Caffeine belongs to the group. What is Caffeine Sodium Benzoate
"Caffeine-sodium benzoate" - medical drug, which has a stimulating effect on the human nervous system. This tool is prescribed to treat migraines, eliminate drowsiness, increase blood pressure and mental capacity. Tablets improve motor activity, eliminate drowsiness, normalize activity respiratory center.
Release form of the medicinal product
The product is available in tablet form. Information about possible side effects, pharmacological action and dosages contains instructions. "Caffeine sodium benzoate" can often be found on sale in the form of a solution.
The effect of the drug on the human body
The pharmacological effect of "Caffeine-sodium benzoate" is to excite the receptors of the cerebral cortex, strengthen reflexes, stimulate the respiratory center medulla oblongata, increasing general motor activity and neuronal conductivity spinal cord, eliminating drowsiness and fatigue, enhancing mental activity.
In the small concentrations mentioned in the instructions, “Caffeine-sodium benzoate” has a stimulating effect on the human nervous system, but its intake in large quantities is fraught with pathological consequences for the body, as it begins to depress the nervous system.
"Caffeine sodium benzoate" is used to increase blood pressure; it affects cardiac and vascular mechanisms. Moreover, the drug acts selectively, that is, at low pressure it increases it, but at normal pressure it has practically no effect.
In addition, "Caffeine-sodium benzoate" has a diuretic effect, stimulates the production gastric juice and reduces platelet aggregation.
"Caffeine-sodium benzoate": application
According to the instructions for the drug, it is prescribed for certain pathological health conditions, which include:
- Increased sleepiness.
- Headaches, including migraines.
- Decreased physical and mental performance.
- Vascular diseases, including hypotension.
Contraindications
Use of this medicine It is not recommended for certain pathologies, which are described in the instructions attached to it. "Caffeine-sodium benzoate" is not recommended for use in such pathological conditions as: cardiovascular diseases organic type, anxiety disorders, ventricular extrasystole, sleep disorders, tachycardia, hypersensitivity to the components of the drug. In addition, tablets are prescribed with extreme caution to elderly people and children under 12 years of age, if there is a risk of seizures and epilepsy. For pregnant and lactating women, "Caffeine-sodium benzoate" is prescribed only when special indications and in extremely small doses.
The use of this drug simultaneously with other drugs - contraceptives, cimetidine and some others - causes a slowdown in the process of removing components from the liver and their accumulation in the blood. When combined with various drinks and foods that contain caffeine, benzoate can cause excessive stimulation. nervous system.
Mexiletine, found in various foods and medications, can significantly slow down the caffeine withdrawal process, while nicotine, on the contrary, speeds it up. The main active substance of the drug slows down the absorption of calcium in the gastrointestinal tract, reduces the effectiveness of narcotic and sleeping pills, increases the amount of lithium excreted from the body.
Side effects
Information about harm medicinal product contains instructions. "Caffeine-sodium benzoate" in the presence of intolerance to its individual components or ignoring medical recommendations can cause restlessness, anxiety, headaches and migraines, epileptic seizures, insomnia, vomiting, nausea, exacerbation of stomach ulcers, and high blood pressure. At misuse An overdose may occur, which is accompanied by increased blood pressure, dehydration, vomiting blood, agitation, increased heart rate and urination, convulsions and ringing in the ears.
When a dose exceeding 300 mg is consumed per day, the first signs of poisoning appear: confusion, headaches, excessive anxiety and extrasystole. The consequences are eliminated by washing the digestive tract, taking activated carbon and laxatives.
"Caffeine-sodium benzoate" - a means for weight loss
Despite the fact that the drug register positions the drug in question as medical, many people, especially athletes, use it to lose a couple of extra pounds. According to numerous reviews, it is an effective fat burner and allows you to achieve excellent weight loss results.
“Caffeine-sodium benzoate,” the recipe for the use of which is often recommended by nutritionists for these purposes, is very effective, especially if it is combined with other drugs.
What is the purpose of caffeine?
The solution of "Caffeine (sodium) benzoate", like its tablets, is used and prescribed as a psychostimulant. It has the following effects on the body:
- Increases performance.
- Deepens and speeds up breathing.
- Increases the overall performance of the body.
- Has a stimulating effect on skeletal muscles.
- Increases heart rate.
- Stimulates the production of gastric juice.
- Increases the rate of fat breakdown.
According to the last point, the drug can indeed be used for fat burning, although the drug register does not position it in this way.
The use of "Caffeine-sodium benzoate" for weight loss
The stimulating effect of the drug is noticeable even when using a minimal dose. Despite this, burning fat in the body requires a dosage significantly higher than the therapeutic one. Before starting training, it is advisable to use about 9-20 mg of caffeine per kilogram of body weight. Reducing the dosage may cause a loss of stimulating effect. The tablets are taken thirty minutes before the start of classes, often together with aspirin to improve vascular patency.
Despite the fact that "Caffeine-sodium benzoate", the price of which does not exceed 10 rubles, is a good means for losing weight, even athletes who use it are advised to start with minimum doses at a rate of 2 mg per kilogram of weight. Gradually, the dosage should be increased to the maximum possible, after which side effects begin. Correct technique The drug allows you to increase metabolism by a third, which increases the rate of breakdown of fats in the body by a similar amount.
Harm of "Caffeine-sodium benzoate"
Numerous doctors and scientists different countries They repeat the same thing over and over again: with regular use of the drug over a long period of time, there is a negative effect on the human body. It has been scientifically proven that caffeine significantly increases blood pressure, can cause the development of myocardial infarction and atherosclerosis.
Of course, some studies refute the claim that caffeine benzoate leads to an increased risk of cardiovascular diseases, but it is in such pathologies that its use is strictly limited or prohibited. The drug is sold without a prescription, therefore, its use is completely uncontrolled, especially coupled with the fact that the price for “Caffeine-Sodium Benzoate” is minimal. Regular use of the drug causes addiction, much like a drug addiction. In fact, the principle of action here is similar to regular coffee: if a coffee lover is denied a drink, he will turn into a lethargic and sleepy creature, since his brain simply will not work without the dose it needs.
Another disadvantage of using "Caffeine-sodium benzoate" is the lack of appetite. At the same time, the drug stimulates the production of gastric juice, which can cause heartburn, gastritis, and ulcers. Actually, in this way, losing extra pounds is achieved - people with similar pathologies gastrointestinal tract They just can't eat normally.
The last pitfall is drug overdose. Symptoms of poisoning include weakness, heartburn, increased blood pressure, nausea, and headaches. For athletes, this becomes a signal to reduce the dose, for ordinary people- to completely stop taking "Caffeine-sodium benzoate". And most importantly: you can lose weight with this medicine only if you exercise.
Gross formula
C8H10N4O2Pharmacological group of the substance Caffeine
Nosological classification (ICD-10)
CAS Code
58-08-2Characteristics of the substance Caffeine
Pharmacology
Pharmacological action- analeptic, cardiotonic, psychostimulant.Has a direct stimulating effect on the central nervous system: regulates and enhances excitation processes in the cerebral cortex, respiratory and vasomotor centers, activates positive conditioned reflexes and motor activity. Stimulates mental activity, increases mental and physical performance, shortens reaction time. After administration, vigor appears, fatigue and drowsiness are temporarily eliminated or reduced. Causes increased and deepening of breathing, especially against the background of depression of the respiratory center. Affects the cardiovascular system: increases strength and heart rate (especially in large doses), increases blood pressure during hypotension (does not change normal). Dilates the bronchi, biliary tract, blood vessels skeletal muscles, heart, kidneys, constricts - organs abdominal cavity(especially when they are dilated). Reduces platelet aggregation. It has a moderate diuretic effect, mainly due to a decrease in the reabsorption of electrolytes in the renal tubules. Stimulates the secretion of gastric glands. Increases basal metabolism, enhances glycogenolysis, causing hyperglycemia.
Blocks central and peripheral adenosine receptors. Promotes the accumulation of cAMP and cGMP by inhibiting the activity of phosphodiesterases involved in their inactivation. To a greater extent inhibits cAMP phosphodiesterase (not only in the central nervous system, but also in the heart, smooth muscle organs, adipose tissue, skeletal muscles). Stabilizes transmission in dopaminergic synapses (psychostimulating properties), beta-adrenergic synapses of the hypothalamus and medulla oblongata (increased tone of the vasomotor center), cholinergic synapses of the cortex (activation of cortical functions) and medulla oblongata (excitation of the respiratory center), noradrenergic synapses (increased physical activity, anorexia).
Caffeine and its water-soluble salts are well absorbed in the intestine (including the colon). T1/2 is about 5 hours, in some people - up to 10 hours. The main part is demethylated and oxidized. About 10% is excreted unchanged by the kidneys. In the body of full-term newborns and infants(1.5-2 months) is eliminated more slowly (T 1/2 - from 80 to 26.3 hours, respectively).
Impact on higher education nervous activity depends largely on the dose and type of nervous system of the patient. In small doses the stimulating effect predominates, in large doses the depressant effect predominates. In older people, the effect on sleep is more pronounced: its onset slows down and decreases. total time sleep, the frequency of awakenings increases (possibly due to faster metabolism of catecholamines in the central nervous system). In premature infants, when eliminating periodic breathing, caffeine reduces the partial pressure of carbon dioxide, the concentration of H + in the blood and at the same time increases the volume of ventilation without changing heart rate.
Use of the substance Caffeine
Diseases accompanied by depression of the central nervous system, cardiovascular and respiratory systems(including drug poisoning, infectious diseases), cerebral vascular spasms (including migraine), decreased mental and physical performance, drowsiness, enuresis in children, breathing disorders (periodic breathing, idiopathic apnea) in newborns (including premature infants).
Contraindications
Expressed arterial hypertension, organic diseases cardiovascular system (including atherosclerosis), increased excitability, glaucoma, sleep disorders, old age.
Side effects of the substance Caffeine
Anxiety, agitation, insomnia, tachycardia, arrhythmias, increased blood pressure, nausea, vomiting. With long-term use, slight addiction is possible (a decrease in the effect of caffeine is associated with the formation of new adenosine receptors in brain cells). Sudden cessation of caffeine administration may lead to increased central nervous system inhibition with symptoms of fatigue, drowsiness and depression.
Interaction
Reduces the effect of sleeping pills and narcotic drugs, increases (improving bioavailability) - acetylsalicylic acid, paracetamol and other non-narcotic analgesics. Improves the absorption of ergotamine in the gastrointestinal tract.
Overdose
When abused, caffeine (more than 300 mg per day, i.e. four 150 ml cups of natural coffee) can cause anxiety, restlessness, tremors, headache, confusion, and cardiac extrasystoles. In newborns (including premature infants), at a blood plasma concentration of 50 mg/ml, toxic effects are possible: anxiety, tachypnea, tachycardia, tremor, increased Moro reflex, and at higher concentrations - convulsions.
In this article you can read the instructions for use of the drug Caffeine. Feedback from site visitors - consumers - is presented of this medicine, as well as the opinions of specialist doctors on the use of Caffeine in their practice. We kindly ask you to actively add your reviews about the drug: whether the medicine helped or did not help get rid of the disease, what complications and side effects were observed, perhaps not stated by the manufacturer in the annotation. Caffeine analogues in the presence of existing structural analogues. Use for treatment low blood pressure(hypotension), spasms and drowsiness in adults, children, as well as during pregnancy and breastfeeding.
Caffeine- psychostimulant and analeptic. It has a stimulating effect on the central nervous system, mainly on the cerebral cortex, respiratory and vasomotor centers. Increases mental and physical performance, reduces drowsiness and fatigue. Weakens the effect of CNS depressants. It has a pronounced effect on the cardiovascular system: it increases the strength and frequency of heart contractions, increases blood pressure during hypotension. Has a moderate diuretic effect. Increases the secretion of gastric glands.
Indications
- diseases accompanied by depression of the central nervous system, functions of the cardiovascular and respiratory systems (including poisoning with opioid analgesics, infectious diseases);
- spasms of cerebral vessels;
- decreased mental and physical performance;
- drowsiness.
Release forms
Solution for subcutaneous administration.
Tablets 100 mg Caffeine sodium benzoate.
Instructions for use and dosage
Injected subcutaneously or taken orally. Adults - 100-200 mg 2-3 times a day; children - 25-100 mg 2-3 times a day.
Side effectsvie
- sleep disturbance;
- excitation;
- anxiety;
- with prolonged use, addiction is possible;
- tachycardia;
- increased blood pressure;
- arrhythmias;
- nausea, vomiting.
Contraindications
- arterial hypertension;
- organic diseases of the cardiovascular system (including severe atherosclerosis);
- glaucoma;
- increased excitability;
- sleep disorders;
- old age.
It can be used as mono- or as part of combination therapy.
Drug interactions
With simultaneous use, the effect of sleeping pills and anesthetics is reduced.
With simultaneous use, it is possible to enhance the effect of analgesics-antipyretics, salicylamide, naproxen.
With the simultaneous use of estrogens (hormonal contraceptives, drugs for HRT), it is possible to increase the intensity and duration of action of caffeine due to inhibition of the CYP1A2 isoenzyme by estrogens.
When administered concomitantly with adenosine, caffeine reduces the increased heart rate and blood pressure changes caused by adenosine infusion; reduces vasodilation caused by the action of adenosine.
With simultaneous use, it is possible to increase the bioavailability, absorption rate and plasma concentration of acetylsalicylic acid.
With simultaneous use, mexiletine reduces the clearance of caffeine and increases its plasma concentrations, apparently due to mexiletine inhibition of caffeine metabolism in the liver.
Methoxsalen reduces the excretion of caffeine from the body with a possible increase in its effect and the development of toxic effects.
Due to the induction of microsomal liver enzymes under the influence of phenytoin, its simultaneous use accelerates the metabolism and excretion of caffeine.
Fluconazole and terbinafine cause a moderate increase in the concentration of caffeine in the blood plasma, ketoconazole - less pronounced.
The most pronounced increase in AUC and decrease in clearance are observed with simultaneous use of caffeine with enoxacin, ciprofloxacin, pipemidic acid; less pronounced changes - with pefloxacin, norfloxacin, fleroxacin.
When used simultaneously, caffeine accelerates the absorption of ergotamine.
Analogues of the drug Caffeine
Structural analogues of the active substance:
- Dia-Activanad-N;
- Caffeine anhydrous;
- Caffeine sodium benzoate.
If there are no analogues of the drug for the active substance, you can follow the links below to the diseases for which the corresponding drug helps, and look at the available analogues for the therapeutic effect.
Caffeine guide: action, effects, correct and lethal doses.
caffeine in lately sing praises and not in vain - on a solid basis scientific research. We have collected the facts about caffeine and will tell you why it is good for your health and under what conditions it is harmful.
Caffeine is used quite widely in the world, but at the same time its image has a certain negative connotation and causes concern among many. For example, since childhood, we have been warned more than once that we should not drink too much coffee. With this text, Zozhnik sheds white light on the substance that gave its name to the world’s most popular dark drink.
Proven effects of caffeine
Caffeine is a central nervous system stimulant, with effects similar to amphetamines, only much weaker. The first study to prove positive influence caffeine on performance during aerobic exercise carried out only in 1978.
Here are more recent facts from one of the extensive studies on the properties of caffeine. Scientists Wilmore and Costeel proved in 2001 the following effects of caffeine:
- increased mental excitability,
- improved concentration,
- improved mood,
- reducing fatigue and delaying its onset,
- stimulation of catecholamine release ( active substances acting as chemical intermediaries and “controlling” molecules in intercellular interactions, including in their brain. Examples of catecholamines: adrenaline, dopamine),
- strengthening the mobilization of free fatty acids(that is, it promotes fat burning processes),
- increasing the use of muscle triglycerides (fuel sources for muscle function, which, for example, helps during intense training),
- the ability to increase muscle activity in sprinters, as well as athletes involved in strength sports: it can promote calcium metabolism in the sarcoplasmic reticulum, enhance the action of the sodium-potassium pump, maintaining the potential of muscle membranes.
Caffeine and its actions continue to be intensively studied, for example, it has not yet been clarified whether caffeine itself has an effect or whether it is a complex effect of caffeine and its metabolites.
The list of proven properties of caffeine, of course, is not complete and many scientists recommend caffeine for sports purposes. For example, coffee diuretics can be used for weight loss when needed.
An increase in performance in aerobic types of exercise has been proven for a long time, but there is no clear opinion about the effect on high-intensity exercise. If caffeine causes an increase in strength and power, it is predominantly in highly trained athletes (research by JR Hoffman and JR Stout, 2008).
Correct doses of caffeine - for athletes and amateurs
A safe dose of caffeine depends on your health condition. Some people drink strong coffee all day without any harmful consequences, while for others, a single cup causes blood pressure to rise, sleep is disturbed, headaches and nerves are unsettled. True, caffeine-induced nervousness can be mitigated by the amino acid L-theanine, which is found in green tea leaves. Interestingly, similar symptoms are observed in people with caffeine withdrawal. They also yawn, complain of fatigue, runny nose, muscle stiffness, and find it difficult to concentrate. Despite its positive properties, caffeine cannot be considered a completely safe product.
Reputable organizations such as the European Safety Agency food products(EFSA), the US National Academies of Sciences (NAS) and Health Canada concluded that Healthy adults can consume up to 400 mg of caffeine per day without problems. More than 400 mg can be taken at special occasions(for example, during emergency preparation for an exam). This dose will not cause side effects, if such force majeure events occur rarely.
Here's an example of which drinks contain a safe daily dose of caffeine:
The effects of caffeination depend on the time of administration. Most people can drink 200 mg of caffeine in one sitting less than 2 hours before intense exercise. physical activity. However, even 100 mg can disrupt sleep if you drink coffee or energy drink at night.
Caffeine leaves the body rather slowly, the half-life is about 5 hours, so people who drank strong coffee less than 10 hours ago still have some amount of alkaloid fermenting in their blood.
Restrictions on caffeine intake: children, pregnant women, those suffering from cardiovascular diseases
European Food Safety Authority Recommends for nursing and pregnant women , as well as for those who are just planning pregnancy, limit daily consumption caffeine 200 mg. Some experts allow 300 mg/day, however, according to some reports, caffeine causes nausea in pregnant women and, much worse, the risk of miscarriage.
Data on safe doses of caffeine for children and teenagers clearly not enough. According to European experts, 3 mg/kg of body weight per day will not harm young consumers. In Canada, a dose of no more than 2.5 mg/kg/day is considered safe. In accordance with these standards, children, depending on age, are allowed to:
- 4-6 years - 45 mg/day
- 7-9 years - 62.5 mg/day
- 10-12 years - 85 mg/day.
In adults healthy people, which do not exceed the permitted 400 mg, the risk of developing cardiovascular diseases does not increase. But for people with high blood pressure or those who have already suffered cardiovascular diseases In other words, for patients for whom stimulants are contraindicated, the effects of caffeine intake are less clear. Caffeine increases blood pressure for 3-4 hours, this is a proven fact. However, with regular consumption this effect is not so noticeable. A moderate amount will not harm them, but it is better to consult a doctor about specific doses.
Lethal dose of caffeine
It is important to choose a dose of caffeine so that, on the one hand, it has an effect on the body, and on the other hand, it does not harm the condition and health. There is even one known death from a caffeine overdose, which was reported to Zozhnik by fitness expert Sergei Strukov: before his death, the deceased consumed 12 grams (not milligrams!) of caffeine, which corresponds to approximately 6 liters of strong coffee. This is one and a half hundred of our most common version of caffeine in tablets.
Scientist Williams in a 1997 study recommended 5 mg of caffeine per kilogram of body weight in competition conditions. That is, the dose for a 70-kilogram athlete is about 350 mg (this is what is contained in about 200 ml of espresso or about a liter of regular instant coffee).
Another scientist, Rosenblum, in a 1999 study recommends 3-6 mg of caffeine per kilogram of body weight - “this leads to increased performance and does not exceed the doping threshold.” By the way, since 2004, caffeine has been removed from the list of doping drugs.
Fitness experts recommend taking caffeine not in the form of coffee or tea, but in tablets - this way it’s easier to control the dosage and you don’t need to consume, for example, huge volumes of liquid. In addition, caffeine tablets affect performance significantly more than consumption from drinks or foods (TE Graham, E Hibbert and P Sathasivam, 1998).
Scientists have found that positive impact caffeine on the nervous system (improved mood, learning abilities, memory, attention and performance) is observed with intake of 1-5 mg/kg body weight (70-350 mg for a 70 kg person), especially in older women. Moreover, the effect of caffeine intake is greater in people who do not consume it constantly (research by MJ Arnaud, 2009).
As the dose increases to 9-13 mg per kilogram of weight (600-1000 mg per 70 kg person), negative influence caffeine for sleep: the total time is reduced, the quality decreases, the number of spontaneous awakenings and body movements increases.
Doses above 15 mg per kilogram of body weight may cause side effects such as headaches, nervousness, restlessness, insomnia, irritability, ringing in the ears, gastrointestinal disorders, muscle twitching and severe rapid heartbeat(a study by a number of scientists in 2006). Such symptoms usually occur with chronic use of high doses of caffeine (there is even such psychological disorder– caffeineism), and vice versa: after sudden cessation of intake.
According to a 2009 study by MJ Arnaud, 100-200 mg of caffeine per kilogram of body weight (7-14 grams of caffeine for a 70-pound person) was associated with confusion, seizures, and death, according to several earlier studies: lethal dose caffeine – more than 18 grams per day (this is contained in approximately 10 liters of medium-strength Americano coffee).
Caffeine tolerance
Caffeine tolerance is a term often used to describe the effects of caffeine on the body. At its core, it describes how much a certain dose of caffeine affects a particular person.
Don't be confused this term with caffeine sensitivity. Resilience occurs over time, while sensitivity is determined by an individual's genetic predisposition to absorb the caffeine molecule.
Consider a person who has never taken caffeine in his life, or who has abstained from caffeine-containing foods and drinks for a long time. It is generally accepted that such a person will have zero tolerance to caffeine. In other words, his body will mistake caffeine for an unfamiliar substance.
It is in such cases that the effect of taking caffeine will be most noticeable. It can be noted:
- Euphoria
- Increased vigilance
- Positive mood,
- Increased motivation
- Increased energy.
However, if you take the same dose of caffeine the next day, you will notice that the above effects are manifested to a lesser extent.
If you continue to consume caffeine daily, the expected effect will decrease in a very short time.
Ultimately, the same amount of caffeine will only bring you to a “normal” state.
This means that the person will feel noticeably tired and complete absence energy – much more noticeable than before starting to drink caffeine. And the usual daily dose will only return him to working mode, and will not give him the expected “superpowers”.
How quickly does caffeine tolerance develop?
One study found that Complete caffeine tolerance developed in subjects within just 1-4 days . Among the indicators measured were an increase in blood pressure, an increase in heart rate, and the level of epinephrine in the blood plasma. After 1-4 days, these indicators returned to their original values.
Another study found that one reason for the development of caffeine resistance is an increase in the number of adenosine receptors in the brain. Purpose given growth is compensation for the “loss” of receptors blocked by caffeine molecules.
Therefore, be prepared that the vigor from a morning cup of coffee and the general feeling of euphoria will quickly fade away. The only way to avoid this is to increasing your daily dose of caffeine every few days to compensate constant growth the number of adenosine receptors and other changes in the body.
Some people realize that drinking liters of coffee is a dubious activity in all respects, so they decide that the “normal” state after the usual dose of caffeine will suit them just fine.
However, not everyone shares this opinion. And unfortunately, here they are waiting main danger: Soon, wanting to continue to feel the surge of energy from drinking caffeine, they risk getting very close to doses that pose a real health risk.
Reversal of caffeine tolerance
Fortunately for all of us, there are ways to restore caffeine tolerance to its original levels or avoid this unpleasant effect altogether.
. This option is intended for those who are already accustomed to daily doses of caffeine. Its essence is to completely abstain from caffeine-containing products for a period of 2 weeks to 2 months (these periods are purely individual and depend on how much caffeine a person usually consumed per day). During this time, the body will adjust to its original mode without caffeine.It is also worth noting that drinking coffee or strong tea late in the evening is not recommended if your caffeine tolerance is zero. There is a very high risk of getting insomnia.
A caffeine reset, or preventing caffeine tolerance, will allow you to experience that wonderful feeling of euphoria with 100-200 mg of caffeine (a dose roughly equal to 1-2 espresso shots). The main thing to remember is to avoid regular (daily) caffeine consumption.
Of course, many people will find it extremely difficult to adhere to such advice. With similar success, you can ask a heavy smoker to smoke only 3 cigarettes at 3-day intervals. Caffeine can be extremely addictive, and some people find it easier to take an all-or-nothing approach: if you drink, then regularly, if you don’t drink, then never at all.
However, if you notice that you have developed a caffeine tolerance, it may be worth considering a reset.
Then everyone can decide for themselves whether caffeine will be their future companion in life. The key question in making this decision is: can you control the quantity and frequency of doses consumed?
Caffeine sensitivity
Caffeine sensitivity, as stated at the beginning of the article, is determined by the ability of a particular organism to metabolize caffeine and is not related to caffeine tolerance.
Caffeine metabolism occurs in the liver with the participation of the enzyme CYP1A2. The body's ability to produce this enzyme is regulated by the CYP1A2 gene. Just small ones individual differences in the DNA sequence of this gene is enough that different people have significant differences in the efficiency of caffeine metabolism and, subsequently, its removal from the body.
Some people's bodies are able to produce this enzyme in very small quantities, while others produce a lot of it. Most of the planet's inhabitants fall approximately into the “golden mean”.
There is a gene called AHR that also plays a role in determining caffeine sensitivity. This gene is responsible for turning the CYP1A2 gene on and off. Approximately 10% of the population metabolizes caffeine very quickly and therefore has low sensitivity to caffeine.
Third genetic factor What affects sensitivity is the type of adenosine receptor in a particular person's brain. People whose structure of these receptors are different from the usual type do not actually feel the invigorating effect of consuming caffeine. Their caffeine molecules simply cannot bind to adenosine receptors.
Recent Study Harvard School The Harvard School of Public Health has identified 6 new types of genes that affect the metabolism of caffeine in different people and the formation of their addiction.
A study of 120,000 participants found:
- 2 genes associated with caffeine metabolism
- 2 Genes Associated with Feelings of Reward from Caffeine Consumption
- 2 genes that regulate fat and blood sugar in response to caffeine.
Other studies conducted in Italy and the Netherlands have shown that the PDSS2 gene may also influence metabolic rate. People who have a specific variety usually drink coffee in smaller quantities.
There is an opinion that the PDSS2 gene determines sensitivity to low levels caffeine consumption, while the CYP1A2 gene is at higher levels.
3 levels of caffeine sensitivity
Based on current data on the genetic nature of sensitivity to caffeine, 3 different levels of this phenomenon can be distinguished. This division, in turn, shows how pronounced the effects of caffeine consumption will be.
- Hypersensitivity to caffeine
People falling into this category, react even to small amounts of caffeine consumed. As small doses as 100 mg and below can cause symptoms of caffeine overdose: insomnia, twitching of limbs, anxiety, rapid heartbeat. In such people, the time it takes for caffeine to be metabolized in the body may be 2 times longer than usual.
- Common sensitivity to caffeine
People with normal sensitivity usually have no problem consuming 200-400 caffeine daily. They also do not have the effect of such doses of caffeine on the quality of sleep if they drink their usual coffee in the first half of the day.
Most people fall into this category. Also, it is for people with normal sensitivity that popular medical standards and recommendations for the amount of caffeine consumed are established.
- Reduced sensitivity to caffeine.
About 10% of the world's population have low sensitivity (hyposensitivity) to caffeine. Their bodies are able to absorb caffeine with such high efficiency that even high doses (>500 mg) do not cause noticeable effects. Even taking caffeine late evening usually does not lead to deterioration in sleep quality.
People with low caffeine sensitivity often consume large amounts of caffeine to achieve the desired effect.
How to determine your level of sensitivity to caffeine?
In order to be able to consume caffeine safely, you should determine your own sensitivity level.
Based on the description of the three sensitivity levels in previous section, you can independently guess which category you fall into.
For hypersensitive to caffeine people can be advised to abstain from drinks with high content caffeine (coffee, energy drinks) and give preference to black or green tea in moderate portions. Complete refusal for caffeine is also an option to consider.
People with normal sensitivity to caffeine can afford 2-3 servings of espresso, 1-2 energy drinks of a standard volume of 500 ml or 3-8 cups of tea (caffeine content greatly depends on the strength and type). The main thing is not to forget about monitoring the consumed dose in accordance with the recommendations (300-400 mg).
But those who were in the group with low sensitivity, may wonder if they need caffeine at all. If you do not experience any positive effects on your mental and physical condition, the feeling of euphoria and increased productivity do not occur even from several doses of espresso, it may be worth giving up caffeine due to its possible toxicity in large doses and the onset of undesirable consequences with prolonged use of such doses.
It is worth noting that the above 3 levels of caffeine sensitivity are not a strict division. Although many coffee, tea or energy drink drinkers will be able to accurately determine their body's reaction based on the signs described, the sensitivity of other people may fall somewhere in the middle.
Some may have normal sensitivity with a bias towards hypersensitivity or, conversely, towards reduced sensitivity. Each person's genetic makeup is unique, and so will their reactions to caffeine. So don’t be surprised if you don’t “fit” perfectly into any of the categories.
Let us add that there are cases when hypersensitivity to caffeine develops over time, and not from birth.
Creatine is not friendly with caffeine
Many readers of Zozhnik know that one of, positive action which has been proven by scientists - creatine. So: scientists have proven that caffeine neutralizes the effect of creatine when taken together, so try to take these drugs at different times days.
Interaction of caffeine with drugs
Caffeine promotes the absorption of acetylsalicylic acid, paracetamol and other non-narcotic analgesics (research by Mashkovsky, 2002).
From negative consequences caffeine: weakening the effect of sleeping pills and narcotic drugs.
Caffeine also (when taken together) increases the likelihood and exacerbates the side effects of these substances: alcohol, disulfiram, estradiol (Estrace), terbinafine (Lamisil), fluvoxamine (Luvox), mexiletine, oral contraceptives, quinolone (Cipro, Penetrex, Tequin, Levaquin, Floxin), riluzole (Rilutek), cimetidine (Tagamet), verapamil (Calan, Isoptin, Verelan), albutyrol (Proventil, Ventolin), metaproterenol (Alupent), ephedrine (Ephedra, Ma Huang), phenylpropanolamine (Dexatrim, Propagest), lithium salts (Eskalith, Lithobid), MAO inhibitors (Nardil, Parnate), methylphenidate (Ritalin), theophylline (Theo-dur).
Caffeine may reduce the effectiveness of: clozapine (Clozaril), clorazepate (Tranxene), oxazepam (Serax), diazepam (Valium).
Caffeine should also not be taken if you are dehydrated.
Caffeine - no sugar
By the way positive effects caffeine may be suppressed by simultaneous intake of sugars according to a study by MJ Arnaud, 2009. Therefore, drink tea and coffee without sugar.
What does caffeine contain?
These foods and medications contain significant amounts of caffeine:
- chocolate: 430 mg/kg,
- instant coffee: 300-480 mg/l,
- Americano coffee: about 300 mg/l,
- espresso coffee: 1700-2250 mg/l,
- cola: about 100 mg/l,
- tea: 180-420 mg/l (such a big difference is due to the difference in varieties and different ways brewing tea),
- standard dose of some aspirin-containing medications: 30-128 mg per dose,
- whiskey: about 150 mg/l,
- energy drinks: 300-350 mg/l.
But this picture shows the caffeine content in various popular drinks:
By the way, “caffeine-free” products still contain it, but in smaller quantities. For example, decaffeinated black tea typically contains 8-42 mg of caffeine per liter, while decaf coffee may contain 5-10 mg of caffeine per liter.
Transparent colorless or slightly yellowish liquid.
Pharmacotherapeutic group
Psychostimulants and nootropics. Xanthine derivatives.
ATX code N06BC01
Pharmacological properties"type="checkbox">
Pharmacological properties
Pharmacokinetics
The drug is quickly distributed in all organs and tissues of the body. Communication with blood proteins (albumin) – 25-36%. Easily penetrates the blood-brain barrier and placenta. Penetrates breast milk. The volume of distribution in adults is 0.4-0.6 l/kg, in newborns – 0.78-0.92 l/kg.
More than 90% of the taken dose of the drug is metabolized in the liver, in children of the first years of life up to 10-15%. In adults, about 80% of a caffeine dose is metabolized to paraxanthine, about 10% to theobromine, and about 4% to
theophylline. These compounds are subsequently demethylated into monomethylxanthines and then into methylated uric acids. The half-life in adults is 3.9-5.3 hours (sometimes up to 10 hours), in newborns (up to 4-7 months of age) - 65-130 hours. Caffeine and its metabolites are excreted by the kidneys (1-2% are excreted unchanged in adults, and up to 85% in newborns).
Pharmacodynamics
Caffeine is an alkaloid found in tea leaves and coffee beans. The pharmacological properties of the drug are divided into central and peripheral.
The central effects, in turn, are divided into psychostimulating and analeptic. The psychostimulant effect of Caffeine-sodium benzoate-Darnitsa is associated with its antagonism to the action of adenosine on purinergic (adenosine) A-1 and A-2 receptors in the central nervous system (CNS). Adenosine is known to suppress central nervous system functions. Under the influence of the drug increases mental activity, mental and physical performance. The psychostimulating effect is directly dependent on the dose. Small doses stimulate the functions of the central nervous system, large doses inhibit them (due to depletion of nerve cells).
The analeptic effect of Caffeine-sodium benzoate-Darnitsa is associated with its effect on the respiratory and hemodynamic centers of the medulla oblongata. As a result, an increase in the frequency and volume of inhalation is observed.
The peripheral effects of the drug are not clear and are related to its dose and level of influence on the vascular bed and myocardium. Coronary blood flow first increases and then decreases, renal blood flow increases, and the vessels of the abdominal cavity and skin narrow. Under the influence of the drug, central blood circulation worsens and cerebrospinal fluid pressure decreases, which explains its effectiveness in migraines. The effect of the drug on the heart is ambiguous. In small doses it causes a positive inotropic effect, in higher doses it causes a positive chronotropic effect. In some people it can cause tachycardia and even arrhythmia.
Indications for use
Infectious and other diseases that are accompanied by depression of the central nervous and cardiovascular systems
Respiratory depression, asphyxia
Poisoning with drugs and other substances that depress the central nervous system
Asthenic syndrome
Spasms of cerebral vessels
Directions for use and doses
For adults, administer the drug subcutaneously in a dose of 1-2 ml of a 10% solution (100-200 mg). The highest single dose is 400 mg, maximum daily dose– 1 year
For children over 12 years of age, the drug should be administered subcutaneously in a dose (depending on
age) 0.25-1 ml of 10% solution (25-100 mg).
Side effects"type="checkbox">
Side effects
Excitement, anxiety, tremor, restlessness, insomnia, headache, dizziness, epileptic seizures, increased reflexes, tachypnea. If the drug is suddenly discontinued after long-term use– increased effect on the central nervous system, increased fatigue,
drowsiness, muscle tension, depression
Palpitations, chest tightness, tachycardia, arrhythmias, increased blood pressure
Nausea, vomiting, diarrhea, exacerbation of peptic ulcer
Hypersensitivity reactions, including rash, itching, urticaria, angioedema, bronchospasm
Hypo- or hyperglycemia, increased creatinine clearance, increased
excretion of sodium and calcium, false increase in urinary concentration
acids in blood plasma determined by the Bittner method, slight increase concentrations of 5-hydroxyindoleacetic acid, vanillylmandelic acid and catecholamines in urine
Other: increased frequency of urination, nasal congestion,
long-term use – addiction, drug addiction
Contraindications
Increased sensitivity to xanthine derivatives and other components of the drug
Increased excitability
Insomnia
Atherosclerosis
Organic diseases of the cardiovascular system, including acute
myocardial infarction
Paroxysmal tachycardia
Arterial hypertension
Glaucoma
Age over 60 years
Pregnancy, lactation period
Children's age up to 12 years
Drug interactions"type="checkbox">
Drug interactions
When used simultaneously with other drugs
Maybe:
with alpha and beta-agonists, analgesics-antipyretics,
clozapine, xanthine derivatives, psychostimulants,
cardiac glycosides, thyroid-stimulatingmimeans– enhancing the effects of the above-mentioned drugs;
with anxiolytics, opioid analgesics, hypnotics and sedatives – weakening of the effects of the above-mentioned drugs;
with antiarrhythmic drugs (mexiletine), hormonal oral contraceptives, disulfiram, enoxacin, erythromycin,
isoniazid, methoxsalen, norfloxacin, ofloxacin, cimetidine,
ciprofloxacin– increased effects of caffeine;
with antidepressants, barbiturates,beta-adrenoblockers, primidone, anticonvulsants(hydantoin derivatives, especially phenytoin), cholestyramine, anticholinergics– weakening the effects of caffeine;
with medications, stimulantsmicentral nervous
system, drinks containing caffeine– overstimulation
central nervous system;
with MAO inhibitors, procarbazine, furazolidone– dangerous arrhythmias or severe increases in blood pressure;
with ergotamine– increased absorption of the latter from the gastrointestinal tract;
with calcium supplements– weakening of absorption of the latter from the gastrointestinal tract;
with drugamilithium– increased excretion of the latter in urine;
with nicotine– increased excretion of caffeine in urine.
The drug slightly increases the concentration of 5-hydroxyindoleacetic acid when determined in urine.
The drug slightly increases the concentration of catecholamines and
vanillylmandelic acid, which can lead to false positive
test results for diagnosing pheochromocytoma and neuroblastoma.
The drug should not be used during tests.
The drug may lead to false results determination of urate concentration in blood serum using the Bittner method.
Caffeine is an adenosine antagonist.
Special instructions
The effect on the central nervous system depends on the type of nervous system and can manifest itself as both excitation and inhibition of the higher nervous system.
activities.
Due to the fact that the effect of caffeine on blood pressure consists of vascular and cardiac components, it can develop as an effect
stimulation of the heart and slight inhibition of its activity.
Use with caution in patients peptic ulcer stomach and duodenum history of epilepsy
For apnea in newborns and infants in postoperative period(prevention) caffeine or caffeine citrate is used, but not
caffeine sodium benzoate.
Children
The drug should not be used in children under 12 years of age.
Pregnancy and lactation
The drug should not be used during pregnancy or breastfeeding.
Features of the effect of the drug on the ability to drive vehicles and potentially dangerous mechanisms
During treatment, care should be taken when driving vehicles and working with other mechanisms, and if side effects from the nervous system occur, refrain from working with potential dangerous species activities that require increased concentration and speed of psychomotor reactions.
