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Drug effects
the observable changes in a person’s physiological processes and behavior due to a drug
Sites of action
where molecules of drugs interact with cells of the body
the steps of Pharmakinetics
drugs are absorbed
drugs are distributed throughout the body
drugs are metabolized
drugs are excreted
Ways drugs can be absorbed
IV injection
IP injection
IM injection
SC injection
Oral
Sublingual administration
inhalation
topical
ICV administration
What is drug absorbtion?
The drug is put into the body and absorbed though tissues
What is drug distribution?
Drug is distributed throughout body and blood
What is drug metabolism?
When the drug is changed to an inactive form by the enzymes, usually in the liver
What is drug excretion?
When the drug is excreted by the kidneys
What determines how fast the drug reaches the site of action?
How soluble the lipid is and can pass through cell membranes
How can drug effectiveness be measured?
Using a dose response curve to map the effects of the drug based on the dose
Why do drugs vary in their effectiveness?
Different drugs have different sites of action
Vary in how well they bind to binding sites
What happens when drugs are used repeatedly?
Tolerance (effects are diminished, need a higher dose)
Sensitization (effects increase)
Withdrawal (opposite effect of the drug, physical dependence)
What is a placebo?
An inactive substance that can effect patients. When patients expect it to have an effect and it does that is the placebo effect
Antagonists
block postsynaptic effects by preventing neurotransmitters from being released
agonists
facilitate postsynaptic effects by increasing the amount of neurotransmitter being released
Glutamate
In the CNS, excitatory
GABA
CNS, inhibitory
Acetylcholine (ACh)
In the CNS: learning, memory, REM sleep
In the PNS: Muscle contraction
Dopamine
CNS, voluntary movement, attention, learning, reinforcement, planning, problem solving
Norepinephrine/Epinephrine
CNS: vigilance
PNS: ANS regulation (heart rate, blood pressure, etc)
Serotonin
CNS: mood regulation, eating, sleeping, dreaming, arousal, impulse control
PNS: digestive system
Histamine
CNS: wakefulness
PNS: Immune response
Opioids
CNS: reinforcement, pain modulation
PNS: pain modulation
Endocannabinoids
CNS: appetite regulation
PNS: immune response
Describe the system of glutamate transport
Glutamate is put into vesicles by the vesicle glutamate transporter
binds to AMPA, NMDA, kainate, and metabotropic glutamate receptors
Metabolized by the enzyme glutamate synthase
Transported into the presynaptic cell by excitatory amino acid transporter
Describe the system of GABA transport
GABA is packaged into vesicles by the vesicle transporter
binds to GABA receptors like the GABAa receptor
metabolized by GABA aminotransferase
Transported into the presynaptic cell by GABA transporters
Describe the ACh system
ACh neurons are organized into three pathways in the brain
Synthesized by choline acetyltransferase
Packaged into vesicles by ACh transporter
Metabolized by acetylcholinestrase
Transported by choline transporters to the presynaptic cell
What are the monoamines?
Classic neurotransmitters such as dopamine, norepinephrine, epinephrine, serotonin, and histamine
Describe the system of monoamine transport
Sythesized from amino acid precursors
loaded onto vesicles by vesicle monoamine transporters
released after an action potential
Bind to ionotropic and metabotropic receptors
Metabolized by enzymes
Reuptake transporters remove monoamines from the synapse
What is special about peptide neurotransmitters?
Synthisized from large polypeptides, can be either neurotransmitters or neuromodulators depending on the sensitivity of the receptors to the neurotransmitters released at the same time
What is the lipid neurotransmitter system?
Synthesized on demand and not stored in vesicles
Endocannabinoids bind to CB1 and CB2 receptors
Anandamide is deactivated by FAAH in the presynaptic neuron and its transporter does reuptake in the presynaptic cell
