by Thomas Incledon, PhD(c), RD, LD/LN, RPT, NSCA-CPT, CSCS
The local gym musclehead throws a bottle of Nivalin at you and starts running his mouth off like Shawn Ray describing his pre-Olympia routine. Skeptical and somewhat reluctant, you try it anyway. Now here you are squeezing out curl after curl and your biceps are about to explode, yet you think can still do another rep. Nine, ten, eleven, twelve. The reps were hard, but you still made them. You marvel at how during your the last biceps workout you could only do eight reps with the same weight. Is Nivalin a real ergogenic aid or is this just some placebo effect?
The Source
The Nivalin supplements sold over the counter usually contain extracts of Leucoium aestivum. While Nivalin is the commonly used trade name, the chemical name is galanthamine. Galanthamine is classified as an alkaloid, the same family of compounds that includes more well known supplements such as ephedrine and yohimbine. It occurs naturally in a variety of plants, including bulbs of the Caucasian snowdrop and the common snowdrop. The amount of galanthamine per dry weight of extract can vary from 0.1% to 2% [1]. With such a wide variance in the amount of galanthamine, determining appropriate dosages can be difficult. For this reason, make sure that the supplement you consider taking is standardized for galanthamine, so you can accurately calculate how much to take.
Blocking an enzyme
Blow the dust off your old physiology textbook and turn to the chapter on skeletal muscle. Messages from the brain eventually make their way down to neurons (nerve cells) that activate muscles cells. The region where the neuron interacts with muscle is called the neuromuscular junction. Here a stimulated neuron releases a neurotransmitter called acetylcholine (ACh). ACh travels through the space between the neuron and muscle cell and stimulates the muscle cell. When enough ACh bombards the muscle cell, it starts the process that eventually leads to muscle contraction. Any ACH that is left over can be degraded by acetylcholinesterase (ACHase). Now here is where Nivalin comes into the picture. By inhibiting the actions of AChase, galanthamine increases the amount and duration of ACh.
Where’s the evidence?
The inhibition of AChase is a unique approach to increasing exercise performance. In general, ACh is not considered the limiting factor when a muscle fatigues. Other factors such as increased lactate and hydrogen ion concentrations are considered to be more important than decreased ACh concentrations inside the fatiguing muscle. Anecdotally, reports from a variety of athletes swear Nivalin has helped them run faster, lift more, and jump higher. Unfortunately, database searches turn up nothing about Nivalin or galanthamine use by athletes or healthy people exercising. There is evidence indicating that galanthamine could increase the effects of ACh, though [2]. While this is an intriguing find, the problem is that the research was done using isolated frog rectus abdominis muscle, or in bodybuilder terms, frog abs! Applying the results of amphibian-related research to humans is really stretching scientific interpretation, so the search continues. Studies using rats, cats, dogs, and rabbits have also showed that galanthamine increases contractile responses to stimulation [3, 4]. Rat studies done recently indicate that galanthamine can prolong the action of ACh at the neuromuscular junction [5-7]. To further potentiate the effects of galanthamine on contractility, it was combined with Pymadin (4-aminopyridine hydrochloride) and resulted in a product called Nivalin-P [8]. So while direct evidence on human performance is not available, there does appear to be some weak evidence to support claims by athletes using Nivalin.
Bodybuilding Applications
Delaying muscular fatigue translates to more reps with a given weight. Increasing contractile forces translates to more weight lifted. Based on anecdotal evidence, Nivalin has been touted to increase strength, speed, and endurance. However, there aren’t any scientific studies on humans to support these claims. It is obvious from animal studies though, that galanthamine can increase the sensitivity of muscle fibers to ACh. One could only speculate at this point that by increasing ACh sensitivity, athletes would experience improvements in performance. For the bodybuilder this would translate to more weight lifted, a stronger training effect, and more muscle growth.
Side Effects
If you’re familiar with acetylcholine, then you realize that it is involved in other functions besides innervating muscle fibers. It serves as a neurotransmitter in the brain, slows down heart rate, and can cause vasodilation of blood vessels. Following this line of thinking, it would make sense that Nivalin may have some side effects. Studies on humans have indicated galanthamine to be safer then other AChase inhibitors [9] and without adverse effects after taking 30-50 mg daily for 16 months [10]. Minor side effects like nausea, sweating, restlessness, and slight bradycardia (slowing of the heart rate) have been reported. In normal dosages, its use is considered safe and FDA approval for the use of galanthamine in the treatment of Alzheimer’s disease is expected [11].
Your choice
If you have used a galanthamine product or you are considering using one, read the label and make sure it indicates the amount of active ingredient in each capsule or tablet. So far only smaller, lesser-known companies have been selling Nivalin, sometimes as Nivalis. Don’t expect huge gains. Since it is common for many athletes to double or triple the suggested label amounts, keep in mind that chronic inhibition of AChase may decrease the number of ACh receptors which means that you’ll lose the effects of galanthamine over time. For this reason you should cycle its use. Suggested cycles have been either 30-60 days, but that may be more due to the number of capsules in a bottle than any scientific reasoning. Also be careful of what you stack with Nivalin as one recent study indicates that while the Nivalin/Pymadin combo may increase contractile forces, it also increases the rate of fatigue. [12]. Maybe just another reason to wait until some more research comes out before using this stuff.
References
1. Harvey, A.L., The pharmacology of galanthamine and its analogues. Pharmacol Ther, 1995. 68(1): p. 113-128.
2. Prozorovskii, V.B., [Sensitization of the cholinoreceptors of striated muscle to acetylcholine]. Biull Eksp Biol Med, 1969. 67(4): p. 56-59.
3. Cheymol, J., et al., [Neuromuscular Action of Galanthamine, Natural Anticholinesterase Agent]. Ann Pharm Fr, 1964. 22: p. 41-48.
4. Irwin, R.L. and S.H. d, The activity of galanthamine and related compounds on muscle. Arch Int Pharmacodyn, 1960. 127: p. 314-330.
5. Krivoi, II, [Quantitative estimation of synaptic acetylcholinesterase inhibition with galanthamine using parameters of miniature endplate currents]. Biull Eksp Biol Med, 1988. 105(6): p. 665-667.
6. Krivoi, II, [An attempt to estimate various characteristics of neuro-muscular transmission from the rising phase of miniature end-plate currents]. Neirofiziologiia, 1989. 21(2): p. 272-275.
7. Krivoi, II and T.P. Sei, [Postsynaptic potentiation of end plate currents in the rat diaphragm at different levels of synaptic acetylcholinesterase activity]. Biull Eksp Biol Med, 1991. 111(5): p. 458-460.
8. Radicheva, N., M. Vydevska, and K. Mileva, Nivalin P-induced changes in muscle fiber membrane processes. Methods Find Exp Clin Pharmacol, 1996. 18(5): p. 301-308.
9. Khmelevskii Ia, M. and V.P. Gadalov, [Effect of myorelaxant antagonists on cardiac activity]. Anesteziol Reanimatol, 1980(1): p. 14-17.
10. Dal-Bianco, P., et al., Galanthamine treatment in Alzheimer’s disease. J Neural Transm Suppl, 1991. 33: p. 59-63.
11. Davis, K.L., Alzheimer’s disease: seeking new ways to preserve brain function [interview by Alice V. Luddington]. Geriatrics, 1999. 54(2): p. 42-7; quiz 48.
12. Radicheva, N., et al., Further studies on Nivalin P-induced changes in muscle fiber membrane processes. Methods Find Exp Clin Pharmacol, 1999. 21(1): p. 5-10.
|
