Caffeine sodium benzoate - why is it used and who will benefit? How to Consume Caffeine to Improve Athletic Performance Caffeine Sodium Benzoate Tablets

Caffeine is one of the stimulant drugs whose daily use, and even abuse, is common. In any grocery store you can find many “energy drinks” enriched with large amounts of caffeine. And coffee in general is almost the most popular and main drink in society. Many people can be said to simply sip caffeine several times throughout their day without a care in the world.

Pay attention to this guide, which contains everything you need to know: what it is, how it works, what the benefits and risks are, and how to take caffeine most effectively.

What is caffeine?

Caffeine, at the molecular level, is an alkali, carbon-based organic compound that belongs to a class of substances called methylxanthines. Methylxanthines are used for excitatory stimulation of the central nervous system (CNS) and the heart. They are found naturally in coffee beans and tea leaves; to a lesser extent - some fruits and other products of plant origin.

The scientific and chemical name of caffeine is as follows: “1,3,7-trimethylxanthine.” Some manufacturers may use this name on the label in the list of ingredients “for disguise.”

You may also come across the name Caffeine Sodium Benzoate. This form comes in tablets and you can buy it at the pharmacy.

The physiological effects of methylxanthines are as follows: they suppress the action of the neurohormone adenosine (a natural sedative substance produced in the body). Trimethylxanthine molecules are identical to adenosine molecules, and they take their place in the central nervous system and brain. Also, under the influence of caffeine, glycogen breaks down, thereby increasing blood sugar levels, which also gives an additional boost of energy. The synthesis of adrenaline with the help of caffeine is optimized and accelerated. Finally, caffeine helps increase the synthesis of another neurohormone in the body - dopamine. This is a substance that has the property of not only invigorating the body, but also inducing a feeling of calm and well-being.

These properties explain the well-known feeling of moral and physical uplift after a cup of coffee. Which, however, soon becomes dull when this drink is abused. By the way, caffeine makes all metabolic processes in cells proceed faster, and this also helps to stimulate vigor and overall vitality of the body.

Caffeine in sports – beneficial effects

Let us remember that the brain and spinal cord are the main components of the central nervous system. In the human body, this is the path for transmitting and receiving signals between each of the parts of our body. After taking CNS stimulant inhibitors, including caffeine, the calming effect of adenosine is negated, and the body goes into such an “overdrive mode.”

Main short term consequences:

  • Cardiopalmus;
  • Increased metabolic rate;
  • Pronounced psychostimulation, beneficial effect on the overall tone of the body;
  • Vasoconstriction (effect of narrowing of blood vessels);
  • Increased urination and excretion (improved intestinal motility, easy release of the body from excrement).

Some of these effects are highly desirable, while others may not be useful for enhancing performance (namely, vasoconstriction and increased urination).

The half-life of caffeine in the body is quite short (about three to six hours), so it should ideally not be taken uncontrollably, but only at the right time (which will be discussed below).

Caffeine for bodybuilding – how to take it?

Research shows that to the already indicated consequences of caffeine intake, less pronounced, but no less important, should be added: an increase in the synthesis of catecholamine hormones and dilation of the bronchi of the lungs. This also helps athletes feel more alert and resilient during training, while reducing their level of perceived exertion.

Essentially, you feel able to work harder and therefore increase your productivity and productivity. Obviously, this is great for recreational athletes in gyms, as it often results in a noticeable improvement in the quality of their workouts. And the training weights increase, and the consumption of kilocalories increases. Therefore, a cup of natural coffee (or better yet, a caffeine-based pre-workout supplement) before class is definitely a good thing.

There are also versions that, along with psychological support for the athlete, caffeine also has direct physiological support. Namely: increasing the thermic effect of nutrition, in the form of improving carbohydrate and fatty acid metabolism during training. However, there is no scientific basis for these statements. This is, to some extent, an advertisement for caffeine supplements. It is aimed at those who want to lose excess fat, and because of this are looking for ways to increase endurance and power to effectively perform exercises.

How to take caffeine before training?

Caffeine is undoubtedly a proven, important addition to a pre-workout supplement. However, you need to apply it in accordance with your goals and current training plans. For example, “classic” bodybuilders benefit from the use of caffeine, whether they are looking to build muscle or are working to burn fat.

However, many other sports require extremely precise coordination of movements. Caffeine, to some extent, negatively affects it, and therefore for such athletes it can reduce their performance during training and competition. Be careful when using caffeine before sporting events if you are prone to cardiovascular problems. This refers to the effect of caffeine on vasoconstriction and an increase in the overall load on the heart.

The main ergogenic (increased endurance, performance) benefits of caffeine are achieved thanks to:

  • Increasing the body's production of catecholamines (especially adrenaline);
  • Bronchodilation effect (dilation of the bronchi, increased saturation of the lungs with oxygen);
  • Increased carbohydrate metabolism and the use of resulting energy;
  • Increased fatty acid oxidation process.

The source of caffeine before a workout can be a cup of coffee, a pre-workout supplement, or pills. It’s clear with coffee and pre-workouts, but how to take caffeine sodium benzoate in tablets? In fact, this option is the simplest and most convenient, since you can calculate the dosage for yourself. Just see how much substance is contained in one tablet and take the required amount.

Possible side effects

Like any drug, there are some side/undesirable effects from using caffeine, namely:

  • The process of dehydration and mild cramps;
  • Manifestations of nervousness, irritability, aggressiveness, anxiety (individually);
  • Increased plasma cortisol levels (this effect decreases in completely healthy people).

Cortisol is the main biologically active catabolic hormone that destroys proteins and promotes the “accumulation of fat for future use.”

These side effects are usually dose dependent; If you don't overuse caffeine, you can avoid most of them and not even know they exist. Like most chemicals, the difference between a drug and a poison is only a matter of dose. Most people will not experience these side effects if they do not consume caffeine uncontrollably and follow a methodical usage pattern.

By the way, this is a good segue into the next section, where we will discuss how much caffeine people should take and when it makes sense to take it.

Proper dosing of caffeine

The most reasonable thing to do is to find a “golden mean”. That is, such a dose and cycle for yourself, which, on the one hand, will not allow you to become dependent on caffeine, and on the other hand, will not help to “dull” its beneficial effects. Studies have shown that consuming excessive amounts of caffeine before training does not provide a noticeable benefit and does not enhance the desired energizing effect. Therefore, an increased dose of caffeine will not provide benefits, but it may contribute to the manifestation of side effects. Therefore, without fanaticism.

So what is the optimal dose of caffeine before a workout, you ask?

It exists, long ago and repeatedly confirmed by scientific research at different levels. Depending on differences in sensitivity to caffeine, this dose varies from one to three mg per kilogram of body weight. For those using the imperial measurement system, 1 kilogram equals 2.2 pounds. Therefore, it makes sense for a 220-pound (or 100-kilogram) athlete to use approximately 100-300 mg of caffeine before training or competition.

It should be noted that the range of recommended doses is quite wide, and therefore everyone should use some trial and error when assessing their individual response to caffeine. It makes sense to start with the minimum recommended dose based on your weight, and then simply increase the dose if you do not feel a particular increase in performance.

Timing of caffeine intake

Let us remember that caffeine has a half-life of 3 to 6 hours. In this regard, it is best if you take an energizing dose of caffeine about thirty to forty-five minutes before training. If you train on an empty stomach and have previously been on a strict diet, then you are likely to see the effects much faster, within ten or fifteen minutes after taking it. Most athletes eat before training. If you are planning a meal before training, then in this case, it would probably be better to take a dose of caffeine about an hour or two after you eat.

This should give you enough time to digest your food and minimize any acute gastrointestinal upset that may occur from caffeine. Again, trial and error is a critical component to optimizing your individual caffeine intake.

Does the source of caffeine matter?

Caffeine is available for consumption in both its natural (coffee, tea, chocolate) and synthetic forms (caffeine tablets, powder, energy drinks, dietary supplements, carbonated drinks). The source does not make much difference in producing the desired effect. The most common and convenient form of supplemental stimulation is dehydrated caffeine in tablets or powder, which can be purchased at almost any pharmacy or sports supplement store.

Caffeine in this form is not only relatively inexpensive. But also: you can absolutely find out “how much pure caffeine in grams” you get and calculate how to take caffeine in tablets. On the other hand, most energy drinks and pre-workout products have caffeine content listed on the label. For natural coffee lovers, a general “rule of thumb” is that one cup of strong black coffee contains about two hundred mg of caffeine.

How to overcome the addictive effect?

There is a significant caveat to using caffeine: the more you use it, the less sensitive you become to its beneficial effects. This, in turn, entails a gradual increase in the dose of caffeine necessary to achieve an invigorating effect and maximum performance. It is not uncommon to meet avid coffee drinkers who do not feel any invigoration, even after drinking “the whole kettle,” or who receive only a short-term burst of energy, lasting no more than 30 minutes.

It is safe to say that if you are in a similar position, when you can swallow several “shot doses” of espresso without noticing anything, then you need to step back from caffeine for a while. Another sign that it's time to stop consuming caffeine for now is when the side effects begin to outweigh its benefits.

There is a well-founded belief that the correct way to use caffeine is in cycles. The basic recommendation is something like this: after every 8-12 weeks of caffeine use, you should give your body a break from it (and other stimulants too!) for a period of 1 to 2 weeks.

Some people might argue that they take caffeine for months on end and still experience its energizing effects. In this case, it must be said: don't think too much about a simple bike if you want to achieve significant results.

On the other hand, many may need a caffeine “rest” cycle more frequently: every 3-4 weeks. If you take caffeine only a couple of times a week, and not every day, then you can keep it in your diet indefinitely, without turning it off at all. Again, the wisdom is to listen to your body and experiment.

Once you understand how your body reacts to different amounts of caffeine, the process of fine-tuning your dose and using it correctly becomes much easier.

Should you use caffeine?

Studies on the effects of caffeine on the body have shown more positive than negative results. Therefore, it is difficult to argue against the axiom that sports and physical performance can be improved through its use. For most athletes, it takes some time to evaluate their experience and understand what the specific effect is, whether it helps them achieve their goals or not. And in the end, decide what specific dose of caffeine they need.

Additionally, as with any supplement or medication, it would be a good idea to consult with a healthcare professional before beginning regular, long-term use of this stimulant. Additionally, caffeine in high enough doses (over 5 grams) can even be fatal, so please be careful when using it in large quantities.

Summing up

We hope this guide has given you a clearer understanding of how to optimize your use of this popular drug. It's hard not to recommend caffeine to any gym-goer. Even if you are just an amateur and do not strive for great results, but are simply looking for active relaxation after a difficult week at the office. However, if you are reading this article on our website, then we can assume that you are a little more serious athlete than the average amateur. So let's get caffeinated and sweat it out!

Instructions for medical use

medicinalfacilities

Caffeine sodium benzoate

Tradename

Caffeine sodium benzoate

International nonproprietary name

Dosage form

Solution for subcutaneous administration 200 mg/ml

Compound

One ampoule contains:

Description

Transparent colorless or slightly yellowish liquid.

Pharmacotherapeutic group

Psychostimulants and nootropics. Xanthine derivatives. Caffeine.

ATX code N06B C01

Pharmacological properties

Pharmacokinetics

After subcutaneous administration, it is absorbed quickly and completely. Penetrates well through all histohematic barriers, distributed throughout organs and tissues. Penetrates the BBB and the hematoplacental barrier. Concentrations in cerebrospinal fluid and amniotic fluid are comparable to caffeine concentrations in blood plasma.

After administration, it undergoes intensive metabolism in the liver with the formation of 7 metabolites. The main route of metabolism is the formation, under the influence of the cytochrome P 450 isoform CYP1A2, of dimethylxanthines (theophylline, paraxanthine), which have pharmacological activity (72-80% of the administered dose).

The half-life of caffeine (T ½) is 2.5-4.5 hours, in newborns the elimination of caffeine is slowed down, T ½ is 80 ± 23 hours, at the age of 3-5 months it decreases to 14.4 hours and at 5-6 months becomes equal to those of an adult. The total clearance of caffeine in an adult is 155 ml/kg/h, in a newborn child it is 31 ml/kg/h.

In smokers, there is a decrease in the half-life of caffeine by 30-50% compared to non-smokers.

Caffeine is excreted primarily in the urine in the form of metabolites. 10% of the administered dose is excreted unchanged.

Pharmacodynamics

It has psychostimulating and analeptic properties.

The mechanism of action is associated with the ability of caffeine to act as a competitive antagonist of purine A 1 and A 2A receptors.

Caffeine has a direct stimulating effect on the central nervous system: it stimulates mental activity, increases mental and physical performance, shortens reaction time, and activates positive conditioned reflexes. After the introduction of caffeine, vigor appears, fatigue and drowsiness are temporarily reduced or eliminated. In older people the effect is more pronounced.

Affects the cardiovascular system: increases the frequency and strength of heart contractions, and with hypotension increases blood pressure (does not affect normal blood pressure levels). In premature infants, it eliminates periodic breathing and increases the volume of ventilation without significantly affecting the function of the cardiovascular system.

Relaxes the smooth muscles of the bronchi, bile ducts, causes dilatation of blood vessels in skeletal muscles, heart and kidneys. It has a weak diuretic effect due to dilation of renal vessels and inhibition of reabsorption of electrolytes in the renal tubules.

Reduces platelet aggregation. Stimulates the secretion of gastric glands. Increases basal metabolism, enhances glycogenolysis, causing hyperglycemia.

Indications for use

Conditions associated with depression of the functions of the central nervous system, respiratory and cardiovascular systems: drug poisoning, severe infectious diseases, conditions after the use of general anesthetics (anesthesia)

Spasms of cerebral vessels

Decreased mental and physical performance during the period of convalescence after severe general somatic and infectious diseases

Narcolepsy

Breathing disorders (periodic breathing, idiopathic apnea) in newborns, incl. premature babies.

Method of application anddoses

Adults are administered subcutaneously 200 mg (1 ml of 20% solution).

The highest single dose is 0.4 g, the highest daily dose is 1 g.

Intramuscular administration of a solution of caffeine-sodium benzoate is not recommended due to the possibility of developing painful spastic muscle contractions at the injection site.

Side effects

Excitement, anxiety, tremor, restlessness, headache, dizziness, epileptic seizures, increased reflexes, tachypnea, insomnia

CNS depression, increased fatigue, drowsiness, muscle tension with sudden discontinuation of the drug after prolonged use

Palpitations, tachycardia, arrhythmia, increased blood pressure

Nausea, vomiting, exacerbation of peptic ulcer

Nasal congestion

Addiction, drug dependence with long-term use.

Contraindications

Hypersensitivity to xanthine derivatives

Increased excitability, insomnia

Atherosclerosis

Organic diseases of the cardiovascular system, including acute myocardial infarction, paroxysmal tachycardia, arterial hypertension

Pregnancy, breastfeeding period

Old age over 60 years

Glaucoma

Children under 18 years of age (20% solution for injection).

Drug interactions

When used simultaneously, caffeine enhances the effect of antiplatelet drugs.

Reduces the effect of sleeping pills, narcotics and other drugs that depress the central nervous system.

When used simultaneously, it increases the bioavailability of acetylsalicylic acid, paracetamol and ergotamine, thereby enhancing their effect.

When used simultaneously with b2-adrenergic agonists in high doses (salmeterol, salbutamol, fenoterol), it increases the risk of developing hypokalemia.

When used simultaneously with methylxanthines (theophylline, aminophylline), there is an increase in the concentration of theophylline in the blood plasma and an increase in the risk of its toxic effect.

Anticonvulsants (carbamazepine, diphenin), barbiturates accelerate the metabolism of caffeine and reduce its concentration in plasma.

Combined oral contraceptives, macrolide antibiotics (clarithromycin, erythromycin), interferon preparations and antifungals (ketoconazole, fluconazole) slow down the metabolism of caffeine and increase its concentration in plasma.

When caffeine sodium benzoate is used in smokers, its plasma concentration is lower than in non-smoking patients.

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 higher nervous activity.

Due to the fact that the effect of caffeine on blood pressure consists of vascular and cardiac components, both the effect of stimulating the heart and a slight inhibition of its activity can develop.

Use in persons with a history of gastric and duodenal ulcers

Caution is required when prescribing caffeine to these groups of patients due to the increased risk of exacerbation of peptic ulcer disease.

Features of the effect of the drug on the ability to drive vehicles and potentially dangerous mechanisms

Reduces neuromuscular reaction time and is not contraindicated for vehicle drivers and persons working with potentially dangerous mechanisms.

Overdose

Symptoms: gastralgia, agitation, anxiety, agitation, restlessness, confusion, delirium, dehydration, tachycardia, arrhythmia, hyperthermia, frequent urination, headache, increased tactile or pain sensitivity, tremor or muscle twitching; nausea and vomiting, sometimes with blood; ringing in the ears, epileptic seizures (in case of acute overdose - tonic-clonic).

Caffeine in doses of more than 300 mg/day (including against the background of coffee abuse - more than 4 cups of natural coffee, 150 ml each) can cause anxiety, tremor, headache, confusion, extrasystole.

Treatment: gastric lavage if caffeine was taken in the last 4 hours at a dose of more than 15 mg/kg and there was no vomiting caused by caffeine; taking activated carbon, laxatives; for hemorrhagic gastritis - administration of antacid drugs and gastric lavage with an ice-cold 0.9% NaCl solution; maintaining pulmonary ventilation and oxygenation; for epileptic seizures - intravenous diazepam, phenobarbital or phenytoin; maintaining fluid and salt balance.

Release form and packaging

1 ml in glass ampoules.

The text is applied to each ampoule using intaglio printing with quick-fixing ink or a label made of paper for multicolor printing or offset paper, or a self-adhesive label is affixed.

10 ampoules, together with a knife for opening ampoules or an ampoule scarifier, are placed in a cardboard box with a corrugated liner made of corrugated paper.

The box is covered with a label-parcel made from paper for multicolor printing or offset paper.

The boxes, along with instructions for medical use in the state and Russian languages, are placed in group containers. The number of instructions for medical use in the state and Russian languages ​​must correspond to the number of packages.

Or 10 ampoules are placed in a polyvinyl chloride film insert. 1 insert with ampoules, along with a knife for opening ampoules or an ampoule scarifier and instructions for medical use in the state and Russian languages, is placed in a pack of chrome-ersatz cardboard.

This is a psychostimulant with an analeptic effect, a derivative of methylxanthine.

Composition and release form

Caffeine sodium benzoate:

  • Available in 100 mg tablets. There are 6-10 tablets in a pack, 2 packs in a pack.
  • Available in ampoules, ampoules of 10% solution of 1 ml and 2 ml in a package of 10 pieces; ampoules of 20% solution of 1 and 2 ml in a package of 10 pieces.

List B. Store in the ear, cool, out of the reach of children.

Composition of the product

Tablets are white, flat-cylindrical in shape, with beveled edges and scored;

  • 1 tablet contains active substance caffeine sodium benzoate in terms of 100% substance - 0.2 g;
  • Excipients: lactose monohydrate, microcrystalline cellulose, corn starch, povidone, calcium stearate.

pharmachologic effect

Caffeine sodium benzoate blocks central and peripheral A1 and A2 adenosine receptors, and also inhibits PDE activity in the central nervous system, smooth muscle organs, adipose tissue, heart and skeleton. The drug promotes the accumulation of cAMP and cGMP in them. The medication stimulates the centers of the medulla oblongata (respiratory and vasomotor) and has a stimulating effect on the cerebral cortex. At high concentrations, the drug facilitates interneuronal conduction in the spinal cord, which significantly enhances reflexes.

The use of the product helps improve performance, both mental and physical, it actively stimulates mental activity, promotes the growth of motor activity, makes reactions faster, and also has a temporary effect of reducing drowsiness and fatigue. However, in large doses, the drug depresses the nervous system; it is indicated in small doses, then it helps stimulate the body.

The medication has a vasodilating effect, which is explained by its relaxing effect on the walls of blood vessels. The tone of the cerebral arteries increases, blood pressure changes under the influence of caffeine. The medication, for hypertension, normalizes blood pressure, and with normal pressure has no effect on it.

The drug also speeds up breathing and has an antispasmodic effect on smooth muscles, and it stimulates striated muscles. Slightly increases the secretory activity of the stomach. The drug also reduces platelet aggregation and slows the release of histamine from mast cells.

Indications for use of Caffeine Sodium Benzoate

The drug is indicated for depression of the central nervous system, drug poisoning and insufficiency of the cardiovascular system.

Caffeine sodium benzoate helps with diseases that are accompanied by depression of the nervous system, functions of the cardiovascular and respiratory systems. The drug is an excellent remedy for poisoning with opioid analgesics, infectious diseases, and the occurrence of brain spasms. The drug helps well with mental and physical fatigue, increases a person’s performance. Reception is indicated in a state of constant drowsiness.

The drug is often taken by athletes to increase physical activity before competitions. This allows for more frequent and intense training.

Contraindications

The drug is contraindicated in the following cases:

  • Insomnia.
  • Increased excitability.
  • Persistent rise in blood pressure.
  • Glaucoma is increased pressure inside the eyes.
  • Atherosclerosis.
  • Diseases of the cardiovascular system.
  • Senile age.

Side effects

Side effects of Caffeine Sodium Benzoate are:

  • Caffeineism is an excessive addiction to the active substance. Occurs with long-term use of the drug.
  • Sleep disorders.
  • Constant feeling of anxiety.
  • Tachycardia.
  • Increased blood pressure.
  • The occurrence of arrhythmia.
  • Nausea.
  • Vomit.

Symptoms disappear after stopping taking the substance.


Instructions for use

Method and dosage

The medication is available in the form of solution and tablets. The solution is administered subcutaneously, the tablets are taken orally. Adults are prescribed 1-2 ml of a 10% or 20% solution under the skin once a day. Tablets are prescribed 100-200 mg 2-3 times a day for adults and 25-100 mg 2-3 times a day for children.

Caffeine sodium benzoate for weight loss

A standard tablet gives an effect of the same intensity as a cup of strong natural coffee. Within a few hours after its use, a surge of strength is felt, the rhythm of breathing and heartbeat increases, and blood pressure rises. The body is in an active state, and therefore the body spends much more energy burning fat, which leads to intense fat burning.

If you exercise after taking Caffeine Sodium Benzoate tablets, you can achieve better results. In addition, after taking the product, blood flows to the skin through the vessels, which allows you to quickly remove toxins accumulated in the body, get rid of swelling and open the access of oxygen to the body, which also helps burn fat.

In order to achieve an effect in losing weight, the drug is taken half an hour before training; it is necessary to take 1 tablet per 30 kg of weight, but the total number of tablets should not exceed 4 pieces.

Caffeine sodium benzoate for children

During pregnancy and lactation

It is not recommended to take it, as excessive activity can increase the already heavy load on the heart and also negatively affect the development of the fetus. However, in some cases, with very low blood pressure in pregnant women, caffeine is prescribed for use.

Overdose

Cases of overdose occur extremely rarely. In this case, abdominal pain, a feeling of increasing anxiety, agitation, mental and sometimes motor agitation, clouding of consciousness, dehydration, headache, tremor, excessive sensitivity to touch, hyperthermia, and frequent urination are observed. Nausea, vomiting blood, and ringing in the ears may occur. In rare cases, seizures of epilepsy are observed.

Overdose may occur when taking a dose of 300 mg. If symptoms occur, gastric lavage is prescribed (in the absence of vomiting and provided that caffeine has been taken recently), taking activated charcoal and laxatives. It is necessary to maintain ventilation and water balance, to prevent dehydration.

special instructions

Sudden cessation of use leads to inhibition of the nervous system, causing excessive drowsiness and depression. The influence can be expressed both in excessive excitability and in inhibition of reactions. Depending on the characteristics of the body, taking medication may have a stimulating or cardiac depressing effect on blood pressure.

It is not recommended to drive a car and perform life-threatening work, operate machinery, and perform any activities that require concentration while using the drug, as it can affect the speed of psychotropic reactions.

Caffeine sodium benzoate is quite addictive, so you should not take this drug for a long time. To achieve optimal effect, you must take the medicine for a month. From time to time, the drug can be taken for several years in a row.

Interaction with other drugs

  • Simultaneous use of the drug with oral contraceptives, such drugs as ciprofloxacin, disulfiram, norfloxacin, cimetidine, can cause its slow elimination from the liver and increase the level of the drug in the blood.
  • It is not recommended to combine the use of the drug with drinks and other medicinal substances containing caffeine, as this leads to excessive excitability. Nicotine in the body increases the rate of elimination of the drug, and mexiletine reduces the rate of elimination.
  • You should not combine sodium benzoate caffeine with sleeping pills, as it removes the effect of sleeping pills and sedatives. The medication interferes with the absorption of calcium by the stomach, reduces the effect of narcotic drugs on the body, ensures rapid absorption of cardiac glycosides and promotes the rapid excretion of lithium in the urine.

Domestic and foreign analogues

Analogue of the product - Sidnocarb

The drug has an active effect on the central nervous system. Sidnocarb has no obvious peripheral activity and is not addictive even with long-term use. With prolonged or repeated therapy, a weakening of the effect is not observed. This analogue is indicated for use against weakness caused by physical or psychological fatigue, for neurotic disorders, and after traumatic brain injury. Indicated in the complex treatment of mild schizophrenia.

Phenamine - analogue

Active stimulant of the nervous system. The drug is characterized by peripheral action. Helps with chronic weakness, depression, and also to stimulate labor. The drug, when taken for a long time, causes addiction.

Analogue of Caffeine sodium benzoate - Etimizol

The drug has a stimulating effect on the nervous system and also promotes the functioning of the respiratory system. Actively used in psychiatry. This analogue is indicated for states of depression, constant feelings of anxiety and weakness. The use of the drug helps in stimulating the airways after anesthesia and is used as a prophylactic action against pneumonia after operations.

Analogue - Dia-Activanad

A drug with a nervous system stimulant and analeptic effect. Stimulates the respiratory tract, cerebral cortex, vasomotor centers. This analog increases mental and physical activity, reduces fatigue and drowsiness. With hypotension, it increases blood pressure, and also helps to increase the strength and frequency of the heart and the secretion of the gastric glands.

Price in pharmacies

The price of Caffeine Sodium Benzoate in different pharmacies may vary significantly. This is due to the use of cheaper components and the pricing policy of the pharmacy chain.

Read the official information about the drug Caffeine sodium benzoate, the instructions for use of which include general information and a treatment regimen. The text is provided for informational purposes only and cannot serve as a substitute for medical advice.

Caffeine: instructions for use and reviews

Caffeine is a psychostimulant drug.

Release form and composition

Caffeine is produced in the form of a solution for subcutaneous administration: transparent, colorless or slightly colored (in ampoules of 2 ml, 5 ampoules in strip packs, 2 packs in a cardboard box; 5 or 10 ampoules in a cardboard box with partitions or bars).

The composition of 1 ml of solution includes:

  • Active substance – caffeine sodium benzoate 100 or 200 mg;
  • Auxiliary components: sodium hydroxide solution 0.1 M - up to pH 6.8-8.5, water for injection - up to 1 ml.

Pharmacological properties

Pharmacodynamics

Caffeine is an antagonist of central adenosine receptors and stimulates the centers of the medulla oblongata: respiratory, vasomotor and vagal. It also activates the central nervous system and respiratory system, improves the functions of skeletal muscles, the production of hydrochloric acid and pepsin in the gastrointestinal tract, and promotes the processes of glycogenolysis. Caffeine increases the sensitivity of the respiratory center to the stimulating influence of carbon dioxide, enhancing alveolar ventilation. The substance increases the frequency and intensity of heart contractions, as well as cardiac output (has a positive chronotropic effect on the sinoatrial node and a positive inotropic effect on the myocardium).

Caffeine is characterized by diuretic and hypertensive effects, reduces uterine contractility and promotes cerebral vasoconstriction.

Pharmacokinetics

Caffeine is approximately 25–36% bound to plasma proteins. Its biotransformation occurs in the liver. In adult patients, 80% of caffeine is metabolized into paraxanthine (1,7-dimethylxanthine), 10% into theobromine (3,7-dimethylxanthine), and 4% into theophylline (1,3-dimethylxanthine). These compounds are demethylated into monomethylxanthines and then into methylated uric acid derivatives. In premature babies, caffeine is formed from theophylline. The half-life is 3–7 hours, lengthening to 65–130 hours in newborns (a decrease to the level of an adult patient occurs at 4–7 months). The maximum concentration is established 50–75 minutes after the substance enters the body.

Caffeine is excreted in the urine in the form of metabolites (1–2% unchanged). In newborns, it is also excreted through the kidneys, with 85% of the dose excreted unchanged.

Indications for use

  • Decreased physical and mental performance;
  • Moderate arterial hypotension;
  • Muscle weakness;
  • Migraine;
  • Drowsiness;
  • Respiratory depression (including in case of mild poisoning with opioid analgesics and hypnotics, carbon monoxide, asphyxia of newborns, to restore the required level of pulmonary ventilation after the use of general anesthesia).

Contraindications

  • Organic diseases of the cardiovascular system (including acute myocardial infarction, atherosclerosis);
  • Arterial hypertension;
  • Sleep disorders;
  • Glaucoma;
  • Paroxysmal tachycardia;
  • Increased excitability;
  • Epilepsy and tendency to seizures;
  • Frequent ventricular extrasystole;
  • Elderly age;
  • Pregnancy and lactation;
  • Hypersensitivity to the components of the drug.

Instructions for use of Caffeine: method and dosage

Caffeine solution is administered subcutaneously.

Adults are usually prescribed 1 ml of 100 mg/ml or 200 mg/ml solution. The maximum dose is: single – 400 mg, daily – 1000 mg.

Children, depending on age, are usually prescribed 0.25-1 ml of a 100 mg/ml caffeine solution.

The frequency and duration of use are determined by the doctor.

Side effects

According to the instructions, Caffeine can cause the following side effects:

  • Central nervous system: tachypnea, sleep disturbance, tremor, agitation, anxiety, headache, convulsions, dizziness;
  • Cardiovascular system: heart rhythm disturbances, tachycardia, increased blood pressure;
  • Digestive system: nausea, diarrhea, vomiting, exacerbation of peptic ulcer.

With prolonged use, slight addiction is possible (a decrease in effect is associated with the formation of new adenosine receptors in brain cells).

Overdose

Signs of a caffeine overdose include trembling of the entire body, observed in newborns, pain in the stomach or abdomen, nausea and vomiting, sometimes with bloody discharge, vomiting or a swollen abdomen in newborns, the palpation of which is accompanied by painful sensations, increased pain or tactile sensitivity, dehydration , frequent urination, arrhythmia, tachycardia. Taking the drug in very high doses can lead to the appearance of central nervous system symptoms such as headache, clouded consciousness or delirium, restlessness or agitation, anxiety, agitation, irritability, tremors or muscle twitching, photopsia, ringing in the ears or sensations of other symptoms. sounds, sleep disturbances, epileptic seizures (mainly clonic-tonic convulsions) in acute overdose.

Symptomatic therapy is recommended as treatment. If Caffeine was taken in the last 4 hours, its dose exceeded 15 mg/kg, and there was no vomiting caused by this drug, gastric lavage should be performed. It is also recommended to take activated charcoal and laxatives, and for hemorrhagic gastritis - gastric lavage with an ice-cold 0.9% sodium chloride solution and the administration of antacids. If necessary, artificial ventilation and oxygenation are performed. For epileptic seizures, phenytoin, phenobarbital or diazepam are administered intravenously. Water and electrolyte balance should also be maintained. Hemodialysis is often effective in case of overdose, and in newborns, if necessary, exchange transfusion.

special instructions

When using Caffeine, it must be taken into account that sudden cessation of therapy can lead to increased inhibition of the central nervous system in the form of drowsiness and depression.

The effect on the central nervous system can be manifested by both excitation and inhibition of the higher nervous system.

Use during pregnancy and lactation

According to FDA recommendations, caffeine is classified as category C. It increases the risk of spontaneous abortion, provokes intrauterine growth retardation and fetal arrhythmia (when administered to pregnant women in high doses). Results from animal experiments have shown that when administered doses equivalent to the caffeine content of 12–24 cups of coffee drunk per day throughout pregnancy or with a single administration of very high doses (50–100 mg/kg), disturbances in skeletal development are observed (as fingers and individual phalanges) of the fetus. When caffeine was introduced into the body of a pregnant female in smaller doses, slow development of the fetal skeleton was observed.

Caffeine passes into breast milk (its amount is approximately 1% of the concentration in the mother's blood plasma). If a nursing mother ingests this substance in an amount equivalent to 6–8 cups of caffeine-containing drinks per day, the baby may develop insomnia and hyperactivity.

Drug interactions

When Caffeine is used simultaneously with certain medications, the following effects may occur:

  • Narcotics and hypnotics: decreased effectiveness;
  • Non-narcotic analgesics and ergotamine: increasing their effectiveness (due to increased absorption);
  • Cardiac glycosides: enhancing their action and increasing toxicity.

Analogs

Terms and conditions of storage

Store out of reach of children at temperatures up to 25 °C.

Shelf life – 5 years.

Pills.

In blister packs 6 or 10 pcs.

Composition and active substance

Caffeine-sodium benzoate tablets contain:

1 tablet contains caffeine (in the form of sodium benzoate) 0.1 or 0.2 g

pharmachologic effect

Analeptic, psychostimulant, cardiotonic. It has a stimulating effect on the central nervous system, increases reflex excitability of the spinal cord, stimulates the respiratory and vasomotor centers, regulates and enhances excitation processes in the cerebral cortex. Increases mental and physical performance, reduces fatigue and drowsiness. Increases the strength and frequency of heart contractions (especially in large doses), increases blood pressure during hypotension (does not change normal). Dilates the blood vessels of skeletal muscles, heart, kidneys, bronchi, narrows the abdominal organs. Increases the secretory activity of the stomach. Reduces platelet aggregation. Has a moderate diuretic effect. Blocks central and peripheral adenosine receptors. Stabilizes transmission at dopaminergic synapses, beta-adrenergic synapses of the hypothalamus and medulla oblongata, cholinergic synapses of the cortex and medulla oblongata, noradrenergic synapses. The effect of the drug largely depends on the type of nervous system in the patient, so the dosage of caffeine should take into account the individual characteristics of nervous activity.

What does Caffeine-sodium benzoate tablets help with: indications

Diseases accompanied by depression of the functions of the central nervous system, cardiovascular system, respiratory system (drug poisoning, infectious diseases, etc.). For cerebral vascular spasms, to increase mental and physical performance, to eliminate drowsiness, breathing problems, enuresis in children.

Contraindications

Severe arterial hypertension, organic diseases of the cardiovascular system (including atherosclerosis), increased excitability, glaucoma, sleep disorders, old age. Side effects
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.

Caffeine benzoate sodium tablets during pregnancy and breastfeeding

Not described.

Caffeine sodium benzoate tablets: instructions for use

Tablets are taken orally - 0.025-0.1 g 2-3 times a day.
The maximum single dose for adults is 0.4 g, daily dose is 1 g.

Side effects

From the nervous system: agitation, anxiety, tremor, restlessness, headache, dizziness, epileptic seizures, increased reflexes, tachypnea, 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.
Other: nasal congestion, with prolonged use - addiction, drug dependence.

special instructions

It should be borne in mind that sudden cessation of use 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 stimulating the heart and inhibition (weak) of its activity can develop.
For apnea in newborns and infants in the postoperative period (prevention), caffeine or caffeine citrate is used, but not caffeine sodium benzoate.
Excessive consumption during pregnancy can lead to spontaneous abortions, slowing of intrauterine development of the fetus, arrhythmias in the fetus, possible disturbances in skeletal development when using large doses and slowdown in skeletal development when using smaller doses.
Passes into breast milk in small quantities, but accumulates in infants and can cause hyperactivity and insomnia.
Do not take before bedtime.

Compatibility with other drugs

Reduces the effect of sleeping pills and narcotics, 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 cups of natural coffee, 150 ml each) 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.