Lecture 3: Regulatory Systems Flashcards
PHARMACODYNAMICS
DRUG ACTION
Neurotransmitter
a chemical used for neuron-to-neuron communication.
Stored in presynaptic neuron (synaptic vesicles)
Released into synaptic cleft
Neurotransmitters (NT) must bind to a receptor to produce an effect.
Termination of Neurotransmitters
Reuptake
Enzymatic Deactivation/degradation
Neuromodulator
a chemical that affects the neurotransmission of a whole group of neurons.
Ex, suboxone
PHARMACODYNAMICS and neurotransmitters - tolerance
Tolerance standpoint:
take cocaine. Neuron releases dopamine (neurotransmitter) to next neuron. Over time, body is like I want to protect you – we need to stop with all this dopamine. We can’t stop the neuron from firing, so we start breaking it down.
But if you take more, still too much dopamine.
So it creates more things to deactivate. If it can’t do that or that is not enough, it reduces dopamine receptors.
So then its harderf for your body to have dopamine at all (raises baseline)
Synaptic Transmission
= the process by which neurons communicate with each other and other cells in the nervous system.
Factors that affect synaptic transmission:
*Number of receptors on the post-synaptic neuron
*Properties of the receptors
*Neurotransmitter type
Most drugs affecting behavior affect…
Synaptic transmissions
Agonist
a molecule that by binding to the receptor stimulates a response = ↑ postsynaptic effects
Addictive drugs (heroin, morphine, oxycodone) stimulation leads to “high”
Antagonists
a molecule that by binding to a receptor blocks or inhibits the response = ↓ postsynaptic effects
Drugs like Naloxone and Naltrexone
Agonist vs antagonists
Agonists Activate (3 syllables) and/or remember
they “pick the lock”.
Antagonists evil villain
trying to block other
characters
Direct agonists
Mimics NT
Binds with and activates the receptor
e.g., nicotine and methadone
Direct antagonists
Receptor Blockers
Bind and block the receptor from being activated.
Sits on receptor and prevents ion channels from opening e.g., naltrexone
Indirect agonist
Attach to alternate binding site
Facilitates/stimulates receptors actions
e.g., Valium, Cocaine
Indirect antagonist
Attach to alternate binding site
*
Blocks/reduces the receptor actions
e.g., Reserpine
Non-Competitive
Indirect (antagonists and agonists)
Two types of primary neurotransmitters
Excitatory - Glutamate
Inhibitory - Gamma-aminobutyric acid (GABA)
- “On” & “Off” Switch in brain
- Impacting one impacts the other
Glutamate
Activation = ↑ brain firing
Main excitatory neurotransmitter in brain and spinal cord
Stored in vesicles and released from presynaptic neuron following an action potential.
Normal Conc. support
- Learning and memory
- Energy
- Brain communication
- Sleep/Wake cycles
- Pain signaling
methamphetamines, nicotine, caffeine, cocaine –> INCREASE glutamateG
GABA
Activation = SLOWED brain firing
Made from Glutamate precursors
Stored in vesicles and released from presynaptic neuron following an action potential.
Normal conc. Support:
- Reduced stress & anxiety
- Improved sleep
- Sedation/Relaxation
THINK: Benzodiazepines, opiates, alcohol, muscle relaxants (things with sedating effects)
Relationship between GABA and Glutamate
GABA made from Glutamate precursors
So it uses it up and you have less glutamate…
how it acts as a “stopper”
GABA agonists
GABA agonists - mimic GABA or enhance its activity, increase the inhibitory effect of GABA, thereby raising the seizure threshold.
(makes it less likely to have seizure when you are taking that substance…not worried about having a seizure when they are drunk…worried about when they are withdrawing from alcohol
Example: Benzodiazepines, Barbiturates, Alcohol
Too much = excessive sedation & thinking and memory problems
GABA antagonists
block GABA receptors, decrease inhibition, lowering the seizure threshold and potentially triggering seizures
because GABA is low…glutamate is high –> increawswe HR, etc. on clozapine
Examples: Clozapine (hence careful monitoring)
Body wants to achieve homeostasis =
tolerance & dependence
Seizure Thresholds with GABA & Glutamate Impacting Substances: Alcohol