Bisphosphonates are chemical-related to pyrophosphate. The oxygen atom in pyrophosphate is substituted by a carbon atom in these compounds, resulting in a P-C-P bond. They are potent antiresorptive medicines because they have a strong inhibitory effect on osteoclasts. It lowers fracture risk by reducing bone turnover, increasing bone mineral density, and decreasing fracture risk in the lumbar spine and hip. Bisphosphonates are strongly attracted to bone surfaces, where they accumulate, primarily at remodeling sites. They are rarely associated with systemic side effects due to their selectivity in action. Irritation of the upper gastrointestinal tract is the most common side effect. A strong third-generation bisphosphonate, zoledronate, is currently approved to treat postmenopausal-induced osteoporosis. This review mainly focuses on the mechanism of action, therapeutic uses, and its adverse effects.