Caffeine is a bitter, white crystalline xanthine alkaloid that is a psychoactive stimulant drug. More than 60 plants produce Caffeine. Caffeine is found naturally in coffee, tea, and chocolate. Colas and some other soft drinks also contain it. Caffeine also comes in tablet and capsule forms. Some pain relievers and medicines for migraine headaches also contain caffeine. It is said to be most widely used drug in the world. It is soluble in water and many organic solvents, and it appears in pure form as white crystals. Caffeine affects the central nervous system by binding to adenosine receptors in the brain, thereby inhibiting the sleeppromoting actions of adenosine that normally increase with prolonged wakefulness. Its chemical name is 1,3,7-trimethylxanthine.






There is no doubt that human beings have consistently consumed caffeine since the Stone Age. It is hypothesized that ancient people discovered that chewing on certain plants had stimulating effects on the body and mind. The Ethiopian myth describes the story of a goatherd named Kaldi, whose goats nibbled on a bush covered in red berries. After the goats had consumed the berries, they became frisky and started to dance on their hind legs. Kaldi was intrigued by the strange actions of his goats and decided to try the berries for himself. After tasting the magical berries he too became energized and started to dance with his goats. A local monk noticed the goatherd¶s behavior, and came to the realization that the invigorating effects of this bean could help monks remain alert and awake during long religious sessions of prayer. It was then that the

monk brewed the first cup of coffee. The consumption of coffee spread across northern Africa, and then into Arabia. And by the sixteenth century, coffee had become a staple throughout the Arab world and was considered to be as important as bread or water. Caffeine was first isolated by the German chemist Friedrich Ferdinand Runge in 1819.Much of the work leading to the full characterization of caffeine's molecular structure was completed by the German chemist Emil Fischer (1852-1919). Fischer first synthesized the compound from materials in 1895, and two years later derived its precise structural formula. 


Caffeine is thought to act on the brain by blocking adenosine receptors. Adenosine, when bound to receptors of nerve cells, slows down nerve cell activity; this happens, among other times, during sleep. The caffeine molecule, being similar to adenosine, binds to the same receptors but doesn't cause the cells to slow down; instead, the caffeine blocks the receptors and thereby the adenosine action. So the main action of caffeine is to block adenosine receptors. The resulting increased nerve activity causes the release of the hormone epinephrine (adrenaline), which in turn leads to several effects such as higher heart rate, increased blood pressure, increased blood flow to muscles, decreased blood flow to the skin and inner organs, and release of glucose by the liver. In addition, caffeine increases the levels of the neurotransmitter dopamine in the brain. 

Caffeine is quickly and completely removed from the brain and, unlike other CNS stimulants or alcohol, its effects are short lived.


What happens when you drink coffee or an energy drink like Red Bull??? Let's take a look.

In the images above, you can see that caffeine molecules attach to adenosine receptors on the nerve endings. Because caffeine blocks the receptors, the nerves can't get adenosine, which causes neurons in the brain to fire 

And here you can see that the pituitary gland senses the increased neuron activity in the brain and releases adrenaline into the body. The adrenal glands pump adrenaline throughout the body, making the heart beat faster and the liver release extra sugar for energy.

Caffeine Metabolism
Caffeine is metabolized (demethylated) in the liver by CYtochrome P450 enzymes known as 1A2 (or CYP1A2). The first products of metabolism are all dimethylxanthines 1.Paraxanthine (1,7-dimethylxanthine) 2.Theobromine ( 3,7-dimethylxanthine) raw and 3.Theophylline (1,3-dimethylxanthine). 

Paraxanthine has the effect of increasing lipolysis(break down of lipid), leading to elevated glycerol and free fatty acid levels in the blood plasma. Theophylline relaxes smooth muscles of the bronchi ² and has been used for this purpose in the treatment of asthma. Theobromine is a diuretic (increases urine production) that can dilate blood vessels and reduce blood pressure Each of these metabolites is further metabolized and then excreted in the urine. The half-life for caffeine metabolism is typically 5-6 hours in an adult.

Caffeine was first isolated in 1819 by the French chemist Pierre Jean Robiquet, from coffee. In its pure state it is an intensely bitter white powder. Caffeine acts as a stimulant of the central nervous system, cardiac muscle and respiratory system as well as a diuretic. As such, it is found to delay fatigue. Caffeine can be isolated directly from tea leaves.The chief problem with isolation is that caffeine does not exist alone in tea leaves but is accompanied by other natural substances from which it must be separated. Caffeine constitutes as much as 5% by weight of the leaf material in tea plants and is water soluble. Unfortunately, Tannins in the tea leaf are also water soluble. Fortunately, Caffeine is soluble in non-polar organic solvents whereas the Tannins are not. Thus, we can carry-out the isolation of caffeine from tea leaves in the following steps

STEPS 1.Take 100ml of boiling water and add 4-6 tea bags into it to make it concentrated. More concentrated solution is preferred. It is then followed by filteration.
2. To a clean 500 mL conical flask, add this 100 mL of tea extract prepared in step 1 into it. 3. Add approximately two grams of sodium carbonate (NaCO3) to this tea/coffee solution. This is to convert Tannins to Phenoxides, which will remain in the aqueous phase during extraction of the caffeine. Phenolic Tannins + Sodium Carbonate Sodium Phenoxides

4. Add 25 mL of methylene chloride (CH2Cl2), and vigorously swirl the mixture for 10 minutes so that caffeine can dissolve in to it. 5. Allow the mixture to stand until 2 layers forms in the flask =>a dark aqueous top layer and =>a clear methylene chloride bottom layer.

6. Carefully pour off into a beaker, as much of the top layer as you can, without removing the bottom layer. This process is called decanting. 7. Place a fluted filter paper in a long stem glass funnel. Put the funnel in a small iron ring and suspend it over a 250 mL flask. 8. Slowly and carefully pour the methylene chloride/water mixture into the fluted filter paper. The excess water will drain through and the methylene chloride solution of caffeine will remain on the filter paper. 9. Using a pipette, transfer the methylene chloride solution to a 50 mL conical flask. To this solution, add a scoop of anhydrous sodium sulfate (Na2SO4), in order to remove the last traces of water. 10.While the solution is drying, weigh a 50 mL beaker to the 0.001 g on a balance. Record this reading. nearest

11.Using a pipette, transfer the dried solution to the tared (empty beaker. 12.Evaporate most of the methylene chloride on a warm hot plate. When only a fraction of a milliliter of liquid is left, remove the beaker from the hot plate. Allow the beaker to stand for a minute or two.The heat remaining in the glass will cause the last amount of methylene chloride to evaporate and produce a solid residue of crude caffeine. 13. In order to determine your recovery of caffeine, reweigh the cool beaker and record this mass. 14. Pure caffeine is a white solid.

Side Effects of Caffeine Consumption
In large doses and usually over a period of time, consumption of caffeine (less than 600 mg/day) present in tea and coffee can trigger "caffeinism". The condition in turn is characterized by not only an excessive caffeine addiction but also mental and physical conditions like anxiety, restlessness, irritability, muscle twitching and caffeine induced sleep disorders. In fact, the negative effects of caffeine on the body include anxiety and panic attacks and may also result in heart palpitations. It has also been reported that chronic, heavy caffeine ingestion may be associated with depression, dizziness, headaches and impotence in men.

Gastrointestinal Side Effects: Gastrointestinal side effects associated with caffeine include gastrointestinal distress, constipation, diarrhea, nausea, vomiting and cramping after consuming caffeine. Psychiatric and Nervous System Effects: Psychiatric side effects have included confusion and psychotic symptoms such as anxiety, light depression and fatigue. The side effects on the nervous system associated with caffeine consumption include central nervous system stimulation such as nervousness, irritability, restlessness, and a jittery feeling. Cardiovascular Side Effects: The most common cardiovascular side effect or caffeine side effect on the heart includes an increased heartbeat and heart rate along with an elevated blood pressure. Research has also qualified the effect of caffeine in exerting an acute unfavorable effect on aortic stiffness in treated hypertensive patients. To know more about the effects on blood pressure read more on effects of caffeine on blood pressure. Endocrine Side Effects: A decrease in insulin sensitivity in individuals was observed following excessive caffeine consumption. The mechanism leads to elevated serum epinephrine levels.

Renal Side Effects: Excessive caffeine consumption results in increased urine flow and sodium and calcium excretion. Caffeine and Pregnancy: Studies have also shown that excessive caffeine during pregnancy may lead to increased chances of a miscarriage. In addition to that caffeine causes constricted blood vessels of the placenta, leading to reduced blood flow. Also, caffeine may directly affect the developing cells of the baby as it crosses the placenta. Like adults, caffeine side effects in children include obesity and weight gain, dehydration, jitteriness, upset stomach, nervousness and difficulty in concentrating and sleeping. However, a sudden withdrawal from caffeine can trigger certain caffeine withdrawal symptoms like cravings, apathy, constipation and throbbing pressure headaches. So the best course of action in this case would be to limit caffeine intake. When consumed in moderation, caffeine speeds up our metabolism and also increases the breakdown of fat thus freeing fatty acids, which are used in energy production during exercise. It can also increase stamina and help in fighting diseases like diabetes and Parkinson's disease.

Decaffeination is the act of removing caffeine from coffee beans, cocoa, tea leaves and other caffeine-containing materials. Despite removal of caffeine, many decaffeinated drinks still have around 1-2% of the original caffeine remaining in them. 


Boiling point: 178 °C Melting point: 238 °C Density: 1.2 g/cm³ Volatility: 0.5% Vapor pressure: 101 Kpa @ 178 °C PH: 6.9 (1% solution) Solubility in water: 2.17% Vapour density: 6.7 g/m³ Molecular weight: 194.19 g/mol 

Molecular Formula: C8 H10 N4 O2

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