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Psychopharmacology
Psychopharmacology
Drug
Medication? Heroin or cocaine? An exogenous chemical not necessary for normal cellular functioning that significantly alters the function of certain cells of the body when taken in relatively low doses
Drug effect
Changes of physiological process and behavior
Site of action
May only have effect on certain neurons at certain locations
Routes of administration
Intravenous (IV), vein Intraperitoneal (IP) injection, abdominal wall Intramuscular (IM) injection Subcutaneous (SC) injection, beneath the skin Oral administration Sublingual administration, beneath the tongue Intrarectal administration Inhalation, lung Topical administration, absorbed by skin Intracerebral administration Intracerebroventricular (ICV) administration
Depot binding
Binding of a drug with various tissues of the body or with protein in the blood
Albumin
A protein found in the blood; serves to transport free fatty acids and can bind with some lipidsoluble drugs
Tolerance
A decrease in the effectiveness of a drug that is administered repeatedly
Withdrawal symptoms
Sensitization
An increase in the effectiveness of a drug that is administered repeatedly
Placebo effects
An inerr substance that is given to an organism lieu of a physiologically active drug; used experimentally to control for the effects of more administration of a drug
Antagonists
A drug that opposes or inhibits the effects of a particular neurotransmitter on the postsynaptic cell
Agonists
A drug that facilitates the effects of a particular neurotransmitter on the postsynaptic cell
Competitive binding: binding of a drug to a site on a receptor interferes with the site for the principal ligand
Direct agonist
A drug that binds with and activates a receptor
Noncompetitive binding: Binding of a drug to a site on a receptor; does not interfere with the binding site for the principal ligand
Indirect antagonist
A drug that attaches to a binding site on a receptor and facilitates the action of the receptor; does not interfere with the binding site for the principal ligand
Presynaptic heteroreceptor
A receptor located in the membrane of a terminal button that receives input from another reminal button by means of an axoaxonic synapse; binds with the neurotransmitter released by the presynaptic terminal button
Acetylcholine
Acetycholinesterase (AChE)
Muscarinic receptor
Metabotropic, slow, dominant in CNS
+ + +
Muscle paralysis
stimulate
block
hemicholinium
deactivate
neostigmine
Stimulate nicotinic receptors Block nicotinic receptors Stimulate muscarinic receptors Block muscarinic receptors
nicotine
curare
+ -
Muscarine
atropine
Monoamine
Classification
Catecholamine
Dopamine, Norepinephrine, Epinephrine Catecholamine Synthesis
L-DOPA---Dopamine--Norepinephrine (NE)
Indolamines
Serotonin
Dopamine
Both excitatory and inhibitory
1. Nigrostriatal system substantia nigra to caudate nucleus and putamen control of movement (Parkinsons disease) 2. Mesolimbic system ventral tegmental area to limbic system (amygdala and hippocampus) reinforcing and rewarding (drug addiction) 3. Mesocortical system ventral tegmental area to prefrontal cortexshortterm memory, planning and strategy.
Receptors, D1 and D2
+ +
inhibit
AMPT
inhibit
reserpine
activate
Postsynaptic receptor
activate
inhibit
+ +
Reuptake
inhibit
Stimulate release
destroy
Norepinephrine (NE)
Autonomic nervous system Final step of synthesis: Domapine norepinephrine occurs inside the vesicles Release through axonal varicosities rather than terminal buttons Originating site: Locus coeruleus in dorsal pons increase in vigilance All adrenergic receptors are metabotropic, 1, 2, 1, 2 Both excitatory and inhibitory effects.
+ +
Same with Dopamine
block
moclobemide
block
idazoxan
inhibit
reserpine
inhibit
Amphetamine MDMA
Serotonin
Mood, eating, sleep, arousal, pain, dreaming Originated from Raphe nuclei and projects to basal ganglia and hippocampal formation Released from varicosities rather than terminal buttons At least 9 types of receptors
+ + + +
inhibit
fenfluramine
inhibit
MDMA
Stimulate releasing
synthesis
inhibit
PCPA
Receptor
stimulate
LSD
Storage in vesicles
inhibit
reserpine
Amino Acids
The most common neurotransmitters in CNS
Glutamate (direct excitatory in brain and spinal cord) Gamma-aminobutyric acid (GABA) (direct inhibitory in the brain) Glycine (direct inhibitory in spinal cord)
Glutamate
Four major receptors Ionotropic
NMDA receptor AMPA receptor Kainate receptor
Metabotropic receptor
Metabotropic glutamate receptor
Modulations
Zinc ion (-) Polyamine (+) PCP (-)
+ + + -
Kainate acid
NMDA
AP5
GABA receptor
5 binding sites Stimulating:
barbiturate, Steroid site, Benzodiazopine Picrotoxin
Inhibiting:
Ionotropic receptor or metabotropic? Voltage or neutrotransmittor dependent Chloride channel? Excitatory or inhibitory?
direct
receptor
stimulate
muscimol
+ +
block
bicuculline
direct
stimulate
stimulate
calming effect
+ -
inhibit
Picrotoxin
Glycine
Inhibitory neurotransmitter in the spinal cord Ionotropic receptor controlling a chloride channel Strychnine blocks glycine receptor (-)
Receptor block Stychnine
Peptides
Neurotransmitter: Endogenous opiods Receptor: Opiate receptor Effects
Analgesia Inhibits defensive response such as fleeing and hiding Reinforcement (addiction)
Receptor
stimulate
+ -
inhibit
Lipids
Neurotransmitter: anandamide Metabotropic receptors Effects
Analgesia and sedation, stimulate appetite, reduce nausea, reduce symptom of motor disorder Interferes with concentration and memory, alter visual and auditory perception and perception of the passage of time
receptor
block
Rimonabant
+ + +
THC MAFP
block
AM1172
Nucleosides
Sugar molecule bound with a purine or pyrimidine base Neuromodulator: adenosine Metabotropic receptors with potassium channels Effects:
Dilate blood vessel and bring oxygen to cells Inhibitory, control of sleep, increase during wakefulness and decrease during sleep
Receptor
block
Caffeine
Soluble gases
Nitric oxide (NO) one nitrogen and one oxygen atom Control of muscle of intestine wall; Dilate blood vessel to become metabolically active Produced in several regions of a nerve cell, including dendrites, release as soon as produced, no vesicles/impulse involved L-NAME deactivate the enzyme that involves in the synthesis of NO, (-)
Synthesis inhibit L-NAME
Originated location Dorsal lateral pons Basal forebrain Medial septum Substantia nigra Ventral tegmental
Functions muscle movement, REM sleep, Memory, learning Motor reward, planning
Dopamine
Amine
Norepinephrine Serotonin
Amine Amine
Glutamate GABA Glycine Enkephalins (Opioids) anandamide adenosine Nitric oxide (NO)
amino acid amino acid amino acid peptides Lipids Nucleosid es Gas
brain brain Spinal cord Painkiller, inhibit defense, reinforcement Analgesia and sedation, perception distortion sleep Dilate blood vessel Caffeine Addiction to opiates Anxiety level Anxiety disorder