Anti-Anxiety and Sedative hypnotics

Question 1

Benzodiazepines - Structure

Answer 1

Basic strxr: contains a benzene ring and a diazepine ring; varying R groups affect lipophilicity and pharmacodynamics
R = H – Xanax (Alprazolam)
R = Cl – Halcion (Triazolam)
R = F – Versed (Midazolam)

Question 2

Benzodiazepines - Mechanism of Action

Answer 2

enhance the ability of GABA (inhibitory NT) to open GABA(A) channels
Primary target = CNS
- sedation, hypnosis, anesthesia, anticonvulsant, muscle relaxant, decreases BP and CO, respiratory depression

Question 3

Lorazepam

Answer 3

Indicated for patients with LIVER DISEASE

Question 4

Alprazolam (Xanax)

Answer 4

Most commonly prescribed antidepressant/antianxiety med today

Question 5

Diazepam (Valium)

Answer 5

Anesthetic adjunct

Skeletal muscle relxant

Question 6

Oxazepam (Serax)

Answer 6

Pts. with LIVER DISEASE

Question 7

Flumazenil (Romazicon)

Answer 7

Benzodiazepine Receptor Antagonist
given through IV
* Speeds up recovery from sedation and anesthesia
- used for BD overdose

Question 8

Zolpidem (Ambien)
Zaleplon (Sonata)
Eszopiclone (Lunesta)

Answer 8

Novel BD receptor agonists
- highly selective for BZ1 receptor
Rx for sleep problems (hypnotic)
Can be prescribed to pregnant women bc no CNS depression

Question 9

Barbiturates

Answer 9

faciliate GABA action like BD
GABA-mimetic at high doses (can open channels on their own)
- inhibit glutamate receptors
** more pronounced CNS depressant than BD

Question 10

Thiopental

Methohexital

Answer 10

Barbiturates
used for induction of anesthesia
used to treat generalized tonic-clonic seizures

Question 11

Barbiturate Therapeutic Uses

Answer 11

sedative/hypnotic
tx of alcohol withdrawal
adjunct to induce anesthesia
anti-convulsant

Question 12

Chloral Hydrate

Answer 12

Used as oral sedative for children in dentistry
metabolized by liver (to active form) and excreted by the kidneys
T(1/2) = 4 to 12 hours
Narrow therapeutic index > dosage should be calculated by WEIGHT

Question 13

Buspirone

Answer 13

Serotonin receptor partial agonist
Mixed (ant)agonist dopamine receptor
Does not bind GABA therefore no: CNS depression, no additive effects, no abrupt withdrawal, no dependence
Takes 1-3 weeks for anti-anxiety effects to materialize

Question 14

Hydroxyzine
Promethazine
Diphenhydramine

Answer 14

H1 histamine receptor antagonist
Enhances sedation and drowsiness, reduces nausea and vomiting
Low toxicity (bc OTC)
Side effects: dry mouth, drowsiness