Anti-Anxiety Medications

What is sedation (3)

decreases activity

- moderates excitement

- calms the recipient

what is hypnosis (2)

- drowsiness

- facilitates the onset and maintenance of sleep that resembles natural sleep

Can a drug produce hypnois and sedation?

yes, one drug can cause both

What receptors are involved in excitatory neuronal signaling?

glutamate (NMDA receptor)

What receptors are involved in inhibitory neuronal signaling?

GABA (GABA-R receptor )

What would happen if you blocked NMDA receptors?

increased GABA signaling

What are top 3 most prescribed anti-anxiety drugs in America? (Both generic and brand names)

1. Clonazepam (Klonopin)

2. Alprazolam (Xanax)

3. Lorazepam (Ativan)

Clonazepam brand name

Klonopin)

Alprazolam brnad name

(Xanax)

Lorazepam brand name

(Ativan)

What class of drugs does the suffix "zepam" belong to?

benzodiazepines

What is the receptor for benzodiazepines? Do they enhance or inhibit the receptor

Which ions are involved here? (3)

GABA-R

enhances the GABA receptor

Cl- chloride ion

How does benzodiazepines change the membrane potential of neurons? Is the neuron more or less likely to fire action potential? (1)

they increase chloride influx, which causes membrane hyperpolarization of the neuron
• Makes it less likely for the neuron to fire an action potential

(benzodiazepines makes more chorlide channels causing chcorldie to come into the nueron

this makes the neruorn more negative than the outisde (HPERPOLAeiZATION) making it less lkey to fire an acitotn poteitonaL

What are adverse effects of benzodiazepines? (5)

1. CNS Depression

2. Anterograde Amnesia

3. Respiratory Effects

4. Visual and Dental Effects

5. Thrombophlebitis

In what ways are benzodiazepines "better" (or safer) than barbiturates? (2)

- wider therapeutic range

- addiction and tolerance only occur with high doses and long term use

Can you be addicted to benzodiazepines? and whats the solution

yes, patients should slowly taper off drugs to prevent seizures due to chemical addiction

Can you develop tolerance to benzodiazepines? AND EXPALIN

yes, making it to where you have to take higher doses to achieve the same effects

What is benzodiazepine antagonist and its generic name? When is it not be used? and why

Flumazenil (reverses sedation)

*don't use with xanax > seizures*

What would be the effects of Rifampin (a drug for treating Tuberculosis) consumption on metabolism of benzodiazepines?

Rifampin induces CYP3A4 → increases metabolism of benzos → decreases bioavailability of benzos → less therapeutic effects of benzos

What would be the effects of grapefruit juice on the metabolism of benzodiazepines?

Grapefruit inhibits CYP3A4 → decreases metabolism of benzos → increases bioavailability of benzos → more therapeutic effects but higher risk of toxicity

How did Marilyn Monroe die? (A potential bonus question)

overdose of barbiturates/

What is "respiratory depression"?

Decreased respiratory rate and level of consciousness, cannot properly supply co2 in the body

the mechanism of drug action for barbiturates

^GABA which ^Cl- channel opening time

the mechanism of drug action for benzos

^GABA which ^Cl- channel opening frequency

Be able to recognize "Z" compounds and what are is it (4)

Non-benzodiazepine, benzodiazepine receptor agonists

Zolpidem (Ambien)

Zaleplon (Sonata)

Eszopiclone (Lunesta)

What receptor do Z compounds act on?

- GABA receptors

What are Z compounds mainly prescribed for?

- mainly prescribed for insomnia tx

( dont stufy this yet)Why is it not a good idea to mix benzos or z

compounds with alcohol?

can lead to:

- liver damage

- breathing problems

- feelings of depression

- headaches, dizziness

etc