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845 > Intro to Neuropharmacology > Flashcards

Intro to Neuropharmacology Flashcards

1
Q

BBB’s Capillaries

A
  • Blood brain barrier
  • Brain capillaries have closed intercellular clefts are closed and form tight junctions
  • Fenestra are absent
  • Astrocytes surround about 85% of capillaries
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2
Q

BBB + Drug

A
  • Reduced diffusion of water-soluble/ionized molecules
  • Drugs MUST be nonionized/lipid-soluble to pass into CNS
  • Water-soluble drugs have to be moved by specific transport processes
  • P-gp transporters can exclude certain compounds from the brain
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3
Q

High Permeability Brain Areas

A
  1. Area Postrema - adjacent to CTZ, allows toxic substances in blood to stimulate vomiting (Apomorphine)
  2. Medium Eminence - hypothalamic releasing factors transported to pituitary gland
  3. Pineal gland - releases hormones into the blood
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4
Q

CTZ

A

Chemoreceptor Trigger Zone

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5
Q

BBB + Pharmacological Uses

A
  1. Loratadine - antihistaminic that blocks H1 receptors in periphery, DOESN’T cross BBB, antagonism caused brain produced sedation (diphenhydramine)
  2. Carbidopa - dopa decarboxylase inhibitor, doesn’t enter brain, prevents levodopa conversion to dopamine in periphery
  3. Naloxegol - Pegylated derivative of naloxone which doesn’t cross BBB and can reverse constipation produced by opiate agonists
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6
Q

Spinal Cord

A
  • Transmits messages cia afferent and efferent nerves from the periphery => CNS
  • Site of some muscle relaxants and opioids
  • Autonomic NS and somatic NS
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7
Q

Brain Stem

A
  • Medula, pons, midbrain, and cerebellum
  • 12 cranial nerves originate here
  • Mediate sensory/motor function and deal with special senses
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8
Q

Cerebellum

A
  • Coordinates motor movement via inputs from vestibular system/cortices
  • Clinical syndromes that occurs here mainly associated with awkwardness of intentional movements
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9
Q

Cerebellum Syndromes

A
  1. Ataxia - poor motor coordination/balance/speech, eye movement problems, can be produced by antiepileptic drugs
  2. Asthenia - muscles tire more easily than normal
  3. Tremor - intention tremor (evident during purposeful movements)
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10
Q

Reticular Formation

A
  • RAS, medulla of midbrain
  • HIGHLY interconnected to other neurons
  • Regulates alertness, sleep, BP, heart rate, and respiration
  • Contains nuclei for monoamine neurons (NE, Epi, 5HT)
  • Locus Ceruleus/Nucleus Tractus Solitarius => NE/Epi
  • Raphe => 5HT
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11
Q

Thalamus

A
  • Main function: relay motor and sensory signals to cortex

- Important for consciousness, sleep, and sensory interpretation

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12
Q

Midbrain

A
  • Relay for auditory and cisual systems
  • Dopamine neurons in substania nigra (motor control, Parkinsons)
  • Ventral tegmental Area (emotion/cognitive fxn, SCZ)
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13
Q

Extrapyramidal Motor System

A
  • Basal ganglia - caudate nucleus, putamen, and globus pallidus
  • Dopaminergic innervation from the substantia nigra
  • Disruption causes movement problems like Parkinson’s
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14
Q

Basal Ganglia Disorders

A
  • Parkinsons - rigid, slownessm resting tremor. Increase dopamine function in BG to treat
  • Chorea - Brief, abrupt, irregular. Treat by decreasing dopamine or enhancing GABA
  • Athetosis - slow writhing, snake-like. Treat by decrease DA
  • Tardive Dyskinesia - repetitive, involuntary, purposeless movements (long-term antipsychotic treatments). Treat by decreasing DA
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15
Q

Hypothalamus

A
  • Integrating region for ANS

- Regulates body temperature, water balance, hunger, and hormone levels

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16
Q

Limbic System

A
  • Prefrontal cortex, cingulate ortex, and entorhinal cortex
  • Cimplex emotions, motivational functions, and short term memory
  • Associated with SCZ, mania, depression, anxiety
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17
Q

Cerebral Cortex

A
  • Higher mental fxn, cognitive/emotion
  • Information processing by modality
  • Somatosensory, special senses, sleep, association
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18
Q

Postsynaptic Receptors

A
  • Receptor number depends on [agonist]
  • Chronic excess of agonist = down regulation of receptors (desensitization)
  • Chronic deficiency of agonist or antagonist blocking receptors => increase/up-regulation in number of receptors (supersensitivity)
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19
Q

Transporters Background

A
  • Exist on presynaptic terminals
  • Control the reuptake of neurotransmitters
  • Transporter antagonists bind directly to transporter and prevent reuptake (leaves more in synapse)
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20
Q

Genetic Transporter Families

A
  1. NET - NE transporter
  2. SERT - 5HT transporter
  3. DAT - Dopamine transporter
  4. GABA transporter - GAT (1-3)
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21
Q

Transporter Characteristics

A
  • DAT/NET may transport both ways
  • Cocaine blcoks all 3 monoamine transporters
  • TCA only block SERT and NET
  • SSRI - blocks SERT (fluoxetine, paroxetine)
  • SNRI - blocks SERT/NET (venlafaxine)
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22
Q

Neurotransmitters

A

-Released from one neuron to induce activity in another neuron or tissue

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23
Q

Neuromodulator

A
  • Substance released from one neuron

- Little effect by itself but alters the response to other neurotransmitters (benzos)

24
Q

ACh

A
  • Acetylcholine
  • CNS action from muscarinic => nicotinic receptors in CNS
  • Associated with several neuropathic syndromes
25
Q

ACh Associated Syndromes

A
  1. Alzheimer’s - severe impairment of cognitive function, treat with choline and anticholinersterases
  2. Parkinsons - extrapyramidal motor impairment, cholinergic/dopaminergic imbalance. Anticholinergics may help
  3. Huntington’s - degeneration of cholinergic interneurons, cholinergic/dopaminergic imbalance. Antipsychotics may help by blocking dopamine
  4. Central side effects - induced by many drugs, cause atropine-like effects
26
Q

Catecholamines

A
  • NE
  • Epi
  • DA
27
Q

NE

A
  • RAS, locus ceruleus, and lateral tegmental system
  • Alpha and Beta receptors
  • Alpha2 - autoreceptors that decrease NE neurons from brain stem
  • Site of action of Clonidine (agonist) - regulates BP, suppresses SNS activity (withdrawal, anxiety, ADHD)
28
Q

Epi

A
  • Located in lower brain stem

- Role in regulating blood pressure

29
Q

DA

A
  • Predominate catecholamine in CNS
  • Nigrostriatal, mesolimbic, mesocortical, tuberinfundibular system
  • DA inhibits prolactin secretion
  • Bromocriptine (dopamine agonist) - treats hyperprolactinemia
30
Q

DA Receptors

A
  • D1 and D5 structurally similar
  • D2, D3, and D4 structurally similar
  • D2 plays the predominent role in Parkinson’s and response to antipsychotic drugs
  • Extrapyramidal symptoms (drug SE), more likely with 1st gen. antipsychotic drugs
31
Q

5-HT

A
  • An indolamine
  • Tryptophan hydroxylase - rate-limiting enzyme, not saturated so diet can influence production
  • Fenfluramine - indirect 5-HT agonist (removed for toxicity)
32
Q

5-HIAA

A

-Principle metabolite, 2 isoforms of MAO
-MAO-A: metabolizes
5-HT, NE, DA, tyramine. Blocked by tranulcypromine (Parnate) which inhibits A and B
-MAO-B: metabolizes DA, blocked selectively by selegiline for Parkinsons

33
Q

SSRI

A
  • Antidepressant with fewer SE than TCA
  • EX: Fluoxetine
  • Used from depression, bulimia, anorexia, and panic disorder
34
Q

5HT1 Receptors

A
  • G-protein linked and decrease adenylyl cyclase
  • 5HT1A postsynaptic receptors that may be responsible for “serotonin syndrome” (overdose of 5-HT uptake inhibitor)
  • Produces myoclonus, tremor, ataxis, akathisia, diaphoresis, delirium, life threatening hyperthermia
35
Q

5HT1A Autoreceptors

A
  • Buspirone (Buspar): selective partial agonist
  • Used to treat anxiety
  • Less sedative properties than other antianxiety drugs
36
Q

5HT1B

A
  • Mediates vasoconstriction on cerebral vascular

- Sumatriptan (Imitrex) is selective agonist useful in treating migraines

37
Q

5HT2 Receptors

A
  • G-protein linked/phospholipase C
  • 5HT2A - receptors mediate forebrain cortical excitations (Risperidone, selective antagonist)
  • 5HT2C - regulate appetite (Lorcaserin, selective agonist to decrease appetite)
38
Q

5HT3 Receptors

A
  • Ligand-gated ion channel
  • Dense in area postrema where they influence emesis
  • Selective antagonist is Zofran
39
Q

5HT + Physiological Roles

A
  • Sleep
  • Anxiety (Buspirone)
  • Cognition (Risperidone)
  • Temperature regulation
  • Appetite
  • Mood
40
Q

GABA

A
  • Gamma aminobutyric acid

- Inhibitory transmitter, primary inhibitory neurotransmitter in CNS

41
Q

GABA-A

A
  • GABA-A, accounts for pharmacological actions of benzos and barbs
  • Ligand-gated Cl- channel, causes hyperpolarization
42
Q

GABA-B

A
  • G-protein coupled receptor
  • Baclofen - agonist, muscle relaxant and antispastic drug
  • NOT modulated by benzos and barbs
  • Presynaptic GABA-B decrease calcium conductance and transitter release
  • Postsynaptic GABA-B mediate IPSP by opening K+ channels
43
Q

Glutamate + Asparate + NMDA Receptor

A
  1. Excitatory amino acids - high concentrations in the brain/increase neuronal activity synthesized from glutamine
  2. Ligand-gated ion channel (Ca++/Na+)
  3. Glutamate receptor site - opened by glutamate causing Ca++/Na+ enter neuron and depolarization/excitation to occur
  4. Synthesized from gltuamine
44
Q

Memantine

A
  • Namenda
  • Competitive antagonist at glutamate receptor
  • Alzheimer’s drug therapy
45
Q

Felbamate

A
  • Felbatol
  • Glycine antagonist
  • Glycine potentiates the binding of glutamate
  • Antiepileptic drug therapy
46
Q

PCP/Ketamine

A
  • Dissociative anesthetic with receptor sites inside the glutamate channel
  • Noncompetitive and indirectly antagonize glutamate
47
Q

General Characteristics of CNS Drugs

A
  1. Physiological State
  2. Physical Dependence
  3. Psychological Dependence
  4. Tolerance
48
Q

Physiological State

A
  • Many CNS drugs stimulate or depress the brain
  • Stimulant/depressant effects are usually additive with other drugs in their class
  • Receptor antagonist represents a true antagonism/”antidote” (opioid => Naloxone, benzo => Flumazenil)
  • Physiological antagonism is more common and is rarely complete (caffeine against ethanol sedation
49
Q

Physical Dependence

A
  • Removal of drug from a dependent person
  • Results in withdrawl or abstinence syndrome
  • Cross-dependent to other drugs in same pharmacological class
50
Q

Psychological Dependence

A
  • Individual feels that the effects of a drug are necessary to maintain an optimal state of well-being
  • Doesn’t necessarily imply pathology, but becomes pathological when the use of drug impairs functioning
  • May occur without physical dependence or tolerance => basis of compulsive drug use and addiction
51
Q

Tolerance

A

-Repeated administration, same dose has lesser effects

6 types of tolerance:

  • Pharmacokinetic
  • Pharmacodynamic
  • Cross Tolerance
  • Behavioral/learned
  • Acute
  • Innate
52
Q

Pharmacokinetic Tolerance

A
  • Less drugs gets tot he site of action

- Increase in hepatic enzymes => increased metabolism => metabolic tolerance

53
Q

Pharmacodynamic Tolerance

A
  • Same amount gets to drug site but response is reduced

- Changes in receptors or mechanisms

54
Q

Cross Tolerance

A
  • Tolerance to most/all drugs within a class
  • May be partial or incomplete
  • “opioid rotation”
55
Q

Behavioral/Learned Tolerance

A
  • Same amount of drugs gets to site

- Individual compensates

56
Q

Acute Tolerance

A
  • Rapid developing tolerance

- Can occur within a few hours after exposure to CNS drugs

57
Q

Innate Tolerance

A
  • Genetically determined

- Less affected by certain drugs on an individual basis

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