W20-L5: Transmitters and Receptors Flashcards Preview

Matt's Block 06 - Neuro block > W20-L5: Transmitters and Receptors > Flashcards

Flashcards in W20-L5: Transmitters and Receptors Deck (14):
1

Where can drugs effect the CNS?

They can effect action potentials, synthesis of NT, release of NT, re-uptake, breakdown and actions at receptor

2

Difference between cocaine and amphetamine

Cocaine blocks re-uptake

Amphetamine causes non-exocytotic release

3

What are two treatment options for epilepsy?

A. Reduce excitatory input (Phenytoin)
B. Enhance inhibitory input (Benzodiazepines)

4

What are benzodiazepines used in?

– Epilepsy
– Anxiety
– Sleep disorders
– Premedication
• Sedation for medical
procedures
– Acute alcohol withdrawal

5

What is the problem with barbiturates?

They have a low therapeutic index and are highly addictive

6

How do benzodiazepines work?

Interact with GABA A receptors only, increases the frequency of Cl- channel opening

7

What type of modulation do benzodiazepines work by?

Allosteric modulation

8

Why can you not die from an overdose of a single benzodiazepines?

There is a ceiling in the amount of activation a receptor channel can open which is below death

9

What are some advantages of allosteric modulators?

• Ceiling of effect of inhibitors – increased therapeutic window
• Positive modulation of endogenous agonist effect rather than continuous effect of exogenous agonist
– physiological regulation continues
• Great receptor subtype selectivity possible

10

What are some problems with benzodiazepines?

• Tolerance
– Gradual escalation of dose needed
• Dependence
– Signs of physical & psychological withdrawal
• Nausea, tremor, also anxiety, depression, insomnia – Gradual dose reduction

11

What is potency?

Relative position of the dose-effect curve along the dose axis

12

When is the only case in which low potency is a disadvantage?

if the dose is so large that it is awkward to administer

13

What is efficacy?

The ability of a drug to do the right thing

14

Barbiturates V Benzodiazpines

Both potentiate the effect of GABA
• Benzodiazepines increase the frequency of the chloride ion channel opening at the GABAA receptor (increases GABA potency)
• Barbiturates produce their pharmacological effects by increasing the duration of chloride ion channel opening at the GABAA receptor (increase GABA efficacy)

Decks in Matt's Block 06 - Neuro block Class (48):