Aconitine is a C19 norditerpenoid alkaloid (DITERPENES) from the root of ACONITUM plants. It activates VOLTAGE-GATED SODIUM CHANNELS. It has been used to induce ARRHYTHMIAS in experimental animals and it has anti-inflammatory and antineuralgic properties.
Aconitine is a diterpenoid that is 20-ethyl-3alpha,13,15alpha-trihydroxy-1alpha,6alpha,16beta-trimethoxy-4-(methoxymethyl)aconitine-8,14alpha-diol having acetate and benzoate groups at the 8- and 14-positions respectively. It derives from an aconite.
Aconite is one of our oldest remedies, having been one of the substances proved by Samuel Hahnemann and described in the first volume of his landmark text, the Materia Medica Pura. The homeopathic remedy is prepared from the whole fresh plant as it comes into flower. Hahnemann saw it as being a short-acting remedy that was very valuable in acute inflammatory and sometimes life-threatening conditions. James Tyler Kent also took this view and said that it is “a short-acting remedy. Its symptoms do not last long… There are no chronic diseases following it.” Since then many homeopathic texts have boldly stated that it is only an acute remedy. Well, I believe that it is indeed a great acute remedy, but it may also have a place in chronic cases when patients have sustained, and never recovered from a major shock. Essentially, I would describe it as a great acute remedy, but also as a “blocked shock” remedy.
Mechanism of Action of Aconitine
Substances that augment, stimulate, activate, potentiate, or modulate the immune response at either the cellular or humoral level. The classical agents (Freund’s adjuvant, BCG, Corynebacterium parvum, et al.) contain bacterial antigens. Some are endogenous (e.g., histamine, interferon, transfer factor, tuftsin, interleukin-1). Their mode of action is either non-specific, resulting in increased immune responsiveness to a wide variety of antigens, or antigen-specific, i.e., affecting a restricted type of immune response to a narrow group of antigens. The therapeutic efficacy of many biological response modifiers is related to their antigen-specific immunoadjuvanticity.
The cardiotoxicity and neurotoxicity of aconitine and related alkaloids are due to their actions on the voltage-sensitive sodium channels of the cell membranes of excitable tissues, including the myocardium, nerves, and muscles. Aconitine and mesaconitine bind with high affinity to the open state of the voltage-sensitive sodium channels at site 2, thereby causing a persistent activation of the sodium channels, which become refractory to excitation. The electrophysiological mechanism of arrhythmia induction is triggered activity due to delayed after-depolarization and early after-depolarization. The arrhythmogenic properties of aconitine are in part due to its cholinolytic (anticholinergic) effects mediated by the vagus nerve. Aconitine has a positive inotropic effect by prolonging sodium influx during the action potential. It has hypotensive and bradycardic actions due to activation of the ventromedial nucleus of the hypothalamus. Through its action on voltage-sensitive sodium channels in the axons, aconitine blocks neuromuscular transmission by decreasing the evoked quantal release of acetylcholine. Aconitine, mesaconitine, and hypaconitine can induce strong contractions of the ileum through acetylcholine release from the postganglionic cholinergic nerves.[#]
Indications of Aconitine of Aconite
Heart failure – Early research suggests that taking 1000 mg of aconite daily for up to 7 months might improve heart and kidney function in people with heart failure.
Feeling of coldness – Early research shows that taking aconite together with other herbs might improve feelings of coldness in the hands and feet.
Various species of Aconitum have been used for centuries both as poisons and medicines. The root is the most toxic plant part, although all parts are considered to be toxic. Extracts of Aconitum species have been given orally in traditional medicine to reduce fever associated with colds, pneumonia, laryngitis, croup, and asthma; for pain, inflammation, and high blood pressure; as a diuretic; to cause sweating; to slow heart rate, and for sedation. In traditional Asian medicine, root extracts are typically mixed with licorice or ginger. Extracts also have been used as arrow poisons. Historically, aconite was most commonly used in Western cultures as a tincture. It was applied topically as a counterirritant liniment for neuralgia, rheumatism, and sciatica. In homeopathy, aconite is used to treat fear, anxiety, and restlessness; acute sudden fever; symptoms from exposure to dry, cold weather or very hot weather; tingling, coldness, and numbness; influenza or colds with congestion; and heavy, pulsating headaches.[#]
The appropriate dose of aconite 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 aconite. 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.
Pregnancy & Lactation of Aconite
Pregnancy and breastfeeding: Do not take aconite by mouth or apply it to your skin if you are pregnant or breastfeeding. It is UNSAFE and can cause serious side effects, including death.