Post Mid-2 Flashcards
Coffee is a ___ preparation, an infusion of complex ___ from a ___ __
Coffee is a botanical preparation, an infusion of complex chemicals from a plant fruit
How are new chemicals from a plant source identified and characterized for pharmacological activity?
- extraction
- purification
- predictions about which chemical we are going to investigate
- characterization
What series of experiments should psychoactive chemicals pass in order to understand the potential addictiveness of a drug?
- animal behaviour e.g. lever presses- drug seeking
- physiological measures
- biochemical assays
Methylxantines resemble a ___ (-rgic) base like __ and ___
Methylxantines resemble a purine (-rgic) base like adenosine and guanine
When people drink coffee, caffeine is metabolized into 3 other methylxantines which are…
1) Theophylline (4%)
2) Theobromine (12%)
3) Paraxanthine (84%)
___ acid induce phase II transferases like GST and other liver enzymes
Chlorogenic acid induce phase II transferases like GST and other liver enzymes
____ acid has anti-inflammatory properties on its own and it also promotes vascular health by increasing NO production
dihydrocaffeic acid has anti-inflammatory properties on its own and it also promotes vascular health by increasing NO production
___ and ___ are diterpenes. They increase phase II enzymes, they induce anti-stress genes (antioxidant) but elevate cholesterol
Kahewol and cafestol are diterpenes. They increase phase II enzymes, they induce anti-stress genes (antioxidant) but elevate cholesterol
___ and ___ are the most common anti-oxidant sources
coffee and tea are the most common anti-oxidant sources
Caffeine is a ___ stimulant in ___ infants, ___ most commonly prescribed ___ drug after antibiotics.
It functions by inhibiting ___ which increases concentration of cAMP within ___ neurons, creating a ___ ___ in those cells.
Promotes ___ and ___ ___ in babies
Caffeine is a respiratory stimulant in premature infants, 2nd most commonly prescribed NICU drug after antibiotics.
It functions by inhibiting PDE4 which increases concentration of cAMP within preBotC neurons, creating a robust rhythm in those cells.
Promotes breathing and blood oxygenation in babies
Caffeine is also used in ___ because it is a bronchodilator
Caffeine is also used in asthma because it is a bronchodilator
Caffeine can be used to treat ___ in certain cases because it reduces cranial blood flow
Caffeine can be used to treat migraines in certain cases because it reduces cranial blood flow
___ is the most commonly consumed psychoactive substance on the planet
Caffeine is the most commonly consumed psychoactive substance on the planet
Absorption of caffeine
- ingestion
- small intestine is where absorption occurs
- 45 min to peak
Distribution of caffeine
- amphipathic
- rapid and widely distributed- penetrates brain tissue
Metabolism of caffeine
- limited or no first-pass metabolism
- CYP1A2 (demethylation reactions)
- paraxanthine: will increase blood glycerol/fatty acid via lipolysis
- theobromine: dilate vessels, increase urine volume- makes caffeine a diuretic
- theophylline: inhibit PDE, increases concentration of cAMP, relaxes smooth muscle
Caffeine is excreted through the __
kidneys
Caffeine also effects ___ release and ___ receptors
Caffeine also effects Ca release and GABA receptors
AR (adenosine receptor) and PDE (phosphodiesterase) are ___ (expressed everywhere in body)
AR (adenosine receptor) and PDE (phosphodiesterase) are ubiquitous (expressed everywhere in body)
Caffeine will antagonize all 3 major types of ___ .
There are 4 main sub-types of __: ___, ___, ___ and ___
___ and ___ play primary roles in caffeine effects. They are mostly pre-synaptic receptors that limit neurotransmitter release
Caffeine will antagonize all 3 major types of ARs (adenosine receptors).
There are 4 main sub-types of AR: A1, A2a, A2b and A3
A1 and A2a play primary roles in caffeine effects. They are mostly pre-synaptic receptors that limit neurotransmitter release
A1 will inhibit ___ ___ and reduce cAMP levels. It will reduce ___ release, because of how neurons are wired that undergo these cellular effects it can lead to increase ___ release
A1 will inhibit adenylyl cyclase and reduce cAMP levels. It will reduce NT release, because of how neurons are wired that undergo these cellular effects it can lead to increase NT release
___ will exist as pairs at rest or after they are triggered by adenosine or some other endogenous ligand. They will come together to form an active receptor complex
AR (adenosine receptors) will exist as pairs at rest or after they are triggered by adenosine or some other endogenous ligand. They will come together to form an active receptor complex
Not only can AR pair with other AR but they can dock onto ___ ___ to form active signalling complexes e.g. 2A2a + 2D2
Not only can AR pair with other AR but they can dock onto dopamine receptors to form active signalling complexes e.g. 2A2a + 2D2
Effects of caffeine on brain
- alertness, arousal, and focus
- enhanced mood, confidence and sociability
- high doses can cause anxiety
- reduced blood flow to brain
- sleep inhibited