Caffeine
- Atc Codes:N06BC01
- CAS Codes:58-08-2#5743-12-4
- PHARMGKB ID:58-08-2#5743-12-4
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
Europe
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.
Asia
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
Chemistry
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).
Contraindications
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.