caffeine (NoDoz, Vivarin)
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Introduction
Tradenames: NoDoz, Vivarin.
Indications
- drowsiness, fatigue
- treatment of apnea in infants
- obesity, weight loss ?[7][9]
- neuroprotection in women ?[6]
- may diminish risk of non melanoma skin cancer[9]
- may reduce risk of diabetes mellitus type 2[15][16]
- may reduce risk of stroke in women[17]
- may reduce risk of depression in women[14]
- nasal congestion, sinusitis[20]
- urinary incontinence[20]
- higher caffeine intake associated with reduced cardiovascular risk[25]
- diminished risk of Parkinson's disease (PD)[26][29]
Dosage
- 100-200 mg PO every 3-4 hours PRN
- maximum: 400 mg/day[12]
- < 500 mg/day considered to be safe[18]
- lethal dose: >= 3 grams within a few hours[18]
Tabs: 100 & 200 mg.
Pharmacokinetics
- metabolized in liver to paraxanthine
- caffeine is a minor metabolite of theophylline
- metabolized by cyt P450 1A2[3]
- maternal metabolism reduced during early pregnancy, clearance is prolonged[8]
- fetal metabolism is low[8]
- high-dose 800 mg in 6 hours increases renal calcium clearance 77%[30]
elimination via liver
1/2life = 3.5 hours
protein binding = 35 %
Adverse effects
- hypertension in adults, adolescents[5]
- moderate use does not increase risk of miscarriage[10]
- high caffeine intake in combination with high stress may be associated with auditory hallucinations[13]
- no association between caffeine intake & cardiovascular events[23]
- no association with arrhythmia (500 mg over 5 hours) in patients with heart failure, even during exercise[24]
- caffeine (>=200 mg/day) during pregnancy associated with overweight offspring up to 5 years of age[27]
- genetic variant in CYP1A2 resulting in slow metabolism of caffeine increases risk of albuminuria, hyperfiltration, & hypertension in heavy coffee consumers (> 3 cups/day)[31]
Drug interactions
- any drug which inhibits cyt P450 1A2 can increase caffeine levels
- any drug which induces cyt P450 1A2 can diminish caffeine levels
- drug interaction(s) of lithium carbonate with xanthine
- drug interaction(s) of MAO inhibitor with caffeine
- drug interaction(s) of methotrexate with caffeine
Laboratory
Mechanism of action
- blocks adenosine A-2A receptors
- relaxes smooth muscle of bronchial airways & pulmonary blood vessels
- in mice, inhibits PP-2A dephosphorylation of threonine 75 on DARPP-32
- may have neuroprotective properties in women[6]
- may have anti-tumor properties[7]
- enhances alertness[19]
- activates arousal[19]
- suppresses the urge to sleep[19]
- may enhance memory consolidation[21]
Notes
- energy drinks may contain significant amounts of caffeine[12]
- FDA recommends avoiding powdered pure caffeine being marketed directly to consumers[23]
More general terms
Additional terms
Component of
- caffeine/ergotamine/suppository
- acetaminophen/caffeine/salicylamide
- acetaminophen/aspirin/caffeine/diphenhydramine
- acetaminophen/aspirin/caffeine/citrate/diphenhydramine
- caffeine/codeine/pheniramine/phenylephrine/salicylate
- caffeine/cobalamin/ibuprofen/pyridoxine/riboflavin/thiamine
- belladonna alkaloid/caffeine/ergotamine/phenobarbital
- belladonna alkaloid/caffeine/ergotamine/pentobarbital
- acetaminophen/caffeine/phenyltoloxamine
- acetaminophen/caffeine/magnesium salicylate/phenyltoloxamine
- acetaminophen/caffeine/isometheptene
- acetaminophen/caffeine/citrate/phenyltoloxamine/salicylamide
- acetaminophen/caffeine/chlorpheniramine/phenylephrine
- acetaminophen/caffeine/chlorpheniramine/hydrocodone/phenylephrine
- acetaminophen/caffeine/chlorpheniramine/guaifenesin
- acetaminophen/caffeine/chlorpheniramine
- acetaminophen/aspirin/caffeine/codeine/salicylamide
- benzoate/caffeine
- caffeine/magnesium salicylate
- aspirin/caffeine/dihydrocodeine
- acetaminophen/caffeine/phenyltoloxamine/salicylamide
- acetaminophen/caffeine/magnesium salicylate
- acetaminophen/caffeine/dihydrocodeine
- caffeine/salicylate
- caffeine/pheniramine/phenylephrine/salicylate
- sodium benzoate/caffeine
- aspirin/caffeine/citrate/orphenadrine
- aspirin/caffeine
- aspirin/butalbital/caffeine/codeine (Fiorinal with Codeine)
- aspirin/caffeine/salicylamide
- acetaminophen/caffeine/pyrilamine
- acetaminophen/caffeine/citrate
- acetaminophen/caffeine/citrate/salicylamide
- acetaminophen/caffeine
- acetaminophen/caffeine/guaifenesin/phenylephrine
- acetaminophen/caffeine/salicylate
- acetaminophen/aspirin/caffeine/salicylamide
- aspirin/caffeine/propoxyphene (Darvon Compound)
- aspirin/butalbital/caffeine (Fiorinal)
- acetaminophen/butalbital/caffeine/codeine (Fioricet with Codeine)
- acetaminophen/butalbital/caffeine (Fioricet, Esgic)
- aspirin/caffeine/orphenadrine (Norgesic)
- caffeine/ergotamine (Cafergot, Ercaf, Wigraine)
- caffeine/ergotamine/pentobarbital (Cafergot PB)
- coffee
- Camellia sinensis (green & black tea)
- guarana
- acetaminophen/aspirin/caffeine (Excedrin Extra, Excedrin migraine)
References
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ Clinical Guide to Laboratory Tests, 3rd ed. Teitz ed., W.B. Saunders, 1995
- ↑ 3.0 3.1 Prescriber's Letter 13(3): 2006 Cytochrome P450 drug interactions Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=220233&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ Lindskog et al. Nature 418:774-8, 2002
- ↑ 5.0 5.1 Journal Watch 24(11):88, 2004 Savoca MR, Evans CD, Wilson ME, Harshfield GA, Ludwig DA. The association of caffeinated beverages with blood pressure in adolescents. Arch Pediatr Adolesc Med. 2004 May;158(5):473-7. PMID: https://www.ncbi.nlm.nih.gov/pubmed/15123481
- ↑ 6.0 6.1 6.2 Ritchie K, Carriere I, de Mendonca A, Portet F, Dartigues JF, Rouaud O, Barberger-Gateau P, Ancelin ML. The neuroprotective effects of caffeine: a prospective population study (the Three City Study). Neurology. 2007 Aug 7;69(6):536-45. PMID: https://www.ncbi.nlm.nih.gov/pubmed/17679672
- ↑ 7.0 7.1 7.2 Lu YP, Nolan B, Lou YR, Peng QY, Wagner GC, Conney AH. Voluntary exercise together with oral caffeine markedly stimulates UVB light-induced apoptosis and decreases tissue fat in SKH-1 mice. Proc Natl Acad Sci U S A. 2007 Jul 31;104(31):12936-41. Epub 2007 Jul 30. PMID: https://www.ncbi.nlm.nih.gov/pubmed/17664435
- ↑ 8.0 8.1 8.2 Prescriber's Letter 15(3): 2008 Caffeine and the Risk of Miscarriage Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=240309&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 9.0 9.1 9.2 Heffernan TP et al. ATR-Chk1 pathway inhibition promotes apoptosis after UV treatment in primary human keratinocytes: Potential basis for the UV protective effects of caffeine. J Invest Dermatol 2009 Feb 26 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/19242509 <Internet> http://dx.doi.org/10.1038/jid.2008.435
- ↑ 10.0 10.1 Committee Opinion No. 462: Moderate Caffeine Consumption During Pregnancy Obstetrics & Gynecology, 2010 116:467-468 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/20664420 <Internet> http://journals.lww.com/greenjournal/Citation/2010/08000/Committee_Opinion_No__462__Moderate_Caffeine.42.aspx
- ↑ Mayo Clinic Staff Caffeine content for coffee, tea, soda and more Mayo clinic Health Information http://www.mayoclinic.com/health/caffeine/AN01211
- ↑ 12.0 12.1 12.2 Prescriber's Letter 18(1): 2011 Energy Drinks Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=270107&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 13.0 13.1 Crowe SF et al The effect of caffeine and stress on auditory hallucinations in a non-clinical sample. Pers Individ Dif 2011 Apr; 50:626 Not indexed in PubMed http://www.sciencedirect.com/science/article/pii/S019188691000591X
Journal Watch Psychiatry July 11, 2011 Massachusetts Medical Society (Subscription required) http://psychiatry.jwatch.org/cgi/content/full/2011/711/1?q=pfw-featured - ↑ 14.0 14.1 Lucas M et al Coffee, Caffeine, and Risk of Depression Among Women Arch Intern Med. 2011;171(17):1571-1578. <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/21949167 <Internet> http://archinte.ama-assn.org/cgi/content/abstract/171/17/1571
Berkowitz SA Coffee Consumption and Depression Risk Arch Intern Med. 2011;171(17):1578 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/21949168 <Internet> http://archinte.ama-assn.org/cgi/content/extract/171/17/1578 - ↑ 15.0 15.1 Salazar-Martinez E et al Ann Intern Med 140:1, 2004 PMID: https://www.ncbi.nlm.nih.gov/pubmed/14706966
- ↑ 16.0 16.1 van Dam RM, Hu FB. Coffee consumption and risk of type 2 diabetes: a systematic review. JAMA. 2005 Jul 6;294(1):97-104. Review. PMID: https://www.ncbi.nlm.nih.gov/pubmed/15998896
- ↑ 17.0 17.1 Larsson SC et al. Coffee consumption and risk of stroke in women. Stroke 2011 Mar 10 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/21393590 <Internet> http://stroke.ahajournals.org/cgi/content/abstract/STROKEAHA.110.603787v
- ↑ 18.0 18.1 18.2 Journal Watch: Massachusetts Medical Society http://www.jwatch.org Sepkowitz KA Energy Drinks and Caffeine-Related Adverse Effects JAMA. 2012, Dec 19 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/23330171 <Internet> http://jama.jamanetwork.com/article.aspx?articleid=1487123
- ↑ 19.0 19.1 19.2 19.3 19.4 Journal Watch. April 10, 2013 Massachusetts Medical Society http://www.jwatch.org
Sharwood LN et al. Use of caffeinated substances and risk of crashes in long distance drivers of commercial vehicles: Case-control study. BMJ 2013 Mar 19; 346:f1140. PMID: https://www.ncbi.nlm.nih.gov/pubmed/23511947 - ↑ 20.0 20.1 20.2 Deprecated Reference
- ↑ 21.0 21.1 Borota D et al Post-study caffeine administration enhances memory consolidation in humans. Nature Neuroscience. Jan 12, 2014 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/24413697 <Internet> http://www.nature.com/neuro/journal/vaop/ncurrent/full/nn.3623.html
- ↑ FDA Safety Alert. July 20, 2014 FDA Consumer Advice on Powdered Pure Caffeine. http://www.fda.gov/Food/RecallsOutbreaksEmergencies/SafetyAlertsAdvisories/ucm405787.htm
- ↑ 23.0 23.1 23.2 Hand L Moderate Tea Drinking Tea May Slow CAC Progression, Cut CV Event Risk: MESA. Medscape. Sep 23, 2016 http://www.medscape.com/viewarticle/869038
- ↑ 24.0 24.1 Zuchinali P et al. Short-term effects of high-dose caffeine on cardiac arrhythmias in patients with heart failure: A randomized clinical trial. JAMA Intern Med 2016 Oct 17; [e-pub] <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/27749954 <Internet> http://jamanetwork.com/journals/jamainternalmedicine/article-abstract/2569283
- ↑ 25.0 25.1 Miller PE, Zhao D, Frazier-Wood AC et al. Associations of coffee, tea, and caffeine intake with coronary artery calcification and cardiovascular events. Am J Med 2017 Feb; 130:188 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/27640739 <Internet> http://www.amjmed.com/article/S0002-9343(16)30925-1/abstract
- ↑ 26.0 26.1 26.2 Postuma RB, Anang J, Pelletier A et al. Caffeine as symptomatic treatment for Parkinson disease (Cafe-PD): A randomized trial. Neurology 2017 Sep 27 PMID: https://www.ncbi.nlm.nih.gov/pubmed/28954882
- ↑ 27.0 27.1 Papadopoulou E, Botton J, Brantsaeter AL. Maternal caffeine intake during pregnancy and childhood growth and overweight: results from a large Norwegian prospective observational cohort study. BMJ Open, Volume 8, Issue 3. April 2018 http://bmjopen.bmj.com/content/8/3/e018895
- ↑ Rothaus C Coffee, Caffeine, and Health NEJM Resident 360. July 22, 2020 https://resident360.nejm.org/clinical-pearls/coffee-caffeine-and-health
- ↑ 29.0 29.1 George J Does Caffeine Protect Against Parkinson's? - Benefit seen even for people with Parkinson's genetic risk MedPage Today September 30, 2020 https://www.medpagetoday.com/neurology/parkinsonsdisease/88893
Crotty GF, Maciuca R, Macklin EA et al Association of caffeine and related analytes with resistance to Parkinson's disease among LRRK2 mutation carriers: A metabolomic study. Neurology 2020. Sept 30. PMID: https://www.ncbi.nlm.nih.gov/pubmed/32999056 https://n.neurology.org/content/early/2020/09/30/WNL.0000000000010863 - ↑ 30.0 30.1 Reuter SE, Schultz HB, Ward MB et al The effect of high-dose, short-term caffeine intake on the renal clearance of calcium, sodium and creatinine in healthy adults. Br J Clin Pharmacol 2021. April 14 PMID: https://www.ncbi.nlm.nih.gov/pubmed/33852164 https://bpspubs.onlinelibrary.wiley.com/doi/10.1111/bcp.14856
- ↑ 31.0 31.1 Mahdavi S, Palatini P, El-Sohem A. CYP1A2 Genetic Variation, Coffee Intake, and Kidney Dysfunction JAMA Netw Open. 2023;6(1):e2247868 PMID: https://www.ncbi.nlm.nih.gov/pubmed/36701157 https://jamanetwork.com/journals/jamanetworkopen/fullarticle/2800839
Database
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=2519
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=64119
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=6241
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=21996
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=28309
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=22181