Exam 1 Lecture 1 Neuro Pharm - Advanced Editor Flashcards Preview

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1

Where are drugs most active

 

at the synapse?

2

Five Main Ways Drugs can Effect neurons at the synapse:

  1. –Agonist
  2. –Antagonist
  3. –Enhance excitatory or inhibitory transmitter binding to receptor by incrasing affinity of the receptor for the transmitter
  4. –Block enzymatic degradation of transmitter
  5. –Block reuptake of transmitters from the synaptic gap
     

(Drugs can also cause a generalized increase or decrease in neuronal excitability (ionic pore blockers), but not just at the synapse)
 

3

One other way (not synapse-specific) can drugs effect neurons?

 


–generalized increase or decrease in neuronal excitability (ionic pore blockers)

I think this means it can happen anywhere along the neuron, not just in the synapses
 

4

7 Neuro Transmitter Systems that work at synpases

  1.  Acetylcholine Transmitter System
  2. Norepinepherine (NE) transmitter system
  3. Dopaminergic Transmitter System
  4. Serotonergic Transmitter System
  5. HIstamine Transmitter System
  6. GABA Transmitter System
  7. Glutimate Transmitter System (Dr. Lake's favorite)

 

5

Three ways that drugs that Act by Mechanism Other than at Synapses work:
 

 

  1. •Blocks resetting of Na+ channels from inactive to active thus increasing absolute refractory period between action potentials (AP) to slow AP frequency
  2. •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
  3. •Increases in K+ and Ca++ permeability (conductance)
     

6

Two types of Acetylcholine Transmitter System Drugs:

 

  1. •Anticholinergic Drugs -
  • blocks CNS (but also autonomic) cholinergic receptors-
  • Used in Parkinson's disease
    • blocks excitatory action of cholinergic interneurons in the basal ganglia
  1. –Anticholinesterase Inhibitors-
  • Used in Alzheimer's Disease
  • •Limits the enzymes ability to breakdown acetylcholine in synaptic cleft
  • used to maintain memory, not restore it. Only slows the loss of memory
    • If receptors don’t get stimulated, they will down-regulate,
    • More Ach in the cleft stimulates receptors and preserves them

7

•Anticholinergic Drugs -

Part of Acetylcholine Transmitter System

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

8

–Anticholinesterase Inhibitors-

Part of Acetylcholine Transmitter System

  • Used in Alzheimer's Disease
  • •Limits the enzymes ability to breakdown acetylcholine in synaptic cleft
  • used to maintain memory, not restore it. Only slows the loss of memory
    • If receptors don’t get stimulated, they will down-regulate,
    • More Ach in the cleft stimulates receptors and preserves them

9

Eight main ways Norepinephrine (NE) Transmitter System has an effect?

 


 

 

  1. Block or stimulate adrenergic receptors (receptors for transmitters in NE system)
    • Example: cardiac treatment (beta-blockers)
  2. Selectivly block norepinepherine from reputake
    • Selective serotonin/norepinepherin reuptake blockers
      • example: mental illness
    • Selective NE re-uptake blockers
      • example: amphetamines
    • Trycyclic & atypical antidepressans can also have a weak NE reuptake blocker effect
  3. Deplate NE by forming a blockade preventing NE reuptake AND re-release
    • example: antiseizure (Tegretol)
  4. Pre-cursur Drug that converts after passing brain barrier
    • example: Levo-Dopa (L-dopa)
      • The principle drug for Parkinson's
  5. Dopamine Agonists
    • used for parkinsons
  6. Dopamine Antagonists
    • used as antipsychotics and for bipolar disorder
  7. MAOIs (Monoamine Oxidase Inhibitors
    • antidepressant
      • cause hypertensive crisis if combined with tyramine from
        • red wine
        • aged cheeses 
  8. COMTIs (Catechol-O-methyltransferase Inhibitors
    • Adjunctive therapy in Parkinson's disease

10

blocking or stimulating adrenergic receptors
is part of what transmitter system ?

drugs with this commonly treat ______

 NE transmitter system

Example: cardiac treatment (beta-blockers)

11

Drugs that selectively block norepinepherin from reuptake have what transmitter system?

 

Also what are Three versions of this type of drug with examples of what they are used for

Norepinephrine (NE) Transmitter System

  1. Selective serotonin/norepinepherin reuptake blockers
    • example: mental illness
  2. Selective NE re-uptake blockers
    • example: amphetamines
  3. Trycyclic & atypical antidepressans can also have a weak NE reuptake blocker effect
    • Deplate NE by forming a blockade preventing NE reuptake AND re-release
      • example: antiseizure (Tegretol)

12

Levo-Dopa (L-dopa):

What transmitter system?

How does it work?

What is it used for?

NE transmitter system

  • Pre-cursur Drug that converts after passing brain barrier
  • The principle drug for Parkinson's

13

Dopamine Agonists:

what transmitter system?

What is it used for?

NE transmitter system

used for parkinsons

14

Dopamine Antagonists:

what system?

What are they used for?

NE Transmitter system

used

  • as antipsychotics
  • for bipolar disorder

15

MAOI:

What does it stand for?

What transmitter system?

What is it used for?

What complications can it cause?

  • MAOIs (Monoamine Oxidase Inhibitor)
  • NE transmitter system
  • antidepressant
  • Interacts with a lot of things
    • will cause hypertensive crisis if combined with tyramine from
      • red wine
      • aged cheeses

16

COMTI:

What does it stand for?

What system is it from?

What is it used for?

  • COMTI (Catechol-O-methyltransferase Inhibitor)
  • NE Transmitter System
  • Adjunctive therapy in Parkinson's disease

17

Three types of Serotonergic Transmitter System Drugs:

(and their common uses)

 

  1. •Serotonin (5-hydroxytryptamine) agonists-
    • migrane headaches
  2. •Selective serotonin reuptake inhibitors - SSRIs
    • –Most commonly used anti-depressants
  3. •Selective serotonin/norepinephrine reuptake inhibitors (SNRIs)
    1. also used as antidepressants
       

18

The HIstamine Transmitter System Drug:

(and it's common uses)

 


•Antihistamine - H1 receptor blocking agent
–anti-emetic (nausea reducing), and anxiolytic (anxiety reducing)
 

19

Four types of GABA Transmitter System Drugs:

  1. Agonist drugs
    • –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
  2. Drugs that increae the Affinity of GABA receptors by binding to a specific receptor for the drug
    • Example: Benzodiazepines
      • Used as minor tranquilizers, anti-anxiety medications
      • Topamax
        • actions may involve the blockade of sodium channels
        • used as anti-seizure medication and for migraine headaches
  3. Drugs that Increase in GABA levels in brain
    • •Depakote (divalproex sodium)
      • –converted to valproic acid which is the active agent
      • –used as anti-seizure medication and for migrane headaches
  4. Drugs that enhancee GABA inhibition (mechanism unspecified)
    • •Gabapentin (Neurontin®)
      • –Also may act blockade of voltage-dependent sodium channels
      • –Used as an anti-seizure medication, 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 tranquilizer, sedative, anti-seizure medication
         

20

GABA Agonist Drugs

How does it work?

Used for what?

 

 

Agonist drugs

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

21

 Drug class that Increases the affinity of the GABA receptor by binding to a specific receptor for the drug

What it is used for

Examples

 

(GABA Transmitter System)

Benzodiazepines

  • •Used as minor tranquilizers, anti-anxiety medications
  • •Topamax
    • –actions may involve the blockade of sodium channels
    • –used as anti-seizure medication and for migraine headaches
       

22

Drugs that increase GABA levels in the brain:

Example

how it works

uses

(GABA Transmiter System)

Depakote (divalproex sodium)

  • converted to valproic acid which is the active agent
  • used as
    • anti-seizure medication
    • for migrane headaches
       

23

2 Drugs that enhance GABA inhibition (mechanism unspecified):

 

 

(GABA Transmitter System)

 

  1. Gabapentin (Neurontin®)
    • –Also may act blockade of voltage-dependent sodium channels
    • –Used as an anti-seizure medication, and to control the pain of diabetic polyneuropathies
  2. •Phenobarbital
    • –Also may act by decreased release of glutamate by blocking Ca++ entry into synaptic terminals
    • –Major tranquilizer, sedative, anti-seizure medication
       

24

Gabapentin (Neurontin®)

What is it?

what transmitter system does it belong to?

What is it used for?

(GABA transmitter system)
An enhanced GABA inhibition (mechanism unspecified) drug

  • Also may act blockade of voltage-dependent sodium channels
  • Used as
    • an anti-seizure medication
    • to control the pain of diabetic polyneuropathies

25

Phenobarbital

What is it?

what transmitter system does it belong to?

What is it used for?

 

(GABA transmitter system)
An enhanced GABA inhibition (mechanism unspecified) drug

or

Glutamate Transmitter System (it is listed under two)

  • acts by decreased release of glutamate by blocking Ca++ entry into synaptic terminals
  • Uses:
    • Major tranquilizer,
    • sedative,
    • anti-seizure medication
       

26

Three Drugs from Glutamate Transmitter system

 

  1. Namenda®   (memantine hydrochloride)
    • •Low to moderate affinity uncompetitive (open-channel) NMDA receptor antagonist which binds preferentially to the NMDA receptor-operated cation channels
    • •Used in the treatment of Alzheimer's Disease
  2. topiramate (Topamax®)
    • •May involve the attenuation of kainate-induced responses
  3. Phenobarbital
    • •Decreased release of glutamate (block Ca++ entry into synaptic terminals)
       
  •  

27

Namenda®   (memantine hydrochloride)

about it

uses

Part of Glutamate Transmitter System

  • Low to moderate affinity uncompetitive (open-channel) NMDA receptor antagonist which binds preferentially to the NMDA receptor-operated cation channels
  • •Used
    • in the treatment of Alzheimer's Disease

28

topiramate (Topamax®)

What transmitter system?

about it

 

 

Glutamate Tramsitter system

 

May involve the attenuation of kainate-induced responses

29

Drugs for Parkinson's

  1. L-Dopa - (dopaminergic transmitter system)
    • principle drug treatment
  2. Anticholinergic Drugs (Acetylcholine transmitter system)
  3. Dopamine Agonist (dopaminergic transmitter system)
  4. Catechol-O-methyltransferase (dopaminergic transmitter system)
    • adjunctive therapy