The Origins of Ketamine

If you’ve ever endured a debilitating or chronic condition before, you know there are many different medications you can take. Some companies even make claims that their medication can cure you completely, while others just suppress your symptoms. Ketamine, a drug used primarily for anesthesia, is very effective in treating a variety of chronic diseases and conditions. Ketamine has also recently shown promise as an alternative therapy for mood disorders such as PTSD, depression, and anxiety.

What is Ketamine?

Ketamine, with chemical formula being C13H16ClNO, belongs to a class of drugs known as dissociative anesthetics. Other drugs in this category include PCP, Dextromethorphan (DXM) and nitrous oxide. Ketamine also goes by brand names Ketalar, Ketanest and Ketaset. The substance is primarily used by doctors and veterinarians when starting and maintaining anesthesia.

Domino noted in the journal article, “The Domino Effect: Ed Domino early studies of Psychoactive Drugs,” that ketamine came about through the search for making better Phencyclidine (PCP) derivatives. The goal of the replacement drug, according to Domino, was for the new drug to be “short acting, less convulsant and less delirium inducing [than PCP].”

Domino and fellow researcher Guenter Corssen proceeded to discover ketamine, and they published the first clinical study of it as an anesthetic in 1956. The drug really took off in the 1960s during the Vietnam War, where it was used as an anesthetic during surgery. The drug was later approved by the FDA in 1970 as an intravenous anesthetic.

Distinguishing Features

The distinguishing features of ketamine anesthesia are breathing maintenance and airway reflexes, moderate bronchodilation and stimulated heart function with elevated blood pressure rate. When given intravenously, the onset of its action occurs in seconds. Also, ketamine is considered safe to use as an anesthetic, since it doesn’t lower blood pressure or suppress breathing. It is a preferred substance of choice for short-term medical procedures when muscle relaxation is not required.

Bioavailability

The bioavailability of a drug, if you are unfamiliar, refers to the extent and rate at which the drug or metabolite enters and circulates throughout your system, thereby accessing the action site. Metabolites of ketamine are norketamine, dehydronorketamine and hydroxynorketamine.
Bioavailability of a drug is largely determined by the properties of the dosage’s form, which, in turn, depends partly on the drug’s design and manufacture. Below are some of the bioavailability rates of ketamine:

Intravenous: 100%
Intramuscular: 93%
Epidural: 77%
Intranasal: 45–50%
Sublingual: 24–30%
Rectal: 25–30%
By mouth: 16–20%

How Ketamine Works

Understanding how this beneficial drug works can help you understand how and why it’s so beneficial for so many clinical purposes other than anesthesia.

Ketamine works on a specific group of cells in your brain that are known as NMDA receptors. NDMA receptors interact with neurotransmitters such as glutamate to deliver cortico-cortical communication dynamics that rev up your neurons. The glutamate triggered by ketamine mediates responses to trauma and stress. In a nutshell, it works to block sensory perceptions such as pain and different levels of discomfort.

Recreational Use

If you’ve heard of ketamine before, it’s probably because of its checkered past as a recreational substance. It is considered a ‘club drug’, like ecstasy, and street names it goes by include Special K, Kit Kat, Cat Valium, Purple, Jet and Vitamin K.

Special K is highly sought after because its effects, which induces anything from feelings of calmness and relaxation to making you feel as if you are detached from sensations and surroundings, to experiencing distorted sights and sounds. However, abuse of large doses can lead to symptoms such as difficulty breathing, muscle spasms or weakness, dizziness, nausea, vomiting, and severe confusion.

Ketamine Side Effects

No drug is without side effects or risks, and not everyone experiences them. The most common side effects associated with ketamine when used medically include dizziness, nausea, double vision, unease, restlessness and confusion.

Medical Uses

Treating cancer pain: Ketamine can help ease pain at lower doses and is used clinically to treat chronic cancer pain.
Limiting addictive painkillers: Ketamine helps sedatives work, and it may also help people need fewer addictive narcotic painkillers like morphine. This is a great advantage, due to the increased likelihood of tolerance and complications arising from long-term narcotic use.
Pediatric Anesthesia: Ketamine, often administered concurrently with midazolam, is one of the most commonly used substaces for sedation procedures in children. In particular, children with cyanotic heart disease, neuromuscular condition and allergies to other anesthetics respond well to ketamine anesthesia.
Treatment-resistant Depression: In 2019, The FDA approved Spravato, a nasal spray that uses ketamine in conjunction with an oral antidepressant to treat depression in adult patients who have tried other antidepressants but did not benefit from them.

Ketamine Therapy

Ketamine has many benefits, and one of the major advantages it has is that it works very quickly and continues to keep working even after it’s been metabolized. This is particularly true when it’s used for treating depression symptoms.

Conventional antidepressant medications need about 6-12 weeks to build up in your system before they start working. Comparatively, ketamine starts working in as littles as 24 hours. Here are a few of the ways it is being researched as alternative therapy:

Migraines: Researchers at Thomas Jefferson Hospital in Philadelphia say this hallucinogenic club drug can reduce painful migraine headaches, which can be notoriously difficult to treat.
PTSD: Post Traumatic Stress Disorder (PTSD) can often be treatment-resistant, and studies are making a compelling argument that ketamine is a very effective therapy for chronic stress disorders, with one small study showing it had clear superiority over the traditionally used midazolam for treating PTSD. With some more investigation, ketamine may prove to be an effective tool for treating PTSD and anxiety in those who don’t respond to more conventional treatments.
Acute suicidal ideation: Along with controlling symptoms of depression, several studies have also found it to be effective for controlling symptoms of seriously thinking of taking your own life.
Seizures: Seizures are often treated with potent intravenous medications that can have serious adverse effects. Ketamine is used in their place sometimes for patients that have failed to adequately respond to these standard treatments. No randomized controlled trials exist in the therapy’s favor, and only limited numbers of case studies support the treatment.
Heroin and Alcohol Addiction: Researchers in Russia claim to have obtained encouraging results by using ketamine as part of a treatment for alcoholism and heroin addiction.

What are Arylcyclohexylamines?

Arylcyclohexylamines are NMDA receptor antagonistics and a synthesized analog of ketamine. The chemical class contains around 90 compounds based on variation of its structure and functional group.

Arylcyclohexylamines as a Research Chemical (RC)

Readily available forms of Arylcyclohexylamines used extensively in pharmacological research include Deschloroketamine (DCK) and 2-Fluorodeschloroketamine (2-FDCK). These compounds are favored for research as pharmacological agents for neurological, psychological and epidemiological applications.

These compounds can be easily obtained online through the RealChems online store in the form of amorphous powders and/or crystals that can be used for research purposes. Domains in which the compounds can be investigated for beneficial effects include treatments for neuro-dissociative disorders such as schizophrenia and other such conditions where the concepts of reality, time, and space are affected in the brain.

What is Ketamine?