Caffeine citrate

Caffeine citrate, sold under the trade name Cafcit among others, is a medication used to treat a lack of breathing in premature babies.[1] Specifically it is given to babies who are born at less than 35 weeks or weight less than 2 kilograms (4.4 lb) once other causes are ruled out.[2] It is given by mouth or slow injection into a vein.[1]

Caffeine citrate
Clinical data
Trade namesCafcit, other
AHFS/Drugs.comMonograph
License data
Pregnancy
category
  • US: C (Risk not ruled out)
    Routes of
    administration    		by mouth, i.v.
    ATC code
    Identifiers
    CAS Number
    PubChem CID
    ChemSpider
    CompTox Dashboard (EPA)
    ECHA InfoCard100.125.472
    Chemical and physical data
    FormulaC14H18N4O9
    Molar mass386.314 g/mol g·mol−1
    3D model (JSmol)
      (verify)

    Side effects can include problems feeding, increased heart rate, low blood sugar, necrotizing enterocolitis, and kidney problems.[2][1] Testing blood caffeine levels is occasionally recommended.[1] It is a citric acid salt of caffeine.[3] Caffeine citrate is in the xanthine family of medication.[2] It works by stimulating the respiratory centers in the brain.[1]

    Caffeine was discovered in 1819.[4] It is on the World Health Organization's List of Essential Medicines, the most effective and safe medicines needed in a health system.[5] In the United Kingdom a 10 mg vial costs £4.90.[6] The intravenous form may also be taken by mouth.[6]

    Medical uses

    Caffeine citrate is generally the preferred treatment for apnea of prematurity.[2] It has fewer side effects as compared to theophylline.[2]

    Caffeine improves airway function in asthma, increasing forced expiratory volume (FEV1) by 5% to 18%, with this effect lasting for up to four hours.[7]

    Mechanism

    In method of action, the preparation is exactly identical to that of caffeine base as the citrate counter ion dissociates in water. Doses of caffeine citrate, due to the added weight of the citrate moiety, are understandably higher than with caffeine base, i.e., it takes a larger dose to get the same amount of caffeine.[6] The ratio of therapeutic doses of caffeine base to its citrate salt is typically 1:2.[6] Dosing should therefore be clearly distinguished.[6]

    Manufacture

    The drug is prepared by combining anhydrous caffeine with citric acid monohydrate and sodium citrate dihydrate.

    References
    1. "Caffeine; Caffeine and Sodium Benzoate Injection; Caffeine Citrate". The American Society of Health-System Pharmacists. Archived from the original on 5 November 2017. Retrieved 8 December 2016.
    2. WHO Model Formulary 2008 (PDF). World Health Organization. 2009. p. X. ISBN 9789241547659. Archived (PDF) from the original on 13 December 2016. Retrieved 8 December 2016.
    3. Donn, Steven M.; Sinha, Sunil K. (2012). Manual of Neonatal Respiratory Care. Springer Science & Business Media. p. 457. ISBN 9781461421559. Archived from the original on 2016-12-30.
    4. Brown, Nathan (2015). In Silico Medicinal Chemistry: Computational Methods to Support Drug Design. Royal Society of Chemistry. p. 20. ISBN 9781782621638. Archived from the original on 2016-12-29.
    5. "WHO Model List of Essential Medicines (19th List)" (PDF). World Health Organization. April 2015. Archived (PDF) from the original on 13 December 2016. Retrieved 8 December 2016.
    6. Ainsworth, Sean B. (2014). Neonatal Formulary: Drug Use in Pregnancy and the First Year of Life (7 ed.). John Wiley & Sons. p. 120. ISBN 9781118819517. Archived from the original on 2016-12-30.
    7. Welsh EJ, Bara A, Barley E, Cates CJ (January 2010). "Caffeine for asthma" (PDF). Cochrane Database Syst Rev (1): CD001112. doi:10.1002/14651858.CD001112.pub2. PMID 20091514.
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