Drug intelligence / Profile preview

citrus aurantium

Development stage
Unknown
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral, Topical, Inhalation
01

Overview

Citrus aurantium (bitter orange) is a plant whose fruit and extracts are used in dietary supplements and traditional medicine. The primary bioactive compound is p-synephrine—a protoalkaloid structurally similar to ephedrine but with different pharmacological properties. Citrus aurantium has been promoted for weight management and sports performance after the ban of ephedra-based products. Its mechanisms include mild stimulation of the cardiovascular system (vasoconstriction and increased heart rate/blood pressure), antioxidant activity via flavonoids (naringin, hesperidin), anti-inflammatory effects through cytokine modulation and COX inhibition[2][5]. It also exhibits antispasmodic and digestive tonic actions; extracts have shown gastroprotective effects in animal models[5]. Bitter orange may inhibit intestinal CYP3A4 enzymes affecting drug metabolism[2][3]. There are safety concerns regarding cardiovascular toxicity when combined with other stimulants or in high doses; adverse events such as arrhythmias or hypertension have been reported mostly with multi-ingredient supplements rather than pure C. aurantium alone[1][2].

Brand names
Advantra ZKinetiqCitrusRx
Other names
bigaradebitter orangebitter orange flowerbitter orange peelgreen orangekijitsularanja-amargalaranja-azedalaranja-cavaloneroli flowersneroli oilseville orangeshangzhou zhiqiaosour orangezhi qiaozhi shi
02

Targets

CYP3A4 (Cytochrome P450 3A4)AR (Adrenergic receptors)

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