic studies, long-term safety assessments, and personalized medicine approaches. Integrating herbal medicines into mainstream healthcare involves regulatory harmonization, development of clinical guidelines, education and training for healthcare providers, and public health initiatives to promote safe use. Collaborative care that combines conventional and alternative medicine practices can enhance patient outcomes and satisfaction. This review underscores the importance of a balanced approach that respects traditional knowledge while embracing scientific rigor, ultimately contributing to the well-being of patients worldwide.