Tx of anxiety

Question 1

Sedative/Anxiolytic vs hypnotic

Answer 1

Calm down, decreases anxiety.
Produces a calming effect with minimum CNS depression.

Sleep. Drowsy. more pronounced cns depression

Question 2

The only NT only found in the CNS

Answer 2

GABA

All neurons in the CNS contain receptors for GABA

Question 3

Two types of GABA receptors

Answer 3

GABA A and GABA B

A is more important for therapeutic drug targets

Question 4

GABA life cycle

Answer 4

Synthesized in the axon terminal.

Glutamine is taken up from extracellular space. Converted to glutamine. Converted to GABA. Then put in storage vesicles.

Removed from gap by transportation back into axon and repackaged into vesicles or into surrounding astrocytes

Question 5

4 GABA binding sites

Answer 5

GABA, barbiturates, benzos and ethanol.

They all have the same MOA- binding to receptor increases affinity of GABA for it’s receptor.

Question 6

Binding of GABA causes what?

Answer 6

Membrane pore to open and allow influx of Cl ions. Causes hyper polarization and is inhibitory.

Question 7

Lack of GABA receptor activation may cause

Overaction of GABA receptor may cause

Answer 7

Lack: Overactivity of neurons.
Overaction: Sedated individual

Question 8

Sequence of response with increasing binding to GABA receptor

Answer 8

Excitation at first, sedation, sleep, anesthesia, coma, death

Question 9

Benzo actions

Answer 9

Reduce anxiety 
Sedative and hypnotic 
Anterograde amnesia - inability to form new memories after dose.
Anit convulsant 
Muscle relaxant

Question 10

Benzo admin and pharmokinetics

Answer 10

Oral or IV
Enter brain rapidly and acts quick.
Metabolized in liver and converted to another benzo prior to final metabolism. = long half life.

Question 11

Benzo functional durations

Answer 11

Short (3-8 hr)
Intermediate (10-12 hr)
Long (1-3 days)

Question 12

Reverse benzo effects

Answer 12

Flumazenil

Injected IV

Question 13

Benzo tolerance

Answer 13

Reduced effectiveness with long term use due to reduced sensitivity. not due to more rapid elimination.

Chronic use of alcohol or barbiturates may cause a reduced sensitivity. Ask pt how much alcohol they drink! Cross tolerance.

Question 14

Benzo dependence and abuse

Answer 14

Taper to prevent signs of withdrawal

Abuse if used along with other drugs. Uncommon alone.

Question 15

Benzo side effects

Answer 15

Amnesia
Daytime sedation
Disinhibition- $400 at taco bell

Question 16

Are benzos analgesics?

Answer 16

no, they do not reduce the perception of pain. They are often used as an additive agent in anesthesia/analgesia.

Question 17

How are barbiturates different from benzos?

Answer 17

STRONG CNS depression. Causes anesthesia, coma, and death at high doses.
can cause respiratory depression and enzyme induction= chronic admin diminishes actions of many drugs including themselves!!

Question 18

One of few drugs that induces its own liver metabolism

Answer 18

Barbiturates

Question 19

3 durations of actions of barbiturates

Answer 19

Short 30 mins
Medium 6-8 hours
Long 1-2 days

Question 20

Can you reverse barbiturates effect by using an antagonist?

Answer 20

No. Competing molecules are not available.

Question 21

Tolerance of benzos vs barbiturates

Answer 21

Benzos: Reduced sensitivity
Barbs: Reduced sensitivity AND increased metabolism.

Question 22

barb dependence and abuse

Answer 22

Dependence: Abrupt discontinuation leads to signs of withdrawal.

Abuse: At low doses can cause excitation/arousal. Abuse on the rise.

Question 23

Barb side effects

Answer 23

Sedation
addiction- highly addictive unlike benzos
Hypotension with IV use
can be lethal in overdose even in the absence of any other drugs. Due to decreased respiratory activity.

Question 24

Buspirone
What kind of agonist
Used to treat __ and will not induce ___

Answer 24

Serotonin receptor agonist
Used to treat anxiety and will not induce sedation.

Must take chronically. Delayed onset.

Question 25

2 types of anxiety

Answer 25

Adaptive- normal reaction

Maladaptive- Reaction in a way that disrupts normal activities. Panic disorder, social phobias, PTSD

Question 26

Why use benzo-like meds to tx insomnia

Answer 26

Short duration of action. Induces sleep within 20-30 mins and lasts only 6-8 hours.
avoids daytime drowsiness.

Question 27

Why would you use benzos as pre-anesthetic or for outpatient surgery?

Answer 27

Relaxes, induces state of amnesia.

Good for out patient because it can be reversed. Midazolam (Versed)

Question 28

What meds can be used to tx muscle spasms?

Answer 28

Barbs and benzos.

Effect is within spinal cord, not at skeletal NMJ

Question 29

Disulfiram MOA

Answer 29

Prolongs hangover. Leaving acetaldehyde in the blood. 
Flushing
Tachy 
Hyperventilation 
Nausea, HA

Question 30

Naltrexone MOA

Answer 30

Long acting opiate antagonist. Used along with counseling to tx alcohol dependence. No adverse effects like with disulfiram.