Psychopharmacology Flashcards
(97 cards)
1
Q
psychopharmacology
A
The study of the effects of drugs on the nervous system and behavior.
2
Q
drugs
A
An exogenous chemical not neces- sary for normal cellular functioning that significantly alters the functions of certain cells of the body when taken in relatively low doses.
3
Q
drug effects
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Observable changes in an individual’s physiology and/or behavior.
4
Q
sites of action
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The locations where drug molecules interact with molecules on or in cells to affect biochemical processes.
5
Q
pharmacokinetics
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The process by which drugs are absorbed, distributed within the body, metabolized, and excreted.
6
Q
intravenous (IV) injection
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Injection of a substance directly into a vein.
7
Q
intraperitoneal (IP) injection
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Injection of a substance into the peritoneal cavity—the space that surrounds the stomach, intestines, liver, and other abdominal organs.
8
Q
intramuscular (IM) injection
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Injection of a substance into a muscle.
9
Q
subcutaneous (SC) injection
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Injection of a substance into the space beneath
the skin.
10
Q
oral administration
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Administration of a substance into the mouth so that it is swallowed. (doesn’t work for things like insulin)
11
Q
sublingual administration
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Administration of a substance by placing it beneath the tongue. (ex: drugs to treat migraines)
12
Q
inhalation
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Administration of a vaporous substance into the lungs. (very quick effect)
13
Q
topical administration
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Administration of a substance directly onto the skin or mucous membrane. (steroid hormones/nicotine)
14
Q
insufflation
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Administration of a sub- stance by sniffing or snorting; drug is absorbed through the mucous membranes of the nose.
15
Q
lipid solubility
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The ability of fat-based molecules to pass through cell membranes.
16
Q
if a substance is more lipid soluble, what happens in terms of rate of effect?
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It is much faster acting (ex: heroin is faster than morphine)
17
Q
Metabolism and excretion of drugs
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- metabolized + deactivated by enzymes (liver plays active role, also in blood, sometimes brain)
- excreted (primarily through kidneys)
18
Q
dose-response curve
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A graph of the magnitude of an effect of a drug as a func- tion of the amount of drug administered.
19
Q
therapeutic index
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The ratio between the dose that produces the desired effect in 50 percent of the animals and the dose that produces toxic effects in 50 percent of the animals.
20
Q
why do drugs vary in effectiveness?
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- may have different sites of action
- the affinity of the drug with its site of action is different
21
Q
affinity
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The readiness with which two molecules join together.
22
Q
tolerance
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A decrease in the effectiveness of a drug that is administered repeatedly.
23
Q
sensitization
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An increase in the effectiveness of a drug that is administered repeatedly.
24
Q
withdrawal symptom
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The appearance of symptoms opposite to those produced by a drug when the drug is administered repeatedly and then suddenly no longer taken.
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physical dependence
Compensatory changes following repeated use of a drug that result in withdrawal symptoms when the drug is no longer taken.
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compensatory mechanism that accompany repeated drug use
- decrease of effectiveness of binding (receptors less sensitive, decreased affinity, less receptors aka receptor downregulation)
- one or more steps in the coupling process becomes less effective
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placebo
An inert substance that is given to an organism in lieu of a physiologically active drug; used experimentally to control for the effects of mere administration of a drug.
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antagonist
A drug that opposes
| or inhibits the effects of a particular neurotransmitter on the postsynaptic cell.
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agonist
A drug that facilitates the effects of a particular neurotransmitter on the postsynaptic cell.
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sequence of synaptic activity
1. Neurotransmitters are synthesized and stored in synaptic vesicles
2. synaptic vesicles travel to the presynaptic membrane and are docked
3. axon fires --> entry of calcium ions
4. calcium interacts with docking protein + neurotransmitters are released
5. bind to postsynaptic receptors --> changes in processes or opening of ion channels --> IPSP/EPSP
6. reuptake/enzyme deactivation/presynaptic auto receptors
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how can drugs increase/decrease neurotransmitter synthesis?
increased: administration of precursor (they synthesize neurotransmitters)
decreased: inactivation of enzymes that control neurotransmitters
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how can drugs increase/decrease neurotransmitter storage/release?
decrease: blocking of transporter molecules that fill synaptic vesicles OR deactivating protein that cause vesicles to fuse with membrane
increase: bind with proteins to release neurotransmitters
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effects of drugs on postsynaptic receptors
- direct agonist
| - receptor blockers/direct antagonist
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effects of drugs on presynaptic receptors
- agonist: block presynaptic auto receptors
| - antagonist: activate presynaptic receptors
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direct agonist
A drug that binds with and activates a receptor.
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receptor blocker/direct antagonist
A drug that binds with a receptor but does not activate it; prevents the natural ligand from binding with the receptor.
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noncompetitive binding
Binding of a drug to a site on a receptor; does not interfere with the binding site for the principal ligand.
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indirect antagonist
A drug that attaches to a binding site on a receptor and interferes with the action of the receptor; does not interfere with the binding site for the principal ligand.
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indirect agonist
A drug that attaches to a binding site on a receptor and facilitates the action of the receptor; does not inter- fere with the binding site for the principal ligand.
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effects on reuptake/destruction of neurotransmitters
- inactivate molecules responsible for reuptake
- bind with enzyme responsible for deactivation (ex: acetylcholinesterase which destroys acetylcholine)
- -> agonists
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glutamate
An amino acid; the most important excitatory neurotransmitter in the brain.
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vesicle glutamate transporter
Proteins in the vesicle membrane that pump gluta- mate into a vesicle.
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four major types of glutamate receptors
- NMDA receptor
- AMPA receptor
- kainate receptor
- metabotropic glutamate receptor
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NMDA receptor
A specialized ionotropic glutamate receptor that controls a calcium channel that is normally blocked by Mg2 + ions; has several other binding sites.
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AMPA receptor
An ionotropic glutamate receptor that controls a sodium channel; stimulated by AMPA.
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kainate receptor
An iono- tropic glutamate receptor that controls a sodium channel; stimulated by kainic acid.
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PCP
Phencyclidine; a drug that binds with the PCP binding site of the NMDA recep- tor and serves as an indirect antagonist.
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ketamine
A drug that binds with a non- competitive binding site of the NMDA receptor and serves as an indirect antagonist.
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excitatory amino acid transporters
Proteins that remove glutamate (and other excitatory amino acids) from the synapse.
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glutamine synthase
Enzyme that breaks down glutamate into its precursor glutamine.
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glutamate excitotoxicity
Too much glutamate stimulation in the synapse, damages neurons by prolonged overexcitation
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GABA
An amino acid; the most important inhibitory neurotransmitter in the brain.
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vesicle GABA transporter
Proteins in the vesicle membrane that pump GABA into a vesicle.
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abnormality in biochemistry of GABA-secreting neurons
causes seizures, because no inhibition
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GABAA receptors
- contain at least five different binding site
| - ionotropic and control chloride channels
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GABA transporter
Proteins that remove GABA from the synapse.
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ACh pathways and function
- dorsolateral pons: REM sleep
- basal forebrain: activate cerebral cortex and facilitates learning (esp perceptual)
- medial septum: electrical rhythms of hippocampus and modulate functions (like formation of memories)
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choline acetyltransferase
The enzyme that transfers the acetate ion from acetyl coenzyme A to choline, producing the neurotransmitter acetylcholine.
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vesicle ACh transporter
Proteins in the vesicle membrane that pump acetylcholine into a vesicle.
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botulinum toxin
An acetylcholine antagonist; prevents release by terminal buttons.
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nicotine
An agonist for the ionotropic acetylcholine receptor. (PNS and a little in CNS)
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muscarine
An agonist for the metabotropic acetylcholine receptor (CNS)
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neostigmine
A drug that inhibits the activity of acetylcholinesterase.
| - treat myasthenia gravis (attacks ACh receptor on skeletal muscles)
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acetylcholinesterase
deactivates ACh
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monoamine
A class of amines that includes indolamines, such as serotonin, and catecholamines, such as dopamine, norepinephrine, and epineph- rine.
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catecholamine
A class of amines that includes the neu- rotransmitters dopamine, norepinephrine, and epinephrine.
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dopamine (DA)
A neurotransmitter; one of the catecholamines. Produces IPSP and EPSPs.
Implicated in movement, attention, learning, reinforcing effects of abuse drugs
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Most important dopamine pathways location
Midbrain: substantia nigra & ventral tegmental area
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nigrostriatal system
A system of neurons originating in the substantia nigra and terminating in the neostriatum (caudate nucleus and putamen).
- control of movements
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mesolimbic system
A system of dopaminergic neurons originat- ing in the ventral tegmental area and terminating in the nucleus accumbens, amygdala, and hippocampus.
- reinforcement (reward)
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mesocortical system
A system of dopaminergic neurons originating in the ventral tegmental area and terminating in the prefrontal cortex.
- short term memories, planning, strategies for problem solving
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Parkinson’s disease
A neurological disease characterized by tremors, rigidity of the limbs, poor balance, and difficulty in initiating movements; caused by de- generation of the nigrostriatal system.
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melanin
produced by breakdown of dopamine, reason why substantial nigra is stained black
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L-DOPA
The levorotatory form of DOPA; the precursor of the catecholamines; often used to treat Parkinson’s disease because of its effect as a dopamine agonist.
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Synthesis of the Catecholamines
Tyrosine --> L-DOPA --> Dopamine --> Norepinephrine
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vesicle monoamine transporter
Proteins in the vesicle membrane that pump monoamine neurotransmitters into a vesicle.
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apomorphine
A drug that blocks dopamine autoreceptors at low doses; at higher doses, blocks post- synaptic receptors as well.
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Drugs that inhibit reuptake of dopamine
amphetamine, methamphetamine, cocaine, and methylphenidate (Ritalin)
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amphetamine & methamphetamine
Antagonists at dopamine and norepinephrine transporters that causes them to run in reverse, releasing these neurotransmitters into the synapse.
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Cocaine
A drug that inhibits the reuptake of dopamine. Also blocks sodium channels & used as topical anesthetic.
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methylphenidate
A drug that inhibits the reuptake of dopamine. Used to enhance attention and impulse control in ADHD.
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monoamine oxidase (MAO)
A class of enzymes that destroy the monoamines: dopamine, norepinephrine, and serotonin.
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Norepinephrine
One of the catecholamines; a neu- rotransmitter found in the brain and in the sympathetic division of the autonomic nervous system.
- Found in both CNS & PNS
- Most important system begins in locus coeruleus
- increase in vigilance
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epinephrine
One of the catecholamines; a hormone secreted by the adrenal medulla; serves also as a neurotransmitter in the brain.
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locus coeruleus
A dark- colored group of noradrenergic cell bodies located in the pons near the rostral end of the floor of the fourth ventricle.
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axonal varicosity
An enlarged region along the length of an axon that contains synaptic vesicles and releases a neu- rotransmitter or neuromodulator. (norepinephrine & serotonin)
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norepinephrine receptors
alpha 1 and 2 adrenergic receptors
| beta 1 and 2 adrenergic receptors
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norepinephrine transporter
Proteins that remove norepinephrine from the synapse.
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serotonin (5-HT)
An indolamine neurotransmitter; also called 5-hydroxytryptamine.
Regulation of mood, control of eating, sleeping, arousal, pain, dreaming
in dorsal and medial raphe nuclei
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Synthesis of
| Serotonin
Tryptophan --> 5-HTP --> 5-HT
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Serotonin receptors
- 9 different
| - one ionotropic: 5-HT3 (controls chloride channels/IPSPs) play role in nausea and vomitting
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serotonin transporter
Proteins that remove serotonin from the synapse.
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fluoxetine
A drug that inhibits the reuptake of 5-HT.
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MDMA
A drug that serves as a norad- renergic and serotonergic agonist, also known as “ecstasy”; has excitatory and hallucinogenic effects.
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histamine
A neurotransmitter that plays an important role in stimulating wakefulness. Located in tuberomammillary nucleus in posterior hypothalamus.
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histamine receptors
4: H1-H4
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diphenhydramine
An antihistamine drug; antagonist at histamine receptors.
