Active substance:
Caffeine-sodium benzoate in terms of dry matter - 100 mg or 200 mg.
Excipients: water for injection - up to 1 ml.
Description: Transparent colorless or slightly colored liquid. Pharmacotherapeutic group:Psychostimulant ATX:N.06.B.C.01 Caffeine
Pharmacodynamics:Caffeine is a methylxanthine that has a psychostimulating and analeptic effect. Competitively blocks central and peripheral
Ai and A 2 adenosine receptors. Inhibits the activity of phosphodiesterase in the central nervous system, heart, smooth muscle organs, skeletal muscles, adipose tissue. Stimulates the centers of the medulla oblongata (respiratory and vasomotor), has a direct stimulating effect on the cerebral cortex. In high doses, it facilitates interneuronal conduction in the spinal cord, enhancing spinal reflexes.Increases mental and physical performance, stimulates mental activity, motor activity, shortens reaction time, temporarily reduces fatigue and drowsiness. In small doses, the stimulating effect predominates, and in large doses, the effect of depression of the nervous system predominates.
It quickens and deepens breathing, stimulates the vasomotor center and has a direct relaxing effect on the vascular wall, which leads to dilation of the blood vessels of the heart, skeletal muscles and kidneys, while the tone of the cerebral arteries increases (causes a narrowing of the brain vessels, which is accompanied by a decrease in cerebral blood flow).
oxygen flow and pressure in the brain). Blood pressure changes under the influence of vascular and cardiac mechanisms of caffeine's influence: with normal initial blood pressure it does not change or slightly increases it, with arterial hypotension it normalizes it.It has an antispasmodic effect on smooth muscles (including a bronchodilator effect), and a stimulating effect on striated muscles. Increases gastric secretory activity and diuresis (decreased reabsorption of sodium ions and water in the proximal and distal renal tubules, as well as dilation of renal vessels and increased filtration in the renal glomeruli).
Reduces platelet aggregation and histamine release from mast cells. Increases basal metabolism: increases glycogenolysis, increases lipolysis.
Pharmacokinetics:It is quickly distributed in all organs and tissues of the body: it easily penetrates the blood-brain barrier and the placenta. The volume of distribution in adults is 0.4-0.6 l/kg, in newborns - 0.78-0.92 l/kg. Communication with blood proteins - 25-36%. More than 90% 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 into paraxanthine, about 10% into theobromine, and about 4% into. These compounds are subsequently demethylated into monomethylxanthates 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 life) - 65-130 hours. Caffeine and its metabolites are excreted by the kidneys (unchanged in 1-2% is excreted in adults, and up to 85% in newborns).
Indications:Decreased mental and physical performance, drowsiness, headache of vascular origin (including migraine), moderate arterial hypotension, respiratory depression (including mild poisoning with narcotic analgesics and hypnotics, carbon monoxide, asphyxia of newborns) , restoration of pulmonary ventilation after the use of general anesthesia.
Ciliochoroidal detachment in adults.
Contraindications:Hypersensitivity (including to other xanthines), anxiety disorders, severe arterial hypertension, organic diseases of the cardiovascular system (including acute myocardial infarction, atherosclerosis), paroxysmal tachycardia, frequent ventricular
extrasystole, sleep disturbances, children under 18 years of age (for subconjunctival administration). Carefully:Use with caution in case of glaucoma, increased excitability, in old age, with epilepsy and a tendency to seizures.
Pregnancy and lactation:Excessive use of the drug during pregnancy can lead to spontaneous abortions, retardation of intrauterine development of the fetus, arrhythmia in the fetus; There may be disturbances in skeletal development when using large doses and a slowdown in skeletal development when using lower doses.
The drug passes into breast milk in small amounts, but accumulates in infants and can cause hyperactivity and insomnia. During treatment with the drug, breastfeeding should be stopped.
Directions for use and dosage:Caffeine sodium benzoate is used subcutaneously and subconjunctivally.
Doses of the drug are selected individually. Higher doses for adults (under the skin): single 0.4 g, daily 1 g. Adults: 1 ml of 10-20% solution (100-200 mg); children (depending on age) - 0.25-1.0 ml of a 10% solution (25-100 mg).
In ophthalmic practice, a 10% solution of 0.3 ml is administered subconjunctivally once a day (30 mg). The number of injections depends on the intraocular pressure and the depth of the anterior chamber.
Side effects:From the nervous system:
agitation, anxiety, tremor, restlessness, headache, dizziness, epileptic seizures, increased reflexes, tachypnea, ringing in the ears, insomnia; with sudden withdrawal - increased inhibition of the central nervous system, increased fatigue, drowsiness, muscle tension.From the cardiovascular system: palpitations, tachycardia, arrhythmias, increased blood pressure.
From the digestive system : nausea, vomiting, exacerbation of peptic ulcer.
Others : nasal congestion, with prolonged use - addiction, drug dependence; with subconjunctival injection - short-term pain, slight local swelling with the possible appearance of single petechiae.
Overdose:Symptoms : gastralgia, agitation, anxiety, agitation, restlessness, confusion, dehydration, tachycardia, arrhythmia, hyperthermia, frequent urination, headache, tremor or muscle twitching; nausea and vomiting; ringing in the ears, epileptic seizures.
In newborns (including premature infants), at a plasma caffeine concentration of 50 mg/ml, toxic effects are possible: anxiety, tachypnea, tachycardia, tremor, painful bloating or vomiting, increased Moro reflex, and at higher concentrations - convulsions.
Treatment: maintaining pulmonary ventilation and oxygenation; for epileptic seizures - intravenously, or phenotoin; maintaining fluid and salt balance. Hemodialysis, in newborns, if necessary, exchange blood transfusion.
Interaction:Reduces the effect of sleeping pills and narcotics, increases (improving bioavailability) - acetylsalicylic acid, paracetamol and other non-narcotic analgesics, increases the excretion of lithium drugs in the urine. Concomitant use of the drug with beta-blockers may lead to mutual suppression of therapeutic effects. Accelerates absorption and enhances the effect of cardiac glycosides, increasing their toxicity.
Special instructions:It should be borne in mind that sudden cessation of the drug may lead to increased inhibition of the central nervous system (drowsiness, depression). The effect on the central nervous system depends on the type of nervous system and can manifest itself as both excitation and inhibition of higher nervous activity.
Due to the fact that the effect of caffeine on blood pressure consists of vascular and cardiac components, as a result, both the effect of stimulation of the heart and inhibition (weak) of its activity can develop.
For apnea in newborns and infants in the postoperative period (prevention), either caffeine citrate is used, but not sodium benzoate.
Do not take before bedtime.
Impact on the ability to drive vehicles. Wed and fur.:Considering the side effects of the drug during treatment, care must be taken when driving vehicles or engaging in other activities.
socially hazardous activities that require increased concentration and speed of psychomotor reactions. Release form/dosage:Solution for subcutaneous and subconjunctival administration 100 mg/ml and 200 mg/ml.
Package:1 ml or 2 ml in neutral glass ampoules. 10 ampoules along with a knife for opening ampoules or an ampoule scarifier and instructions for use in a cardboard box. 5 ampoules per blister pack made of polyvinyl chloride film and printed aluminum foil, varnished or without foil. 2 contour blister packs along with instructions for use and a knife for opening ampoules or an ampoule scarifier in a cardboard pack. When using ampoules with notches, rings and dots, do not insert an ampoule scarifier or a knife for opening ampoules.
Storage conditions:At temperatures from 15 to 25 °C.
Keep out of the reach of children.
Best before date:5 years.
Do not use after expiration date.
Conditions for dispensing from pharmacies: On prescription Registration number: LS-000493 Registration date: 05.05.2010 / 27.12.2012 Expiration date: Indefinite Owner of the Registration Certificate:DALKHIMFARM, JSC Russia Manufacturer: Information update date: 21.01.2018 Illustrated instructionsIt often happens that after a medical examination, the doctor prescribes several types of medications to normalize the condition.
When leaving the office, the patient does not always know what exactly was prescribed to him and why. For peace of mind, you need to read the information about the medicine.
The treatment will go smoothly if you know exactly what you have been prescribed.
You can find out information at the pharmacy, since the employees of these organizations are well versed in medications.
It is important that a person does not self-medicate and does not question prescribed medications. Neither the pharmacist nor the patient can select medications better than the attending physician. He chooses the right drug
from many analogues so that the treatment is as effective as possible.
Treatment with the drug is possible only as prescribed by a doctor.
The dosage is prescribed based on several parameters:
The drug is a psychostimulant drug.
Instructions for using the solution:
These instructions apply to the solution. It is administered subcutaneously. Caffeine tablets are prescribed in a different dosage.
Instructions for use of caffeine tablets:
Important! The dosage is determined by the doctor; it is not recommended to take this drug on your own. A one-time dose is possible for low blood pressure and poor health.
The medicine has contraindications and side effects. Taking medication on a regular basis is possible only after consultation with a specialist.
The medicine is not suitable for everyone; there are a number of contraindications.
If you have been prescribed caffeine sodium benzoate, you have low blood pressure or tone.
There are several reasons for prescribing this drug:
Important! The drug has direct contraindications! Check out the list!
Contraindications:
The drug is well tolerated. In rare cases, side effects are possible:
Composition of the drug caffeine-sodium benzoate per tablet:
The main active ingredient is caffeine. Starch and calcium stearate are excipients that make caffeine easier to digest.
The cost of the drug differs in different regions. Average price in the country: from 27 to 34 rubles.
Analogue:
These drugs are similar in composition and have the same base: the same active ingredient. Citramon has the most similar composition.
It contains caffeine and actively fights headaches, drowsiness, and dizziness caused by low blood pressure.
Helps cope with toothache, migraine, neuralgia. Taken for influenza and acute respiratory infections.
The cost of the medicine varies from 45 to 70 rubles, depending on the region. Citramon is used with caution in the presence of hypertension or sleep disturbances.
Contraindications to the use of Citramon:
Dia-Activanad-N has a similar effect.
Contains substances that distinguish it from Citramon and Caffeine:
Dia-Activanad-N is prescribed for decreased tone, decreased body resistance to various diseases, increased fatigue, and drowsiness.
Indicated for use by people experiencing prolonged mental and physical stress. The drug is useful for patients with diabetes.
Contraindications do not include pregnancy, but manufacturers recommend using the medicine with caution during this period. This also applies to breastfeeding.
Side effects when taking Dia-Activanad-N:
The medicine is taken during or after meals. Taking on an empty stomach will cause indigestion.
Similar medications with slight differences in composition and indications for use.
Only the attending physician can prescribe this or that drug, since self-medication is dangerous, can lead to negative health consequences, and worsen the situation.
Do not self-medicate; for this there are people who have studied this craft for many years. Trust the professionals and be healthy.
Instructions for use of Caffeine sodium benzoate 20% solution for injection
for stimulation of the central nervous and cardiovascular systems in animals
(manufacturing organization: Nita-Pharm CJSC, Saratov)
I. General information
Caffeine sodium benzoate 20% (Coffeinum-natrii benzoas 20% solution pro injectionibus).
International nonproprietary name: Caffeine, sodium benzoate.
The drug is available in the form of a sterile solution for injection.
1 ml of the drug contains caffeine 75 mg, sodium benzoate 120 mg and excipients.
In appearance, the drug is a clear, colorless liquid.
Caffeine sodium benzoate is available packaged in glass bottles of 10, 20, 100 ml, hermetically sealed with rubber stoppers and rolled aluminum caps.
The shelf life, subject to storage conditions, is 2 years from the date of manufacture, after opening the bottle - 28 days.
Do not use Caffeine Sodium Benzoate after the expiration date.
Store the medicinal product with precautions (list B), in the manufacturer's closed packaging, separately from food and feed, in a dry place, protected from direct sunlight, at a temperature from 0°C to + 25°C.
The bottle is opened using a sterile syringe.
It is recommended to store the opened bottle at a temperature of 0 to + 10 ⁰C in a dry place, protected from direct sunlight.
Caffeine sodium benzoate should be kept out of the reach of children.
No special precautions are required when disposing of unused drug.
Unused medicinal product is disposed of in accordance with legal requirements.
II. Pharmacological properties
Caffeine benzoate sodium 20% solution for injection has a stimulating effect on the central nervous system of animals. It enhances and regulates excitation processes in the cerebral cortex, enhances positive conditioned reflexes and increases motor activity. The stimulating effect of caffeine leads to increased physical performance, reduced fatigue and prevents drowsiness. The effect of the drug depends on the dose, as well as on the type of higher nervous activity of animals. Large doses of the drug can lead to depletion of nerve cells.
Under the influence of the drug, cardiac activity increases, in collaptoid and shock conditions, blood pressure rises, gas exchange increases, water and nitrogen metabolism increases, breathing becomes more frequent, breathing becomes deep, especially against the background of depression of the respiratory center. The drug has a moderate diuretic effect.
Caffeine benzoate sodium 20% injection solution according to the degree of impact on the human body according to GOST 12.1.007 is classified as low-hazard substances (hazard class 4).
III. Application procedure
Caffeine benzoate sodium 20% solution for injection is prescribed for horses, cattle, sheep, goats, pigs, and dogs. Used to stimulate the central nervous system in case of poisoning with poisons that depress the central nervous, cardiovascular and respiratory systems, fatigue, muscle weakness that occurs in various diseases.
Used to stimulate the cardiovascular system in case of weakness of cardiac activity, decreased excitability and conductivity in the heart muscle, and shock conditions. The drug is used to stimulate the respiratory center when it is depressed and weakened breathing, with a spastic state of the muscles of the gastrointestinal tract, with a maternity cut in cows. Used for chronic myocarditis, myodystrophies, chronic myodegenerations, as a vasodilator for spasms of blood vessels in the brain, kidneys, and heart.
Contraindications to the use of Caffeine benzoate sodium 20% solution for injection are: individual intolerance to the components of the drug, severe arterial hypertension, organic diseases of the cardiovascular system (including atherosclerosis), increased excitability.
Caffeine benzoate sodium 20% solution for injection is used subcutaneously in the following doses:
Doses and timing of use depend on the weight of the animal and the course of the disease.
In case of overdose or exceeding the duration of the recommended course of treatment, anxiety, agitation, insomnia, tachycardia, arrhythmias, increased blood pressure, nausea, and vomiting are possible. In this case, stop using the drug and prescribe symptomatic treatment.
No peculiarities of action were identified during the first use of the drug and when it was discontinued.
If one or more doses of the drug are missed, use is carried out according to the same scheme in accordance with these instructions. Do not administer a double dose to compensate for a missed dose.
The use of caffeine sodium benzoate 20% solution for injection does not exclude the use of other medications. The drug is combined with cardiac glycosides atropine, bronchodilators, analgesics, ergot alkaloids, bromides, accelerates their absorption and enhances the effect, reduces the effect of sleeping pills and narcotics.
Meat and milk during and after the use of caffeine sodium benzoate 20% solution for injection are used without limitation.
IV. Personal prevention measures
When using Caffeine benzoate sodium 20% solution for injection, no special precautions are required. After finishing work, wash your hands with warm water and soap.
It is prohibited to smoke, eat or drink during work.
All work with the medicinal product should be carried out in compliance with the rules of personal hygiene and safety precautions provided for when working with veterinary medicinal products.
Bottles of Caffeine benzoate sodium 20% injection solution are prohibited from being used for food purposes.
In case of accidental contact of the drug with the skin or mucous membranes of the eyes, rinse with plenty of water.
If ingested, consult a doctor.
Manufacturing organization: Nita-Pharm CJSC; 410010, Saratov st. Osipova, 1.
Address of place of production: 410010, Saratov st. Osipova, 1.
In this article you can read the instructions for use of the drug Caffeine. Reviews of site visitors - consumers of this medicine, as well as the opinions of specialist doctors on the use of Caffeine in their practice are presented. 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 the treatment of low blood pressure (hypotension), spasms and drowsiness in adults, children, as well as during pregnancy and lactation.
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
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
Contraindications
special instructions
It can be used as mono- or as part of combination therapy.
Drug interactions
When used simultaneously, 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:
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 has been getting a lot of praise lately, and for good reason – based on solid 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.
Caffeine is a central nervous system stimulant, with effects similar to amphetamines, only much weaker. The first study to prove the positive effect of caffeine on performance during aerobic exercise was 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:
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).
A safe dose of caffeine depends on your health condition. Some people drink strong coffee all day long without any harmful consequences, while for others, just a single cup causes their blood pressure to rise, their sleep to be disturbed, headaches, and nerves. 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.
Authoritative organizations such as the European Food Safety Authority (EFSA), the US National Academies of Sciences (NAS) and Health Canada have concluded that Healthy adults can consume up to 400 mg of caffeine per day without problems. More than 400 mg can be taken on 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 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.
European Food Safety Authority Recommends for nursing and pregnant women , as well as for those who are just planning a pregnancy, limit daily caffeine consumption to 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:
In healthy adults who 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 in 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.
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. 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 have a significantly greater impact on performance than consumption from drinks or foods (TE Graham, E Hibbert and P Sathasivam, 1998).
Scientists have found that the positive effects of caffeine on the nervous system (improving mood, learning abilities, memory, attention and performance) are observed when taking 1-5 mg/kg body weight (70-350 mg for a 70-kg person), especially in the elderly 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-kilogram person), the negative effect of caffeine on sleep begins to appear: the total time is reduced, the quality decreases, and the number of spontaneous awakenings and body movements increases.
Doses above 15 mg per kilogram of body weight can cause side effects such as headaches, nervousness, restlessness, insomnia, irritability, ringing in the ears, gastrointestinal disorders, muscle twitching and rapid heartbeat (a study by several scientists in 2006) . Such symptoms usually occur with chronic use of high doses of caffeine (there is even such a psychological disorder as caffeineism), and vice versa: after sudden cessation of intake.
According to a 2009 study by MJ Arnaud, consuming 100-200 mg of caffeine per kilogram of body weight (7-14 grams of caffeine for a 70-pound person) causes confusion, seizures, and death, according to 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 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.
This term should not be confused 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. You can note:
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.
What this means is that the person will experience noticeable fatigue and a complete lack of 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”.
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. The purpose of this growth is to compensate 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 the daily dose of caffeine every few days in order to compensate for the constant increase in 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, this is where the main danger awaits them: 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.
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 number and frequency of doses consumed?
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 individual differences in the DNA sequence of this gene are enough for different people to experience 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 a low sensitivity to caffeine.
A third genetic factor that influences 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.
A recent study from The Harvard School of Public Health identified 6 new types of genes that influence caffeine metabolism and addiction in different people.
A study of 120,000 participants found:
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.
It is believed that the PDSS2 gene determines sensitivity at low levels of caffeine consumption, while the CYP1A2 gene determines sensitivity at higher levels.
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.
People who fall into this category react to even 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.
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.
About 10% of the world's population have low sensitivity (hyposensitivity) to caffeine. Their bodies are able to metabolize caffeine with such high efficiency that even high doses (> 500 mg) do not cause noticeable effects. Even taking caffeine late in the evening does not usually cause poor sleep quality.
People with low caffeine sensitivity often consume large amounts of caffeine to achieve the desired effect.
In order to be able to consume caffeine safely, you should determine your own sensitivity level.
Based on the description of the three levels of sensitivity in the previous section, you can make your own guess as to which category you fall into.
For hypersensitive to caffeine People can be advised to avoid drinks with high caffeine content (coffee, energy drinks) and prefer black or green tea in moderate portions. Quitting caffeine completely 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 state, a feeling of euphoria and increased productivity do not occur even after a few shots of espresso, you may want to give up caffeine due to its possible toxicity in large doses and the onset of undesirable effects 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.
Many readers of Zozhnik know that one of the supplements, the positive effects of which have been proven by scientists, is creatine. So: scientists have proven that caffeine neutralizes the effect of creatine when taken together, so try to take these drugs at different times of the day.
Caffeine promotes the absorption of acetylsalicylic acid, paracetamol and other non-narcotic analgesics (research by Mashkovsky, 2002).
Among the negative effects of caffeine: weakening the effect of sleeping pills and narcotics.
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.
By the way, the positive effects of caffeine can be suppressed when taking sugars at the same time, according to a study by MJ Arnaud, 2009. Therefore, drink tea and coffee without sugar.
These foods and medications contain significant amounts of caffeine:
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.
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