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Pharmacy Semester 2 > Neuropharmacy 2 > Flashcards

Neuropharmacy 2 Flashcards

1
Q

What are the divisions of PNS & CNS and ANS?

A

PNS - Somatic and Autonomic
ANS - sympathetic & parasympathetic
CNS - Brain & Spinal Cord

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2
Q

How do drugs cross the BBB?

A

By inflammation - blood vessels are more leaky due to damage
Transporters
P- Glycoproteins - cell membrane pumps

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3
Q

How is the cerebrum split?

A

Into two parts : Creativity - RHS - Contains Grey matter
Logic and learning - LHS

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4
Q

What is the cerebral cortex composed of?

A

Sensory, motor & association areas

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5
Q

What are the four lobes of the cerebrum?

A

Parietal - sensorimotor integration - touch
Temporal - Ears - involved with language
Occipital - Visual Processing
Frontal - Memory & Learning

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6
Q

What is the hypothalamus involved in?

A

Homeostasis, thirst, hunger, emotion & ANS

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7
Q

What abnormalities are associated with the thalamus?

A

OCD, Bipolar & anxiety

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8
Q

What abnormalities is the hippocampus associated with?

A

Alzheimer’s, involved with learning & memory

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9
Q

What part of the brain is associated with addiction?

A

Ventral Tegmental

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10
Q

What regulates coordination of movement, posture & balance?

A

Cerebellum

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11
Q

What is the brainstem?

A

Medulla, pons & midbrain - involved with vision, hearing and body movement alongside major control centres

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12
Q

What is the spinal cord involved in?

A

Conduction pathway to and from the brain.

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13
Q

What are the four functional systems of the brain?

A

Limbic System - Involved in the reward
responsible for memory, emotion and learning. Connects to hypothalamus & communicates with the cerebrum

Reticular Activating system - Acts as a filter
Network of neurons that heightens alertness and arousal of the brain. Sleepiness and awakeness. Projects from brainstem to thalamus

Basal Ganglia - Connected to the limbic system - reward system. Cluster of neurons regulating initiation and termination of skeletal muscle movement.

Extrapyramidal system - part of motor system involved in the coordination of movement. Reflexes, complex movements & postural control

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14
Q

Define a neuron and explain its four parts

A

A neuron is an excitable cell that processes and transmits information by electrochemical signalling.
Dendrite - Input of information
Axon - Transports information
Soma/ perikaryon - Processes & maintains information
Nerve Terminal - Output of information

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15
Q

What regulates gene expression?

A

Neurotrophic factors

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16
Q

Define neuromodulators

A

Released from astrocytes or neurons and produce slower post or pre synaptic responses

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17
Q

Define neurotransmitters

A

Released from presynaptic terminals and produce rapid excitatory or inhibitory responses in postsynaptic neurons

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18
Q

What are three types of glial cells

A

Astrocytes, Oligodendrocytes & microglia

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19
Q

What cells act as macrophages of the brain?

A

Microglia

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20
Q

How do microglia function?

A

Proliferate after injury, move to the site of injury and transform in large macrophages to remove cellular debris

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21
Q

What are oligrodendrocytes?

A

Form the myeline sheath around the axon

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22
Q

What are astrocytes?

A

Separate neurons and modulate the metabolic and ionic microenvironment

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23
Q

Can glial cells undergo cellular division?

A

Yes

24
Q

What are the two forms of neutrotransmitters?

A

Amino Acid derived and amine-containing

25
Q

What are types of inhibitory and excitatory neurotransmitters?

A

GABA & Glycine - inhibitory
Glutamate & Aspartate - Excitatory

26
Q

What is reuptake required?

A

Active reuptake of neurotransmitters into the presynaptic nerve or other supporting cells like glia, terminates the function of neurotransmitters. This is dependent on transporter proteins - each specific for particular transmitters

27
Q

How is glutamate converted to GABA?

A

By the enzyme glutamic acid decarboxylase. Removes a carboxyl group

28
Q

What enzyme is used to convert glutamine to glutamate?

A

Glutaminase

29
Q

What enzyme is used to convert Glutamate to glutamine?

A

Glutamine Synthase

30
Q

Where does glutamate come from?

A

Derived from glucose in the Krebs cycle by action of GABA transaminase or glutamine - synthesised by glial cells

31
Q

How is glutamates action terminated?

A

By carrier-mediated reuptake

32
Q

What is the role of astrocytes with regards to glutamate

A

This reaction takes place in astrocytes. Astrocytes take up glutamate and convert to glutamine, enabling it to be transported - back to neurons to be converted back to glutamate.

33
Q

What are the 4 type of EAA receptors for glutamate?

A

NMDA
AMPA
Kainate
Metabotropic

34
Q

Where are NMDA receptors located?
Where are AMPA receptors located?

A

Expressed on nerve terminals where they can enhance or reduce transmitter release.
Expressed also on astrocytes as well as neurons - play an important communication role

35
Q

How is glutamate released?

A

Stored in synaptic vesicles and released by Ca2+ dependent exocytosis - taken up by nerve terminals and neighbouring astrocytes

36
Q

Describe NMDA transmission

A

Highly permeable to Ca2+
Blocked by physiological Mg2+, if decreases then becomes unblocked
Requires the presence of glycine - allosteric modulator.
Mediate slower excitatory responses than AMPA & Kainate

37
Q

What happens if there are excessive Ca2+ ions?

A

The entry of excessive amounts of Ca2+ produced by NMDA receptor activation can result in cell death known as excitotoxicity.

38
Q

How is GABA formed, enzymes?
How is GABA terminated, enzymes?

A

Formed from glutamate by action of glutamic acid decarboxylase.
Terminated by reuptake and also deamination by GABA transaminase.

39
Q

Where is GABA located?

A

Found only in the brain tissue

40
Q

What effects do GABA receptor agonists have?
What receptors do they act on?

A

anti-anxiety and anti-convulsive
GABAa & GABAb

41
Q

What are GABAa receptors?

A

Located postsynaptically, directly coupled to chloride channels. When these are open they reduce excitability.
Increasing Cl- permeability hyperpolarises the cell

42
Q

What are examples of GABA channel agonist?

A

benzodiazepines, barbiturates & ethanol
Benzodiazipine is an allosteric

43
Q

How does Benzodiazepine work?

A

Act selectively on GABAa receptors- mediating an inhibitory synaptic transmission.
They act as positive allosteric modulators facilitating the opening of GABA -activated chloride ion channels and act allosterically to enhance the affinity for GABA and the receptor. As the cl- conc increases, this hyperpolarises the cell reducing its ability to be excited.

44
Q

Example of sedative benzodiazepines

A

Diazepam

45
Q

Give examples of GABA reuptake inhibitors
& GABA transaminase inhibitors

A

Tiagabine
Valproate, Vigabatrine

46
Q

Where is glycine located and how does it work?

A

Located in spinal cord & brainstem and works the same as GABA
When glycine receptors are activated - CL- enters and hyperpolarises the cell reducing excitability.
Tetanus Toxins - prevent glycine release - causing hyperexcitability & muscle spasams

47
Q

Name amine transmitters

A

Noradrenaline, adrenaline, dopamine, 5-hydroxytryptamine & acetylcholine

48
Q

What is noradrenaline, where is it located & responsible for?

A

Neurotransmitter located in small cluster of noradrenergic cells of the pons & medulla. Most prominent cluster is LC (locus coeruleus).
Affect mood, BP & arousal.
LC is connected to spinal cord & involved in descending control of pain.
Some adrenergic cells located in brainstem release adrenaline - due to them containing phenylethanolamine methyl transferase - enzyme responsible for conversion of noradrenaline to adrenaline.

49
Q

What is dopamine, what are the four pathways?

A

Neurotransmitter and precursor for noradrenaline.
1 - Nigrostriatal - cell bodies in the substantia nigra whose axon terminate in the corpus striatum, movement & motor control.
2 - Misolimbic - Midbrain to Limbic system. Project into parts of nucleus accumbens and amygdaloid nucelus - reward, learning.
3 - Mesocortical - Midbrain to Cortex. Important for emotional control & motivation
4 - Turbohypophyseal neurons - Hypothalamus to pituitary gland - involved with endocrine system

50
Q

What are the dopamine receptors?

A

5
D1 & 5 = stimulate adenylyl cyclase
2,3,4 = inhibit ca2+, stimulate K+ and ultimately inhibit adenylyl cyclase.
D2 - responsible for positives in schizophrenia and parkinsons
D2 - releases prolactin from pituitary gland.

51
Q

What serotonin receptor is responsible for treatment of nausea and vomitting?

A

5-HT3

52
Q

What serotonin receptor is responsible for prophylaxis of migraines?

A

5-HT2
Alongside being the target for hallucinogenic drugs

53
Q

What serotonin receptor is responsible for treatment of anxiety and depression and what other treatment?

A

5-HT1
Agonist drugs act as migraine treatments

54
Q

What is acetylcholine and its effect on the body/location

A

ACh is an excitatory neurotransmitter consisting of various subtypes such as nicotinic (ionotropic) or muscarinic (GCPR).
Synthesised, stored and released the same way as in periphery.
Widely distributed - forebrain, midbrain and brainstem
A cluster provides the main cholinergic supply to the hippocampus which is involved in memory and learning - Alzheimers
Important in Parkinson’s

55
Q

How can neurotransmitter drugs become more specific?

A

By targeting specific receptors/ identifying receptor subtypes. Drugs targeting neurotransmitters affect the whole system.

56
Q

What is meant by complexity - HINT COCAINE

A

Cocaine inhibits reuptake of dopamine into the presynaptic neuron, exposing it for longer in the presynaptic cleft. DA will still bind to the postsynaptic neuron and cause a pleasurable emotional response. Prolonged exposure of DA will cause a downregulation of receptors.

Pharmacy Semester 2 (12 decks)

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