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Fundamentals of Psychopharmacology
Matt Schalles UCSD Cognitive Science [email protected]
Drugs of Interest
l Psycho Stimulants l Dopamine l Caffeine l Adenosine l Opiates l Endorphins l Alcohol l Everything l Marijuana l Endocannabiniods
Serotonin like l Hallucinogens - Catecholamine like - - dissociative
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Neurotransmitters of Interest
Amino Acids Biogenic Amines Neuropeptides Glutamate (Glu) Quaternary Amines Opioid Peptides GABA Acetylcholine (Ach) Enkephalins Monoamines Endorphins Catecholamines Dynorphins Dopamine (DA) Endomorphins Norepinephrine (NE) Indolamines Serotonin (5-HT)
(Others: lipids & soluble gases)
Stimulant Drugs l Psychomotor Stimulants (Catecholamines)
- Cocaine - Methylphenidate (ritalin) - Amphetamines (adderall) l Cholinergic
- Nicotine l Adenosine
- caffeine
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Psychomotor stimulant kinetics
l Absorption l Half Lives
- Nasal membrane - Cocaine: 50-90 min
- stomach/intestinal - Methylphenidate: 3-4 hrs - Lungs - Amphetamines: 6-8 hrs - Bloodstream - Methamphetamine < 12 hr
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Cocaine/Methylphenidate site of action
Amphetamine Site of action
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Medical Uses
l Obesity l Narcolepsy l ADHD l Local anesthetics/ vasoconstrictors
Caffeine
l Adenosine Receptor
- Ligand released by astrocyte
- Inhibits neurons - Competitive antagonist
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Opiates
l Opium l Endogenous opioids
- Morphine - Endorphins - Codeine - Endomorphins - Enkephalins - Dynorphins
Opiate Kinetics
l Absorption l Excreted by
- stomach/intestines 20-30 kidneys min
- Nasal membranes 5-8 min
- Bloodstream 15-30 sec - Lungs 7-10 sec l Metabolism
- 3-5 hr half-life - Liver enzymes
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Opioid Distribution
l 3 receptor types
- Mu - Delta - Kappa
Site of Action
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Opioid Antagonists
l Naloxone l Naltrexone
- High mu receptor - Similar binding profile affinity - Orally active Must be injected - - 4 hr half-life Short action (15-30 - - Induces withdrawal min)
Alcohol – the dirtiest of drugs
l Interacts with
- Glutamate
- GABA - Dopamine - Opiates - Serotonin - endocannabinoids
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Pharmacokinetics
l Absorption l Eliminated through
- Lipid soluble - Urine - Water soluble - Skin Lungs l Metabolism - - feces - Zero order - First pass - Second pass - alcohol-dehydrogenase
Net Alcohol effects?
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EtOH Sites of Action
l GABA
- Direct agonist - Indirect agonist
Cannabinoids
l CB1 receptor
l Endocannabinoids
- 2-AG - anadamide
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Endocannabinoids
l Retrograde signaling
l Negative feedback mechanism
l Depolarization induced Suppression of Excitation
l DS inhibition
Hallucinogens
l Self Administration? l Psychedellics l Entheogens l Psychotomimetics
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Hallucinogens
l 3 Classes
- Serotonin-like - Catecholamine-like - Dissociative / Anesthetics
DMT
l Synthesized by mammals
l Dedicated Receptors in periphery
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Ayahuasca
Acetylcholine
st l 1 Neurotransmitter discovered
l 2 Receptors
- Nicotonic - Muscarinic
l Associated Functions
- Memory - Attention - Muscles
l Acetylcholine esterase
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Compounds Affecting Ach
l Nicotine l Amanita Muscaria l Crotoxin l Latrotoxin l Botulism
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