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Introduction: Ayurveda, India’s ancient system of medicine, describes drug action through unique principles of Rasa Panchaka (Rasa, Guna, Veerya, Vipaka, and Prabhava), which govern both pharmacodynamics and pharmacokinetics. Unlike modern pharmacology that relies on molecular interactions, Ayurveda integrates organoleptic perception, systemic response, and post-digestive transformation into its understanding of drug efficacy. Methods: A comprehensive literature search was conducted using PubMed, Scopus, Web of Science, AYUSH Research Portal, and classical Ayurvedic texts such as Charaka Samhita, Sushruta Samhita, and Ashtanga Hridaya. Articles from 2000–2024 were reviewed, including pharmacological studies, clinical trials, and review articles linking Ayurvedic drug action to biomedical evidence. Inclusion criteria were studies explicitly connecting Ayurvedic principles with pharmacological or pharmacokinetic interpretations. Results: Analysis revealed that Ayurvedic pharmacodynamics correlates with pharmacological properties such as receptor binding, enzymatic modulation, and therapeutic specificity. For instance, tikta rasa (bitter taste) aligns with hepatoprotective and detoxifying activities, while ushna veerya (hot potency) parallels stimulant and thermogenic effects. Ayurvedic pharmacokinetics, described via Vipaka and Prabhava, relates to biotransformation, metabolic fate, and unexplained specific drug actions comparable to receptor selectivity or idiosyncrasy. Advances in metabolomics, pharmacogenomics, and nanomedicine have begun validating these principles. Discussion: While strong conceptual parallels exist, challenges include lack of standardization, insufficient mechanistic studies, and limited translational evidence. Integrating Ayurveda with systems biology and modern pharmacology offers opportunities for personalized medicine and novel drug discovery.

KEYWORDS: Ayurveda; Bioavailability; Pharmacodynamics; Pharmacokinetics; Rasa Panchaka