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21 Cards in this Set
- Front
- Back
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What is an adrenergic agent?
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A compound with adrenergic effect (agonists, antagonists etc.)
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What is an adrenomimetic?
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A compound that doesn't involve a receptor, but mimics adrenergic effect.
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What is a sympathomimetic?
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Produces adrenergic effect. A type of adrenergic
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Describe the mechanism by which an Sympathetic Nerve Terminal Releases neurotransmitter.
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- Tyr is taken into the nerve terminal
- Tyr is converted to Dopa and Dopamine - Dopamine is taken up into a pre-synaptic vesicle - Dopamine is converted to Norepi - Norepi is stored with 4 ATP - An AP reaches the terminal - Vesicle fuses with membrane, releases contents |
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What is COMT? Where is it located?
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Catechol - O - methyl transferase
Degrades catecholamines like Dopamine, Epinephrine and Norepinephrine Located in Synaptic space and Post synaptic terminal |
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What are OCT-1 and OCT-2?
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OCT-1 takes neurotransmitters into the presynaptic terminal
OCT-2 takes neurotransmitters into the post synaptic terminal |
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Describe OCT-1 and OCT-2 function under normal and high activity circumstances.
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OCT- 2 has a higher Km. This means that a higher concentration of neurotransmitter is needed for OCT- 2 function.
Normal circumstances - OCT - 1 is functional High activity - OCT - 1 saturates and OCT - 2 kicks in |
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What are the 4 mechanisms by which the Norepinephrine release can be inhibited?
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- Ganglionic blockade
- Inhibition of Transmitter synthesis - Blocks Dopmine into vesicle - Block fusion of vesicle |
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Name the prototypic drugs involved in these mechanisms.
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- Hexamethonium
- Metyrosine (Tyr -> Dopa), Carbidopa (Dopa -> Dopamine) - Reserpine - Guanethidine, Bretylium |
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What are the 4 mechanisms that can facilitate Norepinephrine release?
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- Facilitation of Transmitter release
- Blockade of Transmitter re-uptake - Inhibition of transmitter metabolism - Interaction with adrenoceptors |
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Name the prototypic drugs associated with these mechanisms.
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- Amphetamine, Tyramine
- Cocaine, Desipramine - Pargyline, Selegiline - Norepinephrine |
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What is a typical adrenoceptor agonist? Antagonist?
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Norepinephrine
Labetalol |
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What is a typical Alpha selective agonist? Antagonist?
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Oxymetazoline
Phentolamine |
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What is a typical Alpha 1 selective agonist? Antagonist?
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Phenylephrine
Prazosin |
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What is a typical Alpha 2 selective agonist? Antagonist?
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Clonidine
Yohimbine |
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What is a typical Beta selective agonist? Antagonist?
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Isoproterenol
Propanolol |
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What is a typical Beta 1 selective agonist? Antagonist?
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Dobutamine
Practolol |
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What is a typical Beta 2 selective agonist? Antagonist?
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Albuterol
Butoxamine |
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What is a typical Beta 3 selective agonist?
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BRL 373344
No consistently used Beta 3 selective antagonists |
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Know Chemical structures of Sympathomimetics
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Catechol
Phenylephrine Norepi Epi Isoproterenol Dopamine Phenylephrine Methylamine Ephedrine Amphetamine |
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Describe Epinephrine and Norepinephrines receptor selectivity?
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Epi = Equal among both alpha and beta receptors
Norepi = Alpha 1 = Alpha 2, Beta 1 >>Beta 2 |
