Bitter Orange

(BAN, rINN)
Synonyms: Aurantii amari flos (bitter-orange flower); Aurantii Amari Pericarpium (bitter orange fruit); Bigaradier; Karčiavaisiu citrinmedžiu (bitter-orange flower); Květ hořkého pomeranče (bitter-orange flower); Naranja Amarga; Naranja amarga, corteza de; Oranger amer, fleur d’ (bitter-orange flower); Owocnia pomarańczy gorzkiej (bitter orange fruit); Pomeransblomma (bitter-orange flower); Pomeranssinkukka (bitter-orange flower); Pomeranze; Seville Orange.
Cyrillic synonym: Апельсин; Померанец.

💊 Chemical information

Pharmacopoeias.

Eur. includes the dried peel and flowers. Jpn includes the peel.

Ph. Eur. 6.2 (Bitter-orange Epicarp and Mesocarp; Aurantii amari epicarpium et mesocarpium; Dried Bitter-orange Peel BP 2008). The dried epicarp and mesocarp of the ripe fruit of Citrus aurantium, partly freed from the white spongy tissue of the mesocarp and endocarp, containing a minimum of 2.0% v/w of essential oil, calculated with reference to the anhydrous drug. It has an aromatic odour and a spicy bitter taste.

Ph. Eur. 6.2 (Bitter-orange Flower; Aurantii amari flos). The whole, dried, unopened flower of C. aurantium subsp. aurantium containing a minimum of 8.0% of total flavonoids, expressed as naringin (C 27 H 32 O 14 = 580.5), calculated with reference to the dried drug.

💊 Profile

The dried peel of the bitter orange, Citrus aurantium subsp. aurantium (Citrus aurantium subsp. amara) (Rutaceae) is used as a flavour and for its bitter and carminative properties. An essential oil is prepared from fresh bitter-orange peel (bitter-orange oil) and is similar to sweet orange oil. Both bitterorange oil and petitgrain bigarade oil (prepared from the leaves and twigs) are used in aromatherapy. The flowers are an ingredient of herbal remedies used for nervous and sleep disorders. Bitter-orange flower is the source of Neroli Oil. The whole dried immature fruit is used similarly to the dried peel. In Chinese medicine, the dried immature fruits are known as zhi shi and zhi qiao. Photosensitivity is associated with citrus oils.

Action and use.

Citrus aurantium was one of the most frequently used herbal remedies in Puerto Rico.1 Indications included sleep disorders, gastrointestinal disorders, respiratory ailments, and raised blood pressure. The volatile oil of dried bitter-orange peel has shown antifungal activity.2 Bitter-orange extract has been added to herbal weight loss remedies as it contains the sympathomimetic synephrine (a name that has been used for both phenylephrine and oxedrine), which is claimed to increase metabolism and promote thermogenesis, although efficacy is not proven. Variant angina3 and ischaemic colitis4 have been reported in patients taking dietary supplements containing bitter orange, and reports of serious cardiovascular adverse effects possibly associated with the synephrine content of bitter orange present in such preparations have been received in Canada.5,6 Raised systolic and diastolic blood pressure and heart rate were seen after ingestion of a proprietary bitter orange preparation in one small randomised placebo-controlled crossover study.7 However, in a similar study8 comparing a single-ingredient bitter orange preparation with a combination preparation, adverse haemodynamic effects appeared to be related to the additional presence of other possible stimulants such as caffeine, rather than directly proportional to the dose of bitter orange alone.
1. Hernández L, et al. Use of medicinal plants by ambulatory patients in Puerto Rico. Am J Hosp Pharm 1984; 41: 2060–4
2. Ramadan W, et al. Oil of bitter orange: new topical antifungal agent. Int J Dermatol 1996; 35: 448–9
3. Gange CA, et al. Variant angina associated with bitter orange in a dietary supplement. Mayo Clin Proc 2006; 81: 545–8
4. Sultan S, et al. Ischemic colitis associated with use of a bitter orange-containing dietary weight-loss supplement. Mayo Clin Proc 2006; 81: 1630–1
5. Health Canada. Products containing bitter orange or synephrine: suspected cardiovascular adverse reactions. Can Adverse React News 2004; 14 (4): 3–4. Also available at: http:// www.hc-sc.gc.ca/dhp-mps/alt_formats/hpfb-dgpsa/pdf/ medeff/carn-bcei_v14n4-eng.pdf (accessed 06/08/08
6. Health Canada. Bitter orange or synephrine: update on cardiovascular adverse reactions. Can Adverse React News 2007; 17 (2): 2–3. Also available at: http://www.hc-sc.gc.ca/dhp-mps/ alt_formats/hpfb-dgpsa/pdf/medeff/carn-bcei_v17n2-eng.pdf (accessed 06/08/08
7. Bui LT, et al. Blood pressure and heart rate effects following a single dose of bitter orange. Ann Pharmacother 2006; 40: 53–7
8. Haller CA, et al. Hemodynamic effects of ephedra-free weightloss supplements in humans. Am J Med 2005; 118: 998–1003.

💊 Preparations

BP 2008: Concentrated Compound Gentian Infusion; Concentrated Orange Peel Infusion; Orange Peel Infusion; Orange Syrup; Ph. Eur.: Bitter-Orange-Epicarp and Mesocarp Tincture.

Proprietary Preparations

Ger.: Carvomin Magentropfen mit Pomeranze†. Multi-ingredient: Arg.: Calmtabs†; Hepatodirectol; Austria: China-Eisenwein; Eicebaer; Ferrovin-Chinaeisenwein; Mariazeller; Montana; SigmanHaustropfen; St Bonifatius-Tee; Tussimont; Canad.: Biotrim†; Cz.: Klosterfrau Melisana; Naturland Grosser Swedenbitter†; Pleumolysin; Schlaf-Nerventee N†; Fr.: Calmophytum; Elixir Bonjean; Elixir Grez†; Mediflor Tisane Calmante Troubles du Sommeil No 14; Quintonine; Vegetoserum; Ger.: Carminativum-Hetterich; Doppelherz Melissengeist†; Gallexier; Gastrosecur†; Montana N; Sedovent; Hong Kong: LEAN Formula w/ Advantra†; India: Toniazol†; Indon.: Jesscool; Israel: Passiflora; Ital.: Assenzio (Specie Composta)†; Gastro-Pepsin; Genziana (Specie Composta)†; Valeriana (Specie Composta)†; Pol.: Herbaton; Krople Zoladkowe; Rus.: Doppelherz Melissa (Доппельгерц Мелисса); Original Grosser Bittner Balsam (Оригинальный Большой Бальзам Биттнера); S.Afr.: Versterkdruppels; Singapore: Chitosano; Spain: Euzymina Lisina I; Euzymina Lisina II; Jaquesor†; Natusor Jaquesan†; Sedonat; Switz.: Pastilles pectorales Demo N; Phytomed Nervo†; Tisane calmante pour les enfants; Tisane pour le sommeil et les nerfs; UK: Vital Eyes.
Published May 08, 2019.