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Caffeine (CUI C0006644) Suggest changes to this concept
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Terms & Properties

Concept Unique Identifier (CUI): C0006644

NCI Thesaurus Code: C328  (see NCI Thesaurus info)

Semantic Type: Organic Chemical

Semantic Type: Pharmacologic Substance

NCIt Definition: A methylxanthine alkaloid found in the seeds, nuts, or leaves of a number of plants native to South America and East Asia that is structurally related to adenosine and acts primarily as an adenosine receptor antagonist with psychotropic and anti-inflammatory activities. Upon ingestion, caffeine binds to adenosine receptors in the central nervous system (CNS), which inhibits adenosine binding. This inhibits the adenosine-mediated downregulation of CNS activity; thus, stimulating the activity of the medullary, vagal, vasomotor, and respiratory centers in the brain. This agent also promotes neurotransmitter release that further stimulates the CNS. The anti-inflammatory effects of caffeine are due the nonselective competitive inhibition of phosphodiesterases (PDEs). Inhibition of PDEs raises the intracellular concentration of cyclic AMP (cAMP), activates protein kinase A, and inhibits leukotriene synthesis, which leads to reduced inflammation and innate immunity.

PDQ Definition: A naturally occurring xanthine derivative with central nervous system (CNS) stimulating activity. Due to the structural similarity to adenosine, caffeine binds to and blocks adenosine receptors, thereby preventing the inhibitory effects of adenosine on nerve cells. This leads to stimulation of medullary, vagal, vasomotor, and respiratory centers in the brain; and the release of epinephrine. Physiologic responses can include bradycardia, tachycardia, vasoconstriction, CNS excitablility, increased respiratory rate, increased blood pressure, increased blood flow to muscles, decreased blood flow to skin and inner organs, and release of glucose by the liver. Due to the interaction between adenosine A2A and dopamine D2 receptors, caffeine can also indirectly increase the levels of dopamine in the brain. Check for active clinical trials using this agent. (NCI Thesaurus)

MEDLINEPLUS Definition: 

Caffeine is a bitter substance found in coffee, tea, soft drinks, chocolate, kola nuts, and certain medicines. It has many effects on the body's metabolism, including stimulating the central nervous system. This can make you more alert and give you a boost of energy.

For most people, the amount of caffeine in two to four cups of coffee a day is not harmful. However, too much caffeine can cause problems. It can

  • Make you jittery and shaky
  • Make it hard to fall asleep or stay asleep
  • Cause headaches or dizziness
  • Make your heart beat faster or cause abnormal heart rhythms
  • Cause dehydration
  • Make you dependent on it so you need to take more of it. If you stop using caffeine, you could get withdrawal symptoms.

Some people are more sensitive to the effects of caffeine than others. They should limit their use of caffeine. So should pregnant and nursing women. Certain drugs and supplements may interact with caffeine. If you have questions about whether caffeine is safe for you, talk with your health care provider.

Food and Drug Administration

NCI-GLOSS Definition: A substance found in the leaves and beans of the coffee tree, in tea, yerba mate, guarana berries, and in small amounts in cocoa. It can also be made in the laboratory, and is added to some soft drinks, foods, and medicines. Caffeine increases brain activity, alertness, attention, and energy. It may also increase blood pressure, heart rate, breathing rate, and the loss of water from the body in urine.

CRCH Definition: An alkaloid stimulant having a purine double-ring structure composed of eight carbons and four nitrogen atoms with methyl groups attached to the nitrogen atoms at the 1, 3, and 7 positions and having double bonds at the carbons in positions 2 and 6.

CSP Definition: 1,3,7-trimethylxanthine, a central nervous system stimulant; action may be mediated by adenosine receptors.

MSH Definition: A methylxanthine naturally occurring in some beverages and also used as a pharmacological agent. Caffeine's most notable pharmacological effect is as a central nervous system stimulant, increasing alertness and producing agitation. It also relaxes SMOOTH MUSCLE, stimulates CARDIAC MUSCLE, stimulates DIURESIS, and appears to be useful in the treatment of some types of headache. Several cellular actions of caffeine have been observed, but it is not entirely clear how each contributes to its pharmacological profile. Among the most important are inhibition of cyclic nucleotide PHOSPHODIESTERASES, antagonism of ADENOSINE RECEPTORS, and modulation of intracellular calcium handling.

Synonyms & Abbreviations: (see Synonym Details)
1,3,7-Trimethyl-2,6-dioxopurine
1,3,7-trimethylpurine-2,6-dione
1,3,7-trimethylxanthine
1-methyltheobromine
1H-Purine-2,6-dione, 3,7-dihydro-1,3,7-trimethyl-
3,7-Dihydro-1,3,7-trimethyl-1H-purin-2,6-dion
3,7-Dihydro-1,3,7-trimethyl-1H-purine-2,6-dione
5036
58-08-2
7-methyltheophylline
Cafeína
Caffeine (substance)
Caffeine [Chemical/Ingredient]
caffeine
CAF
Caféine
Coffein
Guaranine
Koffein
Mateína
Methyltheobromine
Product containing caffeine (medicinal product)
Product containing caffeine
Teina
Theine
Thein
Trimethylxanthine

External Source Codes: 
NCI Thesaurus Code C328 (see NCI Thesaurus info)
CAS Registry Number 58-08-2 (see NLM ChemIDplus info)
FDA UNII Code 3G6A5W338E
NSC Code 5036 (see NCI DTP info)
PDQ Closed Trial Search ID 40817
PDQ Open Trial Search ID 40817 (check for NCI PDQ open clinical trial info)

Other Properties: Property Definitions
Name Value Source
ACTIVE 1 SNOMEDCT_US
AQL AA AD AE AG AI AN BI BL CF CH CL CS CT EC GE HI IM IP ME PD PK PO RE SD SE ST TO TU UR MSH
CASE_SIGNIFICANCE_ID 900000000000448009 SNOMEDCT_US
CHARACTERISTIC_TYPE_ID 900000000000011006 SNOMEDCT_US
CHEBI_ID CHEBI:27732 NCI
Chemical_Formula C8H10N4O2 NCI
Contributing_Source CRCH NCI
Contributing_Source CTRP NCI
Contributing_Source FDA NCI
CTV3ID c44.. SNOMEDCT_US
CTV3ID X7953 SNOMEDCT_US
DATE_CREATED 04/11/2001 MEDLINEPLUS
DATE_LAST_MODIFIED 2008-10-13 PDQ
DC 1 MSH
DEFINITION_STATUS_ID 900000000000074008 SNOMEDCT_US
DID 2503-3751 CSP
DX 19660101 MSH
EFFECTIVE_TIME 20020131 SNOMEDCT_US
FDA_UNII_CODE 3G6A5W338E DRUGBANK
FDA_UNII_CODE 3G6A5W338E NDFRT
INFOODS CAFFN NCI
LEVEL Ingredient NDFRT
MDA 19990101 MSH
MESH_DEFINITION A methylxanthine naturally occurring in some beverages and also used as a pharmacological agent. Caffeine's most notable pharmacological effect is as a central nervous system stimulant, increasing alertness and producing agitation. It also relaxes SMOOTH MUSCLE, stimulates CARDIAC MUSCLE, stimulates DIURESIS, and appears to be useful in the treatment of some types of headache. Several cellular actions of caffeine have been observed, but it is not entirely clear how each contributes to its pharmacological profile. Among the most important are inhibition of cyclic nucleotide PHOSPHODIESTERASES, antagonism of ADENOSINE RECEPTORS, and modulation of intracellular calcium handling. NDFRT
MESH_DUI D002110 NDFRT
MESH_NAME Caffeine NDFRT
MESH_UI M0003138 NDFRT
MMR 20160527 MSH
MN D03.132.960.175 MSH
MN D03.633.100.759.758.824.175 MSH
MODIFIER_ID 900000000000451002 SNOMEDCT_US
MP_HEALTH_TOPIC_URL https://www.nlm.nih.gov/medlineplus/caffeine.html MEDLINEPLUS
MP_OTHER_LANGUAGE_URL Spanish https://www.nlm.nih.gov/medlineplus/spanish/caffeine.html MEDLINEPLUS
NCI_THESAURUS_CODE C328 PDQ
NDFRT_KIND DRUG_KIND NDFRT
NDFRT_KIND INGREDIENT_KIND NDFRT
NUI N0000006506 NDFRT
NUI N0000145919 NDFRT
ORIG_STY Drug/agent PDQ
PA D000697 MSH
PA D010726 MSH
PA D058915 MSH
PID 3846 PDQ
RN 3G6A5W338E MSH
RR 58-08-2 (Caffeine) MSH
RXAUI 2068741 RXNORM
RXAUI 2596591 RXNORM
RXAUI 2598487 RXNORM
RXAUI 2652742 RXNORM
RXAUI 3091170 RXNORM
RXAUI 3091945 RXNORM
RXAUI 3119797 RXNORM
RXAUI 3119798 RXNORM
RXAUI 3128917 RXNORM
RXAUI 3128919 RXNORM
RXAUI 57629 RXNORM
RXCUI 1886 RXNORM
SID APRD00673 DRUGBANK
SOS A xanthine, which is a mild central nervous system stimulant, vasodilator, and diuretic. Caffeine is found in coffee, chocolate, cola and some other soft drinks, and tea, in some cases with other xanthines, such as *BC4 theophylline* or theobromine. Caffeine use disorder and caffeine dependence are among the substance use disorders in ICD-10. Caffeine is a white, bitter, crystalline substance that has stimulant effects and constricts blood vessels in the brain. Toxic reactions to excessive caffeine consumption are manifold and include the following: dizziness, tremulousness, apprehension, nervousness, irritability, agitation, insomnia, diarrhea, headache, lightheadedness, breathlessness, hard breathing, reflex hyperexcitability, muscle twitching, excessive sensibility, ringing in ears, visual flashes of light, heart palpitations, rapidity of heart action, absence of heart rhythm, flushing, and hypotension. AOD
SOS Caffeine is found in coffee, chocolate, cola drinks, and tea, in some cases along with other xanthines. Acute or chronic overuse (e.g., a daily intake of 500 mg or more) with resultant toxicity is termed caffeinism. Symptoms include restlessness; insomnia; flushed face; muscle twitching; tachycardia; gastrointestinal disturbances including abdominal pain, pressured or rambling thought and speech, and sometimes exacerbation of pre-existing anxiety or panic states, depression, or schizophrenia. AOD
SOS The excessive ingestion of large amounts of caffeine, usually in coffee or tea, for prolonged periods is called caffeinism. This practice is a common lifestyle element among certain Canadian Indian groups (excessive strong tea consumption) (Farkas 1979) and certain types of white collar workers. Ingestion of 200 mg of caffeine daily (an average cup of tea contains about 65 mg of caffeine) can cause physiological problems and dosages in the 370 to 650 mg per day range are considered to be indicative of physiological and psychological dependence (Gilvert 1976; Grenden 1974). Classification: stimulants--secondary. (RIS 27:202--6 entries; coffee, RIS 27:204--2 entries) AOD
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SPL_SET_ID f988e6f2-1e5b-416b-8f2a-aa45a3207945 MTHSPL
SPL_SET_ID fa14aff4-2286-42c6-ab2c-054d2b1a188e MTHSPL
SPL_SET_ID fa88f437-830b-48bc-a44c-fd142963a150 MTHSPL
SPL_SET_ID fad1bfe3-13ee-4bcb-abb6-89082be3fbd9 MTHSPL
SPL_SET_ID fada26d2-f858-4916-8ebd-d28078a5b3cd MTHSPL
SPL_SET_ID faf741c4-bfc5-4f52-8773-c50f7b15dd08 MTHSPL
SPL_SET_ID fb6bca25-8d03-4fa5-a3a8-e595fe089a22 MTHSPL
SPL_SET_ID fbd287cf-a557-42ab-a530-9aee849c068d MTHSPL
SPL_SET_ID fbd2a03f-c9cd-4b0d-b9b1-aaa3bc14efb4 MTHSPL
SPL_SET_ID fbdd8197-60f3-4b48-9f36-809beed873c1 MTHSPL
SPL_SET_ID fd3cda41-e095-4811-8918-44356f1275f9 MTHSPL
SPL_SET_ID fe36dc63-673d-4466-b2d6-bada809bdf1c MTHSPL
SPL_SET_ID fef4844c-2b44-4e5c-9da3-e5b2214c9e8d MTHSPL
SPL_SET_ID ff348f48-352b-4f4c-8260-f412ef884213 MTHSPL
SUBSET_MEMBER 900000000000497000~MAPTARGET~c44.. SNOMEDCT_US
SUBSET_MEMBER 900000000000497000~MAPTARGET~X7953 SNOMEDCT_US
SUBSET_MEMBER 900000000000508004~ACCEPTABILITYID~900000000000548007 SNOMEDCT_US
SUBSET_MEMBER 900000000000508004~ACCEPTABILITYID~900000000000549004 SNOMEDCT_US
SUBSET_MEMBER 900000000000509007~ACCEPTABILITYID~900000000000548007 SNOMEDCT_US
SUBSET_MEMBER 900000000000509007~ACCEPTABILITYID~900000000000549004 SNOMEDCT_US
TERMUI T005984 MSH
TERMUI T005985 MSH
TH BAN (19XX) MSH
TH FDA SRS (2014) MSH
TH UNK (19XX) MSH
TH USAN (19XX) MSH
TH USP (19XX) MSH
TYPE_ID 900000000000003001 SNOMEDCT_US
TYPE_ID 900000000000013009 SNOMEDCT_US
Unit mg NCI
USDA_ID 262 NCI
VANDF_RECORD 50.416^130^Active/Master NDFRT
VANDF_RECORD 50.6^2584^Active/Master NDFRT
VUID 4017537 NDFRT

Additional Concept Data:  (none)

URL to Bookmark: https://ncim-stage.nci.nih.gov/ncimbrowser/ConceptReport.jsp?dictionary=NCI Metathesaurus&code=C0006644

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