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The aim of this work was the determination of <i>Pelargonium graveolens</i> (aerial parts) volatile compounds at three developmental stages and the evaluation of their antioxidant, antidiabetic, dermaprotective, anti-inflammatory, and antibacterial effects. The aerial parts of <i>Pelargonium graveolens</i> were collected at three stages, namely the vegetative, beginning, and full flowering. <i>Pelargonium graveolens</i> essential oils were extracted from the dried materials of these aerial parts by hydrodistillation. The volatiles were analyzed by Gas Chromatography-Mass Spectrometry GC-MS, and the antioxidant activity was assessed by DPPH, ABTS, H₂O₂, and FRAP assays. The in vitro antidiabetic effect was evaluated by the inhibition of α-amylase, α-glucosidase, and lipase enzymes, while the antibacterial activity was assessed against six bacterial strains using an agar well diffusion assay and a microdilution method. The main constituents were menthol, menthene, eremophilene, isoborneol, isogeraniol, α-pinene, linalyl acetate, and 3-carene, with quantitative differences at the three phenological stages. The essential oil at the full flowering stage showed the best antioxidant activity, with IC₅₀ values of 83.26 ± 0.01, 116.42 ± 0.07, 132.25 ± 0.11, and 48.67 ± 0.04 μg/mL for DPPH, FRAP, ABTS, and H₂O₂ assays, respectively. This oil also exhibited significant effects against α-amylase (IC₅₀ = 43.33 ± 0.01 μg/mL), α-glucosidase (IC₅₀ = 19.04 ± 0.01 μg/mL), lipase (IC₅₀ = 24.33 ± 0.05 μg/mL), 5-lipoxygenase (IC₅₀ = 39.31 ± 0.01 μg/mL), and tyrosinase (IC₅₀ = 124.49 ± 0.07 μg/mL). The essential oil extracted at the full flowering stage showed the best antibacterial effect against a panel of microorganisms with diameter inhibition zones ranging between 11.00 ± 0.17 mm and 17.30 ± 0.17 mm and MIC values from 0.25% to 2% <i>v</i>/<i>v</i>. Overall, the results presented here suggest that the full flowering stage is the best optimal harvest time of <i>Pelargonium graveolens</i> for food and pharmaceutical applications.