Sedatives- Pharm

Question 1

Benzodiazepines

• metabolism (phase I and II)
• ex and which have active metabolites

Answer 1

Benzodiazepines

• phase 1 rxn (cyp3a4) and phase 2 rxn (glucoronidation)
• a-lam, c-oxide (active metabolite), c-pam, c-pate (active metabolite), d-pam (active metabolite), f-pam (active metabolite), l-pam, m-lam, o-pam, t-lam

Question 2

Barbiturates

-drug name suffix

Answer 2

Barbiturates

“Barbitals”

Question 3

GABAa-R

• explain the molecular pharm of it
• explain MOA of benzodiazepines and barbiturates

Answer 3

GABAa-R

• ligand gated chloride channel that when activated reduces the # of AP and is inhibitory in CNS
• benzodiazepines- inc effects of GABA
• barbiturates- inc duration of GABA-chloride channel opening

Question 4

Flumazenil

• MOA
• what drugs does it block
• what is it used for
• what can its use precipitate

Answer 4

Flumazenil

• MOA- competitive antagonist to benzodiazepine binding site on GABA thus blocking actions of benzodiazepines, zolpidem, zaleplon, and eszopiclone
• used to reverse CNS depressant effects of benzodiazepine OD and shorten recovering following benzodiazepine use as an anesthetics
• can precipitate withdrawal symptoms in pt who have physiological dependence

Question 5

Explain benzodiazepine withdrawal effects

Answer 5

Benzodiazepine withdrawal- sleep disturbances, depression, rebound anxiety, and seizure

Question 6

Explain treatment of sleep problems w/ new agents

• benefits
• when each drug is most appropriate
• what happens w/ abrupt discontinuation
• long term use?

Answer 6

Zolpidem, zaleplon, and eszopiclone

• rapid onset, limited day after psychomotor depression, and few amnestic effects
• zolpidem and zaleplon used for pt w/ trouble GETTING to sleep
• eszopliclone used for pt w/ trouble STAYING asleep
• abrupt discontinuation can cause rebound insomnia
• DO NOT USE LONG-TERM; if insomnia isn’t cured w/in a week its indicative of a psychiatric or medical illness

Question 7

Ramelteon

• MOA
• use
• AE
• caution in what pt

Answer 7

Ramelteon
MOA- MT1 and MT2 melatonin R agonist found in suprachiasmic nuclei
Uses- insomnia w/ difficulty GETTING to sleep
AE- dizzy, somnolence, fatigue, dec T and inc prolactin
Use w/ caution in pt w/ hepatic impairment

Question 8

Buspirone

• uses
• what effects does it not have
• AE
• use w/ caution in who?

Answer 8

Buspirone

• used for gen anxiety disorder
• doesn’t cause sedation, hypnotic, euphoric, anticonvulsant, or m relaxant effects
• AE- inc HR, palpitations, anxious, GI probs, paresthesias, papillary constriction
• caution in pt w/ hepatic impairment

Question 9

Meprobamate

• uses
• AE

Answer 9

Meprobamate

• short term relief of anxiety and relieve anxiety and sedate anxious preop pt
• AE- tolerance, dependence, and abuse

Question 10

Which benzos are fast acting? Which is the fastest?

Which benzos in general have longest T 1/2?

Answer 10

Fast acting- a-lam, c-pate, diazepam (fastest), f-pam

Long t 1/2- benzos w/ active metabolites

Question 11

Which benzo primarily has hypnotic effects (sleep)?

Answer 11

T-lam