Temgicoluril (),
[https://cdn.who.int/media/docs/default-source/international-nonproprietary-names-(inn)/pl124.pdf?sfvrsn=6437f035_10&download=true ] also known as tetramethylglycoluril and sold under the brand names Adaptol and Mebicar, is an
anxiolytic
An anxiolytic (; also antipanic or antianxiety agent) is a medication or other intervention that reduces anxiety. This effect is in contrast to anxiogenic agents which increase anxiety. Anxiolytic medications are used for the treatment of anxi ...
medication produced by Latvian pharmaceutical company
Olainfarm
Olainfarm AS is a Latvian leading manufacturer in the chemical and pharmaceutical sector of the Baltic States.
The company was founded in 1972 as state enterprise "Olaines ķīmiski – farmaceitiskā rūpnīca" (Olaine Chemical-Pharmaceutical ...
and sold in
Latvia
Latvia ( or ; lv, Latvija ; ltg, Latveja; liv, Leţmō), officially the Republic of Latvia ( lv, Latvijas Republika, links=no, ltg, Latvejas Republika, links=no, liv, Leţmō Vabāmō, links=no), is a country in the Baltic region of ...
and
Russia
Russia (, , ), or the Russian Federation, is a List of transcontinental countries, transcontinental country spanning Eastern Europe and North Asia, Northern Asia. It is the List of countries and dependencies by area, largest country in the ...
.
The
chemical structure
A chemical structure determination includes a chemist's specifying the molecular geometry and, when feasible and necessary, the electronic structure of the target molecule or other solid. Molecular geometry refers to the spatial arrangement of at ...
of temgicoluril is similar to
metabolite
In biochemistry, a metabolite is an intermediate or end product of metabolism.
The term is usually used for small molecules. Metabolites have various functions, including fuel, structure, signaling, stimulatory and inhibitory effects on enzymes, c ...
s in human body and it doesn't interact with acids, alkali, oxidants and reducing agents. It affects all major
neurotransmitter
A neurotransmitter is a signaling molecule secreted by a neuron to affect another cell across a synapse. The cell receiving the signal, any main body part or target cell, may be another neuron, but could also be a gland or muscle cell.
Neuro ...
systems.
Temgicoluril has an effect on the structure of limbic–reticular activity, particularly on
hypothalamus
The hypothalamus () is a part of the brain that contains a number of small nuclei with a variety of functions. One of the most important functions is to link the nervous system to the endocrine system via the pituitary gland. The hypothalamu ...
emotional zone, as well as on all several basic neuromediator systems – γ
aminobutyric acid (GABA),
choline Choline is an essential nutrient for humans and many other animals. Choline occurs as a cation that forms various salts (X− in the depicted formula is an undefined counteranion). Humans are capable of some ''de novo synthesis'' of choline but re ...
,
serotonin
Serotonin () or 5-hydroxytryptamine (5-HT) is a monoamine neurotransmitter. Its biological function is complex and multifaceted, modulating mood, cognition, reward, learning, memory, and numerous physiological processes such as vomiting and vas ...
, and adrenergic activity. It decreases brain
norepinephrine
Norepinephrine (NE), also called noradrenaline (NA) or noradrenalin, is an organic chemical in the catecholamine family that functions in the brain and body as both a hormone and neurotransmitter. The name "noradrenaline" (from Latin '' ad'', ...
levels and increases brain serotonin levels without modulating
dopaminergic systems or
cholinergic
Cholinergic agents are compounds which mimic the action of acetylcholine and/or butyrylcholine. In general, the word "choline" describes the various quaternary ammonium salts containing the ''N'',''N'',''N''-trimethylethanolammonium cation. F ...
systems.
Temgicoluril purportedly has anti-anxiety (anxiolytic) properties.
It is also used to aid smoking cessation.
In addition, temgicoluril may be useful in the treatment of
ADHD
Attention deficit hyperactivity disorder (ADHD) is a neurodevelopmental disorder characterised by excessive amounts of inattention, hyperactivity, and impulsivity that are pervasive, impairing in multiple contexts, and otherwise age-inapp ...
symptoms. In contrast with typical anxiolytic medications such as benzodiazepines, temgicoluril is non-habit forming, non-sedating, and does not impair motor function.
It can be prepared by condensation of N,N-dimethylurea with glyoxal. One publication reported an elegant procedure for doing this. They combined N,N-dimethylurea, glyoxal, and a catalytic amount of phosphoric anhydride in an aqueous solution at room temperature and after sufficient time temgicoluril was conveniently isolated by filtration. The filtrate can be re-used by adding more dimethylurea and glyoxal (no additional catalyst) and obtaining respectable yields, although this requires a longer reaction time.
As of 2021, temgicoluril has not been evaluated by the
United States
The United States of America (U.S.A. or USA), commonly known as the United States (U.S. or US) or America, is a country primarily located in North America. It consists of 50 states, a federal district, five major unincorporated territorie ...
medical system.
Medical uses
Temgicoluril is used in Latvia and Russia, as a
pharmaceutical drug
A medication (also called medicament, medicine, pharmaceutical drug, medicinal drug or simply drug) is a drug used to diagnose, cure, treat, or prevent disease. Drug therapy (pharmacotherapy) is an important part of the medical field and re ...
to treat
anxiety
Anxiety is an emotion which is characterized by an unpleasant state of inner turmoil and includes feelings of dread over anticipated events. Anxiety is different than fear in that the former is defined as the anticipation of a future threat wh ...
and to prevent or reduce anxiety, unrest, fear,
internal emotional tension and
irritability
Irritability (also called as crankiness) is the excitatory ability that living organisms have to respond to changes in their environment. The term is used for both the physiological reaction to stimuli and for the pathological, abnormal or excessi ...
, reduce neuroses and neurotic disorders, heartburns of non-coronary heart disease origin. These effects are not accompanied with relaxation of muscle tone and impaired coordination of movement, suppression of mental and physical activity, so the drug can be used without interruption of work or school.
Temgicoluril does not have a direct effect on sleep, however, it enhances the effectiveness of sleep medicines and normalizes the course of disturbed sleep. Temgicoluril alleviates or eliminates the manifestations of
nicotine dependence
Nicotine dependence is a state of dependence upon nicotine. Nicotine dependence is a chronic, relapsing disease defined as a compulsive craving to use the drug, despite social consequences, loss of control over drug intake, and emergence of with ...
that occur after
smoking cessation
Smoking cessation, usually called quitting smoking or stopping smoking, is the process of discontinuing tobacco smoking. Tobacco smoke contains nicotine, which is addictive and can cause dependence. As a result, nicotine withdrawal often make ...
. Temgicoluril does not cause
mood swing
A mood swing is an extreme or sudden change of mood. Such changes can play a positive part in promoting problem solving and in producing flexible forward planning, or be disruptive. When mood swings are severe, they may be categorized as par ...
s or
euphoria
Euphoria ( ) is the experience (or affect) of pleasure or excitement and intense feelings of well-being and happiness. Certain natural rewards and social activities, such as aerobic exercise, laughter, listening to or making music and da ...
, no habituation and addiction, withdrawal syndrome has been observed.
Side effects
Possible and rare
side effect
In medicine, a side effect is an effect, whether therapeutic or adverse, that is secondary to the one intended; although the term is predominantly employed to describe adverse effects, it can also apply to beneficial, but unintended, consequence ...
s may include
dizziness
Dizziness is an imprecise term that can refer to a sense of disorientation in space, vertigo, or lightheadedness. It can also refer to disequilibrium or a non-specific feeling, such as giddiness or foolishness.
Dizziness is a common medical c ...
,
hypotension
Hypotension is low blood pressure. Blood pressure is the force of blood pushing against the walls of the arteries as the heart pumps out blood. Blood pressure is indicated by two numbers, the systolic blood pressure (the top number) and the dias ...
,
indigestion
Indigestion, also known as dyspepsia or upset stomach, is a condition of impaired digestion. Symptoms may include upper abdominal fullness, heartburn, nausea, belching, or upper abdominal pain. People may also experience feeling full earlier t ...
,
allergic reactions
Allergies, also known as allergic diseases, refer a number of conditions caused by the hypersensitivity of the immune system to typically harmless substances in the environment. These diseases include hay fever, food allergies, atopic derma ...
(itchy skin) after high doses,
hypothermia
Hypothermia is defined as a body core temperature below in humans. Symptoms depend on the temperature. In mild hypothermia, there is shivering and mental confusion. In moderate hypothermia, shivering stops and confusion increases. In severe h ...
, fatigue. And lowered
blood pressure
Blood pressure (BP) is the pressure of circulating blood against the walls of blood vessels. Most of this pressure results from the heart pumping blood through the circulatory system. When used without qualification, the term "blood pressure" r ...
and/or
body temperature
Thermoregulation is the ability of an organism to keep its body temperature within certain boundaries, even when the surrounding temperature is very different. A thermoconforming organism, by contrast, simply adopts the surrounding temperature ...
decreased by 1 to 1.5 °C. Blood pressure and body temperature return to normal after completion of treatment.
See also
*
Fabomotizole
*
Phenibut
*
Selank
Selank ( Russian: Cеланк) is a nootropic, anxiolytic peptide based drug developed by the Institute of Molecular Genetics of the Russian Academy of Sciences. Selank is a heptapeptide with the sequence Thr-Lys-Pro-Arg-Pro-Gly-Pro (TKPRPGP). ...
*
Validol
*
Bemethyl
References
{{Anxiolytics
Anxiolytics
Drugs with unknown mechanisms of action
Russian drugs