What is the pharmacology of kratom?

Kratom is a plant that originated from Southeast Asia and Thailand. It has been used to treat opioid withdrawal, cough, diarrhea, and pain in Asia. It is due to these benefits that kratom is becoming popular especially in the field of medicine. This Wiki page is replete with info on Mitragyna Speciosa.

The primary active substances in kratom are mitraphylline, mitragynine, and 7-hydroxymitragynine. Others less active chemicals include: raubasine, corynanthidine, rhynchophylline, and many others. The location of the kratom trees determines the composition of the active chemicals. For instance, the level of active compounds is very high in trees grown in Southeast Asia. The levels are low in trees grown in other areas, greenhouses included.

Pharmacology

The mode of action of kratom is similar to that of an opioid receptor agonist. When compared to the traditional opiates, its effects and pharmacological actions tend to differ significantly. On the mu receptors, mitragynine and 7-hydroxymitragynine bind as partial agonists. On the kappa and delta receptors, they act as an antagonist. Their binding affinities are high in mu and kappa receptors. Kratom also has an affinity for norepinephrine, serotonin, and kappa, unlike the other opioids. The kratom’s stimulating properties are as a result of activation of serotonin and norepinephrine.

 

• Mitragynine

It is the most abundant active alkaloid in the Mitragyna speciosa. 1.2% to 2.1% of the compound is contained in the dried kratom’s leaves.  It is involved in the improvement of mood and has analgesic effects. It also promotes relaxation and stimulation. It acts on mu-opioid receptors. When oxidized, a product called mitragynine pseudoindoxyl is formed. This product works as a selective mu-opioid agonist and has reduced affinity for both kappa and delta receptors. In chronic users, mitragynine has been put under extensive studies. Its metabolism takes place in the liver. it has linear kinetics, and its half-life is long.

Structure

Mitragynine has a molecular weight of 398.503g/mol. Its molecular formula is C₂₃H₃₀N₂0₄.

Properties

It exists as a white amorphous powder. At 235 degrees Celsius and 5 mm of mercury, the compound boils. It has a melting point of 104 degrees Celsius. The substance is soluble in organic compounds such as chloroform, alcohol, acetic acids, and many others.

Body fluids detection

The method of detection is referred to as liquid chromatography-mass spectrometry. People using kratom for recreational purposes have a mitragynine concentration of between 10 and 50 micrograms per liter in their blood.

 

Absorption, distribution, and excretion

On rats, a study was conducted. An oral dose of 20mg/kg of mitragynine was administered to each rat. At the end of the study period, it was observed that the mean plasma concentration was 424ng/ml. The time needed to reach the maximum plasma concentration was found to be 1.26 hours. The elimination half-life was 3.85 hours. 6.35l/hr./kg was the apparent total clearance. Finally, the apparent volume of distribution was 37.90l/kg.

Metabolism and its metabolites

Using Liquid Chromatography-Tandem Mass Spectrometry, mitragynine, paynantheine and speciogynine were found present in rats and human’s urine. Apart from mitragynine and speciogynine, other isomeric substances were detected. The urine of the kratom users was further screened to determine the phase I and II of the speciogynine. It was found that due to its retention times and mass spectra, the speciogynine and its metabolites were hard to identify in human urine. In phase I, seven metabolites were identified. They suggested that mitragynine underwent metabolism through hydrolysis of the methyl ester occupying position 16, O-demethylation of the 9-methoxy group and 17-methoxy group via the intermediate aldehydes by decreasing to alcohols or oxidation to carboxylic acids.

• 7-hydroxymitragynine

7-hydroxymitragynine is a terpenoid indole alkaloid extracted from Mitragyna speciosa. On the mu receptors, 7-hydroxymitragynine acts as an agonist. It has a potency that is thirty-fold high as compared to mitragynine. Morphine has a strength that is 17-fold lower than that 7-hydroxymitragynine. The compound is associated with fewer side effects as compared to morphine.

Benefits

• It is an opioid agonist. An opiate effect is felt when it reacts with the opioid receptors. The effect is essential in relieving pain.
• It possesses a relaxing effect. When in high doses, 7-hydroxymitragynine provides a sedative and relaxing effects.
• It brings about euphoria. Euphoria is felt when kratom is used in low doses. The euphoric effect makes kratom an alternative recreational drug.

Structure

Its molecular formula is C₂₃H₃₀N₂O₅. It has a molecular weight of 414.502g/mol.

Dosing

Factors such as health, age, body size and others determine the required dose. There is no specific dosage provided thus one should follow the directions on the product label. One can consult a healthcare provider. For safety purposes, it is recommended that one should avoid taking kratom regularly and in high amounts. No standardization and quality control in regulating the production and sale of kratom, therefore coming up with a standard dosage is quite challenging.

 

Kratom’s drug interaction

Combination of kratom with other drugs results in adverse drug interactions. The interaction is because some drugs share the same pharmacological properties with kratom. For instance, combining opiates and kratom is not recommended. This is to avoid synergy due to drug interaction, leading to over-sedation and respiratory depression.

https://www.webmd.com/mental-health/addiction/news/20160919/what-is-kratom-dea-ban#1

 

Conclusion

Kratom is extensively being used for both recreational and medical purposes. This due to the many benefits that it is associated with. A variety of active compounds are abundantly found in kratom as research suggest. These compounds are associated with the production of significant pharmacological effects at the opioid receptors. Kratom also has similar pharmacology as compared to other prescription opiates.

They are partial agonists and thus are associated with few side effects unlike other opiates, which are full agonists. Kratom just like other drugs is metabolized in the liver. Due to similar pharmacology, kratom tends to interact with other medications. Therefore, one should avoid combining it with other medicines. On the hand, one can seek the advice from a medical officer on the effectiveness and safety of combining kratom with other drugs. As a general rule, always avoid taking kratom in large doses. To reduce the chances of developing the side effects Kratom should not be used frequently.

 

Multiple Sclerosis sufferers have been wanting to use Kratom for a variety of benefits lately. That is why MS In Europe decided to cover this specific topic.

Metabolism is the chemical process that happens within your system that maintains the life of your cells. Metabolism largely depends on nutrition and constant supply of nutrients. The production of energy is a vital process in the way that metabolism takes the course. On the same note, energy production also depends on catalysts. Scientific research reveals that Kratom speeds up energy production by catalyzing the nutrients’ absorption. Some metabolic activities include:

• Respiration
• Energy production
• Nutrients absorption
• Cell-division
• Bodybuilding
• Elimination of nitrogenous wastes

For metabolism to happen efficiently, there needs to be enough nutrients in your system. That insinuates that a balanced diet is a key to metabolism.  The good news about Kratom is that apart from adding fiber to your diet, it also plays a big role in making other nutrients work efficiently in the body. Two decades ago, a group of specialists found out that Kratom can turn out to add nutritional value to the usual diet. That led to the current observations of the chemical compounds of the herb.

Today, viable evidence on the alkaloids of this unique plant explain that the leaves have a chemical structure that benefits humanity in numerous ways. The different parts of the tree provide more than 40 components that contribute to the well being of humanity across the globe.

The use of Kratom in the right proportions brings noticeable improvement in the process of digestion to those who experience constipation. With that in mind, if you take Kratom with food, digestion runs smoothly, and the body absorbs the nutrients faster. Consequently, energy production flows more instantly compared to when the food gets into the digestive system without the components of the herb.

The efficient production of energy that results from smooth absorption of nutrients enables some of the body processes that require energy like cell division to go on much easier. So, in the case of body repairing process like the healing of wounds, Kratom contributes significantly.

Another remarkable method of taking this herb is through tea. It is simple to prepare Kratom tea, and it takes relatively little time. Out of all the methods devised to take the herb, this particular one seems to be the most efficient one. That is because you take it with water and additionally, it dissolves perfectly in relatively high temperatures.

It’s true that taking Kratom with other beverages like juice is also a good option but the tea made from the herb surpasses this because you enjoy it naturally. Since the herb reaches the digestive system in liquid form, it is absorbed conveniently. That makes it reach the bloodstream faster and combine with other nutrients to bring a stable supply of nutrients to the system.

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Traditionally, many people used the herb to cure diarrhea. Mostly, the cause of this condition is food poisoning or taking dirty foods. For years Kratom has hugely helped to curb this condition by strengthening the immune system by boosting the white blood cells production.

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That way, the antibodies produced by the system to fight diarrhea syndrome multiply fast. The result is that the condition gets a defeat from the immune system.

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Due to the medicinal capability of the herb, the ancient Thai’s as well as those who lived along the swampy jungles of Southeast Asia where kratom grew naturally, used it to fight several health conditions such as diabetes and post-traumatic disoders. Currently, the herb helps to fight diarrhea and enable the body to restore the water that it loses due to the dehydration caused by diarrhea.

A scenario that further explains the importance of Kratom in the body system is whereby some medication related to opiates comes in. Opiates bring numerous side effects to the body. That is to say, that is to say, that they tamper with the body functionality which involves metabolism. On the other hand, Kratom medication when taken in accordance to the right doses enables the body system to run in a balanced way without adding side effects.

For nutrients to get into the body system, they must go through digestion. Breaking down of the nutrients does not end there; they are further broken down into much simpler compounds for the body to absorb them with ease. Lactose intolerance is a condition whereby a natural sugar called lactose fails to break down. The properties of Kratom facilitate the breakdown of food nutrients, and with the herb in your diet, lactose intolerance becomes a story to tell.

Kratom in normal cases, when taken in the right doses, helps in the digestion of food by slowing the movement of food through the gut. The gut comprises of the whole digestive channel. That is from the mouth to the rectum. Food passing through the digestive channel at a low speed gets enough time to mix with the digestive juices efficiently and consequently, the nutrients get into the body in large portions. As a result;

• Energy is produced instantly
• The body remains in a healthy condition
• The body excretes waste perfectly
• The immunity system strengthens

A condition known as Irritable bowel syndrome afflicts numerous people in America and the world at large. It results from imbalanced serotonin in your entrails. This condition is commonly a mental complication. Psychologists reason that the condition occurs due to mental instability which mostly results from stress. Since Kratom proves viability in reducing stress, such a condition is easily curable through the administration of Kratom.

A good mental state hugely contributes to how our body functions. In turn, if our body functions well, the metabolism also runs in the right way. Taking kratom also improves the stimulation of the serotonin receptors found on the walls of the gut. That leads to the production of balanced serotonin hence the condition gets under control.

When acid occurs in the stomach in excess, a lot of pain follows, and it also becomes uncomfortable to eat. That hugely affects your health since you lack enough nutrients to run your system. However, the good news is that Kratom can reduce excess acid in your body to a usable amount. That way, you can stomach food comfortably.