Nature: acrid, bitter, warm
Enters: Spleen, Liver, Kidney
Actions: Dispels wind, eliminates dampness; relaxes the sinews, invigorates the channels, promotes blood circulation.
• Wind damp painful obstruction (Bi) especially when there are problems flexing and extending the joints.
• Swelling and pain due to trauma (internal or external) with blood stasis.
• Difficulty bending and stretching the body with hemiplegia.
• Contains Huperzine-A and B
ITM on Huperzine in Alzheimer’s:
Huperzine, an anticholinesterase alkaloid, is divided into two chemical species, huperzine A and huperzine B, which have similar effects but differing activity levels (huperzine A being about 10 times as strong as huperzine B). Huperzine A was first isolated from the Chinese herb Lycopodium serratum in 1980 at the Zhejiang Academy of Medical Sciences and the Shanghai Institute of Materia Medica of the Chinese Academy of Sciences. Huperzine B was isolated five years later. The plant source, originally called Qian Ceng Ta, meaning thousand-layers pagoda (referring to the tall multi-leafed appearance of the plant), is also known in China as Jin Bu Huan, a term meaning “more valuable than gold,” usually applied to plants that have potent analgesic actions. This herb should not be confused with the patent remedy called Jin Bu Huan made from tetrahydropalmatine. The plant has been reclassified botanically as Huperzia serrata from the new family Huperziaceae, rather than from the closely related family Lycopodiaceae. It is reported that the Lycopodiaceae have two medicinal genera: Lycopodium (now Huperzia) and Phlegmariurus. A common constituent is the alkaloid fordine, which is found in 14 species of Huperzia and has similar action to the huperzines.
Huperzia, as it is now called, contains a wide variety of alkaloids, including lycodoline, lycoclavine, and serratinine, as well as the huperzines. The alkaloids are of a unique structure and have been called Lycopodium alkaloids. In general, they are comprised of four rings, though one of the rings may be opened. The huperzines, like many of the other lycopodium alkaloids, contain a nitrogen within one of the rings and an NH2 group attached to the ring structure (some of the Lycopodium alkaloids contain only a nitrogen within the ring structure).
Huperzia is not much used as a crude herb in Chinese medicine: the dominant application is for blood disorders caused by trauma or acute ailment, such as hematamesis caused by overstrain, bruises, hemorrhoids, and lung abscess. In addition to alkaloids, it contains triterpenoids. Huperzines and other isolated alkaloids are increasingly used in Chinese medicine as an alternative to crude herb preparations.
PHARMACOLOGY AND CLINICAL APPLICATIONS OF HUPERZINE
Huperzines A and B reversibly inhibit cholinesterase; huperzine A has a stronger action than huperzine B, which in turn has a stronger action than galanthamine (an alkaloid from Lycorus radiata that has been used for its anticholinesterase activity). Huperzine A has substantially stronger anticholinesterase activity than physostigmine or neostigmine (chinchona alkaloids obtained from Physostigma venenosum; neostigmine is a common drug for treatment of myasthenia at a dose of 1-2 mg by IM or 0.5 mg IV; physostigmine is also an approved anticholinesterase drug), but huperzine B is three to five times weaker than physostigmine. Huperzines A and B have greater effect on acetylcholinesterase (AChE) than on butyrocholinesterase (BuChE). Huperzine A, because of its cholinesterase inhibiting activity, has been used in myasthenia gravis patients in China, with apparent success.
Both huperzine A and B have been shown to have memory-enhancing activities in animals. At 0.075 mg/kg for huperzine A or 0.5 mg/kg for huperzine B, IP administration to mice significantly facilitated spatial discrimination learning in a Y-maze study. At slightly higher doses (0.075-0.125 mg/kg for A and 0.6-0.8 mg/kg for B) the huperzines given prior to exposure of mice to carbon dioxide prevented hypercapnia-induced impairment of learning. Memory retention and retrieval could be enhanced in animals when the alkaloids were given immediately or 6-12 hours after training. Substantially lower or higher doses of huperzines are not effective. Huperzine has been used for Alzheimer’s and senile dementia with positive results. In a double-blind trial with a group of 56 patients suffering from multi-infarct dementia or senile dementia and a group of 104 patients with senile and presenile memory loss, huperzine A was demonstrated to be effective for improving memory. It was given by intramuscular injection, 0.05 mg twice daily for four weeks to the first group and 0.03 mg twice daily for two weeks to the second group. The only side effect was slight dizziness experienced by a few patients. In rats, fordine, at 0.01-0.04 mg/kg IP, speeds up conditioned avoidance responses, reverses impairment of conditioned avoidance response, and antagonizes hippocampal and cortical EEG changes induced by quinuclidinyl benilate.
Huperzine A has been evaluated at the Mayo Clinic in Jacksonville, Florida. According to Alan Kozikowski, a chemist who is heading the research there, Huperzine A is more effective and more specific than tacrine, another anticholinesterase drug. Interneuron Pharmaceuticals in Lexington, Mass. is testing Huperzine A in human clinical trials.
Huperzine-A is a compound extracted from the herbs of the Huperziceae family. It is known as an acetylcholinesterase inhibitor, which means that it stops an enzyme from breaking down acetylcholine which results in increases in acetylcholine.
Acetylcholine is known as the learning neurotransmitter, and is involved in muscle contraction as well. Increasing levels of acetylcholine is routinely used as a technique amongst weight-lifters and scholars.
Huperzine-A appears to be a relatively safe compound from animal studies of toxicity and studies in humans showing no side-effects at dosages routinely supplemented with. Huperzine-A is in preliminary trials for usage in fighting Alzheimer’s Disease as well.
- Huperzine-A appears to be water-soluble, and taking with food is not needed
- Although its initial spike is quick, it appears to have a long half-life; the pharmacokinetic profile might change when changing dosages though.
Supplementation of huperzine-A tends to be in the range of 50-200mcg daily, and while this can be divided into multiple dosages throughout the day it tends to be taken at a single dose. Supplementation of huperzine-A does not require food to be coingested with it and can be taken in a fasted state.
Cycling of huperzine-A tends to be used since the half-life exceeds 24 hours, and although a ‘cycle’ of huperzine-A tends to last 2-4 weeks followed by a break the optimal cycle length is not yet known.