Table of contents

  • Brand Names
  • Drug Combinations
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Unlabeled Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Toxicological Effects
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Inhibits
  • Induces
  • Drug Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names


Austria: Nymusa; Czech Republic: Nymusa; Estonia: Nymusa; France: Citrate de Cafeine; Germany: Coffeinum N, Percoffedrinol N, SK-Dragees Bonnies; Hungary: Tabletta Coffeini; Ireland: Nymusa; Latvia: Nymusa; Poland: Kofex; Portugal: Nymusa; Romania: Nymusa; Slovakia: Nymusa; Spain: Durvitan; Sweden: Koffein, Nymusa.

North America

Canada: Alert Aid Caffeine, Caffeine, Water Joe; USA: Cafcit, Caffeine.

Latin America

Argentina: Cafeína.


Japan: Caffeine.

Drug combinations

Caffeine and Acetaminophen

Caffeine and Aspirin

Caffeine and Ergotamine

Caffeine and Ibuprofen

Caffeine and Phenylephrine

Caffeine and Propyphenazone

Caffeine, Acetaminophen, and Ascorbic Acid (Vitamin C)

Caffeine, Acetaminophen, and Aspirin

Caffeine, Acetaminophen, and Butalbital

Caffeine, Acetaminophen, and Carbasalate Calcium

Caffeine, Acetaminophen, and Codeine

Caffeine, Acetaminophen, and Dihydrocodeine

Caffeine, Acetaminophen, and Guaifenesin

Caffeine, Acetaminophen, and Phenylephrine

Caffeine, Acetaminophen, and Propyphenazone

Caffeine, Aspirin, and Butalbital

Caffeine, Aspirin, and Chlorpheniramine

Caffeine, Aspirin, and Dihydrocodeine

Caffeine, Aspirin, and Orphenadrine

Caffeine, Aspirin, and Quinine

Caffeine, Dipyrone, and Ergotamine

Caffeine, Ephedrine, and Theophylline

Caffeine, Ergotamine, and Ibuprofen

Caffeine, Ergotamine, and Terapirol

Caffeine, Acetaminophen, Aspirin, and Chlorphenamine

Caffeine, Acetaminophen, Ascorbic Acid (Vitamin C), and Brompheniramine

Caffeine, Acetaminophen, Butalbital, and Codeine

Caffeine, Acetaminophen, Butalbital, and Phenylephrine

Caffeine, Acetaminophen, Butetamate, and Phenylephrine

Caffeine, Acetaminophen, Codeine, and Scopolamine

Caffeine, Acetaminophen, Morphine, and Opium

Caffeine, Acetaminophen, Ascorbic Acid (Vitamin C), and Chlorpheniramine

Caffeine, Acetaminophen, Chlorphenamine, and Ergotamine

Caffeine, Ascorbic Acid (Vitamin C), Aspirin, and Guaifenesin

Caffeine, Dipyrone, Ergotamine, and Metoclopramide

Caffeine, Acetaminophen, Aluminum Hydroxide, Aspirin, and Magnesium Hydroxide

Caffeine, Acetaminophen, Codeine, Dipyrone, and Phenobarbital

Caffeine, Acetaminophen, Propyphenazone, Pyridoxine, and Sodium Benzoate

Caffeine, Chlorphenamine, Dipyrone, Ergotamine, and Metoclopramide

Caffeine, Acetaminophen, Ascorbic Acid (Vitamin C), Codeine, Diphenhydramine, and Phenylephrine

Caffeine, Aluminum Hydroxide, Ascorbic Acid, Aspirin, Chlorpheniramine, and Magnesium Carbonate

Other Caffeine combinations: Ascorbic Acid (Vitamin C); Centella asiatica; Cobalt Sulfate; Coenzyme Q~10~; Cyanocobalamin (Vitamin B~12~); Fucus vesiculosus; Ginkgo biloba; Ginseng; L-Arginine; L-Carnitine; Magnesium; Niacinamide; Pyridoxine (Vitamin B~6~); Riboflavin (Vitamin B~2~); Saccharomyces cerevisiae; Salicylic Acid; Sodium Bicarbonate; Thiamine (Vitamin B~1~); Zinc Sulfate


Caffeine: C~8~H~10~N~4~O~2~. Mw: 194.19. (1) 1H-Purine-2,6-dione, 3,7-dihydro-1,3,7-trimethyl-; (2) 1,3,7-Trimethylxanthine. CAS-58-08-2; CAS-5743-12-4 (monohydrate).

Caffeine Citrate: C~14~H~18~N~4~O~9~. Mw: 386.31.

Pharmacologic Category

Anorexigenic Agents and Respiratory and Cerebral Stimulants, Miscellaneous. (ATC-Code: N06BC01).

Mechanism of action

Increases levels of adenosine 3′,5′-cyclic monophosphate by inhibiting phosphodiesterase. CNS stimulant which increases medullary respiratory center sensitivity to carbon dioxide, stimulates central inspiratory drive, and improves skeletal muscle contraction (diaphragmatic contractility).

Therapeutic use

Apnea of prematurity (caffeine citrate). Acute respiratory depression (caffeine and sodium benzoate). Restore mental alertness or wakefulness (caffeine).

Pregnancy and lactiation implications

Caffeine crosses the placenta; serum levels in the fetus are similar to those in the mother. Moderate consumption (<150 mg/day) is not associated with congenital malformations, spontaneous abortions, preterm birth or low birth weight. Irritability and poor sleeping patterns reported following maternal consumption of large amounts of caffeine. Moderate intake (2-3 cups/day) is compatible with breast-feeding.

Unlabeled use

Spinal puncture headache. CNS stimulant. Diuretic (caffeine and sodium benzoate).


Hypersensitivity to caffeine or any component of the formulation.

Warnings and precautions

Avoid use in agitation, anxiety, or tremor. Use with caution in cardiovascular disease, and avoid use in symptomatic cardiac arrhythmias. Use with caution in history of peptic ulcer and/or gastroesophageal reflux. Use with caution in hepatic or renal impairment. Use with caution in history of seizure disorder (may lower seizure threshold leading to new onset or breakthrough seizure activity). Avoid use of products containing sodium benzoate in neonates (risk of «gasping syndrome»; do not interchange the caffeine citrate salt formulation with the caffeine sodium benzoate formulation). Limit the use of other caffeine-containing beverages or foods. Lithium blood levels may increase during caffeine withdrawal. Analgesia from transcutaneous electrical nerve stimulation may be lessened with concomitant caffeine use.



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