Temgicoluril (),
also known as tetramethylglycoluril and sold under the brand names Adaptol and Mebicar, is an
anxiolytic
An anxiolytic (; also antipanic or anti-anxiety 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 anxie ...
medication produced by Latvian pharmaceutical company
Olainfarm and sold in
Latvia
Latvia, officially the Republic of Latvia, is a country in the Baltic region of Northern Europe. It is one of the three Baltic states, along with Estonia to the north and Lithuania to the south. It borders Russia to the east and Belarus to t ...
and
Russia
Russia, or the Russian Federation, is a country spanning Eastern Europe and North Asia. It is the list of countries and dependencies by area, largest country in the world, and extends across Time in Russia, eleven time zones, sharing Borders ...
.
The
chemical structure
A chemical structure of a molecule is a spatial arrangement of its atoms and their chemical bonds. Its determination includes a chemist's specifying the molecular geometry and, when feasible and necessary, the electronic structure of the target m ...
of temgicoluril is somewhat similar to
uric acid
Uric acid is a heterocyclic compound of carbon, nitrogen, oxygen, and hydrogen with the Chemical formula, formula C5H4N4O3. It forms ions and salts known as urates and acid urates, such as ammonium acid urate. Uric acid is a product of the meta ...
and it doesn't interact with acids, alkali, oxidants and reducing agents. It seems to affect all major
neurotransmitter
A neurotransmitter is a signaling molecule secreted by a neuron to affect another cell across a Chemical synapse, synapse. The cell receiving the signal, or target cell, may be another neuron, but could also be a gland or muscle cell.
Neurotra ...
systems.
Temgicoluril has an effect on the structure of
limbic
The limbic system, also known as the paleomammalian cortex, is a set of brain structures located on both sides of the thalamus, immediately beneath the medial temporal lobe of the cerebrum primarily in the forebrain.Schacter, Daniel L. 2012. ''P ...
–
reticular activity, particularly on
hypothalamus
The hypothalamus (: hypothalami; ) is a small part of the vertebrate brain that contains a number of nucleus (neuroanatomy), nuclei with a variety of functions. One of the most important functions is to link the nervous system to the endocrin ...
emotional zone, as well as on all several basic neuromediator systems – γ
aminobutyric acid (GABA),
choline
Choline is a cation with the chemical formula . Choline forms various Salt (chemistry), salts, such as choline chloride and choline bitartrate. An essential nutrient for animals, it is a structural component of phospholipids and cell membrane ...
,
serotonin
Serotonin (), also known as 5-hydroxytryptamine (5-HT), is a monoamine neurotransmitter with a wide range of functions in both the central nervous system (CNS) and also peripheral tissues. It is involved in mood, cognition, reward, learning, ...
, and adrenergic activity. It decreases brain
norepinephrine
Norepinephrine (NE), also called noradrenaline (NA) or noradrenalin, is an organic compound, organic chemical in the catecholamine family that functions in the brain and human body, body as a hormone, neurotransmitter and neuromodulator. The ...
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 ...
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 symptoms of inattention, hyperactivity, impulsivity, and emotional dysregulation that are excessive and pervasive, impairing in multiple ...
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 described such a procedure. They combined N,N-dimethylurea and glyoxal with a catalytic amount of phosphoric acid 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 is needed) and obtaining respectable yields, although this requires a longer reaction time.
As of 2021, temgicoluril has not been evaluated outside of Latvia and Russia.
Medical uses
Temgicoluril is used in Latvia and Russia, as a
pharmaceutical drug
Medication (also called medicament, medicine, pharmaceutical drug, medicinal product, 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 ...
to treat
anxiety
Anxiety is an emotion characterised by an unpleasant state of inner wikt:turmoil, turmoil and includes feelings of dread over Anticipation, anticipated events. Anxiety is different from fear in that fear is defined as the emotional response ...
and to prevent or reduce anxiety, unrest, fear,
internal emotional tension and
irritability
Irritability 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 excessive sensitivity to stimul ...
, reduce
neuroses and
neurotic disorders, heartburns of non-coronary heart disease origin. These effects are not accompanied with relaxation of
muscle tone
In physiology, medicine, and anatomy, muscle tone (residual muscle tension or tonus) is the continuous and passive partial contraction of the muscles, or the muscle's resistance to passive stretch during resting state.O’Sullivan, S. B. (2007) ...
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 substance dependence on nicotine. It is a Chronic condition, chronic, relapsing disease characterized by a Compulsive behavior, compulsive craving to use the drug despite social consequences, loss of control over ...
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 Addiction, addictive and can cause Substance dependence, dependence. As a resu ...
. Although temgicoluril does not cause
mood swing
A mood swing is an extreme or sudden change of mood. Such changes can play a positive or a disruptive part in promoting problem solving and in producing flexible forward planning. When mood swings are severe, they may be categorized as part ...
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 ...
, habituation, nor addiction, withdrawal syndrome has been observed.
Side effects
Possible and rare
side effect
In medicine, a side effect is an effect of the use of a medicinal drug or other treatment, usually adverse but sometimes beneficial, that is unintended. Herbal and traditional medicines also have side effects.
A drug or procedure usually use ...
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 Balance disorder, disequilibrium or a non-specific feeling, such as giddiness or foolishness.
Dizziness is a ...
,
hypotension
Hypotension, also known as low blood pressure, is a cardiovascular condition characterized by abnormally reduced blood pressure. Blood pressure is the force of blood pushing against the walls of the arteries as the heart pumps out blood and is ...
,
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 ...
,
allergic reactions
Allergies, also known as allergic diseases, are various conditions caused by hypersensitivity of the immune system to typically harmless substances in the environment. These diseases include hay fever, food allergies, atopic dermatitis, alle ...
(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 ...
, fatigue. And lowered
blood pressure
Blood pressure (BP) is the pressure of Circulatory system, 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 ...
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
Phenibut, sold under the brand name Anvifen among others, is a central nervous system (CNS) depressant with anxiolytic effects, and is used to treat anxiety, insomnia, and for a variety of other indications. It is usually taken oral administrat ...
*
Selank
*
Validol
*
Bemethyl
*
List of Russian drugs
This page is a list of Russian drugs, or drugs that were developed in Russia, the former Soviet Union, and/or post-Soviet countries.
Many Russian drugs are indicated for enhancing physical, mental, and/or cognitive performance, including drugs ...
References
{{Anxiolytics
Anxiolytics
Drugs with unknown mechanisms of action
Russian drugs