Exam 1 Lecture 1 Neuro Pharm

Question 1

Astrocytes functions (8)

Answer 1

~Structural 
~Metabolic support
~Blood-brain barrier 
~Transmitter reuptake and release
~Regulation of ion concentration in the extracellular space (Na and K)
~Modulation of synaptic transmission 
~Vasomodulation (neuron controlled)
~Repair of damaged neural tissue

Question 2

Effects of drugs on neural activity (2 main categories)

Answer 2

~most active at synapse

~generalized increase or decrease in neural excitability (ionic pore blockers)

Question 3

Effects of drugs on neural activity at the synapse (5)

Answer 3

~Agonist
~Antagonist
~Enhance excitatory or inhibitory transmitter binding to receptor by  affinity of the receptor for the transmitter
~Block enzymatic degradation of transmitter
~Block reuptake of transmitters from the synaptic gap

Question 4

Blood brain barrier is formed by (3)

Answer 4

~Tight junctions between brain capillary endothelial cells versus relatively porous elsewhere
~Astrocytic processes (feet) covering the outer surface of the capillaries
~Active removal of drugs and toxins within CNS

Question 5

BBB function

Answer 5

designed to protect brain from infectious organisms and toxins

Question 6

BBB has a ____ and ____ filter (details)

Answer 6

Size and Charge!
~that only molecules that have a molecular weight smaller than 500 Daltons can reliably get through the BBB
~(H2O = 18 Daltons, insulin = 5,000 Daltons)
~98% of all known potential CNS drugs have a molecular weight bigger than 500 daltons so they can’t cross the BBB

Question 7

BBB: way to get across the BBB (and details)

Answer 7

~Pro-drug
~An inactive precursor of a drug, converted into its active form in the body by normal metabolic processes
~Used in cancer chemotherapy because of toxicity of active agent
~In neuropharmacology - best example is use of L-dopa a precursor of dopamine in Parkinson’s Disease (helps to aid in the rigidity)

Question 8

Acetylcholine Transmitter System: Anticolinergic Drugs (what is it and the diseases associated with)

Answer 8

~blocks CNS (but also autonomic) cholinergic receptors

~Used to block excitatory action of cholinergic interneurons in the basal ganglia in Parkinson’s disease

Question 9

Acetylcholine Transmitter System: anticholinesterase inhibitors (what are they and the disease it is associated with)

Answer 9

~Limits the enzymes ability to breakdown acetylcholine in synaptic cleft
~Helps to maintain memory, not regain
~The brain will atrophy in Alzheimer’s; the neuron will stay alive and not atrophy in a perfect world to decrease the effect of Alzheimers (decrease the break down of Ach synaptic cleft)

Question 10

Norepinephrine transmitter system: what are they

Answer 10

Number of drugs used to block or stimulate adrenergic receptors- cardiac

Question 11

Norepinephrine transmitter system: when to use them/ the type

Answer 11

~Group of selective serotonin/norepinephrine reuptake blockers- mental illness
~Depletion of NE following blockade of NE reuptake and re-release- Tegretol for seizures (Decreasing in multiple ways)
~Selective NE re-uptake blockers – amphetamines (uppers)

Question 12

Norepinephrine transmitter system: when they are weak

Answer 12

Weak norepinephrine reuptake blocker activities are common in some tricyclic & atypical-antidepressants

Question 13

Dopaminergic Transmitter system: principal drug tx

Answer 13

~L-dopa is the principle drug tx for Parkinson’s disease

Question 14

Dopaminergic Transmitter system: 5 drugs in this system

Answer 14

~L-dopa
~dopamine agonist
~dopamine antagonists
~MAOIs
~catechol-O-methyltransferase inhibitor (COMTIs)

Question 15

Dopaminergic Transmitter system: dopamine agonist

Answer 15

used in Parkinson’s

Question 16

Dopaminergic Transmitter system: dopamine antagonist

Answer 16

antipsychotic medication and in bipolar disorder

Question 17

Dopaminergic Transmitter system: MAOIs

Answer 17

~monoamine oxidase inhibitors
~used as antidressants, but interactions peripherally with tyramine from red wine and aged cheese cause hypertensive crisis when MAO-A was inhibited

Question 18

Dopaminergic Transmitter system: Catechol-O metylthransferase inhibitors (COMTIs)

Answer 18

~in Parkinson’s disease as an adjunct therapy

~not going to allow the reuptake

Question 19

Serotonergic Transmitter System: 3 types

Answer 19

~serotonin agonist
~SSRI
~SNRI

Question 20

Serotonergic Transmitter System: serotonin agonists

Answer 20

for migraine headaches

Question 21

Serotonergic Transmitter System: SSRI

Answer 21

~selective serotonin reuptake inhibitors

~most commonly used antidepressants

Question 22

Serotonergic Transmitter System: SNRI

Answer 22

~selective serotonin/norepinephrine reuptake inhibitors

Question 23

Histamine transmitter system (details)

Answer 23

~antihistamines- H1 receptor blocking agent

~anti-emetic (nausea reducing), anxiolytic (anxiety reducing)

Question 24

GABA transmitter system: what does GABA stand for?

Answer 24

Gama amino butyric acid

Question 25

GABA transmitter system: agonists

Answer 25

~treatment of spasticity, being more effective on spasticity of spinal cord injury than cortical injury
~acts to either inhibit the excitability of ventral horn motor neurons or cells that excite motor neurons

Question 26

GABA transmitter system: increase the affinity of the GABA receptor by _____ (and what drugs)

Answer 26

:by binding to a specific receptor for the drug
~benzodiazepines- used as a minor tranquilizer and anti-anxiety med
~Topamax- actions may involve the blockade of Na channels; used as anti-seizure meds and for migraine headaches

Question 27

GABA transmitter system: increase GABA levels

Answer 27

~Depakote (divalproex sodium)
~converts to valproic acid which is the active agent
~used as anti-seizure med and for migraine headaches

Question 28

GABA transmitter system: enhances GABA inhibition

Answer 28

~Gabapentin (Neurotin)- also may act blockade of voltage- dependent Na channels; used as an anti-seizure med and to control the pain of diabetic polyneuropathies
~Phenobarbital- also may act by decreased release of glutamate by blocking Ca++ entry into synaptic terminals; major tranquilizers, sedative, anti-seizure meds

Question 29

Glutamate transmitter system: 3 meds

Answer 29

~Namenda
~Topamax
~Phenobarbital

Question 30

Glutamate transmitter system: Namenda

Answer 30

(memantine hydrochloride)
~low to moderate affinity uncompetitive (open channel) NMDA receptor antagonist which binds preferentially to the NMSA receptor-operated cation channels
~used in the treatment of Alzheimer’s disease

Question 31

Glutamate transmitter system: Topamax

Answer 31

(topiramate)

~may involve the attenuation of kainite-induced response

Question 32

Glutamate transmitter system: Phenobarbital

Answer 32

~decreased release of glutamate (block Ca++ entry into synaptic terminals)

Question 33

Drugs that act by mechanisms other than at synapse

Answer 33

~blocks resetting of Na+ channels from inactive to active thus increasing absolute refractory period btw action potential to sleep action potential frequency
~blocking voltage-dependent Na+ channels, resulting in stabilization of hyperexcited neural membranes, inhibition of repetitive neuronal firing, and diminution of the propagation of synaptic impulses
~increases in K+ and Ca++ permeability (conductance)