Centrally acting alpha-2a adrenergic agonists

Question 1

centrally-acting drugs

Answer 1

Drugs that act on the BP regulatory system in the brain medulla (sympathetic regulation)

Question 2

In Central BP regulatory system, NE acts on…

Answer 2

alpha-2a adrenergic receptors

–agonists inhibit sympathetic NS activation

Question 3

Pharmacological actions

Answer 3

agonists of postsynaptic a2-adrenoreceptors in rostral ventrolateral medulla (RVLM)

decreases sympathetic outflow from RVLM to heart and vessels

decrease in PVR and HR

Question 4

Clonidine

Answer 4

anti-HTN

analgesic for neuropathic pain (b/c releases endogenous opiates)

ADHD

Question 5

When you hear sedation as a side effect, think…

Answer 5

alpha-2a adrenergic receptor agonist or centrally-acting antihypertensive

Question 6

Guanabenz

Answer 6

lowers cholesterol in plasma

Question 7

side effects

Answer 7

sedation (less w/ Guanfacine), fatigue, drowsiness

contact dermatitis w/ patch

clonidine withdrawl–> –> HTN, so withdraw slowly

Question 8

alpha-methyl-DOPA…MOA

Answer 8

converted into alpha-methyl NE
(dopamine–>NE, but w/ methyl group, it is a false transmitter)

a2a agonist in RVLM

Question 9

alpha-methyl-DOPA…Pharmacological effects

Answer 9

decreases sympathetic tone, reduction in BP due to decrease in TPR

Question 10

alpha-methyl-DOPA…Clinical utility

Answer 10

obsolete

pre-eclampsia

Question 11

alpha-methyl-DOPA…side effects

Answer 11

sedation, sleep disturbances, erectile sexual dysfunction

Na/H2O retention

lactation due to increased prolactin secretion

Sometimes positive Coombs