Sedative - Hypnotic drugs

Question 0

what are the major inhibitory neurotransmitters?

Answer 0

GABA - CNS

glycine - spinal cord (ventral horn)

*monocarboxylic acids

Question 1

difference between sedatives and hypnotics

Answer 1

Sedatives - reduce anxiety; calming effect

Hypnotics - produce drowsiness; onset and maintenance of sleep
more pronounced CNS depression

Question 2

what are the major excitatory neurotransmitters?

Answer 2

glutamate and aspartate

• dicarboxylic acids

Question 3

mechanism of action of BENZODIAZEPINES

Answer 3

binds to GABA-A receptor subunit and increases FREQUENCY of Cl channel opening

membrane hyperpolarization

Question 4

what are the prototype drugs for short/intermediate/long acting BDZ?

Answer 4

short-acting – midazolam
intermediate acting –lorazepam
long acting – diazepam

Question 5

what are the uses of midazolam?

Answer 5

acute anxiety, anesthesia induction, preop sedation

Question 6

what BDZs can be used as tranquilizers and for seizure disorders?

Answer 6

intermediate acting - clonazepam

long acting - diazepam

Question 7

what abnormal sleep pattern results from use if BDZs?

Answer 7

decreased REM sleep

Question 8

Whhuch drugs are considered date-rape drugs?

Answer 8

1. alcohol (most common)
2. flunitrazepam (rohypnol)
3. gamma hydroxybutyrate

Question 9

BDZ with the longest half life

Answer 9

CHLORDIAZEPOXIDE

• 36-200hours half life
• longest spelling!!!

Question 10

Side effects of benzodiazepines in general

Answer 10

ANTEROGRADE AMNESIA, decreased psychomotor skills, unwanted daytime sedation, respiratory depression, tolerance, dependence liability

midazolam exhibits TOLERANCE

Question 11

Antidote for BDZ overdose

Answer 11

FLUMAZENIL
- a BDZ antagonist

bdz overdose - toxic dose is 1000x the therapeutic dose
ssx: slurred speech, ataxia, altered sensorium, respi depression

Question 12

what is the noted side effect of flumazenil?

Answer 12

It can precipitate BDZ withdrawal syndrome

Question 13

what can happen if Flumazenil was given to a patient who took both TCA and BDZ?

Answer 13

seizures and arrhythmias!!

Question 14

Mechanism of action of BARBITURATES

Answer 14

binds to GABA-A receptor sites
increases DURATION of Cl channel opening

read as BarbiDURATes (duration); FRENzodiazepines (frequency)

Question 15

what are the prototyoe drugs for barbiturates?

ultra-short/ short-intermediate/ long acting

Answer 15

ultrashort - thiopental (read as TAYOpental = TAYO agad!)
short - pentobarbital
long - phenobarbital

Question 16

what is a unique side effect of barbiturates?

Answer 16

Acute intermittent porphyria

barbiturates increase production of d-ALA dehydratase

• • accumulation of porphobilinogens
• • urine darkens in exposure to light and air

Question 17

what is the enzyme deficient in acute intermittent porphyria?

Answer 17

HMB synthase

Question 18

what are unique uses of PHENOBARBITAL?

Answer 18

for seizure disorders, status epilepticus, hyperbilirubinemia (gilbert’s syndrome)

Question 19

what Barbs drug is used for Gilberts syndrome?

Answer 19

phenobarbital

gilberts syndrome - disease that reduces the rate of bilirubin conjugation producing UNconjugated hyperbilirubinemia

Question 20

barbiturates are potent ___________ of CYP450 enzymes

Answer 20

potent inducer

Question 21

what is the only indication of use for Zolpidem?

Answer 21

Insomnia

zolpidem is an imidazopyridine

zolpidem/ zaleplon – zzzzzzZzzzzzzz Zzzleeep

Question 22

what drug is used for Generalized anxiety disorder?

Answer 22

Buspirone

• a partial agonist at 5-HT1a receptors and poss D2 receptors
• not used in acute anxiety!!