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