Description

Simple

A chemical that is found in tea, coffee, cola beverages, painkillers, and medications used to increase alertness and to manage some lung conditions in premature babies.

Clinical

A stimulant present in tea, coffee, cola beverages, analgesic drugs, and agents used to increase alertness. It is also used in to prevent and treat pulmonary complications of premature birth.

Overview

Caffeine is a drug of the methylxanthine class used for a variety of purposes, including certain respiratory conditions of the premature newborn, pain relief, and to combat drowsiness. Caffeine is similar in chemical structure to [Theophylline] and [Theobromine].[4,16] It can be sourced from coffee beans, but also occurs naturally in various teas and cacao beans, which are different than coffee beans.[12] Caffeine is also used in a variety of cosmetic products and can be administered topically, orally, by inhalation, or by injection.[12]

The caffeine citrate injection, used for apnea of the premature newborn, was initially approved by the FDA in 1999.[19] According to an article from 2017, more than 15 million babies are born premat... Read more

Pharmacology

Indication

Caffeine is indicated for the short term treatment of apnea of prematurity in infants and off label for the prevention and treatment of bronchopulmonary dysplasia caused by premature birth.[ Read more

Pharmacodynamic

Caffeine stimulates the central nervous system (CNS), heightening alertness, and sometimes causing restlessness and agitation. It relaxes smooth muscle, stimulates the contraction of cardiac muscle, and enhances athletic performance.[ Read more

Mechanism of action

The mechanism of action of caffeine is complex, as it impacts several body systems, which are listed below. The effects as they relate to various body systems are described as follows:

**General and cellular actions**

Caffeine exerts several actions on cells, but the clinical relevance is poor... Read more

Absorption

Caffeine is rapidly absorbed after oral or parenteral administration, reaching peak plasma concentration within 30 minutes to 2 hours after administration.[ Read more

Protein binding

Plasma protein binding of caffeine has not been determined for neonates or infants. In vitro studies indicate a protein binding of about 10%-36%. Caffeine is reversibly bound to plasma proteins.[ Read more

Volume of distribution

Caffeine has the ability to rapidly cross the blood-brain barrier. It is water and fat soluble and distributes throughout the body.[12, Read more

Clearance

The clearance of caffeine varies, but on average, is about 0.078 L/kg/h (1.3 mL/min/kg).[ Read more

Half life

In an average-sized adult or child above the age of 9, the half-life of caffeine is approximately 5 hours. Various characteristics and conditions can alter caffeine half-life. It can be reduced by up to 50% in smokers. Pregnant women show an increased half-life of 15 hours or higher, especially in... Read more

Route of elimination

The major metabolites of caffeine can be found excreted in the urine.[12] About 0.5% to 2% of a caffeine dose is found excreted in urine, as it because it is heavily... Read more

Toxicity

The oral LD50 of caffeine in rats is 192 mg/kg.[MSDS] An acute fatal overdose of caffeine in humans is about 10–14 grams (equivalent to 150–200 mg/kg of body weight).[ Read more

Adverse Effects

Contraindications

  • Regions: US
  • Patient Conditions:
      • Name: Hypersensitivity
      • Drugbank Id: DBCOND0013572

Food Interactions

    Information currently not available.

Interactions

Type in a drug name to check for interaction with Caffeine
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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
(R)-warfarin
The metabolism of (R)-warfarin can be decreased when combined with Caffeine.
2,5-Dimethoxy-4-ethylamphetamine
The risk or severity of adverse effects can be increased when 2,5-Dimethoxy-4-ethylamphetamine is combined with Caffeine.
2,5-Dimethoxy-4-ethylthioamphetamine
The risk or severity of adverse effects can be increased when 2,5-Dimethoxy-4-ethylthioamphetamine is combined with Caffeine.
3,5-Diiodotyrosine
3,5-Diiodotyrosine may decrease the excretion rate of Caffeine which could result in a higher serum level.
4-Bromo-2,5-dimethoxyamphetamine
The risk or severity of adverse effects can be increased when 4-Bromo-2,5-dimethoxyamphetamine is combined with Caffeine.
6-Deoxyerythronolide B
The metabolism of Caffeine can be decreased when combined with 6-Deoxyerythronolide B.
6-O-benzylguanine
The metabolism of 6-O-benzylguanine can be decreased when combined with Caffeine.
7-Nitroindazole
7-Nitroindazole may increase the excretion rate of Caffeine which could result in a lower serum level and potentially a reduction in efficacy.
8-azaguanine
The metabolism of 8-azaguanine can be decreased when combined with Caffeine.
8-chlorotheophylline
The metabolism of 8-chlorotheophylline can be decreased when combined with Caffeine.
9-Deazaguanine
The metabolism of 9-Deazaguanine can be decreased when combined with Caffeine.
9-Methylguanine
The metabolism of 9-Methylguanine can be decreased when combined with Caffeine.
Abatacept
The metabolism of Caffeine can be increased when combined with Abatacept.
Abemaciclib
Caffeine may decrease the excretion rate of Abemaciclib which could result in a higher serum level.
Abiraterone
The serum concentration of Caffeine can be increased when it is combined with Abiraterone.
Acebutolol
The risk or severity of adverse effects can be increased when Acebutolol is combined with Caffeine.
Acefylline
The metabolism of Acefylline can be decreased when combined with Caffeine.
Acenocoumarol
The metabolism of Acenocoumarol can be decreased when combined with Caffeine.
Acetazolamide
Acetazolamide may increase the excretion rate of Caffeine which could result in a lower serum level and potentially a reduction in efficacy.
Acyclovir
The metabolism of Acyclovir can be decreased when combined with Caffeine.
23 References
  1. 1 . Nehlig A, Daval JL, Debry G: Caffeine and the central nervous system: mechanisms of action, biochemical, metabolic and psychostimulant effects. Brain Res Brain Res Rev. 1992 May-Aug;17(2):139-70.PubMed: 1356551
  2. 2 . Ding R, Shi J, Pabon K, Scotto KW: Xanthines down-regulate the drug transporter ABCG2 and reverse multidrug resistance. Mol Pharmacol. 2012 Mar;81(3):328-37. doi: 10.1124/mol.111.075556. Epub 2011 Nov 23.PubMed: 22113078
  3. 3 . Kole J, Barnhill A: Caffeine Content Labeling: A Missed Opportunity for Promoting Personal and Public Health. J Caffeine Res. 2013 Sep;3(3):108-113. doi: 10.1089/jcr.2013.0017.PubMed: 24761278
  4. 4 . Michael Z, Spyropoulos F, Ghanta S, Christou H: Bronchopulmonary Dysplasia: An Update of Current Pharmacologic Therapies and New Approaches. Clin Med Insights Pediatr. 2018 Dec 11;12:1179556518817322. doi: 10.1177/1179556518817322. eCollection 2018.PubMed: 30574005
  5. 5 . Collins JJP, Tibboel D, de Kleer IM, Reiss IKM, Rottier RJ: The Future of Bronchopulmonary Dysplasia: Emerging Pathophysiological Concepts and Potential New Avenues of Treatment. Front Med (Lausanne). 2017 May 22;4:61. doi: 10.3389/fmed.2017.00061. eCollection 2017.PubMed: 28589122
  6. 6 . Lipton RB, Diener HC, Robbins MS, Garas SY, Patel K: Caffeine in the management of patients with headache. J Headache Pain. 2017 Oct 24;18(1):107. doi: 10.1186/s10194-017-0806-2.PubMed: 29067618
  7. 7 . Schneider E, Freundlieb S, Tapio S, Boos W: Molecular characterization of the MalT-dependent periplasmic alpha-amylase of Escherichia coli encoded by malS. J Biol Chem. 1992 Mar 15;267(8):5148-54.PubMed: 1544897
  8. 8 . Cappelletti S, Piacentino D, Sani G, Aromatario M: Caffeine: cognitive and physical performance enhancer or psychoactive drug? Curr Neuropharmacol. 2015 Jan;13(1):71-88. doi: 10.2174/1570159X13666141210215655.PubMed: 26074744
  9. 9 . Boswell-Smith V, Spina D, Page CP: Phosphodiesterase inhibitors. Br J Pharmacol. 2006 Jan;147 Suppl 1:S252-7. doi: 10.1038/sj.bjp.0706495.PubMed: 16402111
  10. 10 . White JR Jr, Padowski JM, Zhong Y, Chen G, Luo S, Lazarus P, Layton ME, McPherson S: Pharmacokinetic analysis and comparison of caffeine administered rapidly or slowly in coffee chilled or hot versus chilled energy drink in healthy young adults. Clin Toxicol (Phila). 2016;54(4):308-12. doi: 10.3109/15563650.2016.1146740.PubMed: 27100333
  11. 11 . Mandel HG: Update on caffeine consumption, disposition and action. Food Chem Toxicol. 2002 Sep;40(9):1231-4. doi: 10.1016/s0278-6915(02)00093-5.PubMed: 12204386
  12. 12 . Justin Evans; Amanda S. Battisti (2019). Caffeine. Stat Pearls Publishing.
  13. 13 . IARC Working Group on the Evaluation of Carcinogenic Risk to Humans (1991). Coffee, Tea, Mate, Methylxanthines and Methylglyoxal. International Agency for Research on Cancer.
  14. 14 . Institute of Medicine (US) Committee on Military Nutrition Research. (2001). Caffeine for the Sustainment of Mental Task Performance: Formulations for Military Operations.. National Academic Press.
  15. 15 . Highly Concentrated Caffeine in Dietary Supplements: Guidance for Industry Link
  16. 16 . Caffeine citrate injection FDA label Link
  17. 17 . DailyMed Search: Caffeine Link
  18. 18 . PDB reference Link
  19. 19 . FDA approval Link
  20. 20 . Alcohol and Drug Foundation, Australia Link
  21. 21 . Migergot, DailyMed Link
  22. 22 . Caffeine pathway: Pharm GKB Link
  23. 23 . Caffeine and sodium benzoate injection Link