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Flashcards in Adrenergic antagonists : Adrenergic neuron blockers Deck (17)
1

sympatholytics are:

adrenergic antagonist

2

define adrenergic neuron blockers

drugs that disrupt the synthesis, storage, or release of norepinephrine

3

Guanethidine
Guanadrel
Act by:

Inhibit norepinephrine release and deplete neuronal amine stores

4

Guanethidine
Guanadrel are
Orally active compounds used to treat

severe hypertension (limited use)

5

which neuron blocker, guanethidine or Guanadrel, is a polar compound -- does not enter the CNS

Guanethidine

6

Guanethidine and Guanadrel are short/long acting

long acting

7

How do guanethidine and guanadrel get into adrenergic nerves?

Via NE transporter NET

8

What drugs may compete with guanethidine and guanadrel? (also inhibit NET)

tricyclic antidepressants

9

Guanethidine and guanadrel have numerous side effects such as:

orthostatic hypotension,
interferes with sexual function,
diarrhea, muscle weakness, edema

10

This drug Diffuses into adrenergic nerves – transport does not require the NET

Reserpine

11

How does Reserpine work?

Depletes nerves of neurotransmitters – by inhibiting the vesicular monoamine transporter 2 (VMAT2) responsible for sequestering dopamine into storage vesicles

12

vesicular monoamine transporter 2 (VMAT2) responsible for

sequestering dopamine into storage vesicles

13

Reserpine is orally active and used to tx:

essential hypertension in combination with other drugs -- rarely used

14

Reserpine enters this system and causes side effects
d. Long-acting, slow onset
e. Side effects -- Sedation, diarrhea, orthostatic hypotension, increased gastric acid secretion

Enters CNS and has CNS side effects. May cause depression, suicide (suicidal tendencies), and sedation

15

This adrenergic neuron blocker can cause depression, suicide (suicidal tendencies), and sedation

Reserpine

16

Reserpine is slow acting/long acting with a slow/fast onset

long acting
slow onset

17

Side effects of Reserpine

Sedation, diarrhea, orthostatic hypotension, increased gastric acid secretion