Medical Uses to Psychedelics
The use of psychedelics was commonly used in the periods preceding the 1950s but was followed by declined use due to potential abuse. There was then a ban imposed on the use of the same substances in the period. Slowly, it is becoming evident that the substances are being introduced into clinical practice. Research is gradually establishing that they can be used in the management of several psychiatric conditions, including post-traumatic stress disorder (PTSD), addiction, depression, and anxiety (Johnson, 2018). Different classes of psychedelic drugs have been shown to be in everyday use, and they include Lysergic acid diethylamide (LSD), MDMA, and psilocybin (Tupper, Wood, Yensen, & Johnson, 2015). This piece brings out the medical use of psychedelic substances. It critically brings out an elaborate review of how these substances can be used as legitimate medications, especially to those who are skeptical.
Lysergic acid diethylamide
This is a semi-synthetic hallucinogen and deemed as one of the most potent drugs that are known on earth. It came to be known as a recreational drug in the 1960s and 1980s, although the use later declined. It was synthesized accidentally by Albert Hoffman, who was making substances from ergots to be used as circulatory and respiratory stimulants. There are more than 80 street names that are associated with LSD in different parts of the world. Some of the names include blotter, dots, mellow yellow, and blotter paper and windowpane (Hwang & Saadabadi, 2020). When the drug is taken in small doses, it can create changes in perception, thought, and mood. When one takes higher doses, there is evident hallucination and disorientation of a person’s space and time.
Based on the physical appearance, the drug is odorless and a crystalline substance. Since minimal amounts of the drug are known to cause effects, the drug is usually dried into sheets of gelatin, sugar cubes, and pieces of a blotting paper, which then release the doses when the drug is swallowed. In other cases, LSD is taken as liquids and capsules or tablets and mixed with other substances to be sold to different users. The drug has also been shown to be very unstable when exposed to light.
Alongside hallucinogenic effects, the drug has been shown to cause other symptoms like nausea, weakness, dizziness, and other complex psychic encounters. There are other physical manifestations of LSD, and they include mild hypertension, occasional rise in body temperature, and dilated pupils. There are times when the drug also leads to cross-sensory perceptions, known as synesthesia (Fuentes, Fonseca, Elices, Farré, & Torrens, 2020). The name LSD was derived from the German word LysergSäureDiethylamid, where Lysergide comes from the family of the indole alkylamine substances, including the psilocin and DMT. The R stereoisomer is more potent when compared to the S form.
In the 1960s and 1970s, LSD was associated with several issues, and abuse was among the most significant concerns, especially evident in the rave parties in the US. The mechanism of action of LSD has not been fully elucidated, but there are suggestions that it binds to serotonin and activating the subtype 2 receptor. As a result, the interference leads to the breakdown of the inhibitory process in the hippocampus and the prefrontal cortex. Specifically, the drug leads to reduce the activity of the brain along the temporal gyrus as well as the cerebellum (Fuentes et al., 2020). In other studies, it has been linked to activation of the right hemisphere, and this alters the functioning of the thalamus. In the end, there is an increase in the activity of the para-limbic structures and hence the resultant visual imageries that are very common.
Typical doses to bring about mental effects are thought to be 20 to 80 mcg, although doses as much as 300mcg were used. When taken orally, the drug is shown to bring about effects within a short period of 30 minutes, and it can last for as long as 8 to 12 hours and even more. In most cases, the duration of the effects is dependent on the dose that is taken. The plasma half-life of the drug has been determined to be about two and a half hours. In humans, LSD is transformed by the liver through the process of hydroxylation as well as glucuronide conjugation, thus forming inactive metabolites. It is estimated that only about 1% of the drug is eliminated in the urine unchanged within 24 hours. The major metabolite of LSD is 2-oxylysergide, which is found in urine.
Therapeutic uses of LSD: How it can be shown to be useful to skeptics
Even though LSD is associated with high addictive effects, which led to a moral panic in the 1960s, studies are currently underway to unravel some of the therapeutic effects of LSD. Evidence has been able to demonstrate that psychedelic drugs and specifically LSD are capable of affecting the structure and function of the brain while promoting neuron growth at the same time (“LSD as a treatment – Alcohol and Drug Foundation,” n.d.). Specifically, promising evidence shows that LSD can encourage transformed ways of thinking, helping one to unlearn old habits that are potentially dangerous. As a result of this, the drug is being explored in the management of, among other conditions, PTSD, anxiety among patients with chronic conditions, and drug dependency.
A study done in London, in 2016 showed that LSD has the potential to transform the entrenched thoughts, flagging off the potential use in managing anxiety and depression. Other trials have also demonstrated positivity in the management of alcohol dependence and the increased ability of people to face their conditions, especially in PTSD. LSD lacks approval in many countries across the world, but there is an excellent promise in the management of the psychiatric conditions that have posed a challenge for a long time. Despite so, when the drugs are administered for therapeutic use, there is a need for the doses to be given under the supervision of a healthcare professional to avoid potential abuse.
Psilocybin
Psilocybin is a component that is contained in about 180 different types of mushrooms. The component is the one responsible for the psychoactive effects of the mushrooms that occur when one ingests them. The mushroom is commonly found in South America, Mexico, and other parts of Southern or Northern of the United States. This compound is frequently classified as an indole-alkylamine and has a similar structure as LSD (“Psilocybin – Alcohol and Drug Foundation,” n.d.). Some of the common names with which this compound is referred to in the streets include mushroom, magic mushroom, purple passion, shrooms, and little smokie.
The use of the magic mushroom can be traced back as far as 2,000 years ago, especially in Central America. There are some traces of the mushrooms that have also been found in Guatemala at around 100 BC when it is said the mushroom was used during some ceremonies. When the mushroom found itself in Mexico around the 1500s, it was termed as God’s flesh. The prevailing culture of the mushroom intensified around 1957, when R. Gordon Wasson discovered a tribe of Mexicans using the mushroom during his vacation (Griffiths et al., 2016). In two decades that followed, Wasson had isolated psilocybin, and this attracted attention over the potential use of the drug in different psychiatric conditions.
There were some studies conducted at Harvard to determine the potential use of psilocybin in disorders like obsessive-compulsive disorder, autism, alcoholism, depression, and schizophrenia. Later on, there was a massive abuse of the drug in the USA, and this led to the ban on the use of psilocybin (“Psilocybin Mushrooms: Basic Info | Psycheplants | ICEERS,” n.d.). Some of the signs and symptoms that were evident when one took mushrooms include changes in mood, nausea, and vomiting, dizziness, abdominal cramps, poor coordination, and sweating. Other symptoms include chills, dry mouth, and dilation of the pupils.
The chemical structure of the drug has been determined to be 4-phosphoryloxy-N, N-dimethyltryptamine. The components, despite being of natural origin, can also be obtained from the lab through the semi-synthetic means. On physical appearance, the mushroom has very slender stems and caps that look grey, with gills that are dark on the lower side. When dried, the mushrooms turn reddish-brown, and when isolated, the colors look off-white. To produce effects, the mushrooms are ingested orally, although they are often mixed with other substances (“Psilocin – an overview | ScienceDirect Topics,” n.d.). Whether dried or fresh, the mushrooms have an exceedingly unpalatable
and very bitter taste.
To produce effects, any dose of the mushrooms contains adequate amounts of psilocybin to produce psychoactive effects. It is estimated that when a person ingests the dried or fresh mushrooms, they will ingest about 0.2 to 0.4% of psilocybin and trace amounts of other components like psilocin (Johnson & Griffiths, 2017). The psychological effects of the drug include distortion of space and time, relaxation, enhancement of sensory abilities, feelings of detachment from one’s body and environment. There is also massive, restlessness, and challenges distinguishing between fantasy and reality.
Mechanism of action of psilocybin
Just like LSD, psilocybin has a complex mechanism of action because of its relatively high affinity for the different neurotransmitters. It has been thought to diminish the activity of the brain and does this through the activation of the various neurotransmitter receptors. Through the process, it modulates the excitatory activity on GABA-ergic and pyramidal neurons (Johnson & Griffiths, 2017). It has also been shown to activate the serotonin receptor, 5HT2A, and this leads to an increase in the activity of the glutamate activity leading to excitation at the postsynaptic areas.
In another mechanism, it is known to activate the 5-HT1A, and this is the mechanism responsible for the inhibition of the pyramidal cells and their activities. The psychoactive activities are also similar to LSD and occur within a period of 20 to 30 minutes after ingestion. The effects are likely to last as long as 8 hours, although it is unlikely that the hallucinogenic effects would last for more than an hour. The peak effects of the component are within 2 hours. The dose for the isolated and purified form of the drug that produces a result is 12 to 30mg. The treatment has been determined to alter consciousness, creating illusions, de-realization, and driving one into dream-like states. Other receptors are affected, and they include 5-HT1D and 5-HT2C.
Psychotherapeutic effects of psilocybin
Before the induction of therapy with psilocybin, there is often a need to screen and exclude other psychiatric conditions. About 0.2mg/kg of the psilocybin is useful in the management of cancer-associated mental distress. It also recently been determined that it can also be used in patients with cancer who encounter depression. It has, therefore, been shown to cause about 60% of remission of the anxiety and depressive symptoms, based on the findings from the Johns Hopkins study (Johnson & Griffiths, 2017). Besides cancer, the drug is being considered for the management of the treatment of resistant depression. Other studies are considering the use of the drug in the management of other conditions like an addiction.
MDMA
This is a synthetic drug which has been shown to alter one’s mood and awareness of their surrounding and time. The history of the use of the drug is linked to the German Pharmaceutical company around 1912. In the early days, it was intended to be used for the synthesis of medications to control bleeding. Over time, the toxicity studies on the drug were done in animal studies in the 1950s at the University of Michigan, US (“Dosing for pleasure and why less is often more | Global Drug Survey,” n.d.). In the 1970s, the dug came to be very common among the psychiatrists in as much as it had not gone through the required clinical trials.
Around 1985, there was an emergency ban on the use of MDMA, and this made the drug to be considered as schedule I. This drug has been shown to have similar effects as other hallucinogens and stimulant drugs. The drug is a derivative of amphetamine and has been known as ecstasy in the streets. In effect, it has been shown to produce effects that combine those of mescaline and amphetamine (“DrugFacts: MDMA (Ecstasy/Molly) | National Institute on Drug Abuse (NIDA),” n.d.). In other cases, these drugs are therefore known as designer drugs since the illegal labs designed them.
Similarly, the drug resembles the neurotransmitters epinephrine and norepinephrine, and therefore, most of the biological effects are related to the neurotransmitters. Some of the street names with which it is referred to include eggs, wee fellas, yolks, pingers, and pills. To be used, the drug is compressed into a pill and turned into appropriate shapes and, at times, stamped on both sides. The drug appears as a crystalline powder, which may be white, grey, light brown, or purple.
Mechanism of action of MDMA
Primarily, the drug acts by indirect agonistic effects on the serotonergic receptors. The drug leads to an increase in the concentration of serotonin in the synapse. Essentially. MDMA acts through the serotonin transporter and thus moved into the nerve terminal. The process, therefore, ensures there is the release of the serotonin through a process termed as the transporter-mediated exchange. Despite the ability of the drug to interfere with the storage of serotonin in the vesicles, it increases the amount of available serotonin (“Department of Health | Pharmacology of MDMA (ecstasy),” n.d.). MDMA has also been shown to lead to an increase in the amount of dopamine and norepinephrine that are released. The release of the norepinephrine and dopamine is shown to occur similarly as serotonin release.
Further, the drug has also been thought to inhibit the reuptake of the monoamines and delay the metabolism through the inhibition of the monoamine oxidase. Particular effects of the medications through dopamine lead to increased energy and reward system reinforcement; norepinephrine leads to an increase in the heart rate and blood pressure. Serotonin potentiates effects on mood, leads to an increase in appetite and sleep states.
Some of the resultant effects of the drug include nausea, blurred vision, involuntary clenching of teeth, and frequent chills. The results of the drugs, when taken, can last for up to 3 to 6 hours. However, it has been shown that abusers often take the second dose even before the initial treatment elapses (“Department of Health | Pharmacology of MDMA (ecstasy),” n.d.). In different cases, the dose of MDMA has been put at 100 to 150mg for every pill with the highest dose being 300mg. The use of this drug has, however, been placed under strict regulation, and laws have been put in place to govern the use of the drug. There are also stringent controls to ensure the regulated availability of the drug to the general public.
Therapeutic uses of MDMA
Ecstasy, dubbed the party drug seems to be the next breakthrough in the management of post-traumatic stress disorder, according to some studies. The drug remains to be grouped under the schedule I drugs, and therefore when used, a lot of caution is practiced. Despite lacking the approval by the FDA, the current progress in the pre-clinical studies has demonstrated a promise of hope. According to the findings by the Multidisciplinary Association for Psychedelic Studies (MAPS) shown that the drug is effective in PTSD (“Exploring Therapeutic Effects of MDMA on Post-Traumatic Stress – MAPS,” n.d.). There are instances where the drug is used as an off-label medication in the management of PTSD.
MAPS has also established that MDMA can be used in the management of social anxiety in adults who have other conditions like autism. The drug, through the study, has been elucidated to suppress the amygdala, an area responsible for fear and anxiety. When used, the drug is shown to produce prosocial and empathetic feelings, all who help in the proper management of anxiety. In other studies, the drug is useful in the management of depression that occurs as a result of life-threatening conditions. Primarily, it manages the depression that occurs as a comorbidity of PTSD. The use of the drug in the management of alcohol addiction has been linked to its ability to control the manifestations of PTSD.
Conclusion
Psychedelic is a term used to denote the agents that, when used, distort one’s perception of reality and their environment. Some of the drugs that have been commonly implicated include psilocybin, LSD, and MDMA. All these drugs have a very high potential for abuse, and this has led to caution in their use in many countries. More, they have abused in the past and therefore been banned or highly regulated by different authorities. Despite the skepticism in the use of the agents by different people, the drugs remain active in clinical studies for their potential in the management of psychiatric conditions. Some of the diseases whose promise is high include PTSD, depression, and anxiety. These drugs are under clinical studies, and there is positivity in the possibility of having them in everyday use.
References
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