Flashcards in W20-L5: Transmitters and Receptors Deck (14):
Where can drugs effect the CNS?
They can effect action potentials, synthesis of NT, release of NT, re-uptake, breakdown and actions at receptor
Difference between cocaine and amphetamine
Cocaine blocks re-uptake
Amphetamine causes non-exocytotic release
What are two treatment options for epilepsy?
A. Reduce excitatory input (Phenytoin)
B. Enhance inhibitory input (Benzodiazepines)
What are benzodiazepines used in?
– Sleep disorders
• Sedation for medical
– Acute alcohol withdrawal
What is the problem with barbiturates?
They have a low therapeutic index and are highly addictive
How do benzodiazepines work?
Interact with GABA A receptors only, increases the frequency of Cl- channel opening
What type of modulation do benzodiazepines work by?
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
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
What are some problems with benzodiazepines?
– Gradual escalation of dose needed
– Signs of physical & psychological withdrawal
• Nausea, tremor, also anxiety, depression, insomnia – Gradual dose reduction
What is potency?
Relative position of the dose-effect curve along the dose axis
When is the only case in which low potency is a disadvantage?
if the dose is so large that it is awkward to administer
What is efficacy?
The ability of a drug to do the right thing