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Caffeine

Uses of Caffeine: – Used for prevention and treatment of bronchopulmonary dysplasia in premature infants – Improproves weight gain, reduces cerebral palsy incidence, and treats […]

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Uses of Caffeine:
– Used for prevention and treatment of bronchopulmonary dysplasia in premature infants
– Improproves weight gain, reduces cerebral palsy incidence, and treats apnea of prematurity
– Primary treatment for orthostatic hypotension and some use for asthma

Performance Enhancement with Caffeine:
– Reduces fatigue, improves reaction time, wakefulness, concentration, and motor coordination
– Effects vary based on body size and tolerance
– Enhances physical performance in aerobic and anaerobic conditions

Health Effects and Safety of Caffeine:
– Treats bronchopulmonary dysplasia and apnea of prematurity
– May have protective effects against diseases like Parkinson’s
– Caffeine can lead to mild drug dependence and withdrawal symptoms

Regulation, Populations, and Physiological Effects:
– Widely consumed and classified as generally safe by the US FDA
– Recommended daily intake limits for different populations
– Physiological effects on gastrointestinal motility, bone loss, and urine output

Psychological Effects, Addiction, and Interactions:
– Psychological effects like anxiety, insomnia, and reduced coordination
– Discontinuing caffeine can reduce anxiety for some individuals
– Interactions with substances like alcohol, tobacco, and medications

Caffeine (Wikipedia)

Caffeine is a central nervous system (CNS) stimulant of the methylxanthine class. It is mainly used as a eugeroic (wakefulness promoter) or as a mild cognitive enhancer to increase alertness and attentional performance. Caffeine acts by blocking binding of adenosine to the adenosine A1 receptor, which enhances release of the neurotransmitter acetylcholine. Caffeine has a three-dimensional structure similar to that of adenosine, which allows it to bind and block its receptors. Caffeine also increases cyclic AMP levels through nonselective inhibition of phosphodiesterase.

Caffeine
2D structure of caffeine
3D structure of caffeine
Clinical data
Pronunciation/kæˈfn, ˈkæfn/
Other namesGuaranine
Methyltheobromine
1,3,7-Trimethylxanthine
7-methyltheophylline Theine
AHFS/Drugs.comMonograph
License data
Pregnancy
category
  • AU: A
Dependence
liability
Physical: Moderate 13% and variable low–high 10-73%
Psychological: Low–moderate
Addiction
liability
Relatively low: 9%
Routes of
administration
Common: By mouth Medical: intravenous
Uncommon: insufflation, enema, rectal, transdermal, topical
Drug classStimulant
Adenosinergic
Eugeroic
Nootropic
Anxiogenic
Analeptic
Anorectic
Parasympathomimetic
Cholinesterase inhibitor
Phosphodiesterase inhibitor
Diuretic
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability99%
Protein binding10–36%
MetabolismPrimary: CYP1A2
Minor: CYP2E1, CYP3A4,
CYP2C8, CYP2C9
MetabolitesParaxanthine 84%
Theobromine 12%
Theophylline 4%
Onset of action45 minutes–1 hour
Elimination half-lifeAdults: 3–7 hours
Infants (full term): 8 hours
Infants (premature): 100 hours
Duration of action3–4 hours
ExcretionUrine (100%)
Identifiers
  • 1,3,7-Trimethyl-3,7-dihydro-1H-purine-2,6-dione
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
PDB ligand
CompTox Dashboard (EPA)
ECHA InfoCard100.000.329 Edit this at Wikidata
Chemical and physical data
FormulaC8H10N4O2
Molar mass194.194 g·mol−1
3D model (JSmol)
Density1.23 g/cm3
Melting point235 to 238 °C (455 to 460 °F) (anhydrous)
  • CN1C=NC2=C1C(=O)N(C(=O)N2C)C
  • InChI=1S/C8H10N4O2/c1-10-4-9-6-5(10)7(13)12(3)8(14)11(6)2/h4H,1-3H3
  • Key:RYYVLZVUVIJVGH-UHFFFAOYSA-N
Data page
Caffeine (data page)

Caffeine is a bitter, white crystalline purine, a methylxanthine alkaloid, and is chemically related to the adenine and guanine bases of deoxyribonucleic acid (DNA) and ribonucleic acid (RNA). It is found in the seeds, fruits, nuts, or leaves of a number of plants native to Africa, East Asia and South America, and helps to protect them against herbivores and from competition by preventing the germination of nearby seeds, as well as encouraging consumption by select animals such as honey bees. The best-known source of caffeine is the coffee bean, the seed of the Coffea plant. People may drink beverages containing caffeine to relieve or prevent drowsiness and to improve cognitive performance. To make these drinks, caffeine is extracted by steeping the plant product in water, a process called infusion. Caffeine-containing drinks, such as coffee, tea, and cola, are consumed globally in high volumes. In 2020, almost 10 million tonnes of coffee beans were consumed globally. Caffeine is the world's most widely consumed psychoactive drug. Unlike most other psychoactive substances, caffeine remains largely unregulated and legal in nearly all parts of the world. Caffeine is also an outlier as its use is seen as socially acceptable in most cultures and even encouraged in others.

Caffeine has both positive and negative health effects. It can treat and prevent the premature infant breathing disorders bronchopulmonary dysplasia of prematurity and apnea of prematurity. Caffeine citrate is on the WHO Model List of Essential Medicines. It may confer a modest protective effect against some diseases, including Parkinson's disease. Some people experience sleep disruption or anxiety if they consume caffeine, but others show little disturbance. Evidence of a risk during pregnancy is equivocal; some authorities recommend that pregnant women limit caffeine to the equivalent of two cups of coffee per day or less. Caffeine can produce a mild form of drug dependence – associated with withdrawal symptoms such as sleepiness, headache, and irritability – when an individual stops using caffeine after repeated daily intake. Tolerance to the autonomic effects of increased blood pressure and heart rate, and increased urine output, develops with chronic use (i.e., these symptoms become less pronounced or do not occur following consistent use).

Caffeine is classified by the US Food and Drug Administration as generally recognized as safe. Toxic doses, over 10 grams per day for an adult, are much higher than the typical dose of under 500 milligrams per day. The European Food Safety Authority reported that up to 400 mg of caffeine per day (around 5.7 mg/kg of body mass per day) does not raise safety concerns for non-pregnant adults, while intakes up to 200 mg per day for pregnant and lactating women do not raise safety concerns for the fetus or the breast-fed infants. A cup of coffee contains 80–175 mg of caffeine, depending on what "bean" (seed) is used, how it is roasted, and how it is prepared (e.g., drip, percolation, or espresso). Thus it requires roughly 50–100 ordinary cups of coffee to reach the toxic dose. However, pure powdered caffeine, which is available as a dietary supplement, can be lethal in tablespoon-sized amounts.

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