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Rabu, 16 Oktober 2013

Kratom extracts

There are a huge array of kratom extracts out there, but in my opinion, not many actually match up to good quality whole leaf.  There are some great extracts out there, of course, but it's not a guarantee that by attempting to concentrate kratom you will end up with something that accurately reflects the effects of the whole leaf.

So first off - how are botanical extracts made?  They are typically made with some type of solvent.  The most basic solvent is water, and indeed there are some kratom extracts that are made only with water as the solvent.  Another basic solvent is ethanol - alcohol.  By soaking kratom leaf in alcohol, you can make a basic version of what is called a tincture.  Alkaloids and other components from kratom are freed into the alcohol.  The leaf is then strained off, and the liquid contains actives from the leaf.  One of the issues that comes up is that different solvents tend to pull out different components.  For instance, the chemical makeup of a water extract is different than an ethanol extract.  With this in mind, some producers make extracts with more than one solvent in order to wring more out of the leaves.

The idea of a "Full spectrum extract" is something that has been around in the herbal and botanical world for a while.  If you use lab equipment (like an HPLC, for instance) to analyze a botanical, you will see a specific pattern that illustrates the chemical makeup of the plant.  The idea of a full spectrum extract is to make an extract that has the same pattern as the whole plant, while at the same time being more concentrated.  Usually this is done by combining different extraction techniques, although for some plants a full spectrum extract can be achieved with a single solvent (if the majority of the plants constituents are soluble in that solvent).  Unfortunately, in the kratom world, the term "Full spectrum" is often misused, and applied to products that don't actually present a balanced spectrum of the plants natural constituents.

Another thing that comes up sometimes is the idea of ratios.  10:1 and 10x are two ways of saying the same thing,  for every 10 units of a starting material, you end up with one unit of the extract.  So if it took 10 kilos of leaf to produce 1 kilo of extract, you could say it was 10x or 10:1.  Due to the lack of full spectrum extractions, the terms 5x,10x 50x etc, don't really tell you how strong an extract is going to be.  It's common to take a gram or two of a 25x product, with good effect, whereas 25 grams of plain leaf for most people would be waaay too much.  Technically, they are supposed to be the same, but it isn't quite that simple.

There are a number of different forms that kratom extracts can come in, including liquid tincture, solid extract, powders, and enhanced leaf.  I have noticed that some people respond less to tinctures than others, and my suspicion is that individual differences in metabolizing the alcohol cause differences in the absorption of the kratom alkaloids.  The short of it is that you may or not be a "tincture person".  If you try a high quality, reliable kratom liquid tincture and it doesn't do much for you, you may want to try some type of dry extract.

While there are many good quality kratom extracts out there, there are also reports of purported kratom extracts that actually contain something else, often some kind of synthetic chemical.  Several years ago, there were a number of deaths in Sweden connected to a product called "Krypton" which was kratom that had been spiked with the synthetic opioid O-Desmethyltramadol.  That is an extreme case, and a deplorable practice when there is plenty of good quality, genuine and safe kratom.  The marketing of kratom as a legal high or drug substitute is another matter, and I don't want to get too sidetracked, but let's just say it's not something I approve of at all. 

There are also some products out there that seem to be spiked with something semi-synthetic that is derived from or similar to kratom alkaloids.  There are reports that some popular "Full Spectrum" extracts out there contain synthetically derived analogs to kratom alkaloids that have a stronger effect than the naturally occurring ones.  It seems to be true, since the effects of those products are noticeably unique compared to any natural kratom.  I haven't done any lab tests on these products myself, but have heard from others who have that there are some unusual lines on the graph that don't correspond to natural leaf.  Also, there are reports of people getting out of hand with tolerance and withdrawal with these products.  While there can be some mild physical withdrawal symptoms with natural kratom, there are reports of people having more serious problems with these products, more akin to a stronger opioid. 

Many people find that the best way to use an extract is to combine a little bit with some plain leaf.   There seems to be an additive synergy with the combination.  While some people prefer the ease of use of a liquid extract and would prefer to do away with the powdered leaf,  they may find that the straight extract doesn't seem to work as well as the combination of the two.

One of the things I really appreciate about Mu Synergetics is that they only carry natural kratom extracts, never any question of synthetics or added junk.  They definitely have some great extracts,  and probably the most interesting one is the custom enhancements.  It let's me create my own perfect enhanced leaf.  BTW, they sometimes can create custom alkaloid blends for you that go beyond what is on the site.  They were able to enhance some white vein for me with a more energizing alk blend, and then a red vein with a different, more mellow extract. You might want to  Contact them if you are interested in extra custom enhancements.


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Selasa, 01 Oktober 2013

Tolerance and Potentiators

Hello friends,

Thanks for checking out the blog! I'm going a little deeper in this post, and there's a little more science than usual.  I hope you find it interesting - and please let me know if you have any comments or suggestions.

Just like so many herbs, supplements and foods, your body will develop a tolerance to kratom if you make it a daily habit.  The body is always seeking balance -- homeostasis -- and will naturally adjust your biochemistry to be less noticeably affected by things you use regularly.  This is something we encounter with so many things in our life, and it's an important capability that keeps us healthy and adaptable in a huge range of situations.

Kratom biochemistry is still relatively unstudied, and the large number of alkaloids in the plant definitely complicate any simple understandings about the way it interacts with the body.  We know that some of the compounds in kratom are µ-opiate receptor agonists (the little squiggly u is the Greek letter "mu"),  and the plant also appears to affect the serotonin and catecholamine (dopamine, epinephrine and norepinephrine) systems.

If the body is exposed things that activate these various receptors,  often it's response is to down-regulate the expression of the receptors (make less of them), which makes whatever you are ingesting less active, this is a main factor in the development of tolerance.

Many people at some point in their journey with kratom notice tolerance developing and wonder if there is anything you can do to prevent or lessen tolerance from forming.  Others may simply wish to enhance the effects of kratom.  Enter potentiators.

There are a number of things that can act as potentiators, and there are different reasons why they work.  Most of the things I am going to mention are things that are related to the µ-opioid receptor, so in theory these things could have an effect on things other than kratom.  Bear in mind, no medical claims or suggestions are being made - just passing on information.   Please use caution.

So - there are a number of different points we can approach the subject of potentiation.  One is the liver,  specifically an enzyme system called cytochrome P450.  This liver enzyme system is responsible for metabolizing a large number of substances from the body, including herbs and pharmaceutical drugs.  By inhibiting this enzyme system - basically slowing down the process of clearing the body of these compounds, the various substances last longer in the system and may have a stronger effect.  The most well known of the P450 inhibitors is probably grapefruit juice.  Bear in mind that this can be quite dangerous in the case of certain pharmaceutical drugs, and it's important to limit your consumption of grapefruit juice if you take certain pharmaceutical drugs.    Kratom appears to be metabolized by the P450 system,  and anecdotal reports do suggest that GF juice can be an effective potentiator.  However, many feel that the body quickly adjusts by raising your tolerance. 

The next group to go over is NMDA AntagonistsNMDA antagonists are known to not only act as potentiators, but also to actually reduce tolerance (to µ-OR agonists).   There are some NMDA antagonists that also happen to be powerful dissociative drugs (ketamine, MXE, PCP, DXM, and related compounds are NMDA antagonists).  Probably not most peoples idea of a helpful step to reducing tolerance (although to each their own, I suppose).   The good news is that there are a few natural, non-psychoactive substances that also act as NMDA antagonists.  An excellent option is magnesium.  Magnesium is an NMDA antagonist as well as being calcium ion channel blocker.  This makes it double duty, it acts as a natural muscle relaxant as well as a mild, non-habit forming laxative.  I should add that most forms of magnesium are not absorbed well in the body (magnesium oxide is especially poorly absorbed), so I recommend using either magnesium citrate or an amino acid chelate (pronounced key-late).  Another interesting and useful natural NMDA antagonist is found in the herb cat's claw aka uña de gato (uncaria spp).  The compound in question is called rhynchophylline, and is present in several species of cat's claw.  I've heard that the asian form of cat's claw (uncaria rhynchophylla) is higher in this compound, but my experience has been that the south American species is at least equal in subjective effect.  Interestingly, kratom contains rhynchophylline too, although it isn't clear how much.  It may actually play a role in the effects of kratom.

Nigella sativa, commonly known as blackseed or black cumin seed is a powerful medicinal herb.  Used in middle eastern cooking and medicine for millenia, it has also been found to be helpful in treating opioid withdrawal.  It is likely that multiple mechanisms are at work, but one of the things happening is that blackseed compounds act as calcium ion channel blockers (like magnesium).  µ-Opioids also have this effect - blocking calcium ions.  Calcium ions are normally used in the body to signal muscle contractions, so by blocking excess calcium ions, you can relax the muscles and prevent spasms.  As I mentioned before, magnesium is also a calcium ion channel blocker, so magnesium is double duty as a potentiator in that sense.  Anecdotally, blackseed seems to potentiate kratom as well as other µ-opiate receptor agonists - sometimes powerfully.

Agmatine is a naturally occurring derivative of the amino acid arginine.  While agmatine is sometimes used by body builders to increase muscle "pump" (due to it's activity on nitric oxide), it has also been studied for it's interesting relationship to opiate tolerance and withdrawal.  Not only does agmatine seem to somewhat prevent tolerance from forming, it also seems to mitigate withdrawal symptoms.  A list of relevant articles can be found here. 

D-Phenylalanine is a form of the amino acid phenylalanine, and some studies suggest that DPA helps to prevent the breakdown of enkephalins - which are a type of endorphin.  Endorphins are the bodies own opiate, and DPA may be able to help keep them circulating in your system a little longer.  DPA is available as a supplement, as is DLPA, which is a combination of both forms of the amino acid.

Synergy is another important factor - the artful combining of herbs or supplements.  Certain herbs might enhance the effects of kratom by virtue of their own effects, not by directly interacting with kratom metabolism.  The herb Rhodiola rosea is an excellent herb in it's own right.  It is considered an adaptogenic herb, and has been shown to be an anti-depressant as well.  I know many find that rhodiola has a synergy with kratom, and I find it to complement nicely.  Herbs and supplements like Mucuna pruriens, Valerian, Kava, and GABA also have some excellent synergy with kratom worth exploring.


One of the great things about Mu Synergetics is that they tend to stay pretty close the science and have basically come to the same conclusions I have about potentiators.  You can get pretty much everything I mention here on their site.









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