General

Question 1

Five steps of neurotransmission

Answer 1

1) NT synthesis
2) Vesicular Storage
3) Synaptic Release
4) Binding to receptor
5) Termination of transmission

Question 2

Botulinum Toxin

Answer 2

Degrades SNARES of the cholinergic NMJ.

skeletal muscle paralysis due to loss of Ach release

Question 3

amphetamine or ephedrine

Answer 3

Bind indirectly to the receptor

stimulates NT release in a Ca independent manner

can reverse the direction of NT transport, resulting in the release of endogenous NT back out of the extracellular side of the membrane without membrane voltage change or Ca influx

reverses monamine uptake transporters. used in the treatment of narcolepsy and ADHD

Question 4

Monamines

Answer 4

Seratonin, NE, Epi, Histamine, serotonin

Question 5

Rate limiting step of catecholamine production

Answer 5

tyrosine hydroxylase

Question 6

Metyrosine

Answer 6

Binds to tyrosine hydroxylase, can’t be transformed into L-DOPA. Decreases dopamine production

used to treat HTN-reduces NE production

Question 7

Carbidopa

Answer 7

blocks the conversion of L-DOPA to dopamine

Does not cross BBB, so protects peripheral adrenergic neurons from producing too much dopamine and NE

used to reduce cardiovascular side effects of L-DOPA

Also used to treat Parkinson’s disease

Question 8

Dopamine-ß-Hydroxylase

Answer 8

Converts Dopamine to NE

Prevents destruction of NE in cytosol

Question 9

Reserpine

Answer 9

Blocks the vesicular monamine transporter (VMAT) uptake of monamines

Results in depletion of monamines DA, NE, serotonin

Crosses BBB and can block vesicular monamine uptake in the CNS

Question 10

Bretylium

Answer 10

inhibits excitability (AP generation) of the nerve temrinal membrane and Ca dependent fusion of the synaptic vessicle with the plasma membrane. causes reduction of NT release.

Has specific effects on adrenergic neurotransmission. taken up by transport proteins that usually take up NE

used to reduce ventricular arrythmia

influences neuropeptide release

Question 11

catecholamine-O-methyltransferase (COMT)

Answer 11

termination of NE

degredation of catecholamines

Question 12

Monoamine oxidase (MAO)

Answer 12

in cell cytoplasm. oxidizes NE and DA

degrades catecholamines

Question 13

Termination of monamines

Answer 13

mediated mainly by reuptake

Question 14

Cocaine

Answer 14

Inhibits re-uptake of monamines NE, DA, serotonin

anelgesic durign surgery

Question 15

Phenylephrine

Answer 15

activates adrenergic receptors. reistant to degradation by COMT, so has a longr half life.

Question 16

Tyramine

Answer 16

When combines with an MAO inhibitor increases NE.

Normally gets metabolized by MAO in the liver, but when MAO is inhibited tyramine accumulates and gets transported into noradrenergic cells where it competes with NE for transport into synaptic vessicles. This raises levels of NE in the cytoplasm.

This can reverse the NE reuptake transporter, causing increased NE in the synapse and can lead to hypertensive crisis sue to excess vasoconstriction.

Question 17

MAO-A

Answer 17

Specifically breaks down serotonin, NE, DA in the brain

Question 18

MAO-B

Answer 18

degrades tyramine in the gut

Question 19

Naloxone

Answer 19

small lipophillic (nonpeptide) opiod receptor antagonist

crosses the BBB, acts in CNS

used to reverse opiod overdose/ dependency

Question 20

Naltrexone

Answer 20

Nonpeptide opiod receptor blocker in CNS. long duration of action

used in treatment of opiate addiction and alcoholism

Question 21

SSRIs

Answer 21

selective inhibition of serotonin reuptake transporter

used to treat depression/anxiety

Question 22

ACE inhibitors

Answer 22

(ex. lisinopril) inhibit peptide cleavage of angiotensin I to angiotensin II.

used to treat hypertension

Question 23

MAO inhibitors

Answer 23

block cytoplasmic metabolism of monoamines

used to treat depression

Question 24

L-DOPA

Answer 24

precursor of dopamine, stimulates dopamine production

Used in Parkinson’s disease