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Higenamine

What other names is Higenamine known by?

1-[(4-Hydroxyphenyl)methyl]-1,2,3,4-tetrahydroisoquinoline-6,7-diol; 1-(p-hydroxybenzyl)-6,7-Dihydroxy-1,2,3,4-Tetrahydroisoquinolin; 1(S)-Norcoclaurine; dl-Demethylcoclaurine; DMC; Higénamine; Higenamine Hydrobromide; Higenamine Hydrochloride; Higenamine Oxalate; Higenamine Tartrate; Norcoclaurine; O-Demethylcoclaurine.

What is Higenamine?

Higenamine is a chemical found in several plants including aconite, Annona squamosa, Nandina domestica (sacred bamboo), and others.

In supplements, higenamine is now showing up in products promoted as a pre-workout supplement for improving athletic performance. There is also interest in using higenamine for weight loss, cough, asthma, heart failure, and erectile dysfunction.

Insufficient Evidence to Rate Effectiveness for...

  • Weight loss.
  • Athletic performance.
  • Cough.
  • Asthma.
  • Breathing disorders.
  • Heart failure.
  • Erectile dysfunction.
  • Other conditions.
More evidence is needed to rate higenamine for these uses.

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How does Higenamine work?

Higenamine works like a stimulant. In some parts of the body it causes tissues to relax. In other parts of the body, such as the heart, it causes tissue to contract. It seems to increase heart contractions and speed up the heart rate.

Are there safety concerns?

Higenamine is POSSIBLY UNSAFE when taken by mouth. The purified or extracted chemical higenamine has not been studied in people. Therefore, its safety is not clear. However, higenamine is one of the main chemicals in a plant called aconite. Aconite has been shown to cause serious heart-related side effects including arrhythmias and even death. These side effects from aconite ingestions may, in part, be caused by the higenamine chemical.

Special Precautions & Warnings:

Pregnancy and breast-feeding: There is not enough information to know if higenamine is safe during pregnancy and breast feeding. It should be avoided.

Irregular heartbeat (heart arrhythmia): Higenamine might cause a rapid heartbeat. Therefore it could potentially worsen an irregular heartbeat. If you have an irregular heartbeat, do not take higenamine.

Surgery: Higenamine acts like a stimulant, so it might interfere with surgery by increasing heart rate. Stop taking higenamine at least 2 weeks before a scheduled surgery.

Are there any interactions with medications?


Medications that slow blood clotting (Anticoagulant / Antiplatelet drugs)Interaction Rating: Moderate Be cautious with this combination.Talk with your health provider.

Higenamine might slow blood clotting. Taking it along with other medications that might slow blood clotting might increase the chances of bruising and bleeding.

Some medications that slow blood clotting include aspirin, clopidogrel (Plavix), diclofenac (Voltaren, Cataflam, others), ibuprofen (Advil, Motrin, others), naproxen (Anaprox, Naprosyn, others), dalteparin (Fragmin), enoxaparin (Lovenox), heparin, warfarin (Coumadin), and others.


Stimulant drugsInteraction Rating: Moderate Be cautious with this combination.Talk with your health provider.

Stimulant drugs can speed up the nervous system and heart. By speeding up the nervous system, stimulant medications can make you feel jittery and speed up your heartbeat. Higenamine might also speed up the nervous system and heart. Taking higenamine along with stimulant drugs might cause serious problems such as an increased heart rate. Avoid taking stimulant drugs along with higenamine.

Some stimulant drugs include diethylpropion (Tenuate), epinephrine, phentermine (Ionamin), pseudoephedrine (Sudafed), and many others.


Propranolol (Inderal)Interaction Rating: Minor Be cautious with this combination.Talk with your health provider.

Higenamine stimulates the heart and causes it to beat faster and stronger. Taking propranolol (Inderal) seems to reduce this effect.

Dosing considerations for Higenamine.

The appropriate dose of higenamine depends on several factors such as the user's age, health, and several other conditions. At this time there is not enough scientific information to determine an appropriate range of doses for higenamine. Keep in mind that natural products are not always necessarily safe and dosages can be important. Be sure to follow relevant directions on product labels and consult your pharmacist or physician or other healthcare professional before using.

Natural Medicines Comprehensive Database rates effectiveness based on scientific evidence according to the following scale: Effective, Likely Effective, Possibly Effective, Possibly Ineffective, Likely Ineffective, and Insufficient Evidence to Rate (detailed description of each of the ratings).

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Reviewed on 9/17/2019
References

Bai G, Yang Y, Shi Q, et al. Identification of higenamine in Radix Aconiti Lateralis Preparata as a beta2-adrenergic receptor agonist1. Acta Pharmacol Sin 2008;29:1187-94. View abstract.

Bao YX, Yu GR, Xu JM, et al. Effect of acute higenamine administration on bradyarrhythmias and HIS bundle. A clinical study of 14 cases and animal experiment on dogs. Chin Med J 1982;95:781-4. View abstract.

But PP, Tai YT, Young K. Three fatal cases of herbal aconite poisoning. Vet Hum Toxicol 1994;36:212-5. View abstract.

Feng S, Hu P, Jiang J. Determination of higenamine in human plasma and urine using liquid chromatography coupled to positive electrospray ionization tandem mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci 2011;879:763-8. View abstract.

Huang XN, Shi JS, Lu WQ, Liu GX. Antiasthmatic effect of higenamine. Chin Pharm Bull 1985;20:462-4.

Kam SC, Do JM, Choi JH, et al. The relaxation effect and mechanism of action of higenamine in the rat corpus cavernosum. Int J Impot Res 2012;24:77-83. View abstract.

Kang YJ, Lee YS, Lee GW, et al. Inhibition of activation of nuclear factor kappaB is responsible for inhibition of inducible nitric oxide synthase expression by higenamine, an active component of aconite root. J Pharmacol Exp Ther 1999;291:314-20. View abstract.

Kosuge T, Yokota M, Nagasawa M. Studies on cardiac principle in aconite roots. 1. Isolation and structural determination of higenamine. J Pharm Soc Jap 1978;98:1370-5. View abstract.

Lin CC, Chan TY, Deng JF. Clinical features and management of herb-induced aconitine poisoning. Ann Emerg Med 2004;43:574-9. View abstract.

Liu WH, Zhou YP, Zeng GY. Effects of dl-demethylcoclaurine on experimental heart failure. Acta Pharm Sinica 1988;23:81-5. View abstract.

Liu Y, Santillo MF. Cytochrome P450 2D6 and 3A4 enzyme inhibition by amine stimulants in dietary supplements. Drug Test Anal. 2016;8(3-4):307-10. View abstract.

Park CW, Chang KC, Lim JK. Effects of higenamine on isolated heart adrenoceptor of rabbit. Arch Int Pharmacodyn Ther 1984;267:279-88. View abstract.

Tai YT, But PP, Young K, et al. Cardiotoxicity after accidental herb-induced aconite poisoning. Lancet 1992;340:1254-6. View abstract.

Tsukiyama M, Ueki T, Yasuda Y, et al. Beta2-adrenoceptor-mediated tracheal relaxation induced by higenamine from Nandina domestica Thunberg. Planta Med 2009;75:1393-9. View abstract.

Wagner H, Reiter M, Ferstl W. New drugs with cardiotonic activity. Part 1. Chemistry and pharmacology of the cardiotonic active principle of Annona squamosa L. Planta Med 1980;40:77-85. View abstract.

Yeih DF, Chiang FT, Huang SKS. Successful treatment of aconitine induced life threatening ventricular tachyarrhythmia with amiodarone. Heart 2000;84:E8. View abstract.

Yun-Choi HS, Pyo MK, Park KM, et al. Anti-thrombotic effects of higenamine. Planta Med 2001;67:619-22. View abstract.

Zhang Z, Liu X, Tao Z, et al. Effects of higeramine on hemodynamics and its tolerability and safety, an experimental study. Zhonghua Yi Xue Za Zhi 2002;82:352-5. View abstract.

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