III. Anti-depressants / mood stabilizing agents II. CNS stimulants / psychomotor agents Source material: Harvey and Champe "Pharmacology" 2000; Kalant and Roschlau “ Medical Pharmacology" 1998; Kandel et al. “Principles of Neural Science" 2000 Pharmacology of mood altering substances I. Central nervous system, basic properties
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H10, K30
H12, K29
III. Anti-depressants / mood stabilizing agents
II. CNS stimulants / psychomotor agents
Source material: Harvey and
Champe "Pharmacology" 2000;
Kalant and Roschlau “ Medical
Pharmacology" 1998; Kandel et al.
“Principles of Neural Science" 2000
Pharmacology of mood altering substances
I. Central nervous system, basic properties
Partial agonist (LSD)
presynaptic
postsynaptic
Neuron, basic properties:
information flow
Agonist:
+
Antagonist (Naloxone)
(displacement)
postsynaptic presynaptic
axon segment
myelin sheath
Na (3)
K (2)
Na, K ATPase (antiporter – Ouabain, Digoxin)
Na+
Voltage gated Na channel (tetrodotoxin)
Neuron, basic properties:
Ca+2 Neurotransmitter (glutamate)
depolarization
action potential
saltatory conduction
(ATP)
Sodium pump
Neuron, basic properties:
threshold
- action potential - Na channel opening
termination
re-equilibration
(hyperpolarization)
axon soma terminals
dendrites
hillocks
resting potential
C B
depolarization
A
-70mv
- opening of Ca channels
-inactivation of Na channels
hyperpolarization
+
_ -90
reduced probability of action potential
depolarization
excitatory +
_
inhibitory
presynaptic postsynaptic
-40
increased prob. of action potential
+
_ -70
NMDA
GABA
Neuron, basic properties:
A – Ligand binding site (neurotransmitter) B - Channel binding site (regulators, poisons, drugs) C - Modifier / co-activator site (co-agonists, drugs)
Ca+2
+
NMDA
A
B
C
(depolarize)
_
Cl -
GABA
A
B
C
(hyperpolarize)
GAD
Neuron, basic properties:
+
_
NMDA
GABA
CNS stimulants:
Psychomotor group:
- excitement and euphoria
- reduction of fatigue, increased B.P.
- increased motor activity - caffeine, theophylline, theobromine
- nicotine
- cocaine
- amphetamines
Psychotomimetic drugs (hallucinogens):
- changes in thought and mood
- few effects on brainstem / spinal cord
- lysergic acid diethylamide (LSD)
- Phenylcyclidine (PCP)
- Tetrahydrocannabinol (THC)
Potential for dependency:
Potential for dependency:
Potential for dependency:
Actions:
- inhibits phosphodiesterase, leading to increased cAMP / cGMP
- used therapeutically to treat anxiety, depression, seizures, muscle spasm
Benzodiazepines:
- highest density of binding sites: cerebral cortex, amygdala (limbic),
hippocampus, hypothalamus
- diazepam (antagonist - flumazenil)
Anxiolytics, Benzodiazepines:
Pharmacology:
- half-lives of benzodiazepines vary tremendously, this is a key component
governing their therapeutic use
A - Ligands binding site (neurotransmitter) B - Channel binding site (regulators, poisons, drugs) C - Modifier / co-activator site (co-agonists, drugs)
GABA Diazepam
Cl-
A
B
C
Anxiolytics, Benzodiazepines:
(hyperpolarize)
GABA a receptor
Anxiolytics, Benzodiazepines:
Anxiolytics, Benzodiazepines:
Antidepressants
Vincent Van Gogh, "Night Cafe“ suicide at 37 AP’s not graded, spatial and temporal summation