Exam 1 Lecture 1 Neuro Pharm Flashcards Preview

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Flashcards in Exam 1 Lecture 1 Neuro Pharm Deck (33)
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1

Astrocytes functions (8)

~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

2

Effects of drugs on neural activity (2 main categories)

~most active at synapse
~generalized increase or decrease in neural excitability (ionic pore blockers)

3

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

~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

4

Blood brain barrier is formed by (3)

~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

5

BBB function

designed to protect brain from infectious organisms and toxins

6

BBB has a ____ and ____ filter (details)

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

7

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

~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)

8

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

~blocks CNS (but also autonomic) cholinergic receptors
~Used to block excitatory action of cholinergic interneurons in the basal ganglia in Parkinson's disease

9

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

~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)

10

Norepinephrine transmitter system: what are they

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

11

Norepinephrine transmitter system: when to use them/ the type

~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)

12

Norepinephrine transmitter system: when they are weak

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

13

Dopaminergic Transmitter system: principal drug tx

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

14

Dopaminergic Transmitter system: 5 drugs in this system

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

15

Dopaminergic Transmitter system: dopamine agonist

used in Parkinson's

16

Dopaminergic Transmitter system: dopamine antagonist

antipsychotic medication and in bipolar disorder

17

Dopaminergic Transmitter system: MAOIs

~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

18

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

~in Parkinson's disease as an adjunct therapy
~not going to allow the reuptake

19

Serotonergic Transmitter System: 3 types

~serotonin agonist
~SSRI
~SNRI

20

Serotonergic Transmitter System: serotonin agonists

for migraine headaches

21

Serotonergic Transmitter System: SSRI

~selective serotonin reuptake inhibitors
~most commonly used antidepressants

22

Serotonergic Transmitter System: SNRI

~selective serotonin/norepinephrine reuptake inhibitors

23

Histamine transmitter system (details)

~antihistamines- H1 receptor blocking agent
~anti-emetic (nausea reducing), anxiolytic (anxiety reducing)

24

GABA transmitter system: what does GABA stand for?

Gama amino butyric acid

25

GABA transmitter system: agonists

~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

26

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

: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

27

GABA transmitter system: increase GABA levels

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

28

GABA transmitter system: enhances GABA inhibition

~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

29

Glutamate transmitter system: 3 meds

~Namenda
~Topamax
~Phenobarbital

30

Glutamate transmitter system: Namenda

(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