Lecture 10: Caffeine and Nicotine Flashcards
Average caffeine content of coffee
100mg (50-150)
Potential energy drink caffeine content
320mg
how soon are significant blood levels of caffeine reached?
30-45 min
complete absorption time for caffeine
90 min
time of peak plasma level of caffeine
2 hours
half life of caffeine
6 hours (2.5-19)
what type of kinetics does caffeine have?
1st order
what enzyme metabolizes caffeine? where?
CYP-1A2, liver
caffeine ___ the ___ enzyjme, which is also responsible for metabolizing ___
induces, CYP-1A2, clozapine & olanzapine
genetic basis for slow vs. fast caffeine metabolizers?
isoenzyme differences in CYP-1A2
____ also induces CYP-1A2 enzyme
tobacco smoke
___ are potent CYP-1A2 inhibitors
SSRIs
caffeinism
severe anxiety reaction
3 things caffeine can help treat
asthma
narcolepsy
migraines
4 behavioral effects of low doses of caffeine
- mental alertness
- wakefulness
- reduced fatigue
- delicate muscular coordination hurt
5 harmful effects of heavy caffeine consumption
- agitation
- anxiety
- tremors
- rapid breathing
- insomnia
lethal dose of caffeine
10 g (100 cups)
french press coffee increases___
blood cholesterol levels and increased risk of coronary artery diseases
2 peripheral effects of caffeine
- increases cardiac contractility and cardiac output
2. dilates coronary arteries, providing more oxygen to heart
5 pharmacological effects of caffeine
- constricts cerebral blood vessels (30% less blood flow to brain)
- anti asthmatic
- increased gastric acid secretion
- increased urine
- lowers risk of type ii diabetes (possibly weight loss)
caffeine is a ___. how does it work?
adenosine receptor antagonist
blocks adenosine effect (adenosine levels rise throughout day promoting sleep). adenosine stimulates GABA neurons
caffeine indirectly stimulates ___. where?
dopaminergic activity
PFC
pregnant women who drank 8+ cups a day had increased risk of ___
stillbirth
reasonable doses of caffeine in pregnant women can cause ___
modest fetal growth restriction
8 withdrawal effects of caffine
- headache
- tiredness
- lack of concentration
- anxiety
- irritability
- increased muscle tension
- depression
- nausea
when does caffeine withdrawal start? peak?
12-24 hours; 20-48 hours
psychiatrically ill nicotine dependent people consume ___ of all cigarettes smoked
70%
nonsmokers live ___ longer than heavy smokers
10 years
___ of all people who have ever smoked have quit
1 million
where is nicotine absorbed?
- lungs
- mucosa
- skin
- GI tract
how is nicotine from cigarettes distributed?
suspended in tars; rapidly absorbed into and satures bloodstream; blood to brain saturated with nicotine, accounting for rush
nicotine is metabolized by ___
CYP-2A6
companies have increased smoke nicotine yield by ___ over the past 7 years
11%
primary metabolite of nicotine
continine
what causes fluid retention in nicotine?
stimulation of hypothalamus, releasing antidiuretic hormone
what leads to muscle relaxation in nicotine?
reduces activity of afferent nerve fibers coming from muscles
how does nicotine lead to weight loss?
reduction in appetite; altered taste bud sensitivity
exposure to cues related to cig smoking increase activation in (3)
PFC, OFC, anterior insula
damage to what area leads to ability to easily quit smoking?
insula
nicotine’s reinforcing action
activation of midbrain DA neurons
what is the effect of nicotine on atherosclerotic coronary arteries?
cannot dilate; leads to angina or heart attack due to cardiac ischemia (lack of oxygen)
4 effects of nicotine on body
- increase heart rate
- increase blood pressure
- increase cardiac contractility
- initiates vasodilation (increases blood flow to meet increased oxygen demand of heart)
almost all effects of nicotine achieved by activating ___
nicotinic receptors
4 nicotinic receptor effects on PNS
- increased bp
- increased hr
- epinephrine release from adrenal glands
- increased GI tract activity
where are nicotinic receptors located in CNS? (3)
presynaptic nerve terminals of 1. DA 2. ACh 3. glutamate secreting neurons
nicotine DA release increases in (2), leading to (4)
- NA
- forebrain
- behavioral reinforcement
- stimulant
- antidepressant
- addictive properties
nicotine ACh increase contributes to (2)
- cognitive potentiation
2. memory facilitation
nicotine glu increase contributes to ___
memory
nicotine may delay onset of ___
cognitive deficits in alzheimers
___ americans die per year as consequence of nicotine addiction
400,000
9 symptoms of nicotine withdrawal
- craving
- irritability
- anxiety
- anger
- concentration probs
- restlessness
- impatience
- increased appetite/weight gain
- insomnia
a person who smokes 2 packs a day for 20 years loses…
13-14 years of life
total economic toll due to nicotine
$157 bn
carbon monoxide in smoke can __
decrease amount of oxygen to heart
what can smoking due to coronary arteries?
increased incidence of atherosclerosis (narrowing) and thrombosis (clotting)
smoking greatly increases risk of ___ in lungs
emphysema
chronic obstructure pulmonary disease
is nicotine carcinogenic?
no, but may promote tumor growth
3 effects of smoking during pregnancy
- small fetus or preterm birth
- asthma
- reduces oxygen delivery to fetus, causing fetal hypoxia
how does varenicline work?
partial nicotine receptor agonist
nicotine patches ___ rate of long term smoking cessation
double
nicotine gum increases cessation rate by ___
50-70%
compliance is highest for ___
patch, gum, inhaler/nasal spray
wellbutrin and nortripyline ___ chance of quitting
double
are SSRIs effective for quitting smoking?
no
what is strattera?
NE reuptake inhibitor, reduces cravings
is chantix or wellbutrin more effective in quitting?
chantix
how does chantix work to reduce smoking?
- reduces withdrawal
- low level release of dopamine
- blocks nicotine’s access toreceptors
side effects of chantix
- nausea
- depression
- agitation
- suicide
how do anti nicotine vaccines work?
induce sufficient antibodies to sequester nicotine and keep it from entering brain, but effective only in people who produce high levels of antibodies