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Agmatine is a well known neurotransmitter. It also works as a neuromodulator in certain processes in the body. Current research shows that agmatine has the potential to be used to treat drug addiction and reduce neuropathic pain. It can also protect the brain from the effect of toxins (1).
Agmatine was discovered over 100 years ago in 1910 by Kossel. Its mechanisms of action on different body functions though, have just been discovered. It is prepared through the removal of a carboxylic group from L-Arginine. It is naturally stored in the neurons and is therefore used in the nervous system whenever required (2).
The direct use of agmatine is not suitable for pain relief as it can elevate pain symptoms in people. The drug has an excellent synergy with most opioids and therefore, works best when combined with a painkiller like morphine (3).
Agmatine affects various processes in animal neurology. It is found to inhibit the enzyme that produces nitric oxide, therefore decreasing its levels. It can also stop receptors such as N-Methyl-D-Aspartate (NMDA) and others (4).
Agmatine also has the ability to inhibit calcium channels in neurons and stop the production of specific serotonin receptors. Currently, more research is required in order to find further information on how agmatine acts within the body (5).
Agmatine’s metabolism is still not understood clearly with multiple pathways discussed to provide an explanation.
Agmatine may be handled by the Diamine Oxidase (DAO) enzyme, which is responsible for metabolizing histamine. DAO converts agmatine into 4-guanidinobutyrate (6).
This mechanism is suggested to dissolve around half of the plasma agmatine, because the inhibition of the DAO enzyme doubles the plasma concentration of the chemical.
This means that agmatine removes quickly from tissues that have high DAO levels, such as in the kidney, epithelial tissues and smooth muscle cells. They remain for a long period in the brain, liver and skeletal tissues due to the naturally lower levels of DAO (7).
10% of the agmatine can also convert into polyamines such as putrescine through different mechanisms. One mechanism produces urea as a byproduct while the other produces ammonia during the indirect conversion (8).
The current research on animals suggests that agmatine has a wide potential for use as a supplement. Some studies on humans have now appeared on the topic, but all of these employ the use of agmatine injections. It needs to be thoroughly tested for ingestion first before being termed suitable for supplement use.
Due to lack of human testing, it is not possible to discuss the toxic nature of agmatine in finer detail. It is therefore best to remain with the current dose of 2670 mg which was used in human experiments (9).
Some studies show that agmatine does not have a significant impact in providing long term pain relief. This can be a result of the short half life of agmatine in some parts of the body.
Agmatine is not effective against heat pain, and has a weak activity against visceral pain. Agmatine however, can provide pain relief in the case of neuropathic and inflammatory pain (10).
Agmatine also showed signification pain relief in a double blind study using patients that have lumbosacral spine degenerative pathologies. More research is needed in this case, because the relief continued even after discontinuing agmatine sulfate (11).
Agmatine is also known to be useful when withdrawing from alcohol. It is suggested that it helps alcohol withdrawal through a mechanism of NMDA antagonism (12).
Research shows that agmatine is very effective in protecting the body against strokes as the inhibition of the nitric oxide synthase (NOS) in the body reduces the amount of toxic nitric oxide levels (13).
Agmatine can also reduce edema which is often associated with the occurrence of a stroke. Edema refers to the condition in which fluid is lost from the arteries into the capillaries and surrounding tissues (14).
Agmatine can increase the activity of NF-kB which in turn increases the concentration of survivin inhibitor. This can save cells from hypoxia and works in contrast to apoptosis or programmed death of the cells (15).
The enzyme that produces agmatine in the body increases during stressful times. This means that it is the natural response of the body to protect it from anxiety. Agmatine increases the activity of neurons in the areas of the brain associated with the handling of stress, anxiety and depression.
Agmatine side effects
There are no general studies on the use of agmatine in humans that can be used to warrant its side effects.
Although research shows that agmatine can protect cells from acidity in the stomach, it is known to increase the chances of developing an ulcer in patients suffering from alcohol withdrawal symptoms (16).
Agmatine can increase the appetite of the person using the drug. This can be helpful for people looking to gain weight but not beneficial for obese people.
The main problem with agmatine is that sufficient research has not been carried out yet, which decreases the potential for widespread use as a health supplement.
Agmatine causes vasodilatation, therefore reducing blood pressure. It should not be used by people who are being treated for hypotension or low blood pressure (17).
There is only a single study that describes the human dosage of agmatine for the treatment of neuropathic pain as employed for daily doses of the people taking part in the experiment. The study used around 1300 to 2670 mgs of agmatine during the research phase.
The current oral dosage value is based on an experiment on rats, which gives an approximation of using 2-6.4 mg/Kg of body weight for humans (18).
One thing to remember though is that agmatine does not absorb well when taken with proteins. This leaves room for research to decide if the oral supplementation of agmatine is possible and carries the same benefits as its delivery through injection.
Summary: Agmatine has great potential for use in the treatment of several adverse health conditions, such as hypertension, anxiety, stress, and alcohol withdrawal symptoms. It can also be a great pain reliever, especially when used with opioids. You should always take care when taking agmatine supplements as its effects are yet to be clearly understood by research.