Phytocannabinoids, naturally occurring compounds derived from the *Cannabis* plant, have garnered significant attention for their potential pharmacological effects and medicinal uses. This comprehensive review explores the intricate pharmacological profiles of phytocannabinoids, focusing on their diverse impacts on biological systems. Among the over one hundred identified cannabinoids, cannabidiol (CBD) and tetrahydrocannabinol (THC) are the most extensively studied. CBD, a non-psychoactive compound, exhibits anti-inflammatory, neuroprotective, and anxiolytic properties, making it a promising candidate for treating various medical conditions. THC, known for its psychoactive effects, has analgesic and antiemetic properties, contributing to its therapeutic potential. Other phytocannabinoids, such as cannabichromene (CBC), cannabigerol (CBG), and cannabiol (CBN), also show intriguing pharmacological effects. The endocannabinoid system, comprising enzymes involved in endocannabinoid production and breakdown, cannabinoid receptors (CB1 and CB2), and endogenous ligands, is crucial for maintaining homeostasis in physiological processes. Phytocannabinoids interact with this system, modifying ion channels, neurotransmitter receptors, and anti-oxidative pathways, offering hope for novel treatment approaches in cannabinoid-based medicine. Key phytocannabinoids, including THC and CBD, have been reviewed for their pharmacological profiles. THC, the primary psychoactive compound, has analgesic and antiemetic effects, while CBD, a non-psychoactive compound, interacts with CB2 receptors and exhibits anti-inflammatory, analgesic, and neuroprotective properties. Preclinical and clinical studies have explored the anti-inflammatory, antioxidant, and pain-relieving effects of these cannabinoids, highlighting their potential in treating various conditions. Therapeutic applications of phytocannabinoids include anti-inflammatory effects, antioxidant properties, pain management, neurological disorder treatment, psychiatric condition management, and cancer treatment support. However, challenges and controversies remain, particularly in legal and regulatory issues, standardization of products, and potential for abuse and dependence. Ongoing research and preclinical trials are advancing the understanding and development of cannabinoid-based therapies. Novel delivery methods, such as transdermal and topical systems, are being explored to improve bioavailability and targeted delivery. The future holds promise for a wider range of cannabinoid-based treatments, but regulatory hurdles and further scientific investigation are necessary to fully realize their therapeutic potential.Phytocannabinoids, naturally occurring compounds derived from the *Cannabis* plant, have garnered significant attention for their potential pharmacological effects and medicinal uses. This comprehensive review explores the intricate pharmacological profiles of phytocannabinoids, focusing on their diverse impacts on biological systems. Among the over one hundred identified cannabinoids, cannabidiol (CBD) and tetrahydrocannabinol (THC) are the most extensively studied. CBD, a non-psychoactive compound, exhibits anti-inflammatory, neuroprotective, and anxiolytic properties, making it a promising candidate for treating various medical conditions. THC, known for its psychoactive effects, has analgesic and antiemetic properties, contributing to its therapeutic potential. Other phytocannabinoids, such as cannabichromene (CBC), cannabigerol (CBG), and cannabiol (CBN), also show intriguing pharmacological effects. The endocannabinoid system, comprising enzymes involved in endocannabinoid production and breakdown, cannabinoid receptors (CB1 and CB2), and endogenous ligands, is crucial for maintaining homeostasis in physiological processes. Phytocannabinoids interact with this system, modifying ion channels, neurotransmitter receptors, and anti-oxidative pathways, offering hope for novel treatment approaches in cannabinoid-based medicine. Key phytocannabinoids, including THC and CBD, have been reviewed for their pharmacological profiles. THC, the primary psychoactive compound, has analgesic and antiemetic effects, while CBD, a non-psychoactive compound, interacts with CB2 receptors and exhibits anti-inflammatory, analgesic, and neuroprotective properties. Preclinical and clinical studies have explored the anti-inflammatory, antioxidant, and pain-relieving effects of these cannabinoids, highlighting their potential in treating various conditions. Therapeutic applications of phytocannabinoids include anti-inflammatory effects, antioxidant properties, pain management, neurological disorder treatment, psychiatric condition management, and cancer treatment support. However, challenges and controversies remain, particularly in legal and regulatory issues, standardization of products, and potential for abuse and dependence. Ongoing research and preclinical trials are advancing the understanding and development of cannabinoid-based therapies. Novel delivery methods, such as transdermal and topical systems, are being explored to improve bioavailability and targeted delivery. The future holds promise for a wider range of cannabinoid-based treatments, but regulatory hurdles and further scientific investigation are necessary to fully realize their therapeutic potential.