Methylxanthines and Nootropics Flashcards
What are the top tea drinking nations?
Turkey
Ireland
UK
What are the top chocolate consuming nations?
Switzerland
Austria
Ireland
What are the top coffee drinking nations?
Finland
Norway
Iceland
How are new chemicals identified and characterized by pharmacological activity?
Extraction
Purification
Predictions
Characterization
What series of experiments should psychoactive chemicals pass?
Animal behavior
Physiological measures
Biochemical assays
What does caffeine metabolize into?
Theophylline, theobromine, paraxanthine
What do chlorogenic acids do?
Induce (phase 2 transferases) liver enzymes
What does dihydrocaffeic acid do?
It is anti-inflammatory with vascular benefits as it promotes NO production
What are kahweol and cafestol?
Diterpenes
What do kahweol and cafestol do?
Increase phase 2 enzymes, induce anti-stress genes, and elevates cholesterol
What are the most common anti-oxidant sources?
Coffee and tea
What is aminophylline?
Anti-asthmatic; treatment of COPD
What is IBMX
A bronchodilator
What is pentoxifylline used to treat?
Vascular disease and is fibrinolytic
What does propentofylline do?
It is neuroprotective
What are the medical indications for caffeine?
Respiratory stimulation in premature infants
Asthma = bronchodilator
Migraines = reduces cranial blood flow
What is the second more commonly prescribed NICU drug?
Caffeine
What is the most commonly consumed psychoactive substance?
Caffeine
Absorption of caffeine?
Ingestion
Absorbed in the small intestine
How long does it take the effects of caffeine absorption to peak?
45 minutes
How is caffeine distributed?
Amphipathic
Rapid
Widely distributed
How is caffeine metabolized?
By liver CYP1A2 via demethylation
Limited or no first-pass
What does paraxanthine do?
Increases blood glycerol/fatty acids via lipolysis
What does theobromine do?
Dilates vessels, increases urine volume
What does theophylline do?
Inhibits PDE, increases [cAMP], relaxes smooth muscle
How is caffeine excreted?
In the kidneys
What are the cellular drug actions of methylxanthines?
Non-selective adenosine receptor antagonist
Non-selective phosphodiesterase antagonist
Also targets Ca release, GABA receptors
ARs and PDE are ubiquitous
Which adenosine receptors play primary roles in caffeine effects?
A1 and A2a