March 12 Exam - set 2

Question 1

What are the local anesthetic prototypes?

Answer 1

Cocaine
Procaine
Lidocaine

Question 2

How do local anesthetics work?

Answer 2

Block voltage gated Na+ channels

–prevent pain transmission

Question 3

Amide local anesthetics

Answer 3

Bupivacaine
Lidocaine
Prilocaine
Ropivacaine

Question 4

Ester local anesthetics

Answer 4

Benzocaine
Cocaine
Procaine
Tetracaine

Question 5

What are the 5 targets of anti-seizure drugs?

Answer 5

1. VG Na+ channel
2. VG Ca2+ channel
3. K+ channels
4. AMPAR
5. NMDAR

Question 6

VG Na+ channel block in seizures

• -what does it do?
• -what drugs?

Answer 6

drugs slow recovery from inactivation, preventing high frequency spiking

phenytoin, carbamazepine, lamotrigine

Question 7

VG Ca2+ channel block in seizures

• -what does it do?
• -what drugs?

Answer 7

drugs diminish excitability, esp at synapses

Ethosuximide, lamotrigine, gabapentin, pregabalin

Question 8

K+ channels in seizures

• -what does it do?
• -what drugs?

Answer 8

K+ channel openers, prolong refractory period and attenuate high frequency spiking

Retigabine

Question 9

AMPAR block in seizure

• -what does it do?
• -what drugs?

Answer 9

blocking will diminish excitability

phenobarbital, topiramate, lamotrigine

Question 10

NMDAR block in seizures

• -what does it do?
• -what drugs?

Answer 10

block will diminish excitability, potentially inhibit LTP

felbamate

Question 11

GABA transporter in seizures

• -what does it do?
• -what drugs?

Answer 11

blocking transporter will permit GABA to build up, decreasing excitability

tiagabine

Question 12

GABA transaminase in seizure

• -what does it do?
• -what drugs?

Answer 12

Transaminase breaks down GABA, so block will increase levels

vigabatrin

Question 13

GABA-A Receptor in seizures

• -what does it do?
• -what drugs?

Answer 13

Bezos act at allosteric site in receptor, augmenting Cl- current and decreasing excitability

Question 14

Benzodiazepines

Answer 14

Bind to GABA-A receptor and increase frequency of Cl- channel opening
(increase single channel conductance)

Question 15

Barbiturates

Answer 15

Binds to GABA-A receptors and increase duration of Cl- channel opening
(increase single channel conductance)

GABA-mimetic at high doses

Question 16

Inverse agonists at BZD site

Answer 16

Bind to GABA-A receptor in BZD site and make it harder for GABA to open the channel

Question 17

BZD site antagnoist

Answer 17

Antagonize action at BZD site, w/o affecting barbiturate binding

E.x. flumazenil

Question 18

Midazolam

Answer 18

Rapid onset, fast recovery

For acute seizure control, pre-surgery anxiolysis, amnesia, sedation

Question 19

Alaprazolam

Answer 19

Mainly for panic and GAD

Rapid acting, moderate duration

Question 20

Flurazepam

Answer 20

LONG duration

For insomnia

Question 21

Buspirone

Answer 21

5-HT_1A receptor partial agonist

Question 22

Z compounds

Answer 22

Zolpidem
Zaleplon
Eszopiclone

Selective for alpha 1 containing GABA-A; act at BZD site

Question 23

Ramelteon

Answer 23

MT1, MT2 agonist (MT = melatonin)
Melatonin mimetic

Acts in suprachiasmatic nucleus to promote sleep

Question 24

How do benzos and barbs effect sleep?

Answer 24

Increase stage 2
Decrease REM
Decrease stage 3/4

Question 25

How do Z compounds effect sleep?

Answer 25

Increase or maintain stage 2

Decrease or maintain REM