Adrenergic Miscellaneous

Question 1

Tyramine

Answer 1

Class: Indirect acting agonist

Mech: Increases cytoplasmic NE release

Ther: N/A

Tox: N/A

Misc: Tyramine is involved with an exchange transporter: tyramine goes in and NE comes out

Question 2

Cocaine

Answer 2

Class: N/A

Mech: Prevents NE reuptake

Thera: Local anesthetic, vasoconstrictor

Tox: Insomnia, anxiety, arrhythmias

Question 3

Guanethidine

Answer 3

Class: Nerve ending blocker

Mech: False NT (vesicle becomes full of this rather than NE)

Thera: Antihypertensive

Tox: Many and serious

Misc: Not used in US.
Does not cross BBB.

Question 4

Reserpine

Answer 4

Class: Nerve ending blocker

Mech: Release of empty vesicles (NE is not taken into vesicles bc this binds uptake transporter and inhibits it)

Thera: Older antihypertensive

Tox: Many and serious (depression and suicide are major ones)

Misc: Cheap, used abroad but not in US

Question 5

Alpha-methyl-tyrosine

Answer 5

Class: Nerve ending blocker

Mech: Inhibits tyrosine hydroxylase (decreasing NE synthesis)

Thera: Pheochromocytoma

Tox: Many and serious

Question 6

Ephedrine

Answer 6

Class: Mixed, direct (B2)/ indirect agonist

Mech: N/A

Therapeutics: Nasal congestion, anorexic