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Flashcards in Caffeine Deck (24)
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Caffeine Products

Soft Drinks
Ice Cream
Fortified Water


US Beverage Consumption

28- Soft Drink
18- Bottled Water
13- Beer
13- Milk
12- Coffee


Caffeine Intro

Most widely used stimulant
Over 80% of world drink daily
Coffee most prevalent form


Caffeine Pharmacokinetics

Rapidly and completely absorbed when consumed
Significant blood levels reached 30-45 min
Peak plasma levels in 90 minutes
Half Life 3.5-6 hours, but longer in infants, elderly, and pregnant women
Freely basses through blood brain barrier and placenta
Metabolized by liver enzymes
SSRIs are major inhibitors of these enzymes, so patients can have toxic reactions to high levels of caffeine


Caffeine Metabolism

Metabolized into theobromine, paraxanthine and theophylline
theobromine- Increases O2 flow
Paraxanthine- Increases fat breakdown to enhance athletic performance
Theophylline- Increases heart rate, open airways and improves concentration
Tobacco shortens caffeine half life,
quitters- caffeine can contribute to withdrawal symptoms as high levels of caffeine causes anxiety



Purine nucleotide
Plays role in energy transfer through ATP and ADP
Plays a neuromodulatory role in promoting sleep and suppressing arousal
Four known adenosine receptors, A1, A2A, A2B, A3 which are G protein coupled
Inhibitory effect on the CNS


Caffeine Mechanism of Action

Caffeine acts as an antagonist to adenosine receptors
Blocks adenosine from binding and having an effect on sleep
- Primary site are adenosine receptors on GABAergic neurons
Also influences dopaminergic, glutaminergic cholinergic and noradrenergic neurons
Does not result in DA release in nucleus accumbens, but does release it in prefrontal cortex
Causes arousal with profound reinforcing effects
Adenosine --> GABA --> Dopamine--> DA


Mild Dose- Caffeine

Brain Activity is increased- causing an alerting effect
Heart rate increase- both direct on the brain center and in heart
Breathing rate increases and smooth muscle relaxes- good for asthma
Constricts blood vessels in brain, but dilates vessels in peripheral system-- Brain blood flow is decreased
Increases "bad cholesterol" and LDL
Increases urine production and inhibits antidiuretic hormone
Oil, acids and caffeine irritate stomach lining
Mild analgesic


High Dose- Caffeine

Tremors, nausea, vomiting, irregular, or very rapid heart beat confusion
Panic attacks and seizures at very high doses


Physical Performance Caffeine

Slight enhancement of physical performance
Delays fatigue
However, excessive urination can cause dehydration
Increased heart rate can cause irregular arrhythmias


Caffeine Dependence and Withdrawal

Chronic use as little as 100 mg/day can cause withdrawal when use is abruptly ended
Headache, drowsiness, difficulty concentrating, impaired motor performance, and dysphoric mood all occur when consumption is stopped
Effects appear slowly and are maximum at 1-2 days


Energy Drink

Beverage that contains mild stimulant drug, most commonly caffeine
Also contains a sugar or sweetener


Abuse Potential- Energy Drink

Combination with alcoholic beverages is popular practice
Caffeine can make depressant effects of alcohol, but has no effects on alcohol metabolism
Mask sensory cues used to regulate drinking
- 3 times more likely to binge drink
- 2 times more likely to be sexually assaulted and drink and drive


Four Loko

Product containing alcohol, caffeine, taurine, guarana
Originally introduced as an "energy drink"-- ethical and legl implication of marketing to younger students
Masked the alcohol induced intoxication, thus causing individuals to black out
Resonsible for many hospitalizations on college campuses


MythBusting Caffeine

People metabolize caffeine at different rates- some fast, some slow
Drinking coffee does not make you sober- can cover some of the depressant effects
Coffee shops have different levels of caffeine in same drink-- temperature, bean composition, and acidity all play a role
Addictive for some individuals, abrupt abstinence can cause withdrawal symptoms- headache, fatigue, dysphoric mood
Does not increase the risk for cancer or heart disease



High concentration of theobromine
N-oleoylethanolamine and N-linoleoylethanolamine- two anadamide like molecules
Acts as antagonists, and increases the duration of action of natural anandamide


Health Benefits of Chocolate

Antioxidants in dark chocolate
Blood pressure reduced due to cocoa phenols


OTC Benefits

Benefits outweigh risks
Potential for abuse and misuse are low
Consumer can use them for self diagnosed conditions
Adequately labeled
Health Practitioners not needed for use of product


OTC Labels

Active/ Inactive Ingredients
Use/ Purpose
Directions/ Dose
Other information


OTC Abuse

Because OTC are unregulated, difficult to track abuse trends
Preparation with alcohol are most often abused
Mild stimulants in weight control, nasal decongestants, antihistamines, sleep aids, anti drowsy aids, antacids



- Used in cold/cough remedies
-Safe in prescribed doses
- 1 out of 10 teens abuse cough medication
- High produces a dissociative effect
- Binds to the same receptors as PCP
Physical symptoms include: confusion, dizziness, double vision, slurred speech, loss of coordination
- More dangerous if it is combined with other drugs


DXT Pharmacology

Morphinan class
Good cough suppresant
Antagonist on N-methyl D-Aspartate receptor
DXM and its metabolite dextrophan can produce a dissociative effect, not unlike ketamine and PCP



Active ingredient in nasal decongestant
Major ingredient in making clandestine methanphetamine
Retailers store decongestants with pseudophedrine behind the counter


Summary OTC

OTC drugs are not inherently safe, must read labels
Not all generic drugs exactly match prescription drugs- especially must be careful with extended release