Adrenergic Receptors as Therapeutic Targets: Neurologic Implications

Question 1

Direct acting sympathomimetics

Answer 1

Analogs of EPI or NE that are agonists at alpha or beta adrenergic recpeotra

Question 2

Indirect acting sympathomimetics

Answer 2

Mimic activation of symp nervous systme by mech other than direct receptor activation

Question 3

Cocaine, amphetamine, tricyclic antidepressant mechs

Answer 3

Block NET and other monoamine transports

amphetamines also release NE from presynaptic nerve terminals

Question 4

TCA mechanism

Answer 4

Inhibit NET leading to an increase of NE in the synaptic cleft

Results in improvmenet of depressive symtosm

Question 5

Tricyclic AD facts and one example

Answer 5

Use has decreased signifcantly
Amitriptyline

Can also be used to tx neuropathic pain

Question 6

Side effects of TCA

Answer 6

Sedation (antihistamine)
Dry mouth (anticholinergic)
Orthostatic hypotension (alpha 1 blockers)
Arrythmias (block cardaic Na channels)

Question 7

Dose response curve of TCAs

Answer 7

Small increases in dose can increase likelihood of toxicity

Question 8

Cocaine mech

Answer 8

Inhibits NET

Also blocks the DAT SERT

Actions at DAT responsible for eurphoria

Question 9

Cocaine therapeutic use

Answer 9

Limited use a local anesthetic and vasoconstricotr in specialized surgical procedures

Anesthetic action due to ability to block Na channels, NOT because of trnasporter effects

Question 10

Cocaine toxicity- CNS

Answer 10

Anorexia 
Euphoria
Agitation 
Hyperthermia
Seizures

Question 11

Cocaine VC

Answer 11

Hypertension
Coronary vasoconstriction
Arrythmias
MI

Question 12

Pharmacodyanmis of cocaine

Answer 12

More rapid into circulation means faster onset of action and greater and faster effects

Question 13

Amphetamine mech

Answer 13

Block NET and disruption of vesicular stoarge of NE resulting in efflux of NET throuh the NET

ALso blocks the DAT SET

Blockade of DAT responsible for euphoria and addictive properties

Question 14

Therapeutic uses of amphetamines

Answer 14

ADHD
Narcolepsy
Appetite suppression

Question 15

Amph in ADHD

Answer 15

Stimulation of post-synaptic alpha 2A-ARs in the prefrontal cortex

All approved ADHD meds increase catecholamine transmission in the prefrontal cortex

Question 16

If overtreated with amphetamine

Answer 16

Misguided attention and mental inflexibility

Question 17

Amph contraindictaions

Answer 17

Hypertension
BPH
Ischemic heart dz
Glaucoma 
Hyperthyroidism

Question 18

Amph drug interactions

Answer 18

Tricyclic antidepressatns
MAO-inhibitors
OTC cold meds

Question 19

Toxicity of ampth

Answer 19

Similar to cocaine but longer duration

Ventriclular arrythmias, hyperthermia and tension, MI

Question 20

Clonidine

Answer 20

Stimulates alpha 2 receptors in preforontal cortex to improve ADHD

Stimulates alpha 2 receptors in NTS to decrease sympathetic outflow decreasing peripheral vascular esistance

Question 21

CLinical uses of clonidine

Answer 21

Hypertension
ADHD
Withdrawl
Neuropathic pain
Tourette's

Question 22

Side effects of clonidine

Answer 22

Drowsiness or xerostomia

Question 23

MAO inhibitors

Answer 23

Inhibit breakdown of NE

Question 24

MAO-A vs. B

Answer 24

A - breaks down NE, SERT, and DA

MAO-B breaks down DA…at high contrations in synapses in striatum

Question 25

Selegilin

Answer 25

Selective MAO-B inhibitor used in parkinsons dz

Question 26

Tyramine

Answer 26

In certain foods and wine

If used with MAOIs then can cause a hypertensive crisis