Log in
Pharmacology · Drugs and Prescriptions

Caffeine-sodium benzoate

Coffeinum-natrii benzoas

Caffeine-sodium benzoate is a psychostimulant from the methylxanthine derivative group. The drug exerts a pronounced stimulating effect on the central nervous system, increasing mental and physical performance.

Test your knowledge on this topicAsk the AI
Pharmacological groupPsychostimulants, methylxanthine derivatives.
Dosage formsTablets 0.1–0.2 g; 10% and 20% solutions in 1 and 2 ml ampoules.
Mechanism of actionAdenosine receptor blockade and phosphodiesterase inhibition.
Dosing regimenOrally 0.1–0.2 g 2–3 times a day; subcutaneously (maximum single dose 0.4 g, maximum daily dose 1.0 g).
How to write a prescription
Rp.: Tab. Coffeini-natrii benzoatis 0,1
D.t.d. N 10
S. Внутрь по 1 таблетке 2-3 раза в сутки

Other notation options: Tab. Coffeini-natrii benzoatis 0,2; Tabulettas Coffeini-natrii benzoatis 0,1; Sol. Coffeini-natrii benzoatis 10% - 1 ml

Dosage form
Tab. 0.1-0.2 g; sol. in amp. 10 and 20% by 1 and 2 ml
Administration
Orally 0.1-0.2 g 2-3 times a day (maximum daily dose 1.5 g); subcutaneously (maximum single dose 0.4 g; maximum daily dose 1.0 g)
Group
Agents affecting the central nervous system
2 min readFor medical studentsUpdated 09/24/2026
Material prepared by WhiteCoat Pro editorial team based on platform study guidesReviewed by medical editor: Aulov A. A., general practitioner · 09/24/2026

Mechanism of action

The drug's effect at the molecular level is realized through three main pathways:

  1. Adenosine receptor blockade: caffeine is a competitive antagonist of adenosine. By eliminating its inhibitory effect (cell hyperpolarization), the drug activates CNS neurons.
  2. Phosphodiesterase (PDE) inhibition: slowing down cAMP degradation leads to its accumulation in brain and myocardial tissues, which enhances metabolic processes.
  3. Effect on intracellular calcium: modulation of Ca2+ ion content in cells.

Pharmacological effects

The drug stimulates mental and physical activity, eliminates drowsiness and fatigue. The hemodynamic effect manifests as stimulation of the vasomotor center: in hypotension, caffeine increases blood pressure, while at normal blood pressure, it practically does not change it. Caffeine also potentiates the effect of non-narcotic analgesics, which makes it widely used in combination drugs (e.g., Citramon).

Test your knowledge on the topicTasks from the «Pharmacology» course bank — instant answers and explanations.

Indications for use

Caffeine-sodium benzoate is prescribed for conditions accompanied by CNS depression, drowsiness, and hypotensive states. In combination therapy, it is used for migraines (in combination with ergot alkaloids) and as a component of analgesic agents.

Side effects and contraindications

Main side effects include psychomotor agitation, insomnia, tachycardia, arrhythmias, and dyspeptic disorders (nausea, vomiting). Prolonged use may lead to dependence development (theism).

Contraindications: pronounced arterial hypertension, atherosclerosis, glaucoma, and insomnia.

Administration and metabolism features

Caffeine is a substrate for the CYP1A2 isoenzyme. Its metabolism depends on diet and environmental factors (e.g., smoking induces this enzyme, accelerating caffeine elimination). The drug is excreted in breast milk. It is important to consider that caffeine is a weakly alkaline substance, so urine acidification accelerates its excretion and weakens its pharmacological action.

Briefly: answers to topical questions

What effect does caffeine have on the respiratory center of the medulla oblongata?

Caffeine has an analeptic effect, stimulating depressed vital centers of the central nervous system. The substance directly excites the respiratory center of the medulla oblongata, reducing the depressing effect of hypnotics and anesthetics. In addition, the drug has a moderate excitatory effect on all parts of the central nervous system.

How does caffeine affect diuresis and glomerular filtration?

Caffeine increases urine output and dilates renal blood vessels. The cited sources do not indicate its effect on glomerular filtration.

How to memorize

Caffeine is an "adenosine blocker": it prevents adenosine from "inhibiting" the brain, keeping us alert.

Class and exam questions

Why does caffeine increase blood pressure?

The drug has a direct stimulating effect on the vasomotor center, leading to an increase in vascular tone.

How does caffeine interact with PDE?

Caffeine inhibits the enzyme phosphodiesterase, which prevents cAMP breakdown and promotes its accumulation in cells.

Does urine pH affect caffeine elimination?

Yes, since caffeine is a weak base, it ionizes more actively in an acidic urine environment and is excreted faster, which shortens its duration of action.

Something unclear? Ask the AIThe AI tutor has read the material on "Caffeine-sodium benzoate" and will explain it in simple terms.

What else to study on this topic

  • Caffeine interaction with other CYP1A2 substrates (theophylline, warfarin).
  • Clinical significance of hepatic microsomal enzyme induction and inhibition.
  • Comparative characteristics of methylxanthine derivatives (theobromine, theophylline).
  • Mechanisms of drug dependence formation (theism).
  • Principles of forced diuresis in poisoning.

Master the entire topic in the «Pharmacology» course

This is a summary. The course covers everything tested in classes and exams.

  • Complete study guide on "Caffeine-sodium benzoate" and 5,304 more pages of the subject
  • Assignments and quizzes after every topic — just like in a colloquium
  • AI tutor answers questions on the topic anytime
  • 116 video lessons on the subject
Open full reviewSubject curriculumfrom 599 ₽ per month

Other topics in the «Drugs and Prescriptions» section

Atropine sulfateAceclidineAeronHexoprenalinePirenzepineIpratropium bromideXylometazolineMetocinium iodideNaphazolineNeostigmineNorepinephrinePipecuronium bromidePlatyphyllineSalmeterolSuxamethoniumTropicamideFenoterolEpinephrineEphedrine hydrochlorideAcetaminophenBromocriptineSodium valproateDiazepamZolpidem
The entire "Drugs and Prescription" section

Free video lessons: pharmacologyShort lessons with study notes — no registration required.

Watch lessons

Prepared by WhiteCoat Pro faculty in accordance with the medical school curriculum. For educational purposes only.